US2013096056A1PendingUtilityA1
Aminothiazole derivatives as human stearoyl-coa desaturase inhibitors
Est. expiryJun 3, 2025(expired)· nominal 20-yr term from priority
Inventors:Jianmin FuDuanjie HouRajender KambojVishnumurthy KodumuruNatalia PokrovskaiaVandna RainaShaoyi SunSerguei SviridovZaihui Zhang
A61P 7/02A61P 9/12A61P 3/10A61P 43/00A61P 3/06A61P 9/10A61P 3/00A61P 3/04A61P 35/00A61P 17/10C07D 277/587A61P 17/00A61K 38/28A61K 31/4439A61P 1/16A61K 31/427A61K 31/5377A61K 45/06A61K 31/426A61P 17/02A61K 38/26C07D 417/12A61K 31/616C07D 277/56A61P 19/06C07D 417/06A61P 17/08A61P 17/06
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Claims
Abstract
Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where V, W, R 1 , R 2 , R 3 and R 4 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.
Claims
exact text as granted — not AI-modified1 .- 24 . (canceled)
25 . A method of inhibiting human stearoyl-CoA desaturase (hSCD) activity comprising contacting a source of hSCD with a compound of formula (I):
wherein:
W is selected from —O—, —OC(O)—, —OC(O)N(R 5 )—, —OS(O) 2 N(R 5 )—, —C(O)—, —C(O)O—, —C(O)N(R 5 )—, —N(R 5 )—, —N(R 5 )C(O)—, —N(R 5 )C(O)O—, —N(R 5 )C(O)N(R 5 )—, —N(R 5 )S(O) 2 —, —S(O) t — (where t is 0, 1 or 2), or —S(O) 2 N(R 5 )—;
V is selected from —C(O)—, —C(O)N(R 5 )—, —C(O)O—, —S(O) t — (where t is 1 or 2) or a direct bond;
R 1 is selected from alkyl, alkenyl, —R 6 —OR 7 , hydroxyalkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl;
or R 1 is a multi-ring structure having 2 to 4 rings wherein the rings are independently selected from cycloalkyl, heterocyclyl, aryl or heteroaryl and where some or all of the rings may be fused to each other;
R 2 is selected from alkyl, alkenyl, —R 6 —OR 7 , hydroxyalkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl or heteroarylalkyl;
or R 2 is a multi-ring structure having 2 to 4 rings wherein the rings are independently selected from cycloalkyl, heterocyclyl, aryl or heteroaryl and where some or all of the rings may be fused to each other;
R 3 is selected from hydrogen, alkyl, alkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, aryl, aralkyl, heteroaryl, fluoro, chloro, bromo, trihaloalkyl, trihaloalkoxy, cyano, nitro, —OR 4 , —OC(O)R 2 , —OC(O)N(R 4 )(R 5 ), —OS(O) 2 N(R 4 )(R 5 ), —S(O) t R 2 (where t is 0, 1 or 2), —S(O) t N(R 4 )(R 5 ) (where t is 1 or 2), —C(O)R 2 , —C(O)OR 2 , —C(O)N(R 4 )(R 5 ), —N(R 4 )(R 5 ), —N(R 5 )C(O)R 5 , —N(R 5 )C(O)OR 5 , —N(R 5 )C(O)N(R 4 )(R 5 ) or —N(R 5 )S(O) 2 R 2 ; and
each R 4 and R 5 is independently selected from —R 6 —N(R 7 ) 2 , —R 6 —OR 7 , —R 6 —C(O)OR 7 , hydrogen, alkyl, cycloalkylalkyl or aralkyl;
each R 6 is a straight or branched alkylene chain; and
each R 7 is hydrogen, alkyl, aryl or aralkyl;
or a stereoisomer, enantiomer or tautomer thereof, or a racemic or non-racemic mixture thereof,
or a pharmaceutically acceptable salt or prodrug thereof.
26 . A method of treating a disease or condition mediated by stearoyl-CoA desaturase in a mammal, wherein the method comprises administering to the mammal in need thereof a therapeutically effective amount of a compound of formula (I):
wherein:
W is selected from —O—, —OC(O)—, —OC(O)N(R 5 )—, —OS(O) 2 N(R 5 )—, —C(O)—, —C(O)O—, —C(O)N(R 5 )—, —N(R 5 )—, —N(R 5 )C(O)—, —N(R 5 )C(O)O—, —N(R 5 )C(O)N(R 5 )—, —N(R 5 )S(O) 2 —, —S(O) t — (where t is 0, 1 or 2) or —S(O) 2 N(R 5 )—;
V is selected from —C(O)—, —C(O)N(R 5 )—, —C(O)O—, —S(O) t — (where t is 1 or 2) or a direct bond;
R 1 is selected from alkyl, alkenyl, —R 6 —OR 7 , hydroxyalkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl or heteroarylalkyl;
or R 1 is a multi-ring structure having 2 to 4 rings wherein the rings are independently selected from cycloalkyl, heterocyclyl, aryl or heteroaryl and where some or all of the rings may be fused to each other;
R 2 is selected from alkyl, alkenyl, —R 6 —OR 7 , hydroxyalkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl or heteroarylalkyl;
or R 2 is a multi-ring structure having 2 to 4 rings wherein the rings are independently selected from cycloalkyl, heterocyclyl, aryl or heteroaryl and where some or all of the rings may be fused to each other;
R 3 is selected from hydrogen, alkyl, alkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, aryl, aralkyl, heteroaryl, fluoro, chloro, bromo, trihaloalkyl, trihaloalkoxy, cyano, nitro, —OR 4 , —OC(O)R 2 , —OC(O)N(R 4 )(R 5 ), —OS(O) 2 N(R 4 )(R 5 ), —S(O) t R 2 (where t is 0, 1 or 2), —S(O) t N(R 4 )(R 5 ) (where t is 1 or 2), —C(O)R 2 , —C(O)OR 2 , —C(O)N(R 4 )(R 5 ), —N(R 4 )(R 5 ), —N(R 5 )C(O)R 5 , —N(R 5 )C(O)OR 5 , —N(R 5 )C(O)N(R 4 )(R 5 ) or —N(R 5 )S(O) 2 R 2 ;
each R 4 and R 5 is independently selected from —R 6 —N(R 7 ) 2 , —R 6 —OR 7 , —R 6 —C(O)OR 7 , hydrogen, alkyl, cycloalkylalkyl or aralkyl;
each R 6 is a straight or branched alkylene chain; and
each R 7 is hydrogen, alkyl, aryl or aralkyl;
or a stereoisomer, enantiomer or tautomer thereof, or a racemic or non-racemic mixture thereof, or a pharmaceutically acceptable salt, solvate or prodrug thereof;
wherein the disease or condition is a body weight disorder, metabolic syndrome, fatty liver, non-alcoholic steatohepatitis or a skin disorder.
