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3 条记录 (耗时 0.015 秒)

    PHARMACEUTICAL COMPOUNDS
    1.
    发明公开
    PHARMACEUTICAL COMPOUNDS 有权
    药物化合物

    公开(公告)号：EP1845973A1

    公开(公告)日：2007-10-24

    申请号：EP06700879.7

    申请日：2006-01-20

    申请人： Astex Therapeutics Limited

    发明人： CURRY, Jayne Elizabeth ,  LYONS, John Francis ,  SQUIRES, Matthew Simon ,  THOMPSON, Neil Thomas ,  THOMPSON, Kyla Merriom ,  WYATT, Paul Graham

    IPC分类号： A61K31/415 ,  A61K31/4155 ,  A61P35/00 ,  A61K31/4196 ,  A61K31/5685 ,  A61K31/135 ,  A61K31/565 ,  A61K31/4535 ,  A61K31/138 ,  A61K39/395 ,  A61K31/255 ,  A61K31/675 ,  A61K31/195 ,  A61K31/4188

    CPC分类号： A61K31/5685 ,  A61K31/135 ,  A61K31/138 ,  A61K31/195 ,  A61K31/255 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4188 ,  A61K31/4196 ,  A61K31/4535 ,  A61K31/565 ,  A61K31/675 ,  A61K39/395 ,  A61K45/06 ,  A61K2300/00

    摘要： The invention provides a combination of an ancillary agent and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein the ancillary agent is selected from: a monoclonal antibody, an alkylating agent, an anticancer agent, a further CDK inhibitor and a hormone, hormone agonist, hormone antagonist or hormone modulating agent; X is a group R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C=O, NR9(C=O) or 0(C=O) wherein R9 is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1 , 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).

    摘要翻译： 本发明提供了辅助剂和具有式（0）的化合物的组合：或其盐或互变异构体或N-氧化物或溶剂合物; 其中所述辅助剂选自：单克隆抗体，烷化剂，抗癌剂，另外的CDK抑制剂和激素，激素激动剂，激素拮抗剂或激素调节剂; X是基团R1-A-NR4-或5-或6-元碳环或杂环; A是键，SO 2，C = O，NR 9（C = O）或O（C = O），其中R 9是氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; Y是长度为1,2或3个碳原子的键或亚烷基链; R1是氢; 具有3至12个环成员的碳环或杂环基; 或任选被一个或多个选自卤素（例如氟），羟基，C 1-4烃氧基，氨基，单或二-C 1-4烃基氨基和具有3至4个碳原子的杂环基团取代的取代基取代的C 1-8烃基 12个环成员，并且其中烃基的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团替代; R2是氢; 卤素; C 1-4烷氧基（例如甲氧基）; 或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基; R3选自氢和具有3至12个环成员的碳环和杂环基团; 并且R 4是氢或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基。