Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Frank M. Nedza"'
Autor:
Jason Boer, William Frietze, Andrew P. Combs, Jack G. Shi, Frank M Nedza, Ruth Young-Sciame, Swamy Yeleswaram, Sharon Diamond, Fiona Lee, Kevin Bowman, Laurine G. Galya, Xiaoqing Yang
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 44(10)
Epacadostat (EPA, INCB024360) is a first-in-class, orally active, investigational drug targeting the enzyme indoleamine 2,3-dioxygenase 1 (IDO1). In Phase I studies, EPA has demonstrated promising clinical activity when used in combination with check
Autor:
Rama Y. Chandrasekaran, Jiri Aubrecht, Frederick R. Nelson, Linda A. Chatman, Hans Rollema, Frank M. Nedza, John M. Marcek, Philip A. Iredale, Jennifer B. Munzner, Betty Pettersen, Raggon Jeffrey W, David M. Rubitski, Julie Cianfrogna, Larry C. James, Karen W. Cook, Michael J. Banker, Diane F. Wong, Anne W. Schmidt, Michael Homiski, Howard Harry R, Daniel J. Lettiere, Butler Todd W, Scot Richard Mente, Jody Freeman, Travis T. Wager, Douglas K. Spracklin
Publikováno v:
Journal of Medicinal Chemistry. 54:7602-7620
The discovery of two histamine H3 antagonist clinical candidates is disclosed. The pathway to identification of the two clinical candidates, 6 (PF-03654746) and 7 (PF-03654764) required five hypothesis driven design cycles. The key to success in iden
Autor:
Matthew W. Miller, F. Fátima Matos, Frank M. Nedza, Yvette E. Savoy, Hans Rollema, Douglas K. Spracklin, Mark H. Hawthorn, Eva Hajos-Korcsok, Michael A. Ashton
Publikováno v:
Schizophrenia Bulletin. 36:410-418
Atypical antipsychotic treatment has been associated with serious metabolic adverse events, such as glucose dysregulation and development of type 2 diabetes. As part of our studies on possible underlying mechanisms, we investigated the acute effects
Autor:
Hans Rollema, Philip A. Iredale, Karen M. Ward, Anne W. Schmidt, Frank M. Nedza, Godek Dennis M, David E. Johnson, Douglas K. Spracklin
Publikováno v:
European Journal of Pharmacology. 506:209-219
Olanzapine and clozapine produce robust increases in hippocampal acetylcholine release during acetylcholinesterase inhibition, while other antipsychotics, including thioridazine, have only small effects. Since thioridazine binds with similar high aff
Autor:
Travis T, Wager, Betty A, Pettersen, Anne W, Schmidt, Douglas K, Spracklin, Scot, Mente, Todd W, Butler, Harry, Howard, Daniel J, Lettiere, David M, Rubitski, Diane F, Wong, Frank M, Nedza, Frederick R, Nelson, Hans, Rollema, Jeffrey W, Raggon, Jiri, Aubrecht, Jody K, Freeman, John M, Marcek, Julie, Cianfrogna, Karen W, Cook, Larry C, James, Linda A, Chatman, Philip A, Iredale, Michael J, Banker, Michael L, Homiski, Jennifer B, Munzner, Rama Y, Chandrasekaran
Publikováno v:
Journal of medicinal chemistry. 54(21)
The discovery of two histamine H(3) antagonist clinical candidates is disclosed. The pathway to identification of the two clinical candidates, 6 (PF-03654746) and 7 (PF-03654764) required five hypothesis driven design cycles. The key to success in id
Autor:
William V. Williams, Adam Shilling, Argyrios G. Arvanitis, Sharon Diamond, James D. Rodgers, Laurine G. Galya, Tai-Yuen Yue, Thomas Emm, Swamy Yeleswaram, Edward G. McKeever, Stacey Shepard, Mei Li, Frank M. Nedza, Naresh Punwani
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 38(11)
The metabolism, excretion, and pharmacokinetics of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile (INCB018424), a potent, selective inhibitor of Janus tyrosine kinase1/2 and the first investigational drug of its c
Autor:
Alka Shrikhande, Eric P. Arnold, Lorraine A. Lebel, Langu Peng, Frank M. Nedza, Brian T. O’Neill, Douglas K. Spracklin, Robert J. Mather, Steven B. Sands, Christopher J. O’Donnell
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(16)
The synthesis and SAR studies about the bicyclic amine, carbamate linker and aromatic ring of a 1,4-diazabicyclo[3.2.2]nonane phenyl carbamate series of alpha7 nAChR agonists is described. The development of the medicinal chemistry strategy and SAR w
Autor:
Douglas K. Spracklin, Frederick R. Nelson, Jennifer L. LaPerle, R. Scott Obach, Karthik Venkatakrishnan, Adam Yasgar, Ellen Q. Wang, Cuiping Chen, Sandhya Rahematpura, John P. Gibbs, Emily R. Olson, Kari Schmidt, Michael J. Logman, Ernesto Callegari, Cornelis E. C. A. Hop, Gary Walens, Xi Chen, Mark A. Szewc, Elaine E. Tseng, Frank M. Nedza, Heather L. Hatch, Meihua Tu, Matthew D. Troutman, Stacey L. Becker, Sabrinia Rogers, Megan A. Gibbs, Debra Maclin, Xingrong Liu, Ilana N. Kasman, Natilie Hosea, Diane Wong, Bill J. Smith, Loretta M. Cox, Jeffrey Van Deusen, Julie Cianfrogna, JianHua Liu, Edna F. Choo, Angela C. Doran, David Raunig, Chenghong Zhang
Publikováno v:
Drug metabolism and disposition: the biological fate of chemicals. 33(1)
Thirty-two structurally diverse drugs used for the treatment of various conditions of the central nervous system (CNS), along with two active metabolites, and eight non-CNS drugs were measured in brain, plasma, and cerebrospinal fluid in the P-glycop
Autor:
Travis T. Wager, Betty A. Pettersen, Anne W. Schmidt, Douglas K. Spracklin, Scot Mente, Todd W. Butler, Harry Howard, Daniel J. Lettiere, David M. Rubitski, Diane F. Wong, Frank M. Nedza, Frederick R. Nelson, Hans Rollema, Jeffrey W. Raggon, Jiri Aubrecht, Jody K. Freeman, John M. Marcek, Julie Cianfrogna, Karen W. Cook, Larry C. James
Publikováno v:
Journal of Medicinal Chemistry; Nov2011, Vol. 54 Issue 21, p7602-7620, 19p