Aliphatic spirolactam CGRP receptor antagonists

Patent metadata

Field	Value
Publication number	US-9227972-B2
Application number	US-201314399649-A
Country	US
Kind code	B2
Filing date	May 3, 2013
Priority date	May 9, 2012
Publication date	Jan 5, 2016
Grant date	Jan 5, 2016

Abstract

The present invention is directed to aliphatic spirolactam derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical\compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

First claim

What is claimed is:

1. A compound which is:
(3′S)-3-(3-(6-Methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,5-trifluorophenyl)piperidin-3-yl)prop-1-en-1-yl)-5,7-dihydrospiro[cyclopenta[b]pyridine-6,3′-pyrrolo[2,3-b]pyridin]-2′(1′H)-one;

or a pharmaceutically acceptable salt thereof.

2. A compound of the Formula:

wherein, “nR A ” is from 0 to 4 halogen substituents and R B and R C are independently C 1-6 -alkyl which are optionally substituted with halogen.

3. A pharmaceutical composition comprising a compound of claim 2 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

4. A method of treating Migraine by providing an effective amount of a pharmaceutical formulation of claim 3 to a patient in need thereof.

Assignees

• Merck Sharp & Dohme

Inventors

• Bell Ian M
• Fraley Mark
• Biftu Tesfaye
• Zhu Cheng
• Nair Anilkumar
• Mitchell Helen

Classifications

• A61P25/06

  Antimigraine agents · CPC title

• A61K31/451

  having a carbocyclic group directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine · CPC title

• A61K31/45

  having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide · CPC title

• A61K31/4523

  containing further heterocyclic ring systems · CPC title

• C07D471/20 Primary

  Spiro-condensed systems · CPC title