Discovery and Structure−Activity Relationship of (1R)-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a Selective Serotonin 5-HT2C Receptor Agonist for the Treatment of Obesity
Smith, Brian M, Smith, Jeffrey M, Tsai, James H, Schultz, Jeffrey A, Gilson, Charles A, Estrada, Scott A, Chen, Rita R, Park, Douglas M, Prieto, Emily B, Gallardo, Charlemagne S, Sengupta, Dipanjan, Dosa, Peter I, Covel, Jon A, Ren, Albert, Webb, Robert R, Beeley, Nigel R. A, Martin, Michael, Morgan, Michael, Espitia, Stephen, Saldana, Hazel R, Bjenning, Christina, Whelan, Kevin T, Grottick, Andrew J, Menzaghi, Frederique, Thomsen, William J
Published in Journal of Medicinal Chemistry (24.01.2008)
Published in Journal of Medicinal Chemistry (24.01.2008)
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Journal Article
Discovery and SAR of new benzazepines as potent and selective 5-HT2C receptor agonists for the treatment of obesity
SMITH, Brian M, SMITH, Jeffrey M, DIPANJAN SENGUPTA, THOMSEN, William J, SALDANA, Hazel R, WHELAN, Kevin T, MENZAGHI, Frederique, WEBB, Robert R, BEELEY, Nigel R. A, TSAI, James H, SCHULTZ, Jeffrey A, GILSON, Charles A, ESTRADA, Scott A, CHEN, Rita R, PARK, Douglas M, PRIETO, Emily B, GALLARDO, Charlemagne S
Published in Bioorganic & Medicinal Chemistry Letters (01.03.2005)
Published in Bioorganic & Medicinal Chemistry Letters (01.03.2005)
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Journal Article
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., 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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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
Discovery and SAR of new benzazepines as potent and selective 5-HT 2C receptor agonists for the treatment of obesity
Smith, Brian M., Smith, Jeffrey M., Tsai, James H., Schultz, Jeffrey A., Gilson, Charles A., Estrada, Scott A., Chen, Rita R., Park, Douglas M., Prieto, Emily B., Gallardo, Charlemagne S., Sengupta, Dipanjan, Thomsen, William J., Saldana, Hazel R., Whelan, Kevin T., Menzaghi, Frederique, Webb, Robert R., Beeley, Nigel R.A.
Published in Bioorganic & medicinal chemistry letters (01.03.2005)
Published in Bioorganic & medicinal chemistry letters (01.03.2005)
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Journal Article
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
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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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., 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
Discovery and Structure-Activity Relationship of (1R)-8-Chloro-2,3,4,5-tetrahydro-l-methyl-1H-3-benzazepine (Lorcaserin), a Selective Serotonin 5-HT2C Receptor Agonist for the Treatment of Obesity
SMITH, Brian M, SMITH, Jeffrey M, SENGUPTA, Dipanjan, DOSA, Peter I, COVEL, Jon A, REN, Albert, WEBB, Robert R, BEELEY, Nigel R. A, MARTIN, Michael, MORGAN, Michael, ESPITIA, Stephen, SALDANA, Hazel R, TSAI, James H, BJENNING, Christina, WHELAN, Kevin T, GROTTICK, Andrew J, MENZAGHI, Frederique, THOMSEN, William J, SCHULTZ, Jeffrey A, GILSON, Charles A, ESTRADA, Scott A, CHEN, Rita R, PARK, Douglas M, PRIETO, Emily B, GALLARDO, Charlemagne S
Published in Journal of medicinal chemistry (2008)
Get full text
Published in Journal of medicinal chemistry (2008)
Journal Article
Discovery and Structure−Activity Relationship of (1 R )-8-Chloro-2,3,4,5-tetrahydro-1-methyl-1 H -3-benzazepine (Lorcaserin), a Selective Serotonin 5-HT 2C Receptor Agonist for the Treatment of Obesity
Smith, Brian M., Smith, Jeffrey M., Tsai, James H., Schultz, Jeffrey A., Gilson, Charles A., Estrada, Scott A., Chen, Rita R., Park, Douglas M., Prieto, Emily B., Gallardo, Charlemagne S., Sengupta, Dipanjan, Dosa, Peter I., Covel, Jon A., Ren, Albert, Webb, Robert R., Beeley, Nigel R. A., Martin, Michael, Morgan, Michael, Espitia, Stephen, Saldana, Hazel R., Bjenning, Christina, Whelan, Kevin T., Grottick, Andrew J., Menzaghi, Frederique, Thomsen, William J.