27 . The method of claim 26 wherein the body weight disorder is obesity, overweight, cachexia or anorexia.
28 . The method according to claim 26 , wherein the metabolic syndrome is dyslipidemia, obesity, insulin resistance, hypertension, microalbuminemia, hyperuricaemia or hypercoagulability.
29 . The method according to claim 26 wherein the skin disorder is eczema, acne, psoriasis or keyloid scar formation.
30 . The method according to any one of claims 25 - 29 wherein the compound of formula (I) is selected from:
2-(4-Bromobenzoylamino)-4-methylthiazole-5-carboxylic acid o-tolylamide;
2-(4-Bromobenzoylamino)-4-methylthiazole-5-carboxylic acid (2-chlorophenyl)amide;
2-(4-Bromobenzoylamino)-4-methylthiazole-5-carboxylic acid (3-methoxyphenyl)amide;
4-Methyl-2-(3,4,5-trimethoxybenzoylamino)thiazole-5-carboxylic acid phenylamide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid (4-methoxyphenyl)amide;
4-Methyl-2-[(thiophene-2-carbonyl)amino]thiazole-5-carboxylic acid (4-chlorophenyl)amide;
2-(Cyclohexanecarbonylamino)-4-methylthiazole-5-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-6-yl)amide,
2-(4-Methoxybenzoylamino)-4-methylthiazole-5-carboxylic acid pyridin-3-ylamide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid (5-methyl[1,3,4]thiadiazol-2-yl)amide;
2-[(Furan-2-carbonyl)amino]-4-methylthiazole-5-carboxylic acid o-tolylamide;
2-[(Furan-2-carbonyl)amino]-4-methylthiazole-5-carboxylic acid (4-bromophenyl)amide;
2-(3-Methoxybenzoylamino)-4-methylthiazole-5-carboxylic acid (4-bromophenyl)amide;
2-[(Furan-2-carbonyl)amino]-4-methylthiazole-5-carboxylic acid (4-chlorophenyl)amide;
2-[(Furan-2-carbonyl)amino]-4-methylthiazole-5-carboxylic acid (3-methoxyphenyl)amide;
2-[(Furan-2-carbonyl)amino]-4-methylthiazole-5-carboxylic acid (4-methoxyphenyl)amide;
4-Methyl-2-(2-phenoxyacetylamino)thiazole-5-carboxylic acid phenylamide;
4-Methyl-2-(2-phenoxyacetylamino)thiazole-5-carboxylic acid benzylamide;
2-Chloro-N-[4-methyl-5-(morpholine-4-carbonyl)thiazol-2-yl]benzamide;
2-(3-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (4-bromophenyl)amide;
2-(2-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (4-bromophenyl)amide;
2-Acetylamino-4-methylthiazole-5-carboxylic acid indan-5-ylamide;
2-Acetylamino-4-methylthiazole-5-carboxylic acid cyclohexylamide;
2-(4-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (4-bromophenyl)amide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid phenylamide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid (3-methoxyphenyl)amide;
2-(4-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (4-methoxyphenyl)amide;
4-Methyl-2-propionylaminothiazole-5-carboxylic acid indan-5-ylamide;
2-(Cyclopropanecarbonylamino)-4-methylthiazole-5-carboxylic acid phenylamide;
2-(Cyclopropanecarbonylamino)-4-methylthiazole-5-carboxylic acid (4-chlorophenyl)amide;
2-(4-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid phenylamide;
2-(4-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid o-tolylamide;
2-(4-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (4-chlorophenyl)amide;
2-(4-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (2-chlorophenyl)amide;
2-(4-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (3-methoxyphenyl)amide;
N-[4-Methyl-5-(piperidine-1-carbonyl)-thiazol-2-yl]benzamide;
2-(Cyclopropanecarbonylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(Cyclopropanecarbonylamino)-4-methylthiazole-5-carboxylic acid indan-5-ylamide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid pyridin-3-ylamide;
4-Methyl-2-propionylaminothiazole-5-carboxylic acid benzylamide;
[(2-Benzoylamino-4-methylthiazole-5-carbonyl)amino]acetic acid ethyl ester;
N-[4-Methyl-5-(morpholine-4-carbonyl)thiazol-2-yl]propionamide;
N-(5-Benzylcarbamoyl-4-methylthiazol-2-yl)isonicotinamide;
N-[5-(3-Chlorophenylcarbamoyl)-4-methylthiazol-2-yl]isonicotinamide;
N-[5-(2-Chlorophenylcarbamoyl)-4-methylthiazol-2-yl]isonicotinamide;
N-(4-Oxo-5,6,7,8-tetrahydro-4H-thiazolo[5,4-c]azepin-2-yl)acetamide;
N-(7,7-Dimethyl-4-oxo-5,6,7,8-tetrahydro-4H-thiazolo[5,4-c]azepin-2-yl)acetamide;
2-(3-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid phenylamide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid o-tolylamide;
2-(2-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid o-tolylamide;
2-(4-Bromobenzoylamino)-4-methylthiazole-5-carboxylic acid (4-chlorophenyl)amide;
