# US 2014/0155490 A1 · Therapeutic compounds

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- Number: US 2014/0155490 A1
- Document ID: US20140155490A1
- Status: Published application
- Kind: A1
- Application number: 14/084,339
- Filed: 2013-11-19
- Published: 2014-06-05
- Earliest claimed: 2007-06-15
- Assignees: University of Florida Research Foundation, Inc.
- Applicants: University of Florida Research Foundation, Inc.
- Inventors: Raymond G. Booth
- Web page: https://patentgrep.com/patent/US20140155490A1

## CPC

- C07C 215/70: with rings other than six-membered aromatic rings being part of the carbon skeleton
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 9/12: Antihypertensives
- A61P 13/10: of the bladder
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- A61P 25/08: Antiepileptics; Anticonvulsants
- A61P 25/16: Anti-Parkinson drugs
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/20: Hypnotics; Sedatives
- A61P 25/22: Anxiolytics
- A61P 25/24: Antidepressants
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A61P 25/30: for treating abuse or dependence
- A61P 25/36: Opioid-abuse
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 211/42: with six-membered aromatic rings being part of the condensed ring systems
- C07D 209/08: with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
- C07D 209/14: Radicals substituted by nitrogen atoms, not forming part of a nitro radical
- C07D 213/38: having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
- C07D 215/12: with substituted hydrocarbon radicals attached to ring carbon atoms
- C07C 2602/10: the other ring being six-membered, e.g. tetraline
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## 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 disorders, including diseases and disorders mediated by GPCRs.

## Claims

### Claim at position 1

1-9. (canceled)

### Claim 10

A method of treating obesity in a subject comprising administering to the subject identified as in need thereof a PAT compound capable of selectively inhibiting the 5-HT2c relative to 5-HT2a or 5-HT2b.

### Claim 11 (depends on 10)

The method of claim 10, wherein the binding interaction for inhibiting 5-HT2c is at least 5-fold greater than for either 5-HT2a or 5-HT2b.

### Claim 12 (depends on 10)

The method of claim 10, wherein the binding interaction for inhibiting 5-HT2c is at least 100-fold greater than for either 5-HT2a or 5-HT2b.

### Claim at position 5

13-14. (canceled)

### Claim 15

A compound that is
wherein,
R1 is independently H, NH2, NH(alkyl), N(alkyl)2;
R2 is independently —(CH2)n-;
Each n is independently 1 or 2;
R3 is independently H, OH, or halo;
R4 is independently H, OH, or halo
Each R5 is independently H, alkyl, or halo;
R6 is independently H or alkyl; and
R7 independently H, N(alkyl)2;
or salt, hydrate or solvate thereof.

### Claim 16 (depends on 15)

The compound of claim 15, wherein the compound substituents at the 1-position and the 3-position are in the trans-orientation to one another.

### Claim 17 (depends on 15)

A composition comprising a compound of claim 15 and a pharmaceutically acceptable carrier.

### Claim 18 (depends on 15, 17)

A method of making a composition of claim 17 comprising combining a compound of claim 15 and a pharmaceutically acceptable carrier.

### Claim 19

A compound of the formula:
wherein,
R1 is independently H, NH2, NH(alkyl), N(alkyl)2;
R2 is independently —(CH2)n-;
Each n is independently 1 or 2;
R3 is independently H, OH, or halo;
R4 is independently H, OH, or halo
Each R5 is independently H, alkyl, or halo;
R6 is independently H or alkyl;
R7 independently H, N(alkyl)2; and
R8 is independently aryl or heteroaryl, each optionally substituted with 1-4 independent R5;
or salt, hydrate or solvate thereof.

### Claim 20 (depends on 15)

The compound of claim 15, wherein the compound is (+)-trans-4-(4-chlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydronaphthalen-2-amine.

### Claim 21 (depends on 15)

The compound of claim 15, wherein the compound is (−)-trans-4-(4-chlorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydronaphthalen-2-amine.

### Claim 22 (depends on 15)

The compound of claim 15, wherein the compound is (+)-trans-4-(4-fluorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydronaphthalen-2-amine.

### Claim 23 (depends on 15)

The compound of claim 15, wherein the compound is (−)-trans-4-(4-fluorophenyl)-N,N-dimethyl-1,2,3,4-tetrahydronaphthalen-2-amine.

### Claim 24 (depends on 15)

The compound of claim 15, wherein the compound is (+)-trans-N,N-dimethyl-4-p-tolyl-1,2,3,4-tetrahydronaphthalen-2-amine.

### Claim 25 (depends on 15)

The compound of claim 15, wherein the compound is (−)-N,N-dimethyl-4-p-tolyl-1,2,3,4-tetrahydronaphthalen-2-amine.

### Claim 26 (depends on 15)

The compound of claim 15, wherein the compound is 4-(3-bromophenyl)-N,N-dimethyl-1,2,3,4-tetrahydronaphthalen-2-amine.

### Claim 27 (depends on 15)

The compound of claim 15, wherein the compound is (+)-trans-4-(3-bromophenyl)-N,N-dimethyl-1,2,3,4-tetrahydronaphthalen-2-amine.

### Claim 28 (depends on 15)

The compound of claim 15, wherein the compound is (−)-trans-4-(3-bromophenyl)-N,N-dimethyl-1,2,3,4-tetrahydronaphthalen-2-amine.

### Claim 29 (depends on 15)

The compound of claim 15, according to the following formula:
wherein R is selected from the group consisting of

### Claim 30 (depends on 29)

The compound of claim 29, wherein R is selected from the group consisting of