DI GIORGIO, PATRICK,HERT, JERÔME,WANG, LISHA,MATTEI, PATRIZIO,RUDOLPH, MARKUS,HUNZIKER, DANIEL
申请号：
PE0006782016
公开号：
PE08452016A1
申请日:
2014.11.24
申请国别(地区):
PE
年份:
2016
代理人:
摘要：
The present Invention relates to compounds of octahidro - - [1,2-c] 3,4-c dipirrol thiocyanatoacetate of formula (i) wherein R1 is quinolinilo replaced, among others and - C (o) - or - S (2 -) R2 is piridilo substituted phenyl substituted among others.Preferred compounds are: [(3aS, 3BS, 6aR, 6BR) - 5 - (1h benzotriazole - 5 - carbonyl) - octahidro - - [1,2-c] dipirrol 3,4-c - yl] - 2 - (6 - Chloro - naftalen - il - 2) - 1 - [methanone (3aS, 3br, 6aS, 6BR) - 5 - (1h benzotriazole - 5 - carbonyl) - octahidro - - [1,2-c] dipirrol 3,4-c il - 2 -] - 3 - (4 - trifluor - methoxy phenyl) - 1 - on - PROPENE A among others.These compounds are inhibitors of i.e., Autotaxin (ATX), which are inhibitors of the production of lysophosphatidic acid (LPA), being useful in the treatment of cancer, fibrotic diseases, among othersLa presente invencion se refiere a compuestos derivados de octahidro-ciclobuta[1,2-C3,4-C]dipirrol-2-ilo de formula (I) donde R1 es quinolinilo sustituido, entre otros Y es –C(O)- o –S(O)2- R2 es piridilo sustituido, fenilo sustituido, entre otros. Son compuestos preferidos: [(3aS,3bS,6aR,6bR)-5-(1H-benzotriazol-5-carbonil)-octahidro-ciclobuta[1,2-c3,4- c]dipirrol-2-il]-(6-cloro-naftalen-2-il)-metanona 1-[(3aS,3bR,6aS,6bR)-5-(1H-benzotriazol-5-carbonil)-octahidro-ciclobuta[1,2-c3,4-c]dipirrol-2-il]-3-(4-trifluor-metoxi-fenil)-propan-1-ona entre otros. Dichos compuestos son inhibidores de autotaxina (ATX), que son inhibidores de la produccion de acido lisofosfatidico (LPA), siendo utiles en el tratamiento de cancer, enfermedades fibroticas, entre otros
