Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Robert P. Rehfuss"'
Autor:
Patrick Y.S. Lam, John Lloyd, Ming Chang, Qimin Wu, Joanna Zheng, Robert P. Rehfuss, James C. Sutton, Christine Huang, Ji Hua, Laura Price, Zulan Pi, Ruth R. Wexler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4206-4209
ADP receptors, P2Y1 and P2Y12 have been recognized as potential targets for antithrombotic drugs. A series of P2Y1 antagonists that contain 2-aminothiazoles as urea surrogates were discovered. Extensive SAR of the thiazole ring is described. The most
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ccf0d15860d86b874bf18a891fcad23
https://doi.org/10.1016/j.bmcl.2013.05.025
https://doi.org/10.1016/j.bmcl.2013.05.025
Autor:
Laura Price, Ruth R. Wexler, Patrick Y.S. Lam, Pancras C. Wong, Dietmar A. Seiffert, Ming Chang, Joanna Zheng, Earl J. Crain, Robert P. Rehfuss, Carol A. Watson, Tammy C. Wang, Gerry Everlof, William A. Schumacher, Christine Huang, Charles G. Clark, Qimin Wu, Anne B. Stewart, Jeffrey S. Bostwick, Jennifer X. Qiao, Ji Jua
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:3239-3243
Preclinical data suggests that P2Y1 antagonists, such as diarylurea compound 1, may provide antithrombotic efficacy similar to P2Y12 antagonists and may have the potential of providing reduced bleeding liabilities. This manuscript describes a series
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4bc55dbb5af3bc1f8108d08c230fc308
https://doi.org/10.1016/j.bmcl.2013.03.125
https://doi.org/10.1016/j.bmcl.2013.03.125
Autor:
Michael A. Poss, Ming Chang, Dora M. Schnur, Timothy F. Herpin, Ruth R. Wexler, Jacques Y. Roberge, Maredith Arcuri, Robert P. Rehfuss, Deborah Celani, Yalei Liu, Huji Turdi, Angela Cacace, Christine Huang, William A. Schumacher, Martin L. Ogletree, Hannguang Chao, Qimin Wu, Anne B. Stewart, Ji Hua, R. Michael Lawrence, Jeffrey S. Bostwick, Thomas E. Steinbacher, Laura Price, Lynn M. Abell
Publikováno v:
Journal of Medicinal Chemistry. 56:1704-1714
Two distinct G protein-coupled purinergic receptors, P2Y1 and P2Y12, mediate ADP-driven platelet activation. The clinical effectiveness of P2Y12 blockade is well established. Recent preclinical data suggest that P2Y1 and P2Y12 inhibition provide equi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::098620dbfa884295461a2bd143f803b4
https://doi.org/10.1021/jm301708u
https://doi.org/10.1021/jm301708u
Autor:
Pancras C. Wong, William A. Schumacher, Ji Hua, Earl J. Crain, Robert P. Rehfuss, Carol A. Watson
Publikováno v:
Thrombosis and Haemostasis. 101:108-115
SummaryThe new P2Y12 antagonist prasugrel produces greater inhibition of ADP-induced platelet aggregation (IPA) and reduction of thrombotic events in patients versus approved doses of clopidogrel, but increases major bleeding. We examined whether IPA
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::b80ab9c169cc5108831dabfad11ae4be
https://doi.org/10.1160/th08-07-0456
https://doi.org/10.1160/th08-07-0456
Autor:
Steven Grant, Suzanne J. Suchard, Robert P. Rehfuss, Steven G. Nadler, Kathleen M. Gillooly, Anish Suri, Robert Kuhn, Ruth Brosius, Yifan Zhang, Rathna Ravishankar, Kathy A Mink, Aaron P. Yamniuk, Sandra Rex-Rabe, Jenny Xie, Philip Drew, Luisa Salter-Cid, Kimberly S Waggie, James William Bryson, Olga Ignatovich, Lin Cheng, Laura Price, Xiadi Zhou, Yongmi An, James K. Tamura, Virna Borowski, Xiaoxia Yang, Bozena Abramczyk, Vojkan Susulic
Publikováno v:
Journal of immunology (Baltimore, Md. : 1950). 192(9)
CD40–CD40L interactions play a critical role in regulating immune responses. Blockade of CD40L by Abs, such as the anti-CD40L Ab 5c8, demonstrated positive clinical effects in patients with autoimmune diseases; however, incidents of thromboembolism
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f805007657a9cec2f3f88fbe5d1db4e8
https://pubmed.ncbi.nlm.nih.gov/24670803
