Delving into the Latest Updates on MK-0489 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

MC4R

Action

agonists

Mechanism

MC4R agonists(Melanocortin receptor 4 agonists)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication-

Inactive Indication

Obesity

Originator Organization

Merck & Co., Inc.

Active Organization-

Inactive Organization

Merck & Co., Inc.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Author: Nargund, Ravi P. ; Liu, Jian ; Miller, Randy R. ; Hong, Qingmei ; Bakshi, Raman K. ; Chen, Airu S. ; Fong, Tung M. ; Dellureficio, James P. ; Tang, Rui ; Strack, Alison M. ; Franklin, Christopher L. ; Chen, Howard Y. ; Tamvakopoulos, Constantin ; Stearns, Ralph A. ; Guo, Liangqin ; Sebhat, Iyassu K. ; Weinberg, David H. ; Ye, Zhixiong ; Wyvratt, Matthew J. Jr. ; Peng, Qianping ; Dobbelaar, Peter H. ; He, Shuwen ; Lai, Yingjie ; Jian, Tianying ; MacNeil, Tanya

We report a series of potent and selective MC4R agonists based on spiroindane amide privileged structures for potential treatments of obesity. Among the synthetic methods used, Method C allows rapid synthesis of the analogs. The series of compounds can afford high potency on MC4R as well as good rodent pharmacokinetic profiles. Compound 1r (MK-0489) demonstrates MC4R mediated reduction of food intake and body weight in mouse models. Compound 1r is efficacious in 14-day diet-induced obese (DIO) rat models.

100 Deals associated with MK-0489

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