US 8,507,473 B2 · 3H-imidazo[4,5-b]pyridin-5-ol derivatives useful in the treatment of GPR81 receptor disorders

Abstract

The present invention is directed to certain 3H-imidazo[4,5-b]pyridin-5-ol derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the GPR81 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of GPR81 associated disorders, for example, dyslipidemia, atherosclerosis, atheromatous disease, hypertension, coronary heart disease, stroke, insulin resistance, impaired glucose tolerance, type 2 diabetes, syndrome X, obesity, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type 1 diabetes and acne.

Claims26

Dependent claims

A compound selected from compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates and hydrates thereof:

wherein:
R1 is aryl, heteroaryl, C3-C10 cycloalkyl, or heterocyclyl, each optionally substituted with 1, 2, or 3 substitutents independently selected from the group consisting of C1-C6 alkoxy, C1-C6 alkoxycarbonyl, C1-C6 alkyl, C1-C6 alkylthio, aryl, C3-C6 cycloalkyl, halogen, C1-C6 haloalkoxy, C1-C6 haloalkyl, C1-C6 haloalkylthio, hydroxyl, nitro, and oxo, wherein C1-C6 alkyl is optionally substituted with aryl;
or
two adjacent substitutents together with the atoms to which they are both bonded form a five-membered cycloalkyl or a five-membered heterocyclyl;
and
R2 is H, C1-C6 alkyl, C1-C6 alkylthio, amino, aryl, C3-C6 cycloalkyl, or halogen.

3 more elements

Dependencies are inferred from the claim text.

Facts

Application

13/063,305Filed 10 Sep 2009 · us provisional application

Priority

11 Sep 2008

Published

US 2011/0172209 A114 Jul 2011

Granted

13 Aug 2013

Term ends

Not estimatedThe source records don’t support an estimate.

Classification15 codes

C07D 471/04
In which the condensed system contains two hetero rings: ortho-condensed systems
A61P 3/04
Drugs for disorders of the metabolism: anorexiants; Antiobesity agents
A61P 3/06
Drugs for disorders of the metabolism: antihyperlipidemics
A61P 3/08
Drugs for disorders of the metabolism: for glucose homeostasis

3H-imidazo[4,5-b]pyridin-5-ol derivatives useful in the treatment of GPR81 receptor disorders

Life of this patent

3H-imidazo[4,5-b]pyridin-5-ol derivatives useful in the treatment of GPR81 receptor disorders

Life of this patent

Abstract

Claims26