https://pubmed.ncbi.nlm.nih.gov/24670803
Autor:
Robert P. Rehfuss, John H. White, Sarah Bevan, Geoffrey N. Hendy, Damian G. Wheeler, Lucie Canaff, Andrew J. Mouland
Publikováno v:
Endocrinology. 139:1184-1196
Chromogranin A (CgA), a member of the granin/secretogranin family of acidic glycoproteins that play multiple roles in the process of regulated secretion of peptide hormones and neurotransmitters, is specifically expressed in endocrine and neuroendocr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::00f05b968101aafdb0d88b3006473e13
https://doi.org/10.1210/endo.139.3.5851
https://doi.org/10.1210/endo.139.3.5851
Autor:
Robert P. Rehfuss, Paul Levesque, Juliang Zhu, Arvind Mathur, Dietmar A. Seiffert, Bang-Chi Chen, Rejean Ruel, Laura Price, Yufeng Wang, Mary F. Malley, Xue-Qing Chen, Wu Yang, Ji Hua, Tammy C. Wang, William A. Schumacher, Yajun Liu, Dauh-Rurng Wu, Silvi A. Chacko, Jeffrey S. Bostwick, Charles G. Clark, Danshi Li, Patrick Y.S. Lam, Henry S. Wong, Anne B. Stewart, Dawn Sun, Ruth R. Wexler, Hong Shen, Sheldon Hiebert, Christine Huang, Ling Li, Jeon Yoon T, Carl Thibeault, Jennifer X. Qiao
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(5)
Spiropiperidine indoline-substituted diaryl ureas had been identified as antagonists of the P2Y1 receptor. Enhancements in potency were realized through the introduction of a 7-hydroxyl substitution on the spiropiperidinylindoline chemotype. SAR stud
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d87ed0cd8e9411cf0132670a06c19e56
https://pubmed.ncbi.nlm.nih.gov/24513044
https://pubmed.ncbi.nlm.nih.gov/24513044
Autor:
Carl Thibeault, Ruth R. Wexler, Dora M. Schnur, John Lloyd, Zulan Pi, Rejean Ruel, Patrick Y.S. Lam, William A. Schumacher, Ji Hua, Jennifer X. Qiao, Patricia A. McDonnell, Lynn M. Abell, Ming Chang, Christine Huang, Laura Price, Qi Gao, Robert P. Rehfuss, Baoqing Ma, Gilles Bouthillier, Eddie C.-K. Liu, Jeffrey S. Bostwick, Tammy C. Wang, Qimin Wu, Alexandre L'Heureux, Steven A. Spronk, Sheldon Hiebert, Joanna Zheng, Thomas E. Steinbacher
Publikováno v:
Journal of medicinal chemistry. 56(22)
Preclinical antithrombotic efficacy and bleeding models have demonstrated that P2Y1 antagonists are efficacious as antiplatelet agents and may offer a safety advantage over P2Y12 antagonists in terms of reduced bleeding liabilities. In this article,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a56313da67977fc86928fe014b6615e4
https://pubmed.ncbi.nlm.nih.gov/24164581
https://pubmed.ncbi.nlm.nih.gov/24164581
Autor:
Qimin Wu, Alexandre L'Heureux, Christine Huang, Ji Hua, Robert P. Rehfuss, Jennifer X. Qiao, Laura Price, Patrick Y.S. Lam, Ming Chang, Ruth R. Wexler, Philippe Lapointe, Rejean Ruel, Alain Martel, Joanna Zheng, Carl Thibeault
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(24)
A number of new amine scaffolds with good inhibitory activity in the ADP-induced platelet aggregation assay have been found to be potent antagonists of the P2Y1 receptor. SAR optimization led to the identification of isoindoline 3c and piperidine 4a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ce63ce6c7d5ef7678a2b3335fed8e2f6
https://pubmed.ncbi.nlm.nih.gov/24269480
https://pubmed.ncbi.nlm.nih.gov/24269480
Autor:
Patrick Y.S. Lam, Jean-Paul Daris, Carl Thibeault, Ruth R. Wexler, Ji Hua, Robert P. Rehfuss, Qimin Wu, Alexandre L'Heureux, Alain Martel, Rejean Ruel, Laura Price
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(12)
Five-membered-ring heterocyclic urea mimics have been found to be potent and selective antagonists of the P2Y1 receptor. SAR of the various heterocyclic replacements is presented, as well as side-chain SAR of the more potent thiadiazole ring system w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::94869f87bcf45a4fbf5948460f5776ea
https://pubmed.ncbi.nlm.nih.gov/23668989
https://pubmed.ncbi.nlm.nih.gov/23668989