582325-22-2Relevant academic research and scientific papers
NICOTINAMIDE DERIVATIVES
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Page/Page column 202, (2010/01/12)
The present invention relates to compounds of the formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are defined herein, to compositions containing such compounds and to the uses of such compounds for the trea
Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1
Westaway, Susan M.,Thompson, Mervyn,Rami, Harshad K.,Stemp, Geoffrey,Trouw, Leontine S.,Mitchell, Darren J.,Seal, Jon T.,Medhurst, Stephen J.,Lappin, Sarah C.,Biggs, James,Wright, James,Arpino, Sandra,Jerman, Jeffrey C.,Cryan, Jennifer E.,Holland, Vicky,Winborn, Kim Y.,Coleman, Tanya,Stevens, Alexander J.,Davis, John B.,Gunthorpe, Martin J.
scheme or table, p. 5609 - 5613 (2009/06/18)
6-Phenylnicotinamide (2) was previously identified as a potent TRPV1 antagonist with activity in an in vivo model of inflammatory pain. Optimization of this lead through modification of both the biaryl and heteroaryl components has resulted in the discovery of 6-(4-fluorophenyl)-2-methyl-N-(2-methylbenzothiazol-5-yl)nicotinamide (32; SB-782443) which possesses an excellent overall profile and has been progressed into pre-clinical development.
Nicotinamide Derivatives
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Page/Page column 20; 30, (2008/12/06)
The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds for the treatment o
