Novel hexahydro-1,4-diazepine derivatives or salts thereof

Details Novel hexahydro-1,4-diazepine derivatives or salts thereof Novel hexahydro-1,4-diazepine derivatives or salts thereof

C - Chemistry, Metallurgy

07

D

C07D 243/08 (2006.01) A61K 31/55 (2006.01) C07D 401/04 (2006.01) C07D 405/12 (2006.01)

Patent

CA 2289572

Hexahydro-1,4-diazepine derivatives represented by general formula (1); pharmaceutically acceptable salts thereof; and drugs containing the same as the active ingredient, such as activated blood coagulation factor X inhibitor, wherein A: phenylene, pyridylene, or the like; B: a 5- or 6-membered aryl or heteroaryl ring; X: -CO-, -CONH-, -CSNH-, SO2-,-SO2NH-, or the like; Y: a bond or alkylene; R1: hydrogen, alkyl, -Y- (hetero)aryl, or the like; R2: hydrogen, alkoxy, -COOH, or the like; R3: amidino or a group capable of being converted into amidino; and R4, R5: each independently hydrogen or lower alkyl.

La présente invention concerne des dérivés d'hexahydro-1,4-diazépine représentés par la formule générale (I), certains de leurs sels pharmaceutiquement admis, et des médicaments dont ils constituent le principe actif en tant que facteur X de coagulation sanguine activé. Dans cette formule générale (I), A est phénylène, pyridylène ou analogue. B est cycle aryle ou hétéroaryle à 5 ou 6 côtés. X est -CO-, -CONH-, -CSNH-, SO¿2?-, SO¿2?NH- ou analogue. Y est liaison ou alkylène. R?1¿ est hydrogène, alkyle, -Y-(hétéro)aryle ou analogue. R?2¿ est hydrogène, alcoxy, -COOH- ou analogue. R?3¿ est amidino ou un groupe capable de se convertir en amidino. R?4¿ et R?5¿ sont chacun indépendamment hydrogène ou alkyle inférieur.

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