IP Library Granted Patent US 7,897,611
Granted Patent B2
US 7,897,611 · App. 12/714,014 · Granted Mar 1, 2011

Pharmaceutical compositions and methods for relieving pain and treating central nervous system disorders

Assignee: Targacept, Inc.
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Quick Facts
Patent No.
US 7,897,611
App. No.
12/714,014
Granted
Mar 1, 2011
Kind
B2
Abstract

Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.

Claims (43)

1. A method for the treatment of pain comprising administration of a compound of Formulae 1 or 2:

wherein

k and p are each 1;

m and n are individually 0 or 1;

provided that if m is 1, then n is 0, and if n is 1, then m is 0;

Ar is pyridine, optionally substituted at any position with a substituent Z is selected from the group consisting of lower alkyl, lower alkenyl, cycloalkyl, phenyl, benzyl, halo, —OR′, —NR′R″, —CF 3 , —CN, —NO 2 , —C≡CR′, —SR′, and —SO 2 R′;

where R′ and R″ are individually hydrogen, lower alkyl, cycloalkyl, phenyl, or benzyl,

and

R is hydrogen, unsubstituted lower alkyl, unsubstituted arylalkyl, unsubstituted alkoxycarbonyl, or unsubstituted aryloxycarbonyl;

or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein the compound is selected from:

6-(3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

7-(3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

6-(3-pyridinyl)-3-azabicyclo[3.3.1]nonane,

7-(3-pyridinyl)-3-azabicyclo[3.3.1]nonane,

6-(5-methoxy-3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

7-(5-methoxy-3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

6-(5-methoxy-3-pyridinyl)-3-azabicyclo[3.3.1]nonane,

7-(5-methoxy-3-pyridinyl)-3-azabicyclo[3.3.1]nonane,

6-(6-methoxy-3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

7-(6-methoxy-3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

6-(6-methoxy-3-pyridinyl)-3-azabicyclo[3.3.1]nonane,

7-(6-methoxy-3-pyridinyl)-3-azabicyclo[3.3.1]nonane,

6-(5-isopropoxy-3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

7-(5-isopropoxy-3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

6-(5-isopropoxy-3-pyridinyl)-3-azabicyclo[3.3.1]nonane,

7-(5-isopropoxy-3-pyridinyl)-3-azabicyclo[3.3.1]nonane,

6-(5-phenoxy-3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

7-(5-phenoxy-3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

6-(5-phenoxy-3-pyridinyl)-3-azabicyclo[3.3.1]nonane,

7-(5-phenoxy-3-pyridinyl)-3-azabicyclo[3.3.1]nonane,

6-(5-phenyl-3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

7-(5-phenyl-3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

6-(5-phenyl-3-pyridinyl)-3-azabicyclo[3.3.1]nonane,

7-(5-phenyl-3-pyridinyl)-3-azabicyclo[3.3.1]nonane,

6-(6-chloro-3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

7-(6-chloro-3-pyridinyl)-3-azabicyclo[3.3.1]non-6-ene,

6-(6-chloro-3-pyridinyl)-3-azabicyclo[3.3.1]nonane, and

7-(6-chloro-3-pyridinyl)-3-azabicyclo[3.3.1]nonane,

or a pharmaceutically acceptable salt thereof.

3. The method of claim 1 , wherein the pain is neurologic, neuropathic, or chronic.

4. The method of claim 1 , wherein the pain is inflammatory pain, pain associated with arthritis, pain associated with rheumatoid disease, pain associated with teno-synovitis, pain associated with vasculitis, neuropathic pain, trigeminal neuralgia, herpetic neuralgia, diabetic neuropathy pain, causalgia, low back pain, deafferentation syndromes, chronic pain, severe chronic pain, post-operative pain, or pain associated with one or more of cancer, angina, renal or billiary colic, menstruation, migraine, and gout.

5. The method of claim 1 , wherein the pain is nociceptive pain.

Continuity (4)
Continuation 12123530 · May 20, 2008
Division 10711969 · Oct 15, 2004
Provisional Application 60511697 · Oct 15, 2003
Related Publication 20100152228A1 · Jun 17, 2010