DERIVATIVES OF 5-AMIDINO-2-HYDROXYBENZENESULFONAMIDE, PHARMACEUTICAL COMPOSITIONS COMPRISING THEREOF AND INTERMEDIATE COMPOUNDS FOR THEIR PREPARING Russian patent published in 2006 - IPC C07C311/37 C07D317/32 C07D277/28 C07D271/10 A61K31/18 A61K31/5375 A61K31/4245 A61K31/426 A61P7/02 A61P9/10 

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to derivatives of 5-amidino-2-hydroxybenzenesulfonamide of the general formula (I): wherein R² means hydrogen atom (H), lower alkyl that can comprise a substitute chosen from the group (A): wherein (A) means -COOR^A, -CONR^BR^C, 3-7-membered monocyclic heterocycloalkyl group comprising one or two heteroatom in ring chosen from atoms N, O, S that can comprise oxo-group and 5-6-membered monocyclic aromatic heterocyclic group comprising one-three heteroatoms in ring chosen from atoms N, O, S that can comprise oxo-group or lower alkyl wherein R^A means hydrogen atom (H), 3-7-membered monocyclic aliphatic alkyl group, lower alkyl that can comprises a substitute chosen from the group (i) wherein (i) means -COOR^A1 wherein R^A1 means hydrogen atom (H), -OCOR^A2 wherein R^A2 means lower alkyl group, -OCOOR^A3 wherein R^A3 means lower alkyl, -OR^A4 wherein R^A4 means hydrogen atom (H), lower alkyl -CONR^A5R^A6 wherein R^A5 and R^A6 mean independently hydrogen atom (H), lower alkyl, or -NR^A5R^A6 forms 5-6-membered monocyclic amino-group comprising one heteroatom in ring chosen from atoms N, O, S and another one distinct from nitrogen atom (N) instead a bond; wherein R^B and R^C mean independently hydrogen atom (H), lower alkyl that can comprise a substitute chosen from the group (ii), or -NR^BR^C forms 5-6-membered monocyclic amino-group comprising one heteroatom in ring chosen from atoms N, O, S and another one distinct from nitrogen atom (N) instead a bond; (ii) means -COOR^B1 wherein R^B1 means hydrogen atom (H), lower alkyl; T means oxygen atom (O), sulfonyl group; or TR¹ means -SO₂NR^B3R^C3 wherein R^B3 and R^C3 means independently hydrogen atom (H), lower alkyl; R² means lower alkyl, phenyl that can comprise one-three substitutes chosen from the group (B) wherein (B) means halogen atom, -COOR^E, sulfamoyl, lower alkylsulfonyl wherein R^E means lower alkyl; Q means hydrogen atom (H), lower alkyl that can comprise a substitute chosen from the group (D) wherein (D) means 5-6-membered monocyclic aromatic heterocyclic group that can comprise one-three heteroatom chosen from atoms N, O, S that can comprise a substitute chosen from the group (iv) wherein (iv) means oxo-group, lower alkyl; Z means hydrogen atom (H), hydroxyl group (OH), -COOR^N wherein R^N means lower alkyl that can comprise a substitute chosen from the group (viii) wherein (viii) means -OCOR⁵ wherein R^N5 means lower alkyl that can comprise -OCOR^N51 wherein R^N51 means lower alkyl; or its pharmaceutically acceptable salt. Compounds of the formula (I) inhibit activated factor X in blood coagulation system that allows their using in pharmaceutical composition. Also, invention describes intermediate compounds.

EFFECT: valuable medicinal properties of compounds and compositions.

12 cl, 5 tbl