Piperazine derivatives as HIV protease inhibitors
View Patent ↗The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
1. A compound of structural Formula I:
or a pharmaceutically acceptable salt thereof, wherein:
X is O or CH 2 ;
Ring A is
wherein * indicates the point of attachment to X* in Formula I and ** indicates the point of attachment to N** in Formula I;
one, two or three of Y 1 , y 2 , y 3 and Y 4 are N and the others are C(R);
HetAr is:
(a) a 5-membered (including the two carbons that are the points of attachment to X* and N** in Formula I) monocyclic heteroaromatic ring containing from 1 to 3 heteroatoms independently selected from N, O and S, or
(b) a 9-, 10- or 11-membered (including the two carbons that are the points of attachment to X* and N** in Formula I) bicyclic heteroaromatic ring system containing from 1 to 4 heteroatoms independently selected from N, O and S;
p is an integer selected from 1, 2 or 3;
R is independently selected at each occurrence from,
(a) —H,
(b) halo, —OH, —SH, —CN, —NO 2 , or —N(R 3a ) 2 ,
(c) —C 1-6 alkyl unsubstituted or substituted with (i) 1 to 6 of —F, or (ii) —OH, —C(O)OC 1-6 alkyl, —O—C 1-6 alkyl or —O—C 1-3 alkyl-phenyl,
(d) —OC 1-6 alkyl unsubstituted or substituted with (i) 1 to 6 of —F, or (ii) —OH, —C(O)OC 1-6 alkyl, —O—C 1-6 alkyl or —O—C 1-3 alkyl-phenyl,
(e) —C 1-6 alkyl-O—C 1-3 alkyl unsubstituted or substituted with 1 to 6 of —F,
(f) —C(O)OC 1-6 alkyl unsubstituted or substituted with 1-6 of —F, or
(g) —C(O)C 1-6 alkyl unsubstituted or substituted with 1-6 of —F;
Z 1 is
R a and R b are independently selected from —H and —C 1-3 alkyl;
R c is —C 1-3 alkyl or —C 3-6 cycloalkyl and R c is unsubstituted or substituted with 1-3 of —F;
R d is —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F or —C 3-6 cycloalkyl unsubstituted or substituted with 1-3 of —F;
m is the integer 1;
Z 2 is —H or —NHR 3 ;
R 2a is
(a) —C 1-6 alkyl unsubstituted or substituted with one to four substituents independently selected at each occurrence from halo; —OH; —C 1-6 alkyl unsubstituted or substituted with 1-3 of —F; or —OR c ;
(b) —C 3-6 cycloalkyl unsubstituted or substituted with one to four substituents independently selected at each occurrence from halo; —OH; —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F; —C 1-3 alkyl —OR c ; —OR d ; —COOH; or —C(O)OR d ;
(c) phenyl unsubstituted or substituted with one to four substituents independently selected at each occurrence from halo; —OH; —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F; —C 1-3 alkyl-O—R c ; —OR d ; —COOH; —C(O)OR d ; or —C 3-6 cycloalkyl unsubstituted or substituted with 1-3 of —F;
wherein the tetrahydropyran is unsubstituted or substituted with one to four substituents independently selected at each occurrence from halo —OH; —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F; or —OC 1-6 alkyl unsubstituted or substituted with 1-6 of —F;
(e) pyridinyl unsubstituted or substituted with one to four substituents independently selected at each occurrence from
(i) halo, (ii) —OH,
(iii) —C 1-6 alkyl unsubstituted or substituted with (i) 1 to 6 of —F, or (ii) —OH, —C(O)OC 1-6 alkyl, —O—C 1-6 alkyl, or —O—C 1-3 alkyl-phenyl,
(iv) —OC 1-6 alkyl unsubstituted or substituted with (i) 1 to 6 of —F, or (ii) —OH, —C(O)OC 1-6 alkyl, —O—C 1-6 alkyl, or —O—C 1-3 alkyl-phenyl,
(v) —C 1-6 alkyl-O—C 1-3 alkyl unsubstituted or substituted with 1 to 6 of —F,
(vi) ═O (oxo),
(vii) —C(O)OC 1-6 alkyl optionally substituted with 1-6 of —F, or
(viii) —C(O)C 1-6 alkyl optionally substituted with 1-6 of —F;
(f) pyrimidinyl, unsubstituted or substituted with one to four substituents independently selected at each occurrence from
(i) halo, (ii) —OH,
(iii) —C 1-6 alkyl unsubstituted or substituted with (i) 1 to 6 of —F, or (ii) —OH, —C(O)OC 1-6 alkyl, —O—C 1-6 alkyl, or —O—C 1-3 alkyl-phenyl,
(iv) —OC 1-6 alkyl unsubstituted or substituted with (i) 1 to 6 of —F, or (ii) —OH, —C(O)OC 1-6 alkyl, —O—C 1-6 alkyl, or —O—C 1-3 alkyl-phenyl,
(v) —C 1-6 alkyl-O—C 1-3 alkyl unsubstituted or substituted with 1 to 6 of —F,
(vi) ═O (oxo),
(vii) —C(O)OC 1-6 alkyl optionally substituted with 1-6 of —F, or
(viii) —C(O)C 1-6 alkyl optionally substituted with 1-6 of —F;
unsubstituted or substituted with one to four substituents independently selected at each occurrence from halo; —OH; —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F; —OC 1-6 alkyl unsubstituted or substituted with 1-6 of —F; or —C 3-6 cycloalkyl unsubstituted or substituted with 1-3 of —F;
(i) morpholinyl;
(j) piperidinyl, unsubstituted or substituted with one to four substituents independently selected at each occurrence from halo; —OH; —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F;
—OC 1-6 alkyl unsubstituted or substituted with 1-6 of —F; or —C(O)OR 1 ;
(k) pyrazinyl, unsubstituted or substituted with one to four substituents independently selected at each occurrence from halo; —OH; —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F; —OC 1-6 alkyl unsubstituted or substituted with 1-6 of —F; or —C(O)OR 1 ;
(l) thiazolyl, unsubstituted or substituted with one to three substituents independently selected at each occurrence from halo; —OH; —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F; —OC 1-6 alkyl unsubstituted or substituted with 1-6 of —F; or —C(O)OR 1 ;
(m) pyrazolyl, unsubstituted or substituted halo; —OH; —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F; —OC 1-6 alkyl unsubstituted or substituted with 1-6 of —F; or —C(O)OR 1 ; or
R 1 is (i) —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F, phenyl or —C 3-6 cycloalkyl, or (ii) —S(O) 2 —C 1-6 alkyl;
R 2b is —H, —C 1-6 alkyl or —OC 1-6 alkyl, wherein each of —C 1-6 alkyl or —OC 1-6 alkyl is unsubstituted or substituted with 1 to 3 substituents independently selected from halo, —OH, or —OC 1-6 alkyl;
or R 2a and R 2b are joined together with the carbon to which they are both attached to form (a) —C 3-6 cycloalkyl, (b) piperidinyl, or (c) tetrahydro-(2H)-furanyl;
wherein each of cycloalkyl, piperidinyl and tetrahydro-(2H)-furan is unsubstituted or substituted with one to four substituents independently selected at each occurrence from halo;
—OH; —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F; —OC 1-6 alkyl unsubstituted or substituted with 1-6 of —F; or —COOC 1-3 alkyl unsubstituted or substituted with 1-6 of —F;
