PREPARATION OF FUSED AZOLE DERIVATIVES AS NOVEL DIACYLGLYCERIDE O-ACYLTRANSFERASE 2 INHIBITORS
摘要:
Provided are compounds of Formula I, Formula Ia and Formula Ib and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are DGAT2 inhibitors. Also provided are methods of making compounds of Formula I, Formula Ia and Formula Ib, pharmaceutical compositions comprising compounds of Formula I, Formula Ia and Formula Ib, and methods of using these compounds to treat hepatic steatosis, nonalcoholic steatohepatitis (NASH), hepatic fibrosis, type-2 diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cognitive decline, dementia, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions, comprising administering a compound of Formula I, Ia and Ib and the pharmaceutically acceptable salts, esters, and prodrugs thereof, to a patient in need thereof.
The invention relates to novel compounds for use as inhibitors of NLRP3 inflammasone production, wherein such compounds are as defined by compounds of formula (I) and wherein the integers R1, R2 and R3 are defined in the description, and where the compounds may be useful as medicaments, for instance for use in the treatment of a disease or disorder that is associated with NLRP3 inflammasome activity.
Substituted piperazine derivatives, the preparation thereofand their use as medicaments
申请人:——
公开号:US20030166637A1
公开(公告)日:2003-09-04
The present invention relates to substituted piperazine derivatives of general formula
1
, (I
wherein
R
a
, R
b
, R
c
, R
f
, R
g
, X, m and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.
Studies on the chemical synthesis of potential antimetabolites.<b>30.</b>Regioselective introduction of a chlorine atom into the imidazo[4,5-<i>b</i>]pyridine nucleus
Reactions of some imidazo[4,5-b]pyridine 4-oxides with phosphoryl chloride are described. Treatment of N-1-substituted imidazo[4,5-b]pyridine 4-oxides with phosphoryl chloride led to the predominant formation of 7-chloro derivatives. This feature was successfully applied to the preparation of a chloroimidazo[4,5-b]pyridine nucleoside, which served as an important precursor of 1-deazaadenosine.
描述了一些咪唑并[4,5 - b ]吡啶4-氧化物与磷酰氯的反应。用磷酰氯处理N -1-取代的咪唑并[4,5- b ]吡啶4-氧化物导致主要形成7-氯衍生物。此功能已成功应用于氯咪唑并[4,5- b ]吡啶核苷的制备,它是1-deazaadenosine的重要前体。
PRMT5 INHIBITORS AND USES THEREOF
申请人:Epizyme, Inc.
公开号:US20150133427A1
公开(公告)日:2015-05-14
Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.