IP Library › Granted Patent US 8,058,262
Granted Patent B2
US 8,058,262 · App. 13/020,425 · Granted Nov 15, 2011

Proteasome inhibitors and methods of using the same

Assignee: Cephalon, Inc.
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Quick Facts
Patent No.
US 8,058,262
App. No.
13/020,425
Granted
Nov 15, 2011
Kind
B2
Abstract

The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity.

Claims (2333)

1. A method for treating cancer comprising administering to a mammal having or predisposed to said cancer a therapeutically effective amount of a compound of Formula (I)

or pharmaceutically acceptable salt, stereoisomeric or tautomeric form thereof, wherein:

R 1 is C 1 -C 8 alkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkynyl, or C 3 -C 7 cycloalkyl;

R 2 is —(CH 2 ) a CH 2 NHC(═NR 4 )NH—Y, —(CH 2 ) b CH 2 CONR 5 R 6 , —(CH 2 ) c CH 2 N(R 4 )CONH 2 , —(CH 2 ) d CH(R 7 )NR 9 R 10 , or —(CH 2 ) e CH(R 7 )ZR 8 ;

a, b, and c are each, independently, 0, 1, 2, 3, 4, 5, or 6;

d and e are each, independently, 0, 1, 2, 3, or 4;

R 4 is H or C 1 -C 10 alkyl;

R 5 and R 6 are each, independently, H, C 1 -C 10 alkyl, carbocyclyl, heterocarbocyclyl, or an amino protecting group;

alternatively, R 5 and R 6 together with the N atom to which they are attached form a heterocarbocyclyl group;

R 7 is H or C 1 -C 10 alkyl;

R 8 is H, C 1 -C 10 alkyl, alkyl-S(═O) 2 —, aryl-S(═O) 2 —, H 2 NS(═O) 2 —, —SO 3 H, or a protecting group;

R 9 is H, C 1 -C 10 alkyl, carbocyclyl, or heterocarbocyclyl;

R 10 is H, C 1 -C 10 alkyl, carbocyclyl, heterocarbocyclyl, C 1 -C 10 alkyl-C(═O)—,

C 2 -C 10 alkenyl-C(═O)—, C 2 -C 10 alkynyl-C(═O)—, carbocyclyl-C(═O)—,

heterocarbocyclyl-C(═O)—, carbocyclylalkyl-C(═O)—,

heterocarbocyclylalkyl-C(═O)—, C 1 -C 10 alkyl-S(═O) 2 —, carbocyclyl-S(═O) 2 —,

heterocarbocyclyl-S(═O) 2 —, carbocyclylalkyl-S(═O) 2 —,

heterocarbocyclylalkyl-S(═O) 2 —, C 1 -C 10 alkyl-NHC(═O)—,

carbocyclyl-NHC(═O)—, heterocarbocyclyl-NHC(═O)—,

carbocyclylalkyl-NHC(═O)—, heterocarbocyclylalkyl-NHC(═O)—,

C 1 -C 10 alkyl-OC(═O)—, carbocyclyl-OC(═O)—, heterocarbocyclyl-OC(═O)—,

carbocyclylalkyl-OC(═O)—, heterocarbocyclylalkyl-OC(═O)—,

C 1 -C 10 alkyl-NH—C(═O)—NHS(═O) 2 —, carbocyclyl-NH—C(═O)—NHS(═O) 2 —,

heterocarbocyclyl-NH—C(═O)—NHS(═O) 2 —, C 1 -C 10 alkyl-S(═O) 2 —NH—C(═O)—,

carbocyclyl-S(═O) 2 —NH—C(═O)—, heterocarbocyclyl-S(═O) 2 —NH—C(═O)—, or an amino protecting group; wherein R 10 is optionally substituted with 1, 2 or 3, R 23 ;

alternatively, R 9 and R 10 together with the N atom to which they are attached form a heterocarbocyclyl group optionally substituted with 1, 2 or 3 R 23 ;

Y is H, —CN, —NO 2 , —S(═O) 2 R 11 , or a guanidino protecting group;

R 11 is C 1 -C 6 alkyl, aryl, or NR 12 R 13 ;

R 12 and R 13 are, independently, H, C 1 -C 10 alkyl, carbocyclyl, heterocarbocyclyl, or an amino protecting group;

alternatively, R 12 and R 13 together with the N atom to which they are attached form a heterocarbocyclyl group;

Z is O, S, Se, or Te;

Q is —B(OH) 2 , —B(OR 14 ) 2 , or a cyclic boronic ester wherein said cyclic boronic ester contains from 2 to 20 carbon atoms, and, optionally, a heteroatom which can be N, S, or O;

R 14 is H, C 1 -C 4 alkyl, cycloalkyl, cycloalkylalkyl, aryl, or aralkyl;

X is R A C(═O)—, R A NHC(═O)—, R A S(═O) 2 —, R A C(═O)—, R A SC(═O)—, or R A ;

R A is morpholino, thiomorpholino, piperazinyl, tetrahydrofuranyl, tetrahydrothienyl, piperidinyl, pyrrolidinyl, isoxazolidinyl, isothiazolidinyl, pyrazolidinyl, oxazolidinyl, thiazolidinyl, imidazolidinyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, furyl, thienyl, imidazolyl, thiazolyl, pyrrolyl, oxazolyl, isoxazolyl, pyrazolyl, triazolyl, tetrazolyl, 1,2,4-thiadiazolyl, isothiazolyl, or purinyl, each optionally substituted with 1-5 R 21 ;

R 21 is selected from the group consisting of:

C 1 -C 20 alkyl, C 2 -C 20 alkenyl, C 2 -C 20 alkynyl, —OR 21a , —SR 21a ,

—CN, halo, haloalkyl, —NH 2 , —NH(alkyl), —N(alkyl) 2 , —NHC(═O)O-alkyl,

—NHC(═O)alkyl, —COOH, —C(═O)O-alkyl, —C(═O)alkyl, —C(O)H,

—S(═O)-alkyl, —S(═O) 2 -alkyl, —S(═O)-aryl, —S(═O) 2 -aryl,

carbocyclyl optionally substituted with 1-5 R 22 , and

heterocarbocyclyl optionally substituted with 1-5 R 22 ;

R 21a is H, C 1 -C 20 alkyl, C 2 -C 20 alkenyl, C 2 -C 20 alkynyl, carbocyclyl or heterocarbocyclyl;

R 22 is selected from the group consisting of:

C 1 -C 10 alkyl, C 2 -C 10 alkenyl, C 2 -C 10 alkynyl, phenyl,

halo, haloalkyl, alkoxy, thialkoxy, amino, alkylamino, dialkylamino,

carboxyl, alkyl-OC(═O)—, alkyl-C(═O)—, aryl-OC(═O)—,

alkyl-OC(═O)NH—, aryl-OC(═O)NH—, alkyl-C(═O)NH—, alkyl-C(═O)O—,

(alkyl-O) r -alkyl, HO-(alkyl-O) r -alkyl-, —OH, —SH, —CN, —N 3 , —CNO, —CNS,

alkyl-S(═O)—, alkyl-S(═O) 2 —, H 2 NS(═O)—, and H 2 NS(═O) 2 —;

R 23 is selected from the group consisting of:

C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, F, Cl, Br, I, haloalkyl, —NH 2 ,

—NHR 23a , —N(R 23a ) 2 , —N 3 , —NO 2 , —CN, —CNO, —CNS, —C(═O)OR 23a , —C(═O)R 23a ,

—OC(═O)R 23a , —N(R 23a )C(═O)R 23a , —N(R 23a )C(═O)OR 23a , —C(═O)N(R 23a ) 2 ,

ureido, —OR 23a , —SR 23a , —S(═O)—(C 1 -C 6 alkyl), —S(═O) 2 —(C 1 -C 6 alkyl),

—S(═O)-aryl, —S(═O) 2 -aryl, —S(═O) 2 —N(R 23a ) 2 ;

carbocyclyl optionally substituted with 1-5 R 24 ; and

heterocarbocyclyl optionally substituted with 1-5 R 24 ;

R 23a is H or C 1 -C 6 alkyl;

alternatively, two R 23a may be combined, together with the N atom to which they are attached, to form a 5 to 7 membered heterocyclic group; and

R 24 is selected from the group consisting of:

C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, phenyl,

halo, haloalkyl, alkoxy, thialkoxy, amino, alkylamino, dialkylamino,

carboxyl, alkyl-OC(═O)—, alkyl-C(═O)—, aryl-OC(═O)—,

alkyl-OC(═O)NH—, aryl-OC(═O)NH—, alkyl-C(═O)NH—, alkyl-C(═O)O—,

(alkyl-O) r -alkyl, HO-(alkyl-O) r -alkyl-, —OH, —SH, —CN, —N 3 , —CNO, —CNS,

alkyl-S(═O)—, alkyl-S(═O) 2 —, H 2 NS(═O)—, and H 2 NS(═O) 2 —; and

r is 1, 2, 3, 4, 5, 6, 7, 8, 9, or 10; and

with the proviso that when Q is a 1,1,2,2-tetramethylethanediol boronic ester, and R 1 is cycloalkyl, then R 2 is not —CH 2 CONH 2 .

2. The method of claim 1 wherein R 1 is C 1 -C 4 alkyl.

3. The method of claim 1 wherein R 1 is 2-propyl.

4. The method of claim 1 wherein R 2 is —(CH 2 ) a CH 2 NHC(═NR 4 )NH—Y.

5. The method of claim 4 wherein a is 1, 2, 3, or 4.

6. The method of claim 4 wherein a is 2.

7. The method of claim 1 wherein R 2 is —(CH 2 ) d CH(R 7 )NR 9 R 10 .

8. The method of claim 7 wherein d is 0, 1, or 2.

9. The method of claim 7 wherein d is 0.

10. The method of claim 7 wherein R 9 is H.

11. The method of claim 1 wherein R 2 is —(CH 2 ) e CH(R 7 )ZR 8 .

12. The method of claim 11 wherein Z is O.

13. The method of claim 12 wherein e is 0, 1, or 2.

14. The method of claim 12 wherein e is 0.

15. The method of claim 1 wherein Q is B(OH) 2 or a cyclic boronic ester wherein said cyclic boronic ester contains from 6 to 10 carbon atoms and contains at least one cycloalkyl moiety.

16. The method of claim 15 wherein Q is pinanediol boronic ester.

17. The method of claim 15 wherein Q is bicyclohexyl-1,1′-diol boronic ester.

18. The method of claim 15 wherein Q is 1,2-dicyclohexyl-ethane-1,2-diol boronic ester.

19. The method of claim 1 wherein X is R A C(═O)—.

20. The method of claim 1 wherein X is R A NHC(═O)—.

21. The method of claim 1 wherein X is R A S(═O) 2 —.

22. The method of claim 1 wherein R 2 is —CH 2 NH—C(═O)OCH 2 (C 6 H 5 ).

23. The method of claim 1 , wherein:

R 10 is H, C 1 -C 10 alkyl, carbocyclyl, heterocarbocyclyl, C 1 -C 10 alkyl-C(═O)—, carbocyclyl-C(═O)—, heterocarbocyclyl-C(═O)—, carbocyclylalkyl-C(═O)—, heterocarbocyclylalkyl-C(═O)—, C 1 -C 10 alkyl-S(═O) 2 —, carbocyclyl-S(═O) 2 —,

heterocarbocyclyl-S(═O) 2 —, carbocyclylalkyl-S(═O) 2 —,

heterocarbocyclylalkyl-S(═O) 2 —, C 1 -C 10 alkyl-NHC(═O)—,

carbocyclyl-NHC(═O)—, heterocarbocyclyl-NHC(═O)—,

carbocyclylalkyl-NHC(═O)—, heterocarbocyclylalkyl-NHC(═O)—,

C 1 -C 10 alkyl-OC(═O)—, carbocyclyl-OC(═O)—, heterocarbocyclyl-OC(═O)—, carbocyclylalkyl-OC(═O)—, heterocarbocyclylalkyl-OC(═O)—, or an amino protecting group; wherein R 10 is optionally substituted with 1, 2, or 3 R 23 ;

alternatively, R 9 and R 10 together with the N atom to which they are attached form a heterocarbocyclyl group;

R A is morpholino, thiomorpholino, piperazinyl, tetrahydrofuranyl, tetrahydrothienyl, piperidinyl, pyrrolidinyl, isoxazolidinyl, isothiazolidinyl, pyrazolidinyl, oxazolidinyl, thiazolidinyl, imidazolidinyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, furyl, thienyl, imidazolyl, thiazolyl, pyrrolyl, oxazolyl, isoxazolyl, pyrazolyl, triazolyl, tetrazolyl, 1,2,4-thiadiazolyl, isothiazolyl, or purinyl, each optionally substituted with 1-2 R 21 ;

R 21 is selected from the group consisting of:

C 1 -C 20 alkyl, C 2 -C 20 alkenyl, C 2 -C 20 alkynyl, C 1 -C 20 alkoxy,

C 1 -C 20 thialkoxy, —OH, —CN, halo, haloalkyl, —NH 2 , —NH(alkyl), —N(alkyl) 2 ,

—NHC(═O)O-alkyl, —NHC(═O)alkyl, —C(═O)O-alkyl, —C(═O)alkyl,

—S(═O)-alkyl, —S(═O) 2 -alkyl, —S(═O)-aryl, —S(═O) 2 -aryl,

carbocyclyl optionally substituted with 1-5 R 22 ; and

heterocarbocyclyl optionally substituted with 1-5 R 22 ;

R 23 is selected from the group consisting of:

C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, F, Cl, Br, I, haloalkyl, —NH 2 ,

—NHR 23a , —N(R 23a ) 2 , —N 3 , —NO 2 , —CN, —CNO, —CNS, —C(═O)OR 23a , —C(═O)R 23a ,

—OC(═O)R 23a , —N(R 23a )C(═O)R 23a , —C(═O)N(R 23a ) 2 , ureido, —OR 23a , —SR 23a ,

—S(═O) 2 —(C 1 -C 6 alkyl), —S(═O) 2 -aryl, and —S(═O) 2 —N(R 23a ) 2 ; and

r is 2, 3, 4, 5, 6, 7, 8, 9, or 10.

24. The method of claim 23 wherein R 1 is 2-propyl.

25. The method of claim 23 wherein Q is —B(OH) 2 .

26. The method of claim 23 wherein Q is pinanediol boronic ester.

27. The method of claim 23 wherein X is R A C(═O)—.

28. The method of claim 23 wherein R 2 is —CH 2 NH—C(═O)OCH 2 (C 6 H 5 ).

29. The method of claim 1 , wherein:

R 1 is C 1 -C 8 alkyl;

R 2 is —(CH 2 ) a CH 2 NHC(═NH)NH—Y, —(CH 2 ) c CH 2 NHCONH 2 , —(CH 2 ) d CH(R 7 )NR 9 R 10 , or —(CH 2 ) e CH(R 7 )ZR 8 ;

a is 1, 2, 3, 4, or 5;

c is 1, 2, 3, 4, or 5;

d is 0, 1, or 2;

e is 0, 1, or 2;

R 7 is H or methyl;

R 10 is H, C 1 -C 10 alkyl, carbocyclyl, heterocarbocyclyl, C 1 -C 10 alkyl-C(═O)—,

carbocyclyl-C(═O)—, heterocarbocyclyl-C(═O)—, carbocyclylalkyl-C(═O)—,

heterocarbocyclylalkyl-C(═O)—, C 1 -C 10 alkyl-S(═O) 2 —, carbocyclyl-S(═O) 2 —,

heterocarbocyclyl-S(═O) 2 —, carbocyclylalkyl-S(═O) 2 —,

heterocarbocyclylalkyl-S(═O) 2 —, alkyl-NHC(═O)—,

carbocyclyl-NHC(═O)—, heterocarbocyclyl-NHC(═O)—,

carbocyclylalkyl-NHC(═O)—, heterocarbocyclylalkyl-NHC(═O)—,

C 1 -C 10 alkyl-OC(═O)—, carbocyclyl-OC(═O)—, heterocarbocyclyl-OC(═O)—,

carbocyclylalkyl-OC(═O)—, heterocarbocyclylalkyl-OC(═O)—, or an amino protecting group; wherein R 10 is optionally substituted with 1, 2 or 3 R 23 ;

alternatively, R 9 and R 10 together with the N atom to which they are attached form a heterocarbocyclyl group;

Z is O or S;

Q is —B(OH) 2 , —B(OR 14 ) 2 , or a cyclic boronic ester wherein said cyclic boronic ester contains from 6 to 20 carbon atoms and contains at least one cycloalkyl moiety;

R 14 is H, C 1 -C 4 alkyl, or cycloalkyl;

R A is

morpholino, thiomorpholino, piperazinyl, tetrahydrofuranyl, tetrahydrothienyl, piperidinyl, pyrrolidinyl, isoxazolidinyl, isothiazolidinyl, pyrazolidinyl, oxazolidinyl, thiazolidinyl, imidazolidinyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, furyl, thienyl, imidazolyl, thiazolyl, pyrrolyl, oxazolyl, isoxazolyl, pyrazolyl, triazolyl, tetrazolyl, 1,2,4-thiadiazolyl, isothiazolyl, or purinyl, each optionally substituted with 1-2 R 21 ;

R 21 is selected from the group consisting of:

C 1 -C 20 alkyl, C 2 -C 20 alkenyl, C 2 -C 20 alkynyl, C 1 -C 20 alkoxy,

C 1 -C 20 thialkoxy, —OH, —CN, halo, haloalkyl, —NH 2 , —NH(alkyl), —N(alkyl) 2 ,

—NHC(═O)O-alkyl, —NHC(═O)alkyl, —C(═O)O-alkyl, —C(═O)alkyl,

—S(═O)-alkyl, —S(═O) 2 -alkyl, —S(═O)-aryl, —S(═O) 2 -aryl,

carbocyclyl optionally substituted with 1-5 R 22 , and

heterocarbocyclyl optionally substituted with 1-5 R 22 ;

R 23 is selected from the group consisting of:

C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, F, Cl, Br, I, haloalkyl, —NH 2 ,

—NHR 23a , —N(R 23a ) 2 , —N 3 , —NO 2 , —CN, —CNO, —CNS, —C(═O)OR 23a , —C(═O)R 23a ,

—OC(═O)R 23a , —N(R 23a )C(═O)R 23a , —C(═O)N(R 23a ) 2 , ureido, —OR 23a , —SR 23a ,

—S(═O) 2 —(C 1 -C 6 alkyl), —S(═O) 2 -aryl, and —S(═O) 2 —N(R 23a ) 2 ;

r is 2, 3, 4, 5, 6, 7, 8, 9, or 10.

30. The method of claim 1 , wherein:

R 1 is C 1 -C 4 alkyl;

R 2 is —(CH 2 ) a CH 2 NHC(═NH)NH—Y, —(CH 2 ) c CH 2 NHCONH 2 , or —(CH 2 ) d CH(R 7 )NR 9 R 10 ;

a is 1, 2, or 3;

c is 1, 2, or 3;

d is 0 or 1;

R 7 is H or methyl;

R 9 is H or C 1 -C 10 alkyl;

R 10 is H, C 1 -C 10 alkyl, or an amino protecting group;

Y is H, CN, or NO 2 ;

Q is —B(OH) 2 , pinanediol boronic ester, bicyclohexyl-1,1′-diol boronic ester, or 1,2-dicyclohexyl-ethane-1,2-diol boronic ester;

R 21 is selected from the group consisting of:

C 1 -C 20 alkyl, C 2 -C 20 alkenyl, C 2 -C 20 alkynyl, C 1 -C 20 alkoxy,

C 1 -C 20 thialkoxy, —OH—CN, halo, haloalkyl, —NH 2 , —NH(alkyl), —N(alkyl) 2 ,

—NHC(═O)O-alkyl, —NHC(═O)alkyl, —C(═O)O-alkyl, —C(═O)alkyl,

—S(═O)-alkyl, —S(═O) 2 -alkyl, —S(═O)-aryl, —S(═O) 2 -aryl,

carbocyclyl optionally substituted with 1-5 R 22 , and

heterocarbocyclyl optionally substituted with 1-5 R 22 ;

r is 2, 3, 4, or 5.

