AM-3189(AM-3189) - 药物靶点：GPR40_专利_临床

概要

基本信息

药物类型

小分子化药

别名-

靶点

GPR40

作用方式

激动剂

作用机制

GPR40激动剂(游离脂肪酸受体-1激动剂)

治疗领域

内分泌与代谢疾病

在研适应症-

非在研适应症

2型糖尿病

原研机构

Amgen, Inc.

在研机构-

非在研机构

Amgen, Inc.

权益机构-

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构/序列

分子式C27H25ClN2O3

InChIKeyGFFXCPIMXLSUGF-VWLOTQADSA-N

CAS号916219-50-6

关联

100 项与 AM-3189 相关的临床结果

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100 项与 AM-3189 相关的转化医学

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100 项与 AM-3189 相关的专利（医药）

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2

项与 AM-3189 相关的文献（医药）

2016-01-01·Bioorganic & medicinal chemistry letters4区 · 医学

Discovery of the imidazole-derived GPR40 agonist AM-3189

4区 · 医学

Article

作者: Li, An-Rong ; Zhu, Liusheng ; Tonn, George R ; Medina, Julio C ; Liu, Jiwen Jim ; Luo, Jian ; Bartberger, Michael D ; Liu, Jinqian ; Ma, Zhihua ; Zhang, Jane ; Li, Frank ; Sharma, Rajiv ; Houze, Jonathan B ; Zhuang, Run ; Wong, Simon ; Kohn, Todd ; Wang, Yingcai ; Lin, Daniel C-H

As a follow-up to the GPR40 agonist AMG 837, which was evaluated in clinical trials for the treatment of type II diabetes, further optimization led to the discovery of AM-3189 (13k). AM-3189 is representative of a new class of compounds with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837.

2014-05-08·ACS medicinal chemistry letters3区 · 医学

Optimization of GPR40 Agonists for Type 2 Diabetes

3区 · 医学

Article

作者: Lin, Daniel C.-H. ; Houze, Jonathan B. ; Brown, Sean P. ; Medina, Julio C. ; Dransfield, Paul J. ; Zhu, Liusheng ; Zhang, Jane ; Swaminath, Gayathri ; Sharma, Rajiv ; Luo, Jian ; Schmitt, Mike ; Sun, Ying ; Ma, Zhihua ; Wang, Yingcai ; Tonn, George R. ; Zhuang, Run ; Guo, Qi ; Wong, Simon ; Liu, Jiwen (Jim)

GPR40 (FFA1 and FFAR1) has gained significant interest as a target for the treatment of type 2 diabetes. TAK-875 (1), a GPR40 agonist, lowered hemoglobin A1c (HbA1c) and lowered both postprandial and fasting blood glucose levels in type 2 diabetic patients in phase II clinical trials. We optimized phenylpropanoic acid derivatives as GPR40 agonists and identified AMG 837 (2) as a clinical candidate. Here we report our efforts in searching for structurally distinct back-ups for AMG 837. These efforts led to the identification of more polar GPR40 agonists, such as AM-4668 (10), that have improved potency, excellent pharmacokinetic properties across species, and minimum central nervous system (CNS) penetration.

100 项与 AM-3189 相关的药物交易

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