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PROCESS FOR THE PREPARATION OF AZACICLOALCANOYLAMINOTIAZOLES

机译：制备氮杂竹碳酰氨基噻唑的方法

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摘要

The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula Ior a pharmaceutically acceptable salt thereof, wherein:R is alkyl, aryl or heteroaryl;R1, R2, R3, R4 and R5 are each independently hydrogen, alkyl, aryl or heteroaryl;R6 and R7 are each independently hydrogen, alkyl, aryl, heteroaryl, halogen, hydroxy or alkoxy;R8 is hydrogen, alkyl, aryl, heteroaryl, CONR9R10, COR11 or COOR12;R9, R10, R11 and R12 are each independently hydrogen, alkyl or aryl;m equals 0 to 5; andn equals 0 to 5,which are novel, potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula III' and a 2-oxazolylalkyl derivative of formula IX.

机译：本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-氮杂环烷酰基氨基噻唑化合物或其药学上可接受的盐的新的有效方法，其中：R为烷基，芳基或杂芳基; R 1，R 2，R 3，R 4和R 5各自独立地为氢，烷基，芳基或杂芳基; R 6和R 7各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; R 8为氢，烷基，芳基，杂芳基，CONR 9 R 10，COR 11或COOR 12; R 9，R 10，R 11 R和R 12各自独立地为氢，烷基或芳基; m等于0至5; andn等于0到5，这是新型的有效的细胞周期蛋白依赖性激酶（cdks）抑制剂。本发明进一步涉及新的关键中间体化合物，式III′的季铵盐和式IX的2-恶唑基烷基衍生物。

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公开/公告号PT1303514E

专利类型
公开/公告日2005-11-30

原文格式PDF
申请/专利权人 BRISTOL-MYERS SQUIBB COMPANY;
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申请/专利号PT20010932879T
发明设计人 SALVATI MARK E.;XIAO HAI-YUN;CHEN BANG-CHI;KIM KYOUNG S.;KIMBALL S. DAVID;MISRA RAJ N.;SUNDEEN JOSEPH E.;ZHAO RULIN;
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申请日2001-05-02
分类号C07D417/14;C07D487/18;C07D263/32;
国家 PT
入库时间 2022-08-21 21:37:51

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