US2010267685A1PendingUtilityA1

Methods For The Prophylaxis And/or Treatment Of Thromboembolic Disorders By Combination Therapy With Substituted Oxazolidinones

Assignee: BAYER SCHERING PHARMA AGPriority: Jun 20, 2001Filed: Apr 23, 2010Published: Oct 21, 2010
Est. expiryJun 20, 2021(expired)· nominal 20-yr term from priority
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-modified
1 - 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.

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