首页> 外国专利> Composed of N - (1R, 4S, 6R) - 3 - (2 - piridinilcarbonil) - 3-azabicyclo hept-3-ene 4,1.0 - 4-yl methyl} - 2 - heteroarilamina, their use for the preparation of a Medicament useful for the treatment of a disease that requires a Orexin receptor antagonist Pharmaceutical composition containing Human and

Composed of N - (1R, 4S, 6R) - 3 - (2 - piridinilcarbonil) - 3-azabicyclo hept-3-ene 4,1.0 - 4-yl methyl} - 2 - heteroarilamina, their use for the preparation of a Medicament useful for the treatment of a disease that requires a Orexin receptor antagonist Pharmaceutical composition containing Human and

机译:由N-[(1R,4S,6R)-3-(2-吡啶碳腈)-3-氮杂双环[]庚-3-烯4,1.0-4-基]甲基}-2-杂芳族聚酰胺组成。用于治疗需要Orexin受体拮抗剂的疾病的药物的制备

摘要

Composed of N - [(1R, 4S, 6R) - 3 - (2 - piridinilcarbonil) - 3-azabicyclo [4.1.0] hept-3-ene - 4-yl] methyl} - 2 - heteroarilamina, formula (1), Het is a heteroaryl Group selected from the group consisting pirazinilo pyridinyl, pirimidinilo, piridazinilo or heteroaryl Group that is optionally substituted with 1, 2 or 3 substituents selected independently You among the group that is c1-4 alkyl, Halo, c1-4 alkoxy, haloalquilo c1-4, haloalcoxi c1-4,And cyano; r1 is c1-4 alkyl, Halo, c1-4 alkoxy, haloalquilo c1-4, haloalcoxi c1-4 alkyl, cyano, C1 - SO2 - 4 - 8 - SO2, cicloalquil C3, C3 cicloalquil - 8 - ch2so2 phenyl or a group of 5 or 6 members heterociclilo containing 1, 2 or 3 Atoms selected from N, o or S, where the phenyl group or heterocicli It is optionally substituted with c1-4 alkyl, Halo, c1-4 alkoxy, haloalquilo c1-4,Haloalcoxi c1-4 alkyl, cyano or; R2 is c1-4 alkoxy, Halo, c1-4, haloalquilo c1-4, haloalcoxi c1-4, cyano, or a phenyl Group of 5 or 6 members heterociclilo containing 1, 2 or 3 Atoms selected from N, o or s, where the phenyl group or heterociclilo is optionally substituted alkyl C 1 - 4, Halo, c1-4 alkoxy, haloalquilo c1-4, haloalcoxi c1-4 or cyano; R3 is c1-4 alkyl, haloC1-4 alkoxy, haloalquilo c1-4, haloalcoxi c1-4 or cyano; M is 0 OR 1; and N is 0 OR 1; or a pharmaceutically acceptable Salt thereof. Use of said Compound for the preparation of a Medicament useful for the treatment of a disease or Disorder that requires Human Orexin receptor antagonist and Pharmaceutical composition containing same.
机译:由N-[(1R,4S,6R)-3-(2-吡啶酮碳)-3-氮杂双环[4.1.0]庚-3-烯-4-基]甲基}-2-杂芳基组成,式(1)组成,Het是杂芳基,其选自吡唑基吡啶基,吡咪唑基基,哌啶子基基或杂芳基,其任选地被1、2或3个独立地选择的取代基取代。在C1-4烷基,卤代,C1-4烷氧基中,halalalquilo c1-4,haloalcoxi c1-4和氰基; r1是c1-4烷基,卤代,c1-4烷氧基,卤代alquilo c1-4,卤代烷氧基c1-4烷基,氰基,C1-SO2-4-8-SO2,cicloalquil C3,C3 cicloalquil-8-ch2so2苯基或一个基团含有1、2或3个选自N,o或S的原子的5或6个成员杂环基,其中苯基或杂环基可选地被c1-4烷基,Halo,c1-4烷氧基,halalalquilo c1-4,Haloalcoxi取代c1-4烷基,氰基或; R 2是c1-4烷氧基,Halo,c1-4,卤代alquilo c1-4,卤代考克西c1-4,氰基或5个或6个杂杂环的苯基,其含有1、2或3个选自N,o或s的原子,其中苯基或杂环基是任选取代的烷基C 1-4,卤代,c 1-4烷氧基,卤代alquilo c1-4,卤代烷氧基c 1-4或氰基; R3是c1-4烷基,卤代C1-4烷氧基,卤代alquiloc1-4,卤代烷氧基c1-4或氰基; M为0或1; N为0或1;或其药学上可接受的盐。所述化合物在制备可用于治疗需要人Orexin受体拮抗剂的疾病或病症的药物中的用途以及包含该化合物的药物组合物。

著录项

  • 公开/公告号AR074238A1

    专利类型

  • 公开/公告日2010-12-29

    原文格式PDF

  • 申请/专利权人 GLAXO GROUP LIMITED;

    申请/专利号AR2009P104606

  • 发明设计人

    申请日2009-11-30

  • 分类号C07D401/12;C07D401/14;C07D413/14;C07D417/14;A61K31/55;A61P25/22;A61P25/24;

  • 国家 AR

  • 入库时间 2022-08-21 18:07:29

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