IP Library Granted Patent US 9,024,071
Granted Patent B2
US 9,024,071 · App. 13/318,877 · Granted May 5, 2015

Therapeutic compounds

Inventor: Raymond G. Booth (Gainesville, FL)
Assignee: University of Florida Research Foundation, Inc.
C07C211/42A61K31/13
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Quick Facts
Patent No.
US 9,024,071
App. No.
13/318,877
Granted
May 5, 2015
Kind
B2
Abstract

The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C and/or RSK disorders, including diseases and disorders mediated by GPCRs and/or RSKs.

Claims (35)

1. A compound of formula (I):

wherein,

R 1 is independently, NH 2 , NH(R′), N(R′) 2 ;

or

 wherein ring A is a 3-8 membered heterocyclic or heteroaryl, containing 0-3 additional heteroatoms selected from O, N and S; wherein ring A is optionally substituted;

each R′ is independently alkyl, alkenyl, or alkynyl, each of which may be optionally substituted;

R 2 is independently —(CH 2 )n—;

each n is independently 1 or 2;

R 3 is independently H, OH, or halo;

R 4 is independently H, OH, or halo

each R 5 is independently alkyl, aryl, halo, nitro, amino, heteroaryl, cycloalkyl, heterocyclic, or a alkoxy;

R 6 is independently H or alkyl;

R 7 independently H, or N(alkyl) 2 ; and

each R 8 is independently cycloalkyl or heterocyclic, optionally substituted with 1, 2, 3, or 4 independent R 5 ;

or salt thereof.

2. A compound of formula (I):

wherein,

R 1 is independently, NH 2 , NH(R′), N(R′) 2 ;

or

 wherein ring A is a 3-8 membered heterocyclic or heteroaryl, containing 0-3 additional heteroatoms selected from O, N and S; wherein ring A is optionally substituted;

each R′ is independently alkyl, alkenyl, or alkynyl, each of which may be optionally substituted;

R 2 is independently —(CH 2 )n—;

each n is independently 1 or 2;

R 3 is independently H, OH, or halo;

R 4 is independently H, OH, or halo;

R 6 is independently H or alkyl;

R 7 independently H, or N(alkyl) 2 ; and

each R 8 is independently cycloalkyl or heterocyclic, wherein each R 8 is substituted with 2, 3 or 4 independent R 5 wherein each R 5 is independently H, alkyl, halo, aryl, nitro, amino, heteroaryl, cycloalkyl;

or salt thereof.

3. The compound of claim 1 , wherein R 1 and R 8 are trans-oriented to one another.

4. A composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

5. A method of making a composition of claim 4 comprising combining a compound of claim 1 and a pharmaceutically acceptable carrier.

6. The compound of claim 1 , wherein the compound is 4-cyclohexyl-N, N-dimethyl-1,2,3,4-tetrahydronaphthalen-2-amine.

7. The compound of claim 1 , wherein the compound is (2S,4R)-4-cyclohexyl-N,N-dimethyl-1,2,3,4-tetrahydronaphthalen-2-amine.

8. The compound of claim 1 , wherein R 8 is selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl.

Assignments (2)
CONFIRMATORY LICENSE Recorded Dec 1, 2016
From: UNIVERSITY OF FLORIDA
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 040801/0335 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 27, 2012
From: BOOTH, RAYMOND G.
To: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION
Reel/Frame 027765/0069 →
Continuity (4)
Provisional Application 61215504 · May 5, 2009
Provisional Application 61241384 · Sep 10, 2009
Provisional Application 61277408 · Sep 24, 2009
Related Publication 20120149693A1 · Jun 14, 2012