31. The method of claim 30 wherein R 1 is 2-propyl.

32. The method of claim 30 wherein Q is —B(OH) 2 .

33. The method of claim 30 wherein Q is pinanediol boronic ester.

34. The method of claim 30 wherein X is R A C(═O)—.

35. The method of claim 30 wherein R 2 is —CH 2 NH—C(═O)OCH 2 (C 6 H 5 ).

36. The method of claim 1 , wherein:

R 1 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, or C 3 -C 7 cycloalkyl;

R 2 is —CH 2 NH 2 or —CH 2 NR 9 R 10 ;

R 9 is H or C 1 -C 10 alkyl;

R 10 is H, C 1 -C 10 alkyl, carbocyclyl, heterocarbocyclyl, C 1 -C 10 alkyl-C(═O)—,

carbocyclyl-C(═O)—, heterocarbocyclyl-C(═O)—, carbocyclylalkyl-C(═O)—,

heterocarbocyclylalkyl-C(═O)—, C 1 -C 10 alkyl-S(═O) 2 —, carbocyclyl-S(═O) 2 —,

heterocarbocyclyl-S(═O) 2 —, carbocyclylalkyl-S(═O) 2 —,

heterocarbocyclylalkyl-S(═O) 2 —, C 1 -C 10 alkyl-NHC(═O)—,

carbocyclyl-NHC(═O)—, heterocarbocyclyl-NHC(═O)—,

carbocyclylalkyl-NHC(═O)—, heterocarbocyclylalkyl-NHC(═O)—,

C 1 -C 10 alkyl-OC(═O)—, carbocyclyl-OC(═O)—, heterocarbocyclyl-OC(═O)—,

carbocyclylalkyl-OC(═O)—, heterocarbocyclylalkyl-OC(═O)—, or an amino protecting group; wherein R 10 is optionally substituted with 1, 2 or 3, R 23 ;

alternatively, R 9 and R 10 together with the N atom to which they are attached form a heterocarbocyclyl group;

R 21 is selected from the group consisting of:

C 1 -C 20 alkyl, C 2 -C 20 alkenyl, C 2 -C 20 alkynyl, C 1 -C 20 alkoxy,

C 1 -C 20 thialkoxy, —OH—CN, halo, haloalkyl, —NH 2 , —NH(alkyl), —N(alkyl) 2 ,

—NHC(═O)O-alkyl, —NHC(═O)alkyl, —C(═O)O-alkyl, —C(═O)alkyl,

—S(═O)-alkyl, —S(═O) 2 -alkyl, —S(═O)-aryl, —S(═O) 2 -aryl,

carbocyclyl optionally substituted with 1-5 R 22 , and

heterocarbocyclyl optionally substituted with 1-5 R 22 ;

R 23 is selected from the group consisting of:

C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, F, Cl, Br, I, haloalkyl, —NH 2 ,

—NHR 23a , —N(R 23a ) 2 , —N 3 , —NO 2 , —CN, —CNO, —CNS, —C(═O)OR 23a , —C(═O)R 23a ,

—OC(═O)R 23a , —N(R 23a )C(═O)R 23a , —C(═O)N(R 23a ) 2 , ureido, —OR 23a , —SR 23a ,

—S(═O) 2 —(C 1 -C 6 alkyl), —S(═O) 2 -aryl, and —S(═O) 2 —N(R 23a ) 2 ;

r is 2, 3, 4, or 5.

37. The method of claim 36 wherein R 1 is 2-propyl.

38. The method of claim 36 wherein Q is —B(OH) 2 .

39. The method of claim 36 wherein Q is pinanediol boronic ester.

40. The method of claim 36 wherein X is R A C(═O)—.

41. The method of claim 36 wherein R 2 is —CH 2 NH—C(═O)OCH 2 (C 6 H 5 ).

42. A method for treating cancer comprising administering to a mammal having or predisposed to said cancer a therapeutically effective amount of a compound of Formula (I):

or pharmaceutically acceptable salt, stereoisomeric or tautomeric form thereof, wherein:

R 1 is 2-propyl;

R 2 is —CH 2 CH 2 CH 2 NHC(═NH)NH—NO 2 , —CH 2 CH 2 CH 2 NHC(═O)NH 2 , —CH(CH 3 )OH, —CH 2 CONH 2 , —CH 2 NH 2 , or —CH 2 NR 9 R 10 ;

R 9 is H;

R 10 is methyl-C(═O)—, ethyl-C(═O)—, propyl-C(═O)—, butyl-C(═O)—, pentyl-C(═O)—,

2-(ethoxycarbonyl)ethyl-C(═O)—, 4-methyl-phenyl-C(═O)—, cyclopropyl-C(═O)—,

4-fluoro-phenyl-C(═O)—, 4-H 2 NSO 2 -phenyl-C(═O)—, 4-H 3 CSO 2 -phenyl-C(═O)—,

4-phenyl-phenyl-C(═O)—, 3,4-dimethoxy-benzyl-C(═O)—, 3-pyridinyl-C(═O)—,

2-(hydroxy)-pyridin-3-yl-C(═O)—, 6-(morpholino)-pyridin-3-yl-C(═O)—,

2-(pyridin-4-yl)thiazol-4-yl-C(═O)—, 2-pyrazinyl-C(═O)—,

2,5-dimethyl-pyrazolyl-C(═O)—, N-methyl-2-pyrrolyl-C(═O)—,

2-pyrrolidinyl-C(═O)—, 2-thiophenyl-C(═O)—, 5-isoxazolyl-C(═O)—,

4-(tetrazol-5-yl)phenyl-C(═O)—, (5-tetrazolyl)CH 2 —C(═O)—,

N—H 3 CSO 2 -piperidinyl-C(═O)—, butyl-OC(═O)—, (benzyl)-OC(═O)—,

(9-fluorenylmethyl)-OC(═O)—, pentyl-NHC(═O)—, propyl-NHC(═O)—,

phenyl-NHC(═O)—, 4-methyl-phenyl-NHC(═O)—, methyl-S(═O) 2 —,

4-fluoro-phenyl-S(═O) 2 —, 4-cyano-phenyl-S(═O) 2 —,

1-methyl-imidazol-4-yl-S(═O) 2 —, 2-thiophenyl-S(═O) 2 —,

(4-methyl-phenyl)-NHC(═O)NH—S(═O) 2 —, and

(4-methyl-phenyl)-S(═O) 2 NHC(═O)—,

alternatively, R 9 and R 10 together with the N atom to which they are attached form pyrrolyl or pyrazolyl;

Q is —B(OH) 2 , pinanediol boronic ester, bicyclohexyl-1,1′-diol boronic ester, or 1,2-dicyclohexyl-ethane-1,2-diol boronic ester;

X is R A C(═O)—, R A NHC(═O)—, R A S(═O) 2 —, or R A C(═O)—;

R A is CH 3 —, C 2 H 5 —, C 3 H 7 —, C 4 H 9 —, C 5 H 11 —, C 6 H 13 —, C 7 H 15 —, C 8 H 17 —, C 9 H 19 —, C 10 H 21 —, C 11 H 23 —, C 12 H 25 —, C 13 H 27 —, adamantyl-, bicycloheptanyl-,

cyclopropyl substituted with 0-3 R 21 ;

cyclopentyl substituted with 0-2 R 21 ;

cyclohexyl substituted with 0-2 R 21 ;

pyrazinyl substituted with 0-1 R 2 ;

imidazolyl substituted with 0-1 R 21 ;

tetrahydrofuranyl substituted with 0-1 R 2 ;

oxothiazolidinyl substituted with 0-1 R 21 ;

thiazolyl substituted with 0-2 R 21 ;

furanyl substituted with 0-2 R 21 ;

pyrrolidinyl substituted with 0-1 R 21 ;

piperidinyl substituted with 0-1 R 21 ;

piperazinyl substituted with 0-1 R 21 ; or

pyridinyl substituted with 0-1 R 21 ; and

R 21 is selected from the group consisting of:

methyl-, ethyl-, propyl-, butyl-, pentyl-, hexyl-, heptyl-, ethenyl-, propenyl-, butenyl-, methoxy-, ethoxy-, propoxy-, phenoxy-, fluoro-, chloro-, bromo-, methyl-C(═O)—, butyl-OC(═O)—, butyl-OC(═O)NH—, phenyl-, methoxyphenyl-,

fluorophenyl-, chlorophenyl-, bromophenyl-, pyrrolyl-, and pyridinyl-.

