Substituted phenylamidines medicaments containing said compounds and method for production thereof
View Patent ↗The present invention relates to phenylamidines of general formula wherein R 6 and R 7 are defined as in claim 1, the tautomers, the stereoisomers including mixtures thereof and the salts thereof, particularly their physiologically acceptable salts with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably antithrombotic effects, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
1. A compound of formula (I):
wherein
R 6 denotes a hydroxy, C 6-12 -alkyloxcarbonyl or, phenylcarbonyl or, and
R 7 denotes C 1-8 -alkyl, C 5-7 -cycloalkyl or phenyl-C 1-4 -alkyl group
or a tautomer, stereoisomer or salt thereof.
2. A compound according to claim 1 , selected from:
(1) 4-[2-[[4-octyloxycarbonylamidino)phenyl]aminocarbonyl]-ethyl]-1-[(ethoxycarbonyl)methyl]-piperazine,
(2) 4-[2-[[4-(hexyloxycarbonylamidino)phenyl]aminocarbonyl]-ethyl]-1-[(ethoxycarbonyl)methyl]-piperazine,
(3) 4-[2-[[4-(benzoylamidino)phenyl]aminocarbonyl]-ethyl]-1-[(ethoxycarbonyl)methyl]-piperazine, and
(4) 4-[2-[[4-(hydroxyamidino)phenyl]aminocarbonyl]-ethyl]-1-[(ethoxycarbonyl)methyl]-piperazine
and the salts thereof.
3. A compound according to claim 1 , selected from:
4-[2-[[4-(octyloxycarbonylamidino)phenyl]aminocarbonyl]-ethyl]-1-[(ethoxycarbonyl)methyl]-piperazine and the salts thereof.
4. A compound according to claim 1 , selected from:
4-[2-[[4-(hexyloxycarbonylamidino)phenyl]aminocarbonyl]-ethyl]-1-[(ethoxycarbonyl)methyl]-piperazine and the salts thereof.
5. A physiologically acceptable salt of a compound according to claim 1 with an inorganic or organic acid or base.
6. A pharmaceutical composition comprising a compound according to claim 1 and optionally one or more inert carriers and/or diluents.
7. A pharmaceutical composition comprising a physiologically acceptable salt according to claim 5 and optionally one or more inert carriers and/or diluents.
8. A method for treating a disease or condition selected from: venous and arterial thromboses, pulmonary embolism, cardiac infarct, arteriosclerosis, comprising administering to a patient in need thereof a therapeutically effective amount of a compound according to claim 1 .