公开(公告)号：EP1990335A1

公开(公告)日：2008-11-12

申请号：EP07737642.4

申请日：2007-03-01

申请人： Astellas Pharma Inc.

发明人： NIIMI, Tatsuya ,  KAMIKAWA, Akio ,  AMANO, Yasushi ,  YAMAGUCHI, Tomohiko ,  SUZUMURA, Kenichi ,  ENJO, Kentaro ,  FURUTANI, Takashi ,  KAKEFUDA, Akio ,  KONDOH, Yutaka ,  HIRANO, Masaaki

IPC分类号： C07D209/42 ,  A61K31/404 ,  A61K31/407 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/428 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/538 ,  A61P5/24 ,  A61P5/38 ,  A61P13/08 ,  A61P15/00 ,  A61P15/08 ,  A61P17/08 ,  A61P17/10 ,  A61P17/14 ,  A61P35/00

CPC分类号： C07D209/08 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D513/04

摘要： To provide a novel and excellent method for treating and/or preventing prostatic cancer, benign prostatic hyperplasia, acne, seborrhea, hirsutism, baldness, alopecia, precocious puberty, adrenal hypertrophy, polycystic ovary syndrome, breast cancer, lung cancer, endometriosis, leiomyoma and the like based on selective inhibitory activity against 17βHSD type 5.
It was found that an N-sulfonylindole derivative, where the indole ring is substituted by a carboxy group, a carboxy-substituted lower alkyl group or a carboxy-substituted lower alkenyl group at its carbon atom, has potent selective inhibitory activity against 17βHSD type 5 and may become a therapeutic agent and/or preventive agent for benign prostatic hyperplasia, prostatic cancer and the like without accompanying adverse drug reactions due to a decrease in testosterone; and the present invention has thus been completed.

摘要翻译： 提供治疗和/或预防前列腺癌，良性前列腺增生，痤疮，皮脂溢，多毛症，秃发，脱发，早熟性青春期，肾上腺肥大，多囊卵巢综合征，乳腺癌，肺癌，子宫内膜异位症，平滑肌瘤和 其基于对17,2HSD型5的选择性抑制活性。发现其吲哚环被羧基取代的N-磺基吲哚衍生物，羧基取代的低级烷基或羧基取代的低级烯基 碳原子对17,2HSD 5型具有有效的选择性抑制活性，并且可能成为由于睾丸激素降低引起的伴有不良药物反应的良性前列腺增生，前列腺癌等的治疗剂和/或预防剂; 从而完成了本发明。