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Isotiazolopiridina - 2 - carboxamidas, their use as inhibitors of transglutaminase 2 (tgm2) and a process for its preparation
专利权人:
SANOFI
发明人:
申请号:
ARP120104822
公开号:
AR089329A1
申请日:
2012.12.19
申请国别(地区):
AR
年份:
2014
代理人:
摘要:
Formula compound (1) is a transglutaminas inhibitor, especially transglutamina 2 (TGM2),They are suitable for the treatment of various diseases, such as degenerative joint diseases, such as osteoarthritis. In addition, the preparation process of formula compound (1) is also specified,They are used as drugs and understand their drug synthesis. 1. Claim 1: a formula compound (1),a. Any form of stereoisomerization, or any proportion of a mixture of stereoisomerized forms, or pharmaceutically acceptable salts, where x from composition = n-y = n (o) -;R1,R2 and R3 are independently selected from the series of hydrogen, halogen and c832131 hydrocarbon;-Cquil-O- alkyl,nitro ciano -alquil C -O-C (O) -R8308n-n (r830909) - C (o) - and r8310n (r8311n) - S (o) 8322 -;R⁴ is selected from the series consisting of hydrogen, -C₁₋₄ alkyl,-C₃₋₇ cycloalkyl,-Cyclokquil c833223-83318327a1 asphalt c83321a8331c8332424a1;1. Phenyl, phenyl tar c833214 -,Het1 and het1 - tar c832131;a. It is optional to replace het; r83090 with one or more r831222 which are the same or different;R⁶ and R⁷ are independently selected from each other from the series consisting of hydrogen, -C₁₋₄ alkyl,-C₃₋₇ -cycloalkyl and -C₃₋₇ -cycloalkyl-C₁₋₄-alkyl;R⁸ is selected from the series consisting of halogen, -C₁₋₄ alkyl,hydroxy, oxo, -C₁₋₄-O- alkyl and cyano; R¹⁰ is selected from the series consisting of hydrogen, -C₁₋₄ alkyl,-C₃₋₇ cycloalkyl,-C8323qul c833183227 asphalt c833217c833183248y asphalt c833218c831218c83331248a-o asphalt c83218324 -;If x = n (o) -, r1830404 can only be hydrogen;R¹¹ is selected from the series consisting of -C₁₋₄ alkyl that is optionally substituted with one or more identical or different R¹² substituents, -C₃₋₇ cycloalkyl that is optionally substituted with one or more identical or different R¹³ substituents, and Het² which it is optionally substituted with one or more identical or different R¹⁴ substituents, and in which Het² is linked through a ring carbon atom; or the groups R¹⁰ and R¹
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