# US 8,772,319 B2 · Diagnostic and therapeutic alkyl piperidine/piperazine compounds and process

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 8,772,319 B2
- Document ID: US8772319B2
- Status: Granted
- Kind: B2
- Application number: 13/396,010
- Filed: 2012-02-14
- Published: 2012-08-16
- Granted: 2014-07-08
- Earliest claimed: 2004-03-31
- Assignees: The General Hospital Corporation
- Applicants: David R. Elmaleh; Choi Sungwoon; Alan J. Fischman
- Inventors: David R. Elmaleh; Choi Sungwoon; Alan J. Fischman
- Web page: https://patentgrep.com/patent/US8772319B2

## CPC

- C07D 295/205: Radicals derived from carbonic acid
- A61P 25/36: Opioid-abuse
- C07D 211/26: with hydrocarbon radicals, substituted by nitrogen atoms
- C07D 211/58: attached in position 4
- C07D 213/74: Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
- C07D 241/06: having one or two double bonds between ring members or between ring members and non-ring members
- C07D 241/08: with oxygen atoms directly attached to ring carbon atoms
- C07D 295/088: to an acyclic saturated chain
- C07D 295/096: with the ring nitrogen atoms and the oxygen or sulfur atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
- C07D 295/135: with the ring nitrogen atoms and the substituent nitrogen atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
- C07D 295/192: from aromatic carboxylic acids
- C07D 295/21: Radicals derived from sulfur analogues of carbonic acid
- C07D 295/26: Sulfur atoms
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

Described herein are piperidine and piperazine compounds useful for treating neurodegenerated diseases characterized by a lack of dopamine neuron activity. The compounds are also useful for imaging dopamine neurons.

## Claims

### Claim 1

A compound of Formula IV
wherein:
m is an integer of 1 to 6;
B is —O—, —N(H)—, —C(═O)N(H)—, or —N(H)C(═O)—;
X and Y can be the same or different and are selected from the group consisting of hydrogen, halo, haloalkyl, alkyl, aryl, (C1-C6)alkoxy, —SH, and —SR;
R is optionally substituted (C1-C6)alkyl, optionally substituted (C2-C6)alkenyl, optionally substituted (C2-C6)alkynyl, or optionally substituted 1,2,4-oxadiazol-5-yl; and
V is hydrogen, —C(═O)N(H)-aryl, —C(═O)-alkyl, —SO2-aryl, alkyl, alkenyl, alkynyl, haloaryl, or alkyl halophenyl, wherein aryl or alkyl is optionally substituted.

### Claim 2 (depends on 1)

A method of treating a mammal afflicted with cocaine abuse which comprises:
administering to the mammal an effective amount of a compound of claim 1.

### Claim 3 (depends on 1)

The compound of claim 1, wherein X is halo.

### Claim 4 (depends on 1)

The compound of claim 1, wherein X is fluoro.

### Claim 5 (depends on 1)

The compound of claim 1, wherein X is 4-fluoro.

### Claim 6 (depends on 1)

The compound of claim 1, wherein Y is halo.

### Claim 7 (depends on 1)

The compound of claim 1, wherein Y is fluoro.

### Claim 8 (depends on 1)

The compound of claim 1, wherein Y is 4-fluoro.

### Claim 9 (depends on 1)

The compound of claim 1, wherein B is —O—.

### Claim 10 (depends on 1)

The compound of claim 1, wherein m is 4.

### Claim 11 (depends on 1)

The compound of claim 1, wherein V is hydrogen.

### Claim 12 (depends on 1)

The compound of claim 1, wherein V is —C(═O)N(H)-aryl.

### Claim 13 (depends on 1)

The compound of claim 1, wherein V is —C(═O)N(H)-(4-fluorophenyl).

### Claim 14 (depends on 1)

The compound of claim 1, wherein V is —C(═O)-alkyl.

### Claim 15 (depends on 1)

The compound of claim 1, wherein V is —C(═O)—CH3.

### Claim 16 (depends on 1)

The compound of claim 1, wherein V is —C(═O)—CH2Cl.

### Claim 17 (depends on 1)

The compound of claim 1, wherein V is

### Claim 18 (depends on 1)

The compound of claim 1, wherein V is —SO2-aryl.

### Claim 19 (depends on 1)

The compound of claim 1, wherein V is —SO2-(4-chlorophenyl).

### Claim 20 (depends on 1)

The compound of claim 1, wherein the compound is selected from the group consisting of