Indoles having anti-diabetic activity
View Patent ↗Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
1. A compound of formula I:
or a pharmaceutically acceptable salt thereof, wherein:
R 1 is selected from
(a) —X-Aryl-Y—Z, and
(b) —X-Heteroaryl-Y—Z,
wherein Aryl and Heteroaryl are unsubstituted or substituted with 1–3 groups independently selected from A;
Aryl is phenyl or naphthyl;
Heteroaryl is a monocyclic or fused bicyclic aromatic ring structure containing 1–4 heteroatoms independently selected from N, O, and S(O) n , wherein the monocyclic ring or each ring of the bicyclic ring structure is a 5–6 membered ring;
X is selected from the group consisting of a bond, CH 2 , CH(CH 3 ), C(CH 3 ) 2 , and C 3 –C 6 cycloalkylidene;
Y is selected from the group consisting of —CH═CH—, —CH(OH)CH(OH)—, —OCR 7 R 8 —, —SCR 7 R 8 —, and —CH 2 CR 5 R 6 —;
Z is selected from the group consisting of —CO 2 H and tetrazole;
A is selected from the group consisting of C 1-4 alkyl, C 1-4 alkenyl, —OC 1-4 alkyl, and halogen, wherein alkyl, alkenyl, and —Oalkyl are each optionally substituted with 1–5 halogens;
R 5 , R 6 , R 7 , and R 8 are each independently selected from the group consisting of H, halogen, C 1 –C 5 alkyl, —OC 1 –C 5 alkyl, C 2 –C 5 alkenyl, —OC 2 –C 5 alkenyl, C 3-6 cycloalkyl, phenyl, and —CO 2 H, wherein C 1 –C 5 alkyl, —OC 1 –C 5 alkyl, C 2 –C 5 alkenyl, —OC 2 –C 5 alkenyl, C 3-6 cycloalkyl, and phenyl are optionally substituted with 1–5 halogens, and C 3-6 cycloalkyl and phenyl are further optionally substituted with 1–3 groups independently selected from C 1 –C 3 alkyl and —OC 1 –C 3 alkyl, said C 1 –C 3 alkyl and —OC 1 –C 3 alkyl being optionally substituted with 1–3 halogens;
Or alternatively R 7 and R 8 may be joined to form a C 3 –C 6 cycloalkyl group, said C 3 –C 6 cycloalkyl group being optionally substituted with 1–3 halogens;
Or alternatively, when R 1 is —X-Phenyl-Y—Z, Y is —OCR 7 R 8 , and R 7 is selected from the group consisting of H, halogen, C 1 –C 5 alkyl, —OC 1 –C 5 alkyl, C 2-5 alkyl, —OC 2-5 alkyl, C 3-6 cycloalkyl, and phenyl, then R 8 may optionally be a 1–2-carbon bridge connected to the phenyl ring at the position ortho to Y, thereby yielding a 5 or 6-membered heterocyclic ring fused to the phenyl ring;
R 2 is C 1 –C 4 alkyl, which is optionally substituted with 1–5 halogens;
R 3 is selected from the group consisting of
(a) benzisoxazolyl,
(b) benzisothiazolyl,
(c) benzpyrazolyl,
(d) Aryl
(e) —C(═O)Aryl,
(f) —C(═O)Heteroaryl,
(g) —OAryl,
(h) —OHeteroaryl,
(i) —S(O) n Aryl, and
(j) —S(O) n Heteroaryl,
wherein R 3 is optionally substituted with 1–3 substituent groups independently selected from halogen, C 1-3 alkyl, —OC 1-3 alkyl, and —SC 1-3 alkyl, wherein C 1-3 alkyl, —OC 1-3 alkyl, and —SC 1-3 alkyl are optionally substituted with 1–5 halogens;
each R 4 is optionally selected from H, halogen, C 1 –C 5 alkyl and —OC 1 –C 5 alkyl, wherein C 1 –C 5 alkyl and —OC 1 –C 5 alkyl are optionally substituted with 1–5 halogens;
n is an integer from 0–2; and
p is an integer from 1 to 3.
2. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 3 is selected from the group consisting of 3-benzisoxazolyl, —O-Phenyl, and —C(═O)Phenyl, wherein R 3 is optionally substituted with 1–3 substituents independently selected from halogen, —OC 1 –C 3 alkyl, and C 1-3 alkyl, wherein said —OC 1 –C 3 alkyl and C 1 –C 3 alkyl are optionally substituted with 1–5 halogens.
3. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is —X-Phenyl-Y—Z, wherein Phenyl is unsubstituted or substituted with 1–3 groups independently selected from A.
4. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein X is a bond.
5. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein X is CH 2 .
6. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein Y is —OCR 7 R 8 —, R 7 is selected from the group consisting of H and C 1 –C 3 alkyl, and R 8 is C 1 –C 3 alkyl, wherein R 7 and R 8 are optionally substituted with 1–3 halogens.
7. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein Y is —OCR 7 R 8 —, R 7 is selected from the group consisting of H and C 1 –C 3 alkyl, and R 8 is C 1 –C 3 alkyl.
8. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein Y is —CH 2 CHR 6 —, wherein R 6 is selected from the group consisting of C 1-3 alkyl and —OC 1-3 alkyl, which are optionally substituted with 1–3 halogens.
9. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein A is selected from the group consisting of C 1 –C 3 alkyl, CF 3 , —OCH 3 , —OCF 3 , and halogen.
10. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 2 is selected from C 1-3 alkyl and CF 3 .
11. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 3 is —C(═O)Phenyl, wherein R 3 is optionally substituted with 1–3 substituents independently selected from the group consisting of —OCH 3 , —OCF 3 , and halogen.
12. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein p is 1.
13. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein Z is —CO 2 H.
14. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is
wherein X is selected from the group consisting of a bond, CH 2 , CH(CH 3 ), C(CH 3 ) 2 , and C 3 –C 6 cycloalkylidene;
Y is selected from the group consisting of —OCR 7 R 8 — and CH 2 CR 5 R 6 ;
Z is selected from —CO 2 H and tetrazole;
A is selected from the group consisting of C 1 –C 3 alkyl, CF 3 , —OCH 3 , —OCF 3 , and halogen;
R 5 , R 6 , and R 7 are each independently selected from the group consisting of H, halogen, C 1 –C 3 alkyl, and —OC 1 –C 3 alkyl, and R 8 is selected from the group consisting of halogen, C 1 –C 3 alkyl, and —OC 1 –C 3 alkyl, wherein C 1 –C 3 alkyl and —OC 1 –C 3 alkyl of R 5 , R 6 , R 7 , and R 8 are each optionally substituted with 1–3 halogens;
q is an integer from 0–3;
p is 1;
R 2 is selected from CF 3 and C 1 –C 3 alkyl;
R 3 is selected from the group consisting of
(a) 3-benzisoxazolyl,
(b) 3-benzisothiazolyl,
(c) 3-benzpyrazolyl,
(d) Aryl
(e) —C(═O)Phenyl,
(f) —C(═O)Heteroaryl,
(g) —OPhenyl,
(h) —OHeteroaryl,
(i) —S(O) n Phenyl, and
(j) —S(O) n Heteroaryl,
wherein Heteroaryl is selected from the group consisting of pyridyl and quinolyl,
n is an integer from 0–2, and
R 3 is optionally substituted with 1–3 groups independently selected from halogen, —OC 1 –C 3 alkyl, and C 1-3 alkyl, wherein said —OC 1 –C 3 alkyl and C 1 –C 3 alkyl are optionally substituted with 1–5 halogens.
15. The compound according to claim 14 , or a pharmaceutically acceptable salt thereof, wherein
X is selected from a bond and CH 2 ;
Y is selected from the group consisting of —OCR 7 R 8 — and —CH 2 CR 5 R 6 —;
Z is —CO 2 H;
A is selected from the group consisting of CH 3 , CF 3 , —OCH 3 , —OCF 3 , and halogen;
R 5 is H;
R 6 is selected from the group consisting of H, C 1 –C 3 alkyl, and —OC 1 –C 3 alkyl, wherein C 1 –C 3 alkyl, and —OC 1 –C 3 alkyl are optionally substituted with 1–3 halogens;
R 7 is selected from the group consisting of H and C 1 –C 3 alkyl;
R 8 is C 1 –C 3 alkyl;
R 2 is CH 3 ;
R 3 is selected from the group consisting of
(a) 3-benzisoxazolyl,
(b) Aryl,
(c) —C(═O)Phenyl,
(d) —C(═O)Pyridyl, and
(e) —C(═O)Quinolyl,
wherein R 3 is optionally substituted with 1–3 groups independently selected from halogen, —OC 1 –C 3 alkyl, and C 1-3 alkyl, wherein said —OC 1 –C 3 alkyl and C 1 –C 3 alkyl are optionally substituted with 1–5 halogens; and
q is an integer from 0–3.
16. The compound according to claim 15 , or a pharmaceutically acceptable salt thereof, wherein q is 0 or 1, and X and YZ are meta or para to each other.
17. The compound according to claim 1 , said compound having Formula 1A, or a pharmaceutically acceptable salt thereof:
wherein X is selected from a bond and CH 2 ;
Y is selected from the group consisting of —OCR 7 R 8 — and —CH 2 CR 5 R 6 —;
Z is —CO 2 H;
A is selected from the group consisting of CH 3 , CF 3 , —OCH 3 , —OCF 3 , and halogen;
q is 0 or 1;
R 4 is selected from the group consisting of C 1-3 alkyl, CF 3 , —OCH 3 , and —OCF 3 ;
p is 0 or 1;
R 5 is selected from the group consisting of H and C 1 –C 3 alkyl, wherein C 1 –C 3 alkyl is optionally substituted with 1–3 halogens;
R 6 is selected from the group consisting of C 1 –C 3 alkyl and —OC 1 –C 3 alkyl, wherein C 1 –C 3 alkyl, and —OC 1 –C 3 alkyl are optionally substituted with 1–3 halogens;
R 7 is selected from the group consisting of H and C 1 –C 3 alkyl, which is optionally substituted with 1–3 halogens;
R 8 is C 1 –C 3 alkyl, which is optionally substituted with 1–3 halogens;
R 2 is CH 3 ; and
R 3 is selected from the group consisting of
(a) 3-benzisoxazolyl,
(b) —O-Phenyl, and
(c) —C(═O)Phenyl,
wherein R 3 is optionally substituted with 1–3 groups independently selected from halogen, —OC 1 –C 3 alkyl, and C 1-3 alkyl, wherein said —OC 1 –C 3 alkyl and C 1 –C 3 alkyl are optionally substituted with 1–5 halogens.
18. The compound according to claim 17 , or a pharmaceutically acceptable salt thereof, wherein X is a bond;
Y is —OC*R 7 R 8 —, wherein C* is an asymmetric carbon atom;
R 4 is selected from the group consisting of CH 3 , CF 3 , —OCH 3 , and —OCF 3 ;
R 7 is H; and
R 8 is C 1 –C 3 alkyl, which is optionally substituted with 1–3 halogens.
19. The compound according to claim 18 , or a pharmaceutically acceptable salt thereof, wherein the carbon atom C* of said group Y has the R stereochemical configuration.
20. The compound according to claim 18 , or a pharmaceutically acceptable salt thereof, wherein the carbon atom C* of said group Y has the S stereochemical configuration.