Published in Journal of medicinal chemistry (01.01.2008)
Published in Journal of medicinal chemistry (01.01.2008)
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Journal Article
COMPUESTOS DERIVADOS DE BIFENILSULFONILOS Y FENIL HETEROARIL SULFONILOS, MODULADORES DEL RECEPTOR H3 DE HISTAMINA; COMPOSICION FARMACEUTICA; PROCESO DE PREPARACION; Y USO PARA EL TRATAMIENTO DE TRASTORNOS TALES COMO EPILEPSIA, DEPRESION, OBESIDAD, TR
SANTORA, VINCENT J.; HART, RYAN M.; IBARRA, JASONB.; PARK, DOUGLAS M.; REN, ALBERT S.; SEMPLE, GRAEME; SCHULTZ, JEFFREY
Year of Publication 06.06.2008
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Year of Publication 06.06.2008
Patent
Discovery and SAR of new benzazepines as potent and selective 5-HT(2C) receptor agonists for the treatment of obesity
Smith, Brian M, Smith, Jeffrey M, Tsai, James H, Schultz, Jeffrey A, Gilson, Charles A, Estrada, Scott A, Chen, Rita R, Park, Douglas M, Prieto, Emily B, Gallardo, Charlemagne S, Sengupta, Dipanjan, Thomsen, William J, Saldana, Hazel R, Whelan, Kevin T, Menzaghi, Frederique, Webb, Robert R, Beeley, Nigel R A
Published in Bioorganic & medicinal chemistry letters (01.03.2005)
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Published in Bioorganic & medicinal chemistry letters (01.03.2005)
Journal Article
BIPHENYL-SULFONYL- UND PHENYL-HETEROARYL-SULFONYL-MODULATOREN DES HISTAMIN-H3-REZEPTORS ZUR BEHANDLUNG VON DAMIT VERBUNDENEN ERKRANKUNGEN
SMITH, BRIAN, SANTORA, VINCENT J, PARK, DOUGLAS M, SCHULTZ, JEFFREY A, SEMPLE, GRAEME, HART, RYAN M, REN, ALBERT S, SMITH, JEFFREY, IBARRA, JASON B
Year of Publication 15.07.2011
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Year of Publication 15.07.2011
Patent
BIPHENYL SULFONYL AND PHENYL-HETEROARYL SULFONYL MODULATORS OF THE HISTAMINE H3-RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
SMITH, BRIAN, SANTORA, VINCENT J, PARK, DOUGLAS M, SCHULTZ, JEFFREY A, SEMPLE, GRAEME, HART, RYAN M, REN, ALBERT S, SMITH, JEFFREY, IBARRA, JASON B
Year of Publication 15.06.2011
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Year of Publication 15.06.2011
Patent
BIPHENYL SULFONYL AND PHENYL-HETEROARYL SULFONYL MODULATORS OF THE HISTAMINE H3-RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
HART RYAN M, SCHULTZ JEFFREY A, REN ALBERT S, SMITH BRIAN M, IBARRA JASON B, SMITH JEFFREY, SANTORA VINCENT J, PARK DOUGLAS M, SEMPLE GRAEME
Year of Publication 23.09.2010
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Year of Publication 23.09.2010
Patent
Biphenyl sulfonyl and phenyl-heteroaryl sulfonyl modulators of the histamine H3-receptor useful for the treatment of disorders related thereto
SMITH, BRIAN, SANTORA, VINCENT J, PARK, DOUGLAS M, SCHULTZ, JEFFREY A, SEMPLE, GRAEME, HART, RYAN M, REN, ALBERT S, SMITH, JEFFREY, IBARRA, JASON B
Year of Publication 31.03.2010
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Year of Publication 31.03.2010
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BIPHENYL SULFONYL AND PHENYL-HETEROARYL SULFONYL MODULATORS OF THE HISTAMINE H3-RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
SMITH, BRIAN, SANTORA, VINCENT J, PARK, DOUGLAS M, SCHULTZ, JEFFREY A, SEMPLE, GRAEME, HART, RYAN M, REN, ALBERT S, SMITH, JEFFREY, IBARRA, JASON B
Year of Publication 01.07.2009
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Year of Publication 01.07.2009
Patent
BIPHENYL SULFONYL AND PHENYL-HETEROARYL SULFONYL MODULATORS OF THE HISTAMINE H3-RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
SMITH BRIAN, HART RYAN M, SCHULTZ JEFFREY A, REN ALBERT S, IBARRA JASON B, SMITH JEFFREY, SANTORA VINCENT J, PARK DOUGLAS M, SEMPLE GRAEME
Year of Publication 30.06.2009
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Year of Publication 30.06.2009
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BIFENILSULFONILOS Y FENIL HETEROARIL SULFONILOS COMO MODULADORES DEL RECEPTOR H3 DE HISTAMINA UTILES PARA EL TRATAMIENTO DE LOS TRASTORNOS RELACIONADOS CON DICHO RECEPTOR
JEFFREY SMITH, GRAEME SEMPLE, DOUGLAS M. PARK, BRIAN SMITH, JEFFREY A. SCHULTZ, ALBERT S. REN, VINCENT J. SANTORA, JASON B. IBARRA, RYAN M. HART
Year of Publication 31.03.2009
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Year of Publication 31.03.2009
Patent