159216-53-2Relevant academic research and scientific papers
AMIDINO-COMPOUNDS POR STABILIZING FACTOR VII POLYPEPTIDE FORMULATIONS
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Page/Page column 30, (2008/06/13)
The invention relates to novel compounds of the formula (I) and their use in stabilization of Factor Vila or other Factor VII polypeptides, particularly in aqueous liquid compositions thereof.
Structure-based design of amidinophenylurea-derivatives for factor VIIa inhibition
Klingler, Otmar,Matter, Hans,Schudok, Manfred,Donghi, Monica,Czech, Joerg,Lorenz, Martin,Nestler, Hans Peter,Szillat, Hauke,Schreuder, Herman
, p. 3715 - 3720 (2007/10/03)
The amidinophenylurea scaffold was earlier shown to provide an excellent template for the synthesis of novel and potent inhibitors of the blood coagulation factor VIIa. In this contribution we describe the structure-based design of potent ligands guided by X-ray crystallography, molecular modeling and docking studies. The design and synthetic efforts were directed towards novel modifications to explore the protease binding region close to the S4 subsite.
Design, synthesis, and structure-activity relationship of a new class of amidinophenylurea-based factor VIIa inhibitors
Klingler, Otmar,Matter, Hans,Schudok, Manfred,Bajaj, S. Paul,Czech, Joerg,Lorenz, Martin,Nestler, Hans Peter,Schreuder, Herman,Wildgoose, Peter
, p. 1463 - 1467 (2007/10/03)
Selective inhibition of coagulation factor VIIa has recently gained attraction as interesting approach towards antithrombotic treatment. Using parallel synthesis supported by structure-based design and X-ray crystallography, we were able to identify a novel series of amidinophenylurea derivatives with remarkable affinity for factor VIIa. The most potent compound displays a Ki value of 23 nM for factor VIIa.
Factor VIIa inhibitory (thio)urea derivatives, their preparation and their use
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, (2008/06/13)
The present invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5, R6, A, X, m and n have the meanings indicated in the claims. The compounds of the formula I are val
Urea derivatives, their preparation and use
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, (2008/06/13)
Urea derivates are disclosed having the formula (I). STR1 in which A, B, W, Z, R, R1, R2, R3 and r have the meaning given in the description, as well as a process for preparing the same and their use as inhibitors of throm
