920511-31-5Relevant articles and documents
The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor
Westaway, Susan M.,Brown, Samantha L.,Conway, Elizabeth,Heightman, Tom D.,Johnson, Christopher N.,Lapsley, Kate,Macdonald, Gregor J.,MacPherson, David T.,Mitchell, Darren J.,Myatt, James W.,Seal, Jon T.,Stanway, Steven J.,Stemp, Geoffrey,Thompson, Mervyn,Celestini, Paolo,Colombo, Andrea,Consonni, Alessandra,Gagliardi, Stefania,Riccaboni, Mauro,Ronzoni, Silvano,Briggs, Michael A.,Matthews, Kim L.,Stevens, Alexander J.,Bolton, Victoria J.,Boyfield, Izzy,Jarvie, Emma M.,Stratton, Sharon C.,Sanger, Gareth J.
scheme or table, p. 6429 - 6436 (2009/09/06)
Optimisation of urea (5), identified from high throughput screening and subsequent array chemistry, has resulted in the identification of pyridine carboxamide (33) which is a potent motilin receptor agonist possessing favourable physicochemical and ADME profiles. Compound (33) has demonstrated prokinetic-like activity both in vitro and in vivo in the rabbit and therefore represents a promising novel small molecule motilin receptor agonist for further evaluation as a gastroprokinetic agent.
PIPERAZINE HETEROARYL DERIVATES AS GPR38 AGONISTS
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Page/Page column 57, (2010/11/25)
The invention provides compounds of formula (I) or pharmaceutically acceptable salts thereof, (I) wherein R1, R2, R3, R4, R5, R6, Z, X and B are as defined in the specification. The compounds are partial or full agonists at the GPR38 receptor. Pharmaceutical compositions comprising the compounds, methods of preparing the compounds, uses of the compounds and methods involving the compounds are also provided.
