Document Detail


Treatment and prevention of various therapeutic conditions using OX receptor antagonistic activity (WO2012081692).
MedLine Citation:
PMID:  23282091     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
Application WO2012081692 from Taisho Pharmaceutical Co. Ltd. claims pyrazole-based antagonists of the orexin-1 and orexin-2 receptors. Utility in a number of therapeutic areas is claimed, including the treatment of sleep disorders; the most likely use of the claimed compounds. Data from in vitro functional assays are presented, with the claimed compounds typically being dual orexin receptor antagonists (DORAs) or having moderate selectivity for orexin-1. Structurally, the claimed compounds represent a variation on established DORA SAR themes and translate features of clinical compounds into a pyrazole-based scaffold. Example 52, the most potent molecule in the application, has similar molecular weight and lipophilicity to suvorexant, the most advanced DORA, with broadly comparable potency in functional assays.
Authors:
John A Christopher; Miles S Congreve
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2013-1-3
Journal Detail:
Title:  Expert opinion on therapeutic patents     Volume:  -     ISSN:  1744-7674     ISO Abbreviation:  Expert Opin Ther Pat     Publication Date:  2013 Jan 
Date Detail:
Created Date:  2013-1-3     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9516419     Medline TA:  Expert Opin Ther Pat     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
Heptares Therapeutics Ltd., BioPark , Broadwater Road, Welwyn Garden City, Hertfordshire AL7 3AX , UK +44 0 1707 358 638 ; +44 0 1707 358 640 ; miles.congreve@heptares.com.
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