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    • 4. 发明公开
    • PHARMACEUTICAL COMPOUNDS
    • 药物化合物
    • EP1845973A1
    • 2007-10-24
    • EP06700879.7
    • 2006-01-20
    • Astex Therapeutics Limited
    • CURRY, Jayne ElizabethLYONS, John FrancisSQUIRES, Matthew SimonTHOMPSON, Neil ThomasTHOMPSON, Kyla MerriomWYATT, Paul Graham
    • A61K31/415A61K31/4155A61P35/00A61K31/4196A61K31/5685A61K31/135A61K31/565A61K31/4535A61K31/138A61K39/395A61K31/255A61K31/675A61K31/195A61K31/4188
    • A61K31/5685A61K31/135A61K31/138A61K31/195A61K31/255A61K31/415A61K31/4155A61K31/4188A61K31/4196A61K31/4535A61K31/565A61K31/675A61K39/395A61K45/06A61K2300/00
    • 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).
    • 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。