首页> 外国专利> Derivatives of 3h imidazo 4, 5-b pyridine as Selective inhibitors of GSK3 and internediarios, Methods for their preparation, Pharmaceutical compositions containing them and their use for the preparation of a Medicament for the treatment of Neurodegenerative Diseases and mental disorders.

Derivatives of 3h imidazo 4, 5-b pyridine as Selective inhibitors of GSK3 and internediarios, Methods for their preparation, Pharmaceutical compositions containing them and their use for the preparation of a Medicament for the treatment of Neurodegenerative Diseases and mental disorders.

机译:3h咪唑并[4,5-b]吡啶作为GSK3和internediarios的选择性抑制剂的衍生物,其制备方法,包含它们的药物组合物及其在制备用于治疗神经退行性疾病和精神疾病的药物中的用途。

摘要

A process for their Preparation and Intermediates used therein, Pharmaceutical formulations containing Said therapeutically Active compounds and to the use of said compounds in therapy of Mental and Neurodegenerative Diseases.Claim 1: a compound of the formula (1) wherein X is as shown in the compound of formula (2); and R1 is selected from h, halogen, CN, CO2H, NO2, c1-3 alkyl, haloalquilo c1-3, prays, so2nrbrc, nrbrc, C (o) ch2nrbrc, ch2orh, so2ri and C (OR) RJ; R2 and R4 are selected. Nera Independent between h, Halo, CN, NO2, c1-3 alkyl, haloalquilo c1-3, prays, so2nrbrc, nrbrc, C (o)Ch2nrbrc, ch2orh, so2ri and C (OR) RJ; R3 and R5 are independently selected from h, alkyl haloalquilo C1 and C1 - 3 - 3; aryl or heteroaryl is optionally substituted with one or more alkyl CO2H CN, C1, C1 - 6 - 6, haloalquilo, Halo, C (o) ra, Ork, prays, nrbrc C (OR), or s (MRN), where the alqui The C1 - 6 - 6 or haloalquilo C1 is optionally substituted with at least one NS,Prays or nrbrc; and Z is selected from alkyl ch2ord C1, - 6, and ch2z heteroaryl; Z is optionally substituted with one or more alkyl C1 CN, - 6, - 6 haloalquilo C1, Halo, C (or c) ra, ork, nrbrc (OR), or s (MRN), where the alkyl or haloalquilo C1 C1 - 6 - 6 is optionally substituted with at least u CN n, ora or nrbrc; ra is selected from h, alkyl haloalquilo C1 and C1 - 3 - 3Where the c1-3 alkyl or haloalquilo c1-3 is optionally substituted with one or more alkoxy c1-3; RB and RC are independently selected from h, heteroaryl alkyl haloalquilo C1 and C1 - 6 - 6, where the alkyl or haloalquilo C1 C1 - 6 - 6 is optionally substituted with one or more S (ORA or nrdre; or RB and RC can form, together with the Atom to which they are United.A Heterocyclic Ring of 4, 5, 6 or 7 members that contain one or more heteroatoms selected from N, o or s, where the Heterocyclic ring is optionally substituted with one or more Halo, prays, nrdre, c1-3 alkyl or haloalquilo c1-3,Where the c1-3 alkyl or haloalquilo c1-3 is optionally substituted with one or more alkoxy c1-3; Rd and re are independently selected from h, alkyl or haloalquilo C1 C1 - 6 - 6, where the alkyl or haloalquilo C1 C1 - 6 - 6 is