发明名称 New peptide-type compounds, useful as protease, especially thrombin, inhibitors for treating e.g. thrombosis and cardiac infarct
摘要 Peptide derivatives (I), their tautomers, stereoisomers (or mixtures) and salts. Peptide derivatives of formula (I), their tautomers, stereoisomers (or mixtures) and salts are new. A = aryl, 3-8C cycloalkyl or cycloalkenyl, optionally fused to phenyl (all optionally substituted by 1-5 halo, OH, SH, CN, CF3, formyl, 1-8C alkylcarbonyl, carboxy, 1-4C alkoxycarbonyl, COOH, 1-4C alkylcarbonyloxy, 1-16C alkyl, 1-8C alkoxy (optionally substituted by 1-8C alkyl), 1-8C alkyl (substituted by 1-8C alkoxy), formyl, or 1-8C alkylcarbonyl), NO2, amino or carboxamido (both optionally substituted by 1-2 1-4C alkyl), 1-4C alkylcarbonylamino, also, for at least partly saturated rings, oxo, and all substituents other than oxo may be present on fused phenyl; D = O or S(O)x; x = 0-2; X = O, S or NR3; R1-R3 = H, 1-16C alkyl, 1-8C alkoxy, 1-8C alkylcarbonyl, 1-4C alkoxycarbonyl, 1-4C alkylcarbonyloxy, 1-8C alkoxy optionally substituted by 1-8C alkyl, 1-8C alkyl substituted by 1-8C alkoxy, formyl, or 1-8C alkylcarbonyl, NO2, amino or carboxamido (both optionally substituted by 1-2 1-4C alkyl), 3-5C cycloalkyl, aryl or benzyl; Y = aryl, 3-8C cycloalkyl or cycloalkenyl, (all of which may be substituents on 1-8C alkyl, alkoxy or 1-8C alkylcarbonyl), all optionally fused to phenyl and optionally substituted as specified for A; E, Z = H, halo, OH, SH, CF3, CN, formyl, 1-8C alkylcarbonyl, carboxy, 1-4C alkoxycarbonyl, COOH, 1-4C alkylcarbonyloxy, 1-16C alkyl, 1-8C alkoxy optionally substituted by 1-8C alkyl, 1-8C alkyl substituted by 1-8C alkoxy, formyl, or 1-8C alkylcarbonyl, NO2, amino or carboxamido (both optionally substituted by 1-2 1-4C alkyl), 1-4C alkylcarbonylamino, aryl, 3-8C cycloalkyl or cycloalkenyl, or 8-12C bicycloalkyl (the last four groups may be linked through CO, 1-8C alkyl, alkoxy, or alkylcarbonyl, aminocarbonyl or 1-8C alkylaminocarbonyl), where all rings may be fused to phenyl and optionally substituted as for A.
申请公布号 DE10124041(A1) 申请公布日期 2002.11.21
申请号 DE2001124041 申请日期 2001.05.16
申请人 GRAFFINITY PHARMACEUTICAL DESIGN GMBH 发明人 CARDEL, BETTINA;METZ, GUENTHER;OTTLEBEN, HOLGER;RAU, HARALD;SCHELLHAAS, NATHALIE;SEKUL, RENATE;VETTER, DIRK
分类号 A61P9/00;A61P19/00;C07D277/30;C07D307/54;C07D405/12;C07D405/14;C07D417/06;C07D417/12;C07D471/04;(IPC1-7):C07D417/02;C07D417/14;C07D307/66;C07B61/00;A61K31/198 主分类号 A61P9/00
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