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US 2019/0315754 A1Published application
Ep4 antagonists
AssigneeEisai R&D Management Co., Ltd.
InventorsWanjun Zheng, Xiaojie Zhu, Hong Du, Maarten Postema, Yimin Jiang, Jing Li, Robert Yu, Hyeong-wook Choi, Jaemoon Lee, Frank Fang, Daniel Custar
Life of this patent
Estimating the term…
Abstract
We provide compounds given by Formula I, which is shown in FIG. 3, or pharmaceutically acceptable salts thereof, as well as formulations thereof and methods of use of those compounds and formulations for treatment of cancer.
Claims20
1-34. (canceled)
A method of treating a chronically inflammatory disease in a subject in need thereof, comprising administering to said subject an effective amount of a pharmaceutical composition comprising:
- a compound represented by formula (I):
- or a pharmaceutically acceptable salt thereof,
- wherein
- R1 is —CH3, —CF3, —CH2CH3, —CH2F, CF2CH2OH, —CHF2, —CH═CH2, —CH2OH, or phenyl;
- R2 is —H, —CH2OH, or —CH3;
- R3 is —H;
- or R2 and R3 taken together form a cyclopropyl with the carbon to which they are attached;
- R4 is —H, —F, or —CH3;
- R5 is —C(O)OH, —C(O)OCH3, —CH2C(O)OH, cyclopropyl, —C(O)NHCN,
- wherein R6 is phenyl, —CH3, cyclopropyl,
- n is 0-1;
- m is 1-2;
- R7 is —H, —CH3, or absent when n is 0;
- R8 is —CF3, —H, —Cl, —F, —CH2CH3, —OCH3, —CH3, —SCH3, —CH2OH, —CH2F, —CH2Cl, —I, —Br, —NH2, —CH2OCH2CH2F, —OCH2CH2F, —CH2CH2CH2F, —OCF3, —OH, —N(CH3)2, —CF2CH2OH, or
- or the bond connecting R8 and ring A is a double bond and
- R8 is CH2;
- R9 is —H, —Cl, or —CF3;
- R10 is —H, —CH3, —CH2F, —CH2OH, or —CH2OCH2-phenyl;
- X1 and X2 are either both C, or one is C and the other is N;
- represents a single bond or a double bond;
- and
- ring A is phenyl or cyclohexyl;
- and
- a pharmaceutically acceptable excipient.
21 more elements
The method of claim 1, wherein the compound is represented by formula (II):
- or a pharmaceutically acceptable salt thereof,
- wherein
- R1 is —CH3, —CF3, —CH2CH3, or phenyl;
- R2 is —H, or —CH3;
- R3 is —H;
- or R2 and R3 taken together form a cyclopropyl with the carbon to which they are attached;
- R4 is —H, —F, or —CH3;
- R5 is —C(O)OH, —C(O)OCH3, —CH2C(O)OH, cyclopropyl, —C(O)NHCN,
- wherein Re is phenyl, —CH3, cyclopropyl, or
- m is 1-2;
- n is 0-1;
- R7 is —H, —CH3, or absent when n is 0;
- R8 is —CF3, —H, —Cl, —F, —CH2CH3, —OCH3, —CH3, or —OCF3;
- R9 is —H, —Cl, or —CF3;
- and
- X1 and X2 are either both C, or one is C and the other is N.
13 more elements
The method of claim 1, wherein R10 is —H.
The method of claim 1, wherein represents a single bond.
The method of claim 1, wherein R1 is —CF3.
The method of claim 1, wherein m is 1.
The method of claim 1, wherein R2 is methyl and R3 is —H.
The method of claim 1, wherein X1 and X2 are both —CH—.
The method of claim 1, wherein R4 is —H.
The method of claim 1, wherein n is 1.
The method of claim 1, wherein R7 is —H.
The method of claim 1, wherein R9 is —H.
The method of claim 1, wherein R8 is —CF3.
The method of claim 1, wherein R5 is —C(O)OH.
The method of claim 1, wherein R8 is —Cl.
The method of claim 1, wherein R5 is —C(O)OH, —C(O)OCH3, —CH2C(O)OH, —C(O)NHCN,
The method of claim 1, wherein m is 2, and wherein R8 and R9, if present, are in a meta position or a para position.
