882689-32-9Relevant academic research and scientific papers
MACROCYCLIC COMPOUNDS USEFUL AS CHITINASE INHIBITORS
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Paragraph 0128; 0173-0174; 0177, (2021/07/29)
The present invention relates to macrocyclic compounds of formula (I) and their use as chitinase inhibitors as well as to pharmaceutical compositions and methods of preparation thereof. The compounds can in particular be used in the treatment, prevention and/or amelioration of asthma.
Zwitterionic CRTh2 antagonists
Luker, Tim,Bonnert, Roger,Paine, Stuart W.,Schmidt, Jerzy,Sargent, Carol,Cook, Anthony R.,Cook, Andrew,Gardiner, Philip,Hill, Steve,Weyman-Jones, Carol,Patel, Anil,Thom, Stephen,Thorne, Philip
, p. 1779 - 1788 (2011/05/05)
A novel series of zwitterions is reported that contains potent, selective antagonists of the chemoattractant receptor-homologous expressed on Th2 lymphocytes receptor (CRTh2 or DP2). A high quality lead compound 2 was discovered from virtual screening based on the pharmacophore features present in a literature compound 1. Lead optimization through side chain modification and preliminary changes around the acid are disclosed. Optimization of physicochemical properties (log D, MWt, and HBA) allowed maintenance of high CRTh2 potency while achieving low rates of metabolism and minimization of other potential concerns such as hERG channel activity and permeability. A step-change increase in potency was achieved through addition of a single methyl group onto the piperazine ring, which gave high quality compounds suitable for progression into in vivo studies.
Novel Compounds
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Page/Page column 16, (2008/12/04)
The invention relates to substituted aryl acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
