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Preladenant, a selective A2A receptor antagonist, is active in primate models of movement disorders

Preladenant, a selective A2A receptor antagonist, is active in primate models of movement disorders

by HODGSON, Robert A, BEDARD, Paul J, DARE, Aurelie, NEUSTADT, Bernard R, STAMFORD, Andrew W, HUNTER, John C, VARTY, Geoffrey B, KAZDOBA, Tatiana M, DI PAOLO, Therese, GRZELAK, Michael E, POND, Annamarie J, HADJTAHAR, Abdallah, BELANGER, Nancy, GREGOIRE, Laurent
Published in Experimental neurology (01.10.2010)

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Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders

Preladenant, a selective A(2A) receptor antagonist, is active in primate models of movement disorders

by Hodgson, Robert A, Bedard, Paul J, Varty, Geoffrey B, Kazdoba, Tatiana M, Di Paolo, Therese, Grzelak, Michael E, Pond, Annamarie J, Hadjtahar, Abdallah, Belanger, Nancy, Gregoire, Laurent, Dare, Aurelie, Neustadt, Bernard R, Stamford, Andrew W, Hunter, John C
Published in Experimental neurology (01.10.2010)

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Potent, selective, and orally active adenosine A2A receptor antagonists : Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1 ,5-c]pyrimidines

Potent, selective, and orally active adenosine A2A receptor antagonists : Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1 ,5-c]pyrimidines

by NEUSTADT, Bernard R, JINSONG HAO, FOSTER, Carolyn, ARIK, Leyla, LACHOWICZ, Jean, NG, Kwokei, FENG, Kung-I, LINDO, Neil, GREENLEE, William J, STAMFORD, Andrew W, TULSHIAN, Deen, ONGINI, Ennio, HUNTER, John, MONOPOLI, Angela, BERTORELLI, Rosalia
Published in Bioorganic & medicinal chemistry letters (01.03.2007)

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Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes

Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes

by Xia, Yan, Chackalamannil, Samuel, Greenlee, William J., Jayne, Charles, Neustadt, Bernard, Stamford, Andrew, Vaccaro, Henry, Xu, Xiaoying (Lucy), Baker, Hana, O’Neill, Kim, Woods, Morgan, Hawes, Brian, Kowalski, Tim
Published in Bioorganic & medicinal chemistry letters (01.06.2011)

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Potent and selective adenosine A₂A receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones

Potent and selective adenosine A₂A receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones

by Harris, Joel M, Neustadt, Bernard R, Zhang, Hongtao, Lachowicz, Jean, Cohen-Williams, Mary, Varty, Geoff, Hao, Jinsong, Stamford, Andrew W
Published in Bioorganic & medicinal chemistry letters (15.04.2011)

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Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones

Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones

by Harris, Joel M, Neustadt, Bernard R, Zhang, Hongtao, Lachowicz, Jean, Cohen-Williams, Mary, Varty, Geoff, Hao, Jinsong, Stamford, Andrew W
Published in Bioorganic & medicinal chemistry letters (15.04.2011)

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Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines

Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines

by Neustadt, Bernard R, Liu, Hong, Hao, Jinsong, Greenlee, William J, Stamford, Andrew W, Foster, Carolyn, Arik, Leyla, Lachowicz, Jean, Zhang, Hongtao, Bertorelli, Rosalia, Fredduzzi, Silva, Varty, Geoffrey, Cohen-Williams, Mary, Ng, Kwokei
Published in Bioorganic & medicinal chemistry letters (01.02.2009)

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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

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

by 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)

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Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists

Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists

by Shah, Unmesh, Lankin, Claire M, Boyle, Craig D, Chackalamannil, Samuel, Greenlee, William J, Neustadt, Bernard R, Cohen-Williams, Mary E, Higgins, Guy A, Ng, Kwokei, Varty, Geoffrey B, Zhang, Hongtao, Lachowicz, Jean E
Published in Bioorganic & medicinal chemistry letters (15.07.2008)

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Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists

Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists

by SHAH, Unmesh, BOYLE, Craig D, SHIYONG WANG, MONOPOLI, Angela, LACHOWICZ, Jean E, CHACKALAMANNIL, Samuel, NEUSTADT, Bernard R, LINDO, Neil, GREENLEE, William J, FOSTER, Carolyn, ARIK, Leyla, YING ZHAI, NG, Kwokei
Published in Bioorganic & medicinal chemistry letters (15.07.2008)

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Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides

Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides

by 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)

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Potent and selective adenosine A2A receptor antagonists : 1,2,4-Triazolo[1,5-c]pyrimidines

