Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. IV. Discovery of 1-[(4,6-Dimethyl-5-pyrimidinyl)carbonyl]- 4-[4-{2-methoxy-1(R)-4-(trifluoromethyl)phenyl}ethyl-3(S)-methyl-1-piperazinyl]- 4-methylpiperidine (Sch-417690/Sch-D), a Potent, Highly Selective, and Orally Bioavailable CCR5 Antagonist
Tagat, Jayaram R, McCombie, Stuart W, Nazareno, Dennis, Labroli, Marc A, Xiao, Yushi, Steensma, Ruo W, Strizki, Julie M, Baroudy, Bahige M, Cox, Kathleen, Lachowicz, Jean, Varty, Geoffrey, Watkins, Robert
Published in Journal of medicinal chemistry (06.05.2004)
Published in Journal of medicinal chemistry (06.05.2004)
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Piperazine-Based CCR5 Antagonists as HIV-1 Inhibitors. II. Discovery of 1-[(2,4-Dimethyl-3-pyridinyl)carbonyl]-4- methyl-4-[3(S)-methyl-4-[1(S)-[4-(trifluoro- methyl)phenyl]ethyl]-1-piperazinyl]- piperidine N1-Oxide (Sch-350634), an Orally Bioavailable, Potent CCR5 Antagonist
Tagat, Jayaram R, Steensma, Ruo W, McCombie, Stuart W, Nazareno, Dennis V, Lin, Sue-Ing, Neustadt, Bernard R, Cox, Kathleen, Xu, Serena, Wojcik, Lisa, Murray, Michael G, Vantuno, Nicole, Baroudy, Bahige M, Strizki, Julie M
Published in Journal of medicinal chemistry (11.10.2001)
Published in Journal of medicinal chemistry (11.10.2001)
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Synthesis of Mono- and Difluoronaphthoic Acids
Tagat, Jayaram R, McCombie, Stuart W, Nazareno, Dennis V, Boyle, Craig D, Kozlowski, Joseph A, Chackalamannil, Samuel, Josien, Hubert, Wang, Yuguang, Zhou, Guowei
Published in Journal of organic chemistry (22.02.2002)
Published in Journal of organic chemistry (22.02.2002)
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Interaction of small molecule inhibitors of HIV-1 entry with CCR5
Seibert, Christoph, Ying, Weiwen, Gavrilov, Svetlana, Tsamis, Fotini, Kuhmann, Shawn E., Palani, Anandan, Tagat, Jayaram R., Clader, John W., McCombie, Stuart W., Baroudy, Bahige M., Smith, Steven O., Dragic, Tatjana, Moore, John P., Sakmar, Thomas P.
Published in Virology (New York, N.Y.) (25.05.2006)
Published in Virology (New York, N.Y.) (25.05.2006)
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Non-aromatic A-ring replacement in the triaryl bis-sulfone CB2 receptor inhibitors
Gilbert, Eric J., Zhou, Guowei, Wong, Michael K.C., Tong, Ling, Shankar, Bandarpalle B., Huang, Chunli, Kelly, Joseph, Lavey, Brian J., McCombie, Stuart W., Chen, Lei, Rizvi, Razia, Dong, Youhao, Shu, Youheng, Kozlowski, Joseph A., Shih, Neng-Yang, Hipkin, R. William, Gonsiorek, Waldemar, Malikzay, Asra, Lunn, Charles A., Favreau, Len, Lundell, Daniel J.
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
Published in Bioorganic & medicinal chemistry letters (15.01.2010)
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Piperazine-Based CCR5 antagonists as HIV-1 inhibitors. I: 2( S)-methyl piperazine as a key pharmacophore element
Tagat, Jayaram R., McCombie, Stuart W., Steensma, Ruo W., Lin, Sue-Ing, Nazareno, Dennis V., Baroudy, Bahige, Vantuno, Nicole, Xu, Serena, Liu, Jia
Published in Bioorganic & medicinal chemistry letters (20.08.2001)
Published in Bioorganic & medicinal chemistry letters (20.08.2001)
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Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides
McCombie, Stuart W., Tagat, Jayaram R., Vice, Susan F., Lin, Sue-Ing, Steensma, Ruo, Palani, Anandan, Neustadt, Bernard R., Baroudy, Bahige M., Strizki, Julie M., Endres, Michael, Cox, Kathleen, Dan, Niya, Chou, Chuan-Chu
Published in Bioorganic & medicinal chemistry letters (10.02.2003)
Published in Bioorganic & medicinal chemistry letters (10.02.2003)
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Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands
Lavey, Brian J., Kozlowski, Joseph A., Shankar, Bandarpalle B., Spitler, James M., Zhou, Guowei, Yang, De-Yi, Shu, Youheng, Wong, Michael K.C., Wong, Shing-Chun, Shih, Neng-Yang, Wu, Jie, McCombie, Stuart W., Rizvi, Razia, Wolin, Ronald L., Lunn, Charles A.
