3-piperidyl-4-oxoquinazoline derivatives and pharmaceutical compositions comprising the same
申请人:Japan Tobacco, Inc.
公开号:US06235730B1
公开(公告)日:2001-05-22
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, R3 and R4 independently 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.
Amines are a very important class of compounds and the selective synthesis of differently substituted primary, secondary and tertiary alkyl amines is challenging. Here we present the synthesis of primary, secondary, and tertiary alkyl aminesfrom ammonia and alcohols, aldehydes, ketones and hydrogen by combining borrowing hydrogen or hydrogen autotransfer and reductive amination with hydrogen. The
3-PIPERIDYL-4-OXOQUINAZOLINE DERIVATIVES AND MEDICINCAL COMPOSITIONS CONTAINING THE SAME
申请人:Japan Tobacco Inc.
公开号:EP0970954A1
公开(公告)日:2000-01-12
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 4, R3 and R4 independently 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.