2,2-DIMETHYL-3-OXO-3,4-DIHYDRO-2H-BENZO[1,4] OXAZINE-6-CARBOXYLIC ACID INDAN-2-YLAMIDE | 450354-96-8

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 2,2-DIMETHYL-3-OXO-3,4-DIHYDRO-2H-BENZO[1,4] OXAZINE-6-CARBOXYLIC ACID INDAN-2-YLAMIDE
• 英文别名: N-(2,3-dihydro-1H-inden-2-yl)-2,2-dimethyl-3-oxo-4H-1,4-benzoxazine-6-carboxamide
• CAS: 450354-96-8
• 化学式: C₂₀H₂₀N₂O₃
• 分子量: 336.39
• InChiKey: IUZUDOFNUQEMMH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  25
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  67.4
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• ACYLATED INDANYL AMINES AND THEIR USE AS PHARMACEUTICALS
  申请人：STROBEL Hartmut

  公开号：US20070082897A1

  公开（公告）日：2007-04-12

  The present invention relates to acylated indanyl amines according to the general formula (I) wherein R 1 —R 4 have the meanings given in the description, A is CH 2 , CHOH or CH—(C 1 -C 3 -alkyl), B is CH 2 or CH—(C 1 -C 3 -alkyl), and R 5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description. These compounds are useful in the upregulation of endothelial nitric oxide synthase (eNOS), and may therefore be useful for the manufacture of medicaments for the treatment of cardiovascular diseases, stable or unstable angina pectoris, coronary heart disease, Prinzmetal angina, acute coronary syndrome, heart failure, myocardial infarction, stroke, thrombosis, peripheral artery occlusive disease, endothelial dysfunction, atherosclerosis, restenosis, endothelial damage after PTCA, hypertension, essential hypertension, pulmonary hypertension, secondary hypertension, renovascular hypertension, chronic glomerulonephritis, erectile dysfunction, ventricular arrhythmia, diabetes or diabetes complications, nephropathy or retinopathy, angiogenesis, asthma bronchiale, chronic renal failure, cirrhosis of the liver, osteoporosis, restricted memory performance, a restricted ability to learn, or for the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.

  本发明涉及通式（I）的酰化吲哚基胺，其中R1-R4具有描述中给出的含义，A为CH2，CHOH或CH-（C1-C3-烷基），B为 或CH-（C1-C3-烷基），而R5为芳基或杂芳基基团，可能被描述中列出的取代基所取代。这些化合物有助于上调内皮型一氧化氮合酶（eNOS），因此可能用于制造用于治疗心血管疾病、稳定或不稳定型心绞痛、冠心病、普林兹梅塔尔心绞痛、急性冠状动脉综合征、心力衰竭、心肌梗死、中风、血栓形成、周围动脉闭塞症、内皮功能障碍、动脉粥样硬化、再狭窄、PTCA后的内皮损伤、高血压、原发性高血压、肺动脉高压、继发性高血压、肾血管性高血压、慢性肾小球肾炎、勃起功能障碍、室性心律失常、糖尿病或糖尿病并发症、肾病或视网膜病变、血管生成、支气管哮喘、慢性肾衰竭、肝硬化、骨质疏松症、受限制的记忆表现、受限制的学习能力或降低绝经后妇女或口服避孕药后的心血管风险。
• US7713963B2
  申请人：——

  公开号：US7713963B2

  公开（公告）日：2010-05-11
• US8163751B2
  申请人：——

  公开号：US8163751B2

  公开（公告）日：2012-04-24