# US 5,700,445 A · N-methyl piperazine compounds having dopamine receptor affinity

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- Number: US 5,700,445 A
- Document ID: US5700445A
- Status: Granted
- Kind: A
- Application number: 08/354,905
- Filed: 1994-12-12
- Granted: 1997-12-23
- Earliest claimed: 1994-12-12
- Assignees: Allelix Biopharmaceuticals Inc.
- Inventors: Jian-Min Fu; Sumanas Rakhit
- Web page: https://patentgrep.com/patent/US5700445A

## CPC

- C07D 267/18: [b, e]-condensed
- C07D 243/38: [b, e]- or [b, f]-condensed with six-membered rings
- C07D 337/14: [b,f]-condensed
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)

## Abstract

Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein X.sub.1 is selected from CH.sub.2, NH, O and S; X.sub.2 - - is selected from CH.dbd., CH.sub.2 13 , and N.dbd.; R.sub.1 to R.sub.8 are each independently selected from H, C.sub.1-4 alkyl, halo, cyano, nitro and halo-substituted C.sub.1-4 alkyl and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.

## Claims

### Claim 1

A compound of Formula I ##STR8## wherein X.sub.1 is NH;
X.sub.2 - - is N.dbd.;
R.sub.1 to R.sub.4 to R.sub.8 are H and R.sub.5 is Cl, and
wherein said compound is 4-chloro-11-(4-methyl-1-piperazinyl)-5H-dibenzo›b,e!›1,4!diazepine.

### Claim 2 (depends on 1)

A pharmaceutical composition, comprising a therapeutically effective amount of a compound according to claim 1, and a pharmaceutically acceptable carrier.

### Claim 3 (depends on 1)

A compound according to claim 1, in a radiolabelled form.

### Claim 4 (depends on 1)

A pharmaceutical composition for treating a condition mediated by the D4 receptor, comprising a compound according to claim 1 in an amount effective to inhibit the D4 receptor, and a pharmaceutically acceptable carrier thereof.

### Claim 5 (depends on 5)

A method for the treatment of a condition mediated by the D4 receptor, comprising the step of administering to a mammal in need of such treatment a composition according to claim 5.

### Claim 6 (depends on 1)

A pharmaceutical composition for treating schizophrenia, comprising a compound according to claim 1 in an amount sufficient to produce an antischizophrenia effect, and a pharmaceutically acceptable carrier therefor.

### Claim 7 (depends on 6)

A method for the treatment of schizophrenia, comprising the step of administering to a mammal in need of such treatment, a composition according to claim 6.

### Claim 8 (depends on 1)

A pharmaceutical composition for treating anxiety, comprising a compound according to claim 1 in an amount sufficient to produce an antianxiety effect, and a pharmaceutically acceptable carrier therefor.

### Claim 9 (depends on 8)

A method for the treatment of anxiety, comprising the step of administering to a mammal in need of such treatment, a composition according to claim 8.