Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Khawja A. Usmani"'
Autor:
Khawja A. Usmani, Dawei Yue, Zhi-Liang Chu, Abu J.M. Sadeque, Chris Carroll, Chuan Chen, Hsin-Hui Shu, Sanju Narayanan, Hussein Al-Sharmma, Dominic P. Behan, Robert M. Jones, Graeme Semple, James N. Leonard, David J. Unett, Daniel J. Buzard, Michael Morgan, Juerg Lehmann, Imelda Calderon, Shiu-Feng Tung, Woo Hyun Yoon, Xiuwen Zhu, Sangdon Han, Andrew M. Kawasaki, Amy Siu-Ting Wong, Sun Hee Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:3034-3038
The design and optimization of a novel trans-1,4-dioxycyclohexane GPR119 agonist series is described. A lead compound 21 was found to be a potent and efficacious GPR119 agonist across species, and possessed overall favorable pharmaceutical properties
Autor:
Hussien A. Al-Shamma, Michael Morgan, Ibragim Gaidarov, Huong T. Dang, Joel Gatlin, Marc Decaire, David J. Unett, Karoline Choi, Jeff Edwards, Dawei Yue, Abu J.M. Sadeque, Kevin Whelan, Yifeng Xiong, Lixia Fu, Jayant Thatte, Graeme Semple, Sonja Strah-Pleynet, Sangdon Han, Michelle Solomon, Dominic P. Behan, Jae-Kyu Jung, Sanju Narayanan, Lars Thoresen, Robert M. Jones, Chuan Chen, Xiuwen Zhu, Khawja A. Usmani, Cameron Pride, Ruoping Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:322-326
The design and synthesis of novel 1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalen-4-carboxamide CB2 selective ligands for the potential treatment of pain is described. Compound (R,R)-25 has good balance between CB2 agonist potency and selecti
Autor:
Ben Johnson, Tawfik Gharbaoui, Moody Jeanne, David J. Unett, Kevin Whelan, Ibragim Gaidarov, Michael Morgan, Lars Thoresen, Michelle Kasem, Abu J.M. Sadeque, Robert M. Jones, Chuan Chen, Sun Hee Kim, Hussien A. Al-Shamma, Minh Le, Joel Gatlin, Lorene Calvano, Andrew M. Kawasaki, Lixia Fu, Yinghong Gao, Scott Stirn, Weichao Chen, Jeremy Barden, Dominic P. Behan, Krishnan Ashwin M, Xiuwen Zhu, Graeme Semple, Dipanjan Sengupta, Christopher Ronald J, Jeff Edwards, Luis Lopez, Jayant Thatte, Daniel J. Buzard, Anthony C. Blackburn, Michelle Solomon, Todd Anthony, Thomas O. Schrader, Khawja A. Usmani
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1334-1339
S1P1 is a validated target for treatment of autoimmune disease, and functional antagonists with superior safety and pharmacokinetic properties are being sought as second generation therapeutics. We describe the discovery and optimization of (7-benzyl
Autor:
Weichao Chen, Andrew M. Kawasaki, Dominic P. Behan, Jeff Edwards, You-An Ma, Tawfik Gharbaoui, Sun Hee Kim, Jayant Thatte, Hussien A. Al-Shamma, Carleton R. Sage, Jeremy Barden, Anthony C. Blackburn, Michelle Solomon, Xiuwen Zhu, Christopher Ronald J, David Mills, Ibragim Gaidarov, Antonio Garrido Montalban, Sangdon Han, Luis Lopez, Dipanjan Sengupta, Michael Morgan, Juerg Lehmann, Daniel J. Buzard, Graeme Semple, Kevin Whelan, Yinghong Gao, Joel Gatlin, Moody Jeanne, David J. Unett, Imelda Calderon, Lars Thoresen, Robert M. Jones, Brett Ullman, Todd Anthony, Chuan Chen, Minh Le, Khawja A. Usmani, Scott Stirn, Jaimie Karyn Rueter, Lixia Fu, Lorene Calvano, Abu J.M. Sadeque
Publikováno v:
ACS Medicinal Chemistry Letters. 5:1313-1317
APD334 was discovered as part of our internal effort to identify potent, centrally available, functional antagonists of the S1P1 receptor for use as next generation therapeutics for treating multiple sclerosis (MS) and other autoimmune diseases. APD3
Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease
Autor:
Joel Gatlin, Kevin Whelan, Michael Morgan, Juerg Lehmann, Lixia Fu, Yinghong Gao, Moody Jeanne, Minh Le, Hussien A. Al-Shamma, Jeremy Barden, Khawja A. Usmani, Jeff Edwards, Chuan Chen, Jayant Thatte, Dipanjan Sengupta, Xiuwen Zhu, Abu J.M. Sadeque, Imelda Calderon, Michelle Solomon, Lars Thoresen, Tawfik Gharbaoui, Robert M. Jones, Ling Liu, Luis Lopez, Daniel J. Buzard, Brett Ullman, Krishnan Ashwin M, Sheryll Espinola, Charles Xing, Sangdon Han, Andrew M. Kawasaki
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:4404-4409
Two series of fused tricyclic indoles were identified as potent and selective S1P(1) agonists. In vivo these agonists produced a significant reduction in circulating lymphocytes which translated into robust efficacy in several rodent models of autoim
Autor:
Weichao G. Chen, Khawja A. Usmani, Chuan Chen, Safet Palamar, Abu J.M. Sadeque, Matthew A. Cerny
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 44(4)
Lorcaserin [(R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine] hydrochloride hemihydrate, a selective serotonin 5-hydroxytryptamine (5-HT) 5-HT(2C) receptor agonist, is approved by the U.S. Food and Drug Administration for chronic weight mana
Publikováno v:
Drug Metabolism and Disposition. 34:1606-1614
Cytochromes P450 (P450s) are major catalysts in the metabolism of xenobiotics and endogenous substrates such as estradiol (E2). It has previously been shown that E2 is predominantly metabolized in humans by CYP1A2 and CYP3A4 with 2-hydroxyestradiol (
Autor:
Khawja A. Usmani, Peter W. Shearer
Publikováno v:
Pest Management Science. 57:822-826
During the development of a resistance-monitoring bioassay that uses males as the life-stage tested, the relationship of adult female and male susceptibility of Grapholita molesta to different classes of insecticides was investigated. Preliminary res
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 40(4)
Lorcaserin, a selective serotonin 5-hydroxytryptamine 2C receptor agonist, is being developed for weight management. The oxidative metabolism of lorcaserin, mediated by recombinant human cytochrome P450 (P450) and flavin-containing monooxygenase (FMO
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 40(4)
Lorcaserin, a selective serotonin 5-HT(2C) receptor agonist, is a weight management agent in clinical development. Lorcaserin N-carbamoyl glucuronidation governs the predominant excretory pathway of lorcaserin in humans. Human UDP-glucuronosyltransfe