Potent and selective adenosine A2A receptor antagonists : 1,2,4-Triazolo[1,5-c]pyrimidines

by NEUSTADT, Bernard R, HONG LIU, FREDDUZZI, Silva, VARTY, Geoffrey, COHEN-WILLIAMS, Mary, NGA, Kwokei, JINSONG HAO, GREENLEE, William J, STAMFORD, Andrew W, FOSTER, Carolyn, ARIK, Leyla, LACHOWICZ, Jean, HONGTAO ZHANG, BERTORELLI, Rosalia
Published in Bioorganic & medicinal chemistry letters (01.02.2009)

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Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists

Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists

by SHAH, Unmesh, LANKIN, Claire M, HONGTAO ZHANG, LACHOWICZ, Jean E, BOYLE, Craig D, CHACKALAMANNIL, Samuel, GREENLEE, William J, NEUSTADT, Bernard R, COHEN-WILLIAMS, Mary E, HIGGINS, Guy A, NG, Kwokei, VARTY, Geoffrey B
Published in Bioorganic & medicinal chemistry letters (01.07.2008)

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Discovery of the oxazabicyclo[3.3.1]nonane derivatives as potent and orally active GPR119 agonists

Discovery of the oxazabicyclo[3.3.1]nonane derivatives as potent and orally active GPR119 agonists

by Dai, Xing, Stamford, Andrew, Liu, Hong, Neustadt, Bernard, Hao, Jingsong, Kowalski, Tim, Hawes, Brian, Xu, Xiaoying, Baker, Hana, O’Neill, Kim, Woods, Morgan, Tang, Huadong, Greenlee, William
Published in Bioorganic & medicinal chemistry letters (15.11.2015)

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Discovery of MK-8282 as a Potent G‑Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes

Discovery of MK-8282 as a Potent G‑Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes

by Neelamkavil, Santhosh F, Stamford, Andrew W, Kowalski, Timothy, Biswas, Dipshikha, Boyle, Craig, Chackalamannil, Samuel, Xia, Yan, Jayne, Charles, Neustadt, Bernard, Hao, Jinsong, Liu, Hong, Dai, Xing, Baker, Hana, Hawes, Brian, O’Neill, Kim, Tang, Huadong, Greenlee, William J
Published in ACS medicinal chemistry letters (10.05.2018)

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Synthesis and pharmacological activity of angiotensin-converting enzyme inhibitors: N-(mercaptoacyl)-4-substituted-(S)-prolines

Synthesis and pharmacological activity of angiotensin-converting enzyme inhibitors: N-(mercaptoacyl)-4-substituted-(S)-prolines

by Smith, Elizabeth M, Swiss, Gerald F, Neustadt, Bernard R, Gold, Elijah H, Sommer, Jane A, Brown, Arthur D, Chiu, Peter J. S, Moran, Rosa, Sybertz, Edmund J, Baum, Thomas
Published in Journal of medicinal chemistry (01.04.1988)

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Potent and selective adenosine A sub(2A receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones)

Potent and selective adenosine A sub(2A receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones)

by Harris, Joel M, Neustadt, Bernard R, Zhang, Hongtao, Lachowicz, Jean, Cohen-Williams, Mary, Varty, Geoff, Hao, Jinsong, Stamford, Andrew W
Published in Bioorganic & medicinal chemistry letters (15.04.2011)

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Potent and selective adenosine A 2A receptor antagonists: [1,2,4]-triazolo[4,3- c]pyrimidin-3-ones

Potent and selective adenosine A 2A receptor antagonists: [1,2,4]-triazolo[4,3- c]pyrimidin-3-ones

by Harris, Joel M., Neustadt, Bernard R., Zhang, Hongtao, Lachowicz, Jean, Cohen-Williams, Mary, Varty, Geoff, Hao, Jinsong, Stamford, Andrew W.
Published in Bioorganic & medicinal chemistry letters (2011)

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Mercaptoacyl aminoacid inhibitors of atriopeptidase. 1. Structure-activity relationship studies of methionine and S-alkylcysteine derivatives

Mercaptoacyl aminoacid inhibitors of atriopeptidase. 1. Structure-activity relationship studies of methionine and S-alkylcysteine derivatives

by Neustadt, Bernard R, Smith, Elizabeth M, Nechuta, Terry L, Bronnenkant, Alan A, Haslanger, Martin F, Watkins, Robert W, Foster, Caroline J, Sybertz, Edmund J
Published in Journal of medicinal chemistry (01.07.1994)

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Angiotensin converting enzyme inhibitors: spirapril and related compounds

Angiotensin converting enzyme inhibitors: spirapril and related compounds

by Smith, Elizabeth M, Swiss, Gerald F, Neustadt, Bernard R, McNamara, Paul, Gold, Elijah H, Sybertz, Edmund J, Baum, Thomas
Published in Journal of medicinal chemistry (01.07.1989)

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