Document Detail


Bradykinin B1 receptor antagonists: a patent update 2009 - 2012.
MedLine Citation:
PMID:  23033970     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
INTRODUCTION: Due to the role of bradykinin B1 receptor (B1R) in pain and inflammation, B1R antagonists have been suggested as promising drug candidates in chronic pain states. The first disclosed B1R antagonists were peptidomimetics, however, during the last few years, novel chemotypes with improved pharmacodynamic and pharmacokinetic properties have been identified.
AREAS COVERED: In this review, we aim to give an overview on B1R antagonists published in patent applications between January 2009 and July 2012.
EXPERT OPINION: Extensive research on B1R antagonists resulted in basically two chemotypes including sulfonamides and carboxamides. The most important achievement is that these scaffolds show improved PK profile relative to previous compounds. Several B1R antagonists entered clinical trials and the results from proof-of-concept Phase II clinical study is expected to be disclosed soon.
Authors:
Éva Bozó; János Éles; György M Keserű
Publication Detail:
Type:  Journal Article; Review     Date:  2012-10-03
Journal Detail:
Title:  Expert opinion on therapeutic patents     Volume:  22     ISSN:  1744-7674     ISO Abbreviation:  Expert Opin Ther Pat     Publication Date:  2012 Dec 
Date Detail:
Created Date:  2012-11-20     Completed Date:  2013-05-10     Revised Date:  2013-11-06    
Medline Journal Info:
Nlm Unique ID:  9516419     Medline TA:  Expert Opin Ther Pat     Country:  England    
Other Details:
Languages:  eng     Pagination:  1443-52     Citation Subset:  IM    
Affiliation:
Discovery Chemistry, Gedeon Richter plc, Gyömrői út 19-21, H-1103 Budapest, Hungary.
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MeSH Terms
Descriptor/Qualifier:
Analgesics / chemistry,  pharmacology*,  therapeutic use
Animals
Anti-Inflammatory Agents / chemistry,  pharmacology*,  therapeutic use
Drug Design*
Humans
Molecular Structure
Patents as Topic*
Protein Conformation
Receptor, Bradykinin B1 / antagonists & inhibitors*
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Analgesics; 0/Anti-Inflammatory Agents; 0/Receptor, Bradykinin B1

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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