Oxadiazole derivative having endothelial lipase inhibitory activity

A compound and solvate technology, applied in the field of oxadiazole derivatives with vascular endosebase inhibitory activity, can solve the problems of record of HDLc elevation without EL inhibitory effect and the like
CN102753545AInactive Publication Date: 2012-10-24SHIONOGI & CO LTD

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHIONOGI & CO LTD
Publication Date
2012-10-24
Estimated Expiration
Not applicable · inactive patent

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Abstract

Provided is a compound useful as an endothelial lipase inhibitor. The compound is a compound represented by formula (I), a pharmaceutically acceptable salt thereof, or a solvate of either. In formula (I), ring A is an aromatic carbocycle or an aromatic heterocycle; Z is -NR5-, -O-, or -S-; R5 is a hydrogen atom, an (un)substituted alkyl, an (un)substituted aryl, etc.; R1 is a hydrogen atom, a halogen atom, hydroxy, cyano, nitro, carboxy, an (un)substituted alkyl, etc.; R2 and R3 each independently is a hydrogen atom, a halogen atom, hydroxy, etc.; R4 is a group represented by the formula -(CR6R7)n-R8 (wherein R6 and R7 each independently is a hydrogen atom, a halogen atom, hydroxy, etc., n is an integer of 0-3, and R8 is carboxy, cyano, an (un)substituted alkyl, etc.); RX is a halogen atom, hydroxy, cyano, nitro, carboxy, an (un)substituted alkyl, etc.; and m is an integer of 0-3.
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Description

technical field

[0001] The present invention relates to a compound having vascular endothelial lipase (Endthelial Lipase, hereinafter referred to as EL) inhibitory activity and usable as a medicine. Background technique

[0002] Endthelial Lipase (EL) is a triglyceride lipase (Triglyceride Lipase) family that is juxtaposed with lipoprotein lipase (Lipoprotein Lipase) (LPL) and liver lipase (Hepatic Lipase) (HL). Analysis of exogenous mice or transgenic mice revealed that they are involved in the metabolism of HDLc through strong phospholipase activity, and have attracted attention as a factor limiting the amount of HDLc in blood (Non-Patent Document 1).

[0003] Previously known coronary artery disease (CAD) has a negative correlation with the amount of HDLc in the blood. HDLc shows anti-arteriosclerosis effects through anti-oxidation, anti-inflammation, reverse cholesterol transport, etc. Low HDLc is considered to be one of the risk factors for CAD.

[0004] Therefore, EL...

Claims

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