IP Library Granted Patent US 8,227,464
Granted Patent B2
US 8,227,464 · App. 13/189,003 · Granted Jul 24, 2012

Substituted oxazolidinone derivatives

Assignee: Concert Pharmaceuticals, Inc.
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Quick Facts
Patent No.
US 8,227,464
App. No.
13/189,003
Granted
Jul 24, 2012
Kind
B2
Abstract

This invention relates to novel compounds that are substituted oxazolidinones derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel oxazolidinones compounds that are derivatives of rivaroxaban. The invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and condition that are beneficially treated by administering a selective inhibitor of factor Xa, such as rivaroxaban.

Claims (8)

1. A method of inhibiting the activity of coagulation factor Xa in a cell, comprising contacting the cell with a compound of Formula I:

or a pharmaceutically acceptable salt thereof, wherein each of X 1a , X 1b , X 2a , X 2b , X 3a , and X 3b is deuterium; and Y 1a , and Y 1b are the same and are selected from hydrogen and deuterium.

2. A method of a therapeutic treatment of a disease selected from pulmonary embolism, stroke, thromboembolism, deep venous thrombosis, thrombosis, myocardial infraction, acute coronary syndrome, disorders of coagulation, microangiopathy and thrombocytopenic purpura in a patient in need thereof comprising administering to said patient an effective amount of a compound of Formula I:

or a pharmaceutically acceptable salt thereof, wherein each of X 1a , X 1b , X 2a , X 2b , X 3a , and X 3b is deuterium; and Y 1a , and Y 1b are the same and are selected from hydrogen and deuterium.

3. The method of claim 2 , wherein the disease is selected from pulmonary embolism, stroke, thromboembolism, deep venous thrombosis, thrombosis, myocardial infarction and acute coronary syndrome.

4. The method of claim 2 , comprising the additional step of co-administering to the patient in need thereof a therapeutic agent useful in the treatment of a disease selected from pulmonary embolism, stroke, thromboembolism, deep venous thrombosis, thrombosis, myocardial infarction, acute coronary syndrome, disorders of coagulation, microangiopathy and thrombocytopenic purpura.

5. The method of claim 3 , comprising the additional step of co-administering to the patient in need thereof a therapeutic agent useful in the treatment of a disease selected from pulmonary embolism, stroke, thromboembolism, deep venous thrombosis, thrombosis, myocardial infarction, acute coronary syndrome, disorders of coagulation, microangiopathy and thrombocytopenic purpura.

6. The method of claim 4 , wherein the disease being treated is acute coronary syndrome; and the therapeutic agent is aspirin.

Assignments (1)
MERGER Recorded Aug 2, 2023
From: CONCERT PHARMACEUTICALS, INC.
To: SUN PHARMACEUTICAL INDUSTRIES, INC.
Reel/Frame 064465/0383 →
Continuity (3)
Division 12228662 · Aug 14, 2008
Provisional Application 60964693 · Aug 14, 2007
Related Publication 20110281828A1 · Nov 17, 2011