N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4-(3-cyclopentylpropyl)-5-tetrazolon-1-yl]benzenesulfonamide | 173900-99-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4-(3-cyclopentylpropyl)-5-tetrazolon-1-yl]benzenesulfonamide
• 英文别名: N-[4-[2-[[2-hydroxy-2-(pyridin-3-yl)ethyl]amino]ethyl]phenyl]-4-[4-(3-cyclopentylpropyl)-5-tetrazolon-1-yl]benzenesulfonamide；4-[4-(3-cyclopentylpropyl)-5-oxotetrazol-1-yl]-N-[4-[2-[(2-hydroxy-2-pyridin-3-ylethyl)amino]ethyl]phenyl]benzenesulfonamide
• CAS: 173900-99-7
• 化学式: C₃₀H₃₇N₇O₄S
• 分子量: 591.734
• InChiKey: GCRTUWDFTYDUFB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  42
• 可旋转键数：
  14
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  148
• 氢给体数：
  3
• 氢受体数：
  9

文献信息

• 6.5 -PYRROLOPIPERIDINE TACHYKININ RECEPTOR ANTAGONISTS
  申请人：Bao Jianming

  公开号：US20100197724A1

  公开（公告）日：2010-08-05

  The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.

  本发明涉及某些羟甲基醚羟异吲哚化合物，其可用作神经激肽-1（NK-1）受体拮抗剂，以及缓激肽和特别是P物质的抑制剂。该发明还涉及包含这些化合物作为活性成分的药物配方，以及这些化合物及其配方在治疗某些疾病，包括呕吐、尿失禁、下尿路症状、抑郁症和焦虑症中的用途。
• [EN] COMBINATION THERAPY FOR THE TREATMENT OF DIABETES AND OBESITY<br/>[FR] TRAITEMENT COMBINE DU DIABETE ET DE L'OBESITE
  申请人：MERCK & CO., INC.

  公开号：WO1997016189A1

  公开（公告）日：1997-05-09

  (EN) The combination of the $g(b)3 adrenergic receptor agonist Compound A and a compound which modifies feeding behavior (e.g., the OB protein) is useful in the treatment of obesity and diabetes, either as compounds, pharmaceutically acceptable salts, pharmaceutical compoisition ingredients. Methods of treating obesity and diabetes are also described.(FR) L'invention porte sur la combinaison d'un composé A agoniste du récepteur adrénergique $g(b)3 et d'un composé modifiant le comportement alimentaire (par exemple la protéine OB) qui s'avèrent utiles contre l'obésité et le diabète. En utilisant soit la composition elle-même, soit ses sels pharmacocompatibles, soit des préparations pharmaceutiques dont ils sont les principes actifs. L'invention porte également sur les procédés de traitement associés.

  将$g(b)3肾上腺素受体激动剂Compound A与改变饮食行为的化合物（例如OB蛋白质）结合使用，可用于治疗肥胖症和糖尿病，无论是作为化合物、药学上可接受的盐、药物组成成分。还描述了治疗肥胖和糖尿病的方法。
• HYDROXYMETHYL ETHER HYDROISOINDOLINE TACHYKININ RECEPTOR ANTAGONISTS
  申请人：DeVita Robert J.

  公开号：US20100105747A1

  公开（公告）日：2010-04-29

  The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.

  本发明涉及某些羟甲基醚羟异吲哚烷化合物，其作为神经激肽-1（NK-1）受体拮抗剂和快速激肽，特别是物质P的抑制剂有用。本发明还涉及包含这些化合物作为活性成分的制药配方，以及这些化合物和它们的配方在治疗某些疾病，包括恶心、尿失禁、下尿路症状、抑郁症和焦虑症中的使用。
• Use of a beta-3 agonist for the treatment of disorders of the prostate and of the lower urogenital tract
  申请人：Michel Christian Martin

  公开号：US20060084700A1

  公开（公告）日：2006-04-20

  This invention describes the use of beta-3-adrenoceptor agonists for the treatment of disorders associated with the prostate. These include disorders like those occurring in a prostatitis, where attributable to inflammatory processes or chronic irritation, or disorders like those associated with benign changes of the prostate. The invention is particularly suitable for the treatment of benign prostatic hyperplasia (BPH).

  本发明描述了使用β-3肾上腺素受体激动剂治疗与前列腺有关的疾病。这些疾病包括由炎症过程或慢性刺激引起的前列腺炎等疾病，或与前列腺良性病变有关的疾病。本发明尤其适用于治疗良性前列腺增生症（BPH）。
• COMBINATION THERAPY FOR THE TREATMENT OF DIABETES AND OBESITY
  申请人：MERCK & CO., INC.

  公开号：EP0858340A1

  公开（公告）日：1998-08-19