# US 5,703,087 A · Phenyl indole compounds

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- Number: US 5,703,087 A
- Document ID: US5703087A
- Status: Granted
- Kind: A
- Application number: 08/635,905
- Filed: 1996-11-27
- Granted: 1997-12-30
- Earliest claimed: 1993-11-01
- Assignees: H. Lundbeck A/S
- Inventors: Jens Kristian Perregaard; Ejner Knud Moltzen; Kim Andersen; Henrik Pedersen; Klaus Peter B.o slashed.ges.o slashed.; Andre Pernet; Barbara Bopp; Darcy Mulford; Kiyoshi Sakamoto
- Web page: https://patentgrep.com/patent/US5703087A

## CPC

- C07D 401/14: containing three or more hetero rings
- A61P 9/12: Antihypertensives
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/18: Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
- A61P 25/24: Antidepressants
- A61P 25/26: Psychostimulants, e.g. nicotine, cocaine
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention relates to phenylindole compounds of formula I: ##STR1## related to atypical neuroleptic sertindole.

## Claims

### Claim 1

A phenylindole compound having formula ##STR9## wherein R.sup.1 -R.sup.4 are independently selected from the group consisting of hydrogen, deuterium, halogen, C.sub.1-6 alkyl, cycloalkyl, cycloalkyl-C.sub.1-6 alkyl, aryl-C.sub.1-6 alkyl, aryl, hydroxy, C.sub.1-6 alkoxy, cycloalkyloxy, cycloalkyl-C.sub.1-6 alkyloxy, aryl-C.sub.1-6 alkyloxy, aryloxy, C.sub.1-6 alkylthio, cycloalkylthio, cycloalkyl-C.sub.1-6 alkylthio, aryl-C.sub.1-6 alkylthio and arylthio, with the proviso that all 4 substituents cannot be hydrogen; or
at least one pair of substituents (R.sup.1, R.sup.2 or R.sup.3, R.sup.4) constitutes an oxo group or a thioxo group and, if only one oxo or thioxo group is present, the other two substituents are selected from the above group defined for R.sup.1 -R.sup.4, with the proviso that they may not both be hydrogen; or
R.sup.1 and R.sup.2 and/or R.sup.3 and R.sup.4, respectively, can be joined together to form a 3-8 membered spiro ring optionally containing one oxygen or sulfur atom in the ring; or acid addition salt thereof.

### Claim 2 (depends on 1)

A compound according to claim 1, wherein R.sup.1 -R.sup.4 are individually selected from the group consisting of hydrogen, deuterium, lower alkyl, hydroxy and lower alkoxy; or
one or both pair of substituents (R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4) constitute an oxo group or are joined together to form a 3-8 membered spiro ring.

### Claim 3 (depends on 1)

A compound according to claim 1, wherein both substituents of at least one pair of substituents (R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4) are both different from hydrogen or constitute together an oxo group or are joined to form a spiro ring.

### Claim 4 (depends on 1)

A pharmaceutical composition, wherein said composition comprises a compound according to claim 1 together with a pharmaceutically acceptable carrier or diluent.

### Claim 5 (depends on 3)

A compound according to claim 3, wherein at least one of (R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4) taken together is oxo.

### Claim 6 (depends on 4)

A method for treatment of psychosis, depression, negative symptoms of schizophrenia, hypertension or extrapyramidal side effects induced by antipsychotic drugs comprising administration, to a patient in need of said treatment, a pharmaceutical composition according to claim 4.