首页> 外国专利> Compound of aryl diazaespiro oxo Intermediate for Synthesis, use thereof for preparing a Medicament for the treatment of a disorder mediated by GlyT1, Pharmaceutical Composition and Association that comprise it.

Compound of aryl diazaespiro oxo Intermediate for Synthesis, use thereof for preparing a Medicament for the treatment of a disorder mediated by GlyT1, Pharmaceutical Composition and Association that comprise it.

机译:用于合成的芳基二氮杂螺氧基羰基化合物的中间体,其在制备用于治疗由GlyT1介导的疾病,药物组合物和组成它的协会中的用途。

摘要

Compuesto derivado del aril-oxo-diazaespiro amidas o cetonas de formula o una sal del mismo en el que R1 se selecciona de hidrogeno alquilo C1-4 alcoxi C1-4 halo haloalquilo C1-4 haloalcoxi C1-4 alquil C1-4 tio cicloalquilo C3 [C1-4 alkyl] sulfonyl, [C1-4 alkoxy] C1-4 alkyl, cyano CONRcRd (wherein Rc and Rd are independently selected from H and C1-4 alkyl or Rc and Rd, together with the nitrogen atom at which are attached, form a 4- to 7-membered ring; R3 selects from hydrogen, C1-4 alkyl, C1-4 alkoxy, halo, C1-4 haloalkyl, C1-4 haloalkoxy, [C1-4 alkyl] thio, C3 cycloalkyl -6, (C3-6 cycloalkyl) C1-4 alkyl, (C1-4 alkyl) sulfonyl, [C1-4 alkoxy] C1-4 alkyl, cyano and CONReRt (wherein Re and Rf are independently selected from H and alkyl C1-4 or Re and Rf, together with the nitrogen atom to which they are attached, form a 4- to 7-membered ring);O R2 and R3 constitute a selected o-ch2-o-y-o-ch2-ch2-o -;R4 is selected from: hydrogen, C1-4 alkyl; halo, C1-4 haloalkyl, C1-4 haloalkoxy, [C1-4 alkyl] thio, C3-6 cycloalkyl, [C3-6 cycloalkyl] C1-4 alkyl, (C1-4 alkyl sulfonyl, (C1-4 alkoxy) alkyl C1-4, cyano and CONRgRh (where Rg and Rh are indecently selected from H and C1-4 alkyl or Rg and Rh, together with the nitrogen atom to which they are attached, form a 4- to 7-membered ring);R5 is selected from: hydrogen, chlorine, fluorination, C1-4 and CF3; R6 is selected from: (alcox C1-4) tar (C1-4 tar), sulfur (C1-4 tar), uncle, cor9 (R9 is hydrogen gene or C1-4 tar); conrirj (in this case, RI and RJ are selected to be independent of C1-4 or hydrocarbon group, Form a 4, 5 or 6-ring and chrkrlrm with the nitrogen atoms connected together (RK is the hydrogen or tar of C1-4 and RL / RM, regardless of C1-4 or RL / RM, plus the nitrogen atoms attached together to form a 4, 5 or 6-member ring);R15 is hydrogen or fluorine; R7 is selected from the following substances: hydrogen, C1-4 tar, alcox C1-4, halogenated C1-4, halogenated C1-4 carbon, cyanogen (Alcoy C1-4) alcox C1-4 and (alcox C1-4) C1-4 tar; R8 is