Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: Discovery of (R)-1-(2-(4&; prime; -(3-methoxypropylsulfonyl)biphenyl-4-yl)e thyl)-2-methylpyrrolidine (APD916)
Semple, Graeme, Santora, Vincent J, Smith, Jeffrey M, Covel, Jonathan A, Hayashi, Rena, Gallardo, Charlemagne, Ibarra, Jason B, Schultz, Jeffrey A, Park, Douglas M, Estrada, Scott A, Hofilena, Brian J, Smith, Brian M, Ren, Albert, Suarez, Marissa, Frazer, John, Edwards, Jeffrey E, Hart, Ryan, Hauser, Erin K, Lorea, Jodie, Grottick, Andrew J
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
Published in Bioorganic & medicinal chemistry letters (01.01.2012)
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Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: Discovery of (R)-1-2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl-2-methylpyrrolidine (APD916)
SEMPLE, Graeme, SANTORA, Vincent J, HOFILENA, Brian J, SMITH, Brian M, REN, Albert, SUAREZ, Marissa, FRAZER, John, EDWARDS, Jeffrey E, HART, Ryan, HAUSER, Erin K, LOREA, Jodie, GROTTICK, Andrew J, SMITH, Jeffrey M, COVEL, Jonathan A, HAYASHI, Rena, GALLARDO, Charlemagne, IBARRA, Jason B, SCHULTZ, Jeffrey A, PARK, Douglas M, ESTRADA, Scott A
Published in Bioorganic & medicinal chemistry letters (2012)
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Published in Bioorganic & medicinal chemistry letters (2012)
Journal Article
Design and Evaluation of Novel Biphenyl Sulfonamide Derivatives with Potent Histamine H(3) Receptor Inverse Agonist Activity
Covel, Jonathan A., Santora, Vincent J., Smith, Jeffrey M., Hayashi, Rena, Gallardo, Charlemagne, Weinhouse, Michael I., Ibarra, Jason B., Schultz, Jeffrey A., Park, Douglas M., Estrada, Scott A., Hofilena, Brian J., Pulley, Michelle D., Smith, Brian M., Ren, Albert, Suarez, Marissa, Frazer, John, Edwards, Jeffrey, Hauser, Erin K., Lorca, Jodie, Semple, Graeme, Grottick, Andrew J.
Published in Journal of medicinal chemistry (24.09.2009)
Published in Journal of medicinal chemistry (24.09.2009)
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Journal Article
Design and Evaluation of Novel Biphenyl Sulfonamide Derivatives with Potent Histamine H3 Receptor Inverse Agonist Activity
Covel, Jonathan A., Santora, Vincent J., Smith, Jeffrey M., Hayashi, Rena, Gallardo, Charlemagne, Weinhouse, Michael I., Ibarra, Jason B., Schultz, Jeffrey A., Park, Douglas M., Estrada, Scott A., Hofilena, Brian J., Pulley, Michelle D., Smith, Brian M., Ren, Albert, Suarez, Marissa, Frazer, John, Edwards, Jeffrey, Hauser, Erin K., Lorea, Jodie, Semple, Graeme, Grottick, Andrew J.