R 3 and R 3a are independently selected at each occurrence from
(a) —H,
(b) —C 1-6 alkyl unsubstituted or substituted with (i) 1 to 6 of —F, (ii) —OH, (iii) —C(O)OC 1-3 alkyl, (iv) —O—C 1-3 alkyl, or (v) —O—C 1-3 alkyl-phenyl,
(c) —C(O)OC 1-6 alkyl unsubstituted or substituted with (i) 1-6 of —F, (ii) —C 3-6 cycloalkyl or (iii) —NH 2 , or
(d) —C(O)C 1-6 alkyl unsubstituted or substituted with (i) 1-6 of —F, (ii) —C 3-6 cycloalkyl or (iii) —NH 2 ;
n is an integer selected from 1, 2 or 3;
R 4 is independently selected at each occurrence from:
(a) —H, —OH, halo, —CN, —C 1-6 alkyl, —O—C 1-6 alkyl, —C 3-6 cycloalkyl, —O—C 3-6 cycloalkyl, —C 2-6 alkenyl-SR 5 , —S—C 3-6 cycloalkyl, —SO 2 R 5 , —N(R 5 ) 2 , —N(H)C(O)—C 1-6 alkyl, —C(O)OR 5 , —C(O)—C 1-6 alkyl, —C 1-6 haloalkyl, —O—C 1-6 haloalkyl, —S—C 1-6 haloalkyl, —NO 2 , —N(H)CH(O), —CH(O), —C(O)N(R 5 ) 2 , —C(O)N(H)C(O)R 5 , or trimethylsilyl,
(b) phenyl, benzyl or phenoxy, each being unsubstituted or substituted with 1 to 5 substituents selected from halogen and, —OH, halo, —CN, —C 1-6 alkyl, —C 1-6 haloalkyl, —O—C 1-6 alkyl, —O—C 1-6 haloalkyl, —S—C 1-6 haloalkyl, —NO 2 , —SO 2 R 5 , —N(R 5 ) 2 , —C(O)OR 5 , or —C(O)—C 1-6 alkyl, or
(c) HetA, —O-HetA or —CH 2 —HetA, optionally substituted with 1 to 5 substituents selected from halogen and C 1-6 alkyl;
wherein —C 1-6 alkyl when present within any R 4 group is unsubstituted or substituted with 1 to 6 substituents independently selected at each occurrence from:
-halo, —CF3, —CN, —NO 2 , —OH, —O—C 1-6 alkyl, —O—C 1-6 haloalkyl, —O—C 3-6 cycloalkyl, —SR 5 , —N(R 5 ) 2 , —C(O)—C 1-6 alkyl, —C(O)OR 5 , or —SO 2 —C 1-6 alkyl;
R 5 is independently selected at each occurrence from —H and C 1-6 alkyl; and
HetA is independently selected from (i) a 5- or 6-membered monocyclic heteroaromatic ring containing from 1 to 3 heteroatoms independently selected from N, O and S, or (ii) a 9-, 10- or 11-membered bicyclic fused heteroaromatic ring system containing from 1 to 4 heteroatoms independently selected from N, O and S.
2. The compound of claim 1 having structural Formula II or a pharmaceutically acceptable salt thereof:
3. The compound of claim 1 having structural Formula III or a pharmaceutically acceptable salt thereof:
4. The compound of claim 1 or a pharmaceutically acceptable salt thereof wherein Z 2 is —NHR 3 .
5. The compound of claim 2 , or a pharmaceutically acceptable salt thereof wherein Z 1 is
6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein Ring A is
7. The compound of claim 6 or a pharmaceutically acceptable salt thereof wherein Ring A is
8. The compound of claim 6 or a pharmaceutically acceptable salt thereof wherein Ring A is
9. The compound of claim 6 or a pharmaceutically acceptable salt thereof wherein Ring A is
and HetAr is
10. The compound of claim 2 , or a pharmaceutically acceptable salt thereof wherein R 2a is:
(a) —C 1-6 alkyl unsubstituted or substituted with one or two substituents independently selected at each occurrence from halo; —OH; —C 1-6 alkyl unsubstituted or substituted with 1-3 of —F; or —Or c ,
(b) —C 3-6 cycloalkyl unsubstituted or substituted with one or two substituents independently selected at each occurrence from halo; —OH; —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F; —C 1-3 alkyl-OR c ; —OR d ; —COOH; or —C(O)Or d ,
(c) phenyl unsubstituted or substituted with one or two substituents independently selected at each occurrence from halo; —OH; —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F; —C 1-3 alkyl-O—R c ; —OR d ; —COOH; —C(O)OR d ; or —C 3-6 cycloalkyl unsubstituted or substituted with 1-3 of —F,
wherein the tetrahydropyran is unsubstituted or substituted with one or two substituents independently selected at each occurrence from halo —OH; —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F; or —OC 1-6 alkyl unsubstituted or substituted with 1-6 of —F,
(e) pyridinyl unsubstituted or substituted with one or two substituents independently selected at each occurrence from
(i) halo, (ii) —OH,
(iii) —C 1-6 alkyl unsubstituted or substituted with (i) 1 to 6 of —F, or (ii) —OH, —C(O)OC 1-6 alkyl, —O—C 1-6 alkyl, or —O—C 1-3 alkyl-phenyl,
(iv) —OC 1-6 alkyl unsubstituted or substituted with (i) 1 to 6 of —F, or (ii) —OH, —C(O)OC 1-6 alkyl, —O—C 1-6 alkyl, or —O—C 1-3 alkyl-phenyl,
(v) —C 1-6 alkyl-O—C 1-3 alkyl unsubstituted or substituted with 1 to 6 of —F,
(vi) ═O (oxo),
(vii) —C(O)OC 1-6 alkyl optionally substituted with 1-6 of —F, or
(viii) —C(O)C 1-6 alkyl optionally substituted with 1-6 of —F,
(f) pyrimidinyl unsubstituted or substituted with one or two substituents independently selected at each occurrence from
(i) halo, (ii) —OH,
(iii) —C 1-6 alkyl unsubstituted or substituted with (i) 1 to 6 of —F, or (ii) —OH, —C(O)OC 1-6 alkyl, —O—C 1-6 alkyl, or —O—C 1-3 alkyl-phenyl,
(iv) —OC 1-6 alkyl unsubstituted or substituted with (i) 1 to 6 of —F, or (ii) —OH, —C(O)OC 1-6 alkyl, —O—C 1-6 alkyl, or —O—C 1-3 alkyl-phenyl,
(v) —C 1-6 alkyl-O—C 1-3 alkyl unsubstituted or substituted with 1 to 6 of —F,
(vi) ═O (oxo),
(vii) —C(O)OC 1-6 alkyl optionally substituted with 1-6 of —F, or
(viii) —C(O)C 1-6 alkyl optionally substituted with 1-6 of —F, or
unsubstituted or substituted with one or two substituents independently selected at each occurrence from halo; —OH; —C 1-6 alkyl unsubstituted or substituted with 1-6 of —F; —OC 1-6 alkyl unsubstituted or substituted with 1-6 of —F; or —C 3-6 cycloalkyl unsubstituted or substituted with 1-3 of —F.
11. The compound of claim 10 , or a pharmaceutically acceptable salt thereof wherein R 2b is —H, —C 1-3 alkyl or —OC 1-3 alkyl wherein each of —C 1-3 alkyl or —OC 1-3 alkyl is unsubstituted or substituted with 1 to 3 substituents independently selected from halo, —OH, or —OC 1-6 alkyl.
12. The compound of claim 2 , or a pharmaceutically acceptable salt thereof wherein R 2a and R 2b are joined together with the carbon to which they are both attached to form (a) cyclohexyl, (b) piperidinyl, or (c) tetrahydro-(2H)-furan; wherein each group is unsubstituted or substituted with one or two substituents independently selected at each occurrence from halo; —OH; —C 1-3 alkyl unsubstituted or substituted with 1-3 of —F; —OC 1-3 alkyl unsubstituted or substituted with 1-3 of —F; or —C(O)OC 1-3 alkyl unsubstituted or substituted with 1-3 of —F.