selected from hydrogen and methyl, and M is selected from 0, 1 and 2. Its purpose is to produce an effective drug for the treatment of glytl's intermediate disorders, such as schizophrenia, dementia and attention deficit disorders. Drug composition and association with one or more therapeutic agents Synthesized by middlemen ILO Convention No. 12: an intermediary integrates the first provision of ILO Convention No. 1.It is a formula (II) or a salt, wherein R6 is selected from (alcox C1-4) C1-4 tar (C1-4 tar) sulfuric acid (C1-4 tar) uncle and cor9 (wherein R9 is C1-4 hydrocarbon),Conrirj (in this case, RI and RJ are selected to form a ring of 4, 5 or 6 members independent of or connected to the nitrogen atom of C1-4 hydrogen or hydrocarbon base): R15 is hydrogen or fluorine; R7 is selected as: hydrogen, C1-4 hydrocarbon base, alcox C1-4, halo-4, halo alcox C1-4, halo, ciao, C1-4 (alcox C1-4) alcox c1-4y (alcox C1-4) C1-4 tar; R8 was selected from 0.1 and 2 as hydrogen and methyl.
机译:阿尔法-阿昔洛斯-阿维达斯-阿昔洛斯-阿维达斯-阿西莫斯酮衍生物的合成衍生物阿尔库洛C1-4阿尔科西C1-4氢硒基化合物阿尔库洛C1-4阿尔科西C1-4阿拉基C1-4环C1-4环氯喹啉C3 [C1-4烷基]磺酰基,[C1-4烷氧基] C1-4烷基,氰基CONRcRd(其中Rc和Rd独立地选自H和C1-4烷基或Rc和Rd以及与之相连的氮原子,形成4至7元环; R 3选自氢,C 1-4烷基,C 1-4烷氧基,卤素,C 1-4卤代烷基,C 1-4卤代烷氧基,[C 1-4烷基]硫代,C 3环烷基-6 ,(C3-6环烷基)C1-4烷基,(C1-4烷基)磺酰基,[C1-4烷氧基] C1-4烷基,氰基和CONReRt(其中Re和Rf独立选自H和烷基C1-4或Re和Rf与它们所连接的氮原子一起形成4至7元环); O R2和R3构成选定的o-ch2-oyo-ch2-ch2-o-; R4选自:氢,C 1-4烷基;卤素,C 1-4卤代烷基,C 1-4卤代烷氧基,[C 1-4 a苄基]硫代,C 3-6环烷基,[C 3-6环烷基] C 1-4烷基,(C 1-4烷基磺酰基,(C 1-4烷氧基)烷基C 1-4,氰基和CONRgRh(其中Rg和Rh不适当地选自H和C1-4烷基或Rg和Rh与它们所连接的氮原子一起形成4至7元环); R5选自:氢,氯,氟化,C1-4和CF3; R6选自:(醇C1-4)焦油(C1-4焦油),硫(C1-4焦油),叔叔,cor9(R9是氢基因或C1-4焦油); conrirj(在这种情况下,RI和RJ被选择为独立于C1-4或烃基,形成4、5或6环和chrkrlrm,氮原子连接在一起(RK是C1-4的氢或焦油)和RL / RM,而不考虑C1-4或RL / RM,加上连接在一起的氮原子形成4、5或6元环); R15是氢或氟; R7选自以下物质:氢,C1-4焦油,Alcox C1-4,卤代C1-4,卤代C1-4碳,氰(Alcoy C1-4)Alcox C1-4和(Alcox C1-4)C1-4焦油; R8选自氢和甲基,M选自0、1和2,其目的是生产一种有效的药物来治疗glytl的中级疾病,例如精神分裂症,痴呆症和注意力缺陷疾病。代理商由中间商合成国际劳工组织第12号公约:中介机构将国际劳工组织第1号公约的第一条规定整合在一起。它是一种式(II)或盐R6选自(醇C1-4)C1-4焦油(C1-4焦油)硫酸(C1-4焦油)叔和cor9(其中R9为C1-4烃),Conrirj(在这种情况下为RI和选择RJ以形成独立于或连接至C1-4氢原子或烃基的氮原子的4、5或6个成员的环):R15为氢或氟; R7选自:氢,C1-4烃基,Alcox C1-4,卤素-4,卤素Alcox C1-4,卤素,Ciao,C1-4(Alcox C1-4)Alcox C1-4y(Alcox C1-4 )C1-4焦油; R8选自0.1和2作为氢和甲基。

著录项

  • 公开/公告号AR065095A1

    专利类型

  • 公开/公告日2009-05-13

    原文格式PDF

  • 申请/专利权人 GLAXO GROUP LIMITED;

    申请/专利号AR2008P100379

  • 发明设计人

    申请日2008-01-30

  • 分类号C07D235/02;A61K31/4184;A61P25/18;A61P25/28;

  • 国家 AR

  • 入库时间 2022-08-21 19:28:42

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