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Heterocyclic compounds and uses thereof
专利权人:
Plexxikon Inc.
发明人:
Songyuan Shi,Prabha N. Ibrahim,Jack Lin,Guoxian Wu,Jeffrey Wu,Jiazhong Zhang,John Buell,Katrina Chan,Phuongly Pham,Wayne Spevak
申请号:
NZ63087514
公开号:
NZ630875A
申请日:
2014.03.14
申请国别(地区):
NZ
年份:
2017
代理人:
摘要:
Disclosed are 4-[1-[1-(pyridin-2-yl)ethyl]pyrrolo[3,2-b]pyridin-6-yl]isoxazole derivatives and analogues of formula (III) or a pharmaceutically acceptable salt, solvate, a tautomer, or a stereoisomer thereof, wherein: Y1 is N R1 is aryl, deuterium substituted aryl, cycloalkyl, cycloalkylalkyl, heteroaryl, or heteroarylalkyl, each of which is optionally substituted R2 is H R3 is an optional substituent R4 is H R5 is isoxazol-4-yl which is optionally substituted with from 1-2 deuterium, CD3, halogen, alkyl, haloalkyl, haloalkoxy, or CN and L is –C(R6)(R7)-, -C(O)-, -S(O)-, -S-, -P(O)(Ra)-, -CH=C(Rb)-, or –Si(Rc)(Rc) and wherein the remaining substituents are as defined herein. Representative compounds of formula (III) include 3,5-dimethyl-4-[3-(1-methylpyrazol-4-yl)-1-[(1S)-1-(pyridin-2-yl)ethyl]pyrrolo[3,2-b]pyridin-6-yl]isoxazole, 4-(6-(3,5-dimethylisoxazol-4-yl)-1-((1S)-1-(pyridin-2-yl)ethyl)pyrrolo[3,2-b]pyridin-3-yl)benzoic acid, methyl 4-(6-(3,5-dimethylisoxazol-4-yl)-1-((pyridazin-3-yl)methyl)pyrrolo[3,2-b]pyridin-3-yl)benzoate, methyl (4-(6-(3,5-dimethylisoxazol-4-yl)-1-((1S)-1-(pyridin-2-yl)ethyl)pyrrolo[3,2-b]pyridin-3-yl)phenyl)acetate and N-methyl-5-(6-(3,5-dimethylisoxazol-4-yl)-1-((1S)-1-(pyridin-2-yl)ethyl)pyrrolo[3,2-b]pyridin-3-yl)pyridine-2-carboxamide. Also disclosed is a pharmaceutical composition comprising a compound as defined above, and optionally another therapeutic agent for the treatment of cancer, rheumatoid arthritis, osteoarthritis, acute gout, psoriasis, systemic lupus erythematosus, multiple sclerosis, inflammatory bowel disease (Crohn’s disease and Ulcerative colitis), asthma, chronic obstructive airways disease, pneumonitis, myocarditis, pericarditis, myositis, eczema, dermatitis, alopecia, vitiligo, bullous skin diseases, nephritis, vasculitis, atherosclerosis, Alzheimer’s disease, depression, retinitis, uveitis, scleritis, hepatitis, pancreatitis, primary biliary cirrhosis, sclerosing cholangitis, Addison’s disease, hypophysitis, th
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