IP Library Granted Patent US 7,081,470
Granted Patent B2
US 7,081,470 · App. 10/414,660 · Granted Jul 25, 2006

Use of GALR3 receptor antagonists for the treatment of depression and/or anxiety and compounds useful in such methods

Assignee: H. Lundbeck A/S
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Quick Facts
Patent No.
US 7,081,470
App. No.
10/414,660
Granted
Jul 25, 2006
Kind
B2
Abstract

This invention is directed to indolone derivatives which are antagonists for the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.

Claims (21)

1. A compound having the structure:

wherein each of Y 1 , Y 2 , Y 3 , and Y 4 is independently —H; straight chained or branched C 1 –C 7 alkyl, —CF 3 , —F, —Cl, —Br, —I, —OR 4 , —N(R 4 ) 2 or —CON(R 4 ) 2 ;

wherein each R 4 is independently —H; straight chained or branched C 1 –C 7 alkyl, monfluoroalkyl or polyfluoroalkyl; straight chained or branched C 2 –C 7 alkenyl or alkynyl; C 3 –C 7 cycloalkyl, C 5 –C 7 cycloalkenyl, aryl or aryl(C 1 –C 6 ) alkyl;

wherein B is aryl;

wherein A is aryl, substituted with —OH; or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein each of Y 1 , Y 2 , Y 3 and Y 4 is independently H or —OR 4 .

3. The compound of claim 2 , wherein A is naphthyl substituted with —OH.

4. The compound of claim 2 , wherein A is phenyl substituted with —OH.

5. A compound having the following structure:

6. A pure Z imine isomer of the compound of claim 1 .

7. A pure E imine isomer of the compound of claim 1 .

8. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1 and a pharmaceutically acceptable carrier.

9. A process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of claim 1 and a pharmaceutically acceptable carrier.

10. A method of treating a subject suffering from depressioh which comprises administering to the subject an amount of the compound of claim 1 effective to treat the subject.

11. A method of treating a subject suffering from anxiety which comprises administering to the subject an amount of the compound of claim 1 effective to treat the subject.

12. A method of treating a subject suffering from depression and anxiety which comprises administering to the subject an amount of the compound of claim 1 effective to treat the subject.

13. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 5 and a pharmaceutically acceptable carrier.

14. A process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of claim 5 and a pharmaceutically acceptable carrier.

15. A method of treating a subject suffering from depression which comprises administering to the subject an amount of the compound of claim 5 effective to treat the subject.

16. A method of treating a subject suffering from anxiety which comprises administering to the subject an amount of the compound of claim 5 effective to treat the subject.

17. A method of treating a subject suffering from depression and anxiety which comprises administering to the subject an amount of the compound of claim 5 effective to treat the subject.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 13, 2004
From: SYNAPTIC PHARMACEUTICAL CORPORATION
To: H. LUNDBECK A/S
Reel/Frame 015156/0196 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 9, 2004
From: KONKEL, MICHAEL; WETZEL, JOHN M.; TALISMAN, JAMIE
To: SYNAPTIC PHARMACEUTICAL CORPORATION
Reel/Frame 014955/0878 →
Continuity (4)
Continuation In Part 1021487300 · Aug 7, 2002
Continuation In Part 1006617500 · Jan 31, 2002
Provisional Application 6026558600 · Jan 31, 2001
Related Publication 20040102507A1 · May 27, 2004