43. A method for treating cancer comprising administering to a mammal having or predisposed to said cancer a therapeutically effective amount of a compound selected from:

Example

No

Compound Name

D.1.1

Naphthalen-2-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.1.2

2-Pyrazinecarboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]-

D.1.3

3-(1,3-Dioxo-1,3-dihydro-isoindol-2-yl)-propanamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.1.4

4-Butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.1.5

3-[(1,1-dimethylethoxy)carbonylamino]benzamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]-

D.1.6

2-(2-methoxyethoxy)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl

D.1.7

2-[2-(2-methoxyethoxy)ethoxy]acetamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl

D.1.8

(E)-3-(Ethoxycarbonyl)acrylamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.1.9

2-Piperidin-1-yl-acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.1.10

4-(1-Methyl-piperidin-4-yl)-butanamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.1.11

2-Acetylamino-acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.2.1

4-(methoxycarbonyl)butanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.2.2

4-(1-Butyl-piperidin-4-yl)-butanamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.2.3

2-Butoxyacetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.1

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.2

Naphthalen-1-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.3

2-Phenylacetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.4

1-Phenylcyclopentanecarboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.5

(2R)-2-Phenylbutanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.6

(2S)-2-Phenylbutanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.7

Dodecanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.8

Octanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.9

Acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.10

4-(1,1-Dimethylethyl)cyclohexanecarboxamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.11

trans-4-Pentylcyclohexanecarboxamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.12

4-Phenylbutanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.13

2-(3-Methoxyphenyl)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.14

4-(1,1-Dimethylethyl)benzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.15

Nonanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.16

(RS)-2-Cyclopentylhexanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.17

Thiophene-2-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.18

2,3-Difluorobenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.19

2-(2-Iodophenyl)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl

D.3.20

Cyclohexanecarboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.21

2-(4-Bromophenyl)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.22

Benzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.23

2-Methylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.24

4-Bromobenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.25

(2S)-2-Phenylpropanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.26

(E)-2-Methyl-3-phenyl-acrylamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.27

2-[(Naphthalen-2-yl)oxy]acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.28

2,2-Dimethylbutanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.29

2-(2-Chlorophenyl)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.30

5-Methylthiophene-2-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.31

cis-3-(2-Methoxyphenyl)acrylamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.32

(2-Methylphenoxy)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.33

2-(2,5-Dimethylphenyl)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.34

trans-3-(2-Bromophenyl)acrylamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.35

4-Isopropylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.36

4-(4-methylphenyl)butanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.37

2-(2-Naphthylsulfanyl)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.38

5-Methylhexanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.39

3-Thiophen-2-yl-propanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.40

2,4-Dimethylthiazole-5-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.41

Furan-3-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.42

(2R)-2-Phenylpropanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.43

2-Cycloheptylacetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.44

1-Methylcyclopropanecarboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.45

1-Methyl-cyclohexanecarboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.46

2-[(1S,2R,5S)-2-isopropyl-5-methylcyclohexyl]oxyacetamide,N-[(1S)-1-

[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.47

(E)-2-Butenamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.48

3-Methylbutanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.49

3-Phenylpropanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.50

4-(4-Methoxyphenyl)-butanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.51

Thiophene-3-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.52

2-Thiophen-3-yl-acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl

D.3.53

(E)-Penta-2,4-dienoic acid amide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.54

2-(4-Isopropylphenoxy)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.55

2-(4-Ethylphenoxy)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.56

(E)-2-Methylhex-2-enoic acid amide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.57

3-(3-Methylphenyl)acrylamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.58

2-Adamantan-1-ylacetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.59

(RS)-2-Cyclopent-2-enylacetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl

D.3.60

4-Diethylaminobenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.61

(RS)-2-Methylbutanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.62

3-(4-Methylphenyl)acrylamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.63

Hexa-2,4-dienoic acid amide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.64

4-Pyrrol-1-yl-benzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.65

(E)-3-Thiophen-3-yl-acrylamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.66

Hept-2-enamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.67

2-(3,4-Dimethylphenoxy)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.68

Dec-9-enamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.69

(E)-Undec-2-enoic acid amide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.70

(E)-Dec-3-enoic acid amide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.71

2,2-Dimethyl-3-(2-methylpropenyl)-cyclopropanecarboxamide,N-[(1S)-1-

[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.72

2-Methylcyclohexanecarboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.73

5-Cyclohexylpentanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.74

3-Methoxycyclohexanecarboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.75

(3R)-3,7-Dimethyl-oct-6-enoic acid amide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl

D.3.76

3-[(4-methylbenzyl)sulfanyl]propanamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.77

(3S)-3,7-Dimethyl-oct-6-enoic acid amide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.78

(RS)-4-Ethyloctanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.79

5-Fluoro-2-methoxybenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.80

2-(4-Bromophenoxy)-acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.81

2-(1-Methyl-1H-indol-3-yl)acetamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.82

Hexahydro-2,5-methanopentalene-3a(1H)-carboxamide,N-[(1S)-1-[[[(1R)-

1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.83

Bicyclo[2.2.1]heptane-2-carboximide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.84

(RS)-2-(4-Chlorophenyl)propionamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.85

(2S)-2-methylbutanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.86

(4RS)-1-[(1,1-dimethylethoxy)carbonyl]-piperidine-4-carboxamide,N-[(1S)-

1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-

1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.87

(RS)-4-Methyloctanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.88

2-Fluoro-5-methylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.89

2-(Bicyclo[2.2.1]hept-2-yl)acetamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.90

Cyclopropanecarboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.91

4-Ethoxybenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.92

(E)-3-(4-Bromophenyl)acrylamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.93

(2S)-2-(6-Methoxynaphthalen-2-yl)-propanamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.94

3-Fluoro-4-methoxybenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.95

4-Fluoro-3-methylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.96

Non-2-enoic acid amide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.97

(E)-3-(Naphthalen-2-yl)acrylamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.98

Quinoline-2-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.99

1-(4-Methoxyphenyl)-cyclopropanecarboxamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.101

3-Butenamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.102

Tetradecanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.103

3-(1H-Indol-3-yl)-propanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.104

4-Phenoxybutanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.105

5-Oxo-5-phenyl-pentanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.106

(2RS)-1-((1,1-dimethylethoxy)carbonyl)-piperidine-2-carboxamide,N-[(1S)-

1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-

1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.107

Pyridine-2-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.108

Pyridine-3-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.109

Pyridine-4-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.110

(2S)-1-((1,1-dimethylethoxy)carbonyl)-piperidine-2-carboxamide,N-[(1S)-

1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-

1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.111

(2R)-1-((1,1-dimethylethoxy)carbonyl)-piperidine-2-carboxamide,N-[(1S)-

1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-

1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.112

3,3-Dimethyl-butanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.113

4-[(Phenylamino)carbonyl]butanamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.114

2,2-Dimethylpentanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.115

5-Thiophen-2-yl-pentanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.116

(3RS)-1-((1,1-dimethylethoxy)carbonyl)-piperidine-3-carboxamide,N-[(1S)-

1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-

1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.117

8-Phenyl-octanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl

D.3.118

3-[[(1,1-dimethylethoxy)carbonyl]amino]propanamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.119

Tridecanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.120

Succinamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.121

Pentanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[imino(nitroamino)methyl]amino]butyl]

D.3.122

[[[(9H-fluoren-9-yl)methoxy]carbonyl]amino]butanamide,N-[(1S)-1-

[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.123

2-(Dimethylamino)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.124

5-(4-Fluorophenyl)-pentanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.125

8-Oxo-8-phenyloctanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.126

4-(Thiophen-2-yl)butanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.127

5-Oxo-5-(thiophen-2-yl)pentanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.128

2-(3-Chlorophenyl)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.129

Undecanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.130

4-Heptylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.131

6-Phenylhexanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.132

5-Phenylpentanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.133

10-Hydroxydecanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.134

5-Oxo-5-(4-phenylpiperazin-1-yl)pentanamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.135

2-(1H-Tetrazol-5-yl)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.136

2-(Tetrazol-1-yl)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.137

2-(Pyrimidin-2-ylsulfanyl)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.138

3-Methylsulfanylpropanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.139

3-(Naphthalen-2-ylsulfanyl)-propanamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.140

2-[(Phenylmethyl)sulfanyl]acetamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.141

6-Oxoheptanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.142

4-(4-Methanesulfonylphenyl)-4-oxobutanamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.143

(2S)-1-Acetylpyrrolidine-2-carboxamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.144

3-Hydroxy-2,2-dimethylpropanamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.145

2-Ethylsulfanylacetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.146

3-Ureidopropanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.147

3-Methoxypropanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.148

2-Methylsulfanylacetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.149

3H-Imidazole-4-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.150

7-Oxo-octanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.151

(E)-3-(Imidazol-4-yl)acrylamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.152

(RS)-Tetrahydrofuran-3-carboxamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.153

(E)-3-(2-Methoxyphenyl)acrylamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.154

2-Ethoxyacetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.155

-Furan-2-yl-propanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.156

-(Benzenesulfonyl)propanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.157

-Sulfamoylbutanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.158

(4S)-2-Oxo-1,3-thiazolidine-4-carboxamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.159

(2R)-1-Acetylpyrrolidine-2-carboxamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.160

-[(Acetylamino)methylsulfanyl]-propanamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.161

-(Acetylsulfanyl)hexanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.162

(Thiophene-2-sulfonyl)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.163

-(Acetylamino)butanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.164

(2Z)-3-(Propylaminocarbonyl)-2-propenamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.165

-(Octylsulfonyl)propanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.166

-(Octylsulfanyl)propanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.167

,2-Dimethylhexanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.168

-Hydroxyhexanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.169

-Oxopentanamide,N-[(1S)-1-[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl]4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.170

-Oxohexanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.171

Benzothiazole-6-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.172

-(Octyloxy)propanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.173

-(2-Oxo-pyrrolidin-1-yl)-acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.174

Benzamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.3.175

-[2-(2-Methoxyethoxy)ethoxy]acetamide,N-[(1S,2R)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.3.176

-Phenylbutanamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.3.177

(4-Methylphenoxy)acetamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.3.178

Hexanamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.3.179

-Butylbenzamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.3.180

Naphthalene-2-carboxamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.3.181

Hexanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.182

-(4-Methylbenzenesulfonyl)acetamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]

D.3.183

Heptanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.184

1-(Carbamoyl)undecanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.185

-(Benzenesulfonyl)acetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.4.1

Naphthalene-1-sulfonamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.4.2

Naphthalene-2-sulfonamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.4.3

Decane-1-sulfonamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.4.4

Octanesulfonamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.4.5

Benzenesulfonamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.5.1

(2S)-4-[[imino(nitroamino)methyl]amino]-2-[(2-naphthylmethyl)-amino]-

pentanamide,N-[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-

methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]

D.5.2

(2S)-4-[[imino(nitroamino)methyl]amino]-2-[(1-naphthylmethyl)-amino]-

pentanamide,N-[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-

methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]

D.5.3

(2S)-4-[[imino(nitroamino)methyl]amino]-2-[undecylamino]-pentanamide,

N-[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]

D.5.4

(2S)-4-[[imino(nitroamino)methyl]amino]-2-[(phenylmethyl)amino]-

pentanamide,N-[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-

methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]