13. The compound of claim 2 , or a pharmaceutically acceptable salt thereof wherein R 4 is independently selected at each occurrence from halo.
14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein p is 1 or 2.
15. The compound of claim 4 or a pharmaceutically acceptable salt thereof wherein R 3 is —H or —C(O)OC 1-6 alkyl.
16. The compound of claim 1 having structural Formula IV, or a pharmaceutically acceptable salt thereof,
wherein R 2a is:
(a) —C 1-4 alkyl unsubstituted or substituted with (a) 1 to 3 of —F, (b) —OH or —OC 1-3 alkyl;
(b) cyclohexyl unsubstituted or substituted with (a) 1 to 3 of —F, or (b) —OH or —OC 1-3 alkyl;
(c) phenyl unsubstituted or substituted with 1 to 2 of halo;
(d) pyridyl unsubstituted or substituted with —F, —Cl, —OC 1-3 alkyl, or —C 1-3 alkyl substituted with 1-3 of —F; or
unsubstituted or substituted with 1 to 3 of —C 1-3 alkyl;
R 2b is —H;
or R 2a and R 2b are joined together with the carbon to which they are both attached to form cyclohexyl unsubstituted or substituted with —OC 1-3 alkyl;
R 3 is —H or —C(O)OC 1-3 alkyl;
R 4 is —F or —Cl; and
Ring A is (a) cyclohexyl, (b) phenyl substituted with 1-2 of —F, or (c) pyridyl substituted with F.
17. The compound of claim 1 which is:
1)
(βS)-N-{2-[2-(2,2-Dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-3,5-difluoro-β-(4-fluorophenyl)-L-phenylalaninamide
2)
(βS)-N-{2-[2-(2,2-Dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-(4-fluorophenyl)-3-(trifluoromethyl)-L-phenylalaninamide
3)
Methyl [(1S,2R)-2-(4-chlorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-3-
methylbutyl]carbamate
4)
Methyl [(1S,2R)-2-(4-chlorophenyl)-2-(3,3-difluorocyclobutyl)-1-({2-[2-(2,2-dioxido-
2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}carbamoyl)ethyl]carbamate
5)
Methyl [(1S,2R)-2-(4-chlorophenyl)-2-(4,4-difluorocyclohexyl)-1-({2-[2-(2,2-dioxido-
2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}carbamoyl)ethyl]carbamate
6)
(2S,3R)-2-amino-3-(4-chlorophenyl)-N-(2-(2-((6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]decan-9-yl)ethyl)-3-fluorophenyl)-3-((1r,4R)-4-
ethoxycyclohexyl)propanamide
7)
(βR)-4-Chloro-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-β-[(1r,4R)-4-methoxycyclohexyl]-L-phenylalaninamide
8)
Methyl (1R,2S)-1-(4-chlorophenyl)-3-((2-(2-((6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)-3-fluorophenyl)amino)-3-oxo-1-((2R,4S)-2-
(2,2,2-trifluoroethyl)tetrahydro-2H-pyran-4-yl)propan-2-yl)carbamate
9)
Methyl [(1S,2R)-2-(4-chloro-3-fluorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-4-(tetrahydro-2H-
pyran-4-yl)butyl]carbamate
10)
(2S, 3R)-2-amino-3-(4-chlorophenyl)-3-((S)-2,2-dimethyltetrahydro-2H-pyran-4-yl)-N-
(2-(2-((6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]decan-9-yl)ethyl)-3-
fluorophenyl)propanamide
11)
(βS)-4-Chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-[6-(1-methylethoxy)pyridin-3-yl]L-phenylalaninamide
12)
(2S,3S)-2-amino-3-(4-chlorophenyl)-3-(6-(1,1-difluoroethyl)pyridin-3-yl)-N-(2-(2-
((6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]decan-9-yl)ethyl)-3-
fluorophenyl)propanamide
13)
Methyl {(1S)-1-[trans-1-(4-chlorophenyl)-4-methoxycyclohexyl]-2-[(2-2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)amino]-2-
oxoethyl}carbamate
14)
Methyl 4-{(1S)-1-amino-2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]}-3-fluorophenyl)amino]-2-oxoethyl}-4-(4-
chlorophenyl)piperidine-1-carboxylate
15)
β-[(2R,4r,6S)-2,6-Dimethyltetrahydro-2H-pyran-4-yl]-N-(2-{2-[(6R,9S)-2,2-dioxido-2-
thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)-4-fluoro-L-
phenylalaninamide
16)
Methyl {(1S,2R)-2-(4-chloro-3-fluorophenyl)-2-[(2R,6S)-2,6-dimethyltetrahydro-2H-
pyran-4-yl]-1-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)carbamoyl]ethyl}carbamate
17)
(βS)-4-Chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-[2-(1-methylethoxy)pyridin-4-yl]-L-phenylalaninamide
18)
Methyl {(1S,2S)-2-(4-chlorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-[2-
(trifluoromethyl)pyridin-4-yl]ethyl}carbamate
19)
Methyl {(1S,2S)-2-(4-chloro-3-fluorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-[5-
(trifluoromethyl)pyridin-3-yl]ethyl}carbamate
20)
(βS)-4-Chloro-β-[5-(1,1-difluoroethyl)pyridin-3-yl]-N-{2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}-L-phenylalaninamide
21)
Methyl {(1S,2S)-2-(4-chlorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}-carbamoyl)-2-[6-
(trifluoromethyl)pyridin-3-yl]ethyl}carbamate
22)
Methyl [(1S)-2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)amino]-1-{(S)-(4-fluorophenyl)[2-(trifluoromethyl)pyrimidin-
5-yl]methyl}-2-oxoethyl]carbamate
23)
(βS)-N-(2-{2-[(6R,9S)-2,2-Dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)-4-fluoro-β-[2-(1-methylethoxy)pyrimidin-5-yl]-L-phenylalaninamide
24)
(βR)-4-Chloro-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]-β-(tetrahydro-2H-pyran-4-yl)-L-
phenylalaninamide
25)
Methyl [(1S,2R)-2-(4-chlorophenyl)-1-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]carbamoyl}-2-(tetrahydro-2H-pyran-4-
yl)ethyl]carbamate
26)
Methyl ((2S,3R)-1-((2-(2-((6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]decan-9-
yl)ethyl)-3,4-difluorophenyl)amino)-3-(4-fluorophenyl)-3-((1r,4R)-4-
methoxycyclohexyl)-1-oxopropan-2-yl)carbamate
27)
(2S,3R)-2-Amino-N-(4-(2-((6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]decan-9-
yl)ethyl)-5-fluoropyridin-3-yl)-3-(4-fluorophenyl)-3-((1r,4R)-4-
methoxycyclohexyl)propanamide
28)
Methyl [(1S,2R)-2-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-1-[(2-{2-[(6R,9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1dec-9-yl]]ethyl}-3,4-difluorophenyl)carbamoyl]-
2-(4-fluorophenyl)ethyl]carbamate
29)
Methyl [(1S,2R)-2-(4-chlorophenyl)-2-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-1-
{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}cyclopentyl]carbamoyl}ethyl]carbamate
30)
Methyl [(1S,2R)-2-[(2R,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-1-[(2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-5-fluorophenyl)carbamoyl]-
2-(4-fluorophenyl)ethyl]carbamate
31)
(2S,3R)-2-Amino-3-(4-chlorophenyl)-3-((2R,4r,6S)-2,6-dimethyltetrahydro-2H-pyran-
4-yl)-N-(4-((6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]decan-9-yl)ethyl)-5-
fluoropyridin-3-yl)propanamide
32)
Methyl [(1S,2R)-2-(4-chlorophenyl)-1-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}-3,6-difluorophenyl)carbamoyl]-2-(tetrahydro-2H-
pyran-4-yl)ethyl]carbamate
33)
(βR)-N-{2-[2-(2,2-Dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-(4-fluorophenyl)-4-(trifluoromethyl)-L-phenylalaninamide
34)
Methyl [(1S,2S)-2-(2,3-dihydro-1H-inden-5-yl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-(4-
fluorophenyl)ethyl]carbamate
35)
