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COMBINATIONS OF PYRAZOLE KINASE INHIBITORS AND FURTHER ANTITUMOR AGENTS.

机译:吡唑激酶抑制剂和进一步的抗肿瘤药物的组合。

摘要

The invention provides a combination of a compound having the formula (0) and two or more further anti-cancer agents: or salts or tautomers or N-oxides or solvates thereof; wherein X is a group Rsup1/sup-A-NRsup4/sup- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C=O, NRsup9/sup(C=O) or 0(C=O) wherein Rsup9/sup is hydrogen or Csub1-4/sub hydrocarbyl optionally substituted by hydroxy or Csub1-4/sub alkoxy; Y is a bond or an alkylene chain of 1 , 2 or 3 carbon atoms in length; Rsup1/sup is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a Csub1-8/sub hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, Csub1-4/sub hydrocarbyloxy, amino, mono- or di-Csub1-4/sub 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, SOsub2/sub; Rsup2/sup is hydrogen; halogen; Csub1-4/sub alkoxy (e.g. methoxy); or a Csub1-4/sub hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or Csub1-4/sub alkoxy (e.g. methoxy); Rsup3/sup is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and Rsup4 /supis hydrogen or a Csub1-4/sub hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or Csub1-4/sub alkoxy (e.g. methoxy).
机译:本发明提供了具有式(0)的化合物和两种或更多种其他抗癌剂的组合:或其盐或互变异构体或N-氧化物或溶剂化物;其中X是基团R 1 -A-NR 4 -或5-或6-元碳环或杂环; A是一个键,SO2,C = O,NR 9 (C = O)或0(C = O)其中R 9 是氢或C 1 -4 烃基,可选地被羟基或C 1-4 烷氧基取代; Y是键或长度为1、2或3个碳原子的亚烷基链; R 1 是氢;具有3至12个环成员的碳环或杂环基;或任选地被一个或多个选自卤素(例如氟),羟基,C 1-4取代的烷氧基,氨基,单-或-的取代基取代的C 1-8取代的C 1-8烷基。 di-C 1-4 烃基氨基和具有3至12个环成员的碳环或杂环基团,其中烃基的1个或2个碳原子可以可选地被原子或基团取代选自O,S,NH,SO,SO 2 ; R 2 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;或R 3 选自氢以及具有3至12个环成员的碳环和杂环基;并且R 4 是氢或C 1-4 烃基,其任选地被卤素(例如氟),羟基或C 1-4 烷氧基取代(例如甲氧基)。

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