D.6.1

N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-

methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]-N′-(2-naphthyl)urea

D.6.2

N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-

methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]-N′-phenyl urea

D.6.3

N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-

methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]-N′-heptyl urea

D.6.4

N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-

methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]-N′-(1-naphthyl) urea

D.6.5

N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-

methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]-N′-undecylurea

D.6.6

N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-

methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-2-

hydroxypropyl]-N′-undecylurea

D.6.7

N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-

methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]-N′-[5-(ethoxycarbonyl)pentyl]urea

D.7.1

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[(2E)-

3-(2-methoxyphenyl)-1-oxoprop-2-enyl]amino]-1-oxopentyl]amino]-3-

methylbutyl]

D.7.2

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((E)-2-

methyl-3-phenylacryl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.3

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-](4-(4-

methylphenyl)butanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.4

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[((2RS)-2-phenylpropanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.5

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-(4-

isopropylphenoxy)acetyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.6

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(5-oxo-

5-phenylpentanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.7

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[[(4RS)-1-[(1,1-dimethylethoxy)carbonyl]piperidine-4-carbonyl]amino]-1-

oxopentyl]amino]-3-methylbutyl]

D.7.8

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(4-

diethylaminobenzoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.9

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((E)-2-

methylhex-2-enoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.10

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(tiophen-3-carbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.11

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(4-

isopropylbenzoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.12

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(5-

methylthiophene-2-carbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.13

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(benzoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.14

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((E)-2-

butenoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.15

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((E)-

penta-2,4-dienoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.16

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(3,3-

dimethyl-butanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.17

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[5-

(2,5-dimethylphenoxy)-2,2-dimethylpentanoyl]amino]-1-oxopentyl]amino]-

3-methylbutyl]

D.7.18

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2,2-

dimethylpentanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.19

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[4-

(thiophen-2-yl)butanoyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.20

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[5-(4-

fluorophenyl)pentanoyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.21

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2,2-

dimethylhexanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.22

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(hex-

2,4-enoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.23

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[3-

(thiophen-2-yl)propenoyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.24

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(5-

cyclohexylpentanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.25

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((3R)-

3,7-dimethyloct-6-enoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.26

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[3-[(4-

methylbenzyl)sulfanyl]propanoyl]amino]-1-oxopentyl]amino]-3-

methylbutyl]

D.7.27

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(4-

pyrrol-1-ylbenzoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.28

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(5-

fluoro-2-methoxybenzoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.29

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((2S)-

2-methylbutanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.30

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(cyclopropanecarbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.31

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(4-

ethoxybenzoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.32

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((E)-3-

(4-bromophenyl)prop-2-enoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.33

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[(2S)-

2-(6-methoxynaphthalen-2-yl)-propanoyl]amino]-1-oxopentyl]amino]-3-

methylbutyl]

D.7.34

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[1-(4-

methoxyphenyl)-cyclopropanecarbonyl]amino]-1-oxopentyl]amino]-3-

methylbutyl]

D.7.35

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(3-

fluoro-4-methoxybenzoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.36

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[(E)-3-

(naphthalen-2-yl)prop-2-enoyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.37

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(4-

fluoro-3-methylbenzyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.38

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[[[[[(9H-fluoren-9-yl)methoxy]carbonyl]amino]butanoyl]amino]-1-

oxopentyl]amino]-3-methylbutyl]

D.7.39

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(4-

bromobenzoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.40

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(3-

butenoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.41

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(undecanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.42

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[4-

(acetylamino)butanoyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.43

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(6-

phenylhexanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]-

D.7.44

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(5-

phenylpentanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]-

D.7.45

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(3-

methoxypropanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]-

D.7.46

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2,2-

dimethyl-3-(2-methylpropenyl)-cyclopropanecarbonyl]amino]-1-

oxopentyl]amino]-3-methylbutyl]-

D.7.47

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(3-

methoxycyclohexanecarbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]-

D.7.48

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[3-

(1H-indol-3-yl)-propanoyl]amino]-1-oxopentyl]amino]-3-methylbutyl]-

D.7.49

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((RS)-

2-cyclopent-2-enyl-acetyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.50

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(5-

thiophen-2-yl-pentanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.51

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(6-oxo-

heptanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.52

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(7-oxo-

octanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.53

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(hexanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.54

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(heptanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.55

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(3-

octyloxy-propanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.56

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(benzothiazol-6-carbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.57

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(undec-2-enoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.58

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(9-

decenoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.7.59

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(tetradecanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

D.8

Decanamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]-

D.8.1

(2S)-2-[(Benzyloxycarbonyl)amino]-4-methylpentanamide,N-[(1S,2R)-1-

[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-2-hydroxypropyl]-

D.8.2

10-(1,3-dioxo-1,3-dihydro-isoindol-2-yl)-decanoic-amide-N-[(1S),(2R)-2-

hydroxy,1-[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-

methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]aminocarbonyl]-

propyl]-

D.9

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[(4-methylbenzoyl)amino]ethyl]-

D.10

2-S-decanoylamino-3-(hexanoylamino)-propionamide,N-[(1S)-1-[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]

D.11

2-S-decanoylamino-3-(4-fluorosulfonylamino)propionamide,N-[(1S)-1-

[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]

D.12

2-S-decanoylamino-3-(3,4-dimethoxyphenylacetamido)propionamide,N-

[(1S)-1-[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-

1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]

D.13

2-S-decanoylamino-3-(phenylureido)propionamide,N-[(1S)-1-[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]

D.14

2-Aminoacetamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl],

Hydrochloride salt

D.15

3-Aminopropanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl];

hydrochloride salt

D.15.1

(4RS)-piperidine-4-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl],

HCl salt

D.15.2

(RS)-Piperidine-2-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl];

HCl salt

D.15.3

(2S)-Piperidine-2-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl];

HCl salt

D.15.4

(2R)-Piperidine-2-carboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl];

HCl salt

D.16.1

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(acetamido)ethyl]-

D.16.2

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(9-fluorenylmethyloxycarbamoyl)ethyl]-

D.16.3

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(pentyl-ureido)ethyl]-

D.16.4

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(methanesolfonamido)ethyl]-

D.16.5

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[ethoxycarbonyl-succinyl]-amide)ethyl]-

E.1.1

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((2E)-

3-ethoxycarbonyl-1-oxoprop-2-enyl)amino]-1-oxopentyl]amino]-3-

methylbutyl]

E.1.2

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

pyrazinecarbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.1.3

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(4-

butylbenzoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.1.4

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

naphthoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.1.5

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(3-

(1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)-1-oxopropylamino]-1-

oxopentyl]amino]-3-methylbutyl]

E.1.6

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-(2-

methoxyethoxy)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl],HCl salt

E.1.7

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

butoxyacetyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.1.8

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-[2-

(2-methoxyethoxy)ethoxy]acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.1.9

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-

(acetylamino)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl],HCl salt

E.1.10

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[4-

(methoxycarbonyl)butanoyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.1.11

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

(naphthalen-2-yloxy)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.1.12

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(3-

thiophen-2-yl-propanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.1.13

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[2-(2-

chlorophenyl)acetyl]amino]-3-methylbutyl]HCl salt

E.1.14

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(1-oxo-

4-(1-butylpiperidin-4-yl)butyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.1.15

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(1-

octanesulfonyl)amino]-1-oxopentyl]amino]-3-methylbutyl],HCl salt

E.1.16

Boronic acid,[(1R)-1-[[(2S)-3-[(4-methylbenzoyl)amino]-2-

[(decanoylamino)]-1-oxopropyl]amino]-3-methylbutyl]

E.1.17

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(decanoyl)amino]-1-

oxobutyl]amino]-3-methylbutyl]

E.1.18

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[[10-(1,3-dioxo-1,3-dihydro-

isoindol-2-yl)-decanoyl]amino]-1-oxobutyl]amino]-3-methylbutyl]

E.2.1

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(1-

oxodecyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.2

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(octanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.3

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(1-

phenylcyclopentanecarbnyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.4

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((2R)-

2-phenylbutanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.5

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[4-

(1,1-Dimethylethyl)cyclohexanecarbonyl]amino]-1-oxopentyl]amino]-3-

methylbutyl]

E.2.6

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(trans-

4-pentylcyclohexanecarbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.7

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(4-

phenylbutanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.8

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(4-

(1,1-dimethylethyl)benzoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.9

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(nonanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.10

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

thiophenecarbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.11

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2,3-

difluorobenzoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.12

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(dodecanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.13

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-(2-

iodophenyl)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.14

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(cyclohexanecarbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.15

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

methylbenzoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.16

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((2S)-

2-phenylpropanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.17

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2,2-

dimethylbutanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.18

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(quinoline-2-carbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.19

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(non-2-

enoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.20

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

methylcyclohexanecarbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.21

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(hept-

2-enoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.22

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-

(3,4-dimethylphenoxy)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.23

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((RS)-

4-ethyloctanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.24

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(hexahydro-2,5-methanopentalene-3a(1H)-carbonyl)amino]-1-

oxopentyl]amino]-3-methylbutyl]

E.2.25

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(bicyclo[2.2.1]heptane-2-carbonyl)amino]-1-oxypentyl]amino]-3-

methylbutyl]

E.2.26

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(5-

methylhexanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.27

Boronic acid,[(1R)-1-[[(2S)-5-imino(nitroamino)methyl]amino]-2-[(2,4-

dimethylthiazole-5-carbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.28

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(furan-

3-carbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.29

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

cycloheptylacetyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.30

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(1-

methylcyclopropanecarbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.31

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(3-

methylbutanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.32

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(3-

phenylpropanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.33

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[(E)-3-

(3-methylphenyl)acryl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.34

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

adamantan-1-ylacetyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.35

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((RS)-

2-methylbutanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.36

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

phenylacetyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.37

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-(4-

methoxyphenyl)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.38

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-(4-

bromophenyl)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.39

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((RS)-

4-methyloctanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.40

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

fluoro-5-methylbenzoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.41

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-

(bicyclo[2.2.1]hept-2-yl)acteyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.42

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(4-

phenoxybutanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.43

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

pyridinecarbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.44

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(3-

pyridinecarbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.45

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(tridecanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.46

