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226 results

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Page 1
New bicyclic cannabinoid receptor-1 (CB1-R) antagonists.
Carpino PA, Griffith DA, Sakya S, Dow RL, Black SC, Hadcock JR, Iredale PA, Scott DO, Fichtner MW, Rose CR, Day R, Dibrino J, Butler M, Debartolo DB, Dutcher D, Gautreau D, Lizano JS, O'connor RE, Sands MA, Kelly-Sullivan D, Ward KM. Carpino PA, et al. Bioorg Med Chem Lett. 2006 Feb;16(3):731-6. doi: 10.1016/j.bmcl.2005.10.019. Epub 2005 Nov 2. Bioorg Med Chem Lett. 2006. PMID: 16263283
Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist.
Griffith DA, Hadcock JR, Black SC, Iredale PA, Carpino PA, DaSilva-Jardine P, Day R, DiBrino J, Dow RL, Landis MS, O'Connor RE, Scott DO. Griffith DA, et al. J Med Chem. 2009 Jan 22;52(2):234-7. doi: 10.1021/jm8012932. J Med Chem. 2009. PMID: 19102698
Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.
Dow RL, Carpino PA, Hadcock JR, Black SC, Iredale PA, DaSilva-Jardine P, Schneider SR, Paight ES, Griffith DA, Scott DO, O'Connor RE, Nduaka CI. Dow RL, et al. J Med Chem. 2009 May 14;52(9):2652-5. doi: 10.1021/jm900255t. J Med Chem. 2009. PMID: 19351113
Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia.
Verhoest PR, Chapin DS, Corman M, Fonseca K, Harms JF, Hou X, Marr ES, Menniti FS, Nelson F, O'Connor R, Pandit J, Proulx-Lafrance C, Schmidt AW, Schmidt CJ, Suiciak JA, Liras S. Verhoest PR, et al. J Med Chem. 2009 Aug 27;52(16):5188-96. doi: 10.1021/jm900521k. J Med Chem. 2009. PMID: 19630403
In vitro and in vivo pharmacology of CP-945,598, a potent and selective cannabinoid CB(1) receptor antagonist for the management of obesity.
Hadcock JR, Griffith DA, Iredale PA, Carpino PA, Dow RL, Black SC, O'Connor R, Gautreau D, Lizano JS, Ward K, Hargrove DM, Kelly-Sullivan D, Scott DO. Hadcock JR, et al. Biochem Biophys Res Commun. 2010 Apr 2;394(2):366-71. doi: 10.1016/j.bbrc.2010.03.015. Epub 2010 Mar 6. Biochem Biophys Res Commun. 2010. PMID: 20211605
Use of structure-based design to discover a potent, selective, in vivo active phosphodiesterase 10A inhibitor lead series for the treatment of schizophrenia.
Helal CJ, Kang Z, Hou X, Pandit J, Chappie TA, Humphrey JM, Marr ES, Fennell KF, Chenard LK, Fox C, Schmidt CJ, Williams RD, Chapin DS, Siuciak J, Lebel L, Menniti F, Cianfrogna J, Fonseca KR, Nelson FR, O'Connor R, MacDougall M, McDowell L, Liras S. Helal CJ, et al. J Med Chem. 2011 Jul 14;54(13):4536-47. doi: 10.1021/jm2001508. Epub 2011 Jun 8. J Med Chem. 2011. PMID: 21650160
Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors.
Claffey MM, Helal CJ, Verhoest PR, Kang Z, Fors KS, Jung S, Zhong J, Bundesmann MW, Hou X, Lui S, Kleiman RJ, Vanase-Frawley M, Schmidt AW, Menniti F, Schmidt CJ, Hoffman WE, Hajos M, McDowell L, O'Connor RE, Macdougall-Murphy M, Fonseca KR, Becker SL, Nelson FR, Liras S. Claffey MM, et al. J Med Chem. 2012 Nov 8;55(21):9055-68. doi: 10.1021/jm3009635. Epub 2012 Oct 12. J Med Chem. 2012. PMID: 23025719
Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor.
Helal CJ, Arnold EP, Boyden TL, Chang C, Chappie TA, Fennell KF, Forman MD, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, Mente S, O'Connor RE, Pandit J, Piotrowski M, Schmidt AW, Schmidt CJ, Ueno H, Verhoest PR, Yang EX. Helal CJ, et al. J Med Chem. 2017 Jul 13;60(13):5673-5698. doi: 10.1021/acs.jmedchem.7b00397. Epub 2017 Jun 16. J Med Chem. 2017. PMID: 28574706
226 results