4-Methyl-2-(3,4,5-trimethoxybenzoylamino)thiazole-5-carboxylic acid (4-chlorophenyl)amide;
2-(4-Bromobenzoylamino)-4-methylthiazole-5-carboxylic acid (3-chlorophenyl)amide;
4-Methyl-2-(3-methylbenzoylamino)thiazole-5-carboxylic acid (3-chlorophenyl)amide;
2-(3-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (3-chlorophenyl)amide;
4-Methyl-2-(2-methylbenzoylamino)thiazole-5-carboxylic acid (2-chlorophenyl)amide;
4-Methyl-2-(3,4,5-trimethoxybenzoylamino)thiazole-5-carboxylic acid (2-chlorophenyl)amide;
4-Methyl-2-(3-methylbenzoylamino)thiazole-5-carboxylic acid (2-chlorophenyl)amide;
2-(3-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (2-chlorophenyl)amide;
2-(4-Bromobenzoylamino)-4-methylthiazole-5-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-6-yl)amide;
2-(4-Methoxybenzoylamino)-4-methylthiazole-5-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-6-yl)amide;
4-Methyl-2-(3-methylbenzoylamino)thiazole-5-carboxylic acid (2,3-dihydrobenzo[1,4]dioxin-6-yl)amide;
2-(4-Bromobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(4-Bromobenzoylamino)-4-methylthiazole-5-carboxylic acid indan-5-ylamide;
4-Methyl-2-(3-methylbenzoylamino)thiazole-5-carboxylic acid indan-5-ylamide;
4-Methyl-2-(3,4,5-trimethoxybenzoylamino)thiazole-5-carboxylic acid cyclohexylamide;
2-Fluoro-N-[4-methyl-5-(piperidine-1-carbonyl)thiazol-2-yl]benzamide;
4-Bromo-N-[4-methyl-5-(morpholine-4-carbonyl)thiazol-2-yl]benzamide;
4-Methoxy-N-[4-methyl-5-(morpholine-4-carbonyl)thiazol-2-yl]benzamide;
2-(Cyclohexanecarbonylamino)-4-methylthiazole-5-carboxylic acid (4-methoxyphenyl)amide;
4-Methyl-2-(3,4,5-trimethoxybenzoylamino)thiazole-5-carboxylic acid o-tolylamide;
4-Methyl-2-(3,4,5-trimethoxybenzoylamino)thiazole-5-carboxylic acid (3-chlorophenyl)amide;
2-(4-Methoxybenzoylamino)-4-methylthiazole-5-carboxylic acid (3-methoxyphenyl)amide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid (2,3-dihydrobenzo[1,4]dioxin-6-yl)amide;
4-Methyl-2-(3,4,5-trimethoxybenzoylamino)thiazole-5-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-6-yl)amide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid benzylamide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid indan-5-ylamide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid (4-chlorophenyl)amide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid (3-chlorophenyl)amide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid (2-chlorophenyl)amide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid (3-methoxyphenyl)amide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid phenylamide;
2-(Cyclohexanecarbonylamino)-4-methylthiazole-5-carboxylic acid (4-chlorophenyl)amide;
2-(Cyclohexanecarbonylamino)-4-methylthiazole-5-carboxylic acid (2-chlorophenyl)amide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid [5-(2-chloro-phenylcarbamoyl)-4-methylthiazol-2-yl]amide;
2-(Cyclohexanecarbonylamino)-4-methylthiazole-5-carboxylic acid indan-5-ylamide;
{[2-(4-Methoxy-benzoylamino)-4-methylthiazole-5-carbonyl]amino}acetic acid ethyl ester;
3-Fluoro-N-[4-methyl-5-(morpholine-4-carbonyl)thiazol-2-yl]benzamide;
2-[(5-Chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbonyl)amino]-4-methylthiazole-5-carboxylic acid cyclohexylamide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid (2-dimethylaminoethyl)amide;
2-[(Furan-2-carbonyl)amino]-4-methylthiazole-5-carboxylic acid phenylamide;
2-[(Adamantane-1-carbonyl)amino]-4-methylthiazole-5-carboxylic acid phenylamide;
2-[(Adamantane-1-carbonyl)amino]-4-methylthiazole-5-carboxylic acid (4-bromophenyl)amide;
2-(3-Methoxybenzoylamino)-4-methylthiazole-5-carboxylic acid (4-chlorophenyl)amide;
2-[(Furan-2-carbonyl)amino]-4-methylthiazole-5-carboxylic acid (3-chlorophenyl)amide;
2-(3-Methoxybenzoylamino)-4-methylthiazole-5-carboxylic acid (3-chlorophenyl)amide;
2-(3-Methoxybenzoylamino)-4-methylthiazole-5-carboxylic acid (2-chlorophenyl)amide;
2-(3-Methoxybenzoylamino)-4-methylthiazole-5-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-6-yl)amide;
2-(3-Methoxybenzoylamino)-4-methylthiazole-5-carboxylic acid indan-5-ylamide;
{[2-(3-Methoxybenzoylamino)-4-methylthiazole-5-carbonyl]amino}acetic acid ethyl ester;
2-(4-Bromobenzoylamino)-4-methylthiazole-5-carboxylic acid (5-methyl[1,3,4]thiadiazol-2-yl)amide;
2-(3-Methoxy-benzoylamino)-4-methylthiazole-5-carboxylic acid (4-methoxyphenyl)amide;
