4-Nitrooxybutyl 2-acetamido-3-[2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetyl]sulfanylpropanoate

• 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: 4-Nitrooxybutyl 2-acetamido-3-[2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetyl]sulfanylpropanoate
• 化学式: C28H30ClN3O9S
• 分子量: 620.1
• InChiKey: VRJSAIFPCMOTPZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  42
• 可旋转键数：
  15
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  184
• 氢给体数：
  1
• 氢受体数：
  10

文献信息

• A GNRH ANTAGONIST FOR USE IN THE TREATMENT OF A WOMEN AFFECTED WITH POLYCYSTIC OVARY SYNDROME
  申请人：Institut National de la Santé et de la Recherche Médicale

  公开号：EP3600373A1

  公开（公告）日：2020-02-05
• [EN] A GNRH ANTAGONIST FOR USE IN THE TREATMENT OF A WOMEN AFFECTED WITH POLYCYSTIC OVARY SYNDROME<br/>[FR] ANTAGONISTE DE LA GNRH DESTINÉ À ÊTRE UTILISÉ DANS LE TRAITEMENT D'UNE FEMME AFFECTÉE PAR LE SYNDROME DES OVAIRES POLYKYSTIQUES
  申请人：INST NAT SANTE RECH MED

  公开号：WO2018177746A1

  公开（公告）日：2018-10-04

  The present invention relates to the field of therapeutic treatment of polycystic ovary syndrome (PCOS). Polycystic ovary syndrome, PCOS, is the most common female reproductive disorder against which no therapeutic solution is available, beyond changes in the lifestyle. The inventors have now shown by using in vivo preclinical models, that individuals affected with PCOS have an abnormal elevated production of GnRH and that this elevated production of GnRH was transmitted to their offspring that also develop PCOS. Further, by examining AMH levels in a cohort of pregnant PCOS and control women, the inventors have found that AMH concentrations are significantly higher in PCOS women as compared to healthy women during the second trimester of gestation. These unexpected findings has allowed conceiving both prevention and treatment therapeutic strategies based on the administration of GnRH antagonists. Especially, the present invention relates to a gonadotropin-releasing hormone (GnRH) antagonist for its use in a woman affected with polycystic ovary syndrome (PCOS) for preventing the occurrence of PCOS in the offspring of the said woman. Even more interestingly, the present invention relates to a gonadotropin-releasing hormone (GnRH) antagonist for its use to rescue ovulation and fertility in postpuberal PCOS affected individuals.