21. The compound according to claim 18 , or a pharmaceutically acceptable salt thereof, wherein R 3 is —C(═O)Phenyl, which is optionally substituted with 1–2 substituents independently selected from the group consisting of Cl, CH 3 , CF 3 , —OCH 3 , and —OCF 3 .
22. The compound according to claim 17 , or a pharmaceutically acceptable salt thereof, wherein X is CH 2 ;
Y is —OC*R 7 R 8 —, wherein C* is an asymmetric carbon atom;
R 4 is selected from the group consisting of CH 3 , CF 3 , —OCH 3 , and —OCF 3 ;
R 7 is H; and
R 8 is C 1 –C 3 alkyl, which is optionally substituted with 1–3 halogens.
23. The compound according to claim 22 , or a pharmaceutically acceptable salt thereof, wherein the carbon atom C* of said group Y has the R stereochemical configuration.
24. The compound according to claim 22 , or a pharmaceutically acceptable salt thereof, wherein the carbon atom C* of said group Y has the S stereochemical configuration.
25. The compound according to claim 22 , or a pharmaceutically acceptable salt thereof, wherein R 3 is —C(═O)Phenyl, which is optionally substituted with 1–2 substituents independently selected from the group consisting of Cl, CH 3 , CF 3 , —OCH 3 , and —OCF 3 .
26. The compound according to claim 1 as named below, or a pharmaceutically acceptable salt thereof:
I
1
(2R)-2-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
2
(2R)-2-(3-{[2-methyl-3-(phenylthio)-1H-indol-1-yl]methyl}phenoxy)butanoic acid
3
(2S)-2-(2-chloro-5-{[2-methyl-3-(phenylthio)-1H-indol-1-yl]methyl}phenoxy)propanoic
acid
4
(2R)-2-(4-chloro-3-{[2-methyl-3-(phenylthio)-1H-indol-1-yl]methyl}phenoxy)propanoic
acid
5
2-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
6
2-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
7
(2S)-2-(3-{[3-[(4-chlorophenyl)thio]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
8
2-(3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
9
2-(3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
10
(2S)-2-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
11
2-(3-{[3-(4-chlorophenoxy)-6-methoxy-2-methyl-1H-indol-1-yl]methyl}phenoxy)butanoic
acid
12
2-(3-{[3-(4-chlorophenoxy)-6-methoxy-2-methyl-1H-indol-1-yl]methyl}phenoxy)butanoic
acid
13
2-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
14
2-(3-{[3-(4-chlorophenoxy)-6-isopropyl-2-methyl-1H-indol-1-yl]methyl}phenoxy)butanoic
acid
15
2-(3-{[3-(4-chlorophenoxy)-6-isopropyl-2-methyl-1H-indol-1-yl]methyl}phenoxy)butanoic
acid
16
(2R)-2-(3-{[3-(4-methoxyphenoxy)-2-methyl-4-(trifluoromethoxyl)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
17
(2S)-2-(3-{[3-(4-methoxyphenoxy)-2-methyl-4-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
18
(2R)-2-(3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
19
(2S)-2-(3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
20
(2R)-2-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
21
2-(3-{[3-(4-chlorophenoxy)-2-methyl-4-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
22
2-(3-{[3-(4-chlorophenoxy)-2-methyl-4-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
23
2-(3-{[3-(4-chlorophenoxy)-6-fluoro-2-methyl-1H-indol-1-yl]methyl}phenoxy)butanoic
acid
24
2-(3-{[3-(4-chlorophenoxy)-6-fluoro-2-methyl-1H-indol-1-yl]methyl}phenoxy)butanoic
acid
25
2-(3-{[3-(4-chlorophenoxy)-4-fluoro-2-methyl-1H-indol-1-yl]methyl}phenoxy)butanoic
acid
26
2-(3-{[3-(4-chlorophenoxy)-4-fluoro-2-methyl-1H-indol-1-yl]methyl}phenoxy)butanoic
acid
27
2-(3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
28
2-(3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
29
2-(3-{[3-(4-methoxyphenoxy)-2-methyl-4-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
30
2-(3-{[3-(4-methoxyphenoxy)-2-methyl-4-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
31
2-(3-{[3-(4-methoxyphenoxy)-2-methyl-4-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
32
2-(3-{[3-(4-methoxyphenoxy)-2-methyl-4-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
33
2-(3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
34
2-(3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
35
2-(4-chloro-3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-methylpropanoic acid
36
2-(2-chloro-5-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-methylbutanoic acid
37
2-(4-chloro-3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)-2-methylpropanoic acid
38
(2S)-2-(2-chloro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
39
(2S)-2-(4-chloro-3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
40
2-(2-chloro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
41
2-(2-chloro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)-2-methylbutanoic acid
42
2-(2-fluoro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
43
2-(2-fluoro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
44
2-(2-chloro-5-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
45
2-(2-chloro-5-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
46
(2S)-2-(2-fluoro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
47
(2R)-2-(2-chloro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
48
(2R)-2-(4-fluoro-3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
49
(2S)-2-(4-fluoro-3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
50
(2R)-2-(2-fluoro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
51
(2S)-2-(4-chloro-3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
52
2-(4-chloro-3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
53
2-(5-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-2-
fluorophenoxy)butanoic acid
54
(2S)-2-(3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
55
2-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-methylpropanoic acid
56
(2R)-2-(2-chloro-5-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
57
2-(4-chloro-3-{[3-[(4-chlorophenyl)thio]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-methylpropanoic acid
58
2-(4-chloro-3-{[3-[(4-chlorophenyl)thio]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
59
2-(4-chloro-3-{[3-[(4-chlorophenyl)thio]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
60
2-{3-[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}butanoic acid
61
2-{3-[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}butanoic acid
62
(2R)-2-(3-{[3-[(4-chlorophenyl)thio]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
63
2-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
64
2-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
65
3-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenyl)-
2-(2,2,2-trifluoroethoxy)propanoic acid
66
2-(2-chloro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
67
2-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-yl]methyl}phenoxy)-
2-methylpropanoic acid
68
2-(2-chloro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
69
