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Expert Opin Ther Pat. 2009 Aug;19(8):1149-55. doi: 10.1517/13543770902798061.

Acyl hydroxypyrazoles as novel agonists for high-affinity nicotinic acid receptor GPR109A: WO2008051403.

Author information

1
Research Fellow Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065-0900, USA. hong_shen@merck.com

Abstract

BACKGROUND:

Acyl hydroxypyrazoles were discovered and claimed by Merck as novel agonists for the high-affinity nicotinic acid receptor, G-protein coupled receptor 109A (GPR109A). The fused bicyclic core contains a hydroxypyrazole that mimics the anthranilide moiety described in their earlier patents and patent publications.

OBJECTIVE:

This article evaluates new GPR109A receptor agonists disclosed by Merck in the recent patent WO2008051403.

CONCLUSION:

The aim of this invention was to provide potential therapy to reduce free fatty acids (FFA), low-density lipoprotein cholesterol (LDL-C), total cholesterol, and serum triglycerides (TG), and to raise high-density lipoprotein cholesterol (HDL-C). Thus, these agonists could - potentially - be used to treat dyslipidemia, atherosclerosis, and metabolic syndromes such as diabetes.

PMID:
19566484
DOI:
10.1517/13543770902798061
[Indexed for MEDLINE]

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