3-amidinobenzenesulfonamide derivatives, medicinal...

C - Chemistry – Metallurgy – 07 – C

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C07C 311/46 (2006.01) A61K 31/18 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) A61P 7/02 (2006.01) A61P 43/00 (2006.01) C07C 311/16 (2006.01) C07C 311/17 (2006.01) C07C 311/19 (2006.01) C07C 311/29 (2006.01) C07D 207/12 (2006.01) C07D 211/26 (2006.01) C07D 211/28 (2006.01) C07D 211/46 (2006.01)

Patent

CA 2368623

3-Amidinobenzenesulfonamide derivatives represented by general formula (I), which have an excellent effect of inhibiting activated blood coagulation factor X activity and thus are useful as activated blood coagulation factor X inhibitor, or pharmacologically acceptable salts thereof, medicinal compositions containing the same and intermediates in the production thereof: wherein R1 represents hydrogen or hydroxy; Y represents a single bond or oxygen; and R2 represents lower alkyl or a group represented by general formula (a): [wherein n is 1 or 2; and T represents hydrogen, lower acyl, halogenated lower acyl or -C(=NH)-W (wherein W represents a lower alkyl)].

L'invention concerne des dérivés de 3-amidinobenzènesulfonamide représentés par la formule générale (I), ces dérivés, qui inhibent efficacement l'action du facteur X de coagulation sanguine activé, faisant office d'inhibiteurs de ce facteur X de coagulation sanguine activé. L'invention concerne également des sels pharmaceutiquement acceptables de ces dérivés, des compositions médicales qui les contiennent, et des produits intermédiaires servant à leur élaboration. Dans cette formule, R?1¿ représente hydrogène ou hydroxy; Y désigne une liaison simple ou oxygène; et R?2¿ symbolise alkyle inférieur ou un groupe représenté par la formule générale (a) [dans laquelle n est égal à 1 ou 2; et T représente hydrogène, acyle inférieur, acyle inférieur halogéné, ou C(=NH)-W (W désignant un alkyle inférieur)].

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