2-(2-fluoro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
70
2-(2-fluoro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
71
2-(2-fluoro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
72
2-(2-fluoro-5-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
73
(2S)-2-(3-{[3-[(4-chlorophenyl)thio]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-
4-fluorophenoxy)propanoic acid
74
(2R)-2-(3-{[3-[(4-chlorophenyl)thio]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-
4-fluorophenoxy)propanoic acid
75
(2S)-2-(5-{[3-[(4-chlorophenyl)thio]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-
2-fluorophenoxy)propanoic acid
76
(2R)-2-(5-{[3-[(4-chlorophenyl)thio]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-
2-fluorophenoxy)propanoic acid
77
(2S)-2-(2-chloro-5-{[3-[(4-chlorophenyl)thio]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
78
(2R)-2-(2-chloro-5-{[3-[(4-chlorophenyl)thio]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
79
2-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-yl]methyl}phenoxy)-
3-methylbutanoic acid
80
2-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-yl]methyl}phenoxy)-
3-methylbutanoic acid
81
2-(3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)-2-methylpropanoic acid
82
(2R)-2-(3-{[3-(4-chlorophenoxy)-5-iodo-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
83
2-(3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)-2-methylbutanoic acid
84
2-(3-{[3-(4-methoxyphenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)-2-methylbutanoic acid
85
(2R)-2-(3-{[3-[(4-chlorophenyl)sulfinyl]-2-methyl-5-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
86
2-{3-[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]phenoxy}-2-
methylpropanoic acid
87
(2S)-2-(3-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-yl]methyl}-4-
fluorophenoxy)propanoic acid
88
(2S)-2-(2-chloro-5-{[3-(4-chlorophenoxy)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
II
1
(2S)-2-(3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-
1-yl]methyl}phenoxy)propanoic acid
2
(2S)-2-(3-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
3
(2R)-2-(3-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
4
(2R)-2-(3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-
1-yl]methyl}phenoxy)propanoic acid
5
(2S)-2-(3-{[3-(7-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-
1-yl]methyl}phenoxy)propanoic acid
6
(2R)-2-(3-{[3-(7-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-
1-yl]methyl}phenoxy)propanoic acid
7
(2R)-2-(2-chloro-5-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-
1H-indol-1-yl]methyl}phenoxy)propanoic acid
8
(2R)-2-(4-chloro-3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-
1H-indol-1-yl]methyl}phenoxy)propanoic acid
9
(2S)-2-(2-chloro-5-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-
1H-indol-1-yl]methyl}phenoxy)propanoic acid
10
(2S)-2-{3-[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
11
(2R)-2-{3-[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}butanoic acid
12
(2R)-2-{3-[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
13
(2S)-2-{3-[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}butanoic acid
14
(2S)-2-(3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-
1-yl]methyl}phenoxy)butanoic acid
15
(2R)-2-(3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-
1-yl]methyl}phenoxy)butanoic acid
16
(2R)-2-(3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-
1-yl]methyl}phenoxy)-3-methylbutanoic acid
17
(2S)-2-(4-chloro-3-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-
indol-1-yl]methyl}phenoxy)propanoic acid
18
(2S)-2-(2-chloro-5-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-
indol-1-yl]methyl}phenoxy)propanoic acid
19
(2R)-2-(4-chloro-3-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-
indol-1-yl]methyl}phenoxy)propanoic acid
20
(2S)-2-(3-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
21
(2R)-2-(3-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
22
(2S)-2-(4-chloro-3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-
1H-indol-1-yl]methyl}phenoxy)propanoic acid
23
(2S)-2-(3-{[3-(5-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-
1-yl]methyl}phenoxy)propanoic acid
24
(2R)-2-(3-{[3-(5-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-
1-yl]methyl}phenoxy)propanoic acid
25
(2R)-2-(4-chloro-3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-
1H-indol-1-yl]methyl}phenoxy)butanoic acid
26
(2S)-2-(4-chloro-3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-
1H-indol-1-yl]methyl}phenoxy)butanoic acid
27
2-(3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
28
2-(3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
29
(2S)-2-(3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-
1-yl]methyl}phenoxy)-3-methylbutanoic acid
30
(2R)-2-(2-chloro-5-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-
indol-1-yl]methyl}phenoxy)propanoic acid
31
(2S)-2-(4-chloro-3-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-
indol-1-yl]methyl}phenoxy)butanoic acid
32
(2R)-2-(4-chloro-3-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-
indol-1-yl]methyl}phenoxy)butanoic acid
33
(2S)-2-(5-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}-2-fluorophenoxy)propanoic acid
34
(2R)-2-(5-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}-2-fluorophenoxy)propanoic acid
35
(2S)-2-(3-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}-4-fluorophenoxy)propanoic acid
36
(2R)-2-(3-{[3-(6-chloro-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}-4-fluorophenoxy)propanoic acid
37
(2S)-2-(2-fluoro-5-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-
1H-indol-1-yl]methyl}phenoxy)propanoic acid
38
(2R)-2-(2-fluoro-5-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-
1H-indol-1-yl]methyl}phenoxy)propanoic acid
39
2-(4-chloro-3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-
indol-1-yl]methyl}phenoxy)-2-methylpropanoic acid
40
(2S)-2-(4-fluoro-3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-
1H-indol-1-yl]methyl}phenoxy)propanoic acid
41
(2R)-2-(4-fluoro-3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-
1H-indol-1-yl]methyl}phenoxy)propanoic acid
42
2-(2-chloro-5-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-
indol-1-yl]methyl}phenoxy)pentanoic acid
43
2-(2-chloro-5-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-
indol-1-yl]methyl}phenoxy)pentanoic acid
44
2-(4-chloro-3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-
indol-1-yl]methyl}phenoxy)pentanoic acid
45
2-(4-chloro-3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-
indol-1-yl]methyl}phenoxy)pentanoic acid
46
2-(4-chloro-3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-
indol-1-yl]methyl}phenoxy)-3-methylbutanoic acid
47
2-(4-chloro-3-{[3-(6-methoxy-1,2-benzisoxazol-3-yl)-2-methyl-6-(trifluoromethoxy)-1H-