The method of claim 1, wherein the compound is selected from the group consisting of the following or a pharmaceutically acceptable salt thereof:
- (S)-4-(1-(1-(3-(methylthio)-5-(trifluoromethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-(hydroxymethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-(fluoromethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-(chloromethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- 4,4′-((1 S, 1′S)-((1,1′-(1,3-phenylenebis(methylene))bis(6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-1,7-diyl-7-carbonyl))bis(azanediyl))bis(ethane-1,1-diyl))dibenzoic acid;
- (S)-4-(1-(1-(4-iodo-3-(trifluoromethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-iodobenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-benzyl-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)—N-(1-(4-(((4-nitrophenyl)sulfonyl)carbamoyl)phenyl)ethyl)-6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamide;
- (S)-4-(1-(1-(4-aminobenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)—N-(1-(4-(((4-aminophenyl)sulfonyl)carbamoyl)phenyl)ethyl)-6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamide;
- (S)-4-(1-(1-(3-((2-fluoroethoxy)methyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-(2-fluoroethoxy)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-hydroxy-5-(trifluoromethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-fluoro-5-(trifluoromethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-((4-(fluoromethyl)cyclohexyl)methyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-((4-methylenecyclohexyl)methyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-(3-fluoropropyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(4-(3-fluoropropyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-(3-fluoropropyl)-5-(trifluoromethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(4-(3-fluoropropyl)-3-(trifluoromethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(6-(fluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(4-chloro-3-(trifluoromethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(3-methyl-6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- 4-((S)-1-((S)-3-(fluoromethyl)-6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(4-hydroxybenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (R)-4-(2-hydroxy-1-(6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(4-(dimethylamino)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-(dimethylamino)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-(dimethylamino)-5-(trifluoromethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(6-(1,1-difluoro-2-hydroxyethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)—N-(1-(4-((1-cyanocyclopropyl)carbamoyl)phenyl)ethyl)-6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamide;
- 4-((S)-1-((S)-3-(hydroxymethyl)-6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- 4-((S)-1-((S)-3-((benzyloxy)methyl)-6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-bromo-5-(trifluoromethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(6-(difluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-(trifluoromethyl)benzyl)-6-vinyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(6-(hydroxymethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-(1,1-difluoro-2-hydroxyethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(6-(trifluoromethyl)-1-(4-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- Methyl (S)-4-(1-(6-(trifluoromethyl)-1-(4-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoate;
- (S)-4-(1-(6-(trifluoromethyl)-1-(2-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3,5-bis(trifluoromethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-chloro-5-(trifluoromethyl)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3,5-dichlorobenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(4-methoxybenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-methoxybenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(4-(trifluoromethoxy)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-(trifluoromethoxy)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-chlorobenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3,4-dichlorobenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(4-fluorobenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-fluorobenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(2-fluorobenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(4-methylbenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-methylbenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(2-methylbenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(4-ethylbenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-2-fluoro-4-(1-(6-(trifluoromethyl)-1-(4-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-3-fluoro-4-(1-(6-(trifluoromethyl)-1-(4-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-3-fluoro-4-(1-(6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-2-fluoro-4-(1-(6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- methyl (S)-2-fluoro-4-(1-(6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoate;
- (S)-2-(4-(1-(6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)phenyl)acetic acid;
- (S)-2-(4-(1-(6-(trifluoromethyl)-1-(4-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)phenyl)acetic acid;
- 4-(1-(6-methyl-1-(4-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)cyclopropyl)benzoic acid;
- 4-(1-(6-(trifluoromethyl)-1-(4-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)cyclopropyl)benzoic acid;
- 4-(1-(1-(4-chlorobenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)cyclopropyl)benzoic acid;
- (S)-4-(1-(1-(4-chlorobenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(4-chlorobenzyl)-6-methyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- 4-((1-(4-chlorobenzyl)-6-methyl-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)methyl)benzoic acid;
- (R)-4-(1-(6-methyl-1-(1-(4-(trifluoromethyl)phenyl)ethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)cyclopropyl)benzoic acid;
- 4-((S)-1-(6-methyl-1-((R)-1-(4-(trifluoromethyl)phenyl)ethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)—N-(1-(4-(2H-tetrazol-5-yl)phenyl)ethyl)-6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamide;
- (S)—N-(1-(4-(2H-tetrazol-5-yl)phenyl)ethyl)-6-(trifluoromethyl)-1-(4-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamide;
- (S)-5-(1-(6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)picolinic acid;
- (S)-6-(1-(6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)nicotinic acid;
- (S)-4-(1-(4-(4-chlorobenzyl)-2-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(4-(3-chlorobenzyl)-2-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(4-(2-chlorobenzyl)-2-(trifluoromethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(2-(trifluoromethyl)-4-(3-(trifluoromethyl)benzyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(2-(trifluoromethyl)-4-(4-(trifluoromethyl)benzyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(2-(trifluoromethyl)-4-(2-(trifluoromethyl)benzyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(6-(trifluoromethyl)-1-(4-(trifluoromethyl)phenyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(6-(trifluoromethyl)-1-(3-(trifluoromethyl)phenyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(3-chlorophenyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(4-chlorophenyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(2-(trifluoromethyl)-4-(4-(trifluoromethyl)phenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamido)ethyl)benzoic acid;
- (S)—N-(1-(4-(cyanocarbamoyl)phenyl)ethyl)-6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamide;
- (S)—N-(1-(4-(((3,4-difluorophenyl)sulfonyl)carbamoyl)phenyl)ethyl)-6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamide;
- (S)—N-(1-(4-((phenylsulfonyl)carbamoyl)phenyl)ethyl)-1-(3-(trifluoromethoxy)benzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamide;
- (S)—N-(1-(4-((methylsulfonyl)carbamoyl)phenyl)ethyl)-6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamide;
- (S)—N-(1-(4-((cyclopropylsulfonyl)carbamoyl)phenyl)ethyl)-6-(trifluoromethyl)-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamide;
- (S)—N-(1-(4-(furan-3-yl)phenyl)ethyl)-6-(trifluoromethyl)-1-(4-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamide;
- (S)—N-(1-(4-cyclopropylphenyl)ethyl)-6-(trifluoromethyl)-1-(4-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamide;
- (S)—N-(1-(3-methyl-4-(2H-tetrazol-5-yl)phenyl)ethyl)-6-(trifluoromethyl)-1-(4-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamide;
- (S)-4-(1-(6-ethyl-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- (S)-4-(1-(1-(2-chlorobenzyl)-6-(trifluoromethyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid;
- and
- (S)-4-(1-(6-phenyl-1-(3-(trifluoromethyl)benzyl)-2,3-dihydro-1H-imidazo[1,2-b]pyrazole-7-carboxamido)ethyl)benzoic acid.
98 more elements
A method of treating a chronically inflammatory disease in a subject in need thereof, comprising administering to said subject an effective amount of a pharmaceutical composition comprising:
- a compound selected from the group consisting of:
- or a pharmaceutically acceptable salt thereof;
- and
- a pharmaceutically acceptable excipient.
1 more element
Dependencies are inferred from the claim text.