431049-86-4Relevant academic research and scientific papers
PEGYLATED CARFILZOMIB COMPOUNDS
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Page/Page column 59, (2017/12/29)
The present invention provides polymeric pegylated carfilzomib compounds, and pharmaceutically acceptable salts thereof, of Formula I wherein R1, R2, linker, PEG, n and o are as defined herein. The invention also provides methods of
Discovery of nonbenzamidine factor VIIa inhibitors using a biaryl acid scaffold
Bolton, Scott A.,Sutton, James C.,Anumula, Rushith,Bisacchi, Gregory S.,Jacobson, Bruce,Slusarchyk, William A.,Treuner, Uwe D.,Wu, Shung C.,Zhao, Guohua,Pi, Zulan,Sheriff, Steven,Smirk, Rebecca A.,Bisaha, Sharon,Cheney, Daniel L.,Wei, Anzhi,Schumacher, William A.,Hartl, Karen S.,Liu, Eddie,Zahler, Robert,Seiler, Steven M.
, p. 5239 - 5243 (2013/09/12)
In this Letter, we describe the synthesis of several nonamidine analogs of biaryl acid factor VIIa inhibitor 1 containing weakly basic or nonbasic P1 groups. 2-Aminoisoquinoline was found to be an excellent surrogate for the benzamidine group (compound 2) wherein potent inhibition of factor VIIa is maintained relative to most other related serine proteases. In an unanticipated result, the m-benzamide P1 (compounds 21a and 21b) proved to be a viable benzamidine replacement, albeit with a 20-40 fold loss in potency against factor VIIa.
Development of a new distyrylbenzene-derivative amyloid-β-aggregation and fibril formation inhibitor
Suzuki, Hideharu,Orimoto, Ayako,Matsuyama, Akihiro,Yokoyama, Yuusaku,Okuno, Hiroaki,Nakakoshi, Masamichi,Ishigami, Akihito,Handa, Setsuko,Maruyam, Naoki
, p. 1164 - 1170,7 (2020/08/31)
Several new amyloid-β (Aβ) aggregation inhibitors were synthesized according to our theory that a hydrophilic moiety could be attached to the Aβ-recognition unit for the purpose of preventing amyloid plaque formation. A distyrylbenzene-derivative, DSB(EEX
Development of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as orally active human chymase inhibitors
Maruoka, Hiroshi,Muto, Tsuyoshi,Tanaka, Taisaku,Imajo, Seiichi,Tomimori, Yoshiaki,Fukuda, Yoshiaki,Nakatsuka, Takashi
, p. 3435 - 3439 (2008/02/10)
A novel series of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones was designed, synthesized, and evaluated as human chymase inhibitors. From this series, we identified several compounds which were effective, via oral administration, in a mou