indol-1-yl]methyl}phenoxy)-3-methylbutanoic acid
III
1
(2S)-2-(3-{[3-(4-methoxybenzoyl)-2-methyl-1H-indol-1-yl]methyl}phenoxy)propanoic
acid
2
(2S)-2-(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
3
(2S)-2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
4
(2S)-2-(3-{[3-(4-methoxybenzoyl)-2-methyl-5-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
5
(2R)-2-(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
6
(2S)-2-{3-[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
7
2-(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-methylpropanoic acid
8
2-{3-[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]phenoxy}-2-
methylpropanoic acid
9
3-(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenyl)propanoic acid
10
2-ethoxy-3-(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenyl)propanoic acid
11
3-(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenyl)
2-(2,2,2-trifluoroethoxy)propanoic acid
12
2-{3-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]phenoxy}-2-
methylpropanoic acid
13
2-{3-[3-[(6-chloropyridin-3-yl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}-2-methylpropanoic acid
14
2-{3-[3-[(6-ethoxypyridin-3-yl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}-2-methylpropanoic acid
15
3-{3-[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenyl}propanoic acid
16
3-{3-[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]phenyl}-2-
(2,2,2-trifluoroethoxy)propanoic acid
17
2-{3-[3-[(2-chloropyridin-3-yl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}-2-methylpropanoic acid
18
2-methyl-2-{3-[2-methyl-3-[(6-methylpyridin-2-yl)carbonyl]-6-(trifluoromethoxy)-1H-
indol-1-yl]phenoxy}propanoic acid
19
2-methyl-2-{3-[2-methyl-3-(quinolin-2-ylcarbonyl)-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
20
3-{3-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]phenyl}-2-(2,2,2-
trifluoroethoxy)propanoic acid
21
2-{3-[3-(2-chloro-6-methylisonicotinoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}-2-methylpropanoic acid
22
2-{3-[3-(isoquinolin-1-ylcarbonyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]phenoxy}-
2-methylpropanoic acid
23
(2S)-2-(2-chloro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
24
(2S)-2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-4-
propylphenoxy)propanoic acid
25
(2R)-2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-4-
propylphenoxy)propanoic acid
26
(2S)-2-(2-chloro-5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
27
(2S)-2-{2-chloro-5-[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
28
(2R)-2-(2-chloro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
29
(2R)-2-(2-chloro-5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
30
(2S)-2-(4-chloro-3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
31
(2S)-2-(4-chloro-3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
32
(2R)-2-{2-chloro-5-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
33
(2S)-2-{2-chloro-5-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
34
(2R)-2-(4-chloro-3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
35
(2R)-2-(4-chloro-3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
36
(2S)-2-(3-{1-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]ethyl}phenoxy)propanoic acid
37
(2S)-2-(3-{[3-(2,4-dichlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
38
(2R)-2-(3-{[3-(2,4-dichlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
39
2-ethyl-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-
2,3-dihydro-1-benzofuran-2-carboxylic acid
40
5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-2-ethyl-2,3-
dihydro-1-benzofuran-2-carboxylic acid
41
6-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-2-
methylchromane-2-carboxylic acid
42
(2S)-2-{3-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
43
(2R)-2-{3-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
44
6-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-2-
methylchromane-2-carboxylic acid
45
(2S)-2-(3-{[3-(4-chloro-2-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
46
(2R)-2-(3-{[3-(4-chloro-2-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
47
(2S)-2-(3-{[3-(4-chloro-2-methylbenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
48
(2R)-2-(3-{[3-(4-chloro-2-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
49
(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)(cyclohexyl)acetic acid
50
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
51
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-
4-methylpentanoic acid
52
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
53
(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)(phenyl)acetic acid
54
1-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)cyclobutanecarboxylic acid
55
(2R)-2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
56
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-
3-methylbutanoic acid
57
(2S)-2-(3-{[3-(4-methoxy-2-methylbenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
58
(2R)-2-(3-{[3-(4-methoxy-2-methylbenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
59
(2S)-2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
60
(2R)-2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
61
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
62
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
63
(2R)-2-ethyl-7-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}chromane-2-carboxylic acid
64
(2R)-7-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-2-
ethylchromane-2-carboxylic acid
65
(2R)-7-{[3-(2,4-dichlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-2-
ethylchromane-2-carboxylic acid
66
(2S)-2-ethyl-7-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}chromane-2-carboxylic acid
67
(2S)-7-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-2-
ethylchromane-2-carboxylic acid
68
(2S)-2-(3-{[2-methyl-3-(2,4,6-trichlorobenzoyl)-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
69
(2R)-2-(3-{[2-methyl-3-(2,4,6-trichlorobenzoyl)-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
70
(2S)-2-{3-[2-methyl-3-(quinolin-2-ylcarbonyl)-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
71
(2R)-2-{3-[2-methyl-3-(quinolin-2-ylcarbonyl)-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
72
2-{3-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]phenoxy}butanoic
acid
73
2-(3-{[3-(2,4-dichlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
74
2-(3-{[3-(2,4-dichlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
75
2-(3-{[3-(2,4-dichlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
76
2-(3-{[3-(2,4-dichlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
77
2-{3-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}pentanoic acid
78
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-