methyl [(1S,2S)-2-(3,5-difluorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-(4-
fluorophenyl)ethyl]carbamate
36)
(βR)-4-chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-(tetrahydro-2H-pyran-4-yl)-L-phenylalaninamide
37)
methyl [(1S,2R)-2-(4-chlorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-(tetrahydro-2H-
pyran-4-yl)ethyl]carbamate
38)
(βR)-4-chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-(1-methylethyl)-L-phenylalaninamide
39)
(2S)-2-amino-2-[4,4-difluoro-1-(4-fluorophenyl)cyclohexyl]-N-(2-{2-[(9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl}-3-fluorophenyl)ethanamide
40)
(2S)-2-amino-2-[4-(4-chlorophenyl)tetrahydro-2H-pyran-4-yl]-N-(2-{2-[(9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl}-3-fluorophenyl)ethanamide
41)
methyl {(1S)-1-[4,4-difluoro-1-(4-fluorophenyl)cyclohexyl]-2-[(2-{2-[(9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)amino]-2-
oxoethyl}carbamate
42)
methyl {(1S)-1-[4-(4-chlorophenyl)tetrahydro-2H-pyran-4-yl]-2-[(2-{2-[(9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)amino]-2-
oxoethyl}carbamate
43)
methyl {(1S,2R)-2-(4-chlorophenyl)-2-[(4S)-2,2-dimethyltetrahydro-2H-pyran-4-yl]-1-
[(2-{2-[(9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)carbamoyl]ethyl}carbamate
44)
(βS)-4-chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-3-fluoro-β-(5-fluoropyridin-3-yl)-L-phenylalaninamide
45)
(βS)-4-chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-(6-methoxypyridin-3-yl)-L-phenylalaninamide
46)
methyl [(1S,2S)-2-(4-chloro-3-fluorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-(5-fluoropyridin-3-
yl)ethyl]carbamate
47)
methyl [(1S,2S)-2-(4-chlorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl-fluorophenyl}carbamoyl)-2-(6-methoxypyridin-3-
yl)ethyl]carbamate
48)
(βR)-4-chloro-β-(3,3-difluorocyclobutyl)-N-{2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}-L-phenylalaninamide
49)
methyl [(1S)-1-[bis(4-fluorophenyl)methyl]-2-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-
thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]amino}-2-oxoethyl]carbamate
50)
methyl [(1S,2R)-2-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-1-{[(1S,2R)-2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl}cyclopentyl]carbamoyl}-2-(4-
fluorophenyl)ethyl]carbamate
51)
(βS)-3-cyclopropyl-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl)ethyl]-3-fluorophenyl}-β-(4-fluorophenyl)-L-phenylalaninamide
52)
methyl [(1S,2S)-2-(3-cyclopropylphenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-(4-
fluorophenyl)ethyl]carbamate
53)
(βR)-4-chloro-β-(4,4-difluorocyclohexyl)-N-{2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}-L-phenylalaninamide
54)
(βR)-β-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-N-[(1S,2R)-2-{2-{(6R,9S)-2,2-dioxido-
2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-4-fluoro-L-
phenylalaninamide
55)
(βR)-4-chloro-β-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-N-[(1S,2R)-2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-L-
phenylalaninamide
56)
methyl [(1S,2S)-2-(3,5-difluorophenyl)-1-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-
1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]carbamoyl}-2-(4-
fluorophenyl)ethyl]carbamate
57)
(βS)-β-(3,5-difluorophenyl)-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-4-fluoro-L-phenylalaninamide
58)
methyl [(1S,2R)-2-(4-chlorophenyl)-1-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]carbamoyl}-2-(tetrahydro-2H-pyran-4-
yl)ethyl]carbamate
59)
(βR)-4-cyclopropyl-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl)ethyl]-3-fluorophenyl}-β-(4-fluorophenyl)-L-phenylalaninamide
60)
methyl [(1S,2R)-2-(4-cyclopropylphenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-(4-
fluorophenyl)ethyl]carbamate
61)
(βS)-β-(4,4-difluorocyclohexyl)-N-{2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}-4-fluoro-L-phenylalaninamide
62)
methyl [(1S,2S)-2-(4,4-difluorocyclohexyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-(4-
fluorophenyl)ethyl]carbamate
63)
methyl [(1S)-2-({2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}amino)-1-{(S)-(4-fluorophenyl)[3-(trifluoromethyl)phenyl]methyl}-2-
oxoethyl]carbamate
64)
(βS)-β-(3,3-difluorocyclobutyl)-N-{2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}-4-fluoro-L-phenylalaninamide
65)
methyl [(1S,2S)-2-(3,3-difluorocyclobutyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-(4-
fluorophenyl)ethyl]carbamate
66)
(βS)-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-3,4-difluoro-β-(6-methoxypyridin-3-yl)-L-phenylalaninamide
67)
(βR)-4-chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-3-fluoro-β-(2-methoxypyridin-4-yl)-L-phenylalaninamide
68)
methyl [(1S,25)-2-(3,4-difluorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-(6-methoxypyridin-3-
yl)ethyl]carbamate
69)
methyl [(1S,2R)-2-(4-chloro-3-fluorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-(2-methoxypyridin-4-
yl)ethyl]carbamate
70)
(βR)-4-chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-(1-ethylpropyl)-L-phenylalaninamide
71)
methyl [(1S,2R)-2-(4-chlorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-3-
ethylpentyl]carbamate
72)
(βS)-4-chloro-β-(5-chloropyridin-3-yl)-N-{2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}-3-fluoro-L-phenylalaninamide
73)
methyl [(1S,2S)-2-(4-chloro-3-fluorophenyl)-2-(5-chloropyridin-3-yl)-1-({2-[2-(2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}carbamoyl)ethyl]carbamate
74)
(βR)-4-chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-3-fluoro-β-[2-(tetrahydro-2H-pyran-4-yl)ethyl]-L-phenylalaninamide
75)
(3S)-3-(4-chloro-3-fluorophenyl)-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-3-morpholin-4-ylpropanamide
76)
(βS)-4-chloro-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-
9-yl]ethyl}cyclopentyl]-3-fluoro-β-[5-(trifluoromethyl)pyridin-3-yl]-L-
phenylalaninamide
77)
methyl [(1S,2S)-2-(4-chloro-3-fluorophenyl)-1-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-
thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]carbamoyl}-2-(5-fluoropyridin-
3-yl)ethyl]carbamate
78)
methyl [(1S,2S)-2-(4-chlorophenyl)-1-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]carbamoyl}-2-(6-methoxypyridin-3-
yl)ethyl]carbamate
79)
methyl {(1S,2S)-2-(4-chloro-3-fluorophenyl)-1-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-
thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]carbamoyl}-2-[5-
(trifluoromethyl)pyridin-3-yl]ethyl}carbamate
80)
(βS)-4-chloro-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-
9-yl]ethyl}cyclopentyl]-β-(6-methoxypyridin-3-yl)-L-phenylalaninamide
81)
(βS)-4-chloro-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-
9-yl]ethyl}cyclopentyl]-3-fluoro-β-(5-fluoropyridin-3-yl)-L-phenylalaninamide
82)
methyl {(1S)-2-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-
