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专利概况
专利名称 CONDENSED DERIVATIVES OF IMIDAZOLE AND PYRAZOLE AS MODULATORS OF ACTIVITY TNF
申请号 RU2016126971 申请日
公开(公告)号 RU2687093C1 公开(公告)日
申请(专利权)人 UCB BIOPHARMA SPRL 发明人 ALEKSANDER Rikki Piter; BENTLI Dzhonatan Mark; BREJS Garet Nil; BRUKINGS Daniel Kristofer; CHOVATIA Praful Tulshi; DEBOV Erve Zhan Klod; DZHONSTOUN Krejg; DZHOUNS Elizabet Perl; KROPLIN Boris; LEKOMT Faben Klod; MADDEN Dzhejms; MILLER Krejg Ejdrian; PORTER Dzhon Robert; SELBI Mattyu Dankan; SHO Majkl Alan; VAIDYA Darshan Gunvant; YULE Ajan Endryu
专利来源 国家知识产权局 转化方式
摘要

FIELD : chemistry.SUBSTANCE : present invention relates to a compound of formula (IIB-A) and a pharmaceutically acceptable salt thereof, which can be used in medicine : (IIB-A), where A denotes C-R2 or N; D denotes C-R4 or N; E denotes -CH2- or -CH(CH3)-; Y denotes a group of formula : , where sign (*) denotes position of attachment to the rest of the molecule; R1g denotes hydrogen, fluorine, chlorine, bromine, cyano group, trifluoromethyl, hydroxyisopropyl, methylthio group, methylsulphinyl, methylsulphonyl, carboxy group, methoxycarbonyl, aminocarbonyl, methylaminocarbonyl, ethylaminocarbonyl, isopropylaminocarbonyl, dimethylaminocarbonyl, hydroxyethylaminocarbonyl, hydroxyisopropylaminocarbonyl, 1-hydroxy-2-methylprop-2-ylaminocarbonyl, methoxyethylaminocarbonyl, cyclopropylaminocarbonyl, oxazolylmethylaminocarbonyl, hydroxyoxetanyl, methoxy oxetanyl, piperazinylcarbonyl, hydroxypyrrolidinylcarbonyl, oxopiperazinylcarbonyl, methylsulphonylazetidinylcarbonyl or tert-butoxycarbonylpiperazinylcarbonyl; R2g and R3g are hydrogen or halogen; R7a and R7b denote hydrogen or C1-C6-alkyl; R8a and R8b denote hydrogen, halogen or C1-C6-alkyl; or R8a and R8b together with the carbon atom to which they are both bonded, denote cyclopropyl; R9a and R9b independently denote hydrogen or C1-C6-alkyl; R2 is hydrogen or halogen; R4 denotes hydrogen; R5 denotes C1-C6-alkyl, optionally substituted with halogen, hydroxy group or C1-C6-alkoxy group; V denotes C-R22 or N; R21 denotes hydroxy(C1-C6)alkyl, methylsulphonyl, methylsulphoxyminyl, ethylsulphoxyminyl or (methyl)(N-methyl)sulfoxyminyl; or R21 denotes cyclopropyl, cyclobutyl, cyclohexyl, oxetanyl, azetidinyl, tetrahydropyranyl, piperidinyl, piperazinyl, morpholinyl, diazepanyl, 6-oxa-3-azabicyclo[3.1.1]heptanyl, 3-azabicyclo-[3.2.1]octanyl, 3, 7-dioxa-9-azabicyclo[3.3.1]nonanyl, 3-oxa-6-azaspiro[3.3]heptanyl or 6-thia-2-azaspiro[3.3]heptanyl, any of these groups may optionally contain 1, 2 or 3 substitutes independently selected from a group comprising halogen, C1-C6-alkyl, trifluoromethyl, hydroxy group, oxo group, amino group, carboxy group and C2-C6-alkoxycarbonyl; R22 denotes hydrogen, halogen or C1-C6-alkyl; and R23 denotes hydrogen, C1-C6-alkyl, trifluoromethyl or C1-C6-alkoxy group.EFFECT : novel effective inhibitors of TNFα activity are disclosed and pharmaceutical compositions based thereon for treating rheumatoid arthritis or Crohn' s disease.7 cl, 256 ex

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