3-methylbutanoic acid
79
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-
3-methylbutanoic acid
80
2-(4-chloro-3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
81
2-(2-chloro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
82
2-(2-chloro-5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
83
2-(4-chloro-3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
84
2-(2-chloro-5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
85
2-(4-chloro-3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
86
2-(4-chloro-3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
87
2-(4-chloro-3-{[3-(2,4-dichlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
88
2-(4-chloro-3-{[3-(2,4-dichlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
89
(2R)-2-(3-{[3-(2-chloro-4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
90
(2S)-2-(3-{[3-(2-chloro-4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
91
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-
2-methylbutanoic acid
92
2-(3-{[3-(4-chlorobenzoyl)-2-ethyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-2-
methylbutanoic acid
93
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-
2-methylpentanoic acid
94
2-(2-chloro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-methylbutanoic acid
95
2-(2-chloro-5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-methylbutanoic acid
96
2-(2-chloro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-methylpentanoic acid
97
2-(2-chloro-5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-methylpentanoic acid
98
2-(2-chloro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-ethylbutanoic acid
99
2-(2-chloro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-ethylpentanoic acid
100
2-(2-chloro-5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-ethylbutanoic acid
101
2-(2-chloro-5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-ethylpentanoic acid
102
2-(3-{[3-(2,4-dichlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-3,3,3-trifluoropropanoic acid
103
2-(3-{[3-(2-chloro-4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
104
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-
2-methylbutanoic acid
105
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-
2-methylbutanoic acid
106
2-(2-chloro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
107
2-(2-chloro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
108
2-(2-fluoro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
109
2-(2-fluoro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
110
2-(2-fluoro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)pentanoic acid
111
(4-chlorophenyl)[2-methyl-1-{3-[(1S)-1-(2H-tetrazol-5-yl)ethoxy]benzyl}-6-
(trifluoromethoxy)-1H-indol-3-yl]methanone
112
2-(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}benzyl)butanoic acid
113
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}benzyl)butanoic acid
114
(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}benzyl)(methyl)malonic acid
115
3-(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenyl)
2-phenylpropanoic acid
116
3-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenyl)-2-
phenylpropanoic acid
117
2-(2-fluoro-5-{[3-(4-methoxybezoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
118
2-(5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-2-
fluorophenoxy)-3-methylbutanoic acid
119
2-(2-chloro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
120
2-(2-chloro-5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
121
3-(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenyl)
2-methylpropanoic acid
122
3-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenyl)-2-
methylpropanoic acid
123
2-(5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-2-
fluorophenoxy)pentanoic acid
124
(2S)-2-{5-[3-[4-(ethylthio)benzoyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]-2-
fluorophenoxy}propanoic acid
125
(2R)-2-(3-{[3-(4-fluorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
126
(2R)-2-[3-({2-methyl-6-(trifluoromethoxy)-3-[4-(trifluoromethoxy)benzoyl]-1H-indol-1-
yl}methyl)phenoxy]propanoic acid
127
(2E)-3-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenyl)acrylic acid
128
(2S,3R)-3-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenyl)-2,3-dihydroxypropanoic acid
129
(4-chlorophenyl)[2-methyl-1-{3-[1-(2H-tetrazol-5-yl)propoxy]benzyl}-6-
(trifluoromethoxy)-1H-indol-3-yl]methanone
130
(2R)-2-(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
131
2-(2-fluoro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
132
2-(2-fluoro-5-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
133
2-(5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-2-
fluorophenoxy)butanoic acid
134
2-(5-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-2-
fluorophenoxy)butanoic acid
135
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-
4,4,4-trifluorobutanoic acid
136
(2R)-2-(3-{[3-(4-chlorobenzoyl)-2-ethyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
137
(2S)-2-(3-{[3-(4-chlorobenzoyl)-2-ethyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
138
2-{-5-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]-2-fluorophenoxy}
2-methylpropanoic acid
139
(2S)-2-{5-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]-2-
fluorophenoxy}propanoic acid
140
(2R)-2-{5-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]-2-
fluorophenoxy}propanoic acid
141
2-(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-methylbutanoic acid
142
2-(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-2-methylpentanoic acid
143
2-(3-{[3-(4-chlorobenzoyl)-2-ethyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-3-
methylbutanoic acid
144
2-(3-{[3-(4-chlorobenzoyl)-2-isopropyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
145
2-(3-{[3-(4-chlorobenzoyl)-2-propyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
146
2-(3-{[3-(4-chlorobenzoyl)-2-propyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
147
2-(3-{[3-(4-chlorobenzoyl)-2-propyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-
3-methylbutanoic acid
148
2-(3-{[3-(4-chlorobenzoyl)-2-propyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-
3-methylbutanoic acid
149
2-(3-{[3-(4-chlorobenzoyl)-2-ethyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-3-
methylbutanoic acid
150
2-(3-{[3-(4-chlorobenzoyl)-2-ethyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-3-
methylbutanoic acid
151
2-(3-{[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}-4-
fluorophenoxy)-4,4,4-trifluorobutanoic acid
152
2-{3-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]-5-fluorophenoxy}
2-methylpropanoic acid
153
(2S)-2-{3-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]-5-
fluorophenoxy}propanoic acid
154
(2R)-2-{3-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]-5-
