Zobrazeno 1 - 4
of 4
pro vyhledávání: '"Susana C. Neira"'
Autor:
Andrew Tasker, Andrea Itano, Anu Gore, Paul E. Harrington, Mike Frohn, Victor J. Cee, Michele McElvain, Min Wong, Mike Fiorino, Alexander J. Pickrell, Kelvin K. C. Sham, Han Xu, Brian A. Lanman, Anthony B. Reed, Yang Xu, Susana C. Neira, Scot Middleton, Henry Morrison
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1779-1783
Replacement of the azetidine carboxylate of an S1P1 agonist development candidate, AMG 369, with a range of acyclic head-groups led to the identification of a novel, S1P3-sparing S1P1 agonist, (−)-2-amino-4-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiaz
Autor:
Min Wong, Yang Xu, Scot Middleton, Matthew R. Lee, Anu Gore, Mike Fiorino, Alex Pickrell, Kristine M. Muller, Andrea Itano, Mike Frohn, Heather A. Arnett, Janet Buys, Michelle Horner, Dalia Rivenzon-Segal, Jennifer E. Golden, Victor J. Cee, Hugo M. Vargas, Roland Burli, Susana C. Neira, Michael Schrag, Han Xu, Brian A. Lanman, Michele McElvain, Xuxia Zhang, Jerry Siu
Publikováno v:
ACS Medicinal Chemistry Letters. 2:107-112
The optimization of a series of thiazolopyridine S1P1 agonists with limited activity at the S1P3 receptor is reported. These efforts resulted in the discovery of 1-(3-fluoro-4-(5-(1-phenylcyclopropyl)thiazolo-[5,4-b]pyridin-2-yl)benzyl)azetidine-3-ca
Autor:
Michelle Horner, Kristine M. Muller, Xuxia Zhang, Xiang Yu, Nili Schutz, Jerry Siu, Dalia Rivenzon-Segal, Roland Burli, Zhang Zhaoda, Susana C. Neira, Hugo M. Vargas, Alexander J. Pickrell, Jennifer E. Golden, Yang Xu, Victor J. Cee, Michael Schrag, Scot Middleton, Jian Lin, Yael Marantz, Andrea Itano, Mercedes Lobera, Han Xu, Brian A. Lanman, Michele McElvain, Janet Buys, Anu Gore, Srinivasa R Cheruku, Anurag Sharadendu, Mike Fiorino, Mike Frohn
Optimization of a benzofuranyl S1P1 agonist lead compound (3) led to the discovery of 1-(3-fluoro-4-(5-(2-fluorobenzyl)benzo[d]thiazol-2-yl)benzyl)azetidine-3-carboxylic acid (14), a potent S1P1 agonist with minimal activity at S1P3. Dosed orally at
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4114b66ba763963fd644e7ff1f508317
https://europepmc.org/articles/PMC4018108/
https://europepmc.org/articles/PMC4018108/
Autor:
Andrea Itano, Dawei Zhang, Matthew H. Plant, Yen Nguyen, Xuxia Zhang, Matthew R. Lee, Gordon Ng, Essa Hu, Violeta Yu, Kristin Meagher, Susana C. Neira, Roland Burli, Randall W. Hungate, Shaun Flynn, Ning Chen, Michael Schrag, Yang Xu, Yanyan Tudor
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(14)
A potent and selective c-Kit inhibitor 20 was identified through a structure–activity relationship study. In an in vivo mouse model of mast cell activation, 20 blocked the SCF-induced histamine release with an EC50 of 26 nM.