2-[(Adamantane-1-carbonyl)amino]-4-methylthiazole-5-carboxylic acid (4-methoxyphenyl)amide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid (4-methyl-5-phenylcarbamoyl-thiazol-2-yl)amide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid (4-methyl-5-o-tolylcarbamoyl-thiazol-2-yl)amide;
2-[(5-Chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbonyl)amino]-4-methylthiazole-5-carboxylic acid (4-bromophenyl)amide;
2-[(5-Chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbonyl)amino]-4-methylthiazole-5-carboxylic acid (2-chlorophenyl)amide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid [5-(2,3-dihydro-benzo[1,4]dioxin-6-ylcarbamoyl)-4-methylthiazol-2-yl]amide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid [5-(indan-5-ylcarbamoyl)-4-methylthiazol-2-yl]amide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid [4-methyl-5-(5-methyl-[1,3,4]thiadiazol-2-ylcarbamoyl)thiazol-2-yl]amide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid [4-methyl-5-(piperidine-1-carbonyl)thiazol-2-yl]amide;
3-Methyl-N-[4-methyl-5-(piperidine-1-carbonyl)thiazol-2-yl]benzamide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid [5-(4-methoxy-phenylcarbamoyl)-4-methylthiazol-2-yl]amide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid cyclohexylamide;
2-(Cyclohexanecarbonylamino)-4-methylthiazole-5-carboxylic acid (3-chlorophenyl)amide;
4-Methyl-2-[(thiophene-2-carbonyl)amino]thiazole-5-carboxylic acid (2,3-dihydro-benzo[1,4]dioxin-6-yl)amide;
2-[(Adamantane-1-carbonyl)amino]-4-methylthiazole-5-carboxylic acid benzylamide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid (4-bromophenyl)amide;
2-(Cyclohexanecarbonylamino)-4-methylthiazole-5-carboxylic acid (4-bromophenyl)amide;
4-Methyl-2-(3-methylbenzoylamino)thiazole-5-carboxylic acid (4-bromophenyl)amide;
2-(2-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (4-chlorophenyl)amide;
2-(2-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (2-chlorophenyl)amide;
2-(3-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid indan-5-ylamide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid [5-(4-chloro-phenylcarbamoyl)-4-methylthiazol-2-yl]amide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid (3-chlorophenyl)amide;
2-Acetylamino-4-methylthiazole-5-carboxylic acid (3-methoxyphenyl)amide;
4-Methyl-2-(4-nitrobenzoylamino)thiazole-5-carboxylic acid (4-methoxyphenyl)amide;
2-Acetylamino-4-methylthiazole-5-carboxylic acid (4-chlorophenyl)amide;
2-Acetylamino-4-methylthiazole-5-carboxylic acid (4-methoxyphenyl)amide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid (5-methyl[1,3,4]thiadiazol-2-yl)amide;
2-(4-Bromobenzoylamino)-4-methylthiazole-5-carboxylic acid phenylamide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid (4-methoxyphenyl)amide;
4-Methyl-2-propionylaminothiazole-5-carboxylic acid (4-methoxyphenyl)amide;
2-(Cyclopropanecarbonylamino)-4-methylthiazole-5-carboxylic acid (4-methoxyphenyl)amide;
4-Methyl-2-propionylamino-thiazole-5-carboxylic acid (4-bromophenyl)amide;
4-Methyl-2-(4-nitrobenzoylamino)thiazole-5-carboxylic acid (2-chlorophenyl)amide;
{[2-(4-Fluorobenzoylamino)-4-methylthiazole-5-carbonyl]amino}acetic acid ethyl ester;
{[2-(3-Fluorobenzoylamino)-4-methylthiazole-5-carbonyl]amino}acetic acid ethyl ester;
2-(2-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (4-methoxyphenyl)amide;
N-[4-Methyl-5-(piperidine-1-carbonyl)thiazol-2-yl]-2-phenoxyacetamide;
2-(4-tert-Butylbenzoylamino)-4-methylthiazole-5-carboxylic acid (4-bromophenyl)amide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid (4-bromophenyl)amide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid (4-chlorophenyl)amide;
2-(4-tert-Butylbenzoylamino)-4-methylthiazole-5-carboxylic acid (3-chlorophenyl)amide;
2-(4-tert-Butylbenzoylamino)-4-methylthiazole-5-carboxylic acid (2-chlorophenyl)amide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid benzylamide;
2-(4-tert-Butylbenzoylamino)-4-methylthiazole-5-carboxylic acid cyclohexylamide;
2-(4-Methoxybenzoylamino)-4-methylthiazole-5-carboxylic acid (5-methyl[1,3,4]thiadiazol-2-yl)amide;
4-Methyl-2-(4-nitro-benzoylamino)thiazole-5-carboxylic acid o-tolylamide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid (4-bromophenyl)amide;
4-Methyl-2-(2-methylbenzoylamino)thiazole-5-carboxylic acid (4-bromophenyl)amide;
4-Methyl-2-(2-phenoxyacetylamino)thiazole-5-carboxylic acid (4-bromophenyl)amide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid [5-(4-bromo-phenylcarbamoyl)-4-methylthiazol-2-yl]amide;
