Organic Compounds
申请(专利)号:
AR2006P100917
申请日期:
2006-03-10
公开/公告号:
AR053826A1
公开/公告日期:
2007-05-23
申请(专利权)人:
SPEEDEL EXPERIMENTA AG
摘要:
Compounds of the general formula (1) that possess renin inhibitory properties and can be used as medicines. Claim 1: A compound of the formula (1) in which R 1 is a) saturated heterocyclyl which is optionally substituted one or more times with C 1-8 alkanoyl, C 2-6 alkenyl, C 2-6 alkynyl, C 1-6 alkoxy, C1-6 alkoxy-C1-6 alkoxy, C1-6 alkoxy-C1-6 alkyl, C1-6 alkoxycarbonylamino, C1-6 alkyl, C0-6 alkylcarbonylamino, C1-6 alkylcarbonyloxy, C1-6 alkylenedioxy, optionally N- amino mono or N, N-di-amino C1-6 alkylated, aryl, carbamoyl optionally N-mono or N, N-di-alkylated C1-6, optionally esterified carboxy, cyano, C3-8 cycloalkoxy,Cycloquil c3-8-c0-6, halogeno, halo alcoxi C1-6, halo Oceano C1-6, heteromorphic, unsaturated or saturated, partially saturated or saturated, hydroxi, nitro, oxidized or oxo, connected by C atom; or (b) azepanilo -,Al Dingaziridinyl-,Nitrous oxideTwo propylene oxideDimethoxypropyleneDitianilo...Xylene esterF la la Naoxathianyl-,Oxepanlo...Four pyridineTetrahydrofuranFour hydrogen sulfur phosphorusFour hydrazineC17-6, C17, c17-6, c17-6, c17-6 Optional amino acids N-mono or N, n-di-rent C1-6, arilo, carbamoyo optional N-mono or N, n-di-rent C1-6, optional carbon chloride carboxi, cyanogen, cyclopropyloxy C3-8, cyclopentanediol c3-8-tar c0-6, halogen, halogen-methoxyc1-6, heteromorphic, unsaturated, partially saturated, Xi,oxide or oxo; or c) C2-8 alkynyl which is optionally substituted one or more times with C1-8 alkanoyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C1-6 alkoxy-C1-6 alkoxy, C1-6 alkoxy -C 1-6 alkyl, C 1-6 alkoxycarbonylamino, C 1-6 alkyl, C 1-6 alkylcarbonylamino, C 1-6 alkylcarbonyloxy, C 1-6 alkylenedioxy, optionally N-mono or N amino, N-di-C 1-6 alkylated, aryl , optionally N-mono or N, N-di-alkylated C1-6 carbamoyl, optionally esterified carboxy, cyano, C3-8 cycloalkoxy, C3-8 cycloalkyl-C0-6 alkyl, halogen, halo C1-6 alkoxy, halo- C1-6 alkyl, heteroaryl, unsaturated heterocyclyl, partially saturated or saturated, hydroxy, nitro or oxo, or R2 is,independently from each other, 1-4 radicals selected from: C1-8 alkanoyl, C1-8 alkanoyl-C2-4 alkoxy carrying the alkanoyl group in a position greater than alpha, C1-8 alkanoylamino-C1-4 alkoxy, N-C1-4 alkanoylamino-C1-4 alkyl, C1-8 alkanoyloxy-C1-4 alkyl, N'-alkanoyl piperazin C2-8-C1-4 alkoxy, N'-alkanoyl piperazine-C2-8-C1-4 alkyl , C1-8 alkanesulfonyl-C1-4 alkoxy, C1-8 alkanesulfonyl-C1-4 alkyl, alkanesulfonylamino C1-8-C1-4 alkoxy, C1-4-sulfonylamino-C1-4 alkyl, C1-8 sulfonyl- ( hydroxy) C 1-4 alkoxy, C 2-8 alkenyloxy, C 2-8 alkenyloxy, C 1-4 alkoxy, C 2-8 alkenyloxy-C 1-4 alkyl, C 1-8 alkoxy, C 1-6 alkoxy-C 1-6 alkanoyl, C 1- alkoxy 4-C2-4 alkenyl,C1-4 alkoxy-C2-4 alkenyloxy, C1-4 alkoxy- C1-4 alkoxy, C1-4 alkoxy-C1-4 alkoxy-C1-4 alkyl, C1-4 alkoxy-C1-4 alkyl, C1-4 alkoxycarbonyl -C 1-4 alkoxy, C 1-4 alkoxycarbonyl-C 1-4 alkyl, C 1-8 alkoxycarbonylamino-C 1-4 alkoxycarboxylaminoC 1-4 alkyl, C 1-8 alkyl, C 1-4 alkyl, N, N- di-C 1-4 alkylamino, C 1-4 alkylaminoalkoxy, N, N-di-C 1-4 alkylaminoC 1-4 alkoxy, C 1-4 alkylamino-C 1-4 alkyl, N, N-di-C 1-4 alkylamino C1-4, N-mono- or N, N-di-alkylcarbamoyl C1-4-alkoxy C1-4, N-mono- or N, N-di-alkylcarbamoyl C1-4-alkyl C1-4, N'-alkylpiperazin C1-4-C1-4 alkoxy, N'-C1-4 alkylpiperazin-C1-4 alkyl, C1-4 alkylthio-C1-4 alkoxy, C1-4 alkylthio- (hydroxy) C1-4 alkoxy,C 1-4 alkylthio-C 1-4 alkyl, C2-4 amino-alkoxy, C 1-4 alkyl-alkyl, carbamoyl-C 1-4 alkoxy, carbamoyl-C 1-8 alkyl, carboxy-C 1-4 alkoxy, carboxy-C 1- alkyl 4, cyano-C 1-4 alkoxy, cyano-C 1-4 alkyl, C 3-8 cycloalkoxy, C 3-8 cycloalkoxy, C 1-4 alkoxy, C 3-8 cycloalkoxy-C 1-4 alkyl, C 3-8 cycloalkyl, S, S- dioxothiomorpholino-C1-4 alkoxy, S, S-dioxothiomorpholin-alkyl 14, halogen, halo-C1-4 alkoxy, halo-C1-4 alkyl, halo- (hydroxy) C2-8 alkoxy, hydroxy, hydroxy-C2-8 alkoxy , hydroxy-C2-8 alkyl, imidazolylthio-C1-4 alkoxy, imidazolylthio-1-4 alkyl, optionally N-oxidized morpholino-C1-4 alkoxy, morpholin-C1-4 alkyl, S-oxothiomorpholino-C1-4 alkoxy, S -oxythiomorpholino-C1-4alkyl,piperazino-C1-4 alkoxy, piperazino-C1-4 alkyl, piperidino-C1-4 alkoxy, pip
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