5-chloro-N²-(1-methyl-1H-pyrazol-4-yl)-N⁴-((1-(methylsulfonyl)azetidin-3-yl)methyl)pyrimidine-2,4-diamine | 1445704-41-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 5-chloro-N²-(1-methyl-1H-pyrazol-4-yl)-N⁴-((1-(methylsulfonyl)azetidin-3-yl)methyl)pyrimidine-2,4-diamine
• 英文别名: 5-chloro-2-N-(1-methylpyrazol-4-yl)-4-N-[(1-methylsulfonylazetidin-3-yl)methyl]pyrimidine-2,4-diamine
• CAS: 1445704-41-5
• 化学式: C₁₃H₁₈ClN₇O₂S
• 分子量: 371.851
• InChiKey: BCVYWCYHGNITQN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  24
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  113
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• [EN] PYRIMIDINE-2,4-DIAMINE DERIVATIVES AS KINASE INHIBITORS<br/>[FR] DÉRIVÉS DE PYRIMIDINE-2,4-DIAMINE EN TANT QU'INHIBITEURS DE KINASE
  申请人：CELLZOME LTD

  公开号：WO2013092854A1

  公开（公告）日：2013-06-27

  The present invention relates to compounds of formula (I) wherein X, R, Y0, T0A, T0B have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immuno logically-mediated diseases. The invention also relates to pharmaceutical compositions including said compoundsand their use as medicaments.

  本发明涉及式(I)的化合物，其中X、R、Y0、T0A、T0B的含义如描述和权利要求中所述。所述化合物可用作JAK抑制剂，用于治疗或预防免疫、炎症、自身免疫、过敏性疾病和免疫学介导的疾病。该发明还涉及包括所述化合物的药物组合物及其作为药物的用途。
• PYRIMIDINE-2,4-DIAMINE DERIVATIVES AS KINASE INHIBITORS
  申请人：Cellzome Limited

  公开号：US20150005281A1

  公开（公告）日：2015-01-01

  The present invention relates to compounds of formula (I) wherein X, R, Y 0 , T 0A , T 0B have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds and their use as medicaments.

  本发明涉及式(I)的化合物，其中X，R，Y0，T0A，T0B的含义如所述和权利要求中所述。所述化合物可用作JAK抑制剂，用于治疗或预防免疫、炎症、自身免疫、过敏性疾病和免疫介导的疾病。本发明还涉及包括所述化合物的制药组合物及其作为药物的用途。
• HETEROAROMATIC COMPOUNDS AND THEIR USE AS DOPAMINE D1 LIGANDS
  申请人：PFIZER INC.

  公开号：US20150005313A1

  公开（公告）日：2015-01-01

  The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), age-related cognitive decline, dementia, and Parkinson's disease.

  本发明提供了部分I式化合物及其药学上可接受的盐；用于制备的过程；制备中使用的中间体；以及含有这些化合物或盐的组合物，并且它们的用途是治疗D1介导（或D1相关）的疾病，包括例如精神分裂症（例如其认知和消极症状），认知障碍（例如与精神分裂症，老年痴呆症，帕金森病或药物治疗相关的认知障碍），年龄相关的认知衰退，痴呆症和帕金森病。
• Heteroaromatic compounds and their use as dopamine D1 ligands
  申请人：PFIZER INC.

  公开号：US10093655B2

  公开（公告）日：2018-10-09

  The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), and Parkinson's disease.

  本发明部分提供了式 I 的化合物： 及其药学上可接受的盐；制备过程；制备过程中使用的中间体；以及含有此类化合物或盐的组合物，及其用于治疗D1介导的（或D1相关的）疾病，包括如精神分裂症（如其认知症状和阴性症状）、认知障碍（如与精神分裂症、AD、PD或药物治疗相关的认知障碍）和帕金森病。
• US9107923B2
  申请人：——

  公开号：US9107923B2

  公开（公告）日：2015-08-18