9-yl]ethyl}cyclopentyl]amino}-1-[(S)-(6-methoxypyridin-3-yl)(phenyl)methyl]-2-
oxoethyl}carbamate
83)
methyl [(1S)-2-[(2R,4r,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-1-[(2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)carbamoyl]-
2-(4-fluorophenyl)ethyl]carbamate
84)
(βS)-β-(3,5-difluorophenyl)-N-{2-[(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl)methoxy]-3-fluorophenyl}-4-fluoro-L-phenylalaninamide
85)
methyl [(1S,2S)-2-(3,5-difluorophenyl)-1-({2-[(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)methoxy]-3-fluorophenyl}carbamoyl)-2-(4-
fluorophenyl)ethyl]carbamate
86)
(βR)-β-bicyclo[1.1.1]pent-1-yl-N-{2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}-4-fluoro-L-phenylalaninamide
87)
methyl [(1S,2R)-2-bicyclo[1.1.1]pent-l-yl-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-(4-
fluorophenyl)ethyl]carbamate
88)
(βR)-N-(2-{2-[(6R)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)-4-fluoro-β-[(1R)-1-methoxy-2-methylpropyl]-L-phenylalaninamide
89)
(βS)-4-chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-[6-(trifluoromethyl)pyridin-3-yl]-L-phenylalaninamide
90)
methyl [(1S,2R)-1-[(2-{2-[(6R)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)carbamoyl]-2-(4-fluorophenyl)-4-methylpentyl]carbamate
91)
(βR)-4-chloro-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3,6-difluorophenyl)-β-(tetrahydro-2H-pyran-4-yl)-L-phenylalaninamide
92)
methyl [(1S)-1-[bis(4-fluorophenyl)methyl]-2-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-
thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]amino}-2-oxoethyl]carbamate
93)
N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}cyclohexyl]-4-fluoro-β-(4-fluorophenyl)-L-phenylalaninamide
94)
methyl {(1S,2S)-2-(4-chlorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-[6-(1-
methylethoxy)pyridin-3-yl]ethyl}carbamate
95)
(βS)-4-chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-[1-(1-methylethyl)-6-oxo-1,6-dihydropyridin-3-yl]-L-
phenylalaninamide
96)
methyl [(1S,2R)-2-(4-chlorophenyl)-1-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]carbamoyl}-3-methylbutyl]carbamate
97)
methyl {(1S,2S)-2-(4-chloro-3-fluorophenyl)-1-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-
thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]carbamoyl}-2-[5-
(trifluoromethyl)pyridin-3-yl]ethyl}carbamate
98)
methyl [(1S,2S)-2-(4-chlorophenyl)-1-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]carbamoyl}-2-(6-methoxypyridin-3-
yl)ethyl]carbamate
99)
methyl [(1S,2S)-2-(4-chloro-3-fluorophenyl)-1-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-
thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]carbamoyl}-2-(5-fluoropyridin-
3-yl)ethyl]carbamate
100)
methyl [(1S,2S)-2-(4-chlorophenyl)-2-(3,5-difluorophenyl)-1-{[(1S,2R)-2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}cyclohexyl]carbamoyl}ethyl]carbamate
101)
methyl {(1S,2S)-2-(4-chlorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-[1-(1-methylethyl)-6-
oxo-1,6-dihydropyridin-3-yl]ethyl}carbamate
102)
methyl {(1S)-2-[(2-{2-[(6R,9S)-3,3-dimethyl-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)amino]-1-[(R)-[(2R,4r,6S)-2,6-
dimethyltetrahydro-2H-pyran-4-yl](4-fluorophenyl)methyl]-2-oxoethyl}carbamate
103)
methyl {(1S)-2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)amino]-1-[(R)-(4-fluorophenyl)(tetrahydro-2H-pyran-2-
yl)methyl]-2-oxoethyl}carbamate
104)
(βR)-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)-4-fluoro-β-(tetrahydro-2H-pyran-2-yl)-L-phenylalaninamide
105)
methyl [(1S)-2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)amino]-1-{(R)-(4-fluorophenyl)[(1s,3S)-3-
methoxycyclobutyl]methyl}-2-oxoethyl]carbamate
106)
(βR)-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)-4-fluoro-β-[(1s,3S)-3-methoxycyclobutyl]-L-phenylalaninamide
107)
(βR)-β-[(2R,4s,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-N-[(1S,2R)-2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-4-fluoro-L-
phenylalaninamide
108)
methyl [(1S,2R)-2-[(2R,4s,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-1-{[(1S,2R)-2-
{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}cyclopentyl]carbamoyl}-2-(4-fluorophenyl)ethyl]carbamate
109)
methyl [(1S,2R)-2-[(2R,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-1-[(3-fluoro-2-{2-
[(6R,9S)-3-methyl-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}phenyl)carbamoyl]-2-(4-fluorophenyl)ethyl]carbamate
110)
(βR)-β-[(2R,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-4-fluoro-N-(3-fluoro-2-{2-
[(6R,9S)-3-methyl-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}phenyl)-L-
phenylalaninamide
112)
methyl [(1S,2R)-2-[(2R,6R)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-1-[(2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)carbamoyl]-
2-(4-fluorophenyl)ethyl]carbamate
113)
(βR)-β-[(2R,6R)-2,6-dimethyltetrahydro-2H-pyran-4-yl]N-(2-{2-[(6R,9S)-2,2-dioxido-
2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)-4-fluoro-L-
phenylalaninamide
114)
methyl [(1S,2S)-2-(4-chlorophenyl)-2-[5-(1,1-difluoroethyl)pyridin-3-yl]-1-({2-[2-(2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}carbamoyl)ethyl]carbamate
115)
methyl {(1S)-2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)amino]-1-[(R)-(4-fluorophenyl)(tetrahydro-2H-pyran-2-
yl)methyl]-2-oxoethyl}carbamate
116)
methyl [(1S,2S)-2-(4-chlorophenyl)-2-[6-(1,1-difluoroethyl)pyridin-3-yl]-1-({2-[2-(2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}carbamoyl)ethyl]carbamate
117)
methyl [(1S)-2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)amino]-1-{(R)-(4-fluorophenyl)[(1r,4R)-4-
methoxycyclohexyl]methyl}-2-oxoethyl]carbamate
118)
(βR)-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)-4-fluoro-β-[(1r,4R)-4-methoxycyclohexyl]-L-phenylalaninamide
119)
(βR)-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)-4-fluoro-β-(tetrahydro-2H-pyran-2-yl)-L-phenylalaninamide
120)
methyl {(1S,2R)-2-(4-chlorophenyl)-2-[(2R,4r,6S)-2,6-dimethyltetrahydro-2H-pyran-4-
yl]-1-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)carbamoyl]ethyl}carbamate
121)
(βR)-4-chloro-β-[(2R,4r,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-N-(2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)-L-
phenylalaninamide
122)
methyl {(1S,2S)-2-(4-chlorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-[2-(1-
methylethoxy)pyridin-4-yl]ethyl}carbamate
123)
(βS)-4-chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-[2-(trifluoromethyl)pyridin-4-yl]-L-phenylalaninamide
124)
(βR)-4-chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-[2-(1-methylethyl)tetrahydro-2H-pyran-4-yl]-L-phenylalaninamide
125)
methyl {(1S)-1-[cis-1-(4-chlorophenyl)-4-methoxycyclohexyl]-2-[(2-{2-[(6R,9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)amino]-2-
