(Hetero)aryl-substituted-piperidinyl derivatives, a process for their preparation and pharmaceutical compositions containing them
申请人:LES LABORATOIRES SERVIER
公开号:US10654849B2
公开(公告)日:2020-05-19
Compounds of formula (I):
wherein R1, R2, J, K, L, n and W are as defined in the description.
Medicinal products containing the same which are useful in treating conditions requiring pro-apoptotic and/or anti-proliferative agents.
式(I)化合物:
其中 R1、R2、J、K、L、n 和 W 如说明中所定义。
含有相同成分的医药产品,可用于治疗需要促凋亡剂和/或抗增生剂的病症。
Metabolic stability optimization and metabolite identification of 2,5-thiophene amide 17β-hydroxysteroid dehydrogenase type 2 inhibitors
作者:Emanuele M. Gargano、Enrico Perspicace、Nina Hanke、Angelo Carotti、Sandrine Marchais-Oberwinkler、Rolf W. Hartmann
DOI:10.1016/j.ejmech.2014.09.061
日期:2014.11
17 beta-HSD2 is a promising new target for the treatment of osteoporosis. In this paper, a rational strategy to overcome the metabolic liability in the 2,5-thiophene amide class of 17 beta-HSD2 inhibitors is described, and the biological activity of the new inhibitors. Applying different strategies, as lowering the cLogP or modifying the structures of the molecules, compounds 27, 31 and 35 with strongly improved metabolic stability were obtained. For understanding biotransformation in the 2,5-thiophene amide class the main metabolic pathways of three properly selected compounds were elucidated. (C) 2014 Elsevier Masson SAS. All rights reserved.
NEW (HETERO)ARYL-SUBSTITUTED-PIPERIDINYL DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM