Benzene derivative or salt thereof

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 211/74 (2006.01) A61K 31/435 (2006.01) A61K 31/44 (2006.01) A61K 31/4433 (2006.01) A61K 31/4436 (2006.01) A61K 31/444 (2006.01) A61K 31/4545 (2006.01) A61K 31/496 (2006.01) A61K 31/506 (2006.01) A61K 31/5377 (2006.01) A61K 31/541 (2006.01) A61K 31/553 (2006.01) A61P 7/02 (2006.01) A61P 9/10 (2006.01) A61P 9/14 (2006.01) A61P 11/00 (2006.01) A61P 31/16 (2006.01) C07D 213/64 (2006.01) C07D 213/75 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01) C07D 405/12 (2006.01) C07D 405/14 (2006.01) C07D 409/12

Patent

CA 2628963

Problem: To provide compounds which have an anticoagulation effect based on their ability to inhibit the activated blood coagulation factor X and are useful as coagulation inhibitors or agents for prevention or treatment for diseases caused by thrombi or emboli. Means for Solution: Benzene derivatives or their salts having a characteristic chemical structure with a phenol ring and a benzene ring bonding to each other via an amide bond, in which the phenol ring further bonds to a benzene ring or a heteroaryl ring via an amide bond. They have an excellent effect of inhibiting the activated blood coagulation factor X, and especially have an excellent oral activity.

L~invention concerne un composé présentant une activité anticoagulante se fondant sur l'inhibition d'un facteur X de coagulation sanguine activé et étant utile en tant qu'inhibiteur de la coagulation sanguine ou en tant qu~agent thérapeutique ou préventif d~une maladie provoquée par un thrombus ou une embole. Le composé selon l~invention consiste en un dérivé de benzène caractérisé en ce qu~il présente une structure chimique selon laquelle un cycle phénolique et un cycle benzénique sont reliés par une liaison amide, le cycle phénolique étant également lié à un cycle benzénique ou à un cycle hétéroarylique par une liaison amide, ou un sel de ce dérivé de benzène. Ces composés présentent une excellente action d~inhibition du facteur X de coagulation sanguine activé et notamment une excellente activité orale.

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