Patent · US Expired

Polymorphic form of a tachykinin receptor antagonist

US6432952B1 · kind B1 · utility

3Cited by

1References

14Claims

0Family size

Assignee

MERCK & CO., INC. · US

Inventors

Louis Crocker · Montgomery, US
Dongwei Cai · Edison, US
Jiang Wang · Shanghai, CN

Key dates

Filing date	Oct 26, 2000
Grant date	Aug 13, 2002
Priority date	—
Expiry date	Oct 26, 2020

Classification

Technology area (CPC C)Chemistry; Metallurgy
CPC primaryC07C45/004
WIPO fieldPharmaceuticals
WIPO sectorChemistry

Abstract

This invention is concerned with a novel polymorphic forms of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)4-( 5-(dimethyl-amino)methyl-1,2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl)morpholine hydrochloride which is a tachykinin receptor antagonist useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, pain or migraine, asthma, and emesis. The instant polymorphic forms have advantages over the other known forms of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)4-( 5-(dimethylamino)methyl-1,2,3-triazol-4-yl)methyl-3-(S)-(4-fluorophenyl)morpholine hydrochloride in terms of thermodynamic stability and suitability for inclusion in pharmaceutical formulations.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.