Aryl dihydro-2H-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease
View Patent ↗The invention provides aryl dihydro-2H-benzo[b] [1,4]oxazine sulfonamide and related compounds, pharmaceutical compositions, methods of promoting RORy activity, methods of increasing the amount of IL-17 in a subject, and methods of treating cancer and other medical disorders using such compounds.
1. A compound represented by Formula I:
or a pharmaceutically acceptable salt thereof; wherein:
A 1 is phenylene, 5-6 membered heteroarylene, or 3-6 membered heterocycloalkylene;
X is phenyl or 5-10 membered heteroaryl, each of which is optionally substituted by 1, 2, 3, or 4 substituents independently selected from the group consisting of C 1-6 alkyl, C 3-6 cycloalkyl, halogen, C 1-6 haloalkyl, hydroxyl, C 1-6 alkoxy, C 1-6 haloalkoxy, —O—C 3-6 cycloalkyl, —O—(C 1-6 alkylene)-OH, cyano, —N(R 4 )(R 5 ), —S(O) 2 —R 6 , acetyl, and C 6-10 aryl;
R 1 represents independently for each occurrence halogen, C 1-6 alkyl, C 1-6 haloalkyl, or C 3-6 cycloalkyl;
R 2A is one of the following:
(i) —(C 1-6 alkylene)-A 2 , —(C 3-6 cycloalkylene)-A 2 , -(2-6 membered heteroalkylene)-A 2 , —(C 1-3 alkylene)-(C 3-6 cycloalkylene)-(C 0-3 alkylene)-A 2 , —(C 1-3 alkylene)-(3-6 membered heterocycloalkylene)-(C 0-3 alkylene)-A 2 , C 2-6 hydroxyalkyl, or —CO 2 R 4 ;
where
A 2 is —CO 2 R 4 , —C(O)-A 3 , —C(O)R 6 , —C(O)N(R 4 )(R 5 ), —C(O)N(R 4 )—(C 1-4 alkylene)-CO 2 R 4 , —C(O)N(R 4 )SO 2 R 4 , —C(O)N(R 4 )SO 2 A 3 , —C(O)N(R 4 )—(C 1-6 alkylene)-N(R 7 )C(O)R 6 , —C(O)N(R 4 )—(C 1-6 alkylene)-SO 2 N(R 7 ) 2 , —C(O)N(R 4 )—(C 1-6 alkylene)-CN, —C(O)N(R 4 )—(C 1-6 alkylene)-OC(O)R 6 , —N(R 4 )C(O)R 7 , —N(R 4 )C(O)A 3 , —N(R 4 )C(O)—(C 1-6 alkylene)-CO 2 R 4 , —N(R 4 )C(O)—(C 1-6 alkylene)-N(R 7 )C(O)R 6 , —N(R 4 )C(O)—(C 1-6 alkylene)-SO 2 N(R 7 ) 2 , —N(R 4 )C(O)—(C 1-6 alkylene)-CN, —N(R 4 )C(O)—(C 1-6 alkylene)-OC(O)R 6 , —N(R 4 )C(O)N(R 4 )—(C 1-6 alkylene)-CO 2 R 4 , —N(R 4 )C(O)N(R 7 ) 2 , —N(R 4 )CO 2 R 6 , —N(R 4 )S(O) 2 R 7 , —N(R 4 )S(O) 2 N(R 4 )(R 5 ), —N(R 4 )(R 5 ), hydroxyl, or -A 3 ;
A 3 is aryl, C 3-6 cycloalkyl, or a 5-8 membered heterocyclic group, each of which is optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of C 1-6 alkyl, C 1-6 haloalkyl, C 3-6 cycloalkyl, halogen, C 1-6 alkoxy, C 1-6 haloalkoxy, oxo, —C(O)R 6 , —CO 2 R 7 , —N(R 4 )C(O)(R 6 ), and —N(R 4 )(R 5 ); and
any alkylene, cycloalkylene, or heteroalkylene within the definition of R 2A is optionally substituted by 1, 2, or 3 substitutents independently selected from the group consisting of hydroxyl and C 1-6 alkoxy; or
(ii) —OH, —N(R 4 )C(O)R 6 , —N(R 4 )CO 2 R 6 , or —N(R 4 )C(O)N(R 7 ) 2 ;
R 2B represents independently for each occurrence C 1-6 alkyl or C 1-3 haloalkyl;
R 3 represents independently for each occurrence hydrogen, C 1-6 haloalkyl, halogen, hydroxyl, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkoxy, C 1-6 haloalkoxy, —O—(C 1-6 alkylene)-OH, or —O—(C 1-6 alkylene)-CO 2 R 4 ; or two vicinal occurrences of R 3 are taken together with intervening atoms to form a 4-6 membered ring optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of C 1-6 alkyl, C 1-6 haloalkyl, C 3-6 cycloalkyl, halogen, C 1-6 alkoxy, C 1-6 haloalkoxy, —C(O)R 6 , and —CO 2 R 7 ;
R 4 and R 5 each represent independently for each occurrence hydrogen, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxylalkyl, or C 3-6 cycloalkyl; or an occurrence of R 4 and R 5 attached to the same nitrogen atom are taken together with the nitrogen atom to which they are attached to form a 3-7 membered heterocyclic ring;
R 6 represents independently for each occurrence C 1-6 alkyl, C 3-6 cycloalkyl, or aralkyl;
R 7 represents independently for each occurrence hydrogen, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 haloalkyl, C 1-6 hydroxyhaloalkyl, C 3-6 cycloalkyl, C 3-6 hydroxycycloalkyl, —(C 1-6 alkylene)-(C 3-6 cycloalkyl), —(C 1-6 alkylene)-(C 2-4 alkenyl), or aralkyl;
R 8 and R 9 each represent independently for each occurrence hydrogen, halogen, or C 1-6 alkyl, or R 8 and R 9 are taken together with the carbon atom to which they are attached to form a 3-6 membered carbocyclic ring; or R 8 and R 2B may taken together to form a bond when R 2B is attached to the same carbon atom as R 2A ;
Y is —O—, —C(O)—, —S(O) p —, or —C(R 8 )(R 9 )—;
m and p each represent independently for each occurrence 0, 1, or 2; and
n is 1, 2, or 3.
2. The compound of claim 1 , wherein the compound is represented by Formula I-A:
or a pharmaceutically acceptable salt thereof; wherein:
A 1 is phenylene or a 5-6 membered heteroarylene;
X is phenyl or 5-6 membered heteroaryl, each of which is optionally substituted by 1, 2, or 3 substituents independently selected from the group consisting of C 1-6 alkyl, C 3-6 cycloalkyl, halogen, C 1-6 haloalkyl, hydroxyl, C 1-6 alkoxy, C 1-6 haloalkoxy, —O—C 3-6 cycloalkyl, —O—(C 1-6 alkylene)-OH, cyano, —N(R 4 )(R 5 ), and C 6-10 aryl;
R 1 represents independently for each occurrence halogen, C 1-6 alkyl, or C 1-6 haloalkyl;
R 2A is —(C 1-6 alkylene)-A 2 , —(C 3-6 cycloalkylene)-A 2 , -(2-6 membered heteroalkylene)-A 2 , or —CO 2 R 4 ; wherein A 2 is —CO 2 R 4 , —C(O)-A 3 , —C(O)N(R 4 )(R 5 ), —C(O)N(R 4 )—(C 1-4 alkylene)-CO 2 R 4 , —N(R 4 )C(O)R 7 , —N(R 4 )C(O)A 3 , —N(R 4 )C(O)—(C 1-6 alkylene)-CO 2 R 4 , —N(R 4 )C(O)N(R 4 )—(C 1-6 alkylene)-CO 2 R 4 , —N(R 4 )CO 2 R 6 , or A 3 ; and A 3 is a 5-8 membered heterocyclic group optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of C 1-6 alkyl, C 1-6 haloalkyl, C 3-6 cycloalkyl, halogen, C 1-6 alkoxy, C 1-6 haloalkoxy, oxo, —C(O)R 6 , and —CO 2 R 7 ;
R 2B represents independently for each occurrence C 1-6 alkyl or C 1-3 haloalkyl;
R 3 represents independently for each occurrence hydrogen, C 1-6 haloalkyl, halogen, hydroxyl, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkoxy, C 1-6 haloalkoxy, —O—(C 1-6 alkylene)-OH, or —O—(C 1-6 alkylene)-CO 2 R 4 ;
R 4 and R 5 each represent independently for each occurrence hydrogen, C 1-6 alkyl, or C 3-6 cycloalkyl; or an occurrence of R 4 and R 5 attached to the same nitrogen atom are taken together with the nitrogen atom to which they are attached to form a 3-7 membered heterocyclic ring;
R 6 represents independently for each occurrence C 1-6 alkyl, C 3-6 cycloalkyl, or aralkyl;
R 7 represents independently for each occurrence hydrogen, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 3-6 cycloalkyl, C 3-6 hydroxycycloalkyl, or aralkyl;
m and p are independently 0, 1, or 2; and
n is 1, 2, or 3.
3. The compound of claim 2 , wherein the compound is represented by Formula I-A.
4. The compound of claim 2 , wherein A 1 is phenylene.
5. The compound of claim 4 , wherein n is 1.
6. The compound of claim 2 , wherein A 1 is
7. The compound of claim 5 , wherein m is 0.
8. The compound of claim 7 , wherein R 2A is —(C 1-6 alkylene)-A 2 .
9. The compound of claim 8 , wherein A 2 is —CO 2 R 4 .
10. The compound of claim 8 , wherein A 2 is —CO 2 H.
11. The compound of claim 8 , wherein A 2 is A 3 .
12. The compound of claim 11 , wherein A 3 is a 5-6 membered saturated heterocyclic group optionally substituted by 1 or 2 substituents independently selected from the group consisting of methyl, ethyl, isopropyl, trifluoromethyl, cyclopropyl, C 1-6 alkoxy, oxo, and —CO 2 R 7 .
13. The compound of claim 10 , wherein R 3 is trifluoromethyl, fluoro, chloro, or methoxy.
14. The compound of claim 10 , wherein R 3 is trifluoromethyl.
15. The compound of claim 14 , wherein p is 0.
16. The compound of claim 8 , wherein X is phenyl substituted by 1, 2, or 3 substituents independently selected from the group consisting of C 1-6 alkyl, C 3-6 cycloalkyl, halogen, C 1-6 haloalkyl, hydroxyl, C 1-6 alkoxy, C 1-6 haloalkoxy, —O—C 3-6 cycloalkyl, and —O—(C 1-6 alkylene)-OH.
17. The compound of claim 14 , wherein X is phenyl substituted by 1, 2, or 3 substituents independently selected from the group consisting of C 1-6 alkyl, cyclopropyl, halogen, C 1-3 haloalkyl, hydroxyl, C 1-3 alkoxy, and C 1-3 haloalkoxy.
18. The compound of claim 1 , wherein the compound is represented by Formula I-B:
or a pharmaceutically acceptable salt thereof; wherein:
X is phenyl or 2-pyridinyl, each of which is substituted by 1, 2, or 3 substituents independently selected from the group consisting of chloro, fluoro, C 1-2 fluoroalkyl, C 1-2 alkoxy, and C 1-2 fluoroalkoxy;
R 2A is —(C 1-6 alkylene)-CO 2 H or —(C 1-6 alkylene)-N(R 4 )C(O)R 7 ;
R 3 represents independently for each occurrence C 1-2 fluoroalkyl, chloro, fluoro, cyclopropyl, C 1-3 alkyl, C 1-2 alkoxy, or C 1-2 fluoroalkoxy;
R 4 is hydrogen or C 1-6 alkyl;
R 7 is C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 haloalkyl, C 1-6 hydroxyhaloalkyl, C 3-6 cycloalkyl, or C 3-6 hydroxycycloalkyl; and
n is 1 or 2.
19. The compound of claim 18 , wherein X is phenyl substituted by 1, 2, or 3 substituents independently selected from the group consisting of chloro, fluoro, C 1-2 fluoroalkyl, C 1-2 alkoxy, and C 1-2 fluoroalkoxy, where at least 1 substituent is located at a meta-position on the phenyl group.
20. The compound of claim 19 , wherein R 2A is —(CH 2 ) 2 —CO 2 H or —CH 2 C(CH 3 ) 2 —CO 2 H.
21. The compound of claim 20 , wherein R 3 is —CF 3 , which is attached at a meta-position on the phenyl group.
22. The compound of claim 21 , wherein n is 1.
23. The compound of claim 1 , wherein the compound is one of the following or a pharmaceutically acceptable salt thereof:
24. The compound of claim 1 , wherein the compound is
or a pharmaceutically acceptable salt thereof.
25. The compound of claim 1 , wherein the compound is
26. The compound of claim 1 , wherein the compound is
or a pharmaceutically acceptable salt thereof.
27. The compound of claim 1 , wherein the compound is
28. A compound represented by Formula II:
or a pharmaceutically acceptable salt thereof; wherein:
A 1 is phenylene, 5-6 membered heteroarylene, or 3-6 membered heterocycloalkylene;
X is phenyl or 5-10 membered heteroaryl, each of which is optionally substituted by 1, 2, 3, or 4 substituents independently selected from the group consisting of C 1-6 alkyl, C 3-6 cycloalkyl, halogen, C 1-6 haloalkyl, hydroxyl, C 1-6 alkoxy, C 1-6 haloalkoxy, —O—C 3-6 cycloalkyl, —O—(C 1-6 alkylene)-OH, cyano, —N(R 4 )(R 5 ), —S(O) 2 —R 6 , acetyl, and C 6-10 aryl;
R 1 represents independently for each occurrence halogen, C 1-6 alkyl, C 1-6 haloalkyl, or C 3-6 cycloalkyl;
R 2A is —(C 1-3 alkylene)-(C 3-6 cycloalkenylene)-(C 0-3 alkylene)-A 2 , —(C 1-3 alkylene)-(C 3-6 cycloalkylene substituted by hydroxyl and C 1-4 hydroxyalkyl)-(C 0-3 alkylene)-A 2 , —(C 1-3 alkylene)-(3-6 membered carbocyclylene substituted by)═C(R 10 ) 2 )—(C 0-3 alkylene)-A 2 , or hydroxyl, wherein the cycloalkenylene, cycloalkylene, and carbocyclylene are optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of C 1-6 alkyl, C 1-6 haloalkyl, C 3-6 cycloalkyl, halogen, C 1-6 alkoxy, C 1-6 haloalkoxy, oxo, —C(O)R 6 , —CO 2 R 7 , —N(R 4 )C(O)(R 6 ), and —N(R 4 )(R 5 ); and A 2 is —CO 2 R 4 , —C(O)R 6 , —C(O)N(R 4 )(R 5 ), —C(O)N(R 4 )—(C 1-4 alkylene)-CO 2 R 4 , or —C(O)N(R 4 )SO 2 R 4 ; and
R 2B represents independently for each occurrence C 1-6 alkyl or C 1-3 haloalkyl;
R 3 represents independently for each occurrence hydrogen, C 1-6 haloalkyl, halogen, hydroxyl, C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkoxy, C 1-6 haloalkoxy, —O—(C 1-6 alkylene)-OH, or —O—(C 1-6 alkylene)-CO 2 R 4 ; or two vicinal occurrences of R 3 are taken together with intervening atoms to form a 4-6 membered ring optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of C 1-6 alkyl, C 1-6 haloalkyl, C 3-6 cycloalkyl, halogen, C 1-6 alkoxy, C 1-6 haloalkoxy, —C(O)R 6 , and —CO 2 R 7 ;
R 4 and R 5 each represent independently for each occurrence hydrogen, C 1-6 alkyl, C 1-6 haloalkyl, C 1-6 hydroxylalkyl, or C 3-6 cycloalkyl; or an occurrence of R 4 and R 5 attached to the same nitrogen atom are taken together with the nitrogen atom to which they are attached to form a 3-7 membered heterocyclic ring;
R 6 represents independently for each occurrence C 1-6 alkyl, C 3-6 cycloalkyl, or aralkyl;
R 7 represents independently for each occurrence hydrogen, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 haloalkyl, C 1-6 hydroxyhaloalkyl, C 3-6 cycloalkyl, C 3-6 hydroxycycloalkyl, —(C 1-6 alkylene)-(C 3-6 cycloalkyl), —(C 1-6 alkylene)-(C 2-4 alkenyl), or aralkyl;
R 8 and R 9 each represent independently for each occurrence hydrogen, halogen, or C 1-6 alkyl, or R 8 and R 9 are taken together with the carbon atom to which they are attached to form a 3-6 membered carbocyclic ring; or R 8 and R 2B may taken together to form a bond when R 2B is attached to the same carbon atom as R 2A ;
R 10 represents independently for each occurrence hydrogen or C 1-6 alkyl; or two occurrences of R 10 bound to the same carbon atom are taken together with the carbon atom to which they are bound to form a 3-6 membered carbocycle;
Y is —O—, —C(O)—, —S(O) p —, or —C(R 8 )(R 9 )—;
m and p each represent independently for each occurrence 0, 1, or 2; and
n is 1, 2, or 3.
29. A compound in any one of Tables 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, or 23-I below or a pharmaceutically acceptable salt thereof:
TABLE 1
No.
X
Z
I-1
I-2
I-3
I-4
I-5
I-6
I-7
I-8
I-9
I-10
I-11
I-12
I-13
I-14
I-15
I-16
I-17
I-18
I-19
I-20
I-21
I-22
I-23
I-24
I-25
I-26
I-27
I-28
I-29
I-30
I-31
I-32
I-33
I-34
I-35
I-36
I-37
I-38
I-39
I-40
I-41
I-42
I-43
I-44
I-45
I-46
I-47
I-48
I-49
I-50
I-51
I-52
I-53
I-54
I-55
I-56
I-57
I-58
I-59
I-60
TABLE 2
Compd
No.
