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    Process for preparing azacycloalkanoylaminothiazoles
    6.
    发明授权
    Process for preparing azacycloalkanoylaminothiazoles 有权
    制备氮杂环烷酰氨基噻唑的方法

    公开(公告)号：US06414156B2

    公开(公告)日：2002-07-02

    申请号：US09746060

    申请日：2000-12-22

    申请人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Mark E. Salvati ,  Joseph E. Sundeen ,  Hai-Yun Xiao ,  Rulin Zhao

    发明人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Mark E. Salvati ,  Joseph E. Sundeen ,  Hai-Yun Xiao ,  Rulin Zhao

    IPC分类号： C07D41714

    CPC分类号： C07D417/12 ,  A61K31/427 ,  A61K31/454 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D417/14

    摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or 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; and n 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.

    摘要翻译： 本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的，有效的方法，其中：R是烷基，芳基或杂芳基; R 1，R 2，R 3， R4和R5各自独立地为氢，烷基，芳基或杂芳基; R6和R7各自独立地为氢，烷基，芳基，杂芳基，卤素，羟基或烷氧基; R8为氢，烷基，芳基，杂芳基，CONR9R10，COR11或COOR12; R9，R10，R11和R12各自独立地为氢，烷基或芳基; m等于0至5; 和等于0至5，这是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。 本发明还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。

    Process for preparing azacycloalkanoylaminothiazoles
    8.
    发明授权
    Process for preparing azacycloalkanoylaminothiazoles 有权
    制备氮杂环烷酰氨基噻唑的方法

    公开(公告)号：US06639074B2

    公开(公告)日：2003-10-28

    申请号：US10100129

    申请日：2002-03-18

    申请人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Mark E. Salvati ,  Joseph E. Sundeen ,  Hai-Yun Xiao ,  Rulin Zhao

    发明人： Bang-Chi Chen ,  Kyoung S. Kim ,  S. David Kimball ,  Raj N. Misra ,  Mark E. Salvati ,  Joseph E. Sundeen ,  Hai-Yun Xiao ,  Rulin Zhao

    IPC分类号： C07D47100

    CPC分类号： C07D417/12 ,  A61K31/427 ,  A61K31/454 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D417/14

    摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula I or 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; and n 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.

    摘要翻译： 本发明涉及制备式I的5-（2-恶唑基烷硫基）-2-氮杂环烷酰氨基噻唑化合物或其药学上可接受的盐的新的，有效的方法，其中：R是烷基，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是氢，烷基，芳基，杂芳基，CONR 9 R 10，COR 11或COOR 12; R 9，R 10，R 11 且R 12各自独立地为氢，烷基或芳基; m等于0至5; 和等于0至5，这是细胞周期蛋白依赖性激酶（cdks）的新型有效抑制剂。 本发明还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。