Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Sandra A. Filla"'
Autor:
Junliang Hao, James Beck, Xin Zhou, Gregory L. Lackner, Richard Johnston, Matt Reinhard, Paul Goldsmith, Sean Hollinshead, Veronique Dehlinger, Sandra A. Filla, Xu-shan Wang, Jeffery Richardson, Maria Posada, Mike Mohutsky, Doug Schober, Jason S. Katner, Qi Chen, Bingjie Hu, David M. Remick, David A. Coates, Brian M. Mathes, Mai K. Hawk, Kjell A. Svensson, Erik Hembre
Publikováno v:
Journal of Medicinal Chemistry. 65:3786-3797
Results from recently completed clinical studies suggest the dopamine D1 receptor positive allosteric modulator (PAM) mevidalen (
Autor:
Yao-Chang Xu, Brian Michael Mathes, John Mehnert Schaus, Qi Chen, Maria-Jesus Blanco, Suzanne E. Nutter, David L. Nelson, Deanna Piatt Zacherl, Sidney Xi Liang, Sandra Ann Filla, Wendy H. Gough, Cohen Michael Philip, Kevin John Hudziak, Bai-Ping Ying, Deyi Zhang, Joseph H. Krushinski, Daniel Timothy Kohlman, Frantz Victor, David B. Wainscott
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:4337-4341
Preclinical experiments and clinical observations suggest the potential effectiveness of selective 5-HT1F receptor agonists in migraine. Identifying compounds with enhanced selectivity is crucial to assess its therapeutic value. Replacement of the in
Autor:
Brian M. Arnold, Miriam del Prado, Smriti Iyengar, Edward L. Mattiuz, Zhipei Wu, Mark A. Winter, David Bleakman, Ken H. Ho, Ann Marie L. Ogden, Paul L. Ornstein, Carrie K. Jones, Sandra Ann Filla, Brian Michael Mathes, Michael Gregory Bell, Douglas Richard Stack, Ana Maria Escribano, Thomas J. Bleisch, Ana I. Mateo, Kevin John Hudziak, Andrew Alt, Rosa Maria A. Simmons, Harlan E. Shannon, Robert E. Stratford, Jose A. Martinez-Perez, Esteban Dominguez, Ana M. Castaño
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6459-6462
The synthesis and structure-activity relationship of decahydroisoquinoline derivatives with various benzoic acid substitutions as GluK1 antagonists are described. Potent and selective antagonists were selected for a tailored prodrug approach in order
Autor:
Gustavo Pascual, Smriti Iyengar, Gregory A. Stephenson, Laura J. Martin, Sandra Ann Filla, Craig E. Thomas, Susan K. Hemrick-Luecke, Kirk W. Johnson, Jikesh Arvind Shah, Eric George Tromiczak, Magnus Wilhelm Walter, Karsten Fynboe, Lance Allen Pfeifer, Mark A. Muhlhauser, Juan A. Rincón, Nicolas Dreyfus, Chunjin Ding, Jia Shaojuan, María Luz de la Puente, Beverly A. Heinz, Lee A. Phebus, Michael P. Johnson, Simon James Richards, Thomas J. Perun, Michael J. McCoy, Pilar Lopez, Hamideh Zarrinmayeh, Thierry Masquelin, Rosa Maria A. Simmons, Douglas Linn Gernert, Oscar de Frutos, Elizabeth M. Joshi, Denise Morrow, Wayne W. Weber, Anette M. Johansson, Linda K. Thompson, Eric P. Seest, Valentina O. Badescu, Javier Mendiola, Jason K. Myers, Patrick L. Love
Publikováno v:
ACS Medicinal Chemistry Letters. 4:560-564
The objective of the described research effort was to identify a novel serotonin and norepinephrine reuptake inhibitor (SNRI) with improved norepinephrine transporter activity and acceptable metabolic stability and exhibiting minimal drug-drug intera
Autor:
Deyi, Zhang, Maria-Jesus, Blanco, Bai-Ping, Ying, Daniel, Kohlman, Sidney X, Liang, Frantz, Victor, Qi, Chen, Joseph, Krushinski, Sandra A, Filla, Kevin J, Hudziak, Brian M, Mathes, Michael P, Cohen, DeAnna, Zacherl, David L G, Nelson, David B, Wainscott, Suzanne E, Nutter, Wendy H, Gough, John M, Schaus, Yao-Chang, Xu