Published in Journal of medicinal chemistry (24.09.2009)
Published in Journal of medicinal chemistry (24.09.2009)
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Journal Article
Synthesis and in Vivo Evaluation of Phenethylpiperazine Amides: Selective 5-Hydroxytryptamine2A Receptor Antagonists for the Treatment of Insomnia
Xiong, Yifeng, Ullman, Brett, Choi, Jin-Sun Karoline, Cherrier, Martin, Strah-Pleynet, Sonja, Decaire, Marc, Dosa, Peter I, Feichtinger, Konrad, Teegarden, Bradley R, Frazer, John M, Yoon, Woo H, Shan, Yun, Whelan, Kevin, Hauser, Erin K, Grottick, Andrew J, Semple, Graeme, Al-Shamma, Hussien
Published in Journal of medicinal chemistry (12.08.2010)
Published in Journal of medicinal chemistry (12.08.2010)
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Identification of 4-amino-2-cyclohexylaminoquinazolines as metabolically stable melanin-concentrating hormone receptor 1 antagonists
Kanuma, Kosuke, Omodera, Katsunori, Nishiguchi, Mariko, Funakoshi, Takeo, Chaki, Shigeyuki, Nagase, Yasuko, Iida, Izumi, Yamaguchi, Jun-ichi, Semple, Graeme, Tran, Thuy-Anh, Sekiguchi, Yoshinori
Published in Bioorganic & medicinal chemistry (15.05.2006)
Published in Bioorganic & medicinal chemistry (15.05.2006)
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Journal Article
Synthesis and in Vivo Evaluation of Phenethylpiperazine Amides: Selective 5-Hydroxytryptamine 2A Receptor Antagonists for the Treatment of Insomnia
Xiong, Yifeng, Ullman, Brett, Choi, Jin-Sun Karoline, Cherrier, Martin, Strah-Pleynet, Sonja, Decaire, Marc, Dosa, Peter I., Feichtinger, Konrad, Teegarden, Bradley R., Frazer, John M., Yoon, Woo H., Shan, Yun, Whelan, Kevin, Hauser, Erin K., Grottick, Andrew J., Semple, Graeme, Al-Shamma, Hussien
Published in Journal of medicinal chemistry (12.08.2010)
Published in Journal of medicinal chemistry (12.08.2010)
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3-Nitro-4-amino benzoic acids and 6-amino nicotinic acids are highly selective agonists of GPR109b
Skinner, Philip J., Cherrier, Martin C., Webb, Peter J., Sage, Carleton R., Dang, Huong T., Pride, Cameron C., Chen, Ruoping, Tamura, Susan Y., Richman, Jeremy G., Connolly, Daniel T., Semple, Graeme
Published in Bioorganic & medicinal chemistry (01.12.2007)
Published in Bioorganic & medicinal chemistry (01.12.2007)
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Agonist lead identification for the high affinity niacin receptor GPR109a
Gharbaoui, Tawfik, Skinner, Philip J., Shin, Young-Jun, Averbuj, Claudia, Jung, Jae-Kyu, Johnson, Benjamin R., Duong, Tracy, Decaire, Marc, Uy, Jane, Cherrier, Martin C., Webb, Peter J., Tamura, Susan Y., Zou, Ning, Rodriguez, Nathalie, Boatman, P. Douglas, Sage, Carleton R., Lindstrom, Andrew, Xu, Jerry, Schrader, Thomas O., Smith, Brian M., Chen, Ruoping, Richman, Jeremy G., Connolly, Daniel T., Colletti, Steven L., Tata, James R., Semple, Graeme
Published in Bioorganic & medicinal chemistry letters (01.09.2007)
Published in Bioorganic & medicinal chemistry letters (01.09.2007)
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(7-Benzyloxy-2,3-dihydro- 1H -pyrrolo[1,2- a ]indol-1-yl)acetic Acids as S1P 1 Functional Antagonists
Buzard, Daniel J., Lopez, Luis, Moody, Jeanne, Kawasaki, Andrew, Schrader, Thomas O., Kasem, Michelle, Johnson, Ben, Zhu, Xiuwen, Thoresen, Lars, Kim, Sun Hee, Gharbaoui, Tawfik, Sengupta, Dipanjan, Calvano, Lorene, Krishnan, Ashwin, Gao, Yinghong, Semple, Graeme, Edwards, Jeff, Barden, Jeremy, Morgan, Michael, Usmani, Khawja, Chen, Chuan, Sadeque, Abu, Chen, Weichao, Christopher, Ronald J., Thatte, Jayant, Fu, Lixia, Solomon, Michelle, Whelan, Kevin, Al-Shamma, Hussien, Gatlin, Joel, Gaidarov, Ibragim, Anthony, Todd, Le, Minh, Unett, David J., Stirn, Scott, Blackburn, Anthony, Behan, Dominic P., Jones, Robert M.
