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Heteroaryl amines - derivatives of pyrimidine and pyridazine as inhibitors of glycogenesis synthase kinase 3-beta (GSK3 inhibitors)

机译:杂芳基胺-嘧啶和哒嗪衍生物,作为糖原合成酶激酶3-beta的抑制剂(GSK3抑制剂)

摘要

This invention relates to a compound of formula (I) with its N-oxide, pharmaceutically acceptable addition salt, quaternary amine and stereochemically isomeric form, wherein ring A is a 6-membered substituted heterocyclyl derivative of pyrimidinyl or pyridazinyl; R is hydrogen; aryl; formed; C-alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6 alkyloxycarbonyl; X is a direct bond or a linker atom or a linker group; Z is a direct bond or a linker atom or a linker group; R1 is hydrogen, C1-6alkyl, C1-6alkenyl, C1-6alkynyl, carbocycle or heterocycle, each of these groups may be optionally substituted; R is hydrogen; hydroxy; halogen; optionally substituted C1-6alkyl or C1-6alkenyl or C1-6alkynyl; C1-6 alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di (C1-6alkyl) amino; polyhaloSalkyl; polyhaloSalkyloxy; polyhaloSalkylthio; R; R-C1-6alkyl; R-O-; R-S-; R-C (= O) -; R-S (= O) -; R-S (= O) -; R-S (= O) -NH-; R-S (= O) -NH-; R-C (= O) -; -NHC (= O) H; -C (= O) NHNH; R-C (= O) -NH-; R-C (= O) -NH-; -C (= NH) R; -C (= NH) R; R 1 is an optionally substituted heterocycle, with the proviso that —X — R 1 and / or R is other than hydrogen; their use, pharmaceutical compositions containing them and methods for their preparation.
机译:本发明涉及具有N-氧化物,可药用加成盐,季胺和立体化学异构形式的式(Ⅰ)化合物,其中环A是嘧啶基或哒嗪基的6元取代杂环基衍生物; R是氢;芳基形成C-烷基羰基;任选取代的C 1-6烷基; C 1-6烷氧基羰基;任选取代的C 1-6烷氧羰基; X是直接键或连接原子或连接基团; Z是直接键或连接原子或连接基团; R 1是氢,C 1-6烷基,C 1-6烯基,C 1-6炔基,碳环或杂环,这些基团中的每一个可任选地被取代; R是氢;羟基卤素;任选取代的C 1-6烷基或C 1-6烯基或C 1-6炔基; C 1-6烷氧基; C 1-6烷硫基; C 1-6烷氧基羰基; C 1-6烷基羰氧基;羧基;氰基;硝基氨基单或二(C 1-6烷基)氨基;聚卤代烷基;聚卤代烷氧基;多卤代烷硫基; R; R 1 -C 1-6烷基; R-O-; R-S-; R-C(= O)-; R-S(= O)-; R-S(= O)-; R-S(= O)-NH-; R-S(= O)-NH-; R-C(= O)-; -NHC(= O)H; -C(= O)NHNH; R C(= O)-NH-; R C(= O)-NH-; -C(= NH)R; -C(= NH)R; R 1是任选取代的杂环,条件是-X-R 1和/或R不是氢;它们的用途,包含它们的药物组合物及其制备方法。

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