187084-44-2Relevant academic research and scientific papers
Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand
Nazare, Marc,Essrich, Melanie,Will, David W.,Matter, Hans,Ritter, Kurt,Urmann, Matthias,Bauer, Armin,Schreuder, Herman,Czech, Joerg,Lorenz, Martin,Laux, Volker,Wehner, Volkmar
, p. 4197 - 4201 (2004)
A series of novel, highly potent 2-carboxyindole-based factor Xa inhibitors is described. Structural requirements for P4 ligands in combination with a neutral biaryl P1 ligand were investigated with the 2-carboxyindole scaffold. A diverse set of P4 substituents was identified, which, in conjunction with a biaryl P1 ligand, gave highly potent factor Xa inhibitors, which were also selective versus other proteases and efficacious in various antithrombotic secondary assays.
NOVEL COMPOUNDS
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Page/Page column 150, (2011/12/13)
Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases. The following is exemplary:
Pyrazole-derivatives as factor Xa inhibitors
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Page 46, (2008/06/13)
The present invention relates to compounds of the formula I, in which R0 ; R1 ; R2 ; R3 ; R4; Q; V, G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Amidine compounds
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, (2008/06/13)
A compound of the formula [I] wherein R1, R2and R3are the same or different and each is hydrogen atom, wherein each symbol is as defined in the specification, a salt thereof or a prodrug thereof. The compound of the presen
Antithrombotic agents
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, (2008/06/13)
This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
Oxazolidinone derivatives, processes for the production thereof and pharmaceutical agents containing these compounds
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, (2008/06/13)
The present invention concerns new oxazolidinone derivatives, processes for their production as well as pharmaceutical agents containing these substances. The present invention concerns compounds of the general formula I STR1 in which the symbols have the meanings as listed in the claims.