Published in ACS medicinal chemistry letters (11.12.2014)
Published in ACS medicinal chemistry letters (11.12.2014)
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Solubilized phenyl-pyrazole ureas as potent, selective 5-HT2A inverse-agonists and their application as antiplatelet agents
DOSA, Peter I, STRAH-PLEYNET, Sonja, WEBB, Robert R, ADAMS, John W, RAMIREZ, Juan, RICHMAN, Jeremy G, THOMSEN, William, SEMPLE, Graeme, TEEGARDEN, Bradley R, JAYAKUMAR, Honnappa, CASPER, Martin, DECAIRE, Marc, YIFENG XIONG, LEHMANN, Juerg, CHOI, Karoline, ELWELL, Katie, WONG, Amy
Published in Bioorganic & medicinal chemistry letters (15.09.2009)
Published in Bioorganic & medicinal chemistry letters (15.09.2009)
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Discovery and Structure−Activity Relationship of 3-Methoxy- N -(3-(1-methyl-1 H -pyrazol-5-yl)-4-(2-morpholinoethoxy)phenyl)benzamide (APD791): A Highly Selective 5-Hydroxytryptamine 2A Receptor Inverse Agonist for the Treatment of Arterial Thrombosis
Xiong, Yifeng, Teegarden, Bradley R., Choi, Jin-Sun Karoline, Strah-Pleynet, Sonja, Decaire, Marc, Jayakumar, Honnappa, Dosa, Peter I., Casper, Martin D., Pham, Lan, Feichtinger, Konrad, Ullman, Brett, Adams, John, Yuskin, Diane, Frazer, John, Morgan, Michael, Sadeque, Abu, Chen, Weichao, Webb, Robert R., Connolly, Daniel T., Semple, Graeme, Al-Shamma, Hussien
Published in Journal of medicinal chemistry (10.06.2010)
Published in Journal of medicinal chemistry (10.06.2010)
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Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1
Kanuma, Kosuke, Omodera, Katsunori, Nishiguchi, Mariko, Funakoshi, Takeo, Chaki, Shigeyuki, Semple, Graeme, Tran, Thuy-Anh, Kramer, Bryan, Hsu, Debbie, Casper, Martin, Thomsen, Bill, Sekiguchi, Yoshinori
Published in Bioorganic & medicinal chemistry letters (01.09.2005)
Published in Bioorganic & medicinal chemistry letters (01.09.2005)
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GnRH Antagonists: A New Generation of Long Acting Analogues Incorporating p-Ureido-phenylalanines at Positions 5 and 6
Jiang, Guangcheng, Stalewski, Jacek, Galyean, Robert, Dykert, John, Schteingart, Claudio, Broqua, Pierre, Aebi, Audrey, Aubert, Michel L, Semple, Graeme, Robson, Peter, Akinsanya, Karen, Haigh, Robert, Riviere, Pierre, Trojnar, Jerzy, Junien, Jean Louis, Rivier, Jean E
Published in Journal of medicinal chemistry (01.02.2001)
Published in Journal of medicinal chemistry (01.02.2001)
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Solubilized phenyl-pyrazole ureas as potent, selective 5-HT sub(2A) inverse-agonists and their application as antiplatelet agents
Dosa, Peter I, Strah-Pleynet, Sonja, Jayakumar, Honnappa, Casper, Martin, Decaire, Marc, Xiong, Yifeng, Lehmann, Juerg, Choi, Karoline, Elwell, Katie, Wong, Amy, Webb, Robert R, Adams, John W, Ramirez, Juan, Richman, Jeremy G, Thomsen, William, Semple, Graeme, Teegarden, Bradley R
Published in Bioorganic & medicinal chemistry letters (15.09.2009)
Published in Bioorganic & medicinal chemistry letters (15.09.2009)
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