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(8-

phenyloctanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.47

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[4-(4-

methanesulfonylphenyl)-4-oxobutanoyl]amino]-1-oxopentyl]amino]-3-

methylbutyl]

E.2.48

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[3-

(naphthalen-2-ylsulfanyl)-propanoyl]amino]-1-oxopentyl]amino]-3-

methylbutyl]

E.2.49

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-

[(phenylmethyl)sulfanyl]acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.50

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(3-

Methylsulfanylpropanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.51

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[((2S)-

1-acetylpyrrolidine-2-carbonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.52

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[trans-

3-(2-bromophenyl)acryl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.53

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-

(tetrazol-1-yl)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.54

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-

(pyrimidin-2-ylsulfanyl)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.55

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-(4-

ethylphenoxy)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.56

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-

(2,5-dimethylphenyl)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.57

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(8-oxo-

8-phenyloctanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.58

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-(2-

naphthylsulfanyl)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.59

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[(RS)-

2-cyclopentylhexanoyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.60

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[3-(4-

methylphenyl)acryl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.61

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[4-(4-

methoxyphenyl)-butanoyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.62

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

thiophen-3-yl-acetyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.63

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-

(dimethylamino)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.64

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[5-oxo-

5-(thiophen-3-yl)pentanoyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.65

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(acetyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.66

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

ethylsulfanylacetyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.67

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(10-

hydroxydecanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.68

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(2-

methylsulfanylacetyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.69

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[[(thiophene-2-sulfonyl)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.70

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[3-

(benzenesulfonyl)propanoyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.71

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[(RS)-

tetrahydrofuran-3-carbonyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.72

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(naphthalene-1-sulfonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]-

E.2.73

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(naphthalene-2-sulfonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]-

E.2.74

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-

[(benzenesulfonyl)amino]-1-oxopentyl]amino]-3-methylbutyl]-

F.1

Decanamide,N-[(1S)-1-[[[(1R)-1-[(4R,5R)-4,5-dicyclohexyl-

[1,3,2]dioxaborolan-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]-

F.2

4-Phenylbutanamide,N-[(1S)-1-[[[(1R)-1-[13,15-dioxa-14-bora-

dispiro[5.0.5.3]-pentadec-14-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]-amino]butyl]-

or a pharmaceutically acceptable salt, free base, or boronic ester thereof.

44. A method for treating cancer comprising administering to a mammal having or predisposed to said cancer a therapeutically effective amount of a compound selected from:

Example

Compound

No

Name

D.2.6

2-[2-(2-methoxyethoxy)acetylamino]acetamide,N-[(1S)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl

D.2.7

Decanamide,N-[1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-

4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]methyl]

D.2.8

2-[2-(2-methoxyethoxy)ethoxy]acetamide,N-[1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]methyl]

D.2.9

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-5-ureidopentyl]-

D.2.10

4-Butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-5-ureidopentyl]-

D.3.190

3-[4-(2-Propyl)phenyl]propanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.191

3-[4-(Ethyl)phenyl]propanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.3.192

6-hydroxyhexanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.4.6

4-Butoxyenzenesulfonamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.4.7

4-Butyl-benzenesulfonamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.4.8

4-Pentyl-benzenesulfonamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-4-[[imino(nitroamino)methyl]amino]butyl]

D.6.8

N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-

methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]-N′-(4-butylphenyl)urea

D.6.9

N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-

methano-1,3,2-benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-4-

[[imino(nitroamino)methyl]amino]butyl]-N′-(4-heptyloxylphenyl)urea

D.8.3

4-(Pyridin-3-yl)benzamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.8.4

2-Pyrazinecarbossamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.8.5

Tridecanamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.8.6

4-Phenylbenzamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.8.7

2,2-Dimethydecanamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.8.8

(4-phenoxy)benzamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.8.9

5-Butyl-2-pyridinecarboxamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.8.10

4-propoxybenzamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.8.11

3-(3-Pyridyl)benzamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.8.12

6-Phenyl-2-pyridinecarboxamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.8.13

3-propoxybenzamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.8.14

1-Bromonaphthalene-2-carboxamide,N-[(1S,2R)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-2-hydroxypropyl]

D.8.15

6-Bromonaphthalene-2-carboxamide,N-[(1S,2R)-1-[[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]-2-hydroxypropyl].

D.8.16

3-Phenylbenzamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl].

D.8.17

4-(2-Fluorophenyl)benzamide,N-[(1S,2R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-

hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-hydroxypropyl].

D.8.18

2-Pyrazinecarboxamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-carbamoylethyl]

D.8.19

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-carbamoylethyl]

D.8.20

4-Butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-carbamoylethyl]

D.16.6

4-Butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[(benzyloxycarbonylamide)ethyl]-

D.16.7

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(1H-pyrazol)ethyl]-

D.16.8

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[(benzyloxycarbonylamide)ethyl]-

D.16.9

4-Phenoxybenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[(benzyloxycarbonylamide)ethyl]-

D.17

4-Butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(aminoethyl)-hydrochloride salt

D.18

2-S-(4-Butylbenzoylamino)-3-(2-pyrazinocarbonylamino)-N-[(1S)-1-[[(1R)-1-

[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-trimethyl-4,6-methano-1,3,2-

benzodioxaborol-2-yl]-3-methylbutyl]amino]carbonyl]

D.19

4-Butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[4-fluoro-benzenesulfonammide]ethyl]-

D.20

4-Butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-[(2,5-dimethyl-2H-

pyrazole)carbonylamino]ethyl]-

D.21

4-Butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(4-methylphenyluriedosulfonylamino)ethyl]-

D.22

4-Phenoxybenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(3-phenyl-ureido)ethyl]-

D.23

4-Butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(4-methylphenylsulfonylureido)ethyl]-

D.24.1

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[4-fluoro-benzenesulfonammide]ethyl]-

D.24.2

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[(4-sulfonamidophenyl)carbonylamido]ethyl]-

D.24.3

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(acetamido)ethyl]-

D.24.4

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(methanesulfonamido)ethyl]-

D.24.5

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(propylureido)ethyl]-

D.24.6

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-[(4-methylphenyl)carbonylamino]ethyl]-

D.24.7

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-[(1,1-dimethylethoxycarbonyl)amino]ethyl]-

D.24.8

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[(thien-2-ylcarbonyl)amino]ethyl]-

D.24.9

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[(thien-2-ylcarbonyl)amino]ethyl]-

D.24.10

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(hexanonylamino)ethyl]-

D.24.11

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano,1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(cyclopropancarbonylamino)ethyl]-

D.24.12

4-Butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(3-phenyl-ureido)ethyl]-

D.24.13

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[(N-methyl-2-pyrrolylcarbonylamide)ethyl]-

D.24.14

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano,1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-[(3,4-dimethoxyphenyl)acetylamino]ethyl]-

D.24.15

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(nicotinonylamino)ethyl]-

D.24.16

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano,1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-[(4-sulfonylamino)benzoylamino]ethyl]-

D.24.17

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano,1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-[(1H-tertazol-5-yl-acetylamino]ethyl]-

D.24.18

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-[(4-

methysulfonylphenyl)carbonylamino]ethyl]-

D.24.19

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(nicotinonylamino)ethyl]-

D.24.20

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-[(4-(2H-tetrazol-5-

yl)phenyl)carbonylamino]ethyl]-

D.24.21

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-[(1-isoxazol-5-yl)-carbonylamino]ethyl]-

D.24.22

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-[(4-cyanophenyl)sulfonylamino]ethyl]-

D.24.23

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-[(1-methyl-1H-imidazole-4-)

sulfonylamino]ethyl]-

D.24.24

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-[(2-thiophene)sulfonylamino]ethyl]-

D.24.25

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(6-morpholin-4-nicotinoylamino)ethyl]-

D.24.26

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(2-pyridin-4-thiazolecarbonylamino)ethyl]-

D.24.27

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(4-methylphenyluriedosulfonylamino)ethyl]-

D.24.28

4-phenoxybenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[(benzyloxycarbonylamide)ethyl]-

D.24.29

4-phenoxybenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[4-fluoro-benzenesulfonammide]ethyl]-

D.24.30

4-phenoxybenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-[(2,5-dimethyl-2H-pyrazole)

carbonylamino]ethyl]-

D.24.31

4-phenoxybenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-

3a,5,5-trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(4-phenylbenzoylamino)ethyl]-

D.24.32

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(4-phenylbenzoylamino)ethyl]-

D.24.33

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(3-phenylpropynoylamino)ethyl]-

D.24.34

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(2-hydroxy-3-nicotinoylamino)ethyl]-

D.24.35

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(D-piroglutamoylamino)ethyl]-

D.24.36

4-butylbenzamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(1-methanesulfonyl-piperidine-4-

carbonylamino)ethyl]-

D.24.37

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-(3-phenyl-ureido)ethyl]-

D.24.38

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-(acetamido)ethyl]-

D.25.1

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-amino]ethyl]-hydrochloride salt

D.25.2

Decanamide,N-[(1S)-1-[[[(1R)-1-[(3aS,aS,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl-]-3-

methylbutyl]amino]carbonyl]-2-amino]ethyl]-hydrochloride salt

D.26

4-Butylbenzamide,N-[(1R)-1-[[[(1R)-1-[(3aS,4S,6S,7aR)-hexahydro-3a,5,5-

trimethyl-4,6-methano-1,3,2-benzodioxaborol-2-yl]-3-

methylbutyl]amino]carbonyl]-2-[(4-methylbenzoyl)amino]ethyl]-

E.1.23

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(4-phenylbutanoyl)amino]-1-

oxobutyl]amino]-3-methylbutyl]

E.1.24

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(undecylaminocarbonyl)amino]-

1-oxobutyl]amino]-3-methylbutyl]

E.1.25

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(1-Bromo-2-naphthoyl)amino]-

1-oxobutyl]amino]-3-methylbutyl]

E.1.26

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(6-Bromo-2-naphthoyl)amino]-

1-oxobutyl]amino]-3-methylbutyl]

E.1.27

Boronic acid,[(1R)-1-[[(2S)-3-carbamoyl-2-[(decanoyl)amino]-1-

oxopropyl]amino]-3-methylbutyl]