4-Methyl-2-(4-nitrobenzoylamino)thiazole-5-carboxylic acid (4-chlorophenyl)amide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid (3-chlorophenyl)amide;
4-Methyl-2-(2-phenoxyacetylamino)thiazole-5-carboxylic acid (3-chlorophenyl)amide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid [5-(3-chloro-phenylcarbamoyl)-4-methylthiazol-2-yl]amide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid o-tolylamide;
4-Methyl-2-(2-phenoxy-acetylamino)thiazole-5-carboxylic acid (3-methoxyphenyl)amide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid (2,3-dihydrobenzo[1,4]dioxin-6-yl)amide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid (5-benzylcarbamoyl-4-methylthiazol-2-yl)amide;
4-Methyl-2-propionylaminothiazole-5-carboxylic acid (3-methoxyphenyl)amide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid [5-(3-methoxy-phenylcarbamoyl)-4-methylthiazol-2-yl]amide;
4-Methyl-2-(2-methylbenzoylamino)thiazole-5-carboxylic acid indan-5-ylamide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid (4-methoxyphenyl)amide;
4-Methyl-2-(2-phenoxyacetylamino)thiazole-5-carboxylic acid (4-methoxyphenyl)amide;
4-Methyl-2-(3,4,5-trimethoxybenzoylamino)thiazole-5-carboxylic acid (4-methoxyphenyl)amide;
2-(Cyclopropanecarbonylamino)-4-methylthiazole-5-carboxylic acid o-tolylamide;
4-Methyl-2-propionylaminothiazole-5-carboxylic acid (4-chlorophenyl)amide;
4-Methyl-2-propionylaminothiazole-5-carboxylic acid (3-chlorophenyl)amide;
4-Methyl-2-propionylaminothiazole-5-carboxylic acid (2-chlorophenyl)amide;
4-Methyl-2-(4-nitrobenzoylamino)thiazole-5-carboxylic acid (3-chlorophenyl)amide;
2-(4-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (2,3-dihydrobenzo[1,4]dioxin-6-yl)amide;
2-(4-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid indan-5-ylamide;
4-Fluoro-N-[4-methyl-5-(piperidine-1-carbonyl)thiazol-2-yl]benzamide;
2-(4-tert-Butylbenzoylamino)-4-methylthiazole-5-carboxylic acid indan-5-ylamide;
4-Methyl-2-propionylaminothiazole-5-carboxylic acid cyclohexylamide;
N-[4-Methyl-5-(piperidine-1-carbonyl)thiazol-2-yl]propionamide;
2-(Cyclopropanecarbonylamino)-4-methylthiazole-5-carboxylic acid (3-chlorophenyl)amide;
2-(3-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid (3-methoxyphenyl)amide;
2-(Cyclopropanecarbonylamino)-4-methylthiazole-5-carboxylic acid (2-chlorophenyl)amide;
4-Methyl-2-(4-nitrobenzoylamino)thiazole-5-carboxylic acid phenylamide;
2-(Cyclopropanecarbonylamino)-4-methylthiazole-5-carboxylic acid cyclohexylamide;
4-Methyl-2-(4-nitrobenzoylamino)thiazole-5-carboxylic acid (2,3-dihydrobenzo[1,4]dioxin-6-yl)amide;
2-(4-tert-Butylbenzoylamino)-4-methylthiazole-5-carboxylic acid phenylamide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid phenylamide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid o-tolylamide;
4-Methyl-2-[(thiophene-2-carbonyl)amino]thiazole-5-carboxylic acid (5-methyl-[1,3,4]thiadiazol-2-yl)amide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid (2-chlorophenyl)amide;
4-Methyl-2-(4-nitrobenzoylamino)thiazole-5-carboxylic acid (4-bromophenyl)amide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid indan-5-ylamide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid (2-hydroxy-ethyl)amide;
3-Methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxylic acid (5-cyclohexylcarbamoyl-4-methylthiazol-2-yl)amide;
{[2-(2-Fluorobenzoylamino)-4-methylthiazole-5-carbonyl]amino}acetic acid ethyl ester;
4-Methyl-2-(3,4,5-trimethoxybenzoylamino)thiazole-5-carboxylic acid (4-bromophenyl)amide;
2-(Cyclohexanecarbonylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
N-[4-Methyl-5-(morpholine-4-carbonyl)thiazol-2-yl]-3-phenylacrylamide;
N-[4-Methyl-5-(morpholine-4-carbonyl)thiazol-2-yl]-4-nitrobenzamide;
{[4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carbonyl]amino}acetic acid ethyl ester;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid (2,3-dihydrobenzo[1,4]dioxin-6-yl)amide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid pyridin-3-ylamide;
N-[4-Methyl-5-(piperidine-1-carbonyl)thiazol-2-yl]-3-phenylacrylamide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid cyclohexylamide;
4-Methyl-2-(3,4,5-trimethoxybenzoylamino)thiazole-5-carboxylic acid (5-methyl-[1,3,4]thiadiazol-2-yl)amide;
4-Methyl-2-propionylaminothiazole-5-carboxylic acid o-tolylamide;
Cyclopropanecarboxylic acid [4-methyl-5-(piperidine-1-carbonyl)thiazol-2-yl]amide;
4-Methyl-2-(2-phenoxyacetylamino)thiazole-5-carboxylic acid o-tolylamide;
