发明名称 Antagonists of CB1 Receptor
摘要 The invention relates to an antagonist of CB1 receptor for use in the treatment of a pathologic condition or disorder selected from the group consisting of bladder and gastrointestinal disorders; inflammatory diseases; cardiovascular diseases; nephropathies; glaucoma; spasticity; cancer; osteoporosis; metabolic disorders; obesity; addiction, dependence, abuse and relapse related disorders; psychiatric and neurological disorders; neurodegenerative disorders; autoimmune hepatitis and encephalitis; pain; reproductive disorders and skin inflammatory and fibrotic diseases.
申请公布号 US2016145294(A1) 申请公布日期 2016.05.26
申请号 US201615012471 申请日期 2016.02.01
申请人 INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE) ;UNIVERSITE DE BORDEAUX 发明人 Piazza Pier Vincenzo;Vallee Monique;Marsicano Giovanni;Felpin Francois-Xavier;Bellocchio Luigi;Cota Daniela;Revest Jean-Michel;Vitiello Sergio;Spampinato Umberto;Maldonado Rafael
分类号 C07J7/00;C07J41/00 主分类号 C07J7/00
代理机构 代理人
主权项 1. A compound of formula (A) or a pharmaceutical salt thereof: wherein: denotes that the bound is a single or a double bond, R1 denotes that C3 is substituted with —H,-halogen,—OH,C1-8 alkoxy,Bn-O—Bn- optionally substituted with C1-8 alkyl, C1-8 alkoxy, cyano, nitro, amino, carboxyl or halogen,Ph- optionally substituted with C1-8 alkyl, C1-8 alkoxy, cyano, nitro, amino, carboxyl or halogen,═O,—NR5R6 wherein R5 and R6 each independently is H, C1-8 alkyl, Bn or Ph,—O—CO—R7 wherein R7 is alkyl,O—CO—C2H4—COOH, or—N3, —R2 denotes that C17 is substituted with —H,—OH,halogen,C1-8 alkyl,C1-8 alkoxy,C2-6 alkenyl,Bn optionally substituted with C1-8 alkyl, C1-8 alkoxy, cyano, nitro, amino, carboxyl or halogen,Ph- optionally substituted with C1-8 alkyl, C1-8 alkoxy, cyano, nitro, carboxyl or halogen, orBn-O—, R3 denotes that C20 is substituted with —H,—OH,C1-8 alkyl,Bn,—NR8R9 wherein R8 and R9 each independently is H, C1-8 alkyl or Bn,═CR10R11 wherein R10 and R11 each independently is H or C1-7 alkyl, or═O, R4 denotes that C16 is substituted with —H,—OH, or=0, with the proviso that when the bond between C16 and C17 is double, R2 is absent and the bond between C17 and C20 is single, andwhen the bond between C17 and C20 is double, C20 is substituted with —H or —OH and R2 is absent,when the bond between C4 and C5 is double, the bond between C5 and C6 is single and inversely, for use in the treatment of a pathologic condition or disorder selected from the group consisting of bladder and gastrointestinal disorders; inflammatory diseases; cardiovascular diseases; nephropathies; glaucoma; spasticity; cancer; osteoporosis; metabolic disorders; obesity; addiction, dependence, abuse and relapse related disorders; psychiatric and neurological disorders; neurodegenerative disorders; autoimmune hepatitis and encephalitis; pain; reproductive disorders and skin inflammatory and fibrotic diseases.
地址 Paris FR