(S)-3-(1H-indol-3-yl)-2-(5-isoxazol-3-yl-thiophene-2-sulfonylamino)-2-methyl-N-(1-pyridin-2-yl-cyclohexylmethyl)-propionamide | 425641-05-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: (S)-3-(1H-indol-3-yl)-2-(5-isoxazol-3-yl-thiophene-2-sulfonylamino)-2-methyl-N-(1-pyridin-2-yl-cyclohexylmethyl)-propionamide
• 英文别名: (2S)-3-(1H-indol-3-yl)-2-methyl-2-[[5-(1,2-oxazol-3-yl)thiophen-2-yl]sulfonylamino]-N-[(1-pyridin-2-ylcyclohexyl)methyl]propanamide
• CAS: 425641-05-0
• 化学式: C₃₁H₃₃N₅O₄S₂
• 分子量: 603.766
• InChiKey: WMYMZKAUWMBOGB-PMERELPUSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  42
• 可旋转键数：
  10
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  167
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• Treatment of sexual dysfunction
  申请人：——

  公开号：US20020169101A1

  公开（公告）日：2002-11-14

  Bombesin receptor antagonists have been found to be useful in the treatment of sexual dysfunction in both males and females. They may be selective BB1 antagonists or mixed BB1/BB2 antagonists. Combinations are disclosed of bombesin receptor antagonists with a range of other active compounds, for example PDE5 inhibitors, NEP inhibitors and lasofoxifene.

  Bombesin受体拮抗剂已被发现在男性和女性的性功能障碍治疗中非常有用。它们可以是选择性BB1拮抗剂或混合BB1 / BB2拮抗剂。揭示了与一系列其他活性化合物的Bombesin受体拮抗剂的组合，例如PDE5抑制剂，NEP抑制剂和lasofoxifene。
• Bombesin receptor antagonists
  申请人：——

  公开号：US20040110768A1

  公开（公告）日：2004-06-10

  Bombesin receptor antagonists are provided which are compounds of formula (I) or pharmaceutically acceptable salts thereof: 1 wherein j, k, l, m, n, q, r, Ar, Ar 1 , R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and X are as defined in the description. The compounds of the invention have an affinity for the BB 1 receptor and some of them also have affinity for the BB 2 receptor. Accordingly they may be useful for the diagnosis, prevention, or treatment of male and female sexual dysfunction. They can also be used in the diagnosis, prevention or treatment of anxiety and panic disorders, social phobia, depression, psychoses, sleeping disorders, memory impairment, pulmonary hypertension, lung repair and lung development disorders, cancer including prostate cancer and pancreatic cancer, hepatic porphyria, gastrointestinal secretory disturbances, gastrointestinal disorders including colitis, Crohn's disease and inflammatory bowel disease, emesis, anorexia, pain, seasonal affective disorders, feeding disorders or pruritus.

  提供了化合物(I)或其药学上可接受的盐，其是Bombesin受体拮抗剂：1其中j、k、l、m、n、q、r、Ar、Ar1、R1、R2、R3、R4、R5、R6和X如说明书中所定义的。本发明的化合物具有对BB1受体的亲和力，其中一些化合物还具有对BB2受体的亲和力。因此，它们可能对男性和女性的性功能障碍的诊断、预防或治疗有用。它们还可用于焦虑和恐慌障碍、社交恐惧症、抑郁症、精神病、睡眠障碍、记忆障碍、肺动脉高压、肺修复和肺发育障碍、包括前列腺癌和胰腺癌在内的癌症、肝卟啉症、胃肠分泌紊乱、包括结肠炎、克罗恩病和炎症性肠病在内的胃肠疾病、呕吐、厌食、疼痛、季节性情感障碍、进食障碍或瘙痒的诊断、预防或治疗中使用。
• TREATMENT OF SEXUAL DYSFUNCTION WITH BOMBESIN RECEPTOR ANTAGONISTS
  申请人：Warner-Lambert Company LLC

  公开号：EP1333824B1

  公开（公告）日：2005-09-07
• TREATMENT OF SEXUAL DYSFUNCTION
  申请人：Warner-Lambert Company LLC

  公开号：EP1333824A2

  公开（公告）日：2003-08-13
• TREATMENT OF SEXUAL DYSFUNCTION USING BOMBESIN ANTAGONISTS
  申请人：Warner-Lambert Company LLC

  公开号：EP1333829A1

  公开（公告）日：2003-08-13