optionally substituted with one or more or A; or Rd and re can form, together with the Atom to which they are United, a Heterocyclic Ring 4, 56 or 7 members that contain one or more heteroatoms selected from N, o or s, where the Heterocyclic ring is optionally substituted with one or more Halo, c1-3 alkyl or haloalquilo c1-3 alkyl, wherein the C1 - 3 or haloalquilo c1-3 is optionally substituted by one or more S alkoxy c1-3; RH is HC1-3 alkyl or haloalquilo c1-3 optionally substituted with one or more alkoxy c1-3; RI is haloalquilo c1-3 alkyl or c1-3 alkyl, wherein the C1 - 3 or haloalquilo c1-3 is optionally substituted with one or more ora; RJ is aryl or heteroaryl, aryl or heteroaryl where that is optionally s Ustituido with one or more alkyl c1-3, ora, Halo or CN; rk is alkyl or haloalquilo C1 C1 - 6 - 6Where the alkyl or haloalquilo C1 C1 - 6 - 6 is optionally substituted with at least one CN, prays, nrbrc, C (o) or nrbrc NRBC (or RC); Rm is c1-3 alkyl optionally substituted with at least one Halo, CN, prays, nrbrc (or nrbrc; or (c) n is 0 to 3; in the form of Free Base or a Salt, solvate or solvate The pharmaceutically acceptable Salt thereof.
机译:1制备它们的方法和中间体,包含所述治疗活性化合物的药物制剂,以及所述化合物在精神和神经退行性疾病的治疗中的用途。权利要求1:式(1)的化合物,其中X如式(2)化合物; R1选自h,卤素,CN,CO2H,NO2,c1-3烷基,卤代alquiloc1-3,p2,so2nrbrc,nrbrc,C(o)ch2nrbrc,ch2orh,so2ri和C(OR)RJ;选择R2和R4。在h,Halo,CN,NO2,c1-3烷基,halalalquilo c1-3之间独立的Nera祈祷,so2nrbrc,nrbrc,C(o)Ch2nrbrc,ch2orh,so2ri和C(OR)RJ R3和R5独立地选自h,烷基卤代烷基C1和C1-3-3;和芳基或杂芳基可任选地被一个或多个烷基CO2H CN,C1,C1-6-6取代,卤代alquilo,Halo,C(o)ra,Ork,prises,nrbrc C(OR)或s(MRN),其中C1-6-6或卤代C1任选地被至少一种NS,Prays或nrbrc取代; Z选自烷基ch 2ord C 1-6和ch 2z杂芳基; Z任选地被一个或多个烷基C1 CN,-6,-6卤代alquilo C1,Halo,C(或c)ra,ork,nrbrc(OR)或s(MRN)取代,其中烷基或卤代alquilo C1- 6-6任选地被至少u CN n,ora或nrbrc取代; ra选自h,烷基卤代烷基C1和C1-3-3,其中c1-3烷基或卤代烷基c1-3任选地被一个或多个烷氧基c1-3取代; RB和RC独立地选自h,杂芳基烷基卤代基C1和C1-6-6,其中烷基或卤代基C1 C1-6-6可选地被一个或多个S(ORA或nrdre)取代;或者RB和RC可以形成一个由4、5、6或7个成员组成的杂环,其中含有一个或多个选自N,o或s的杂原子,其中杂环可选地被一个或多个Halo取代,求nrdre,c1-3烷基或卤代alquiloc1-3,其中c1-3烷基或卤代alquiloc1-3任选地被一个或多个烷氧基c1-3取代; Rd和re独立地选自h,烷基或卤代alquilo C1-6-6,其中烷基或卤代alquilo C1 C1-6-6任选被一个或多个或A取代;或Rd和re可以与它们所连接的原子一起形成杂环4、56或7个成员,它们含有一个或多个选自N,o或s的杂原子,其中杂环可选地被取代一个或多个卤代,c 1-3烷基或卤代alquilo c1-3烷基,其中C 1-3或卤代alquilo c1-3任选地被一个或多个S烷氧基c1-3取代; RH是任选被一个或多个烷氧基c1-3取代的HC1-3烷基或卤代烷基c1-3; RI为卤代alquilo c1-3烷基或c1-3烷基,其中C1-3或卤代alquilo c1-3任选地被一个或多个ora取代; RJ为芳基或杂芳基,芳基或杂芳基,其中其任选为具有一个或多个烷基c1-3,ora,Halo或CN的Usituituido; rk是烷基或卤代芳基C1-6-6,其中烷基或卤代基C1-6-6任选地被至少一个CN,p,nrbrc,C(o)或nrbrc NRBC(或RC)取代。 Rm为c1-3烷基,可选地被至少一个Halo,CN取代,nrbrc(或nrbrc;或(c)n为0至3;呈游离碱或盐,溶剂化物或溶剂化物的形式其。

著录项

  • 公开/公告号AR055669A1

    专利类型

  • 公开/公告日2007-08-29

    原文格式PDF

  • 申请/专利权人 ASTRAZENECA AB;

    申请/专利号AR2006P104308

  • 发明设计人

    申请日2006-09-29

  • 分类号C07D471/04;A61K31/437;A61P25/00;

  • 国家 AR

  • 入库时间 2022-08-21 20:59:36

相似文献

  • 专利
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号