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    PURINE COMPOUNDS AS HSP90 PROTEIN INHIBITORS FOR THE TREATMENT OF CANCER
    1.
    发明公开
    PURINE COMPOUNDS AS HSP90 PROTEIN INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
    嘌呤化合物AS HSP90蛋白抑制剂用于癌症的治疗

    公开(公告)号：EP2004648A1

    公开(公告)日：2008-12-24

    申请号：EP06779505.4

    申请日：2006-09-20

    申请人： Vernalis (R&D) Limited ,  Cancer Research Technology Limited ,  The Institute of Cancer Research

    发明人： BROUGH, Paul ,  DRYSDALE, Martin ,  BARRIL-ALONSO, Xavier

    IPC分类号： C07D473/40 ,  C07D473/36 ,  C07D473/28 ,  A61K31/52 ,  A61P35/00

    CPC分类号： C07D473/40 ,  C07D473/30 ,  C07D473/36

    摘要： Compounds of formula (I) are inhibitors of HSP90, and of utility in the treatment of, for example, cancers: wherein ring A is an aryl or heteroaryl ring or ring system; R1 is hydrogen, fluoro, chloro, bromo, or a radical of formula (1A): -X-AIk1 -(Z)m-(Alk2)n-Q (IA) wherein X is a bond, -O-, -S- -S(O)-, -SO2-, or -NH-, Z is -O-, -S-, -(C=O)-, -(C=S)-, -S(O)-, -SO2-, -NRA-, or, in either orientation -C(=O)O-, -C(=O)NRA-, -C(=S)NRA-, -SO2NRA-, -NRAC(=O)-, or -NRASO2- wherein RA is hydrogen or C1-C6 alkyl in which one or more hydrogens is optionally substituted by fluorine; AIk1 and AIk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m and n are independently 0 or 1 , and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is cyano (-CN), fluoro, chloro, bromo, methyl, ethyl, -OH, -CH2OH, -C(=O)NH2, -C(=O)H, -C(=O)CH3, or -NH2; R3 and R4 are independently selected from hydrogen, fluoro, chloro, bromo, cyano (-CN), C1C3alkyl optionally substituted with one or more fluorine substituents, C1C3alkoxy optionally substituted with one or more fluorine substituents, -CH=CH2, -C=CH, cyclopropyl and -NH2, or R3 and R4 together represent a carbocyclic or heterocyclic ring fused to ring A, or methylenedioxy (-OCH2O-) or ethylenedioxy (-OCH2CH2O-) in either of which one or more hydrogens are optionally replaced by fluorine; Si is hydrogen, or a substituent as defined in the specification.

    PYRIMIDOTHIOPHENE COMPOUNDS
    2.
    发明公开
    PYRIMIDOTHIOPHENE COMPOUNDS 有权
    嘧啶并噻吩化合物

    公开(公告)号：EP1675861A1

    公开(公告)日：2006-07-05

    申请号：EP04768197.8

    申请日：2004-08-26

    申请人： Vernalis (Cambridge) Limited ,  Cancer Research Technology Limited ,  The Institute of Cancer Research

    发明人： DYMOCK, Brian William, Evotec OAI Ltd ,  DRYSDALE, Martin James, Vernalis (Cambridge) Ltd ,  FROMONT, Christofe, Vernalis (Cambridge) Ltd ,  JORDAN, Allan, Vernalis (Cambridge) Limited ,  BARRIL-ALONSO, Xavier

    IPC分类号： C07D495/04 ,  A61K31/00 ,  A61P35/00

    CPC分类号： C07D495/04 ,  A61K31/519

    摘要： Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer: wherein R2 is a group of formula -(Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk' and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is -0-, -S-, -(C=O)-, -(C=S)-, -S02-, -C(=O)O-, -C(=O) NR A- , -C(=S)NR A-, -S02NR A-, -NR AC(=O)_, -NR AS02- or-NR A-wherein R A is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.

    摘要翻译： 式（1）化合物是体外或体内HSP90活性抑制剂，特别是用于治疗癌症：其中R2是式 - （Ar1）m-（Alk1）P-（Z） （Alk2）SQ其中Ar1是任选取代的芳基或杂芳基，Alk'和Alk2是任选取代的二价C1-C3亚烷基或C2-C3亚烯基，m，p，r和s独立地是0或1， （O）O - ， - C（= O）NR A - ， - （C = （= S）NR A - ， - SO 2 NR A - ， - NR AC（= O） - ，-NR ASO 2 - 或-NR A - ，其中RA是氢或C 1 -C 6烷基，并且Q是氢或任选 取代的碳环或杂环基团; R3是氢，任选的取代基或任选取代的（C1-C6）烷基，芳基或杂芳基; R4是羧酸酯，羧酰胺或磺酰胺基团。