Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)
摘要:
The synthesis and SAR of a series of arylsulfonylpiperazine inhibitors of 11 beta-HSD1 are described. Optimization rapidly led to potent, selective, and orally bioavailable inhibitors demonstrating efficacy in a cynomolgus monkey ex vivo enzyme inhibition model. (C) 2009 Elsevier Ltd. All rights reserved.
DOI:
10.1016/j.bmcl.2008.12.114
作为产物:
描述:
3-吡啶乙酸乙酯 、 1,2-二溴乙烷 以to give ethyl 1-pyridin-3-ylcyclopropane-1-carboxylate which的产率得到1-(吡啶-3-基)环丙烷羧酸乙酯
[EN] COMPOSITION AND METHODS FOR TREATING CHRONIC KIDNEY DISEASE<br/>[FR] COMPOSITION ET PROCÉDÉS DE TRAITEMENT DE MALADIE RÉNALE CHRONIQUE
申请人:MERCK SHARP & DOHME
公开号:WO2016154369A1
公开(公告)日:2016-09-29
This invention relates to the treatment of chronic kidney disease, including diabetic nephropathy, focal segmental glomerulosclerosis (FSGS), nephrotic syndrome, non-diabetic chronic kidney disease, renal fibrosis or acute kidney injury by the administration of an RGD mimetic integrin receptor antagonist, either as a single agent or in combination with other agents.
[EN] DIACYLGLYCEROL ACYLTRANSFERASE 2 INHIBITORS<br/>[FR] INHIBITEURS DE DIACYLGLYCÉROL ACYLTRANSFÉRASE 2
申请人:PFIZER
公开号:WO2013150416A1
公开(公告)日:2013-10-10
Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H- imidazo[4,5-d]pyrazine of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.
Compounds of formula (I):
wherein variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are described.
Compounds of formula (I):
wherein variable groups are defined within; their use in the inhibition of 11βHSD1, processes for making them and pharmaceutical compositions comprising them are described.
Derivatives of purine, 3H-imidazo[4,5-b]pyrimidine and 1H-imidazo[4,5-d]pyrazine of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein.