Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Martin C. Cherrier"'
Autor:
Jerry Xu, Milton L. Hammond, Brett Lauring, James R. Tata, Philip J. Skinner, Jens Knudsen, Daniel T. Connolly, Eseng Lai, Graeme Semple, Wen-Lin Luo, M. Gerard Waters, P. Douglas Boatman, John A. Wagner, Martin C. Cherrier, Jae-Kyu Jung, Steven L. Colletti, Andrew K.P. Taggart, Ester Carballo-Jane, Ruoping Chen, Benjamin R. Johnson, Thomas O. Schrader, Josee Cote, Carleton R. Sage, Luzelena Caro, Jeremy G. Richman, Michelle Kasem, Peter J. Webb
Publikováno v:
Journal of Medicinal Chemistry. 55:3644-3666
G-protein coupled receptor (GPCR) GPR109a is a molecular target for nicotinic acid and is expressed in adipocytes, spleen, and immune cells. Nicotinic acid has long been used for the treatment of dyslipidemia due to its capacity to positively affect
Autor:
Marc Decaire, Graeme Semple, Yifeng Xiong, Andrew J. Grottick, Woo H. Yoon, Kevin Whelan, Sonja Strah-Pleynet, Martin C. Cherrier, Brett Ullman, John Frazer, Hussien A. Al-Shamma, Jin-Sun Karoline Choi, Konrad Feichtinger, Erin K. Sanabria
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1870-1873
A series of fused bicyclic heterocycles was identified as potent and selective 5-HT 2A receptor antagonists. Optimization of the series resulted in compounds that had improved PK properties, favorable CNS partitioning, good pharmacokinetic properties
Autor:
Huong T. Dang, Philip J. Skinner, Graeme Semple, Martin C. Cherrier, Peter J. Webb, Ruoping Chen, Susan Y. Tamura, Carleton R. Sage, Daniel T. Connolly, Cameron Pride, Jeremy G. Richman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:6619-6622
A series of 3-nitro-4-substituted-aminobenzoic acids were prepared and found to act as potent and highly selective agonists of the orphan human GPCR GPR109b, a low affinity receptor for niacin. No activity was observed at the closely homologous high
Autor:
Philip J. Skinner, Tawfik Gharbaoui, Vu Hong, Ruoping Chen, Graeme Semple, Huong T. Dang, Martin C. Cherrier, Jeremy G. Richman, Young-Jun Shin, Cameron Pride, Peter J. Webb, Andrew K. Lindstrom, Daniel T. Connolly, Susan Y. Tamura
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5620-5623
A series of 5-alkyl pyrazole-3-carboxylic acids were prepared and found to act as potent and selective agonists of the human GPCR, GPR109a, the high affinity nicotinic acid receptor. No activity was observed at the highly homologous low affinity niac
Autor:
Peter J. Webb, Martin C. Cherrier, Graeme Semple, Carleton R. Sage, Philip J. Skinner, Jeremy G. Richman, Ruoping Chen, Susan Y. Tamura, Daniel T. Connolly
Publikováno v:
Journal of Medicinal Chemistry. 49:1227-1230
1-Substituted benzotriazole carboxylic acids have been identified as the first reported examples of selective small-molecule agonists of the human orphan G-protein-coupled receptor GPR109b (HM74), a low-affinity receptor for the HDL-raising drug niac
Autor:
Marc Decaire, Woo H. Yoon, Sonja Strah-Pleynet, Martin C. Cherrier, Yifeng Xiong, Andrew J. Grottick, Yun Shan, Konrad Feichtinger, Jin-Sun Karoline Choi, Peter I. Dosa, Erin K. Hauser, Graeme Semple, Bradley Teegarden, Brett Ullman, Hussien A. Al-Shamma, John Frazer, Kevin Whelan
Publikováno v:
Journal of medicinal chemistry. 53(15)
Recent developments in sleep research suggest that antagonism of the serotonin 5-HT(2A) receptor may improve sleep maintenance insomnia. We herein report the discovery of a series of potent and selective serotonin 5-HT(2A) receptor antagonists based
Autor:
Philip J. Skinner, Jeremy G. Richman, Andrew K.P. Taggart, P. Douglas Boatman, Martin C. Cherrier, Graeme Semple, Carleton R. Sage, Ruoping Chen, Benjamin R. Johnson, Jae-Kyu Jung, Jerry Xu, Thomas O. Schrader, Michelle Kasem, Jens Knudsen, Ester Carballo-Jane, Peter J. Webb
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(9)
Tricyclic pyrazole tetrazoles which are potent partial agonists of the high affinity niacin receptor, GPR109a, have been discovered and optimized. One of these compounds has proven to be effective at lowering free fatty acids in vitro and in vivo.
Autor:
Philip J. Skinner, Dominic P. Behan, Ester Carballo-Jane, Carleton R. Sage, Peter J. Webb, Daniel T. Connolly, Ruoping Chen, Jeremy G. Richman, Graeme Semple, Susan Y. Tamura, Thomas O. Schrader, James R Tata, Tawfik Gharbaoui, M Gerard Waters, Steven L. Colletti, Kang Cheng, Martin C. Cherrier, Andrew K Taggart, P. Douglas Boatman, Tian-Quan Cai, Jae-Kyu Jung, Young-Jun Shin
Publikováno v:
Journal of medicinal chemistry. 51(16)
The discovery and profiling of 3-(1H-tetrazol-5-yl)-1,4,5,6-tetrahydro-cyclopentapyrazole (5a, MK-0354), a partial agonist of GPR109a, is described. Compound 5a retained the plasma free fatty acid lowering effects in mice associated with GPR109a agon
Autor:
Marc Decaire, Uy Jane, James R. Tata, Jerry Xu, Daniel T. Connolly, P. Douglas Boatman, Philip J. Skinner, Martin C. Cherrier, Nathalie Rodriguez, Peter J. Webb, Jeremy G. Richman, Susan Y. Tamura, Carleton R. Sage, Tracy Duong, Claudia Averbuj, Andrew K. Lindstrom, Benjamin R. Johnson, Ning Zou, Brian M. Smith, Tawfik Gharbaoui, Young-Jun Shin, Ruoping Chen, Thomas O. Schrader, Graeme Semple, Steven L. Colletti, Jae-Kyu Jung
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(17)
A strategy for lead identification of new agonists of GPR109a, starting from known compounds shown to activate the receptor, is described. Early compound triage led to the formulation of a binding hypothesis and eventually to our focus on a series of
Autor:
Graeme Semple, Philip J. Skinner, Tawfik Gharbaoui, Young-Jun Shin, Jae-Kyu Jung, Martin C. Cherrier, Peter J. Webb, Susan Y. Tamura, P. Douglas Boatman, Carleton R. Sage, Thomas O. Schrader, Ruoping Chen, Steven L. Colletti, James R. Tata, M. Gerard Waters, Kang Cheng, Andrew K. Taggart, Tian-Quan Cai, Ester Carballo-Jane, Dominic P. Behan
Publikováno v:
Journal of Medicinal Chemistry; Jul2008, Vol. 51 Issue 16, p5101-5108, 8p