1-(4-methoxyphenyl)-5-methyl-N-[(2S)-1,2,3,4-tetrahydronaphthalen-2-yl]pyrazole-4-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 1-(4-methoxyphenyl)-5-methyl-N-[(2S)-1,2,3,4-tetrahydronaphthalen-2-yl]pyrazole-4-carboxamide
• 化学式: C₂₂H₂₃N₃O₂
• 分子量: 361.4
• InChiKey: XNDPXLHDMIMFBD-SFHVURJKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  56.2
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• Acylated 1,2,3,4-tetrahydronaphthyl amines and their use as pharmaceutical agents
  申请人：——

  公开号：US20030022935A1

  公开（公告）日：2003-01-30

  The present invention relates to compounds of general formula (I), 1 wherein R 1 -R 4 have the meanings given in the specification, A is CH2, CHOH or CH-(C 1 -C 3 -alkyl), B and C are independently CH 2 or CH-(C 1 -C 3 -alkyl), and R 5 is an aryl or heteroaryl group optionally substituted by the substituents listed in the specification. The compounds are 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, and restricted memory performance or a restricted ability to learn, or the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.

  本发明涉及通式(I)的化合物、 1 其中 R 1 -R 4 具有说明书中给出的含义，A 是 CH2、CHOH 或 CH-（C 1 -C 3 -烷基），B 和 C 独立地为 CH 2 或 CH-（C 1 -C 3 -烷基），以及 R 5 是芳基或杂芳基，可任选被说明书中列出的取代基取代。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、慢性肾功能衰竭、肝硬化、骨质疏松症、记忆力受限或学习能力受限，或降低绝经后妇女或服用避孕药后的心血管风险。
• ACYLATED 1,2,3,4-TETRAHYDRONAPHTHYL AMINES AND THEIR USE AS PHARMACEUTICAL
  申请人：Aventis Pharma Deutschland GmbH

  公开号：EP1370530A1

  公开（公告）日：2003-12-17
• US6949556B2
  申请人：——

  公开号：US6949556B2

  公开（公告）日：2005-09-27
• [EN] ACYLATED 1,2,3,4-TETRAHYDRONAPHTHYL AMINES AND THEIR USE AS PHARMACEUTICAL<br/>[FR] AMINES 1,2,3,4-TETRAHYDRONAPHTYLE ACYLEES ET LEUR UTILISATION EN TANT QU'AGENT PHARMACEUTIQUE
  申请人：AVENTIS PHARMA GMBH

  公开号：WO2002064565A1

  公开（公告）日：2002-08-22

  The present invention relates to compounds of general formula (I), wherein R1-R4 have the meanings given in the description, A is CH¿2?, CHOH or CH-(C1-C3-alkyl), B and C are independently CH2 or CH-(C1-C3-alkyl), and R?5¿ is heteroaryl group possibly substituted by the substituents listed in the description. The compounds are 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, endothel 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, and restricted memory performance or a restricted ability to learn, or the lowering of cardiovascular risk of postmenopausal women or after intake of contraceptives.