| abstract |
This refers to mandelic acid derivatives of the formula (1), as well as physiologically acceptable salts thereof. These compounds inhibit the formation of the coagulation factors Xa, IXa and thrombin induced by factor VIIa and the tissue factor and can be used as medicaments. Claim 1: Compounds of the formula (1) wherein R1 is H, -OH, -NH2, (lower alkoxy) -carbonyl, aryl- (lower alkoxy) -carbonyl, aryloxycarbonyl, (lower alkyl) -carbonyl, aryl carbonyl or (lower alkoxy) -carbonyl which is substituted by halogen; R2, R3, and R4 independently of each other are chosen from H, halogen, hydroxy, and lower alkoxy; whose lower alkoxy may be optionally substituted by hydroxy, carboxy or carbamoyl; R5 is lower alkyl or cycloalkyl or, if X is O or NR12, R5 may also be H; R6 is H, lower alkyl or fluorine-lower alkyl; Y is N or C-R11; R7, R8, R9, R10 and R11 independently of each other are chosen from H, hydroxy, halogen, amino, (lower alkyl) -amino, di- (lower alkyl) -amino, (lower alkyl) -carbonyl-amino, NO2 , lower fluorine-alkyl, lower alkoxy, lower hydroxy-alkoxy, lower fluorine-alkoxy, lower alkynyl, lower hydroxy-alkynyl, aryl, aryl-lower alkoxy, aryloxy, aryloxy-lower alkoxy, heterocyclyl, heterocyclyloxy, (lower alkoxy) - lower carbonyl-alkoxy, lower carbamoyl-alkoxy, lower carboxy-alkoxy, cycloalkyloxy, heteroaryl, lower amino-alkoxy, (lower alkyl) -amino-lower alkoxy and di- (lower alkyl) -amino-lower alkoxy; or R8 and R9 or R8 and R7 are linked together to form a ring together with the C atoms to which they are attached and R8 and R9 together or R8 and R7 together are -O-CH2-O-, -O-CH2 -CO-NH-, -O-CH2-CH2-CH2- or -CH = CH-CH = CH-, which may eventually be substituted by lower alkyl or lower alkoxy and R10, R11 and R7 or R9 respectively have the meanings defined previously; X is O, S, NR12 or SO2; R12 is H, lower alkyl or (lower alkyl) -carbonyl; and pharmaceutically acceptable salts thereof. Claim 37: The use of the compounds according to any one of claims 1-26 for the manufacture of medicaments for the therapeutic and / or prophylactic treatment of arterial and venous thrombosis, deep vein thrombosis, pulmonary embolism, unstable angina pectoris, infarction heart, stroke due to atrial fibrillation, inflammation, arteriosclerosis and / or tumors. |