IP Library Granted Patent US 7,994,156
Granted Patent B2
US 7,994,156 · App. 12/745,530 · Granted Aug 9, 2011

Carboxylic acid 4-phenylazo-phenyl ester derivatives and their use as monoamine neurotransmitter re-uptake inhibitors

Assignee: Neurosearch A/S
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Quick Facts
Patent No.
US 7,994,156
App. No.
12/745,530
Granted
Aug 9, 2011
Kind
B2
Abstract

This invention relates to novel carboxylic acid 4-phenylazo-phenyl ester derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Claims (52)

1. A compound of Formula I:

any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein

Q represents a phenyl group;

which phenyl group is optionally substituted with one or more substituents independently selected from the group consisting of:

halo, trifluoromethyl, trifluoromethoxy, cyano and alkoxy;

n is 0 or 1;

R 1 represents hydrogen or alkyl; and

either R 2 and R 3 together form —CH 2 —CH 2 —, —CH 2 —CH 2 —CH 2 — or —CH 2 —CH 2 —CH 2 —CH 2 —; and R 4 represents hydrogen;

or R 1 and R 4 together form —CH 2 —CH 2 —; and R 3 represents hydrogen;

or R 2 , R 3 and R 4 each represent hydrogen.

2. The compound according to claim 1 , any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein

n is 1;

R 1 and R 4 together form —CH 2 —CH 2 —; and

R 3 represents hydrogen.

3. The compound according to claim 1 , any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein

n is 0; and

R 2 and R 3 together form —CH 2 —CH 2 —.

4. The compound according to claim 1 , any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein

n is 0; and

R 2 and R 3 together form —CH 2 —CH 2 —CH 2 —.

5. The compound according to claim 1 , any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein

n is 0; and

R 2 and R 3 together form —CH 2 —CH 2 —CH 2 —CH 2 —.

6. The compound according to claim 1 , any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein

n is 1;

R 2 and R 3 together form —CH 2 —CH 2 —; and

R 4 represents hydrogen.

7. The compound according to claim 1 , any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein

n is 1;

R 2 and R 3 together form —CH 2 —CH 2 —CH 2 —; and

R 4 represents hydrogen.

8. The compound according to claim 1 , any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein

n is 0; and

R 2 and R 3 each represent hydrogen.

9. The compound according to claim 1 , any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein

n is 1; and

R 2 and R 3 each represent hydrogen.

10. The compound according to claim 1 , any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein

R 1 represents alkyl.

11. The compound according to claim 1 , any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, wherein

Q represents phenyl.

12. The compound according to claim 1 , selected from the group consisting of

1,4-Diaza-bicyclo[3.2.2]nonane-4-carboxylic acid 4-phenylazo-phenyl ester;

9-Methyl-3,9-diaza-bicyclo[3.3.1]nonane-3-carboxylic acid 4-phenylazo-phenyl ester;

4-Methyl-piperazine-1-carboxylic acid 4-phenylazo-phenyl ester;

4-Methyl-[1,4]diazepane-1-carboxylic acid 4-phenylazo-phenyl ester;

8-Methyl-3,8-diaza-bicyclo[3.2.1]octane-3-carboxylic acid 4-phenylazo-phenyl ester;

10-Methyl-8,10-diaza-bicyclo[4.3.1]decane-8-carboxylic acid 4-phenylazo-phenyl ester;

10-Methyl-3,10-diaza-bicyclo[4.3.1]decane-3-carboxylic acid 4-phenylazo-phenyl ester;

and

9-Methyl-3,9-diaza-bicyclo[4.2.1]nonane-3-carboxylic acid 4-phenylazo-phenyl ester; or any of its stereoisomers or any mixture of its stereoisomers or a pharmaceutically acceptable salt thereof.

13. A pharmaceutical composition, comprising a therapeutically effective amount of a compound according to claim 1 , any of its stereoisomers or any mixture of its stereoisomers, or a pharmaceutically acceptable salt thereof, together with at least one pharmaceutically acceptable carrier, excipient or diluent.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 20, 2013
From: NEUROSEARCH A/S
To: ANIONA APS
Reel/Frame 030049/0894 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 18, 2010
From: PETERS, DAN; REDROBE, JOHN PAUL; NIELSEN, ELSEBET OSTERGAARD
To: NEUROSEARCH A/S
Reel/Frame 024853/0861 →
Priority Claims (1)
DK 2007 01715 · Nov 30, 2007 · national
Continuity (1)
Related Publication 20100311699A1 · Dec 9, 2010