21908-10-1Relevant academic research and scientific papers
Development of an in vivo active, dual EP1 and EP3 selective antagonist based on a novel acyl sulfonamide bioisostere
Downey, Jason D.,Saleh, Sam A.,Bridges, Thomas M.,Morrison, Ryan D.,Scott Daniels,Lindsley, Craig W.,Breyer, Richard M.
, p. 37 - 41 (2013/02/23)
Recent preclinical studies demonstrate a role for the prostaglandin E 2 (PGE2) subtype 1 (EP1) receptor in mediating, at least in part, the pathophysiology of hypertension and diabetes mellitus. A series of amide and N-acylsulfonamid
Selection and development of the manufacturing route for EP1 antagonist GSK269984B
Whiting, Matthew,Harwood, Kathy,Hossner, Frank,Turner, Peter G.,Wilkinson, Mark C.
experimental part, p. 820 - 831 (2011/03/19)
A potential manufacturing route for the EP1 antagonist GSK269984B was developed. Four synthetic approaches were examined, and a successful realisation of each is presented. The rationale supporting selection of the preferred route is discussed.
Theramutein modulators
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Page/Page column 194, (2010/02/17)
This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
A versatile method for the hydrolysis of gem-dibromomethylarenes bearing carboxylate or boronate group into aldehydes
Augustine, John Kallikat,Naik, Y. Arthoba,Mandal, Ashis Baran,Chowdappa, Nagaraja,Praveen, Vinuthan B.
, p. 688 - 695 (2008/04/12)
Hydrolysis of gem-dibromomethylarenes bearing carboxylate or boronate group to corresponding aldehydes without affecting the ester group was successfully accomplished in high yields by subjecting them to refluxing pyridine. Both aromatic and heteroaromatic substrates gave the corresponding aldehydes in good yields. This method was efficiently adapted for the large scale synthesis of 2d and 2f.
THERAMUTEIN MODULATORS
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Page/Page column 229, (2008/12/07)
This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
