Substituted oxazolidinones and their use
View Patent ↗The invention relates to novel substituted oxazolidinones, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.
1. A compound of formula (I):
in which
n represents the number 0, 1, 2 or 3,
R 1 represents chlorine, trifluoromethoxy, methyl, ethyl, n-propyl, methoxy, methoxymethyl or ethoxymethyl, and
R 2 represents hydrogen or methyl,
or a salt thereof.
2. The compound of claim 1 , wherein
n represents the number 0, 1 or 2,
R 1 represents chlorine, trifluoromethoxy, methyl, n-propyl, methoxy or methoxymethyl,
R 2 represents hydrogen or methyl.
3. The compound of claim 1 , wherein
n represents the number 0, 1 or 2,
R 1 represents methyl, methoxy or methoxymethyl,
R 2 represents hydrogen.
4. The compound of claim 1 , wherein
n represents the number 1 or 2,
R 1 represents methyl,
R 2 represents hydrogen.
5. A process for preparing a compound of formula (I), according to claim 1 , comprising
[A] reacting a compound of formula (II):
with a compound of formula (III):
in which n, R 1 and R 2 have the meaning given in claim 1 ,
to give a compound of formula (IV):
in which n, R 1 and R 2 have the meaning given in claim 1 ,
and cyclizing the compound of formula (IV) in the presence of phosgene or phosgene equivalents, to give a compound of formula (I);
or
[B] reacting a compound of formula (V):
in which n, R 1 and R 2 have the meaning given in claim 1 ,
with a compound of formula (VI):
in which
X represents halogen
to give the compound of formula (I).
6. A pharmaceutical composition comprising a compound of claim 1 and an inert nontoxic pharmaceutically acceptable auxiliary.
7. A method of treatment and/or prophylaxis of a thromboembolic disorders comprising administering an anticoagulatory effective amount of at least one compound of claim 1 to a human or animal in need thereof.
8. The method of claim 7 , wherein the thromboembolic disorder is selected from the group consisting of: myocardial infarction with ST segment elevation (STEMI) and without ST segment elevation (non-STEMI), stable angina pectoris, unstable angina pectoris, reocclusions and restenoses after coronary intervention, peripheral arterial occlusion diseases, pulmonary embolisms, deep venous thromboses and kidney venous thromboses, transitory ischaemic attacks, and thrombotic and thromboembolic stroke.