4-Methyl-2-(2-phenoxyacetylamino)thiazole-5-carboxylic acid (2,3-dihydrobenzo[1,4]dioxin-6-yl)amide;
2-(Cyclopropanecarbonylamino)-4-methylthiazole-5-carboxylic acid (4-bromophenyl)amide;
4-Methyl-2-(3,4,5-trimethoxybenzoylamino)thiazole-5-carboxylic acid indan-5-ylamide;
2-[(Adamantane-1-carbonyl)amino]-4-methylthiazole-5-carboxylic acid cyclohexylamide;
2-(3-Chlorobenzoylamino)-4-methylthiazole-5-carboxylic acid pyridin-3-ylamide;
2-(3-Chlorobenzoylamino)-4-methylthiazole-5-carboxylic acid cyclohexylamide;
{[4-Methyl-2-(3,4,5-trimethoxybenzoylamino)thiazole-5-carbonyl]amino}acetic acid ethyl ester;
4-Methyl-2-(2-methylbenzoylamino)thiazole-5-carboxylic acid (3-chlorophenyl)amide;
2-(4-Chlorobenzoylamino)-4-methylthiazole-5-carboxylic acid cyclohexylamide;
4-Methyl-2-(4-methylbenzoylamino)thiazole-5-carboxylic acid (2-dimethylaminoethyl)amide;
5-tert-Butyl-2-methyl-2H-pyrazole-3-carboxylic acid (7,7-dimethyl-4-oxo-5,6,7,8-tetrahydro-4H-thiazolo[5,4-c]azepin-2-yl)amide;
2-[(5-Chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbonyl)amino]-4-methylthiazole-5-carboxylic acid indan-5-ylamide;
4-Methyl-2-(4-nitrobenzoylamino)thiazole-5-carboxylic acid indan-5-ylamide;
2-Acetylamino-4-methylthiazole-5-carboxylic acid (5-methyl[1,3,4]thiadiazol-2-yl)amide;
2-Chloro-N-(7,7-dimethyl-4-oxo-5,6,7,8-tetrahydro-4H-thiazolo[5,4-c]azepin-2-yl)-benzamide;
N-(7,7-Dimethyl-4-oxo-5,6,7,8-tetrahydro-4H-thiazolo[5,4-c]azepin-2-yl)benzamide;
N-(4-Oxo-5,6,7,8-tetrahydro-4H-thiazolo[5,4-c]azepin-2-yl)benzamide;
2-Chloro-N-(4-oxo-5,6,7,8-tetrahydro-4H-thiazolo[5,4-c]azepin-2-yl)benzamide;
2-(3,4-Dimethoxybenzoylamino)-4-methylthiazole-5-carboxylic acid dimethylamide;
4-Methyl-2-(2-phenyl-propionylamino)thiazole-5-carboxylic acid dimethylamide;
2-(2,6-Difluorobenzoylamino)-4-methylthiazole-5-carboxylic acid dimethylamide;
3-Chloro-N-[4-methyl-5-(piperidine-1-carbonyl)thiazol-2-yl]benzamide;
2-[2-(4-Chloro-2-methylphenoxy)propionylamino]-4-methylthiazole-5-carboxylic acid dimethylamide;
6,8-Dimethyl-2-pyridin-4-ylquinoline-4-carboxylic acid (5-dimethylcarbamoyl-4-methylthiazol-2-yl)amide;
4-Methyl-2-[(3-methylbenzofuran-2-carbonyl)amino]thiazole-5-carboxylic acid dimethylamide;
2-Acetylamino-4-methylthiazole-5-carboxylic acid (3-chlorophenyl)amide;
4-Methyl-2-(2-phenoxyacetylamino)thiazole-5-carboxylic acid indan-5-ylamide;
5-(7,7-Dimethyl-4-oxo-5,6,7,8-tetrahydro-4H-thiazolo[5,4-c]azepin-2-ylcarbamoyl)-thiophene-2-carboxylic acid methyl ester;
4-Methyl-2-(3-methylbenzoylamino)thiazole-5-carboxylic acid cyclohexylamide;
4-Methyl-2-(3-phenylacryloylamino)thiazole-5-carboxylic acid (3-methoxyphenyl)amide;
4-Methyl-2-(4-nitrobenzoylamino)thiazole-5-carboxylic acid (3-methoxyphenyl)amide;
2-[(Adamantane-1-carbonyl)amino]-4-methylthiazole-5-carboxylic acid (3-methoxyphenyl)amide;
N-[5-(2-Cyclopropylethylcarbamoyl)-4-methylthiazol-2-yl]isonicotinamide;
N-(4-Methyl-5-phenethylcarbamoylthiazol-2-yl)isonicotinamide;
N-[4-Methyl-5-(3-phenylpropylcarbamoyl)thiazol-2-yl]isonicotinamide;
N-[5-(4-Chlorobenzylcarbamoyl)-4-methylthiazol-2-yl]isonicotinamide;
2-(Cyclopropanecarbonylamino)-4-methylthiazole-5-carboxylic acid 4-chloro-benzylamide;
2-(2,5-Difluorobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(Cyclobutanecarbonylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
4-Methyl-2-[(2-phenylcyclopropanecarbonyl)amino]thiazole-5-carboxylic acid benzylamide;
2-(2-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(2,2-Dimethylpropionylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid benzylamide;
4-Methyl-2-(2-trifluoromethylbenzoylamino)thiazole-5-carboxylic acid benzylamide;
2-(4-Chlorobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(4-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
4-Methyl-2-(4-trifluoromethylbenzoylamino)thiazole-5-carboxylic acid benzylamide;
2-(2-Chlorobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(2,4-Dichlorobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(Cyclopentanecarbonylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(2-Chloro-4-fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(3-Chlorobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
4-Methyl-2-(2-trifluoromethoxybenzoylamino)thiazole-5-carboxylic acid benzylamide;
2-(3,5-Dichlorobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(3-Cyanobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(5-Chloro-2-fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(3-Fluorobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