Structure
Name
2A
(S)-3-(6-(2-chlorophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2B
(S)-3-(6-(4-chlorophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2C
(S)-3-(6-(5-chloro-2- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2D
(S)-3-(6-(2,4-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2E
(S)-3-(6-(3,4-dichlorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2F
(S)-3-(6-(3,4-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2G
(S)-3-(6-(3- (trifluoromethyl)phenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2H
(S)-3-(6-(3,5-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2I
(S)-3-(6-(3-chloro-5- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
2J
(S)-3-(6-(3-chloro-4- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2K
(S)-3-(6-(3-methoxyphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2L
(S)-3-(6-(3,5-dichlorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2M
(S)-3-(6-(3-chlorophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2N
(S)-3-(6-(2-fluoro-3- (trifluoromethyl)phenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2O
(S)-3-(6-(2-fluoro-5- (trifluoromethyl)phenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2P
(S)-3-(6-(o-tolyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2Q
(S)-3-(6-(m-tolyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2R
(S)-3-(6-(3-chloro-2- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2S
(S)-3-(6-(5-chloro-2- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2T
(S)-3-(6-(2-methoxyphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2U
(S)-3-(6-(4-methoxyphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2V
(S)-3-(6-(5-methoxypyridin-3-yl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2W
(S)-3-(6-(2-chloro-4- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2X
(S)-3-(6-(p-tolyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2Y
(S)-3-(6-(3-isopropylphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2Z
(S)-3-(6-(4-isopropylphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AA
(S)-3-(4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(2- (trifluoromethyl)pyridin-4-yl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AB
(S)-3-(6-(2,4-dichlorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AC
(S)-3-(6-(3-chloro-2-methoxy- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AD
(S)-3-(6-(2,5-difluorophenyl)-4- ((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AE
(S)-3-(6-(3-fluoro-5- (trifluoromethyl)phenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AF
(S)-3-(6-(4-fluoro-3- (trifluoromethyl)phenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AG
(S)-3-(6-(2-chloro-6-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AH
(S)-3-(6-(2-chloro-3-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AI
(S)-3-(6-(2-chloro-5-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AJ
(S)-3-(6-(2-isopropylphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AK
(S)-3-(4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(5- (trifluoromethyl)pyridin-3-yl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AL
(S)-3-(6-(2,3-dichlorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AM
(S)-3-(6-(2,5-dichlorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AN
(S)-3-(6-(3-chloro-4- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AO
(S)-3-(6-(3-chloro-5- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AP
(S)-3-(6-(3-(trifluoromethoxy)- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AQ
(S)-3-(6-(1-methyl-1H-pyrazol-4- yl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AR
(S)-3-(6-(1-methyl-1H-pyrazol-5- yl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AS
(S)-3-(6-(3-ethoxyphenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]-oxazin-2- yl)propanoic acid
2AT
(S)-3-(6-(3-cyanophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AU
(S)-3-(6-(3-hydroxyphenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AV
(S)-3-(6-(3-isopropoxyphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AW
(S)-3-(6-(2-hydroxyphenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AX
(S)-3-(6-(3-fluorophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2AY
(S)-3-(6-(2-fluoro-3-methyl- phenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
2AZ
(S)-3-(6-(5-methyl-1,3,4- thiadiazol-2-yl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BA
(S)-3-(6-(5-fluoro-2- methylphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BC
(S)-3-(6-(3,5-difluoro-2- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BD
(S)-3-(6-(2-ethylphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BE
(S)-3-(6-(2-chloropyridin-3-yl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BF
(S)-3-(6-(3-fluoro-5-methoxy- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BG
(S)-3-(6-(2-methoxypyridin-3-yl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BH
(S)-3-(6-(1-isobutyl-1H-pyrazol- 4-yl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BI
(S)-3-(6-(2-(methylsulfonyl)- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BJ
(S)-3-(6-(2-cyano-6-methoxy- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BK
(S)-3-(6-(2-chloro-5-methyl- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BL
(S)-3-(6-(2-fluoro-5-methyl- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BM
(S)-3-(6-(2-(trifluoromethyl)- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BN
(S)-3-(6-(3-fluoro-5-methyl- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BO
(S)-3-(6-(3,5-dimethylisoxazol-4- yl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
TABLE 3
Compd
No.
Structure
Name
4A
(S)-3-(4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4B
(S)-3-(4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(4- (trifluoromethyl)pyrimidin-2- yl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4C
(S)-3-(6-(4-methoxypyrimidin- 2-yl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4D
(S)-3-(6-(2-methoxypyridin-4- yl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4E
(S)-3-(6-(6-methoxypyridin-2- yl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4F
(S)-3-(6-(4-methoxypyridin-2- yl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4G
(S)-3-(4-((3- (trifluoromethyl)phenyl)sulfonyl)- 6-(4-(trifluoromethyl)thiazol- 2-yl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4H
(S)-3-(4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(5- (trifluoromethyl)thiazol-2-yl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4I
(S)-3-(6-(6-chloropyridin-2-yl)- 4-((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4J
(S)-3-(6-(imidazo[1,2- a]pyridin-8-yl)-4-((3- (trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4K
(S)-3-(6-(1-methyl-1H- imidazol-5-yl)-4-((3- (trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4L
(S)-3-(6-(1-methyl-1H- imidazol-2-yl)-4-((3- (trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4M
(S)-3-(6-(1-methyl-1H-1,2,4- triazol-3-yl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
4N
(S)-3-(6-(imidazo[1,5- a]pyridin-3-yl)-4-((3- (trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4O
(S)-3-(6-(pyrazolo[1,5- a]pyridin-3-yl)-4-((3- (trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4P
(S)-3-(6-(imidazo[1,2- a]pyridin-5-yl)-4-((3- (trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4Q
(S)-3-(6-(1-methyl-1H- imidazol-4-yl)-4-((3- (trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4R
(S)-3-(6-(3-cyclopropylphenyl)- 4-((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4S
(S)-3-(6-(6-methylpyridin-2-yl)- 4-((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4T
(S)-3-(6-(3-(difluoromethoxy)- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4U
(S)-3-(4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(1,3,5- trimethyl-1H-pyrazol-4-yl)-3,4- dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
4V
(S)-3-(6-(pyrazolo[1,5-a]- pyridin-7-yl)-4-((3-(trifluoro- methyl)-phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
4W
(S)-3-(6-(1-methyl-1H-pyrazol- 3-yl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4X
(S)-3-(6-(6-(dimethylamino)- pyridin-2-yl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
4Y
(S)-3-(6-(6-methoxypyrazin-2- yl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4Z
(S)-3-(6-(5-methyl-1,3,4- oxadiazol-2-yl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
4AA
(S)-3-(6-(3-ethoxy-2- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4] oxazin-2-yl)propanoic acid
4AB
(S)-3-(6-(3-(2-hydroxyethoxy)- phenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AC
(S)-3-(6-(1-isopropyl-1H- pyrazol-4-yl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4] oxazin-2-yl)propanoic acid
4AD
(S)-3-(6-(2-phenylpyridin-3-yl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4AE
(S)-3-(6-(2-methylpyridin-3-yl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4AF
(S)-3-(6-(5-fluoro-2- methylpyridin-3-yl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AG
(S)-3-(6-(3-fluoro-2- methylphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AH
(S)-3-(6-(3-ethylphenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AI
(S)-3-(6-(6-phenylpyridin-2-yl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4AJ
(S)-3-(6-(3,5-difluoro-2- methylphenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AK
(S)-3-(4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(2,3,5- trifluorophenyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4AL
(S)-3-(6-(6-(dimethylamino)- pyrazin-2-yl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AM
(S)-3-(6-(6-(methylamino)- pyridin-2-yl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AN
(S)-3-(6-(6-(dimethylamino)-4- methylpyridin-2-yl)-4-((3- (trifluoromethyl)phenyl)sul- fonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AO
(S)-3-(6-(6-(dimethylamino)-3- methylpyridin-2-yl)-4-((3- (trifluoromethyl)phenyl)sul- fonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AP
(S)-3-(6-(6-(dimethylamino)-4- methoxypyridin-2-yl)-4-((3- (trifluoromethyl)phenyl)sul- fonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AQ
(S)-3-(6-(5-chloro-2,3- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sul- fonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AR
(S)-3-(6-(2,3-difluoro-5- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sul- fonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AS
(S)-3-(6-(2,3-difluoro-5- (trifluoromethyl)phenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AT
(S)-3-(6-(6-(dimethylamino)-4- (trifluoromethyl)pyridin-2-yl)- 4-((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AU
(S)-3-(6-(4-(dimethylamino)- pyrimidin-2-yl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AV
(S)-3-(6-(2-(dimethylamino)- pyrimidin-4-yl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AX
(S)-3-(6-(2-chloropyrimidin-4- yl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4AY
(S)-3-(6-(3-chloro-2,5- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
4AZ
(S)-3-(6-(2,5-difluoro-3- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
TABLE 4
Compd
No.
