- 3-piperidyl-4-oxoquinazoline derivatives and pharmaceutical compositions comprising the same
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3-piperidyl-4-oxoquinazoline derivatives are provided, which is represented by the formula (I): wherein R represents an amino group or a cyclic amino group such as dibenzoazepine, each of which is substituted with a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, or the like, n is an integer of 1 to 3, R3and R4independently represents a hydrogen atom, a lower alkyl group, or the like, or a pharmaceutically acceptable salt thereof. Compounds (I) of the present invention have excellent MTP-inhibitory activity. Thus, these compounds not only inhibit formation of LDL that is a cause of arteriosclerotic diseases but also regulate TG, cholesterol, and lipoproteins such as LDL in the blood and regulate cellular lipids through regulation of MTP activity. They can also be used as a new type of preventive or therapeutic agents for hyperlipemia or arteriosclerotic diseases. Furthermore, they can be used as therapeutic or preventive agents for pancreatitis, obesity, hypercholesterolemia, and hypertriglyceridemia.
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- Synthesis and antiarrhythmic activity of new [(dialkylamino)alkyl]pyridylacetamides
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The synthesis of new [(dialkylamino)alkyl]pyridylacetamides is reported. These compounds displayed a potent antiarrhythmic activity, as demonstrated on a model of myocardial infarction in the conscious dog. Structure-activity relationships are discussed within a series of 22 homologues, comparing relative antiarrhythmic properties and cardiac side effects. One of these compounds, 15, has been selected as a candidate for clinical evaluation in man.
- Bernhart,Condamine,Demarne,Roncucci,Gagnol,Gautier,Serre
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p. 451 - 455
(2007/10/02)
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