darifenacin hydrochloride | 586346-94-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: darifenacin hydrochloride
• 英文别名: 2-[(3S)-1-[2-(2,3-dihydro-1-benzofuran-5-yl)ethyl]pyrrolidin-3-yl]-2,2-diphenylacetamide;hydrochloride
• CAS: 586346-94-3
• 化学式: C₂₈H₃₀N₂O₂*ClH
• 分子量: 463.019
• InChiKey: WSIWCVQJVQFZQW-VQIWEWKSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.38
• 重原子数：
  33
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  55.6
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  达非那新 在 盐酸 作用下， 以 水 、 丙酮 为溶剂， 反应 12.0h， 生成 darifenacin hydrochloride
  参考文献：
  名称：

  [EN] NOVEL AND IMPROVED PROCESSES FOR THE PREPARATION OF INTERMEDIATES OF DARIFENACIN, DARIFENACIN AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS
  [FR] PROCÉDÉS NOUVEAUX ET PERFECTIONNÉS POUR LA PRÉPARATION D'INTERMÉDIAIRES DE DARIFÉNACINE, DE LA DARIFÉNACINE ET DE SES SELS PHARMACEUTIQUEMENT ACCEPTABLES

  摘要：

  公开号：

  WO2008126106A3

文献信息

• Process for Preparation of Darifenacin and Intermediates Used in the Process
  申请人：Bhanu Manjunath Narayan

  公开号：US20110144354A1

  公开（公告）日：2011-06-16

  Disclosed herein is a process for the preparation of darifenacin and physiologically acceptable salts thereof. Also disclosed is a compound of formula X: wherein R is linear or branched C 1-10 alkyl, phenyl, tolyl, ortho-, meta- or para-xylyl which is useful as a intermediate in the preparation of darifenacin.

  本文揭示了一种制备达利那新及其生理上可接受的盐的方法。同时还揭示了一种公式X的化合物：其中R是线性或支链C1-10烷基，苯基，甲苯基，邻、间或对二甲苯基，可用作制备达利那新的中间体。
• Use of cyclooxygenase inhibitors and antimuscarinic agents for the treatment of incontinence
  申请人：Pharmacia Corporation

  公开号：EP1915992A1

  公开（公告）日：2008-04-30

  The present invention provides a method for the use of a cyclooxygenase-2 inhibitor in combination with an anti-muscarinic agent, for the treatment or prophylaxis of interstitial cystitis in a subject in need of such treatment or prevention, comprising administering to the subject an effective amount of the cyclooxygenase-2 inhibitor and the anti-muscarinic agent.

  本发明提供了一种将环氧化酶-2 抑制剂与抗毒蕈碱类药物结合使用的方法，用于治疗或预防需要治疗或预防的受试者的间质性膀胱炎，包括向受试者施用有效量的环氧化酶-2 抑制剂和抗毒蕈碱类药物。
• THERAPEUTIC AGENT FOR STRESS URINARY INCONTINENCE AND FECAL INCONTINENCE
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP3733204A1

  公开（公告）日：2020-11-04

  The present invention provides a medicament for use in treating stress urinary incontinence with fewer adverse effects including a body weight lowering effect. The present invention also provides a medicament for use in treating a disease such as incontinence of feces and further provide a medicament for use in treating a disease such as incontinence of feces with fewer adverse effects including a body weight lowering effect. A medicament for use in treating stress urinary incontinence, comprising a 5-HT2C receptor agonist, wherein the medicament is administered at a dosage lower than the minimum dosage of the agonist as an anti-obesity drug. A medicament for use in treating incontinence of feces, etc., comprising a 5-HT2C receptor agonist. A medicament for use in treating incontinence of feces, comprising a 5-HT2C receptor agonist, wherein the medicament is administered at a dosage lower than the minimum dosage of the agonist as an anti-obesity drug.

  本发明提供了一种用于治疗压力性尿失禁的药物，其不良反应较少，包括降低体重的效果。本发明还提供了一种用于治疗大便失禁等疾病的药物，并进一步提供了一种用于治疗大便失禁等疾病的药物，其不良反应较少，包括有降低体重的作用。 一种用于治疗压力性尿失禁的药物，包含一种5-HT2C受体激动剂，其中该药物的给药剂量低于作为抗肥胖药物的激动剂的最小剂量。一种用于治疗大便失禁等的药物，包含一种 5-HT2C 受体激动剂。一种用于治疗大便失禁等的药物，包含一种5-HT2C受体激动剂，其中该药物作为抗肥胖药物以低于该激动剂最小剂量的剂量给药。
• Method of using cyclooxygenase inhibitors and antimuscarinic agents
  申请人：——

  公开号：US20030191172A1

  公开（公告）日：2003-10-09

  The present invention provides a method for the use of a cyclooxygenase-2 inhibitor, alone or in combination with an anti-muscarinic agent, for the treatment or prophylaxis of a urinary incontinence condition in a subject in need of such treatment or prevention, comprising administering to the subject an effective amount of the cyclooxygenase-2 inhibitor and, optionally, the anti-muscarinic agent.

  本发明提供了一种方法，用于将环氧化酶-2 抑制剂单独或与抗子宫内膜异位症药物联合使用，以治疗或预防需要治疗或预防的受试者的尿失禁病症，该方法包括向受试者施用有效量的环氧化酶-2 抑制剂和可选的抗子宫内膜异位症药物。
• 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）。