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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 /SUPis hydrogen or CSUB1-4 /SUBhydrocarbyl optionally substituted by hydroxy or CSUB1-4 /SUBalkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; RSUP1 /SUPis hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a CSUB1-8 /SUBhydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, CSUB1-4 /SUBhydrocarbyloxy, amino, mono- or di-CSUB1-4 /SUBhydrocarbylamino, 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 /SUPis hydrogen; halogen; CSUB1-4 /SUBalkoxy (e.g. methoxy); or a CSUB1-4 /SUBhydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or CSUB1-4 /SUBalkoxy (e.g. methoxy); RSUP3 /SUPis selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and RSUP4 /SUPis hydrogen or a CSUB1-4 /SUBhydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or CSUB1-4 /SUBalkoxy (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,CO,NR 9 (CO)或0(CO),其中R 9 是氢或C 1-4 任选地被羟基或C 1-4 烷氧基取代的烃基; Y是长为1、2或3个碳原子的键或亚烷基链; 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 SUB 1-4 烷氧基,氨基,单-或-的取代基取代的C 1-8 烃基二-C 1-4 烃基氨基和具有3至12个环成员的碳环或杂环基,其中烃基的碳原子中的1个或2个可以任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);或任选地被卤素(例如氟),羟基或C 1-4烷氧基(例如甲氧基)取代的C SUB 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 是氢或任选被卤素(例如氟),羟基或C 1-4 烷氧基取代的C 1-4 烃基(例如甲氧基)。

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