Zobrazeno 1 - 10
of 130
pro vyhledávání: '"J. J. Hale"'
Autor:
Urmi R. Bhatt, James R. Tata, Xinchun Tong, Hong C. Shen, Andreas Verras, Renee M. Chabin, Michael E. Lassman, Changyou Zhou, Margarita Garcia-Calvo, J. J. Hale, Ranabir SinhaRoy, Steven L. Colletti, Yusheng Xiong, Dong-Ming Shen, Dunlu Chen, Wayne M. Geissler, Fa-Xiang Ding, Shirly Pinto, Suoyu Xu, Dan Xie, Zhu Shen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1299-1305
A series of benzimidazole pyrrolidinyl amides containing a piperidinyl group were discovered as novel prolylcarboxypeptidase (PrCP) inhibitors. Low-nanomolar IC(50)'s were achieved for several analogs, of which compound 9b displayed modest ex vivo ta
Autor:
Margaret A. Cascieri, Salvatore J. Siciliano, Karen Holmes, Sandra L. Gould, Kevin T. Chapman, William A. Schleif, J. J. Hale, Richard J. Budhu, Renee Danzeisen, Joseph Kessler, Anthony Carella, Julie A. DeMartino, Christopher A. Willoughby, Daria J. Hazuda, Sander G. Mills, Malcolm MacCoss, Michael W. Miller, Janet Lineberger, Emilio A. Emini, Lorraine Malkowitz, Keith G. Rosauer, Martin S. Springer, Gwen Carver
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:427-431
A new class of 4-(aminoheterocycle)piperidine derived 1,3,4 trisubstituted pyrrolidine CCR5 antagonists is reported. Compound 4a is shown to have good binding affinity (1.8 nM) and antiviral activity in PBMC's (IC95=50 nM). Compound 4a also has impro
Autor:
M. Maccoss, Paul E. Finke, Bruce L. Daugherty, Youmin Weng, Di Salvo J, Julie A. DeMartino, Christopher L. Lynch, Laurie A. Castonguay, Marty S. Springer, J. J. Hale, Sander G. Mills, Adolfsen W, Charles G. Caldwell, Ruth Kilburn
Publikováno v:
Biochemistry. 42:1544-1550
The results of investigations in these laboratories of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines as human CCR5 antagonists have recently been disclosed. To facilitate further development of these antagonists, we have
Autor:
Richard Hargreaves, D. E. Macintyre, G Mason, S Tye, E. Ber, F.D. Tattersall, Michael J Cumberbatch, J. J. Hale, Malcolm MacCoss, Margaret A. Cascieri, W. Rycroft, Paul E. Finke, Raymond G. Hill, Sharon Sadowski, David J. Williamson, Sander G. Mills
Publikováno v:
Neuropharmacology. 39:652-663
The anti-emetic profile of the novel brain penetrant tachykinin NK1 receptor antagonist MK-0869 (L-754,030) 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluor o)phenyl-4-(3-oxo-1,2,4-triazol-5-yl)methylmorpholine and its water soluble
Autor:
P. E. Finke, Gary G. Chicchi, Nadia M.J. Rupniak, George J. Eiermann, Nancy N. Tsou, E. Ber, Angela Williams, W. Rycroft, Margaret A. Cascieri, Sander G. Mills, Richard Hargreaves, M. Maccoss, Joe Metzger, D. E. Macintyre, Myra B. Kurtz, Sharon Sadowski, J. J. Hale, F.D. Tattersall
Publikováno v:
Journal of Medicinal Chemistry. 41:4607-4614
Structural modifications requiring novel synthetic chemistry were made to the morpholine acetal human neurokinin-1 (hNK-1) receptor antagonist 4, and this resulted in the discovery of 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluor
Autor:
S. K. Shah, H. Weston, W. K. Hagmann, Richard A. Mumford, Karen A. Brause, J. B. Doherty, D. S. Fletcher, W. B. Knight, C. P. Jun. Dorn, Dennis J. Underwood, Pam S. Dellea, J. J. Hale, Amy L. Kissinger, P. E. Finke, Karen M. Hand, Alan L. Maycock, Bonnie M. Ashe, G. O. Chandler
Publikováno v:
ChemInform. 24
Autor:
D. E. Macintyre, Hongbo Qi, David J. Mathre, Sander G. Mills, J. J. Hale, M. Maccoss, Catherine D. Strader, Joseph M. Metzger, Margaret A. Cascieri, Sharon Sadowski, S. K. Shah
Publikováno v:
ChemInform. 27
Autor:
S K, Shah, C P, Dorn, P E, Finke, J J, Hale, W K, Hagmann, K A, Brause, G O, Chandler, A L, Kissinger, B M, Ashe, H, Weston
Publikováno v:
Journal of Medicinal Chemistry. 35:3745-3754
A thorough analysis of the mechanism of inhibition of human leukocyte elastase (HLE) by a monocyclic beta-lactam and the mechanism of beta-lactam hydrolysis led to the preparation of potent and highly stable inhibitors of HLE. This work led to the id
Autor:
Dennis M. Zaller, Yan Cui, Richard Hajdu, Kalpit A. Vora, J. J. Hale, Elizabeth A. Nichols, William E. Neway, Gene Porter, Carol Ann Keohane, Suzanne M. Mandala
Publikováno v:
Journal of leukocyte biology. 78(2)
FTY720 is an immunosuppressive agent that modulates lymphocyte trafficking. It is phosphorylated in vivo to FTY720-phosphate (FTY-P) and binds to a family of G protein-coupled receptors recognizing sphingosine 1-phosphate (S1P) as the natural ligand.
Autor:
D. E. Macintyre, Catherine D. Strader, J. J. Hale, Margaret A. Cascieri, S. K. Shah, Sharon Sadowski, Joseph M. Metzger, Hongbo Qi, M. Maccoss, D J Mathre, Sander G. Mills
Publikováno v:
Journal of Medicinal Chemistry. 39:1760-1762