发明名称 FUSED IMIDAZOLYL-4 PIPERIDINAMINES
摘要 Pharmaceutical compsn. comprises as active ingredient a therapeuticall effective ant. of an N-(4-piperidinyl)-3H-imidazo (4,5-b) pyridine-2-amine or N-(4-piperidinyl)-1H-benzimidazole-2-amine cpd. of formula (I) or its pharmaceutically acceptable acid addn. salt or steroisomer: where L=H, 1-6C alkoxy-carbonyl or benzyloxyearbonyl, A= gp. of formula (a) -CH=CH-CH=CH-, (b) -N=CH-CH=CH-, (c) -CH2N-CH=CH-, (d) -CH0CH-N=CH- or (e) -CH=CH-CH=N-, where 1 or 2 H atoms of (a) - (e) may be replaced by halogen, 1-6C alkyl, 1-6C alkoxy, CF3 and/or OH gp(s).; R= H or 1-6C alkyl; R1=H, 1-10C alky, 3-6C cycloalkyl, Ar1 or 1-6C alkyl substd. by 1 or 2 Ar1; R2= H, 1-6C alkyl, 3-6C cycloalkyl, 1-6C alkyl -(O-, 1-6C alkoxy-CO- or Ar2 - 1-6C alkyl; Ar1 = phenyl (opt. substd. by 1-3 of halogen, OH, N02, CN CF3, 1-6C alyl, 1-6C alkoxy, 1-6C alkylthio, SH, NH2, mono-or di-(1-6C alkyl)-amino, carboxyl, 1-6C alkoxy -carbonyl and/or 1-6C alkyl -co-), thienyl, halothienyl, furanyl, 1-6C alkyl-furanyl, pyridinyl, pyraxinyl, thiazolyl or imidazolyl opt. substd. by 1-6C alkyl, and Ar2 = phenyl opt. substd. as in Ar1. Cpds. of formula (I) and salts and stereoisomers are new where R1=R1a= 1-6C alkyl substd. with 1-6C alkyl-substd. furanyl other than 5-methyl-2-furanyl.
申请公布号 AU6821887(A) 申请公布日期 1987.08.06
申请号 AU19870068218 申请日期 1987.02.02
申请人 JANSSEN PHARMACEUTICAL N.V. 发明人 FRANS EDUARD JANSSENS;JOZEF FRANCIS HENS;JOSEPH LEO GHISLANUS TORREMANS;JOZEF JAN PIETER HEYKANTS
分类号 A61K31/415;A61K31/4184;A61K31/435;A61K31/4427;A61K31/443;A61K31/4433;A61K31/445;A61K31/454;A61P37/08;A61P43/00;C07D235/30;C07D401/12;C07D401/14;C07D405/14;C07D409/14;C07D417/14;C07D471/04 主分类号 A61K31/415
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