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Page 1
Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.
Westaway SM, Brown SL, Fell SC, Johnson CN, MacPherson DT, Mitchell DJ, Myatt JW, Stanway SJ, Seal JT, Stemp G, Thompson M, Lawless K, McKay F, Muir AI, Barford JM, Cluff C, Mahmood SR, Matthews KL, Mohamed S, Smith B, Stevens AJ, Bolton VJ, Jarvie EM, Sanger GJ. Westaway SM, et al. Among authors: bolton vj. J Med Chem. 2009 Feb 26;52(4):1180-9. doi: 10.1021/jm801332q. J Med Chem. 2009. PMID: 19191554
The discovery of biaryl carboxamides as novel small molecule agonists of the motilin receptor.
Westaway SM, Brown SL, Conway E, Heightman TD, Johnson CN, Lapsley K, Macdonald GJ, MacPherson DT, Mitchell DJ, Myatt JW, Seal JT, Stanway SJ, Stemp G, Thompson M, Celestini P, Colombo A, Consonni A, Gagliardi S, Riccaboni M, Ronzoni S, Briggs MA, Matthews KL, Stevens AJ, Bolton VJ, Boyfield I, Jarvie EM, Stratton SC, Sanger GJ. Westaway SM, et al. Among authors: bolton vj. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6429-36. doi: 10.1016/j.bmcl.2008.10.072. Epub 2008 Oct 19. Bioorg Med Chem Lett. 2008. PMID: 19006669
The discovery and optimisation of benzazepine sulfonamide and sulfones as potent agonists of the motilin receptor.
Bailey JM, Scott JS, Basilla JB, Bolton VJ, Boyfield I, Evans DG, Fleury E, Heightman TD, Jarvie EM, Lawless K, Matthews KL, McKay F, Mok H, Muir A, Orlek BS, Sanger GJ, Stemp G, Stevens AJ, Thompson M, Ward J, Vaidya K, Westaway SM. Bailey JM, et al. Among authors: bolton vj. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6452-8. doi: 10.1016/j.bmcl.2009.09.027. Epub 2009 Sep 12. Bioorg Med Chem Lett. 2009. PMID: 19804969