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Page 1
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: jarvie em. 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
Identification of small molecule agonists of the motilin receptor.
Heightman TD, Conway E, Corbett DF, Macdonald GJ, Stemp G, Westaway SM, Celestini P, Gagliardi S, Riccaboni M, Ronzoni S, Vaidya K, Butler S, McKay F, Muir A, Powney B, Winborn K, Wise A, Jarvie EM, Sanger GJ. Heightman TD, et al. Among authors: jarvie em. Bioorg Med Chem Lett. 2008 Dec 15;18(24):6423-8. doi: 10.1016/j.bmcl.2008.10.071. Epub 2008 Oct 19. Bioorg Med Chem Lett. 2008. PMID: 18980843
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: jarvie em. 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
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: jarvie em. J Med Chem. 2009 Feb 26;52(4):1180-9. doi: 10.1021/jm801332q. J Med Chem. 2009. PMID: 19191554
GSK962040: a small molecule, selective motilin receptor agonist, effective as a stimulant of human and rabbit gastrointestinal motility.
Sanger GJ, Westaway SM, Barnes AA, Macpherson DT, Muir AI, Jarvie EM, Bolton VN, Cellek S, Näslund E, Hellström PM, Borman RA, Unsworth WP, Matthews KL, Lee K. Sanger GJ, et al. Among authors: jarvie em. Neurogastroenterol Motil. 2009 Jun;21(6):657-64, e30-1. doi: 10.1111/j.1365-2982.2008.01270.x. Neurogastroenterol Motil. 2009. PMID: 19374732
22 results