4-Methyl-2-(4-trifluoromethoxybenzoylamino)thiazole-5-carboxylic acid benzylamide;
4-Methyl-2-(3-trifluoromethylbenzoylamino)thiazole-5-carboxylic acid benzylamide;
2-(3-Methoxybenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
4-Methyl-2-[(naphthalene-1-carbonyl)amino]thiazole-5-carboxylic acid benzylamide;
2-(4-Cyanobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(3,5-Difluorobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
4-Methyl-2-(3-trifluoromethoxybenzoylamino)thiazole-5-carboxylic acid benzylamide;
2-(4-Methoxybenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(3-Methanesulfonylbenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(2-Methanesulfonylbenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-Benzoylamino-4-trifluoromethylthiazole-5-carboxylic acid benzylamide;
N-(5-Benzylcarbamoyl-4-methylthiazol-2-yl)nicotinamide;
2-(3,4-Dichlorobenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-(4-Methanesulfonylbenzoylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
4-Methyl-2-(3-phenylpropionylamino)thiazole-5-carboxylic acid benzylamide;
2-Benzylamino-4-methylthiazole-5-carboxylic acid benzylamide;
4-Methyl-2-phenylacetylaminothiazole-5-carboxylic acid benzylamide;
2-Benzoylamino-4-phenylthiazole-5-carboxylic acid benzylamide;
4-Methyl-2-(3-phenylureido)thiazole-5-carboxylic acid benzylamide;
2-[3-(4-Fluorophenyl)ureido]-4-methylthiazole-5-carboxylic acid benzylamide;
2-[3-(4-Chlorophenyl)ureido]-4-methylthiazole-5-carboxylic acid benzylamide;
2-(2-Cyclopropylacetylamino)-4-methylthiazole-5-carboxylic acid benzylamide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid 2-trifluoromethylbenzylamide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid 3-chlorobenzylamide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid cyclopropylmethyl-amide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid 3-fluorobenzylamide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid 2-chlorobenzylamide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid 2-fluorobenzylamide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid 4-fluorobenzylamide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid benzylmethylamide;
2-Benzoylamino-4-chlorothiazole-5-carboxylic acid benzylamide;
2-[(4-Pentylbenzoyl)amino]-N-(phenylmethyl)-4-(trifluoromethyl)-5-thiazolecarboxamide;
2-Benzoylamino-4-methylthiazole-5-carboxylic acid (1-phenylpropyl)amide;
4-Methyl-2-(toluene-4-sulfonylamino)thiazole-5-carboxylic acid benzylamide;
4-Methyl-2-[4-(2H-tetrazol-5-yl)benzoylamino]thiazole-5-carboxylic acid benzylamide;
2-Benzoylamino-thiazole-5-carboxylic acid benzylamide;
4-Amino-2-benzoylaminothiazole-5-carboxylic acid benzylamide;
N-[5-(N-Benzoylhydrazinocarbonyl)-4-methylthiazol-2-yl]benzamide;
N-[5-(Imidazole-1-carbonyl)-4-methylthiazol-2-yl]benzamide;
4-Methyl-2-(4-phenylbutyrylamino)thiazole-5-carboxylic acid benzylamide;
4-Methyl-2-(5-phenylpentanoylamino)thiazole-5-carboxylic acid benzylamide;
4-Methyl-2-[4-(2-oxo-2H-pyridin-1-yl)benzoylamino]thiazole-5-carboxylic acid benzylamide;
2-[(5-Benzylcarbamoyl-4-methyl-thiazol-2-ylcarbamoyl)methyl]benzoic acid;
N-(5-Benzylcarbamoyl-4-methylthiazol-2-yl)-2-methoxyisonicotinamide;
2-Oxo-1,2-dihydropyridine-4-carboxylic acid (5-benzylcarbamoyl-4-methylthiazol-2-yl)amide;
2-Oxo-1-phenyl-1,2-dihydropyridine-4-carboxylic acid (5-benzylcarbamoyl-4-methyl-thiazol-2-yl)amide;
N,4-Dibenzyl-2-(3-phenylpropanamido)thiazole-5-carboxamide;
2-Benzamido-N,4-dibenzylthiazole-5-carboxamide,
2-(4-Bromo-2-hydroxymethylbenzoylamino)-4-methyl-thiazole-5-carboxylic acid benzylamide;
N-benzyl-4-methyl-2-(N-methylbenzamido)thiazole-5-carboxamide;
N-benzyl-N,4-dimethyl-2-(N-methylbenzamido)thiazole-5-carboxamide;
2-(4-((1H-pyrazol-1-yl)methyl)benzamido)-N-benzyl-4-methylthiazole-5-carboxamide;
N-Benzyl-4-(morpholinomethyl)-2-(3-phenylpropanamido)thiazole-5-carboxamide;
N-benzyl-2-(4-benzylbenzamido)-4-methylthiazole-5-carboxamide;
2-(4-Benzylbenzoylamino)-4-diethylaminomethylthiazole-5-carboxylic acid benzylamide;
2-Benzamido-N-benzyl-4-((diethylamino)methyl)thiazole-5-carboxamide;
2-(4-Benzylbenzamido)-N-(2-cyanoethyl)-4-methylthiazole-5-carboxamide;
2-(4-Benzylbenzamido)-N-ethyl-4-methylthiazole-5-carboxamide; or
N-Benzyl-2-(4-benzylbenzamido)-4-((methylamino)methyl)thiazole-5-carboxamide.