oxoethyl}carbamate
126)
(2S)-2-amino-2-[cis-1-(4-chlorophenyl)-4-methoxycyclohexyl]-N-(2-{2-[(6R,9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)ethanamide
128)
methyl {(1S,2R)-2-(4-chlorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-2-[2-(1-
methylethyl)tetrahydro-2H-pyran-4-yl]ethyl}carbamate
129)
(βR)-4-chloro-β-[(4S)-2,2-dimethyltetrahydro-2H-pyran-4-yl]-N-[(1S,2R)-2-{2-
[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]-L-
phenylalaninamide
131)
methyl [(1S,2R)-2-(4-chlorophenyl)-2-[(4R)-2,2-dimethyltetrahydro-2H-pyran-4-yl]-1-
{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}cyclohexyl]carbamoyl}ethyl]carbamate
132)
(βS)-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)-4-fluoro-β-[2-(trifluoromethyl)pyrimidin-5-yl]-L-phenylalaninamide
137)
benzyl 4-{(1R,2R)-1-(4-chlorophenyl)-3-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-
1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]amino}-2-
[(methoxycarbonyl)amino]-3-oxopropyl}piperidine-1-carboxylate
138)
1-methylcyclopropyl 4-{(1R,2R)-1-(4-chlorophenyl)-3-{[(1S,2R)-2-{2-[(6R,9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]amino}-2-
[(methoxycarbonyl)amino]-3-oxopropyl}piperidine-1-carboxylate
139)
N-(2-{2-[(9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)-4-fluoro-β-(3-fluoropropyl)-β-(methoxymethyl)-L-phenylalaninamide
141)
methyl [(1S)-1-[(2-{2-[(9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-
3-fluorophenyl)carbamoyl]-5-fluoro-2-(4-fluorophenyl)-2-
(methoxymethyl)pentyl]carbamate
143)
(βR)-4-chloro-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3,5-difluorophenyl)-β-(tetrahydro-2H-pyran-4-yl)-L-phenylalaninamide
144)
methyl [(1S,2R)-2-(4-chlorophenyl)-1-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}-3,5-difluorophenyl)carbamoyl]-2-(tetrahydro-2H-
pyran-4-yl)ethyl]carbamate
145)
(βS)-4-chloro-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-
9-yl]ethyl}cyclohexyl]-3-fluoro-β-(5-fluoropyridin-3-yl)-L-phenylalaninamide
146)
(βR)-β-[(2R,4r,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-N-(2-{2-[(6R,9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3,6-difluorophenyl)-4-fluoro-L-
phenylalaninamide
147)
methyl [(1S,2R)-2-[(2R,4r,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-1-[(2-{2-
[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3,6-
difluorophenyl)carbamoyl]-2-(4-fluorophenyl)ethyl]carbamate
148)
(βR)-β-[(4S)-2,2-dimethyltetrahydro-2H-pyran-4-yl]-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]-4-fluoro-L-
phenylalaninamide
149)
(βR)-β-[(2R,4r,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-N-[(1S,2R)-2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]-4-fluoro-L-
phenylalaninamide
150)
(βS)-4-chloro-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-
9-yl]ethyl}6cyclohexyl]-3-fluoro-β-[5-(trifluoromethyl)pyridin-3-yl]-L-
phenylalaninamide
151)
(βR)-4-chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-[2-(tetrahydro-2H-pyran-2-yl)ethyl]-L-phenylalaninamide
153)
methyl [(1S,2R)-2-(4-chlorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}carbamoyl)-4-(tetrahydro-2H-
pyran-2-yl)butyl]carbamate
155)
(βS)-4-chloro-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-
9-yl]ethyl}cyclohexyl]-β-(6-methoxypyridin-3-yl)-L-phenylalaninamide
156)
(βR)-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}cyclohexyl]-4-fluoro-β-(tetrahydro-2H-pyran-4-yl)-L-phenylalaninamide
157)
(βR)-4-chloro-β-(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)-N-[(1S,2R)-2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-L-
phenylalaninamide
158)
(βR)-4-chloro-β-(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)-N-(2-{2-[(9S)-2,2-dioxido-
2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)-L-phenylalaninamide
159)
methyl {(1S,2R)-2-(4-chlorophenyl)-2-(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)-1-
[(2-{2-[(9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)carbamoyl]ethyl}carbamate
160)
(βS)-β-(4-chlorophenyl)-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]-3,5-difluoro-L-phenylalaninamide
161)
(βR)-4-chloro-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]-β-(1-methylethyl)-L-phenylalaninamide
162)
(βR)-4-chloro-β-[(2R,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-N-[(1S,2R)-2-{2-
[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]-L-
phenylalaninamide
163)
(βR)-4-chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-β-[2-(2,2,2-trifluoroethyl)tetrahydro-2H-pyran-4-yl]-L-
phenylalaninamide
165)
(βR)-4-chloro-β-[(2R,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-N-(2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)-3-fluoro-L-
phenylalaninamide
166)
(βR)-β-[(2R,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-N-(2-{2-[(6R,9S)-2,2-dioxido-
2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3,4-difluorophenyl)-4-fluoro-L-
phenylalaninamide
167)
methyl {(1S)-1-[(2R,4r,6S)-4-(4-chlorophenyl)-2,6-dimethyltetrahydro-2H-pyran-4-
yl]-2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)amino]-2-oxoethyl}carbamate
168)
(2S)-2-amino-2-[(2R,4r,6S)-4-(4-chlorophenyl)-2,6-dimethyltetrahydro-2H-pyran-4-
yl]-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)ethanamide
169)
methyl [(1S)-1-[(2R,4r,6S)-4-(4-chlorophenyl)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-
2-{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}cyclohexyl]amino}-2-oxoethyl]carbamate
170)
(2S)-2-amino-2-[(2R,4r,6S)-4-(4-chlorophenyl)-2,6-dimethyltetrahydro-2H-pyran-4-
yl]-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}cyclohexyl]ethanamide
171)
(2S)-2-amino-2-[trans-1-(4-chlorophenyl)-4-methoxycyclohexyl]-N-(2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)ethanamide
172)
methyl {(1S,2R)-2-(4-chlorophenyl)-1-({2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl]-3-fluorophenyl}carbamoyl)-2-[2-(2,2,2-
trifluoroethyl)tetrahydro-2H-pyran-4-yl]ethyl}carbamate
173)
(βR)-4-chloro-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-5-fluoropyridin-3-yl)-β-(tetrahydro-2H-pyran-4-yl)-L-phenylalaninamide
174)
methyl [(1S,2R)-2-(4-chlorophenyl)-1-[(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}-5-fluoropyridin-3-yl)carbamoyl]-2-(tetrahydro-2H-
pyran-4-yl)ethyl]carbamate
177)
(βR)-4-chloro-β-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-N-[(1S,2R)-2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-Nα-propyl-L-
phenylalaninamide
178)
methyl {(1S)-2-[(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-5-fluoropyridin-3-yl)amino]-1-[(R)-(4-fluorophenyl)(tetrahydro-2H-pyran-4-
yl)methyl]-2-oxoethyl}carbamate
179)
(βR)-β-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-
1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3,4-difluorophenyl)-4-fluoro-L-
phenylalaninamide
180)
