203258-20-2Relevant academic research and scientific papers
SUBSTITUTED PYRROLIDINES AS FACTOR XIA INHIBITORS FOR THE TREATMENT THROMBOEMBOLIC DISEASES
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Paragraph 0514-0515, (2015/06/10)
The present invention provides compounds of the general formula (I), their salts and N-oxides, and solvates and prodrugs thereof (wherein the substituents are as defined in the description). The compounds of the general formula (I) are inhibitors of factor XIa, and are useful in the prevention of and/or therapy for thromboembolic diseases.
SUBSTITUTED PYRROLIDINES AS FACTOR XIA INHIBITORS FOR THE TREATMENT THROMBOEMBOLIC DISEASES
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Page/Page column 85, (2014/01/07)
The present invention provides compounds of the general formula (I), their salts and N- oxides, and solvates and prodrugs thereof (wherein the substituents are as defined in the description). The compounds of the general formula (I) are inhibitors of factor XIa, and are useful in the prevention of and/or therapy for thromboembolic diseases.
Tobramycin analogues with C-5 aminoalkyl ether chains intended to mimic rings III and IV of paromomycin
Hanessian, Stephen,Tremblay, Martin,Swayze, Eric E.
, p. 983 - 993 (2007/10/03)
Based on available X-ray structural and modeling data, a series of tobramycin derivatives with C-5 ether chains bearing basic groups were synthesized. These were intended to be hybrid molecules that combine features of tobramycin and paromomycin. Their binding to ribosomes and their antibacterial activity were determined. The 5-O-(2-guanidylethyl) ether of tobramycin (9g) was the most active analogue in the series.
Design, synthesis and biological evaluation of nonpeptide integrin antagonists
Nicolaou,Trujillo, John I.,Jandeleit, Bernd,Chibale, Kelly,Rosenfeld,Diefenbach,Cheresh,Goodman
, p. 1185 - 1208 (2007/10/03)
Recent studies demonstrated that peptide and antibody antagonists of integrin α(v)β3 block angiogenesis and tumor growth. In this article, the design, synthesis and biological evaluation of a series of nitroaryl ether-based, nonpeptide mimetics are described. The design of these compounds was based on Merck's arylether/α-aminoacid/guanidine framework and incorporates a novel nitroaryl system. The synthesized mimetics were tested against a variety of integrins (α(v)β3, α(IIb)β3, and α(v)β5) in order to determine their binding selectivity and ability to inhibit cell adhesion. Selected compounds were also tested for their ability to inhibit angiogenesis in vivo in the CAM (chick chorioallantoic membrane) assay. From the generated compound library, compounds 16 and 19 proved to be potent and selective inhibitors of α(IIb)β3 (IC50=14nM) whereas compound 11 showed excellent in vivo inhibition of angiogenesis (at 30μg/embryo). Copyright (C) 1998 Elsevier Science Ltd.
Solution phase combinatorial chemistry. Discovery of 13- and 15-membered polyazapyridinocyclophane libraries with antibacterial activity
An, Haoyun,Wang, Tingmin,Mohan, Venkatraman,Griffey, Richard H.,Dan Cook
, p. 3999 - 4012 (2007/10/03)
A solution phase simultaneous addition of functionalities (SPSAF) combinatorial approach was utilized to synthesize 40 polyazacyclophane libraries (total complexity of 4275). Eighteen different functionality sets, utilizing 42 functionalities, were design
