Structure and activity relationships of tartrate-based TACE inhibitors
The syntheses and structure-activity relationships of the tartrate-based TACE inhibitors are discussed. The optimization of both the prime and non-prime sites led to compounds with picomolar activity. Several analogs demonstrated good rat pharmacokinetics
Li, Dansu,Popovici-Muller, Janeta,Belanger, David B.,Caldwell, John,Dai, Chaoyang,David, Maria,Girijavallabhan, Vinay M.,Lavey, Brian J.,Lee, Joe F.,Liu, Zhidan,Mazzola, Rob,Rizvi, Razia,Rosner, Kristin E.,Shankar, Bandarpalle,Spitler, Jim,Ting, Pauline C.,Vaccaro, Henry,Yu, Wensheng,Zhou, Guowei,Zhu, Zhaoning,Niu, Xiaoda,Sun, Jing,Guo, Zhuyan,Orth, Peter,Chen, Shiying,Kozlowski, Joseph A.,Lundell, Daniel J.,Madison, Vincent,McKittrick, Brian,Piwinski, John J.,Shih, Neng-Yang,Shipps Jr., Gerald W.,Siddiqui, M. Arshad,Strickland, Corey O.
scheme or table
p. 4812 - 4815
(2010/10/02)
COMPOUNDS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
This invention relates to compounds of the Formula (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-α or combinations thereof.
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Page/Page column 361
(2010/02/15)
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