C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 211/56 (2006.01) A61K 31/00 (2006.01) A61K 31/403 (2006.01) A61K 31/438 (2006.01) A61K 31/439 (2006.01) A61K 31/445 (2006.01) A61K 31/454 (2006.01) A61K 31/5377 (2006.01) A61P 11/06 (2006.01) A61P 19/02 (2006.01) A61P 25/06 (2006.01) A61P 25/24 (2006.01) C07D 209/08 (2006.01) C07D 209/52 (2006.01) C07D 211/42 (2006.01) C07D 401/12 (2006.01) C07D 413/06 (2006.01) C07D 453/02 (2006.01) C07D 471/10 (2006.01) C07D 471/18 (2006.01) C07K 14/705 (2006.01) G01N 33/566 (2006.01) G01N 37/00 (2006.01) G06F 19/00
Patent
CA 2332208
The present invention relates to novel screening methods which enable the selection of neurokinin-1 (NK-1) receptor antagonist compounds which do not possess significant inhibitory potency towards cytochrome P450 enzymes, in particular, CYP2D6. The present invention also relates to a method of generating a pharmacophore model for the CYP2D6 inhibitory activity of NK-1. receptor antagonist compounds; to methods for the discovery of molecules that are potential NK-1 receptors antagonist compounds which do not possess significant inhibitory potency towards the CYP2D6 enzyme; to methods of modeling the features of the CYP2D6 pharmacophore useful in selecting NK-1 receptor antagonist molecules which do not possess significant potency towards CYP2D6. Further, the invention also relates to pharmaceutical compositions comprising a NK-1 receptor .antagonist compound which does not possess significant potency towards the CYP2D6 enzyme identified by methods of the invention; to the users of a NK-1 receptor antagonist compound identified by the methods of the invention for the manufacture of medicaments and for the treatment of a condition, a disorder or a disease in a mammal for which an NK-1 antagonist receptor compound identified by the method of the invention is therapeutically useful.
Ekins Sean
Smith Bill Joe
Pfizer Products Inc.
Smart & Biggar
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