# US 5,703,112 A · Method of preventing emesis using tetrahydrobenz ›CD!indole-6-carbonxamides

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- Number: US 5,703,112 A
- Document ID: US5703112A
- Status: Granted
- Kind: A
- Application number: 08/560,174
- Filed: 1995-11-17
- Granted: 1997-12-30
- Earliest claimed: 1993-06-10
- Assignees: Eli Lilly and Company
- Inventors: Mark M. Foreman; J. David Leander
- Web page: https://patentgrep.com/patent/US5703112A

## CPC

- A61K 31/404: Indoles, e.g. pindolol
- A61K 31/40: having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61P 1/08: for nausea, cinetosis or vertigo; Antiemetics
- A61P 13/02: of urine or of the urinary tract, e.g. urine acidifiers
- A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives
- A61P 15/08: for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
- A61P 15/10: for impotence
- A61P 25/00: Drugs for disorders of the nervous system
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The present invention provides methods of preventing emesis and treating sexual dysfunction in mammals utilizing certain tetrahydrobenz›cd!indoles. The invention further provides pharmaceutical formulations suitable for use in such methods.

## Claims

### Claim 1

A method of preventing emesis in mammals comprising administering to a mammal susceptible to or suffering from emesis an effective amount of a compound of the formula ##STR6## wherein: R.sup.1 is hydrogen, C.sub.1 -C.sub.4 alkyl or allyl;
R.sup.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or allyl; or a pharmaceutically acceptable acid addition salt thereof.

### Claim 2 (depends on 1)

A method of claim 1 wherein the mammal is a human.

### Claim 3 (depends on 2)

A method of claim 2 wherein in the compound employed R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl.

### Claim 4 (depends on 3)

A method of claim 3 wherein in the compound employed is (.+-.)-4-dipropylamino-1,3,4,5-tetrahydrobenz›cd!indole-6-carboxamide or a pharmaceutically acceptable acid addition salt thereof.

### Claim 5 (depends on 4)

A method of claim 4 wherein the acid addition salt is the hippurate salt.

### Claim 6 (depends on 3)

A method of claim 3 wherein the compound employed is (-)-4-dipropylamino-1,3,4,5-tetrahydrobenz›cd!indole-6-carboxamide or a pharmaceutically acceptable acid addition salt thereof.

### Claim 7 (depends on 6)

A method of claim 6 wherein the acid addition salt is the hippurate salt.

### Claim 8 (depends on 3)

A method of claim 3 wherein the compound employed is (+)-4-dipropylamino-1,3,4,5-tetrahydrobenz ›cd!indole-6-carboxamide or a pharmaceutically acceptable acid addition salt thereof.

### Claim 9 (depends on 8)

A method of claim 8 wherein the acid addition salt is the hippurate salt .