477178-65-7Relevant academic research and scientific papers
ANTHELMINTIC AGENTS AND THEIR USE
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Page/Page column 124, (2010/11/03)
This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceut
Discovery of N-(3-fluorophenyl)-1-[(4-([(35)-3-methyl-1-piperazinyl]methyl) phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate
Westaway, Susan M.,Brown, Samantha L.,Fell, Stephen C. M.,Johnson, Christopher N.,MacPherson, David T.,Mitchell, Darren J.,Myatt, James W.,Stanway, Steven J.,Seal, Jon T.,Stemp, Geoffrey,Thompson, Mervyn,Lawless, Kirk,McKay, Fiona,Muir, Alison I.,Barford, Jonathan M.,Cluff, Chermaine,Mahmood, Sadhia R.,Matthews, Kim L.,Mohamed, Shiyam,Smith, Beverley,Stevens, Alexander J.,Bolton, Victoria J.,Jarvie, Emma M.,Sanger, Gareth J.
experimental part, p. 1180 - 1189 (2010/01/16)
N-(3-Fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl) acetyl]-4-piperidinamine 12 (GSK962040) is a novel small molecule motilin receptor agonist. It possesses excellent activity at the recombinant human motilin receptor and also at the native rabbit motilin receptor where its agonist activity results in potentiation of the amplitude of neuronal-mediated contractions of isolated gastric antrum tissue. Compound 12 also possesses highly promising pharmacokinetic profiles in both rat and dog, and these results, in combination with further profiling in human native tissue and an in vivo model of gastrointestinal transit in the rabbit, have led to its selection as a candidate for further development.
BENZYLPIPERAZINE DERIVATIVES AS MOTILIN RECEPTOR ANTAGONISTS
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Page/Page column 27, (2008/06/13)
The invention relates to compounds of formula (I) processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions or disorders which are mediated via the GPR38 receptor.
