NVP-LBX192(NVP-LBX192) - 药物靶点：glucokinase_在研适应症：糖尿病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

glucokinase

作用方式

激活剂

作用机制

glucokinase激活剂(葡萄糖激酶激活剂)

治疗领域

内分泌与代谢疾病

在研适应症

糖尿病

非在研适应症-

原研机构

Novartis Institutes for Biomedical Research, Inc.

在研机构

Novartis Institutes for Biomedical Research, Inc.

非在研机构-

权益机构-

最高研发阶段临床前

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C26H33N5O4S2

InChIKeyGMGMDWSPSKXMJH-OAQYLSRUSA-N

CAS号866772-52-3

关联

100 项与 NVP-LBX192 相关的临床结果

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100 项与 NVP-LBX192 相关的转化医学

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100 项与 NVP-LBX192 相关的专利（医药）

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1

项与 NVP-LBX192 相关的文献（医药）

2009-10-08·Journal of Medicinal Chemistry1区 · 医学

Investigation of Functionally Liver Selective Glucokinase Activators for the Treatment of Type 2 Diabetes

1区 · 医学

Article

作者: Taslimi, Paul M. ; Deacon, Richard ; Caplan, Shari L. ; St. Denny, Irene ; Munshi, Siralee ; Vash, Brian ; Dale, Bethany A. ; Gao, Jiaping ; Stams, Travis ; Kakmak, Mesut ; Beaulieu, Valerie ; Gupta, Ramesh C. ; Schuster, Herbert F. ; Duttaroy, Alokesh ; Bebernitz, Gregory R. ; Grondine, Melissa S. ; Nadkarni, Sunil S. ; Kavana, Michael ; Kirman, Louise C. ; Liang, Jinsheng ; Maniara, Wieslawa M.

Type 2 diabetes is a polygenic disease which afflicts nearly 200 million people worldwide and is expected to increase to near epidemic levels over the next 10-15 years. Glucokinase (GK) activators are currently under investigation by a number of pharmaceutical companies with only a few reaching early clinical evaluation. A GK activator has the promise of potentially affecting both the beta-cells of the pancreas, by improving glucose sensitive insulin secretion, as well as the liver, by reducing uncontrolled glucose output and restoring post-prandial glucose uptake and storage as glycogen. Herein, we report our efforts on a sulfonamide chemotype with the aim to generate liver selective GK activators which culminated in the discovery of 3-cyclopentyl-N-(5-methoxy-thiazolo[5,4-b]pyridin-2-yl)-2-[4-(4-methyl-piperazine-1-sulfonyl)-phenyl]-propionamide (17c). This compound activated the GK enzyme (alphaK(a) = 39 nM) in vitro at low nanomolar concentrations and significantly reduced glucose levels during an oral glucose tolerance test in normal mice.

100 项与 NVP-LBX192 相关的药物交易

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