5-(3,5-dimethylisoxazol-4-yl)-2-[6-fluoro-3-(2,3,6-trifluorobenzyl)imidazo[1,5-a]pyridin-1-yl]pyrimidin-4-amine | 1337565-30-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯并吡啶类
• 英文名称: 5-(3,5-dimethylisoxazol-4-yl)-2-[6-fluoro-3-(2,3,6-trifluorobenzyl)imidazo[1,5-a]pyridin-1-yl]pyrimidin-4-amine
• 英文别名: 5-(3,5-Dimethyl-1,2-oxazol-4-yl)-2-[6-fluoro-3-[(2,3,6-trifluorophenyl)methyl]imidazo[1,5-a]pyridin-1-yl]pyrimidin-4-amine
• CAS: 1337565-30-6
• 化学式: C₂₃H₁₆F₄N₆O
• 分子量: 468.413
• InChiKey: VHDBDDOUWMITOM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  34
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  95.1
• 氢给体数：
  1
• 氢受体数：
  10

文献信息

• [EN] SOLUBLE GUANYLATE CYCLASE ACTIVATORS<br/>[FR] ACTIVATEURS DE GUANYLATE CYCLASE SOLUBLES
  申请人：MERCK SHARP & DOHME

  公开号：WO2011119518A1

  公开（公告）日：2011-09-29

  The invention relates to compounds having the structure of Formula (I) and pharmaceutically acceptable salts thereof, which are soluble guanylate cyclase activators. The compounds are capable of modulating the body's production of cyclic guanosine monophosphate ("cGMP") and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.

  该发明涉及具有结构式（I）的化合物及其药用可接受盐，这些化合物是可溶性鸟苷酸环化酶激活剂。这些化合物能够调节人体对环鸟苷酸单磷酸（"cGMP"）的产生，并一般适用于治疗和预防与紊乱的cGMP平衡相关的疾病。这些化合物可用于治疗或预防心血管疾病、内皮功能障碍、舒张功能障碍、动脉粥样硬化、高血压、肺动脉高压、心绞痛、血栓形成、再狭窄、心肌梗死、中风、心功能不全、肺动脉高压、勃起功能障碍、支气管哮喘、慢性肾功能不全、糖尿病或肝硬化。
• The use of sGC stimulators, sGC activators, alone and combinations with PDE5 inhibitors for the treatment of systemic sclerosis (SSc)
  申请人：BIP Patents

  公开号：EP2594270A2

  公开（公告）日：2013-05-22

  The use of sGC stimulators, sGC activators alone, or in combination with PDE5 inhibitors for the prevention and treatment of fibrotic diseases, such as systemic sclerosis, scleroderma, and the concomitant fibrosis of internal organs.

  将 sGC 刺激剂、sGC 激活剂单独使用或与 PDE5 抑制剂联合使用，用于预防和治疗纤维化疾病，如系统性硬化症、硬皮病以及伴随而来的内脏器官纤维化。
• SOLUBLE GUANYLATE CYCLASE ACTIVATORS
  申请人：Merck Sharp & Dohme Corp.

  公开号：EP2549875B1

  公开（公告）日：2015-05-13
• US9284301B2
  申请人：——

  公开号：US9284301B2

  公开（公告）日：2016-03-15