6-Chloro-1-cyclopentyl-1H-pyrazolo[3,4-d]pyrimidine | 1443286-82-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡唑并嘧啶类
• 英文名称: 6-Chloro-1-cyclopentyl-1H-pyrazolo[3,4-d]pyrimidine
• 英文别名: 6-chloro-1-cyclopentylpyrazolo[3,4-d]pyrimidine
• CAS: 1443286-82-5
• 化学式: C₁₀H₁₁ClN₄
• 分子量: 222.67
• InChiKey: BZFWNKBVEUBYDG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.3
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  43.6
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• BICYCLIC LACTAMS AS RECEPTOR-INTERACTING PROTEIN-1 (RIP1) KINASE INHIBITORS FOR TREATING E.G. INFLAMMATORY DISEASES
  申请人：F. Hoffmann-La Roche AG

  公开号：EP3760625A1

  公开（公告）日：2021-01-06

  The invention provides compounds having the general formula (I) wherein R1, X, Z1, L, n, the A ring, the B ring, and the C ring are as described herein, pharmaceutical compositions including the compounds and the compounds for use in methods of medical treatment. The present compounds are receptor-interacting protein-1 (RIP1) kinase inhibitors useful for treating e.g. inflammatory diseases, such as e.g. irritable bowel disorders (IBD), irritable bowel syndrome (IBS), Crohn's disease, ulcerative colitis, myocardial infarction, stroke, traumatic brain injury, atherosclerosis, ischemia-reperfusion injury of kidneys, liver and lungs, cisplatin-induced kidney injury, sepsis, systemic inflammatory response syndrome (SIRS), pancreatits, psoriasis, retinitis pigmentosa, retinal degeneration, chronic kidney diseases, acute respiratory distress syndrome (ARDS), chronic obstructive pulmonary disease (COPD). The present description discloses the preparation of exemplary and reference compounds, as well as pharmacological data thereof (e.g. pages 116 to 1221; examples 1 to 793; examples A to C; tables). An exemplary compound is e.g. 5a-methyl-N-((S)-5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-1,4,4a,5,5a,6-hexahydrocyclopropa[f]indazole-3-carboxamide (example 1)

  本发明提供具有通式 (I) 的化合物 其中 R1、X、Z1、L、n、A 环、B 环和 C 环如本文所述；包括本发明化合物的药物组合物；以及本发明化合物在医疗方法中的用途。 本化合物是受体相互作用蛋白-1（RIP1）激酶抑制剂，可用于治疗炎症性疾病，例如肠易激综合征 (IBS)、克罗恩病、溃疡性结肠炎、心肌梗塞、中风、脑外伤、动脉粥样硬化、肾脏、肝脏和肺部缺血再灌注损伤、顺铂诱导的肾损伤、败血症、全身性炎症性休克、溃疡性结肠炎等、败血症、全身炎症反应综合征（SIRS）、胰腺炎、银屑病、色素性视网膜炎、视网膜变性、慢性肾脏疾病、急性呼吸窘迫综合征（ARDS）、慢性阻塞性肺病（COPD）。 本说明书公开了示例化合物和参考化合物的制备方法及其药理数据（如第 116 页至第 1221 页；例 1 至例 793；例 A 至例 C；表）。 示例化合物如 5a-甲基-N-((S)-5-甲基-4-氧代-2,3,4,5-四氢苯并[b][1,4]氧氮杂卓-3-基)-1,4,4a,5,5a,6-六氢环丙基[f]吲唑-3-甲酰胺（例 1）
• Bicyclic lactams and methods of use thereof
  申请人：Genentech, Inc.

  公开号：US10988459B2

  公开（公告）日：2021-04-27

  The invention provides novel compounds having the general formula I: wherein R1, X, Z1, L, n, the A ring, the B ring, and the C ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.

  本发明提供了具有通式 I 的新型化合物： 其中 R1、X、Z1、L、n、A 环、B 环和 C 环如本文所述，提供了包括该化合物的药物组合物和使用该化合物的方法。
• [EN] BICYCLIC LACTAMS AND METHODS OF USE THEREOF<br/>[FR] LACTAMES BICYCLIQUES ET LEURS MÉTHODES D'UTILISATION
  申请人：GENENTECH INC

  公开号：WO2017004500A9

  公开（公告）日：2017-11-30
• BICYCLIC LACTAMS AND METHODS OF USE THEREOF
  申请人：Genentech, Inc.

  公开号：US20170008877A1

  公开（公告）日：2017-01-12

  The invention provides novel compounds having the general formula I: wherein R 1 , X, Z 1 , L, n, the A ring, the B ring, and the C ring are as described herein, pharmaceutical compositions including the compounds and methods of using the compounds.