936098-38-3Relevant articles and documents
2-Arylacetamides as Versatile Precursors for 3-Aminoisocoumarin and Homophthalimide Derivatives: Palladium-Catalyzed Cascade Double Carbonylation Reactions
Frutos-Pedre?o, Roberto,García-López, José-Antonio
supporting information, p. 2692 - 2700 (2016/08/30)
The synthesis of biologically relevant homophthalimide and 3-aminoisocoumarin nuclei via palladium-catalyzed carbonylation of 2-(2-iodoaryl)acetamides has been developed. The degree of N-substitution on the starting amide substrate dictates whether C?N or
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.
HETEROCYCLIC SPIRO-COMPOUNDS
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Page/Page column 31, (2008/12/04)
The patent application relates to new heterocyclic compounds of the general formula (I), in which R, R1, R2, Q, T, n and p have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.