Imidazo[1,2-a]pyridines and their use as pharmaceuticals
申请人:sanofi-aventis
公开号:EP1964840A1
公开(公告)日:2008-09-03
Imidazo[1,2-a]pyridines and their use as pharmaceuticals
The present invention relates to derivatives of imidazo[1,2-a]pyridines of the formula (I),
in which R, R1 to R4 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
Metal-free, efficient hydrazination of imidazo[1,2-a]pyridine with diethyl azodicarboxylate in neutral media
作者:Yuanxiang Wang、Brendan Frett、Nick McConnell、Hong-yu Li
DOI:10.1039/c4ob02284j
日期:——
The first example of metal-free regioselective hydrazination of imidazo[1,2-a]pyridine with diethyl azodicarboxylate is accomplished.
第一个无金属的选择性取代咪唑[1,2-a]吡啶与双乙酰基叠氮甲酸乙酯的氢化反应已成功实现。
IMIDAZO[1,2-a]PYRIDINES AND THEIR USE AS PHARMACEUTICALS
申请人:ZOLLER Gerhard
公开号:US20100113412A1
公开(公告)日:2010-05-06
The present invention relates to derivatives of imidazo[1,2-a]pyridines of formula I,
in which R, R1 to R4 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
The present invention provides a GPR receptor function regulator comprising the compound represented by the formula:
[wherein ring A is an optionally substituted isocyclic or heterocyclic ring, P is a bond or spacer, ring D is an optionally substituted monocyclic aromatic ring which may be condensed with a 5-to 7-membered ring, V is a bond or the group represented by the formula -CR14=CR15 - or - N=CR16- (wherein R14, R15 and R16 each represents a hydrogen atom or optionally substituted hydrocarbon group), Q is a bond or spacer, and W is a carboxyl or a group biologically equivalent to a carboxyl] or its salt or a prodrug thereof