IP Library Granted Patent US 7,432,258
Granted Patent B2
US 7,432,258 · App. 11/780,584 · Granted Oct 7, 2008

Morpholinyl and pyrrolidinyl analogs

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Quick Facts
Patent No.
US 7,432,258
App. No.
11/780,584
Granted
Oct 7, 2008
Kind
B2
Abstract

The present invention relates to 4′-[(1R)-1-[[(6,7-dichloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin- 4-yl)acetyl](methyl)amino]-2-(4-morpholinyl)ethyl]-4-biphenylcarboxylic acid and its pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.

Claims (10)

1. A compound which is 4′-[(1R)-1-[[(6,7-dichloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetyl](methyl)amino]-2-(4-morpholinyl)ethyl]-4-biphenylcarboxylic acid; or a pharmaceutically acceptable salt thereof.

2. A compound of claim 1 which is 4′-[(1R)-1-[[(6,7- dichloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetyl](methyl)amino]-2-(4-morpholinyl)ethyl]-4-biphenylcarboxylic acid HCL salt.

3. A compound of claim 1 which is 4′-[(1R)-1-[[(6,7-dichloro-3-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetyl](methyl)amino]-2-(4-morpholinyl)ethyl]-4-biphenylcarboxylic acid Trifluoroacetate salt.

4. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier or excipient.

5. A pharmaceutical composition comprising a compound of claim 2 and a pharmaceutically acceptable carrier or excipient.

6. A pharmaceutical composition comprising a compound of claim 3 and a pharmaceutically acceptable carrier or excipient.

7. A method of treating congestive heart failure, ischemic heart disease, angina, myocardial ischemia, overactive bladder, or cardiac arrhythmia which comprises administering to a patient in need thereof, a compound of claim 1 .

8. A method of treating hypertension which comprises administering to a patient in need thereof, a compound of claim 1 .

9. A method of treating hypertension which comprises administering to a patient in need thereof, a compound of claim 2 .

10. A method of treating hypertension which comprises administering to a patient in need thereof, a compound of claim 3 .

Assignments (2)
CHANGE OF NAME Recorded Jan 6, 2010
From: SMITHKLINE BEECHAM CORPORATION
To: GLAXOSMITHKLINE LLC
Reel/Frame 023731/0761 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 21, 2008
From: GOODMAN, KRISTA B.; NEEB, MICHAEL J.; SEHON, CLARK A.; VIET, ANDREW Q.; WANG, GREN Z.
To: SMITHKLINE BEECHAM CORPORATION
Reel/Frame 021422/0119 →