Structure
Name
6A
(S)-3-(6-(3-chlorophenyl)-4-((3- ethoxy-1-ethyl-1H-pyrazol-4- yl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)propanoic acid
6B
(S)-3-(6-(3-chlorophenyl)-4-((3- chlorophenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
6C
(S)-3-(4-((3-chloro-1-ethyl-1H- pyrazol-4-yl)sulfonyl)-6-(3- chlorophenyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)propanoic acid
6D
(S)-3-(6-(3-chlorophenyl)-4-((2- ethoxy-5-(trifluoromethyl)-pyridin- 3-yl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]-oxazin-2-yl)propanoic acid
6E
(S)-3-(6-(3-chlorophenyl)-4-((3- (difluoromethoxy)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
6F
(S)-3-(6-(3-chlorophenyl)-4-((3- isopropylphenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
6G
(S)-3-(6-(3-chlorophenyl)-4-((2-(2- hydroxyethoxy-5- (trifluoromethyl)-pyridin-3- yl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)propanoic acid
6H
(S)-3-(6-(3-chlorophenyl)-4-((3- cyclopropylphenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
6I
(S)-3-(6-(2,5-difluorophenyl)-4-((2- methyl-3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)propanoic acid
6J
(S)-3-(6-(2,5-difluorophenyl)-4-((3- fluoro-5-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)propanoic acid
6K
(S)-3-(6-(2-chloro-3,5- difluorophenyl)-4-((4-fluoro-3- methoxyphenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
6L
(S)-3-(6-(2-chloro-3,5-difluoro- phenyl)-4-((3-(difluoromethoxy)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)propanoic acid
TABLE 5
Compd
No.
Structure
Name
21A
(S)-4-(6-(2,3-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)butanoic acid
21B
(S)-4-(6-(3-methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)butanoic acid
21C
(S)-4-(4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)butanoic acid
21D
(S)-4-(6-(2-chloro-3,5- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)butanoic acid
TABLE 6
Compd
No.
Structure
Name
22A
(S)-3-(8-fluoro-4-((3- (trifluoromethyl)phenyl)-sulfonyl)- 6-(6-(trifluoromethyl)pyridin-2- yl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
22B
(S)-3-(7-chloro-6-(2,3- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
22C
(S)-3-(7-chloro-6-(3- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
22D
(S)-3-(8-fluoro-6-(3- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
22E
(S)-3-(6-(2,3-difluorophenyl)-8- fluoro-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
22F
(S)-3-(7-chloro-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 6-(6-(trifluoromethyl)pyridin-2- yl)-3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
22G
(S)-3-(7-chloro-6-(2-chloro-3,5- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
TABLE 7
Compd
No.
Structure
Name
23A
(S)-(6-(3-chlorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]-oxazin-2- yl)-1-(1,1-dioxidothio- morpholino)propan-1-one
23B
(S)-3-(6-(3-chlorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]-oxazin-2- yl)-1-morpholino-propan-1-one
23C
(S)-1-(3-(6-(3-chlorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanoyl)piperidine-4-carboxylic acid
23D
(S)-3-(3-(6-(3-chlorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanamido)propanoic acid
23E
(S)-1-(3-(8-fluoro-4-((3- (trifluoromethyl)phenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanoyl)piperidine-4-carboxylic acid
23F
(S)-1-(3-(4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(6-(trifluoro- methyl)pyridin-2-yl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoyl)piperidine-4-carboxylic acid
23G
(S)-1-(1,1-dioxidothio-morpholino)-3- (4-((3-(trifluoro- methyl)phenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]-oxazin-2- yl)propan-1-one
23H
(S)-1-(3-(8-fluoro-6-(3- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanoyl)piperidine-4-carboxylic acid
23I
(S)-1-(3-(6-(2,3-difluorophenyl)-8- fluoro-4-((3- (trifluoromethyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanoyl)piperidine-4-carboxylic acid
23J
(S)-(3-(4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanoyl)glycine
23K
(S)-(3-(6-(3-methoxyphenyl)-4-((3- (trifluoromethyl)-phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanoyl)glycine
23L
(S)-1-(3-(6-(3-methoxyphenyl)-4-((3- (trifluoromethyl)-phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanoyl)piperidine-4-carboxylic acid
23M
(S)-1-(1,1-dioxidothio-morpholino)-3- (6-(3-methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]-oxazin-2- yl)propan-1-one
23N
(S)-3-(6-(2,3-difluorophenyl)-4-((3- (trifluoromethyl)-phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2-yl)- 1-(1,1-dioxidothiomorpholino)propan- 1-one
23O
(S)-(3-(6-(2,3-difluorophenyl)-4-((3- (trifluoromethyl)-phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanoyl)glycine
23P
(S)-1-(3-(6-(2,3-difluorophenyl)-4-((3- (trifluoromethyl)-phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanoyl)piperidine-4-carboxylic acid
23Q
(S)-1-(((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)-phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)carbamoyl)piperidine-4- carboxylic acid
23R
(S)-3-(3-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-1-methylureido)propanoic acid
23S
(S)-3-(3-((S)-6-(2,5-difluoro-phenyl)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanamido)-2-hydroxypropanoic acid
23T
(S)-1-((2-(6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)ethyl)carbamoyl)piperidine-4- carboxylic acid
23U
((2-((S)-6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)ethyl)carbamoyl)-D-proline
23V
((2-((S)-6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)ethyl)carbamoyl)-L-proline
23W
(S)-N-((2-(6-(2,5-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)-sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin-2- yl)ethyl)carbamoyl)-N-methylglycine
23X
(S)-((2-(6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)ethyl)carbamoyl)glycine
23Y
(S)-3-(3-(2-(6-(2,5-difluoro-phenyl)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin-2- yl)ethyl)-1-methylureido)propanoic acid
23Z
(S)-3-(3-(2-((S)-6-(2,5-difluorophenyl)- 4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)ethyl)ureido)-2-hydroxypropanoic acid
TABLE 8
Compd
No.
Structure
Name
28A
(S)-5-(2-(4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)ethyl)-1,3,4-oxadiazol-2(3H)- one
28B
(S)-5-(2-(6-(6-(dimethylamino)- pyridin-2-yl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)ethyl)-1,3,4-oxadiazol-2(3H)- one
28C
(S)-5-(2-(4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(5- (trifluoromethyl)pyridin-3-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)ethyl)-1,3,4-oxadiazol-2(3H)- one
28D
(S)-5-(2-(6-(2,5-difluorophenyl)- 4-((3-isopropylphenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)ethyl)-1,3,4- oxadiazol-2(3H)-one
28E
(S)-5-(2-(6-(3-methoxyphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)ethyl)- 1,3,4-oxadiazol-2(3H)-one
28F
(S)-5-(2-(6-(6-(dimethylamino)- pyridin-2-yl)-4-((3-isopropyl- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)ethyl)- 1,3,4-oxadiazol-2(3H)-one
28G
(S)-5-(2-(6-(2,5-difluoro-3- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)ethyl)-1,3,4- oxadiazol-2(3H)-one
28H
(S)-5-(2-(6-(6-(dimethylamino)-4- methoxypyridin-2-yl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)ethyl)-1,3,4- oxadiazol-2(3H)-one
28I
(S)-5-(2-(6-(2-chloro-3,5- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)ethyl)- 1,3,4-oxadiazol-2(3H)-one
28J
(S)-5-(2-(6-(2,5-difluorophenyl)- 4-((4-fluoro-3-methoxyphenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)ethyl)- 1,3,4-oxadiazol-2(3H)-one
28K
(S)-5-(2-(4-((4-fluoro-3- methoxyphenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)ethyl)-1,3,4-oxadiazol-2(3H)- one
TABLE 9
Compd
No.