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(19)
Preclinical experiments and clinical observations suggest the potential effectiveness of selective 5-HT1F receptor agonists in migraine. Identifying compounds with enhanced selectivity is crucial to assess its therapeutic value. Replacement of the in
Autor:
Edward L. Mattiuz, Ann Marie L. Ogden, Ana M. Castaño, Zhipei Wu, Robert E. Stratford, E. Dominguez, Thomas J. Bleisch, Brian Michael Mathes, Brian M. Arnold, David Bleakman, Smriti Iyengar, Rosa Maria A. Simmons, Harlan E. Shannon, Sandra Ann Filla, Jose A. Martinez-Perez, Douglas Richard Stack, Ana I. Mateo, Miriam del Prado, Kevin John Hudziak, Andrew Alt, Michael Gregory Bell, Carrie K. Jones, Paul L. Ornstein, Jennifer L. Buckmaster, Ana Maria Escribano, Mark A. Winter, Ken H. Ho
Publikováno v:
Journal of Medicinal Chemistry. 48:4200-4203
Amino acids 5 and 7, two potent and selective competitive GluR5 KA receptor antagonists, exhibited high GluR5 receptor affinity over other glutamate receptors. Their ester prodrugs 6 and 8 were orally active in three models of pain: reversal of forma
Autor:
David B. Wainscott, John Mehnert Schaus, Wendy H. Gough, Yao-Chang Xu, Brian Michael Mathes, John M. Zgombick, Sandra Ann Filla, David L. Nelson, Suzanne E. Nutter, Kevin John Hudziak, Theresa Branchek
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:167-170
Synthesis and evaluation of a series of 2,3,5- and 3,5-substituted furo[3,2- b ]pyridines were undertaken in order to investigate their utility as bioisosteres of 5-HT 1F receptor agonist indole analogues, 1 – 3 . The replacement proved to be effec
Autor:
John Mehnert Schaus, Lee A. Phebus, John M. Zgombick, David B. Wainscott, Kirk W. Johnson, Kathryn W. Schenck, Brian Michael Mathes, Marlene L. Cohen, David L. Nelson, Jon A. Erickson, Sandra Ann Filla, Theresa A Branchek
Publikováno v:
Journal of Medicinal Chemistry. 46:3060-3071
Compound 1a (LY334370), a selective 5-HT(1F) receptor agonist (SSOFRA), inhibited dural inflammation in the neurogenic plasma protein extravasation model of migraine and demonstrated clinical efficacy for the acute treatment of migraine. Although 1a
Autor:
Ken H. Ho, Edward L. Mattiuz, Ann Marie L. Ogden, Brian Michael Mathes, Ana I. Mateo, David Bleakman, Kevin John Hudziak, Donna K. Dieckman, Sandra Ann Filla, Mark A. Winter, Thomas J. Bleisch, Ana Maria Escribano, Paul L. Ornstein, Kirk W. Johnson, Douglas Richard Stack, Amy Clemens-Smith, Miriam del Prado, Ana M. Castaño, Mary A. Katofiasc, Robert E. Stratford, E. Dominguez, Michael Gregory Bell, Lee A. Phebus, Jose A. Martinez-Perez
Publikováno v:
Journal of Medicinal Chemistry. 45:4383-4386
Amino diacid 3, a highly selective competitive GluR5 kainate receptor antagonist, exhibited high GluR5 receptor affinity and selectivity over other glutamate receptors. Its diethyl ester prodrug 4 was orally active in two models of migraine: the neur
Publikováno v:
Tetrahedron Letters. 40:5449-5453
The C1C8 and C9C24 fragments of (−)-discodermolide, the antipode of the marine natural product (+)-discodermolide, have been synthesized with excellent stereoselectivities. These syntheses feature the utilization of the isoxazolidine-mediated