首页> 外国专利> HETEROARYL AMINES AS GLYCOGEN SYNTHASE KINASE 3 BETA INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

HETEROARYL AMINES AS GLYCOGEN SYNTHASE KINASE 3 BETA INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

机译:异戊酰胺作为糖原合成酶激酶3β抑制剂,其制备方法和包含它们的药物成分

摘要

This invention concerns a compound of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein ring A is a 6-membered heterocycle; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyloxyC1-6alkylcarbonyl; X is a direct bond or a linker atom or group; Z is a direct bond or a linker atom or group; R2 is hydrogen, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, a carbocycle or a heterocycle, each of said groups may optionally be substituted; R3 is hydrogen; hydroxy; halo; optionally substituted C1-6alkyl or C2-6alkenyl or C2-6alkynyl; C1-6alkyloxy; C1-6alkylthio; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; polyhaloC1-6alkylthio; R21; R21-C1-6alkyl; R21-O-; R21-S-; R21-C(-O)-; R21-S(-O)p-; R7-S(-O)p-; R7-S(-O)p-NH-; R21-S(-O)p-NH-; R7-C(-O)-; -NHC(-O)H; -C(-O)NHNH2; R7-C(-O)-NH-; R21-C(-O)-NH-; -C(-NH)R7-C(-NH)R21; R4 is an optionally substituted heterocycle provided that -X-R2 and/or R3 is other than hydrogen; their use, pharmaceutical compositions comprising them and processes for their preparation.
机译:本发明涉及式N化合物,其药学上可接受的加成盐,季胺及其立体化学异构形式,其中环A为6元杂环。 R1是氢;芳基甲酰基C 1-6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烷氧基C 1-6烷基羰基; X是直接键或连接原子或基团; Z是直接键或连接原子或基团; R 2是氢,C 1-10烷基,C 2-10烯基,C 2-10炔基,碳环或杂环,每个所述基团可任选地被取代; R3是氢;羟基光环;任选取代的C 1-6烷基或C 2-6烯基或C 2-6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;多卤代C 1-6烷基;聚卤代C 1-6烷氧基;聚卤代C 1-6烷硫基; R21; R21-C1-6烷基; R21-O-; R21-S-; R21-C(-O)-; R21-S(-O)p-; R7-S(-O)p-; R7-S(-O)p-NH-; R21-S(-O)对-NH-; R7-C(-O)-; -NHC(-O)H; -C(-O)NHNH 2; R7-C(-O)-NH-; R21-C(-O)-NH-; -C(-NH)R 7 -C(-NH)R 21; R4是任选取代的杂环,条件是-X-R2和/或R3不是氢;它们的用途,包含它们的药物组合物及其制备方法。

著录项

  • 公开/公告号HU0402106A3

    专利类型

  • 公开/公告日2009-07-28

    原文格式PDF

  • 申请/专利权人 JANSSEN PHARMACEUTICA N.V.;

    申请/专利号HU20040002106

  • 发明设计人

    申请日2002-10-29

  • 分类号A61K31/435;A61K31/4406;A61K31/50;A61K31/501;A61K31/505;A61K31/506;A61K31/5377;A61P3/10;A61P17;A61P21/04;A61P25;A61P25/04;A61P25/16;A61P25/18;A61P25/24;A61P25/28;A61P29;A61P31/18;A61P35;A61P35/02;C07D213/53;C07D213/74;C07D239/42;C07D239/48;C07D401/04;C07D401/12;C07D403/04;C07D403/12;C07D405/12;C07D409/12;C07D417/12;

  • 国家 HU

  • 入库时间 2022-08-21 19:27:54

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