Structure
Name
30A
(S)-N-(2-(6-(6-(dimethylamino)- pyridin-2-yl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2-yl)ethyl)- 2-hydroxy-2-methylpropanamide
30B
(S)-2-hydroxy-2-methyl-N-(2-(4-((3- (trifluoromethyl)phenyl)-sulfonyl)-6- (6-(trifluoromethyl)-pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)ethyl)propanamide
30C
(S)-2-hydroxy-2-methyl-N-(2-(4-((3- (trifluoromethyl)-phenyl)sulfonyl)-6- (5-(trifluoromethyl)pyridin-3-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)ethyl)propanamide
30D
(S)-N-(2-(6-(2,5-difluoro-phenyl)-4- ((3-isopropylphenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)ethyl)-2-hydroxy-2- methylpropanamide
30E
(S)-2-hydroxy-N-(2-(6-(3- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)ethyl)-2-methylpropanamide
30F
(S)-N-(2-(6-(2,5-difluoro-3- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)ethyl)-2-hydroxy-2- methylpropanamide
30G
(S)-N-(2-(6-(6-(dimethylamino)- pyridin-2-yl)-4-((3-isopropyl- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)ethyl)-2- hydroxy-2-methylpropanamide
30H
(S)-N-((6-(6-(dimethylamino)-pyridin- 2-yl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-2-hydroxy-2- methylpropanamide
30I
(S)-2-hydroxy-2-methyl-N-((4-((3- (trifluoromethyl)phenyl)-sulfonyl)-6- (6-(trifluoromethyl)-pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)propanamide
30J
(S)-N-((6-(6-(dimethylamino)-pyridin- 2-yl)-4-((3-isopropylphenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)-2-hydroxy-2- methylpropanamide
30K
(S)-N-((6-(2,5-difluorophenyl)-4-((3- isopropylphenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-2-hydroxy-2- methylpropanamide
30L
(S)-N-((6-(2,5-difluoro-3- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-2-hydroxy-2- methylpropanamide
30M
(S)-N-(2-(6-(2,5-difluorophenyl)-4-((4- fluoro-3-methoxyphenyl)-sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)ethyl)-2-hydroxy-2- methylpropanamide
30N
(S)-N-(2-(4-((4-fluoro-3- methoxyphenyl)sulfonyl)-6-(3- methoxyphenyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)ethyl)-2- hydroxy-2-methylpropanamide
30O
(S)-N-(2-(4-((4-fluoro-3- methoxyphenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)ethyl)-2-hydroxy-2- methylpropanamide
30P
(S)-N-(2-(4-((3-(difluoro- methoxy)phenyl)sulfonyl)-6-(2,5- difluorophenyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)ethyl)-2- hydroxy-2-methylpropanamide
30Q
(S)-N-((6-(2,5-difluorophenyl)-4-((4- fluoro-3-methoxyphenyl)-sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)-2-hydroxy-2- methylpropanamide
30R
(S)-N-((4-((3-(difluoromethoxy)- phenyl)sulfonyl)-6-(2,5- difluorophenyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-2- hydroxy-2-methylpropanamide
30S
(S)-N-((4-((4-fluoro-3- methoxyphenyl)sulfonyl)-6-(3- methoxyphenyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-2- hydroxy-2-methylpropanamide
30T
(S)-N-((4-((4-fluoro-3- methoxyphenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-2-hydroxy-2- methylpropanamide
30U
(S)-N-((6-(2,5-difluorophenyl)-4-((5- (trifluoromethyl)pyridin-3- yl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-2- hydroxy-2-methylpropanamide
30V
(R)-N-(((S)-6-(2,5-difluoro-phenyl)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)-3,3,3-trifluoro-2- hydroxy-2-methylpropanamide
30W
(S)-N-(((S)-6-(2,5-difluoro-phenyl)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)-3,3,3-trifluoro-2- hydroxy-2-methylpropanamide
30X
(R)-N-(((S)-6-(2,5-difluorophenyl)-4- ((4-fluoro-3-methoxyphenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)-3,3,3-trifluoro-2- hydroxy-2-methylpropanamide
30Y
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2-yl)- methyl)cyclopropane-carboxamide
30Z
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)oxetane-3-carboxamide
30AA
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-3-oxocyclobutane-1- carboxamide
30AB
(S)-2-cyclopropyl-N-((6-(2,5- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)acetamide
30AC
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-1H-pyrazole-4- carboxamide
30AD
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-1H-pyrazole-3- carboxamide
30AE
(S)-N-(((S)-6-(2,5-difluoro-phenyl)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-methyl)-2-hydroxypropanamide
30AF
(R)-N-(((S)-6-(2,5-difluoro-phenyl)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-methyl)-2-hydroxypropanamide
30AG
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-1-hydroxycyclo-propane-1- carboxamide
30AH
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-1-methyl-1H-pyrazole-4- carboxamide
30AI
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-1-methyl-1H-pyrazole-3- carboxamide
30AJ
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)oxazole-4-carboxamide
30AK
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)oxazole-5-carboxamide
30AL
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-3-sulfamoyl-propanamide
30AM
(1S,2S)-N-(((S)-6-(2,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-2- fluorocyclo-propane-1-carboxamide
30AN
(1R,2R)-N-(((S)-6-(2,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-2- fluorocyclo-propane-1-carboxamide
30AO
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)pivalamide
30AP
(S)-2-cyano-N-((6-(2,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)acetamide
30AQ
(S)-2-cyano-N-((6-(2,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,410xazi11-2-yl)methyl)-2- methylpropanamide
30AR
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2-yl)- methyl)-1-fluorocyclopropane-1- carboxamide
30AS
(R)-2-acetamido-N-(((S)-6-(2,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2-yl)methyl)- 3-methylbutanamide
30AT
(R)-2-acetamido-N-(((S)-6-(2,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)propanamide
30AU
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-3-hydroxy-2,2- dimethylpropanamide
30AV
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-1-methylcyclo-propane-1- carboxamide
30AW
(S)-N-(((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)but-3-enamide
30AX
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2 yl)methyl)isobutyramide
30AY
(S)-2-(((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)amino)-2-oxoethyl acetate
30AZ
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo-[b][1,4]oxazin-2- yl)methyl)-cyclopentanecarboxamide
30BA
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-2-hydroxyacetamide
30BB
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo-[b][1,4]oxazin-2- yl)methyl)-cyclobutanecarboxamide
30BC
(S)-N-((6-(6-(dimethylamino)-pyridin- 2-yl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)cyclo-propanecarboxamide
30BD
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)acetamide
30BE
(S)-N-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-2-fluoro-2- methylpropanamide
30BF
(R)-N-(((S)-6-(2,5-difluoro-3- methoxyphenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2-yl)methyl)- 3,3,3-trifluoro-2-hydroxy-2- methylpropanamide
30BG
(S)-3-sulfamoyl-N-((4-((3- (trifluoromethyl)phenyl)-sulfonyl)-6- (6-(trifluoro-methyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-propanamide
30BH
(S)-2-cyano-N-((4-((3- (trifluoromethyl)phenyl)-sulfonyl)-6- (6-(trifluoro-methyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)acetamide
30BI
(S)-3-hydroxy-2,2-dimethyl-N-((4-((3- (trifluoromethyl)-phenyl)sulfonyl)-6- (6-(trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]-oxazin-2- yl)methyl)-propanamide
TABLE 10
Compd
No.
Structure
Name
32A
(S)-4-(6-(2,5-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylbutanoic acid
32B
(S)-3-(6-(3-methoxyphenyl)-4- ((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32C
(S)-3-(6-(2,5-difluoro-3- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32D
(S)-3-(6-(6-(dimethylamino)- pyridin-2-yl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32E
(S)-2,2-dimethyl-3-(4-((3- (trifluoromethyl)phenyl)sulfonyl)- 6-(6-(trifluoromethyl)pyridin-2- yl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
32F
(S)-2,2-dimethyl-3-(6-(3- (trifluoromethoxy)phenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
32G
(S)-3-(6-(3-(difluoromethoxy)- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32H
(S)-3-(6-(2-chloro-3- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32I
(S)-3-(6-(2-chloro-5- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32J
(S)-3-(6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32K
(S)-3-(6-(2,3-difluorophenyl)-4- ((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32L
(S)-3-(6-(3-chloro-2-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32M
(S)-3-(6-(2,5-difluorophenyl)-4- ((3-isopropylphenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32N
(S)-3-(6-(3,5-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32O
(S)-2,2-dimethyl-3-(6-(3- (trifluoromethyl)phenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
32P
(S)-2,2-dimethyl-4-(4-((3- (trifluoromethyl)phenyl)sulfonyl)- 6-(6-(trifluoromethyl)pyridin-2- yl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)butanoic acid
32Q
(S)-3-(6-(3,5-dimethoxyphenyl)- 4-((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32R
(S)-3-(6-(3-chloro-5-(difluoro- methoxy)phenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2,2-dimethylpropanoic acid
32S
(S)-4-(6-(2,5-difluoro-3- methoxyphenyl)-4-((4-fluoro-3- methoxyphenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2,2-dimethylbutanoic acid
32T
(S)-4-(4-((3-(difluoro- methoxy)phenyl)sulfonyl)-6-(2,5- difluorophenyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylbutanoic acid
32U
(S)-3-(6-(2-chloro-3,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
TABLE 11
Compd
No.
Structure
Name
34A
(S)-3-(6-(2,4-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propan-1-ol
34B
(S)-3-(6-(3,4-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propan-1-ol
34C
(S)-3-(6-(3,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propan-1-ol
34D
(S)-3-(6-(3-chlorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propan-1-ol
34E
(S)-3-(6-(2,3-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propan-1-ol
34F
(S)-3-(6-(3-methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propan-1-ol
34G
(S)-3-(4-((3-trifluoromethyl)- phenyl)-sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propan-1-ol
34H
(S)-3-(6-(6-(dimethylamino)-pyridin-2- yl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2-yl)propan- 1-ol
TABLE 12
Compd
No.
Structure
Name
36A
(S)-3-(3-(6-(3,5-difluoro-phenyl)- 4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]-oxazin- 2-yl)propoxy)-1,2,4-oxadiazol- 5(4H)-one
36B
(S)-3-(3-(6-(3-methoxyphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propoxy)-1,2,4-oxadiazol- 5(4H)-one
36C
(S)-3-(3-(4-((3-(trifluoro- methyl)phenyl)sulfonyl)-6-(6- (trifluoromethyl)-pyridin-2-yl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propoxy)-1,2,4-oxadiazol- 5(4H)-one
TABLE 13
Compd
No.
Structure
Name
43A
(S)-3-(6-(2,4-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-N- (phenylsulfonyl)propanamide
43B
(S)-N-(cyclopropylsulfonyl)-3-(6- (2,4-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanamide
TABLE 14
Compd
No.
Structure
Name
45A
([[(2S)-6-(2,5-difluorophenyl)-4- [[3-(trifluoromethyl)-benzene]- sulfonyl]-3,4-dihydro-2H-1,4- benzoxazin-2- yl]methyl]sulfamoyl)- (dimethyl)amine
45C
([[(2S)-6-(2,5-difluorophenyl)-4- [[4-fluoro-3-methoxy-benzene]- sulfonyl]-3,4-dihydro-2H-1,4- benzoxazin-2- yl]methyl]sulfamoyl)- (dimethyl)amine
45D
([[(2S)-6-(2,5-difluorophenyl)-4- [[4-fluoro-3-methoxy-benzene]- sulfonyl]-3,4-dihydro-2H-1,4- benzoxazin-2- yl]methyl]sulfamoyl)-(N-methyl- N-2-hydroxyethyl)-amine
TABLE 15
Compd
No.
