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新型取代杂芳族化合物作为硬脂酰辅酶 A 去饱和酶抑制剂。

Novel substituted heteroaromatic compounds as inhibitors of stearoyl-CoA desaturase.

机构信息

Nencki Institute of Experimental Biology, Laboratory of Cell Signaling and Metabolic Disorders, Pasteura 3, 02-093 Warsaw, Poland.

出版信息

Expert Opin Ther Pat. 2010 Jun;20(6):849-53. doi: 10.1517/13543771003702432.

Abstract

Stearoyl-CoA desaturase 1 (SCD1) has been implicated as a novel therapeutic target for the treatment of a variety of metabolic diseases, including diabetes, obesity, hepatic steatosis, atherosclerosis and cardiovascular disease. The application WO2009129625 from Merck Frosst Canada claims novel substituted heteroaromatic compounds as inhibitors of SCD and potential drugs for the pharmacological treatment of metabolic disorders, when used alone or in combination with other drugs. Based on in vitro activity of the patented compounds, these molecules may be considered as potential SCD inhibitors and could be of therapeutic value. However, further preclinical studies are needed to evaluate their curative potential and safety before clinical development.

摘要

硬脂酰辅酶 A 去饱和酶 1(SCD1)已被认为是治疗多种代谢性疾病的新的治疗靶点,包括糖尿病、肥胖、肝脂肪变性、动脉粥样硬化和心血管疾病。加拿大默克·弗雷斯特的 WO2009129625 号申请声称,新型取代的杂芳族化合物作为 SCD 的抑制剂和用于代谢紊乱的药物治疗的潜在药物,单独使用或与其他药物联合使用。基于专利化合物的体外活性,这些分子可以被认为是潜在的 SCD 抑制剂,并具有治疗价值。然而,在进行临床开发之前,还需要进行进一步的临床前研究来评估它们的治疗潜力和安全性。

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