E.1.28

Boronic acid,[(1R)-1-[[(2S)-3-carbamoyl-2-[4-butyl(benzoyl)amino]-1-

oxopropyl]amino]-3-methylbutyl]

E.1.29

Boronic acid,[(1R)-1-[[(2S)-2-[(decanoyl)amino]-1-oxo-5-ureido-

pentyl]amino]-3-methylbutyl]

E.1.30

Boronic acid,[(1R)-1-[[(2S)-2-[(4-butylbenzoyl)amino]-1-oxo-5-ureido-

pentyl]amino]-3-methylbutyl]

E.2.76

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[(RS)-2-

(4-chlorophenyl)propanoyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.77

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[2-(4-

bromophenoxy)acetyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.78

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[3-(4-

ethylphenyl)propanoyl]amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.79

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[3-[4-

(heptyloxy)phenyl]-ureido]-1-oxopentyl]amino]-3-methylbutyl]

E.2.80

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[(5-

oxohexanoyl)amino]-1-oxopentyl]amino]-3-methylbutyl]

E.2.81

Boronic acid,[(1R)-1-[[(2S)-5-[[imino(nitroamino)methyl]amino]-2-[[(2RS)-

1-[(1,1-dimethylethoxy)carbonyl]piperidine-2-carbonyl]amino]-1-

oxopentyl]amino]-3-methylbutyl]

E.3.1

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(2-naphthoyl)amino]-1-

oxobutyl]amino]-3-methylbutyl]

E.3.2

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(p-tolyloxyacetamide]-1-

oxobutyl]amino]-3-methylbutyl]

E.3.3

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(tridecanoyl)amino]-1-

oxobutyl]amino]-3-methylbutyl]

E.3.4

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(naphthalene-2-

sulfonyl)amino]-1-oxobutyl]amino]-3-methylbutyl]

E.3.5

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(4-phenylbenzoyl)amino]-1-

oxobutyl]amino]-3-methylbutyl]

E.3.6

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(2,2dimethyl-decanoyl)amino]-

1-oxobutyl]amino]-3-methylbutyl]

E.3.7

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(4-Phenoxybenzoyl)amino]-1-

oxobutyl]amino]-3-methylbutyl]

E.3.8

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[[4-(1-

propoxy)butylbenzoyl]amino]-1-oxobutyl]amino]-3-methylbutyl]

E.3.9

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(3-pyridin-3-yl-

benzoyl)amino]-1-oxobutyl]amino]-3-methylbutyl],hydrochloride salt

E.3.10

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(3-propoxy-benzoyl)amino]-1-

oxobutyl]amino]-3-methylbutyl]

E.3.11

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(3-phenylbenzoyl)amino]-1-

oxobutyl]amino]-3-methylbutyl]

E.3.12

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(4-(2-

fluorophenyl)benzoyl)amino]-1-oxobutyl]amino]-3-methylbutyl]

E.4

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[[4-(3-pyridyl)benzoyl]amino]-1-

oxobutyl]amino]-3-methylbutyl]

E.4.1

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(2-pyrazinecarbonyl)amino]-1-

oxobutyl]amino]-3-methylbutyl]

E.4.2

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(5-butyl-pyridine-2-

carbonyl)amino]-1-oxobutyl]amino]-3-methylbutyl]

E.4.3

Boronic acid,[(1R)-1-[[(2S,3R)-3-hydroxy-2-[(6-phenyl-pyridine-2-

carbonyl)amino]-1-oxobutyl]amino]-3-methylbutyl]

E.5

Boronic acid,[(1R)-1-[[(2S)-3-(2-pyrazincarbonylamino)-2-[(4-

butylbenzoylamino)]-1-oxopropyl]amino]-3-methylbutyl]

E.5.1

Boronic acid,[(1R)-1-[[(2S)-3-(acetylamino)-2-[(decanoylamino)]-1-

oxopropyl]amino]-3-methylbutyl]

E.5.2

Boronic acid,[(1R)-1-[[(2S)-3-(propylureido)-2-[(4-butyl)-benzoylamino]-1-

oxopropyl]amino]-3-methylbutyl]

E.5.3

Boronic acid,[(1R)-1-[[(2S)-3-(methanesulfamido)-2-[(4-butyl)-

benzoylamino]-1-oxopropyl]amino]-3-methylbutyl]

E.5.4

Boronic acid,[(1R)-1-[[(2S)-3[2-(1H-pyrazol)ethyl]-2-[(4-butyl)-

benzoylamino]-1-oxopropyl]amino]-3-methylbutyl]

E.5.5

Boronic acid,[(1R)-1-[[(2S)-3-(methanesulfamido)-2-[(4-butyl)-

benzoylamino]-1-oxopropyl]amino]-3-methylbutyl]

E.5.6

Boronic acid,[(1R)-1-[[(2S)-3-[(carbobenzyloxyamino]-2-[(4-

butylbenzoylamino)]-1-oxopropyl]amino]-3-methylbutyl]

E.5.7

Boronic acid,[(1R)-1-[[(2S)-3-[(thien-2-ylcarbonyl)amino]-2-[(4-

butylbenzoylamino)]-1-oxopropyl]amino]-3-methylbutyl]

E.5.8

Boronic acid,[(1R)-1-[[(2S)-3-(acetylamino)-2-[4-butyl-benzoylamino)]-1-

oxopropyl]amino]-3-methylbutyl]

E.5.9

Boronic acid,[(1R)-1-[[(2S)-3-[(thien-2-ylcarbonyl)amino)]-2-

[(decanoylamino)]-1-oxopropyl]amino]-3-methylbutyl]

E.5.10

Boronic acid,[(1R)-1-[[(2S)-3-(hexanoylamino)-2-[(4-butylbenzoylamino)]-1-

oxopropyl]amino]-3-methylbutyl]

E.5.11

Boronic acid,[(1R)-1-[[(2S)-3-[4-fluoro-benzenesulfonamide]-2-[(4-

butylbenzoyl)amino]-1-oxopropyl]amino]-3-methylbutyl]

E.5.12

Boronic acid,[(1R)-1-[[(2S)-3-[4-fluoro-benzenesulfonamide]-2-

[(decanoyl)amino]-1-oxopropyl]amino]-3-methylbutyl]

E.5.13

Boronic acid,[(1R)-1-[[(2S)-3-(hexanonylamino)-2-[(decanoylamino)]-1-

oxopropyl]amino]-3-methylbutyl]

E.5.14

Boronic acid,[(1R)-1-[[(2S)-3-(hexanonylamino)-2-

[(cyclopropancarbonylamino)]-1-oxopropyl]amino]-3-methylbutyl]

3-methylbutyl]amino]carbonyl]-2-(cyclopropancarbonylamino)ethyl]-

E.5.15

Boronic acid,[(1R)-1-[[(2S)-3-[(3,4-dimethoxyphenyl)acetylamino]-2-[(4-

butylbenzoylamino)]-1-oxopropyl]amino]-3-methylbutyl]

E.5.16

Boronic acid,[(1R)-1-[[(2S)-3-[1-N-methyl-2-pyrrolylcarbonylamino]-2-[(4-

butylbenzoyl)amino]-1-oxopropyl]amino]-3-methylbutyl]

E.5.17

Boronic acid,[(1R)-1-[[(2S)-3-[4-sulfamylbenzoylamino]-2-[(4-

butylbenzoyl)amino]-1-oxopropyl]amino]-3-methylbutyl]

E.5.18

Boronic acid,[(1R)-1-[[(2S)-3-(nicotinoylamino)-2-[(4-butylbenzoylamino)]-

1-oxopropyl]amino]-3-methylbutyl]

E.5.19

Boronic acid,[(1R)-1-[[(2S)-3-(3-phenylureido)-2-(4-butylbenzoylamino)-1-

oxopropyl]amino]-3-methylbutyl]

E.5.20

Boronic acid,[(1R)-1-[[(2S)-3-[(4-methylsulfonyl)benzoylamino]-2-[(4-

butylbenzoylamino)]-1-oxopropyl]amino]-3-methylbutyl]

E.5.21

Boronic acid,[(1R)-1-[[(2S)-3-(3-phenylureido)-2-(decanoylamino)-1-

oxopropyl]amino]-3-methylbutyl]

E.5.22

Boronic acid,[(1R)-1-[[(2S)-3-(nicotinoylamino)-2-(decanoylamino)-1-

oxopropyl]amino]-3-methylbutyl]

E.5.23

Boronic acid,[(1R)-1-[[(2R)-3-(4-methylphenylcarbonyl)-2-(decanoylamino)-

1-oxopropyl]amino]-3-methylbutyl]

E.5.24

Boronic acid,[(1R)-1-[[(2S)-3-[4-(1H-tetrazolyl)-phenylcarbonylamino]-2-

[(4-butylbenzoylamino)]-1-oxopropyl]amino]-

3-methylbutyl]

E.5.25

Boronic acid,[(1R)-1-[[(2S)-3-(2-isoxazolylcarbonylamino)-2-[(4-

butylbenzoylamino)]-1-oxopropyl]amino]-3-methylbutyl]

E.5.26

Boronic acid,[(1R)-1-[[(2S)-3-[1-methyl-1H-imidazole-4-sulfamoyl]-2-[(4-

butylbenzoyl)amino]-1-oxopropyl]amino]-3-methylbutyl]

E.5.27

Boronic acid,[(1R)-1-[[(2S)-3-[6-morpholin-4-yl-pyridine-3-sulfamoyl]-2-

[(4-butylbenzoyl)amino]-1-oxopropyl]amino]-

3-methylbutyl]hydrochloride

E.5.28

Boronic acid,[(1R)-1-[[(2S)-3-(6-morpholinonicotinamide]-2-[(4-

butylbenzoyl)amino]-1-oxopropyl]amino]-

3-methylbutyl]

E.5.29

Boronic acid,[(1R)-1-[[(2S)-3-(4-(1,3-dimethyl-1H-pyrazole-5-

carbonylamino]-2-[4-butylbenzoyl)amino]-1-oxopropyl]amino]-

3-methylbutyl]hydrochloride

E.5.30

Boronic acid,[(1R)-1-[[(2S)-3-[4-fluoro-benzenesulfonamide]-2-[(4-

phenoxybenzoyl)amino]-1-oxopropyl]amino]-3-methylbutyl]

E.5.31

Boronic acid,[(1R)-1-[[(2S)-3-(4-(1,3-dimethyl-1H-pyrazole-5-

carbonylamino]-2-[(4-phenoxybenzoyl)amino]-1-oxopropyl]amino]-

3-methylbutyl]carbonylamino]ethyl]-

E.5.32

Boronic acid,[(1R)-1-[[(2S)-3-(4-phenylureido]-2-[(4-

phenoxybenzoyl)amino]-1-oxopropyl]amino]-

3-methylbutyl]

E.5.33

Boronic acid,[(1R)-1-[[(2S)-3-(4-phenybenzamide]-2-[(4-

butylbenzoyl)amino]-1-oxopropyl]amino]-

3-methylbutyl]

E.5.34

Boronic acid,[(1R)-1-[[(2S)-3-(4-phenylbenzamide]-2-[(4-

phenoxybenzoyl)amino]-1-oxopropyl]amino]-

3-methylbutyl]

E.5.35

Boronic acid,[(1R)-1-[[(2S)-3-(phenylpropionamide]-2-[(4-

butylbenzoyl)amino]-1-oxopropyl]amino]-

3-methylbutyl]

E.5.36

Boronic acid,[(1R)-1-[[(2S)-3-(4-methylphenylsulfonyl)-ureido]-2-[(4-

butylbenzoyl)amino]-1-oxopropyl]amino]-

3-methylbutyl]

E.5.37

Boronic acid,[(1R)-1-[[(2S)-3-(4-(2-(4-pyridyl)-1,3-thiazole-4-

carbonylamino)]-2-[(4-butylbenzoyl)amino]-1-oxopropyl]amino]-

3-methylbutyl]

E.5.38

Boronic acid,[(1R)-1-[[(2S)-3-(1-methanesulfonylpiperidine-4-

carbonylamino)-2-[(4-butylbenzoylamino)]-1-

oxopropyl]amino]-3-methylbutyl]

E.5.39

Boronic acid,[(1R)-1-[[(2S)-3-[(2-thiophene)sulfonylamino]-2-[(4-

butylbenzoylamino)]-1-oxopropyl]amino]-3-methylbutyl]

E.5.40

Boronic acid,[(1R)-1-[[(2S)-3-(4-(1H-1,2,4-triazol-1-yl)benzoylamide)]-2-

[(4-butylbenzoyl)amino]-1-oxopropyl]amino]-3-methylbutyl]hydrochloride

E.5.41

Boronic acid,[(1R)-1-[[(2R)-3-(4-methylphenylcarbonyl)-2-(decanoylamino)-

1-oxopropyl]amino]-3-methylbutyl]

E.5.42

Boronic acid,[(1R)-1-[[(2S)-3-(4-phenylureido]-2-(decanoylamino)-1-

oxopropyl]amino]-3-methylbutyl]

E.5.43

Boronic acid,[(1R)-1-[[(2S)-3-acetylamino-2-decanoylamino-1-

oxopropyl]amino]-

3-methylbutyl]

F.2.1

4-Butylbenzamide,N-[(1S,2R)-1-[[[(1R)-1-[13,15-dioxa-14-bora-

dispiro[5.0.5.3]pentadec-14-yl]-3-methylbutyl]amino]carbonyl]-2-

hydroxypropyl]-

or a pharmaceutically acceptable salt, free base, or boronic ester thereof.

45. The method of claim 1 , wherein the compound is boronic acid, [(1R)-1-[[(2S,3R)-3-hydroxy-2-[(6-phenyl-pyridine-2-carbonyl)amino]-1-oxobutyl]amino]-3-methylbutyl], or a pharmaceutically acceptable salt or boronic ester thereof.

46. The method of claim 1 , wherein the cancer is selected from skin, prostate, colorectal, pancreas, kidney, ovary, mammary, liver, tongue, lung, and smooth muscle tissue.

47. The method of claim 23 , wherein the cancer is selected from skin, prostate, colorectal, pancreas, kidney, ovary, mammary, liver, tongue, lung, and smooth muscle tissue.

48. The method of claim 29 , wherein the cancer is selected from skin, prostate, colorectal, pancreas, kidney, ovary, mammary, liver, tongue, lung, and smooth muscle tissue.

49. The method of claim 30 , wherein the cancer is selected from skin, prostate, colorectal, pancreas, kidney, ovary, mammary, liver, tongue, lung, and smooth muscle tissue.

50. The method of claim 36 , wherein the cancer is selected from skin, prostate, colorectal, pancreas, kidney, ovary, mammary, liver, tongue, lung, and smooth muscle tissue.

51. The method of claim 42 , wherein the cancer is selected from skin, prostate, colorectal, pancreas, kidney, ovary, mammary, liver, tongue, lung, and smooth muscle tissue.

52. The method of claim 43 , wherein the cancer is selected from skin, prostate, colorectal, pancreas, kidney, ovary, mammary, liver, tongue, lung, and smooth muscle tissue.

53. The method of claim 44 , wherein the cancer is selected from skin, prostate, colorectal, pancreas, kidney, ovary, mammary, liver, tongue, lung, and smooth muscle tissue.

54. The method of claim 45 , wherein the cancer is selected from skin, prostate, colorectal, pancreas, kidney, ovary, mammary, liver, tongue, lung, and smooth muscle tissue.

55. The method of claim 1 , wherein the cancer is selected from leukemia, lymphoma, non-Hodgkin lymphoma, myeloma, and multiple myeloma.

56. The method of claim 23 , wherein the cancer is selected from leukemia, lymphoma, non-Hodgkin lymphoma, myeloma, and multiple myeloma.

57. The method of claim 29 , wherein the cancer is selected from leukemia, lymphoma, non-Hodgkin lymphoma, myeloma, and multiple myeloma.

58. The method of claim 30 , wherein the cancer is selected from leukemia, lymphoma, non-Hodgkin lymphoma, myeloma, and multiple myeloma.

59. The method of claim 36 , wherein the cancer is selected from leukemia, lymphoma, non-Hodgkin lymphoma, myeloma, and multiple myeloma.

60. The method of claim 42 , wherein the cancer is selected from leukemia, lymphoma, non-Hodgkin lymphoma, myeloma, and multiple myeloma.

61. The method of claim 43 , wherein the cancer is selected from leukemia, lymphoma, non-Hodgkin lymphoma, myeloma, and multiple myeloma.

62. The method of claim 44 , wherein the cancer is selected from leukemia, lymphoma, non-Hodgkin lymphoma, myeloma, and multiple myeloma.

63. The method of claim 45 , wherein the cancer is selected from leukemia, lymphoma, non-Hodgkin lymphoma, myeloma, and multiple myeloma.

64. The method of claim 1 , wherein the cancer is multiple myeloma.

65. The method of claim 23 , wherein the cancer is multiple myeloma.

66. The method of claim 29 , wherein the cancer is multiple myeloma.

67. The method of claim 30 , wherein the cancer is multiple myeloma.

68. The method of claim 36 , wherein the cancer is multiple myeloma.

69. The method of claim 42 , wherein the cancer is multiple myeloma.

70. The method of claim 43 , wherein the cancer is multiple myeloma.

71. The method of claim 44 , wherein the cancer is multiple myeloma.

72. The method of claim 45 , wherein the cancer is multiple myeloma.

73. The method of claim 1 , comprising administering the compound in combination with one or more antitumor or anticancer agent and/or radiotherapy.

74. The method of claim 23 , comprising administering the compound in combination with one or more antitumor or anticancer agent and/or radiotherapy.

75. The method of claim 29 , comprising administering the compound in combination with one or more antitumor or anticancer agent and/or radiotherapy.

76. The method of claim 30 , comprising administering the compound in combination with one or more antitumor or anticancer agent and/or radiotherapy.

77. The method of claim 36 , comprising administering the compound in combination with one or more antitumor or anticancer agent and/or radiotherapy.

78. The method of claim 42 , comprising administering the compound in combination with one or more antitumor or anticancer agent and/or radiotherapy.

79. The method of claim 43 , comprising administering the compound in combination with one or more antitumor or anticancer agent and/or radiotherapy.

80. The method of claim 44 , comprising administering the compound in combination with one or more antitumor or anticancer agent and/or radiotherapy.

81. The method of claim 45 , comprising administering the compound in combination with one or more antitumor or anticancer agent and/or radiotherapy.

82. The method of claim 72 , comprising administering the compound in combination with one or more antitumor or anticancer agent and/or radiotherapy.

Assignments (5)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 10, 2022
From: MILLENNIUM PHARMACEUTICALS, INC.
To: TAKEDA PHARMACEUTICAL COMPANY LIMITED
Reel/Frame 061725/0893 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 11, 2015
From: TEVA PHARMACEUTICALS
To: MILLENNIUM PHARMACEUTICALS, INC.
Reel/Frame 037267/0401 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 16, 2011
From: CHATTERJEE, SANKAR; IQBAL, MOHAMED; MESSINA MCLAUGHLIN, PATRICIA A.
To: CEPHALON, INC.
Reel/Frame 025817/0619 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 16, 2011
From: BERNARDINI, RAFFAELLA; BERNAREGGI, ALBERTO; CASSARA, PAOLO G.; D'ARASMO, GERMANO; DE MUNARI, SERGIO; FERRETTI, EDMONDO; MENTA, ERNESTO; OLIVA, AMBROGIO
To: CELL THERAPEUTICS EUROPE S.R.L.
Reel/Frame 025817/0979 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 16, 2011
From: CELL THERAPEUTICS EUROPE S.R.L.
To: CEPHALON, INC.
Reel/Frame 025820/0392 →
Continuity (4)
Continuation 12496359 · Jul 1, 2009
Division 10918664 · Aug 12, 2004
Provisional Application 60495764 · Aug 14, 2003
Related Publication 20110144033A1 · Jun 16, 2011