1-Tert-butyl-3-(trifluoromethyl)azetidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂环丁烷
• 英文名称: 1-Tert-butyl-3-(trifluoromethyl)azetidine
• 英文别名: 1-tert-butyl-3-(trifluoromethyl)azetidine
• 化学式: C₈H₁₄F₃N
• 分子量: 181.2
• InChiKey: IDTRJHGERMMXOO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  3.2
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof
  申请人：Beijing Tide Pharmaceutical Co., Ltd.

  公开号：US10329282B2

  公开（公告）日：2019-06-25

  The present invention relates to a Rho-associated protein kinase inhibitor of Formula (I), a pharmaceutical composition comprising the same, a preparation method thereof, and use thereof for the prevention or treatment of a disease mediated by the Rho-associated protein kinase (ROCK).

  本发明涉及一种式（I）的Rho相关蛋白激酶抑制剂、一种包含其的药物组合物、其制备方法以及其用于预防或治疗由Rho相关蛋白激酶（ROCK）介导的疾病的用途。
• Benzothiophene estrogen receptor modulators
  申请人：G1 Therapeutics, Inc.

  公开号：US10633362B2

  公开（公告）日：2020-04-28

  This invention is a benzothiophene estrogen receptor modulator or its pharmaceutically acceptable salt or a pharmaceutically acceptable composition thereof to treat an estrogen-related medical disorder.

  本发明是一种苯并噻吩雌激素受体调节剂或其药学上可接受的盐或其药学上可接受的组合物，用于治疗与雌激素相关的疾病。
• Phenyl substituted pyrazoles as modulators of RORγt
  申请人：Janssen Pharmaceutica NV

  公开号：US10975037B2

  公开（公告）日：2021-04-13

  The present invention comprises compounds of Formula I. wherein: R1, R3, R4, R5, R6, R7, R8, and Q are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

  本发明包括式 I 的化合物。 其中 R1、R3、R4、R5、R6、R7、R8 和 Q 的定义见说明书。 本发明还包括一种治疗或改善 ROR-γ-t 介导的综合征、紊乱或疾病的方法，其中综合征、紊乱或疾病选自由类风湿性关节炎、银屑病关节炎和银屑病组成的组。本发明还包括一种通过施用治疗有效量的至少一种式 I 化合物来调节哺乳动物体内 RORγt 活性的方法。
• Small molecule inhibitors of NF-κB inducing kinase
  申请人：Janssen Pharmaceutica NV

  公开号：US11254673B2

  公开（公告）日：2022-02-22

  The present invention relates to compounds that inhibit NIK and pharmaceutical compositions comprising such compounds and methods of using the same. These compounds and pharmaceutical compositions are envisaged to be useful for preventing or treating diseases such as cancer (such as B-cell malignancies including leukemias, lymphomas and myeloma), inflammatory disorders, autoimmune disorders, immunodermatologic disorders such as palmoplantar pustulosis and hidradenitis suppurativa, and metabolic disorders such as obesity and diabetes.

  本发明涉及抑制 NIK 的化合物、含有此类化合物的药物组合物以及使用方法。根据设想，这些化合物和药物组合物可用于预防或治疗癌症（如 B 细胞恶性肿瘤，包括白血病、淋巴瘤和骨髓瘤）、炎症性疾病、自身免疫性疾病、免疫性皮肤病（如掌跖脓疱病和化脓性扁桃体炎）以及代谢性疾病（如肥胖症和糖尿病）等疾病。
• Phenyl and pyridinyl substituted imidazoles as modulators of RORγT
  申请人：Janssen Pharmaceutica NV

  公开号：US11345666B2

  公开（公告）日：2022-05-31

  The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, Ra, Rb, Q1, and Q2 are defined in the specification. The invention also comprises a method of treating or ameliorating a ROR-γ-t mediated syndrome, disorder or disease, including wherein the syndrome, disorder or disease is selected from the group consisting of rheumatoid arthritis, psoriatic arthritis, and psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula I.

  本发明包括式 I 的化合物。 其中 R1、R2、R3、R4、R5、Ra、Rb、Q1 和 Q2 在说明书中定义。 本发明还包括一种治疗或改善 ROR-γ-t 介导的综合征、紊乱或疾病的方法，其中综合征、紊乱或疾病选自由类风湿性关节炎、银屑病关节炎和银屑病组成的组。本发明还包括一种通过施用治疗有效量的至少一种式 I 化合物来调节哺乳动物体内 RORγt 活性的方法。