公开(公告)号：US5185341A

公开(公告)日：1993-02-09

申请号：US787064

申请日：1991-11-04

申请人： Wolfgang Sauer ,  Hans-Joachim Jansch ,  Angelika Rostock ,  Gottfried Faust ,  Christine Siegemund ,  Dieter Lohmann ,  Reni Bartsch

发明人： Wolfgang Sauer ,  Hans-Joachim Jansch ,  Angelika Rostock ,  Gottfried Faust ,  Christine Siegemund ,  Dieter Lohmann ,  Reni Bartsch

IPC分类号： A61K31/505 ,  A61P25/28 ,  C07D239/54 ,  C07D239/545

CPC分类号： C07D239/545

摘要： The substituted 5-(phenoxyalkanoylamino)-uracil compounds have the following formula I: ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen; a branched or linear alkyl group having 1 to 6 carbon atoms; a branched or straight chain alkenyl or alkynyl group having 1 to 6 carbons atoms; a cycloalkyl group having from 3 to 7 carbon atoms or a cycloalkylmethyl group having a cycloalkyl residue of 3 to 7 carbon atoms; or a phenylalkyl group having an alkyl residue having from 1 to 3 carbon atoms and a phenyl residue, the phenyl residue being unsubstituted or having a halogen, methoxy, methyl or trifluoromethyl substituent; R.sub.3 is a hydrogen, methyl or amino groups; R.sub.4 is halogen, methoxy or methyl groups, and n is 1 or 2. Pharmaceutical compositions for treating cerebrovascular, neuronal-degenerative and senility-induced disorders associated with learning, memory and cognitive dysfunctions are described which contain a therapeutically effective amount of the substituted 5-(phenoxyalkanoylamino)-uracil in a pharmaceutically acceptable carrier.

摘要翻译： 取代的5-（苯氧烷酰氨基） - 尿嘧啶化合物具有下式I：其中R 1和R 2各自独立地为氢; 具有1至6个碳原子的支链或直链烷基; 具有1至6个碳原子的支链或直链烯基或炔基; 具有3至7个碳原子的环烷基或具有3至7个碳原子的环烷基残基的环烷基甲基; 或具有1至3个碳原子的烷基残基和苯基残基的苯基烷基，所述苯基残基是未取代的或具有卤素，甲氧基，甲基或三氟甲基取代基; R3是氢，甲基或氨基; R4是卤素，甲氧基或甲基，n是1或2.描述了用于治疗与学习，记忆和认知功能障碍相关的脑血管，神经元退行性和衰老性疾病的药物组合物，其含有治疗有效量的取代的5 - （苯氧烷酰氨基） - 尿嘧啶。

公开(公告)号：US5441973A

公开(公告)日：1995-08-15

申请号：US182665

申请日：1994-01-13

申请人： Lothar Zenker ,  Helmut Wunderlich ,  Dieter Lohmann ,  Angelika Rostock ,  Christine Siegemund ,  Artur V. Valdman ,  Tatjana A. Voronina ,  Ilmira C. Rachmankulova ,  Oleg M. Glozman ,  Taisija L. Garibova ,  Larisa M. Mescerjakova ,  Ljudmila A. Zmurenko ,  Sergej B. Seredenin ,  Grigorij G. Rozancev

发明人： Lothar Zenker ,  Helmut Wunderlich ,  Dieter Lohmann ,  Angelika Rostock ,  Christine Siegemund ,  Artur V. Valdman ,  Tatjana A. Voronina ,  Ilmira C. Rachmankulova ,  Oleg M. Glozman ,  Taisija L. Garibova ,  Larisa M. Mescerjakova ,  Ljudmila A. Zmurenko ,  Sergej B. Seredenin ,  Grigorij G. Rozancev

IPC分类号： A61K31/40 ,  A61K31/4015 ,  A61P25/28 ,  C07D207/26 ,  C07D207/263 ,  C07D207/277 ,  C07D401/06 ,  A61K31/455 ,  C07D401/02 ,  C07D403/02

CPC分类号： C07D207/27 ,  C07D207/26 ,  C07D207/277 ,  C07D401/06

摘要： The invention is directed to N-acetyl-4-phenyl-pyrrolidin-2-ones, which, because of their pronounced cerebroprotective effect in human medicine, can be used for the prophylaxis and treatment of cerebral functional disorders. Pursuant to the invention, these compounds are synthesized by reacting 4-phenyl-pyrrolidin-2-ones with a reactive derivative of a carboxylic acid, or by cyclizing N-acylaminobutyric acid derivatives.

摘要翻译： 本发明涉及N-乙酰基-4-苯基 - 吡咯烷-2-酮，由于其在人类医学中的显着的保护脑保护作用，可用于预防和治疗脑功能障碍。 根据本发明，这些化合物通过4-苯基 - 吡咯烷-2-酮与羧酸的反应性衍生物反应或通过环化N-酰基氨基丁酸衍生物而合成。