Carboxymide derivatives and their use in the treatment of...

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C - Chemistry, Metallurgy

07

C

C07C 317/32 (2006.01) A61K 31/175 (2006.01) A61K 31/381 (2006.01) A61K 31/4172 (2006.01) A61K 31/4402 (2006.01) C07C 271/28 (2006.01) C07C 275/28 (2006.01) C07C 275/30 (2006.01) C07C 275/42 (2006.01) C07C 311/45 (2006.01) C07C 311/46 (2006.01) C07C 323/52 (2006.01) C07C 323/60 (2006.01) C07D 207/27 (2006.01) C07D 209/20 (2006.01) C07D 211/20 (2006.01) C07D 211/58 (2006.01) C07D 211/76 (2006.01) C07D 213/56 (2006.01) C07D 213/64 (2006.01) C07D 213/75 (2006.01) C07D 223/10 (2006.01) C07D 233/54 (2006.01) C07D

Patent

CA 2431766

The invention relates to compounds of formula (I), wherein the variables have the following meanings: D means a phenyl or a pyridyl which is unsubstituted or is mono- or polysubstituted by Hal, A, OR2, N(R2)2, NO2, CN, COOR2 or CON(R2)2; R1 means H, Ar, Het, cycloalkyl or A, which can be substituted by OR2, SR2, N(R2)2, Ar, Het, cycloalkyl, CN, COOR2 or CON(R2)2; R2 means H or A, E means phenylene which can be mono- or polysubstituted by Hal, A, OR2, N(R2)2, NO2, CN, COOR2 or CON(R2)2 or piperidin-1,4-diyl, W means AR, Het or N(R2)2 and if E=piperidin-1,4-diyl, also R2 or cycloalkyl; and X means NH or O. These compounds are inhibitors of the coagulation factor Xa and can be used for the prevention and/or therapy of thromboembolic diseases and for treating tumours.

Composés de formule (I) dans laquelle les variables ont les désignations suivantes : D : phényle ou pyridyle non substitué ou substitué une ou plusieurs fois par hal, A, OR?2¿, N(R?2¿)¿2?, NO¿2?, CN, COOR?2¿ ou CON(R?2¿)¿2?; R?1¿ : H, Ar, Het, cycloalkyle ou A, pouvant être substitué par OR?2¿, SR?2¿, N(R?2¿)¿2?, Ar, Het, cycloalkyle, CN, COOR?2¿ ou CON(R?2¿)¿2?; R?2¿ : H ou A; E : phénylène pouvant être substitué une ou plusieurs fois par hal, A, OR?2¿, N(R?2¿)¿2?, NO¿2?, CN, COOR?2¿ ou CON(R?2¿)¿2? ou pipéridine-1,4-diyle, W : AR, Het ou N(R?2¿)¿2?, et, dans le cas où E=pipéridine-1, 4-diyle, également R?2¿ ou cycloalkyle, X ; NH ou O. Les composés selon l'invention sont des inhibiteurs du facteur de coagulation Xa et peuvent être utilisés pour la prophylaxie et la thérapie de troubles thrombo-emboliques et pour le traitement de tumeurs.

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