Structure
Name
46A
3-((S)-6-(2-chloro-3,5-difluoro-4- methylphenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2-methylpropanoic acid
46B
(R)-3-((S)-6-(2-chloro-3,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2-methylpropanoic acid
46C
(S)-3-((S)-6-(2-chloro-3,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2-methylpropanoic acid
TABLE 23-I
Title Compound
from Example No.
Structure
1
3
5
7
8
9
10
11
12
19
20
24
25
26
27
29
31
35
37
38
39
40
41
42
44
30. A compound in any one of Tables 2A, 3A, 6A, 9A, 10A, 14A, 15A, 16-22, or 23A-I below or a pharmaceutically acceptable salt thereof:
TABLE 2A
Compd
No.
Structure
Name
2BP
(R)-3-(6-(2,5-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BQ
(R)-3-(6-(3-chlorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
2BR
(S)-3-(6-(2,3-dimethylphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
TABLE 3A
Compd
No.
Structure
Name
4BB
(S)-3-(6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)propanoic acid
4BC
(R)-3-(6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)propanoic acid
4BD
(S)-3-(4-(3-(trifluoromethyl)- phenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)propanoic acid
4BE
(R)-3-(6-(2-chloro-3,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)propanoic acid
TABLE 6A
Compd
No.
Structure
Name
22H
(S)-3-(6-(2-chloro-3,5-difluoro- phenyl)-8-fluoro-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)propanoic acid
22I
(S)-3-(6-(3-chloro-2-fluoro- phenyl)-8-fluoro-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
22J
(S)-3-(7-chloro-6-(3-chloro-2- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)propanoic acid
22K
(S)-3-(6-(3,5-difluorophenyl)-8- fluoro-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
22L
(S)-3-(7-chloro-6-(3,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
22M
(S)-3-(6-(3-(difluoromethoxy)-5- fluorophenyl)-8-fluoro-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
22N
(S)-3-(7-chloro-6-(3-(difluoro- methoxy)-5-fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
TABLE 9A
Compd
No.
Structure
Name
30BJ
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)- 3,3,3-trifluoro-2,2- dimethylpropanamide
30BK
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-3- sulfamoylpropanamide
30BL
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-1- cyanocyclo-propane-1-carboxamide
30BM
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-1- fluorocyclo-propane-1-carboxamide
30BN
(S)-1-methyl-3-(trifluoro-methyl)-N- ((4-((3-(trifluoro- methyl)phenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4|-oxazin-2- yl)methyl)-1H-pyrazole-4- carboxamidc
30BO
(S)-N-((4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]-oxazin-2- yl)methyl)-1H-pyrazole-5- carboxamidc
30BP
(S)-1-cyano-N-((4-((3- (trifluoromethyl)phenyl)sulfonyl)-6- (6-(trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)cyclopropane-1- carboxamide
30BQ
(S)-1-fluoro-N-((4-((3-(trifluoro- methyl)phenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]-oxazin-2- yl)methyl)cyclo-propane-1- carboxamide
30BR
(S)-2-acetamido-3-methyl-N-(((S)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 6-(6-(trifluoro-methyl)pyridin-2-yl)- 3,4-dihydro-2H-benzo[b][1,4]-oxazin- 2-yl)methyl)butanamide
30BS
(S)-N-((6-(2-chloro-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-1- methyl-3-(trifluoromethyl)-1H- pyrazole-4-carboxamide
30BT
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-1H- pyrazole-5-carboxamide
30BU
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-2- cyanoacetamide
30BV
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-3- hydroxy-2,2-dimethylpropanamide
30BW
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-1- methylcyclo-propane-1-carboxamide
30BX
(S)-N-((6-(2-chloro-3-fluorophenyl)-4- ((3-(trifluoro-methyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]-oxazin- 2-yl)methyl)but-3-enamide
30BY
(S)-3,3,3-trifluoro-2,2-dimethyl-N-((4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 6-(6-(trifluoro-methyl)pyridin-2-yl)- 3,4-dihydro-2H-benzo[b][1,4]-oxazin- 2-yl)methyl)propanamide
30BZ
(S)-N-((6-(2-chloro-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-2- fluoro-2-methylpropanamide
30CA
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-2- cyclopropyl-2-oxoacetamide
30CB
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-1- (hydroxymethyl)-cyclopropane-1- carboxamide
30CC
(R)-3,3,3-trifluoro-N-(((S)-4-((4- fluoro-3-methoxyphenyl)-sulfonyl)-6- (6-(trifluoromethyl)-pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-2-hydroxy-2- methylpropanamide
30CD
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-1- methyl-1H-pyrazole-4-carboxamide
30CE
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-2,2- difluoro-propanamide
30CF
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)cyclopropanecarbox-amide
30CG
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-3- hydroxy-3-methylbutanamide
30CH
(S)-N-((6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-3- methoxy-propanamide
30CI
(S)-N-(((S)-6-(2-chloro-3- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)-2-methoxypropanamide
30CJ
(R)-2-acetamido-N-(((S)-6-(2-chloro- 3-fluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4)oxazin-2- yl)methyl)propanamide
30CK
N-((S)-6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-2- fluoropropanamide
30CL
(S)-N-((6-(2-chloro-3,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)- 3,3,3-trifluoro-2,2- dimethylpropanamide
30CM
N-(((S)-6-(2-chloro-3-fluoro-phenyl)- 4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-3- hydroxy-2-methylpropanamide
30CN
(S)-N-((6-(2-chloro-3,5-di- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)-1-methyl-3- (trifluoromethyl)-1H-pyrazole-4- carboxamide
30CO
(S)-N-((6-(2-chloro-3,5-di- fuorophenyl)-4-((3-(trifluoro-methyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]-oxazin-2-yl)methyl)-3- sulfamoylpropanamide
30CP
(S)-N-((6-(2-chloro-3,5-di- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)-1H-pyrazole-5- carboxamide
30CQ
(S)-N-((6-(2-chloro-3,5-di- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)-2-fluoro-2- methylpropanamide
30CR
(S)-N-((6-(2-chloro-3,5-di- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)but-3-enamide
30CS
(S)-N-((6-(2-chloro-3,5-di- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)-2-fluoro-2- methylpropanamide
30CT
tert-butyl (R)-(2-(6-(2,5-di- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)ethyl)carbamate
30CU
(R)-N-(2-(6-(2,5-difluoro-phenyl)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)ethyl)acetamide
30CV
(S)-N-(1-(6-(2,5-difluoro-phenyl)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2-methylpropan-2-yl)acetamide
30CW
(S)-N-((6-(2-chloro-3,5- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-2-hydroxy-2- methylpropanamide
30CX
(S)-N-1-(6-(2,5-difluoro-phenyl)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2-methylpropan-2-yl)-2- hydroxy-2-methylpropanamide
30CY
(S)-N-((6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)-3,3,3-trifluoro-2,2- dimethyl-propanamide
30CZ
(S)-N-((6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)-1-methyl-3- (trifluoromethyl)-1H-pyrazole-4- carboxamide
30DA
(S)-N-((6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)-3-sulfamoylpropanamide
30DB
(S)-N-((6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)-1H-pyrazole-5- carboxamide
30DC
(R)-N-(1-(6-(2,5-difluoro-phenyl)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2-methylpropan-2-yl)acetamide
30DD
(R)-N-(1-(6-(2,5-difluoro-phenyl)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2-methylpropan-2-yl)-2- hydroxy-2-methylpropanamide
30DE
(S)-N-(1-(6-(2,5-difluoro-phenyl)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2-methylpropan-2-yl)methane- sulfonamide
30DF
(R)-N-(1-(6-(2,5-difluoro-phenyl)-4- ((3-(trifluoromethyl)-phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2-methylpropan-2-yl)methane- sulfonamide
30DG
(S)-N-((6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)-2-fluoro-2- methylpropanamide
30DH
(S)-N-((6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)-3-hydroxy-2,2- dimethylpropanamide
30DI
(S)-N-((6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)but-3-enamide
30DJ
(S)-N-((6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)-1-fluorocyclopropane-1- carboxamide
30DK
(S)-N-(1-(6-(3-methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)-sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)-2-methylpropan-2-yl)acetamide
TABLE 10A
Compd
No.
