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1.发明授权Pyrimido�5,4!-dipyrimidines, pharmaceuticals containing them, their use and processes for the preparation thereof 失效嘧啶并[5,4] - 二嘧啶，含有它们的药物，其用途和制备方法
公开(公告)号：US5821240A
公开(公告)日：1998-10-13
申请号：US811907
申请日：1997-03-05
IPC分类号： A61K31/00 , A61K31/505 , A61K31/519 , A61K31/529 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K31/541 , A61K31/55 , A61K31/551 , A61P17/00 , A61P17/06 , A61P35/00 , A61P37/00 , A61P43/00 , C07D487/04 , C07D519/00
CPC分类号： C07D487/04
摘要： Pyrimido�5,4-d!pyrimidines of the general formula ##STR1## which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of disorders, in particular of oncoses, and their preparation. Exemplary compounds are: 4-�(3-Chloro-4-fluorophenyl)amino!-6-�1-methyl-4-piperidinylamino!pyrimido�5,4-d!pyrimidine, and 4-�(3-Chloro-4-fluorophenyl)amino!-6-�trans-4-dimethyl-aminocycohexylamino!pyrimido�5,4-d!pyrimidine.
摘要翻译： 对通过酪氨酸激酶介导的信号转导具有抑制作用的通式为（IMA）的吡啶并[5,4-d]嘧啶，其用于治疗疾病，特别是肿瘤的用途及其制备。 示例性的化合物是：4 - [（3-氯-4-氟苯基）氨基] -6- [1-甲基-4-哌啶基氨基]吡啶并[5,4-d]嘧啶和4 - [（3-氯 - 4-氟苯基）氨基] -6- [反式-4-二甲基 - 氨基胞嘧啶]嘧啶并[5,4-d]嘧啶。
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2.发明授权Pyrimido�5,4-D!pyrimidines, medicaments comprising these compounds, their use and processes for their preparation 失效嘧啶并[5,4-D]嘧啶，包含这些化合物的药物，其用途和制备方法
公开(公告)号：US5707989A
公开(公告)日：1998-01-13
申请号：US524707
申请日：1995-09-07
IPC分类号： A61K31/505 , A61P7/00 , A61P9/00 , A61P17/06 , A61P29/00 , A61P35/00 , A61P37/00 , C07D487/04 , C07F9/6561 , C07D413/14 , A61K31/535 , A61K31/54 , C07D417/14
CPC分类号： C07D487/04 , C07F9/6561
摘要： The present invention relates to pyrimido�5,4-d!pyrimidines of the general formula ##STR1## in which R.sub.a to R.sub.c are as defined herein, their tautomers, their stereoisomers and their salts, in particular their physiologically tolerated salts with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibiting action on signal transduction mediated by tyrosine kinases, their use for the treatment of diseases, in particular tumor diseases.
摘要翻译： 本发明涉及通式为（I）的其中R a至R c如本文所定义的嘧啶并[5,4-d]嘧啶，其互变异构体，其立体异构体及其盐，特别是其生理上耐受的盐， 具有有价值的药理学特性的无机或有机酸或碱，特别是对由酪氨酸激酶介导的信号转导的抑制作用，其用于治疗疾病，特别是肿瘤疾病的用途。
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3.发明授权Pyrimido [5, 4-d] pyrimidines, pharmaceuticals containing these compounds, their use and processes for their preparation 失效嘧啶并[4,5-d]嘧啶，含有这些化合物的药物，其用途及其制备方法
公开(公告)号：US5977102A
公开(公告)日：1999-11-02
申请号：US812002
申请日：1997-03-05
IPC分类号： A61K31/00 , A61K31/505 , A61K31/519 , A61K31/529 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61P17/00 , A61P17/06 , A61P35/00 , A61P37/00 , A61P43/00 , C07D487/04 , C07D519/00 , A61K31/495
CPC分类号： C07D487/04
摘要： Pyrimido[5,4-d]pyrimidines of the general formula ##STR1## which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of oncoses, and their preparation. Exemplary compounds are:(a) 4-(5-indolylamino)-6-morpholinopyrimido[5,4-d]pyrimidine;(b) 4-(5-indolylamino)-6-[trans-(4-hydroxycyclohexyl)amino]pyrimido[5,4-d]pyrimidine;(c) 4-[(3-chloro-4-fluorophenyl)amino]-6-[4-(morpholinocarbonylmethyl)-1-piperazinyl]pyrimido[5,4-d]pyrimidine;(d) 4-[(3-chloro-4-fluorophenyl)amino]-6-[(4-morpholinyl)amino]pyrimido[5,4-d]pyrimidine;(e) 4-[(3-chloro-4-fluorophenyl)amino]-6-(4-picolylamino)pyrimido[5,4-d]pyrimidine;(f) 4-[(3-chloro-4-fluorophenyl)amino]-6-[1-trifluoroacetyl-4-piperidinylamino]pyrimido[5,4-d]pyrimidine;(g) 4-[(3-chloro-4-fluorophenyl)amino]-6-(endo-tropinylamino)pyrimido[5,4-d]pyrimidine; and,(h) 4-[(3-chloro-4-fluorophenyl)amino]-6-(exo-tropinylamino)pyrimido[5,4-d]pyrimidine.
摘要翻译： 对通过酪氨酸激酶介导的信号转导具有抑制作用的通式的嘧啶并[5,4-d]嘧啶，其用于治疗肿瘤的用途及其制备。 示例性化合物是：（a）4-（5-吲哚基氨基）-6-吗啉代嘧啶并嘧啶并[5,4-d]嘧啶; （b）4-（5-吲哚基氨基）-6- [反 - （4-羟基环己基）氨基]嘧啶并[5,4-d]嘧啶; （c）4 - [（3-氯-4-氟苯基）氨基] -6- [4-（吗啉代羰基甲基）-1-哌嗪基]嘧啶并[5,4-d]嘧啶; （d）4 - [（3-氯-4-氟苯基）氨基] -6 - [（4-吗啉基）氨基]嘧啶并[5,4-d]嘧啶; （e）4 - [（3-氯-4-氟苯基）氨基] -6-（4-吡啶甲基氨基）嘧啶并[5,4-d]嘧啶; （f）4 - [（3-氯-4-氟苯基）氨基] -6- [1-三氟乙酰基-4-哌啶基氨基]嘧啶并[5,4-d]嘧啶; （g）4 - [（3-氯-4-氟苯基）氨基] -6-（内酰基氨基）嘧啶并[5,4-d]嘧啶; 和（h）4 - [（3-氯-4-氟苯基）氨基] -6-（外 - 叔丙基氨基）嘧啶并[5,4-d]嘧啶。
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