Published in Bioorganic & medicinal chemistry letters (01.07.2007)
Published in Bioorganic & medicinal chemistry letters (01.07.2007)
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Inhibition of the development of collagen‐induced arthritis in rhesus monkeys by a small molecular weight antagonist of CCR5
Vierboom, Michel P. M., Zavodny, Paul J., Chou, Chuan‐Chu, Tagat, Jayaram R., Pugliese‐Sivo, Catherine, Strizki, Julie, Steensma, Ruo W., McCombie, Stuart W., Çelebi‐Paul, Liesbeth, Remarque, Ed, Jonker, Margreet, Narula, Satwant K., Hart, Bert't
Published in Arthritis and rheumatism (01.02.2005)
Published in Arthritis and rheumatism (01.02.2005)
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Muscarinic M2 antagonists: anthranilamide derivatives with exceptional selectivity and in vivo activity
CLADER, John W, BILLARD, William, LIU, Charles, MCCOMBIE, Stuart W, VICE, Susan, GOWEI ZHOU, GREENLEE, William J, BINCH, Herbert III, CHEN, Lian-Yong, CROSBY, Gordon JR, DUFFY, Ruth A, FORD, Jennifer, KOZLOWSKI, Joseph A, LACHOWICZ, Jean E, SHENGJIAN LI
Published in Bioorganic & medicinal chemistry (15.01.2004)
Published in Bioorganic & medicinal chemistry (15.01.2004)
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Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M2 muscarinic receptor antagonists via benzamide modification
BOYLE, Craig D, VICE, Susan F, COFFIN, Vicki L, COX, Kathleen A, GROTZ, Diane E, DUFFY, Ruth A, RUPERTO, Vilma, LACHOWICZ, Jean E, CAMPION, Jennifer, CHACKALAMANNIL, Samuel, LANKIN, Claire M, MCCOMBIE, Stuart W, BILLARD, William, BINCH, Herbert III, CROSBY, Gordon, WILLIAMS, Mary-Cohen
Published in Bioorganic & medicinal chemistry letters (01.12.2002)
Published in Bioorganic & medicinal chemistry letters (01.12.2002)
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Synthesis and structure-activity relationships of M2-selective muscarinic receptor ligands in the 1-[4-(4-arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family
MCCOMBIE, Stuart W, LIN, Sue-Ing, RUPERTO, Vilma B, DUFFY, Ruth A, LACHOWICZ, Jean E, TAGAT, Jayaram R, NAZARENO, Dennis, VICE, Susan, FORD, Jennifer, ASBEROM, Theodros, LEONE, Daria, KOZLOWSKI, Joseph A, GUOWEI ZHOU
Published in Bioorganic & medicinal chemistry letters (11.03.2002)
Published in Bioorganic & medicinal chemistry letters (11.03.2002)
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Metabolic stabilization of benzylidene ketal M2 muscarinic receptor antagonists via halonaphthoic acid substitution
BOYLE, Craig D, CHACKALAMANNIL, Samuel, YUGUANG WANG, GUOWEI ZHOU, BILLARD, William, BINCH, Herbert III, CROSBY, Gordon, COHEN-WILLIAMS, Mary, COFFIN, Vicki L, COX, Kathleen A, GROTZ, Diane E, DUFFY, Ruth A, CLADER, John W, RUPERTO, Vilma, LACHOWICZ, Jean E, GREENLEE, William J, JOSIEN, Hubert B, KAMINSKI, James J, KOZLOWSKI, Joseph A, MCCOMBIE, Stuart W, NAZARENO, Dennis V, TAGAT, Jayaram R
Published in Bioorganic & medicinal chemistry letters (03.09.2001)
Published in Bioorganic & medicinal chemistry letters (03.09.2001)
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Indolocarbazoles. 1. Total synthesis and protein kinase inhibiting characteristics of compounds related to K-252c
McCombie, Stuart W, Bishop, Robert W, Carr, Donna, Dobek, Emily, Kirkup, Michael P, Kirschmeier, Paul, Lin, Sue-Ing, Petrin, Joanne, Rosinski, Karen, Shankar, Bandarpalle B, Wilson, Oswald
Published in Bioorganic & medicinal chemistry letters (01.08.1993)
Published in Bioorganic & medicinal chemistry letters (01.08.1993)
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Generation and in situ acylation of enaminone anions: a convenient synthesis of 3-carbethoxy-4(1H)-pyridinones and -4-pyrones and related compounds
McCombie, Stuart W, Metz, William A, Nazareno, Dennis, Shankar, Bandarpalle B, Tagat, Jayaram
Published in Journal of organic chemistry (01.08.1991)
Published in Journal of organic chemistry (01.08.1991)
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