Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Vincent J Colandrea"'
Autor:
Jiaqiang Cai, Bimjhana Bishwokarma, Dennis Leung, William J. Morris, Feroze Ujjainwalla, Candice Alleyne, Xiaoxing Du, Vincent J. Colandrea, Jennifer Piesvaux, Jianwu Bai, Liming Yang, Carla Alpert, Joseph M. Metzger, Vincenzo Pucci, Xiaofang Li, Jeffrey J. Hale, Dominique Stickens, Weiguo Quan, Byron G. DuBois, Rongqiang Liu, Mark Zielstorff, Chi-Sung Chiu, Christopher Joseph Sinz, Mangeng Cheng, Kallol Ray, Liping Wang, Ping Liu, Stella H. Vincent, Alejandro Crespo
Publikováno v:
ACS Medicinal Chemistry Letters. 9:1193-1198
[Image: see text] We report herein the design and synthesis of a series of orally active, liver-targeted hypoxia-inducible factor prolyl hydroxylase (HIF-PHD) inhibitors for the treatment of anemia. In order to mitigate the concerns for potential sys
Autor:
Vincent J. Colandrea, Ravi Kurukulasuriya, Petr Vachal, Beth Ann Murphy, Rajan Anand, Kake Zhao, Mikhail Reibarkh, Alejandro Crespo, Ruth A. Duffy, Joseph L. Duffy, Jonathan E. Wilson, Anne-Marie Cumiskey, Maud Reiter, Aaron Zwicker, Fengqi Zhang, Kaushik Mitra, Douglas G. Johns
Using the collective body of known (CETP) inhibitors as inspiration for design, a structurally novel series of tetrahydroquinoxaline CETP inhibitors were discovered. An exemplar from this series, compound 5, displayed potent in vitro CETP inhibition
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::50f1f63cab482d2b7431e81a19537bcf
https://europepmc.org/articles/PMC4789658/
https://europepmc.org/articles/PMC4789658/
Publikováno v:
Expert Opinion on Therapeutic Patents. 20:1219-1245
Anemia caused by chronic kidney disease and other chronic diseases or conditions can be managed by the treatment of biologic-based erythropoiesis stimulating agents (ESAs). Although these ESAs are successful in treating these anemic conditions, a sma
Autor:
Tung M. Fong, Helen E. Armstrong, Thomas J. Lanza, Sookhee Ha, Julie Lao, James P. Jewell, Quang Truong, Lauren P. Shearman, Vincent J. Colandrea, Grace M. Quaker, William K. Hagmann, Guthikonda Ravi N, D. Sloan Stribling, Junying Wang, Chun-Pyn Shen, Sherry Xu, Linus S. Lin, Amy Galka, Xinchun Tong, Mark T. Goulet, Shrenik K. Shah, Linda L. Chang, Lex H.T. Van der Ploeg, Alison M. Strack, Jing Chen, Kimberly Rosko
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2184-2187
Sulfonamide analogues of the potent CB1R inverse agonist taranabant were prepared and optimized for potency and selectivity for CB1R. They were variably more potent than the corresponding amide analogues. The most potent representative 22 had good ph
Autor:
Charles Lee Jayne, Francisco Velazquez, Zhuyan Guo, Donald M. Sperbeck, Murali Rajagopalan, Duane Burnette, Karen Marcantonio, Shouwu Miao, Sathesh Bhat, Santhosh Neelamkavil, Linda Brockunier, Stacia Kargman, Yan Xia, Rebecca T. Ruck, Vincent J. Colandrea, John A. Howe, Nicole Buist, Andrew Nolting, Yongxin Han, Pinto Patrick A, Thomas Bara, Mark Cartwright, Robert Chase, Martin C. Clasby, Srikanth Venkatraman, Randy R. Miller, Keith Eagen, Samuel Chackalamannil, Josien Hubert B, Chad Bennett, Mariappan V. Chelliah, Ian W. Davies, Austin Chen, Shah Unmesh G, Sony Agrawal, Dipshikha Biswas, Jin Wu, Aileen Soriano
Publikováno v:
ACS medicinal chemistry letters. 7(1)
We have been focused on identifying a structurally different next generation inhibitor to MK-5172 (our Ns3/4a protease inhibitor currently under regulatory review), which would achieve superior pangenotypic activity with acceptable safety and pharmac
Autor:
Carol Ann Keohane, Suzanne M. Mandala, Mark Rosenbach, Gary Chebret, Gan-Ju Shei, James D. Bergstrom, Vincent J. Colandrea, Irene E. Legiec, Lin Yan, Deborah Card, Pei Huo, James A. Milligan, Sander G. Mills, Richard Hajdu, Jeffrey J. Hale
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:2905-2908
A series of 2,5-cis-disubstituted pyrrolidines were synthesized and evaluated as S1P receptor agonists. Compounds 15-21 were identified with good selectivity over S1P3 which lowered circulating lymphocytes after oral administration in mice.
Autor:
Carol Ann Keohane, Gloria Y. Kwei, Wei Tang, Susan A. Iliff, Adria Colletti, Vincent J. Colandrea, Frank S. Tang, Ann E. Weber, Randy R. Miller, Shuet-Hing Lee Chiu, William P. Feeney, Ralph A. Stearns, John R. Strauss, Dawn Chitty, Elizabeth M. Naylor, Robert J. Mathvink
Publikováno v:
Drug Metabolism and Disposition. 30:771-777
The pharmacokinetics and oral bioavailability of (R)-N-[4-[2-[[2-hydroxy-2-(pyridin-3-yl)ethyl]amino]ethyl]phenyl]-4-[4-[4-(trifluoromethylphenyl]thiazol-2-yl]benzenesulfonamide (1), a 3-pyridyl thiazole benzenesulfonamide beta3-adrenergic receptor a
Publikováno v:
Tetrahedron Letters. 41:8053-8057
A regioselective alkylation of naphthyridines 4a–d, through the action of ethylchloroformate and benzylstannane 5, afforded the benzyl substituted dihydronaphthyridines 3a–d. These key intermediates 3a–d were transformed into the desired target
Publikováno v:
Tetrahedron. 55:10659-10672
Various dialkyl- and diarylvinylsulfonium salts react with indole-2-carboxaldehydes in the presence of sodium hydride and sodium azide to form tricyclic azido alcohols analogous to 2 . With pyrrole-2-carboxaldehyde, [2,3] sigmatropic and other rearra
Autor:
Matthew J. Wyvratt, Leroy Perkins, Randall R. Miller, Ann E. Weber, William P. Feeney, Vincent J. Colandrea, Michael J. Forrest, Emma R. Parmee, Laurie Tota, Michael H. Fisher, Mari R. Candelore, Gary J Hom, Hyun O. Ok, Elizabeth M. Naylor, Catherine D. Strader, Margaret A. Cascieri, Ralph A. Stearns, Liping Deng, D. Euan MacIntyre
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:749-754
Human beta3 adrenergic receptor agonists containing 5-membered ring ureas were shown to be potent partial agonists with excellent selectivity over beta1 and beta2 binding. L-760,087 (4a) and L-764,646 (5a) (beta3 EC50 = 18 and 14 nM, respectively) st