764659-69-0Relevant academic research and scientific papers
Discovery and structure-activity relationships of 4-aminoquinazoline derivatives, a novel class of opioid receptor like-1 (ORL1) antagonists
Okano, Masahiko,Mito, Jun,Maruyama, Yasufumi,Masuda, Hirofumi,Niwa, Tomoko,Nakagawa, Shin-ichiro,Nakamura, Yoshitaka,Matsuura, Akira
experimental part, p. 119 - 132 (2011/02/25)
Synthesis and structure-activity relationship studies of a series of 4-aminoquinazoline derivatives led to the identification of (1R,2S)-17, N-[(1R,2S)-2-({2-[(4-chlorophenyl)carbonyl]amino-6-methylquinazolin-4-yl}amino)cyclohexyl]guanidine dihydrochloride, as a highly potent ORL1 antagonist with up to 3000-fold selectivity over the μ, δ, and κ opioid receptors. Molecular modeling clarified the structural factors contributing to the high affinity and selectivity of (1R,2S)-17.
SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa
Qiao, Jennifer X.,Chang, Chong-Hwan,Cheney, Daniel L.,Morin, Paul E.,Wang, Gren Z.,King, Sarah R.,Wang, Tammy C.,Rendina, Alan R.,Luettgen, Joseph M.,Knabb, Robert M.,Wexler, Ruth R.,Lam, Patrick Y.S.
, p. 4419 - 4427 (2008/02/10)
In the search of Factor Xa (FXa) inhibitors structurally different from the pyrazole-based series, we identified a viable series of enantiopure cis-(1R,2S)-cycloalkyldiamine derivatives as potent and selective inhibitors of FXa. Among them, cyclohexyldiam
SULFUR COMPOUNDS AS INHIBITORS OF HEPATITIS C VIRUS NS3 SERINE PROTEASE
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Page/Page column 320-321, (2010/02/14)
The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
SULFONYL-AMIDINO CONTAINING AND TETRAHYDROPYRIMIDINO CONTAINING COMPOUNDS AS FACTOR XA INHIBITORS
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Page 172, (2010/02/08)
The present application describes sulfonyl-amidino-containing and tetrahydropyrimidino-containing compounds and derivatives thereof of Formula (I): P4-P-M-M4 or pharmaceutically acceptable salt forms thereof, wherein M is a ring, P is an optional ring, and P4 and M4 are as defined below. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