fluorophenoxy}propanoic acid
155
2-({6-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]pyridin-2-yl}oxy)-
2-methylpropanoic acid
156
2-(3-{[3-(4-chlorobenzoyl)-2-(methoxymethyl)-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
157
2-(3-{[3-(4-chlorobenzoyl)-2-(chloromethyl)-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
158
2-(3-{[3-(4-chlorobenzoyl)-2-(hydroxymethyl)-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
159
2-(3-{[2-(bromomethyl)-3-(4-chlorobenzoyl)-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
160
2-[3-({2-methyl-6-(trifluoromethoxy)-3-[4-(trifluoromethoxy)benzoyl]-1H-indol-1-
yl}methyl)phenoxy]butanoic acid
161
2-[3-({2-methyl-6-(trifluoromethoxy)-3-[4-(trifluoromethoxy)benzoyl]-1H-indol-1-
yl}methyl)phenoxy]butanoic acid
162
3-methyl-2-[3-({2-methyl-6-(trifluoromethoxy)-3-[4-(trifluoromethoxy)benzoyl]-1H-indol-
1-yl}methyl)phenoxy]butanoic acid
163
3-methyl-2-[3-({2-methyl-6-(trifluoromethoxy)-3-[4-(trifluoromethoxy)benzoyl]-1H-indol-
1-yl}methyl)phenoxy]butanoic acid
164
(2R)-2-(3-{[3-(4-chlorobenzoyl)-2-methyl-1H-indol-1-yl]methyl}phenoxy)propanoic acid
165
(2S)-2-(3-{[3-(4-chlorobenzoyl)-2-methyl-1H-indol-1-yl]methyl}phenoxy)propanoic acid
166
(2R)-2-(3-{[3-(4-methoxybenzoyl)-2-methyl-1H-indol-1-yl]methyl}phenoxy)propanoic
acid
167
2-(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}benzyl)butanoic acid
168
2-({6-[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]pyridin-2-
yl}oxy)-2-methylpropanoic acid
169
(2R)-2-(3-{[3-(4-chlorobenzoyl)-2-(chloromethyl)-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
170
(2R)-2-(3-{[3-(4-chlorobenzoyl)-2-(fluoromethyl)-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
171
2-[(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenyl)sulfinyl]-2-methylpropanoic acid
172
2-[(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenyl)sulfonyl]-2-methylpropanoic acid
173
2-[(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenyl)thio]-2-methylpropanoic acid
174
2-[(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenyl)thio]propanoic acid
175
2-[(3-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenyl)thio]propanoic acid
176
(2R)-2-{3-[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}butanoic acid
177
(2R)-2-{3-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}butanoic acid
178
(2R)-2-{3-fluoro-5-[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
179
(2R)-2-{3-[3-(4-chlorobenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]-5-
fluorophenoxy}butanoic acid
180
(2S)-2-(2-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
181
(2S)-2-(2-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
182
2-(2-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-2-
methylpropanoic acid
183
(2R)-2-(2-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
184
(2S)-2-(2-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
185
(2S)-2-(4-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
186
(2R)-2-(4-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
187
2-(4-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-2-
methylpropanoic acid
188
(2R)-2-(4-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
189
2-(4-{[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-2-
methylpropanoic acid
IV
1
(2S)-2-(3-{[3-(4-methoxyphenyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
2
(2R)-2-(3-{[3-(4-methoxyphenyl)-2-methyl-6-(trifluromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
3
2-(3-{[3-(4-methoxyphenyl)-2-methyl-6-(trifluromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
4
2-(3-{[3-(4-methoxyphenyl)-2-methyl-6-(trifluromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
5
(2S)-2-(3-{[3-(4-methoxyphenyl)-2-methyl-4-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
6
(2R)-2-(3-{[3-(4-methoxyphenyl)-2-methyl-4-(trifluromethoxy)-1H-indol-1-
yl]methyl}phenoxy)propanoic acid
7
2-(3-{[3-(4-methoxyphenyl)-2-methyl-4-(trifluromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
8
2-(3-{[3-(4-methoxyphenyl)-2-methyl-4-(trifluromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
9
2-(3-{[3-(4-methoxyphenyl)-2-methyl-6-(trifluromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
10
2-(3-{[3-(4-methoxyphenyl)-2-methyl-6-(trifluromethoxy)-1H-indol-1-
yl]methyl}phenoxy)-3-methylbutanoic acid
11
2-(3-{[3-(4-methoxyphenyl)-6-(trifluoromethoxy)-2-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
12
2-(3-{[3-(4-methoxyphenyl)-6-(trifluoromethoxy)-2-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
13
2-(2-chloro-5-{[3-(4-methoxyphenyl)-6-(trifluoromethoxy)-2-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
14
(2S)-2-(3-{[3-(4-chlorophenyl)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
15
(2S)-2-(3-{[3-(4-chlorophenyl)-2-methyl-4-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
16
(2S)-2-{3-[3-(4-chlorophenyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
17
(2R)-2-{3-[3-(4-chlorophenyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]phenoxy}propanoic acid
18
2-(3-{[3-(4-chlorophenyl)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
19
2-(3-{[3-(4-chlorophenyl)-2-methyl-6-(trifluoromethyl)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
20
2-(3-{[3-(4-chlorophenyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-
yl]methyl}phenoxy)butanoic acid
21
2-(3-{[3-(4-chlorophenyl)-2-methyl-6-(trifluoromethyl)-1H-indol-1-yl]methyl}phenoxy)-2-
methylpropanoic acid
22
2-(3-{[3-(4-chlorophenyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]methyl}phenoxy)-
2-methylpropanoic acid
23
2-{3-[3-(4-chlorophenyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]phenoxy}butanoic
acid
24
2-{3-[3-(4-chlorophenyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]phenoxy}butanoic
acid
27. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.
28. A method of treating one or more diseases, disorders, or conditions selected from the group consisting of (1) non-insulin dependent diabetes mellitus (NIDDM), (2) hyperglycemia, (3) low glucose tolerance, (4) insulin resistance, (5) obesity, (6) lipid disorders, (7) dyslipidemia, (8) hyperlipidemia, (9) hypertriglyceridemia, (10) hypercholesterolemia, (11) low HDL levels, (12) high LDL levels, (13) atherosclerosis and its sequelae, (14) vascular restenosis, (15) irritable bowel syndrome, (16) inflammatory bowel disease, (17) Crohn's disease, (18) ulcerative colitis, (19) abdominal obesity, (20) retinopathy, (21) psoriasis, (22) high blood pressure, (23) metabolic syndrome, (24) ovarian hyperandrogenism (polycystic ovarian syndrome), and other diseases, disorders or conditions where insulin resistance is a component, said method comprising the administration of an effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.
