发明名称 SUBSTITUTED PYRROLIDINONE DERIVATIVES AND PROCESSES FOR THE MANUFACTURE THEREOF
摘要 Lactam peptides of the formula I and their salts <IMAGE> which can be used for the treatment of insufficiency of cerebral ability, process and novel intermediate products for the preparation of these compounds, pharmaceutical preparations which contain these compounds, and their use for the production of pharmaceutical preparations or as pharmacologically active compounds. In formula I, Z denotes an alkylene radical which is unsubstituted or substituted by free or functionally modified hydroxyl and/or by aryl and which, together with the amide group, forms a five-membered ring, R<1> denotes hydrogen, or lower alkyl or aryl which are unsubstituted or substituted by aryl or by free or functionally modified hydroxyl, X denotes oxygen or the group NR<2> in which R<2> represents hydrogen or lower alkyl, R<3> denotes hydrogen, or lower alkyl or aryl which are unsubstituted or substituted by free or functionally modified hydroxyl, aryl, aminocarbonyl, mercapto, methylthio, free, alkylated or acylated amino, guanidino, free, esterified or amidated carboxyl or imidazol-4-yl, or R<2> and R<3> together denote trimethylene which is unsubstituted or substituted by free or functionally modified hydroxyl, R<4> denotes hydrogen or lower alkyl, W denotes a radical, which is in each case bonded to the carbonyl C atom in the radical of the formula II <IMAGE> of the formula III, IV, V or VI <IMAGE> in which R<6>, R<8> and R<1><0> independently of one another represent hydrogen or lower alkyl, R<5>, R<7>, R<9> and R<1><1> independently of one another represent hydrogen, or lower alkyl or aryl which are unsubstituted or substituted by free or functionally modified hydroxyl, aryl, aminocarbonyl, mercapto, methylthio, free, alkylated or acylated amino, guanidino, free, esterified or amidated carboxyl or imidazol-4-yl, or R<4> and R<5> together, R<6> and R<7> together, R<8> and R<9> together and/or R<1><0> and R<1><1> together each independently of one another represent trimethylene which is unsubstituted or substituted by free or functionally modified hydroxyl, and R<1><2> and R<1><3> independently of one another denote hydrogen or lower alkyl or R<1><2> and R<1><3> together denote tetra- or pentamethylene, 3-oxa-1,5-pentylene or 3-aza-3-methyl-1,5-pentylene which is unsubstituted or substituted by oxo or methyl. The subject-matter of the invention does not include compounds of the formula I in which Z denotes unsubstituted alkylene having 3 C atoms and at the same time R<1> denotes hydrogen, unsubstituted alkyl having 1-4 C atoms, aryl or aryl-lower alkyl, X denotes the radical NH, R<3> denotes aryl, unsubstituted alkyl or hydrogen, R<4> denotes hydrogen, W denotes a radical of the formula III in which R<5> has a meaning identical to the radical R<3>, and R<1><2> and R<1><3> denote hydrogen.t
申请公布号 ZA8400595(B) 申请公布日期 1984.11.28
申请号 ZA19840000595 申请日期 1984.01.26
申请人 CIBA-GEIGY AG. 发明人 WILLIAM BENCZE;BRUNO KAMBER;ANGELO STORNI
分类号 C09D11/00;A61K38/00;A61P25/04;C07D207/12;C07K1/113;C07K5/04;C07K5/06;C07K5/103;C07K7/06;C09D11/10 主分类号 C09D11/00
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