US2010267685A1PendingUtilityA1
Methods For The Prophylaxis And/or Treatment Of Thromboembolic Disorders By Combination Therapy With Substituted Oxazolidinones
Est. expiryJun 20, 2021(expired)· nominal 20-yr term from priority
Inventors:Alexander StraubThomas LampeJosef PernerstorferElisabeth PerzbornJens PohlmannSusanne RöhrigKarl-Heinz Schlemmer
A61P 7/12A61P 7/02A61P 9/00A61P 9/10A61P 9/08A61P 43/00A61P 7/00A61K 31/5377A61P 9/04A61K 31/421A61K 31/422A61P 3/06A61K 45/06
44
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Claims
Abstract
The invention relates to combinations of A) oxazolidinones of formula (I) and B) other active ingredients, to a method for producing said combinations and to the use thereof as medicaments, in particular for the treatment and/or prophylaxis of thrombo-embolic diseases.
Claims
exact text as granted — not AI-modified1 - 9 . (canceled)
10 . A method for the prophylaxis and/or treatment of thromboembolic disorders comprising administering to a subject in need thereof an effective amount of a combination comprising
A) at least one compound of the formula (I)
in which
R 1 is 2-thiophene which is substituted in position 5 by a radical selected from chlorine, bromine, methyl and trifluoromethyl,
R 2 is D-A-:
where:
the radical “A” is phenylene;
the radical “D” is a saturated 5- or 6-membered heterocycle which is linked via a nitrogen atom to “A”, and
which has a carbonyl group directly adjacent to the linking nitrogen atom, and
in which a ring carbon member may be replaced by a heteroatom selected from the series S, N and O;
where
the group “A” defined above may optionally be substituted once or twice in the meta position relative to the linkage to the oxazolidinone by a radical selected from fluorine, chlorine, nitro, amino, trifluoromethyl, methyl and cyano,
R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are hydrogen,
or a pharmaceutically acceptable salt or hydrate thereof, or their mixture
and
B) at least one further active pharmaceutical ingredient.
11 . The method of claim 10 , wherein the compound of the formula (I) is 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide of the formula
or a pharmaceutically acceptable salt or hydrate thereof, or their mixture.
12 . The method of claim 10 , wherein the further active pharmaceutical ingredient B) is a platelet aggregation inhibitor, anticoagulant, fibrinolytic, lipid-lowering agent, coronary therapeutic agent and/or vasodilator.
13 . The method of claim 11 , wherein the further active pharmaceutical ingredient B) is a platelet aggregation inhibitor, anticoagulant, fibrinolytic, lipid-lowering agent, coronary therapeutic agent and/or vasodilator.
14 . A method for the prophylaxis and/or treatment of myocardial infarction, angina pectoris, sudden heart death, reocclusions and restenoses after angioplasty or aortocoronary bypass, stroke, transient ischemic attacks, peripheral arterial occlusive diseases, pulmonary embolisms or deep venous thromboses comprising administering to a subject in need thereof an effective amount of a combination comprising
A) at least one compound of the formula (I)
in which
R 1 is 2-thiophene which is substituted in position 5 by a radical selected from chlorine, bromine, methyl and trifluoromethyl,
R 2 is D-A-:
where:
the radical “A” is phenylene;
the radical “D” is a saturated 5- or 6-membered heterocycle which is linked via a nitrogen atom to “A”, and
which has a carbonyl group directly adjacent to the linking nitrogen atom, and
in which a ring carbon member may be replaced by a heteroatom selected from the series S, N and O;
where
the group “A” defined above may optionally be substituted once or twice in the meta position relative to the linkage to the oxazolidinone by a radical selected from fluorine, chlorine, nitro, amino, trifluoromethyl, methyl and cyano,
R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are hydrogen,
or a pharmaceutically acceptable salt or hydrate thereof, or their mixture
and
B) at least one further active pharmaceutical ingredient.
15 . The method of claim 14 , wherein the compound of formula (I) is 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide of the formula
or a pharmaceutically acceptable salt or hydrate thereof, or their mixture.
16 . The method of claim 14 , wherein the further active pharmaceutical ingredient B) is a platelet aggregation inhibitor, anticoagulant, fibrinolytic, lipid-lowering agent, coronary therapeutic agent and/or vasodilator.
17 . The method of claim 15 , wherein the further active pharmaceutical ingredient B) is a platelet aggregation inhibitor, anticoagulant, fibrinolytic, lipid-lowering agent, coronary therapeutic agent and/or vasodilator.
18 . The method of claim 14 , wherein the method is for the prophylaxis and/or treatment of angina pectoris that is unstable angina.
19 . The method of claim 15 , wherein the method is for the prophylaxis and/or treatment of angina pectoris that is unstable angina.Join the waitlist — get patent alerts
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