Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Humberto Bartolome Arzeno"'
Autor:
R. Ursula Kammlott, Deborah Carol Reuter, Teresa Alejandra Trejo-Martin, Leyi Gong, Christophe Michoud, Andreas Kuglstatter, Patricia Tran, David Michael Goldstein, Yun-Chou Tan, Parcharee Tivitmahaisoon, Linghao Niu, Shao-Yong Wu, Sue Jin, Paul Weller, Gary Hsieh, Karin Ann Stein, Humberto Bartolome Arzeno, James Patrick Dunn, Ada Shao, Wylie Solang Palmer, J. Heather Hogg, Johannes C. Hermann, Kung-ching Chang, Bindu Goyal, Alam Jahangir, Cheryl Janson, Tania Silva, Christine Lukacs, Paul J. Wagner, Muzaffar Alam
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:1486-1492
A series of amino-pyrimidines was developed based upon an initial kinase cross-screening hit from a CDK2 program. Kinase profiling and structure-based drug design guided the optimization from the initial 1,2,3-benzotriazole hit to a potent and select
Autor:
Mcintosh Joel, Andreas Kuglstatter, Paul Weller, Sarah C. Abbot, David C. Swinney, Brad Loe, Tobias Gabriel, Roland J. Billedeau, Martin Stahl, Hasim Zecic, Nidhi Arora, Eva Papp, Humberto Bartolome Arzeno, Brian Wong, Allassan Abubakari, Nolan James Dewdney, David Michael Goldstein, Man-Ling Sung, Rebecca T Suttman, Michael Soth, Jaehyeon Park, Kieran Durkin, Fujun Li, Manjiri Ghate, Kristen Lynn Mccaleb, Sandra Frauchiger, Ronald J. Hill
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:3452-3456
Learnings from previous Roche p38-selective inhibitors were applied to a new fragment hit, which was optimized to a potent, exquisitely selective preclinical lead with a good pharmacokinetic profile.
Autor:
Jaehyeon Park, Harlan F Reese, Yun-Chou Tan, Hasim Zecic, Martin Stahl, Keshab Sarma, Renee Litman, Alejandra Trejo, William Bingenheimer, Michael Soth, David Michael Goldstein, Mary Welch, Eric Brian Sjogren, Man-Ling Sung, Sandra Frauchiger, Nolan James Dewdney, Bong San Pablo, Eva Papp, Daniel McWeeney, Ronald J. Hill, Paul Weller, Manjiri Ghate, JoAnn La Fargue, Brian Wong, Stacie A. Dalrymple, James Patrick Dunn, David Mark Rotstein, Richard T. Roberts, Bradford Graves, Rebecca T Suttman, Mcintosh Joel, Farrell Robert P, Andreas Kuglstatter, Chen Jian Jeffrey, Fujun Li, Humberto Bartolome Arzeno, Brad Loe, Tobias Gabriel
Publikováno v:
Journal of Medicinal Chemistry. 54:2255-2265
The development of a new series of p38α inhibitors resulted in the identification of two clinical candidates, one of which was advanced into a phase 2 clinical study for rheumatoid arthritis. The original lead, an lck inhibitor that also potently in
Design and synthesis of orally active inhibitors of TNF synthesis as anti-rheumatoid arthritis drugs
Autor:
Xiaohong Lin, Nolan James Dewdney, Harold E. Van Wart, Jane Huang, Humberto Bartolome Arzeno, Elsie M. Eugui, Keshab Sarma, Jian Jeffrey Chen, Frances Chu, Yong Kim, Robert L. Martin, Anna Mirkovich, Keith A. M. Walker
Publikováno v:
Bioorganicmedicinal chemistry letters. 13(22)
A novel series of TNF inhibitors was identified based on the screening of existing MMP inhibitor libraries. Further SAR optimization led to the discovery of a novel lead compound. Its synthesis, efficacy in experimental animal models, and pharmacokin
Autor:
Stacie A. Dalrymple, Rick Roberts, Kyung Song, Mcintosh Joel, Jennifer L. Miller, Julie Lim, Pete William Dunten, Florentino Sanpablo, Paul Weller, Phyllis E. Whiteley, Lu Zeng, Jose Freire-Moar, Armando G. Villaseñor, Humberto Bartolome Arzeno, David Michael Goldstein, JoAnn LaFargue, Deborah Carol Reuter, Stephen D. Warren, Brett Lovejoy, Sushmita Chanda, Saunders John, Alejandra Trejo, Daniel D. Comer, Michelle F. Browner, Mary Welch, Soan Cheng, Eva Papp
Publikováno v:
Journal of medicinal chemistry. 46(22)
Inhibition of the biosynthesis of proinflammatory cytokines such as tumor necrosis factor and interleukin-1 via p38 has been an approach toward the development of a disease modifying agent for the treatment of chronic inflammation and autoimmune dise