Substituted heterocyclic acetamides as kappa opioid receptor (KOR) agonists

Patent metadata

Field	Value
Publication number	US-9487510-B2
Application number	US-201314382645-A
Country	US
Kind code	B2
Filing date	Mar 5, 2013
Priority date	Mar 5, 2012
Publication date	Nov 8, 2016
Grant date	Nov 8, 2016

Abstract

The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts, wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.

First claim

What is claimed is:

1. A compound of formula (I)

stereoisomers thereof or pharmaceutically acceptable salts thereof;
wherein,
R 1 represents hydrogen, alkyl, haloalkyl or —(CH 2 ) m -cycloalkyl;
R 2 represents
(1) cycloalkyl, or
(2) a group selected from heterocyclyl, heteroaryl or aryl, wherein such group is optionally substituted with 1 to 3 substituents…

Assignees

• Dr Reddys Laboratories Ltd

Inventors

• Sasmal Pradip Kumar
• Vamseekrishna Chintakunta
• Potluri Vijay
• Tehim Ashok
• Gai Yonghua
• Zhang Hang

Classifications

• A61P43/00

  Human Necessities · mapped topic

• A61P29/00

  Human Necessities · mapped topic

• A61P25/04

  Human Necessities · mapped topic

• C07D417/12

  Chemistry & Metallurgy · mapped topic

• C07D403/12 Primary

  Chemistry & Metallurgy · mapped topic