IP Library Granted Patent US 9,233,109
Granted Patent B2
US 9,233,109 · App. 13/642,907 · Granted Jan 12, 2016

Compositions, methods of use, and methods of treatment

Inventors: Roger Lee Papke (Gainesville, FL); Adriaan Willem Bruijnzeel (Gainesville, FL); Sara Jo Nixon (Gainesville, FL); William Kem (Gainesville, FL); Ferenc Soti (Gainesville, FL)
Assignee: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
A61K31/4995A61K31/44A61K31/444A61K31/445A61K45/06
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Quick Facts
Patent No.
US 9,233,109
App. No.
13/642,907
Granted
Jan 12, 2016
Kind
B2
Abstract

Briefly described, embodiments of this disclosure, among others, include compositions, pharmaceutical compositions, methods of treating nicotine dependence, methods of treating a subject who smokes and has a risk for depression or other neuropsychiatric disorder, method of treating a subject who smokes and has a risk for depression or other neuropsychiatric disorders, and the like.

Claims (15)

1. A method of reducing nicotine-induced rewarding effects in a subject who smokes comprising: delivering to a subject in need thereof a pharmaceutical composition, wherein the pharmaceutical composition includes a therapeutically effective amount of each of a α7 N-acetylcholine receptor (nAChR)-selective partial agonist and a α4β2 nAChR partial agonist, or a pharmaceutically acceptable salt of one or both of the α7-selective partial agonist and the α4β2 nAChR partial agonist, and a pharmaceutically acceptable carrier, wherein the α7 nAChR-selective partial agonist is 3-(2,4-dimethoxybenzylidene)anabaseine (DiMeOBA) (GTS-21) and in an amount therapeutically effective for reducing depression induced in said subject by the α4β2 nAChR partial agonist, and wherein the α4β2 nAChR partial agonist is varenicline, and in an amount therapeutically effective for reducing nicotine-induced rewarding effects in a subject by reducing the agonist effect of nicotine on the α4β2 nAChR.

2. A method of reducing nicotine-induced rewarding effects in a subject who smokes comprising: delivering to a subject in need thereof, a therapeutically effective amount of both a α7 N-acetylcholine receptor (nAChR)-selective partial agonist and a α4β2 nAChR partial agonist or a pharmaceutically acceptable salt of one or both of the α7 nAChR-selective partial agonist and the α4β2 nAChR partial agonist, wherein the α7 nAChR-selective partial agonist is 3-(2,4-dimethoxybenzylidene)anabaseine (DiMeOBA) (GTS-21),or a pharmaceutically acceptable salt thereof, and in an amount therapeutically effective for reducing depression induced in said subject by the α4β2 nAChR partial agonist, and wherein the α4β2 nAChR partial agonist is varenicline, or a pharmaceutically acceptable salt thereof, and in an amount therapeutically effective for reducing nicotine-induced rewarding effects in a subject by reducing the agonist effect of nicotine on the α4β2 nAChR.

3. The method of claim 2 , wherein the α7 nAChR-selective partial agonist and the α4β2 nAChR partial agonist are separately delivered to the subject.

4. The method of claim 2 , wherein the α7 nAChR-selective partial agonist and the α4β2 nAChR partial agonist are delivered to the subject in a composition including both the α7-selective partial agonist and the α4β2 nAChR partial agonist.

5. A method of reducing nicotine-induced rewarding effects in a subject who smokes comprising:

delivering to a subject in need thereof, a pharmaceutical composition comprising:

the α4β2 N-acetylcholine receptor (nAChR) partial agonist varenicline, or a pharmaceutically acceptable salt thereof, in an amount therapeutically effective for reducing nicotine-induced rewarding effects in a subject by reducing the agonist effect of nicotine on the α4β2 nAChR;

the α7 nAChR-selective partial agonist 3-(2,4- dimethoxybenzylidene)anabaseine (DiMeOBA) (GTS-21), or a pharmaceutically acceptable salt thereof, in an amount therapeutically effective for reducing depression induced in said subject by the α4β2 nAChR partial agonist; and

a pharmaceutically acceptable carrier.

6. A method of reducing nicotine-induced rewarding effects in a subject who smokes comprising:

delivering to a subject in need thereof:

the α4β2 nAChR partial agonist varenicline, or a pharmaceutically acceptable salt thereof, in an amount therapeutically effective for reducing the agonist effect of nicotine on the α4β2 nAChR;

the α7 nAChR-selective partial agonist 3-(2,4-dimethoxybenzylidene)anabaseine (DiMeOBA) (GTS-21), or a pharmaceutically acceptable salt thereof, in an amount therapeutically effective for reducing depression induced in said subject by the α4β2 nAChR partial agonist.

7. The method of claim 6 , wherein the α7 nAChR-selective partial agonist and the α4β2 nAChR partial agonist are separately delivered to the subject.

8. The method of claim 6 , wherein the α7 nAChR-selective partial agonist and the α4β2 partial agonist are delivered to the subject in a composition including both the α7 nAChR-selective partial agonist and the α4β2 nAChR partial agonist.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 9, 2012
From: PAPKE, ROGER LEE; BRUIJNZEEL, ADRIAAN WILLEM; NIXON, SARA JO; KEM, WILLIAM; SOTI, FERENC
To: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
Reel/Frame 029270/0923 →
CONFIRMATORY LICENSE Recorded Nov 6, 2012
From: UNIVERSITY OF FLORIDA
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 029246/0939 →
Continuity (2)
Provisional Application 61327321 · Apr 23, 2010
Related Publication 20130137697A1 · May 30, 2013