29. A method for treating non-insulin dependent (Type 2) diabetes mellitus in a patient in need of such treatment which comprises administering to said patient a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.
30. A method for treating hyperglycemia in a patient in need of such treatment which comprises administering to said patient a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.
31. A method for treating one or more diseases or conditions selected from the group consisting of hypercholesterolemia, atherosclerosis, low HDL levels, high LDL levels, hyperlipidemia, hypertriglyceridemia, and dyslipidemia, which method comprises administering to a patient in need of such treatment a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.
32. A method for treating obesity in a patient in need of such treatment which comprises administering to said patient a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.
33. A method for treating or reducing the risk of developing atherosclerosis in a patient in need of such treatment which comprises administering to said patient a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.
34. A method of treating one or more diseases, disorders, or conditions selected from the group consisting of (1) non-insulin dependent Type 2 diabetes mellitus (NIDDM), (2) hyperglycemia, (3) low glucose tolerance, (4) insulin resistance, (5) obesity, (6) lipid disorders, (7) dyslipidemia, (8) hyperlipidemia, (9) hypertriglyceridemia, (10) hypercholesterolemia, (11) low HDL levels, (12) high LDL levels, (13) atherosclerosis and its sequelae, (14) vascular restenosis, (15) irritable bowel syndrome, (16) inflammatory bowel disease, (17) Crohn's disease, (18) ulcerative colitis, (19) abdominal obesity, (20) retinopathy, (21) psoriasis, (22) high blood pressure, (23) metabolic syndrome, (24) ovarian hyperandrogenism (polycystic ovarian syndrome), and other diseases, disorders or conditions where insulin resistance is a component, said method comprising the administration of an effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and an effective amount of one or more other compounds selected from the group consisting of:
(1) PPAR gamma agonists and partial agonists;
(2) biguanides;
(3) protein tyrosine phosphatase-1B (PTP-1B) inhibitors;
(4) dipeptidyl peptidase IV (DP-IV) inhibitors;
(5) insulin or an insulin mimetic;
(6) sulfonylureas;
(7) α-glucosidase inhibitors;
(8) agents which improve a patient's lipid profile, said agents being selected from the group consisting of (a) HMG-CoA reductase inhibitors, (b) bile acid sequestrants, (c) nicotinyl alcohol, nicotinic acid or a salt thereof, (d) PPARα agonists, (e) cholesterol absorption inhibitors, (f) acyl CoA:cholesterol acyltransferase (ACAT) inhibitors, (g) CETP inhibitors, and (h) phenolic anti-oxidants;
(9) PPARα/γ dual agonists;
(10) PPARδ agonists;
(11) antiobesity compounds;
(12) ileal bile acid transporter inhibitors;
(13) anti-inflammatory agents;
(14) glucagon receptor antagonists;
(15) GLP-1;
(16) GIP-1; and
(17) GLP-1 analogs.
35. A method for treating one or more diseases or conditions selected from the group consisting of hypercholesterolemia, atherosclerosis, low HDL levels, high LDL levels, hyperlipidemia, hypertriglyceridemia, and dyslipidemia, which method comprises administering to a patient in need of such treatment a therapeutically effective amount of a combination of the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and an HMG-CoA reductase inhibitor.
36. The method of claim 35 , wherein the HMG-CoA reductase inhibitor is a statin selected from the group consisting of lovastatin, simvastatin, pravastatin, fluvastatin, atorvastatin, itavastatin, ZD4522, rivastatin, and rosuvastatin.
37. A method for treating or reducing the risk of developing atherosclerosis in a patient in need of such treatment comprising the administration to said patient of an effective amount of a combination of the compound of claim 1 , or a pharmaceutically acceptable salt thereof, and an HMG-CoA reductase inhibitor.
38. A pharmaceutical composition comprising
(1) the compound of claim 1 , or a pharmaceutically acceptable salt thereof;
(2) one or more compounds selected from the group consisting of:
(a) PPAR gamma agonists and partial agonists;
(b) biguanides;
(c) protein tyrosine phosphatase-1B (PTP-1B) inhibitors;
(d) dipeptidyl peptidase IV (DP-IV) inhibitors;
(e) insulin or an insulin mimetic;
(f) sulfonylureas;
(g) α-glucosidase inhibitors;
(h) agents which improve a patient's lipid profile, said agents being selected from the group consisting of (i) HMG-CoA reductase inhibitors, (ii) bile acid sequestrants, (iii) nicotinyl alcohol, nicotinic acid or a salt thereof, (iv) PPARα agonists, (v) cholesterol absorption inhibitors, (h) acyl CoA:cholesterol acyltransferase (ACAT) inhibitors, (i) CETP inhibitors, and (j) phenolic anti-oxidants;
(i) PPARα/γ dual agonists,
(j) PPARδ agonists,
(k) antiobesity compounds,
(l) ileal bile acid transporter inhibitors;
(m) anti-inflammatory agents;
(n) glucagon receptor antagonists;
(o) GLP-1;
(p) GIP-1; and
(q) GLP-1 analogs; and
(3) a pharmaceutically acceptable carrier.
39. The compound of claim 1 , which is selected from the group consisting of the following compounds, or a pharmaceutically acceptable salt thereof:
40. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
41. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
42. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
43. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
44. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
45. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
46. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
47. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
48. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
49. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
50. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
51. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
52. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
53. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof:
54. The compound of claim 39 , shown below, or a pharmaceutically acceptable salt thereof: