[EN] MTP INHIBITING ARYL PIPERIDINES OR PIPERAZINES SUBSTITUTED WITH 5-MEMBERED HETEROCYCLES<br/>[FR] PIPERIDINES D'ARYLE OU PIPERAZINES SUBSTITUEES PAR DES HETEROCYCLES A 5 RAMIFICATIONS INHIBANT LA MTP
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2005085226A1
公开(公告)日:2005-09-15
The present invention is concerned with novel aryl piperidine or piperazine compounds substituted with certain 5-membered heterocycles having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes (Formula (I)). The invention further relates to methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of atherosclerosis, pancreatitis, obesity, hypertriglyceridemia, hypercholesterolemia, hyperlipidemia, diabetes and type II diabetes.
Nickel-catalyzed reductive cross-coupling of polyfluoroarenes with alkyl electrophiles by site-selective C–F bond activation
作者:Longlong Xi、Liting Du、Zhuangzhi Shi
DOI:10.1016/j.cclet.2022.01.077
日期:2022.9
A nickel-catalyzed reductive cross-coupling reactions between polyfluoroarenes and alkyl electrophiles is reported to access substituted fluoroarenes through chelation-assisted C–F activation. Diverse primary and secondary alkyl (pseudo)halides can be employed to couple with polyfluoroarenes, showing excellent regioselectivity. Furthermore, the nickel-catalyzed asymmetric cross-coupling of polyfluoroarenes
NOVEL 2,3-DIHYDRO-1H-IMIDAZO(1,2-A)PYRIMIDIN-5-ONE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF
申请人:Brolio Maurice
公开号:US20120142679A1
公开(公告)日:2012-06-07
The invention relates to the novel materials of formula (I), where R
1
is an optionally substituted L-aryl or
-heteroaryl, such that L is: an alkyl or CO, or L
X, with L
being an alkyl and X being O or S; R
2
is H or an alkyl; R
3
is an alkyl optionally substituted by Hal; and R
4
is Hou Hal, wherein said materials are in any isomeric form and the salts thereof, to be used as drugs.
NOVEL 1,2,3,4-TETRAHYDRO-PYRIMIDO(1,2-A)PYRIMIDIN-6-ONE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF
申请人:Bacque Eric
公开号:US20120208810A1
公开(公告)日:2012-08-16
The invention relates to the novel materials of formula (I), where: R
1
is an optionally substituted L-aryl or L-heteroaryl, such that L is a single bond, alkyl, CO, or CO-alk, or L-X, with L□ being an alkyl and X being O or S; R
2
is H or alkyl; R
3
is an alkyl optionally substituted by Hal; and R
4
is Hou Hal, wherein said materials are in any isomeric form and the salts thereof, to be used as drugs.
1,2,3,4-tetrahydro-pyrimido(1,2-a)pyrimidin-6-one derivatives, preparation thereof, and pharmaceutical use thereof
申请人:Bacque Eric
公开号:US08846670B2
公开(公告)日:2014-09-30
The invention relates to compounds of the formula:
or their racemic, enantiomeric or diastereoisomeric isomers, or pharmaceutically acceptable salts of the compounds of formula I or the racemic, enantiomeric or diasteroisomeric isomers.