(βR)-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3,4-
difluorophenyl)-4-fluoro-β-[(1r,4R)-4-methoxycyclohexyl]-L-phenylalaninamide
182)
(βR)-4-chloro-β-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-N-[(1S,2R)-2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-Nα-(2-
methoxyethyl)-L-phenylalaninamide
183)
(βR)-4-chloro-β-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-N-[(1S,2R)-2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-Nα-[(1S)-1-
methylpropyl]-L-phenylalaninamide
184)
(βR)-4-chloro-β-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-N-[(1S,2R)-2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-Nα-(4,4,4-
trifluorobutyl)-L-phenylalaninamide
185)
(2S)-2-amino-2-[4-(4-chlorophenyl)piperidin-4-yl]-N-(2-{2-[(6R,9S)-2,2-dioxido-2-
thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)ethanamide
187)
methyl {(1S,2R)-2-(4-chlorophenyl)-1-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)carbamoyl]-2-[(1r,4R)-4-
methoxycyclohexyl]ethyl}carbamate
188)
(βR)-β-[(2R,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-N-(2-{2-[(6R,9S)-2,2-dioxido-
2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-5-fluorophenyl)-4-fluoro-L-
phenylalaninamide
189)
(βR)-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}cyclohexyl]-4-fluoro-β-[(1r,4R)-4-methoxycyclohexyl]-L-phenylalaninamide
190)
methyl {(1S)-2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)amino-[(R)-[(2S,4S)-2-ethyltetrahydro-2H-pyran-4-yl](4-
fluorophenyl)methyl]-2-oxoethyl}carbamate
191)
(βR)-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)-β-[(2S,4S)-2-ethyltetrahydro-2H-pyran-4-yl]-4-fluoro-L-
phenylalaninamide
194)
(βR)-4-chloro-β-[(4S)-2,2-dimethyltetrahydro-2H-pyran-4-yl]-N-(2-{2-[(6R,9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3,6-difluorophenyl)-L-
phenylalaninamide
195)
(βR)-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-5-
fluoropyridin-3-yl)-4-fluoro-β-(tetrahydro-2H-pyran-4-yl)-L-phenylalaninamide
196)
(βR)-4-chloro-β-[(2R,4s,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-N-[(1S,2R)-2-{2-
[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-L-
phenylalaninamide
197)
(βR)-4-chloro-N-(2-{2-[(9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-β-(3-methoxycyclohexyl)-L-phenylalaninamide
200)
methyl {(1S,2R)-2-(4-chlorophenyl)-2-[(4S)-2,2-dimethyltetrahydro-2H-pyran-4-yl]-1-
[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3,6-
difluorophenyl)carbamoy]ethyl}carbamate
201)
methyl [(1S)-2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)amino]-1-{(R)-(4-fluorophenyl)[(1r,4R)-4-
hydroxycyclohexyl]methyl}-2-oxoethyl]carbamate
202)
(βR)-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)-4-fluoro-β-[(1r,4R)-4-hydroxycyclohexyl]-L-phenylalaninamide
203)
methyl [(1S,2R)-2-[(2R,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-1-{[2-{2-[6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
(trifluoromethyl)phenyl]carbamoyl}-2-(4-fluorophenyl)ethyl]carbamate
204)
(βR)-β-[(2R,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-N-[2-{2-[(6R,9S)-2,2-dioxido-
2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-(trifluoromethyl)phenyl]-4-fluoro-L-
phenylalaninamide
205)
(2S)-2-amino-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-2-[trans-1-(4-fluorophenyl)-4-
methoxycyclohexyl]ethanamide
206)
methyl [(1S)-2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)amino]-1-{(S)-(4-fluorophenyl)[2-(1-
methylethoxy)pyrimidin-5-yl]methyl}-2-oxoethyl]carbamate
207)
(βR)-4-chloro-N-[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclohexyl]-β-[(1r,4R)-4-methoxycyclohexyl]-L-
phenylalaninamide
208)
1-methylcyclopropyl 4-[(1R,2S)-2-amino-1-(4-chlorophenyl)-3-{[(1S,2R)-2-{2-
[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]amino}-
3-oxopropyl]piperidine-1-carboxylate
209)
N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)-4-fluoro-β-[5-(trifluoromethyl)pyridin-2-yl]phenylalaninamide
210)
methyl {(1S)-2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)amino]-1-[trans-1-(4-fluorophenyl)-4-methoxycyclohexyl]-2-
oxoethyl}carbamate
211)
methyl {(1S)-2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)amino]-1-[(R)-[(1r,4R)-4-ethoxycyclohexyl](4-
fluorophenyl)methyl]-2-oxoethyl}carbamate
212)
(βR)-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)-β-[(1r,4R)-4-ethoxycyclohexyl]-4-fluoro-L-phenylalaninamide
215)
(βR)-4-chloro-β-[(4S)-2,2-dimethyltetrahydro-2H-pyran-4-yl]-N-(4-{2-[(6R,9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-5-fluoropyridin-3-yl)-L-
phenylalaninamide
216)
methyl (2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)amino]-1-{(4-fluorophenyl)[5-(trifluoromethyl)pyridin-2-yl]methyl}-2-
oxoethyl)carbamate
217)
(βR)-4-chloro-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-β-[(1r,4R)-4-hydroxycyclohexyl]-L-phenylalaninamide
224)
Methyl [(1S)-2-({2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl]-3-
fluorophenyl}amino)-1-{(R)-(4-fluorophenyl)[4-(trifluoromethyl)phenyl]methyl}-2-
oxoethyl]carbamate
225)
(2S,3S)-2-Amino-3-(2,3-dihydro-1H-inden-5-yl)-N-{2-[2-(2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-fluorophenyl}-3-(4-fluorophenyl)propanamide
227)
(βS)-4-Chloro-N-{2-[2-(2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl)ethyl]-3-
fluorophenyl}-3-fluoro-β-[5-(trifluoromethyl)pyridin-3-yl]-L-phenylalaninamide
228)
Methyl [(1S,2R)-2-[(2R,6S)-2,6-dimethyltetrahydro-2H-pyran-4-yl]-1-[(2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3,4-
difluorophenyl)carbamoyl]-2-(4-fluorophenyl)ethyl]carbamate
229)
methyl 4-{[(1S,2R)-2-(4-chlorophenyl)-2-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-1-
{[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}cyclopentyl]carbamoyl}ethyl]amino}butanoate
230)
(βR)-Nα-[2-(benzyloxy)ethyl]-4-chloro-β-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-N-
[(1S,2R)-2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}cyclopentyl]-L-phenylalaninamide
231)
(βR)-4-chloro-β-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-N-[(1S,2R)-2-{2-[(6R,9S)-
2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-Nα-(2-
hydroxyethyl)-L-phenylalaninamide
232)
glycyl-(βR)-4-chloro-β-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-N-[(1S,2R)-2-{2-
[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-L-
phenylalaninamide
233)
(2S)-2-amino-2-[4-(4-chlorophenyl)tetrahydro-2H-pyran-4-yl]-N-(4-{2-[(6R,9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-5-fluoropyridin-3-yl)ethanamide
234)
(βS)-4-chloro-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-5-fluoropyridin-3-yl)-3-fluoro-β-(5-fluoropyridin-3-yl)-L-phenylalaninamide
235)
(2S)-2-amino-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-5-fluoropyridin-3-yl)-2-[trans-1-(4-fluorophenyl)-4-
methoxycyclohexyl]ethanamide
236)
