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Page 1
1,2-diamino-ethane-substituted-6,7,8,9-tetrahydro-5H-pyrimido[4,5-d]azepines as TRPV1 antagonists with improved properties.
Lebsack AD, Rech JC, Branstetter BJ, Hawryluk NA, Merit JE, Allison B, Rynberg R, Buma J, Rizzolio M, Swanson N, Ao H, Maher MP, Herrmann M, Freedman J, Scott BP, Luo L, Bhattacharya A, Wang Q, Chaplan SR, Wickenden AD, Breitenbucher JG. Lebsack AD, et al. Among authors: rizzolio m. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7142-6. doi: 10.1016/j.bmcl.2010.09.006. Epub 2010 Sep 7. Bioorg Med Chem Lett. 2010. PMID: 20932750
N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution.
Musso DL, Andersen MW, Andrews RC, Austin R, Beaudet EJ, Becherer JD, Bubacz DG, Bickett DM, Chan JH, Conway JG, Cowan DJ, Gaul MD, Glennon KC, Hedeen KM, Lambert MH, Leesnitzer MA, McDougald DL, Mitchell JL, Moss ML, Rabinowitz MH, Rizzolio MC, Schaller LT, Stanford JB, Tippin T, Warner JR, Whitesell LG, Wiethe RW. Musso DL, et al. Among authors: rizzolio mc. Bioorg Med Chem Lett. 2001 Aug 20;11(16):2147-51. doi: 10.1016/s0960-894x(01)00377-8. Bioorg Med Chem Lett. 2001. PMID: 11514157
Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist.
Swanson DM, Dubin AE, Shah C, Nasser N, Chang L, Dax SL, Jetter M, Breitenbucher JG, Liu C, Mazur C, Lord B, Gonzales L, Hoey K, Rizzolio M, Bogenstaetter M, Codd EE, Lee DH, Zhang SP, Chaplan SR, Carruthers NI. Swanson DM, et al. Among authors: rizzolio m. J Med Chem. 2005 Mar 24;48(6):1857-72. doi: 10.1021/jm0495071. J Med Chem. 2005. PMID: 15771431
Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists.
Allison BD, Phuong VK, McAtee LC, Rosen M, Morton M, Prendergast C, Barrett T, Lagaud G, Freedman J, Li L, Wu X, Venkatesan H, Pippel M, Woods C, Rizzolio MC, Hack M, Hoey K, Deng X, King C, Shankley NP, Rabinowitz MH. Allison BD, et al. Among authors: rizzolio mc. J Med Chem. 2006 Oct 19;49(21):6371-90. doi: 10.1021/jm060590x. J Med Chem. 2006. PMID: 17034143
3-[5-(3,4-Dichloro-phenyl)-1-(4-methoxy-phenyl)-1H-pyrazol-3-yl]-2-m-tolyl-propionate (JNJ-17156516), a novel, potent, and selective cholecystokinin 1 receptor antagonist: in vitro and in vivo pharmacological comparison with dexloxiglumide.
Morton MF, Barrett TD, Yan W, Freedman JM, Lagaud G, Prendergast CE, Moreno V, Pyati J, Figueroa K, Li L, Wu X, Rizzolio M, Breitenbucher JG, McClure K, Shankley NP. Morton MF, et al. Among authors: rizzolio m. J Pharmacol Exp Ther. 2007 Nov;323(2):562-9. doi: 10.1124/jpet.107.124578. Epub 2007 Aug 7. J Pharmacol Exp Ther. 2007. PMID: 17684117
Identification and synthesis of 2,7-diamino-thiazolo[5,4-d]pyrimidine derivatives as TRPV1 antagonists.
Lebsack AD, Branstetter BJ, Hack MD, Xiao W, Peterson ML, Nasser N, Maher MP, Ao H, Bhattacharya A, Kansagara M, Scott BP, Luo L, Rynberg R, Rizzolio M, Chaplan SR, Wickenden AD, Guy Breitenbucher J. Lebsack AD, et al. Among authors: rizzolio m. Bioorg Med Chem Lett. 2009 Jan 1;19(1):40-6. doi: 10.1016/j.bmcl.2008.11.024. Epub 2008 Nov 13. Bioorg Med Chem Lett. 2009. PMID: 19038548
Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.
Letavic MA, Aluisio L, Atack JR, Bonaventure P, Carruthers NI, Dugovic C, Everson A, Feinstein MA, Fraser IC, Hoey K, Jiang X, Keith JM, Koudriakova T, Leung P, Lord B, Lovenberg TW, Ly KS, Morton KL, Motley ST, Nepomuceno D, Rizzolio M, Rynberg R, Sepassi K, Shelton J. Letavic MA, et al. Among authors: rizzolio m. Bioorg Med Chem Lett. 2010 Jul 15;20(14):4210-4. doi: 10.1016/j.bmcl.2010.05.041. Epub 2010 May 16. Bioorg Med Chem Lett. 2010. PMID: 20561786
JNJ-26070109 [(R)4-bromo-N-[1-(2,4-difluoro-phenyl)-ethyl]-2-(quinoxaline-5-sulfonylamino)-benzamide]: a novel, potent, and selective cholecystokinin 2 receptor antagonist with good oral bioavailability.
Morton MF, Barrett TD, Freedman J, Li L, Rizzolio MC, Prendergast CE, Wu X, Moreno V, Pyati J, Figueroa K, Cagnon L, Lagaud G, Ver Donck L, Ghoos E, Allison B, Rabinowitz MH, Shankley NP. Morton MF, et al. J Pharmacol Exp Ther. 2011 Jul;338(1):328-36. doi: 10.1124/jpet.110.178483. Epub 2011 Apr 14. J Pharmacol Exp Ther. 2011. PMID: 21493750
Characterization of 2-(2,6-dichloro-benzyl)-thiazolo[5,4-d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine (JNJ-39729209) as a novel TRPV1 antagonist.
Maher MP, Bhattacharya A, Ao H, Swanson N, Wu NT, Freedman J, Kansagara M, Scott B, Li DH, Eckert WA 3rd, Liu Y, Sepassi K, Rizzolio M, Fitzgerald A, Liu J, Branstetter BJ, Rech JC, Lebsack AD, Breitenbucher JG, Wickenden AD, Chaplan SR. Maher MP, et al. Among authors: rizzolio m. Eur J Pharmacol. 2011 Aug 1;663(1-3):40-50. doi: 10.1016/j.ejphar.2011.05.001. Epub 2011 May 10. Eur J Pharmacol. 2011. PMID: 21575625
28 results