IP Library Granted Patent US 7,781,456
Granted Patent B2
US 7,781,456 · App. 11/793,137 · Granted Aug 24, 2010

Enantiomers of 3-heteroaryl-8H-8-azabicyclo(3.2.1)oct-2-ene and their use as monoamine neurotransmitter re-uptake inhibitors

Assignee: Neurosearch A/S
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Quick Facts
Patent No.
US 7,781,456
App. No.
11/793,137
Granted
Aug 24, 2010
Kind
B2
Abstract

This invention relates to novel enantiomers 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 (26)

1. An enantiopure chemical compound or a pharmaceutically acceptable salt thereof, wherein said compound is 3-(2-benzothienyl)-8H-8-azabicyclo[3.2.1]oct-2-ene.

2. An enantiopure chemical compound of

3-(7-fluoro-benzo[b]thiophen-2-yl)-8-aza-bicyclo[3.2.1]oct-2-ene;

3-(7-chloro-benzo[b]thiophen-2-yl)-8-aza-bicyclo[3.2.1]oct-2-ene;

3-(2-benzothienyl)-8-methyl-8-azabicyclo[3.2.1]oct-2-ene;

3-(7-fluoro-benzo[b]thiophen-2-yl)-8-methyl-8-aza-bicyclo[3.2.1]oct-2-ene;

or a pharmaceutically acceptable salt thereof.

3. The chemical compound of claim 1 , being enantiopure (+)-3-(2-benzothienyl)-8H-8-azabicyclo[3.2.1]oct-2-ene;

or a pharmaceutically acceptable salt thereof.

4. The chemical compound of claim 1 , being enantiopure (−)-3-(2-benzothienyl)-8H-8-azabicyclo[3.2.1]oct-2-ene;

or a pharmaceutically acceptable salt thereof.

5. The chemical compound of claim 2 , being

enantiopure (+)-3-(7-fluoro-benzo[b]thiophen-2-yl)-8-aza-bicyclo[3.2.1]oct-2-ene;

enantiopure (−)-3-(7-fluoro-benzo[b]thiophen-2-yl)-8-aza-bicyclo[3.2.1]oct-2-ene;

enantiopure (−)-3-(7-chloro-benzo[b]thiophen-2-yl)-8-aza-bicyclo[3.2.1]oct-2-ene;

enantiopure (+)-3-(2-benzothienyl)-8-methyl-8-azabicyclo[3.2.1]oct-2-ene;

enantiopure (+)-3-(2-benzothienyl)-8-methyl-8-azabicyclo[3.2.1]oct-2-ene;

enantiopure (+)-3-(7-fluoro-benzo[b]thiophen-2-yl)-8-methyl-8-aza-bicyclo[3.2.1]oct-2-ene;

enantiopure (−)-3-(7-fluoro-benzo[b]thiophen-2-yl)-8-methyl-8-aza-bicyclo[3.2.1]oct-2-ene;

or a pharmaceutically acceptable salt thereof.

6. A pharmaceutical composition, comprising a therapeutically effective amount of a compound of claim 2 , or a pharmaceutically acceptable salt thereof, together with at least one pharmaceutically acceptable carrier, excipient or diluent.

7. A method for treatment of a disease or a disorder or a condition of a living animal body, including a human, which disorder, disease, or condition is depression or pain, which method comprises the step of administering to the living animal body in need thereof a therapeutically effective amount of a compound according to claim 2 , or a pharmaceutically acceptable salt thereof.

8. The chemical compound of claim 2 or the pharmaceutically acceptable salt thereof, wherein the enantiopure compound is in enantiomeric excess of at least 99.0% over the opposite enantiomer.

9. A pharmaceutical composition, comprising a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof, together with at least one pharmaceutically acceptable carrier, excipient or diluent.

10. A method for treatment of a disease or a disorder or a condition of a living animal body, including a human, which disorder, disease, or condition is depression or pain, which method comprises the step of administering to the living animal body in need thereof a therapeutically effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof.

11. The chemical compound of claim 1 or the pharmaceutically acceptable salt thereof, wherein the enantiopure compound is in enantiomeric excess of at least 99.0% over the opposite enantiomer.

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 14, 2007
From: PETERS, DAN; BROWN, DAVID TRISTAM; EGESTAD (DECEASED), BORJE; DAM, EVA; JONES, DAVID SPENCER; FROSTRUP, BRIAN; NIELSEN, ELSEBET OSTERGAARD; OLSEN, GUNNAR M.; REDROBE, JOHN PAUL; TAURIO (LEGAL REPRESENTATIVE), SINIKKA MARJATTA
To: NEUROSEARCH A/S
Reel/Frame 019693/0078 →
Priority Claims (2)
DK 2004 01950 · Dec 17, 2004 · national
DK 2005 00506 · Apr 8, 2005 · national
Continuity (3)
Provisional Application 6063686900 · Dec 20, 2004
Provisional Application 6066988700 · Apr 11, 2005
Related Publication 20080214820A1 · Sep 4, 2008