(βS)-β-(4-chlorophenyl)-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}-5-fluoropyridin-3-yl)-3,5-difluoro-L-
phenylalaninamide
237)
2-methylalanyl-(βR)-4-chloro-β-(2,2-dimethyltetrahydro-2H-pyran-4-yl)-N-[(1S,2R)-2-
{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}cyclopentyl]-L-
phenylalaninamide
238)
(2S,3R)-2-amino-3-(4-chlorophenyl)-N-(4-(2-((6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]decan-9-yl)ethyl)-5-fluoropyridin-3-yl)-4-methylpentanamide
239)
(2S,3R)-2-amino-3-(4-chlorophenyl)-N-(4-(2-((6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]decan-9-yl)ethyl)-5-fluoropyridin-3-yl)-3-((1r,4R)-4-
methoxycyclohexyl)propanamide
240)
(2S,3S)-2-amino-3-(4-chlorophenyl)-N-(4-(2-((6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]decan-9-yl)ethyl)-5-fluoropyridin-3-yl)-3-(6-isopropoxypyridin-3-
yl)propanamide
241)
(2S,3R)-2-amino-3-(4-chlorophenyl)-3-(4,4-difluorocyclohexyl)-N-(4-(24(6R,9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]decan-9-yl)ethyl)-5-fluoropyridin-3-
yl)propanamide
242)
(2S,3R)-2-amino-3-(4-chlorophenyl)-N-(4-(2-((6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]decan-9-yl)ethyl)-5-fluoropyridin-3-yl)-4-ethylhexanamide
243)
(2S,3R)-2-amino-3-(4-chloro-3-fluorophenyl)-3-((S)-2,2-dimethyltetrahydro-2H-pyran-
4-yl)-N-(4-(2-((6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]decan-9-yl)ethyl)-5-
fluoropyridin-3-yl)propanamide
244)
(2S,3R)-2-amino-3-(4-chloro-3-fluorophenyl)-3-cyclohexyl-N-(4-(2-((6R,9S)-2,2-
dioxido-2-thia-1,7-diazabicyclo[4.3.1]decan-9-yl)ethyl)-5-fluoropyridin-3-
yl)propanamide
245)
(2S,3R)-2-amino-3-(4-chloro-3-fluorophenyl)-3-((2R,6S)-2,6-dimethyltetrahydro-2H-
pyran-4-yl)-N-(4-(2-((6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]decan-9-
yl)ethyl)-5-fluoropyridin-3-yl)propanamide
246)
(2S,3S)-2-amino-3-(4-chlorophenyl)-3-(6-(1,1-difluoroethyl)pyridin-3-yl)-N-(4-(2-
((6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]decan-9-yl)ethyl)-5-fluoropyridin-
3-yl)propanamide
247)
(βS)-4-chloro-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-β-[2-(1-methylethoxy)pyrimidin-5-yl]-L-phenylalaninamide
248)
(βR)-4-chloro-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-β-[(1r,4R)-4-ethoxycyclohexyl]-3-fluoro-L-
phenylalaninamide
249)
(βS)-4-chloro-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-3-fluoro-β-[2-(trifluoromethyl)pyrimidin-5-yl]-L-
phenylalaninamide
250)
(βR)-4-chloro-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-5-fluoropyridin-3-yl)-β-[(1r,4R)-4-(1-methylethoxy)cyclohexyl]-L-
phenylalaninamide
251)
(βR)-4-chloro-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-β-[2-(trifluoromethyl)-1,3-thiazol-4-yl]-L-
phenylalaninamide
252)
methyl {(1S,2R)-2-(4-chlorophenyl)-1-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]lethyl}-3-fluorophenyl)carbamoyl]-2-[2-(trifluoromethyl)-
1,3-thiazol-4-yl]ethyl}carbamate
253)
(βR)-4-chloro-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-5-fluoropyridin-3-yl)-β-[(1r,4R)-4-ethoxycyclohexyl]-3-fluoro-L-
phenylalaninamide
254)
(βR)-4-chloro-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-5-fluoropyridin-3-yl)-β-[(1r,4R)-4-(methoxymethyl)cyclohexyl]-L-
phenylalaninamide
255)
ethyl 4-(4-chlorophenyl)-4-{(1S)-2-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)amino]-1-
[(methoxycarbonyl)amino]-2-oxoethyl}piperidine-1-carboxylate
256)
methyl {(1S,2R)-2-(4-chlorophenyl)-1-[(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}-5-fluoropyridin-3-yl)carbamoyl]-2-[(1r,4R)-4-
(trifluoromethyl)cyclohexyl]ethyl}carbamate
257)
methyl {(1S,2R)-2-(4-chlorophenyl)-2-[(1r,4R)-4-(cyclopropyloxy)cyclohexyl]-1-[(2-
{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)carbamoyflethyl}carbamate
258)
(βR)-4-chloro-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-5-fluoropyridin-3-yl)-β-[(1r,4R)-4-(ethoxymethyl)cyclohexyl]-L-
phenylalaninamide
259)
(βR)-4-chloro-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-β-[5-(1-methylethoxy)pyrazin-2-yl]-L-phenylalaninamide
260)
(βR)-4-chloro-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-β-[1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl]-L-
phenylalaninamide
261)
(βR)-4-chloro-N-(2-{2-+(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-β-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl]-L-
phenylalaninamide
262)
(βR)-4-chloro-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-5-fluoropyridin-3-yl)-β-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl]-L-
phenylalaninamide
263)
(βR)-4-chloro-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-5-fluoropyridin-3-yl)-β-[5-(1-methylethoxy)pyrazin-2-yl]-L-
phenylalaninamide
264)
(βR)-4-chloro-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-β-[4-(trifluoromethyl)-1,3-thiazol-2-yl]-L-
phenylalaninamide
265)
(βR)-4-chloro-N-(2{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-3-fluoro-β-[1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl]-
L-phenylalaninamide
266)
(βR)-4-chloro-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-5-fluoropyridin-3-yl)-3-fluoro-β-[1-methyl-5-(trifluoromethyl)-1H-pyrazol-
3-yl]-L-phenylalaninamide
267)
(βR)-4-chloro-N-(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-3-fluorophenyl)-3-fluoro-β-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl]-
L-phenylalaninamide
268)
(βR)-4-chloro-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-5-fluoropyridin-3-yl)-3-fluoro-β-[1-methyl-3-(trifluoromethyl)-1H-pyrazol-
5-yl]-L-phenylalaninamide
269)
(βR)-4-chloro-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-
yl]ethyl}-5-fluoropyridin-3-yl)-β-[2-(trifluoromethyl)-1,3-thiazol-4-yl]-L-
phenylalaninamide
270)
methyl {(1S)-1-[cis-1-(4-chlorophenyl)-4-(trifluoromethyl)cyclohexyl]-2-[(4-{2-
[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-5-fluoropyridin-3-
yl)amino]-2-oxoethyl}carbamate
271)
methyl {(1S,2R)-2-(4-chlorophenyl)-2-(6,6-dimethyltetrahydro-2H-pyran-3-yl)-1-[(2-
{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-
fluorophenyl)carbamoyl]ethyl}carbamate
272)
(βR)-4-chloro-β-(3,3-difluorocyclohexyl)-N-(4-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}-5-fluoropyridin-3-yl)-L-phenylalaninamide, or
273)
methyl {(1S,2R)-2-(4-chlorophenyl)-1-[(2-{2-[(6R,9S)-2,2-dioxido-2-thia-1,7-
diazabicyclo[4.3.1]dec-9-yl]ethyl}-3-fluorophenyl)carbamoyl]-2-[6-
(trifluoromethyl)tetrahydro-2H-pyran-3-yl]ethyl}carbamate;
or a pharmaceutically acceptable salt thereof.
18. A pharmaceutical composition comprising an effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
19. A method for the treatment of infection by HIV or for the treatment or delay in the onset of AIDS in a subject in need thereof, which comprises administering to the subject an effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.