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新型三氮唑衍生物作为生长激素释放肽受体的胃饥饿素拮抗剂:具有改善的受体活性和生物利用度特性(WO2012035124):专利评价。

Novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors (WO2012035124): a patent evaluation.

机构信息

Dipartimento di Scienze Farmaceutiche, Università di Modena e R.E, Via Campi 183 41100, Modena, Italy.

出版信息

Expert Opin Ther Pat. 2012 Sep;22(9):1099-104. doi: 10.1517/13543776.2012.701283. Epub 2012 Jul 19.

DOI:10.1517/13543776.2012.701283
PMID:22809244
Abstract

The patent claims triazole compounds as inhibitors of the ghrelin receptor, the growth-hormone secretagogue receptor (GHS-R1a). These compounds are potent GHS-R1a ligands with an improved in vitro antagonistic activity against ghrelin receptors of at least factor 3 compared with a representative compound disclosed in a previous patent, and are expected to possess, on the basis of the results of in vitro assays, improved safety and human oral bioavailability with respect to the lead.

摘要

专利要求将三唑类化合物作为胃饥饿素受体(GHS-R1a)的抑制剂。这些化合物是有效的 GHS-R1a 配体,与之前专利中公开的代表性化合物相比,对胃饥饿素受体的体外拮抗活性提高了至少 3 倍,并且根据体外试验的结果,预计相对于先导化合物具有更好的安全性和人体口服生物利用度。

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