1,3,3-trimethyl-6-(1-(3-methylpyridin-4-yl)-1H-imidazol-4-yl)indolin-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 1,3,3-trimethyl-6-(1-(3-methylpyridin-4-yl)-1H-imidazol-4-yl)indolin-2-one
• 英文别名: 1,3,3-Trimethyl-6-[1-(3-methylpyridin-4-yl)imidazol-4-yl]indol-2-one；1,3,3-trimethyl-6-[1-(3-methylpyridin-4-yl)imidazol-4-yl]indol-2-one
• 化学式: C₂₀H₂₀N₄O
• 分子量: 332.405
• InChiKey: NCRPYGXBJRJCFG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  25
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  51
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• [EN] INDOLIN-2-ONE AND 1,3-DIHYDRO-PYRROLO[3,2-c]PYRIDIN-2-ONE DERIVATIVES<br/>[FR] DÉRIVÉS D'INDOLIN-2-ONE ET DE 1,3-DIHYDRO-PYRROLO[3,2-C]PYRIDIN-2-ONE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2015177110A1

  公开（公告）日：2015-11-26

  The present invention is concerned with indolin-2-one and l,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula (I) wherein Ar1 is phenyl, pyridinyl or pyrimidinyl; Ar2 is a 5 or 6 membered heteroaryl group, containing 2 or 3 heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, halogen or lower alkoxy; R2 is hydrogen or lower alkyl; R3 is hydrogen, lower alkyl, lower alkyl substituted by hydroxy, cycloalkyl, oxetan-3-yl, pyridinyl, imidazolyl, pyrazolyl, pyrimidinyl, which rings may optionally substituted by lower alkyl, or is -(CH2)3-S(O)2-cyclopropyl; X is CH or N; n is 1 or 2; as well as with a pharmaceutically acceptable salts thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof, for use in the treatment of certain central nervous system disorders which are positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, sleep disturbances, chronic fatigue syndrome, stiffness, antiinflammatory effects in arthritis and balance problems.

  本发明涉及一般式(I)的吲哚啉-2-酮和1,3-二氢吡咯并[3,2-c]吡啶-2-酮衍生物，其中Ar1是苯基、吡啶基或嘧啶基；Ar2是含有2个或3个N、O或S杂原子的5或6元杂芳基团；R1是氢、低碳基、卤素或低烷氧基；R2是氢或低碳基；R3是氢、低碳基、低碳基取代的羟基、环烷基、氧杂环丙烯基、吡啶基、咪唑基、吡唑基、嘧啶基，这些环可能被低碳基取代，或者是-(CH2)3-S(O)2-环丙基；X是CH或N；n为1或2；以及其药学上可接受的盐、消旋混合物、对映体和/或光学异构体和/或立体异构体，用于治疗某些中枢神经系统疾病，包括精神病（正性症状和负性症状）、精神分裂症、物质滥用、酒精和药物成瘾、强迫症、认知障碍、双相情感障碍、情绪障碍、重度抑郁症、治疗难治性抑郁症、焦虑症、阿尔茨海默病、自闭症、帕金森病、慢性疼痛、边缘性人格障碍、睡眠障碍、慢性疲劳综合征、僵硬、关节炎中的抗炎作用和平衡问题。
• Indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives
  申请人：Hoffmann-La Roche Inc.

  公开号：US10112938B2

  公开（公告）日：2018-10-30

  The present invention is concerned with indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula I wherein Ar1, A2, R1, R2, R3, X and n are as described herein and pharmaceutically acceptable salts thereof for treatment of central nervous system disorders

  本发明涉及通式 I 的吲哚啉-2-酮和 1,3-二氢-吡咯并[3,2-c]吡啶-2-酮衍生物（其中 Ar1、A2、R1、R2、R3、X 和 n 如本文所述）及其药学上可接受的盐，用于治疗中枢神经系统疾病。
• INDOLIN-2-ONE AND 1,3-DIHYDRO-PYRROLO[3,2-C]PYRIDIN-2-ONE DERIVATIVES
  申请人：F. Hoffmann-La Roche AG

  公开号：EP3145923B1

  公开（公告）日：2019-01-30
• INDOLIN-2-ONE AND 1,3-DIHYDRO-PYRROLO[3,2-c]PYRIDIN-2-ONE DERIVATIVES
  申请人：F. Hoffmann-La Roche AG

  公开号：EP3145923A1

  公开（公告）日：2017-03-29