Substituted oxazolidinones for combinational therapy

• US 20040242660A1
• Filed: 06/28/2004
• Published: 12/02/2004
• Est. Priority Date: 06/20/2001
• Status: Active Grant

• Current Assignee: Bayer Intellectual Property GmbH (Bayer AG)
• Original Assignee: Bayer Schering Pharma AG (Bayer AG)
• Inventors: Lampe, Thomas, Pernerstorfer, Josef, Perzborn, Elisabeth, Schlemmer, Karl-Heinz, Straub, Alexander, Pohlmann, Jens, Rohrig, Susanne
• Granted Patent: US 7,767,702 B2
• Time in Patent Office: Days
• US Class Current: 514/376
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/421 1,3-Oxazoles, e.g. pemoline, trimethadione
• CPC Class Codes: A61K 31/422 not condensed and containing further heterocyclic rings
• CPC Class Codes: A61K 31/5377 not condensed and containing further heterocyclic rings, e.g. timolol
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 7/00 Drugs for disorders of the blood or the extracellular fluid
• CPC Class Codes: A61P 7/02 Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
• CPC Class Codes: A61P 7/12 Antidiuretics, e.g. drugs for diabetes insipidus ADH A61P5/10
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/04 Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
• CPC Class Codes: A61P 9/08 Vasodilators for multiple indications
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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

1. A combination comprising

A) at least one compound of the formula (I)

in which

R¹ is 2-thiophene which is substituted in position 5 by a radical from the group of chlorine, bromine, methyl or trifluoromethyl,

R² 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”

,

which has a carbonyl group in direct vicinity to the linking nitrogen atom, and

in which a ring carbon member may be replaced by a heteroatom 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 from the group of fluorine, chlorine, nitro, amino, trifluoromethyl, methyl or cyano,

R³, R⁴, R⁵, R⁶, R⁷ and R⁸ are hydrogen,

the pharmaceutically acceptable salts, hydrates, prodrugs thereof for mixtures thereof

and

B) at least one further active pharmaceutical ingredient.

2. A combination as claimed in claim 1, characterized in that the compound A) 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

3. A combination as claimed in claim 1 or 2, whose further active pharmaceutical ingredients B) are platelet aggregation inhibitors, anticoagulants, fibrinolytics, lipid-lowering agents, coronary therapeutic agents and/or vasodilators.

4. A process for producing the combinations as claimed in claims 1 to 3, characterized in that oxazolidinones of the formula (I) and combination active ingredients are combined or prepared in a suitable way.

5. A combination as claimed in claims 1 to 3 for the prophylaxis and/or treatment of disorders.

6. A medicament comprising at least one combination as claimed in claims 1 to 3 and, where appropriate, further active pharmaceutical ingredients.

7. A medicament comprising at least one combination as claimed in claims 1 to 3 and one or more pharmacologically suitable excipients and/or carriers.

8. The use of combinations of claims 1 to 3 for producing a medicament for the prophylaxis and/or treatment of thromboembolic disorders.

9. The use of combinations of claims 1 to 3 for producing a medicament for the prophylaxis and/or treatment of myocardial infarction, angina pectoris (including unstable angina), 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.