Structure
Name
32V
(S)-3-(6-(2,3-dimethoxyphenyl)- 4-((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32W
(S)-3-(6-(3-chlorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)-2,2-dimethyl- propanoic acid
32X
(S)-2,2-dimethyl-3-(4-((3- (trifluoromethyl)phenyl)sulfonyl)- 6-(2,3,5-trifluorophenyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)propanoic acid
32Y
(S)-3-(6-(3-chloro-5-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32Z
(S)-2,2-dimethyl-3-(6-(2- (trifluoromethoxy)phenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
32AA
(S)-3-(6-(2-chloro-3- (trifluoromethyl)phenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)-2,2-dimethyl- propanoic acid
32AB
(S)-3-(6-(3-chloro-5-(trifluoro- methyl)phenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2,2-dimethylpropanoic acid
32AC
(S)-3-(6-(2,2-difluorobenzo[d]- [1,3]dioxo1-4-yl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2,2-dimethylpropanoic acid
32AD
(S)-3-(6-(2-chloro-5-(trifluoro- methyl)phenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2,2-dimethylpropanoic acid
32AE
(S)-3-(6-(5-acetyl-2-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32AF
(S)-3-(6-(2-cyanophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)-2,2-dimethyl- propanoic acid
32AG
(S)-3-(6-(3-fluoro-5-methoxy- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32AH
(S)-3-(6-(3-chloro-5-methoxy- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32AI
(S)-3-(6-(3-chloro-2,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32AJ
(S)-4-(4-((4-fluoro-3-methoxy- phenyl)sulfonyl)-6-(6-(trifluoro- methyl)pyridin-2-yl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2-yl)- 2,2-dimethylbutanoic acid
32AK
(S)-3-(6-(6-(difluoromethyl)- pyridin-2-yl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2,2-dimethylpropanoic acid
32AL
(S)-3-(6-(3-(difluoromethyl)- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32AM
(S)-3-(6-(6-(difluoromethoxy)- pyridin-2-yl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2,2-dimethylpropanoic acid
32AN
(R)-3-(6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32AO
(R)-3-(6-(3-chloro-2,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32AP
(R)-1-((6-(3,5-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)cyclobutane-1- carboxylic acid
32AQ
(R)-1-((6-(2,5-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)cyclobutane-1- carboxylic acid
32AR
(S)-3-(6-(5-chloro-2-methyl- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32AS
(S)-3-(6-(3,5-dimethylphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32AT
(S)-3-(6-(2,5-dimethylphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32AU
(S)-3-(6-(2,6-dichlorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32AV
(S)-3-(6-(5-fluoro-2-(trifluoro- methyl)phenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2,2-dimethylpropanoic acid
32AW
(S)-3-(6-(2,5-dichloro-3-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32AX
(S)-3-(6-(2-chloro-3-methyl- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32AY
(S)-3-(6-(2-fluoro-6-(trifluoro- methyl)phenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)-2,2-dimethylpropanoic acid
32AZ
(S)-3-(6-(3-chloro-2-methyl- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32BA
(S)-3-(6-(2,6-dimethylphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32BB
(S)-3-(6-(3-chloro-5-methyl- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32BC
(S)-3-(6-(3-fluoro-2- (trifluoromethyl)phenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32BD
(S)-1-((6-(3,5-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)cyclobutane-1- carboxylic acid
32BE
(S)-1-((6-(2,5-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)cyclobutane-1- carboxylic acid
32BF
(S)-1-((6-(3-chloro-2-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)- methyl)cyclobutane -1-carboxylic acid
32BG
(S)-3-(6-(3-(difluoromethoxy)- 2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)-2,2-dimethyl- propanoic acid
32BH
(S)-1-((6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)cyclobutane-1- carboxylic acid
32BI
(S)-3-(6-(5-(difluoromethoxy)-2- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32BJ
(S)-3-(6-(3-(difluoromethoxy)-2- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32BK
(S)-3-(6-(2,6-difluoro-3- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2,2- dimethylpropanoic acid
32BL
(S)-1-((4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(6-(trifluoro- methyl)pyridin-2-yl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)methyl)cyclobutane-1- carboxylic acid
32BM
(S)-2,2-dimethyl-3-(4-((3- (trifluoromethyl)phenyl)sulfonyl)- 6-(2,3,6-trifluorophenyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)propanoic acid
32BN
(S)-2,2-dimethyl-3-(6-(2,3,5,6- tetrafluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)propanoic acid
TABLE 14A
Compd
No.
Structure
Name
45E
(S)-N-(((S)-6-(2,5-difluoro- phenyl)-4-((4-fluoro-3- methoxyphenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)-3-hydroxy- pyrrolidine-1-sulfonamide
45F
(S)-N-((6-(2,5-difluorophenyl)-4- ((4-fluoro-3- methoxyphenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)pyrrolidine-1- sulfonamide
TABLE 15A
Compd
No.
Structure
Name
46D
(R)-3-((S)-6-(3-chloro-2-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2- methylpropanoic acid
46E
(S)-3-((S)-6-(3-chloro-2-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2- methylpropanoic acid
46F
(R)-2-(((S)-6-(2-chloro-3,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)butanoic acid
46G
(S)-2-(((S)-6-(2-chloro-3,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)butanoic acid
46H
(R)-3-((S)-6-(2-chloro-3,5- difluorophenyl)-8-fluoro-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)-2-methylpropanoic acid
46I
(S)-3-((S)-6-(2-chloro-3,5- difluorophenyl)-8-fluoro-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)-2-methylpropanoic acid
46J
(R)-3-((S)-6-(3,5-difluorophenyl)- 4-((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2- methylpropanoic acid
46K
(R)-2-methyl-3-((S)-6-(3- (trifluoromethyl)phenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
46L
(S)-2-methyl-3-((S)-6-(3- (trifluoromethyl)phenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
46M
(R)-3-((S)-6-(2-chloro-3,5- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2- methylpropanoic acid
46N
(S)-3-((S)-6-(2-chloro-3,5- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2- methylpropanoic acid
46O
(R)-3-((S)-6-(3-(difluoro- methoxy)-5-fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)-2-methylpropanoic acid
46P
(S)-3-((S)-6-(3-(difluoro- methoxy)-5-fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)-2-methylpropanoic acid
46Q
(R)-3-((S)-6-(3-chloro-5- (difluoromethoxy)phenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)-2-methylpropanoic acid
46R
(S)-3-((S)-6-(3-chloro-5- (difluoromethoxy)phenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)-2-methylpropanoic acid
46S
(S)-3-((S)-6-(3,5-difluorophenyl)- 4-((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)-2- methylpropanoic acid
46T
(S)-2-methyl-3-((S)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 6-(6-(trifluoromethyl)pyridin-2- yl)-3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
46U
(R)-2-methyl-3-((S)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 6-(6-(trifluoromethyl)pyridin-2- yl)-3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)propanoic acid
46V
(R)-2-(((S)-6-(3- (difluoromethoxy)-5- fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)butanoic acid
TABLE 16
Compd
No.
Structure
Name
51A
(S)-(3-((6-(2-chloro-3,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)oxetan-3-yl)methanol
51B
(S)-3-((6-(2-chloro-3,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3 ,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)oxetane-3-carboxylic acid
51C
(S)-3-((6-(2,5-difluoro-3- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)oxetane-3-carboxylic acid
51D
(S)-3-((4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(6-(trifluoro- methyl)pyridin-2-yl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)methyl)oxetane-3-carboxylic acid
51E
(S)-3-((4-((3- cyclopropylphenyl)sulfonyl)-6- (2,5-difluorophenyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)methyl)oxetane-3-carboxylic acid
51F
(S)-3-((4-((3-cyclopropyl- phenyl)sulfonyl)-6-(3-(difluoro- methoxy)-5-fluorophenyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)oxetane-3-carboxylic acid
51G
(S)-3-((6-(2,5-difluorophenyl)-4- ((3-fluoro-5-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)oxetane-3-carboxylic acid
51H
(S)-3-((4-((3-(difluoromethyl)- phenyl)sulfonyl)-6-(2,5- difluorophenyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)oxetane-3-carboxylic acid
51I
(S)-3-((6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3-fluoro-5- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)methyl)oxetane-3- carboxylic acid
51J
(S)-3-((6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((3-(difluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)oxetane-3-carboxylic acid
51K
(S)-3-((6-(2,5-difluorophenyl)-4- ((5-(trifluoromethyl)pyridin-3- yl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)oxetane-3-carboxylic acid
51L
(S)-3-((6-(3-(difluoromethoxy)-5- fluorophenyl)-4-((5-(trifluoro- methyl)pyridin-3-yl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)oxetane-3-carboxylic acid
51M
(S)-N-(3-((4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)oxetan-3- yl)acetamide
TABLE 17
Compd
No.
