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Page 1
Improving the oral efficacy of CNS drug candidates: discovery of highly orally efficacious piperidinyl piperidine M2 muscarinic receptor antagonists.
Wang Y, Chackalamannil S, Hu Z, Greenlee WJ, Clader J, Boyle CD, Kaminski JJ, Billard W, Binch H 3rd, Crosby G, Ruperto V, Duffy RA, Cohen-Williams M, Coffin VL, Cox KA, Grotz DE, Lachowicz JE. Wang Y, et al. Among authors: coffin vl. J Med Chem. 2002 Dec 5;45(25):5415-8. doi: 10.1021/jm0255163. J Med Chem. 2002. PMID: 12459007
Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification.
Boyle CD, Vice SF, Campion J, Chackalamannil S, Lankin CM, McCombie SW, Billard W, Binch H 3rd, Crosby G, Williams MC, Coffin VL, Cox KA, Grotz DE, Duffy RA, Ruperto V, Lachowicz JE. Boyle CD, et al. Among authors: coffin vl. Bioorg Med Chem Lett. 2002 Dec 2;12(23):3479-82. doi: 10.1016/s0960-894x(02)00742-4. Bioorg Med Chem Lett. 2002. PMID: 12419388
Cyclic urea derivatives as potent NK1 selective antagonists.
Shue HJ, Chen X, Shih NY, Blythin DJ, Paliwal S, Lin L, Gu D, Schwerdt JH, Shah S, Reichard GA, Piwinski JJ, Duffy RA, Lachowicz JE, Coffin VL, Liu F, Nomeir AA, Morgan CA, Varty GB. Shue HJ, et al. Among authors: coffin vl. Bioorg Med Chem Lett. 2005 Sep 1;15(17):3896-9. doi: 10.1016/j.bmcl.2005.05.111. Bioorg Med Chem Lett. 2005. PMID: 16019209
Muscarinic agonists and antagonists in the treatment of Alzheimer's disease.
Greenlee W, Clader J, Asberom T, McCombie S, Ford J, Guzik H, Kozlowski J, Li S, Liu C, Lowe D, Vice S, Zhao H, Zhou G, Billard W, Binch H, Crosby R, Duffy R, Lachowicz J, Coffin V, Watkins R, Ruperto V, Strader C, Taylor L, Cox K. Greenlee W, et al. Farmaco. 2001 Apr;56(4):247-50. doi: 10.1016/s0014-827x(01)01102-8. Farmaco. 2001. PMID: 11421251 Review.
Benzylidene ketal derivatives as M2 muscarinic receptor antagonists.
Boyle CD, Chackalamannil S, Chen LY, Dugar S, Pushpavanam P, Billard W, Binch H 3rd, Crosby G, Cohen-Williams M, Coffin VL, Duffy RA, Ruperto V, Lachowicz JE. Boyle CD, et al. Among authors: coffin vl. Bioorg Med Chem Lett. 2000 Dec 18;10(24):2727-30. doi: 10.1016/s0960-894x(00)00553-9. Bioorg Med Chem Lett. 2000. PMID: 11133078
Metabolic stabilization of benzylidene ketal M(2) muscarinic receptor antagonists via halonaphthoic acid substitution.
Boyle CD, Chackalamannil S, Clader JW, Greenlee WJ, Josien HB, Kaminski JJ, Kozlowski JA, McCombie SW, Nazareno DV, Tagat JR, Wang Y, Zhou G, Billard W, Binch H, Crosby G, Cohen-Williams M, Coffin VL, Cox KA, Grotz DE, Duffy RA, Ruperto V, Lachowicz JE. Boyle CD, et al. Among authors: coffin vl. Bioorg Med Chem Lett. 2001 Sep 3;11(17):2311-4. doi: 10.1016/s0960-894x(01)00435-8. Bioorg Med Chem Lett. 2001. PMID: 11527721
Cyclic urea derivatives as potent NK1 selective antagonists. Part II: Effects of fluoro and benzylic methyl substitutions.
Shue HJ, Chen X, Schwerdt JH, Paliwal S, Blythin DJ, Lin L, Gu D, Wang C, Reichard GA, Wang H, Piwinski JJ, Duffy RA, Lachowicz JE, Coffin VL, Nomeir AA, Morgan CA, Varty GB, Shih NY. Shue HJ, et al. Among authors: coffin vl. Bioorg Med Chem Lett. 2006 Feb 15;16(4):1065-9. doi: 10.1016/j.bmcl.2005.10.072. Epub 2005 Nov 14. Bioorg Med Chem Lett. 2006. PMID: 16290143
44 results