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1. (WO2001032656) POLYMORPHIC FORM OF A TACHYKININ RECEPTOR ANTAGONIST

Pub. No.:    WO/2001/032656    International Application No.:    PCT/US2000/029394
Publication Date: Fri May 11 01:59:59 CEST 2001 International Filing Date: Thu Oct 26 01:59:59 CEST 2000
IPC: C07C 17/12
C07C 45/00
C07D 413/06
Applicants: MERCK & CO., INC.
CROCKER, Louis
CAI, Dongwei
WANG, Jian
Inventors: CROCKER, Louis
CAI, Dongwei
WANG, Jian
Title: POLYMORPHIC FORM OF A TACHYKININ RECEPTOR ANTAGONIST
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.