Structure
Name
60A
(1S,3r)-3-(((S)-6-(2,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)methyl)cyclobutane-1- carboxylic acid
60B
(1S,3r)-3-(((S)-6-(2-chloro-3,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)cyclobutane-1- carboxylic acid
60C
(1S,3r)-3-(((S)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-6-(6- (trifluoromethyl)pyridin-2-yl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)methyl)cyclobutane- 1-carboxylic acid
60D
N-((1S,3r)-3-(((S)-6-(3- (difluoro-methoxy)-5-fluoro- phenyl)-4-((3-(trifluoro-methyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]-oxazin-2- yl)methyl)cyclo-butyl)- acetamide
60E
N-((1S,3r)-3-(((S)-6-(2,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)cyclobutyl)-acetamide
60F
(1S,3r)-3-(((S)-6-(2-chloro-3,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)-1-methylcyclo- butane-1-carboxylic acid
60G
(1R,3s)-3-(((S)-6-(2-chloro-3,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)-1-methylcyclo- butane-1-carboxylic acid
60H
(1R,3s)-3-((S)-6-(2,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)cyclobutane-1-carboxylic acid
60I
(1S,3r)-3-((S)-6-(2,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro- 2H-benzo[b][1,4]oxazin-2- yl)cyclobutane-1-carboxylic acid
60J
(1R,3s)-3-((S)-6-(3-(difluoro- methoxy)-5-fluorophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]-oxazin-2- yl)cyclobutane-1-carboxylic acid
60K
(1S,3r)-3-((S)-6-(3-(difluoro- methoxy)-5-fluorophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)cyclobutane-1-carboxylic acid
60L
N-((1R,3s)-3-((S)-6-(2,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]- oxazin-2-yl)cyclobutyl)- acetamide
60M
N-((1S,3r)-3-((S)-6-(2,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]- oxazin-2-yl)cyclobutyl)- acetamide
60N
(1S,3r)-1-methyl-3-(((S)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-6-(6-(trifluoro- methyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]- oxazin-2-yl)methyl)cyclobutane- 1-carboxylic acid
60O
(1R,3s)-1-methyl-3-(((S)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-6-(6-(trifluoro- methyl)pyridin-2-yl)-3,4- dihydro-2H-benzo[b][1,4]- oxazin-2-yl)methyl)cyclobutane- 1-carboxylic acid
TABLE 18
Compd
No.
Structure
Name
77A
(S)-3-(((S)-6-(2,5-difluorophenyl)- 4-((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)- 2-oxopyrrolidine-3-carboxylic acid
77B
(R)-3-(((S)-6-(2,5- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)- 2-oxopyrrolidine-3-carboxylic acid
77C
(R)-2-(((S)-6-(3-(difluoro- methoxy)-5-fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)methyl)-5- oxopyrrolidine-2-carboxylic acid
77D
(S)-2-(((S)-6-(3-(difluoro- methoxy)-5-fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)methyl)-5- oxopyrrolidine-2-carboxylic acid
TABLE 19
Compd
No.
Structure
Name
78A
(S)-4-((6-(3-chlorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)methyl)tetrahydro- 2H-pyran-4-carboxylic acid
78B
(S)-4-((6-(3-chloro-5-methyl- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78C
(S)-4-((6-(2-chloro-3,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78D
(S)-4-((6-(2-chloro-5-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78E
(S)-4-((6-(3-chloro-5-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78F
(S)-4-((6-(3-chloro-2-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78G
(S)-4-((6-(3,5-dimethylphenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78H
(S)-4-((6-(3-(trifluoromethyl)- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78I
(S)-N-(4-((6-(3-(difluoro- methoxy)-5-fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)methyl)tetrahydro- 2H-pyran-4-yl)acetamide
78J
(S)-N-(4-((6-(2,5-difluorophenyl)- 4-((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- yl)acetamide
78K
(S)-4-((6-(3-(trifluoromethoxy)- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][ 1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78L
(S)-4-((6-(3-chloro-5-methoxy- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78M
(S)-4-((6-(2-chloro-3-fluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78N
(S)-4-((6-(3,5-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78O
(S)-4-((6-(3-fluoro-5-(trifluoro- methyl)phenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)tetrahydro-2H-pyran- 4-carboxylic acid
78P
(S)-4-((6-(2,3-difluorophenyl)-4- ((3-(trifluoromethyl)phenyl)- sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78Q
(S)-4-((6-(3-fluoro-5-methyl- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78R
(S)-4-((6-(3-fluoro-5-methoxy- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78S
(S)-4-((6-(2,5-difluoro-3- methoxyphenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin- 2-yl)methyl)tetrahydro-2H-pyran- 4-carboxylic acid
78T
(S)-4-((4-((3-(trifluoromethyl)- phenyl)sulfonyl)-6-(2,3,5- trifluorophenyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78U
(S)-4-((6-(2,3-difluoro-5- methoxyphenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78V
(S)-4-((6-(3-(difluoromethoxy)- 2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
78W
(S)-4-((6-(5-chloro-2,3- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H- benzo[b][1,4]oxazin-2- yl)methyl)tetrahydro-2H-pyran-4- carboxylic acid
TABLE 20
Compd
No.
Structure
Name
80A
(S)-3-((S)-6-(3-(difluoro- methoxy)-5-fluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)butanoic acid
80B
(R)-3-((S)-6-(2-chloro-3,5- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)butanoic acid
80C
(S)-3-((5)-6-(2-chloro-3,5- difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)butanoic acid
TABLE 21
Compd
No.
Structure
Name
83A
(S)-7-(2,5-difluorophenyl)-1-((3- (trifluoromethyl)phenyl)sulfonyl)- 1,2,3,4-tetrahydroquinolin-3-ol
83B
(R)-2-((7-(2,5-difluorophenyl)-1-((3- (trifluoromethyl)phenyl)sulfonyl)- 1,2,3,4-tetrahydroquinolin-3-yl)oxy)- 2-methylpropanoic acid
83C
(S)-2-((7-(2,5-difluorophenyl)-1-((3- (trifluoromethyl)phenyl)sulfonyl)- 1,2,3,4-tetrahydroquinolin-3-yl)oxy)- 2-methylpropanoic acid
83D
(R)-2-((7-(3-(difluoromethoxy)-5- fluorophenyl)-1-((3- (trifluoromethyl)phenyl)sulfonyl)- 1,2,3,4-tetrahydroquinolin-3-yl)oxy)- 2-methylpropanoic acid
83E
(R)-2-((7-(3-(difluoromethoxy)-5- fluorophenyl)-1-((3-(trifluoro- methyl)phenyl)sulfonyl)-1,2,3,4- tetrahydroquinolin-3-yl)oxy)acetic acid
83F
(S)-2-((7-(3-(difluoromethoxy)-5- fluorophenyl)-1-((3- (trifluoromethyl)phenyl)sulfonyl)- 1,2,3,4-tetrahydroquinolin-3-yl)oxy)- 2-methylpropanoic acid
TABLE 22
Compd
No.
Structure
Name
89A
(1s,3R)-3-acetamido-1-(((S)-6-(2,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)cyclobutane-l-carboxylic acid
89B
(1r,3S)-3-acetamido-1-(((S)-6-(2,5- difluorophenyl)-4-((3-(trifluoro- methyl)phenyl)sulfonyl)-3,4- dihydro-2H-benzo[b][1,4]oxazin-2- yl)methyl)cyclobutane-l-carboxylic acid
89C
(S)-1-((6-(2,5-difluorophenyl)-4-((3- (trifluoromethyl)phenyl)sulfonyl)- 3,4-dihydro-2H-benzo[b][1,4]- oxazin-2-yl)methyl)-3-methylene- cyclobutane-l-carboxylic acid
89D
(1r,3R)-1-(((S)-6-(2,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-3- hydroxy-3-(hydroxymethyl)- cyclobutane-l-carboxylic acid
89E
(1s,3S)-1-(((S)-6-(2,5-difluoro- phenyl)-4-((3-(trifluoromethyl)- phenyl)sulfonyl)-3,4-dihydro-2H- benzo[b][1,4]oxazin-2-yl)methyl)-3- hydroxy-3-(hydroxymethyl)- cyclobutane-l-carboxylic acid
TABLE 23A-I
Title Compound from
Example No.
Structure
13
16
17
18
32S
32T
32U
45D
49
50
52
53
54
55
56
57
58
59
61
62
63
64
65
67
68
69
70
71
72
73
74
75
82
84
85
87
.
31. The compound of claim 1 , wherein the compound is
32. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.
33. A pharmaceutical composition comprising a compound of claim 26 and a pharmaceutically acceptable carrier.
34. A pharmaceutical composition comprising a compound of claim 31 and a pharmaceutically acceptable carrier.
35. A method of treating a disorder selected from the group consisting of cancer, bacterial infection, fungal infection, and immune deficiency disorder, comprising administering a therapeutically effective amount of a compound of claim 1 to a subject in need thereof to ameliorate a symptom of the disorder.
36. The method of claim 35 , wherein the disorder is cancer.
37. The method of claim 35 , wherein the disorder is colon cancer, pancreatic cancer, breast cancer, ovarian cancer, prostate cancer, squamous cell carcinoma, basal cell carcinoma, adenocarcinoma, sweat gland carcinoma, sebaceous gland carcinoma, lung cancer, leukemia, bladder cancer, stomach cancer, cervical cancer, testicular cancer, skin cancer, rectal cancer, thyroid cancer, kidney cancer, uterus cancer, espophagus cancer, liver cancer, an acoustic neuroma, oligodendroglioma, meningioma, neuroblastoma, or retinoblastoma.
38. The method of claim 37 , wherein the subject is a human.
39. The method of claim 35 , wherein the compound is
or a pharmaceutically acceptable salt thereof.
40. The method of claim 36 , wherein the compound is
or a pharmaceutically acceptable salt thereof.
41. The method of claim 37 , wherein the compound is
or a pharmaceutically acceptable salt thereof.
42. A method of promoting the activity of RORγ, comprising exposing a RORγ to an effective amount of a compound of claim 1 to promote the activity of said RORγ.
43. A method of increasing the amount of IL-17 in a subject, comprising administering to a subject an effective amount of a compound of claim 1 to increase the amount of IL-17 in the subject.
44. The method of claim 42 , wherein the compound is
or a pharmaceutically acceptable salt thereof.