首页> 外国专利> 3,4-tvíútskipt 1H-pýrasólefnasambönd og notkun þeirra sem stilla syklínháðra kínasa (CDK) og glýkógensyntasakínasa-3 (GSK-3)

3,4-tvíútskipt 1H-pýrasólefnasambönd og notkun þeirra sem stilla syklínháðra kínasa (CDK) og glýkógensyntasakínasa-3 (GSK-3)

机译:3,4-双取代的1H-吡唑化合物及其作为细胞周期蛋白依赖性激酶(CDK)和糖原合酶激酶3(GSK-3)调节剂的用途

摘要

The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dcpcndcnt kinase and glycogen synthase kinase-3. In formula (0): X is a group R 1 -A-NR 4 - or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO 2 , C=O, NR g (C=O) or O(C=O) wherein R g is hydrogen or C 1-4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R 1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C 1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C 1-4 hydrocarbyloxy, amino, mono- or di-C 1-4 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, SO 2 ; R 2 is hydrogen; halogen; C 1-4 alkoxy (e.g. methoxy); or a C 1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C 1-4 alkoxy (e.g. methoxy); R 3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R 4 is hydrogen or a C 1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C 1-4 alkoxy (e.g. methoxy).
机译:本发明提供式(0)化合物或其盐或互变异构体或N-氧化物或溶剂化物,其用于预防或治疗疾病状态和病症,例如由细胞周期蛋白-dcpcndcnt激酶和糖原合酶激酶-3介导的癌症。在公式(0)中:X是基团R 1 -A-NR 4-或5-或6-元碳环或杂环;A为键,SO 2,C = O,NR g(C = O)或O(C = O),其中R g为氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基;Y是长为1、2或3个碳原子的键或亚烷基链;R 1为氢;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以下的取代基取代的C 1-8烃基:卤素(例如氟),羟基,C 1-4烃氧基,氨基,单或二C 1-4烃基氨基以及具有以下基团的碳环或杂环基3至12个环成员,并且其中烃基的碳原子中的1或2可以任选地被选自O,S,NH,SO,SO 2的原子或基团取代;R 2为氢;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 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;和R 4是氢或任选地被卤素(例如氟),羟基或C 1-4烷氧基(例如甲氧基)取代的C 1-4烃基。

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