31 . A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a therapeutically effective amount of a compound of formula (I):
wherein:
W is selected from —O—, —OC(O)—, —OC(O)N(R 5 )—, —OS(O) 2 N(R 5 )—, —C(O)—, —C(O)O—, —C(O)N(R 5 )—, —N(R 5 )—, —N(R 5 )C(O)—, —N(R 5 )C(O)O—, —N(R 5 )C(O)N(R 5 )—, —N(R 5 )S(O) 2 —, —S(O) t — (where t is 0, 1 or 2), or —S(O) 2 N(R 5 )—;
V is selected from —C(O)—, —C(O)N(R 5 )—, —C(O)O—, —S(O) t — (where t is 1 or 2) or a direct bond;
R 1 is selected from alkyl, alkenyl, —R 6 —OR 7 , hydroxyalkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl;
or R 1 is a multi-ring structure having 2 to 4 rings wherein the rings are independently selected from cycloalkyl, heterocyclyl, aryl or heteroaryl and where some or all of the rings may be fused to each other;
R 2 is selected from alkyl, alkenyl, —R 6 —OR 7 , hydroxyalkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl or heteroarylalkyl;
or R 2 is a multi-ring structure having 2 to 4 rings wherein the rings are independently selected from cycloalkyl, heterocyclyl, aryl or heteroaryl and where some or all of the rings may be fused to each other;
R 3 is selected from hydrogen, alkyl, alkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, aryl, aralkyl, heteroaryl, fluoro, chloro, bromo, trihaloalkyl, trihaloalkoxy, cyano, nitro, —OR 4 , —OC(O)R 2 , —OC(O)N(R 4 )(R 5 ), —OS(O) 2 N(R 4 )(R 5 ), —S(O) t R 2 (where t is 0, 1 or 2), —S(O) t N(R 4 )(R 5 ) (where t is 1 or 2), —C(O)R 2 , —C(O)OR 2 , —C(O)N(R 4 )(R 5 ), —N(R 4 )(R 5 ), —N(R 5 )C(O)R 5 , —N(R 5 )C(O)OR 5 , —N(R 5 )C(O)N(R 4 )(R 5 ) or —N(R 5 )S(O) 2 R 2 ;
each R 4 and R 5 is independently selected from —R 6 —N(R 7 ) 2 , —R 6 —OR 7 , —R 6 —C(O)OR 7 , hydrogen, alkyl, cycloalkylalkyl or aralkyl;
each R 6 is a straight or branched alkylene chain; and
each R 7 is hydrogen, alkyl, aryl or aralkyl;
or a stereoisomer, enantiomer or tautomer thereof, or a racemic or non-racemic mixture thereof, or a pharmaceutically acceptable salt, solvate or prodrug thereof.
32 . A pharmaceutical composition comprising a pharmaceutically acceptable excipient; a therapeutically effective amount of a compound of formula (I):
wherein:
W is selected from —O—, —OC(O)—, —OC(O)N(R 5 )—, —OS(O) 2 N(R 5 )—, —C(O)—, —C(O)O—, —C(O)N(R 5 )—, —N(R 5 )—, —N(R 5 )C(O)—, —N(R 5 )C(O)O—, —N(R 5 )C(O)N(R 5 )—, —N(R 5 )S(O) 2 —, —S(O) t — (where t is 0, 1 or 2), or —S(O) 2 N(R 5 )—;
V is selected from —C(O)—, —C(O)N(R 5 )—, —C(O)O—, —S(O) t — (where t is 1 or 2) or a direct bond;
R 1 is selected from alkyl, alkenyl, —R 6 —OR 7 , hydroxyalkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, or heteroarylalkyl;
or R 1 is a multi-ring structure having 2 to 4 rings wherein the rings are independently selected from cycloalkyl, heterocyclyl, aryl or heteroaryl and where some or all of the rings may be fused to each other;
R 2 is selected from alkyl, alkenyl, —R 6 —OR 7 , hydroxyalkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl or heteroarylalkyl;
or R 2 is a multi-ring structure having 2 to 4 rings wherein the rings are independently selected from cycloalkyl, heterocyclyl, aryl or heteroaryl and where some or all of the rings may be fused to each other;
R 3 is selected from hydrogen, alkyl, alkenyl, hydroxyalkyl, hydroxyalkenyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, aryl, aralkyl, heteroaryl, fluoro, chloro, bromo, trihaloalkyl, trihaloalkoxy, cyano, nitro, —OR 4 , —OC(O)R 2 , —OC(O)N(R 4 )(R 5 ), —OS(O) 2 N(R 4 )(R 5 ), —S(O) t R 2 (where t is 0, 1 or 2), —S(O) t N(R 4 )(R 5 ) (where t is 1 or 2), —C(O)R 2 , —C(O)OR 2 , —C(O)N(R 4 )(R 5 ), —N(R 4 )(R 5 ), —N(R 5 )C(O)R 5 , —N(R 5 )C(O)OR 5 , —N(R 5 )C(O)N(R 4 )(R 5 ) or —N(R 5 )S(O) 2 R 2 ;
each R 4 and R 5 is independently selected from —R 6 —N(R 7 ) 2 , —R 6 —OR 7 , —R 6 —C(O)OR 7 , hydrogen, alkyl, cycloalkylalkyl or aralkyl;
each R 6 is a straight or branched alkylene chain; and
each R 7 is hydrogen, alkyl, aryl or aralkyl;
or a stereoisomer, enantiomer or tautomer thereof, or a racemic or non-racemic mixture thereof, or a pharmaceutically acceptable salt, solvate or prodrug thereof; and
a therapeutically effective amount of insulin, insulin derivative, insulin mimetic, insulin secretagogue, insulinotropic sulfonylurea receptor ligand, PPAR ligand, insulin sensitizer, biguanide, alpha-glucosidase inhibitors, GLP-1, GLP-1 analog, GLP-1 mimetic, DPPIV inhibitor, HMG-CoA reductase inhibitor, squalene synthase inhibitor, FXR ligand, LXR ligand, cholestyramine, fibrates, nicotinic acid or aspirin.Join the waitlist — get patent alerts
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