# US 4,400,377 A · Use of polypeptides as analgesic drugs

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- Number: US 4,400,377 A
- Document ID: US4400377A
- Status: Granted
- Kind: A
- Application number: 06/355,252
- Filed: 1982-03-05
- Granted: 1983-08-23
- Earliest claimed: 1980-09-26
- Assignees: Farmitalia Carlo Erba S.p.A.
- Inventors: Gerhard Zetler; Alessandro Rossi; Chiara De Paolis
- Web page: https://patentgrep.com/patent/US4400377A

## CPC

- C07K 5/1021: {with the first amino acid being acidic}
- C07K 14/595: Gastrins; Cholecystokinins [CCK]
- C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00)

## Abstract

A method of treating pain of whatever origin and nature in human and animal which comprises administering to the patient in need an effective amount of a polypeptide of structure: ##STR1## wherein X is selected from the group consisting of hydrogen, t-butyloxycarbonyl(Boc), Asp, Pyr-Glu, Pyr-Gln-Asp, Pyr-Asn-Asp; Y is selected from the group consisting of Thr, Met, Leu, Nle, Val; W is selected from the group consisting of Met, Nle, Leu.

## Claims

### Claim 1

A method of inducing analgesia in animal and human patients suffering from severe pains selected from biliary and renal colic pains, pains caused by peripheral vascular diseases of the extremities, migraine, chronic pains in cancer diseases, post-operatory-, traumatological-, large burns-, myocardial infarction- and angina pectoris-pains, which comprises administering to the patient in need an effective amount of a polypeptide of the general structure: ##STR13## wherein X is selected from the group consisting of hydrogen, t-butyl-oxycarbonyl(Boc), Asp, Pyr-Glu, Pyr-Gln-Asp, Pyr-Asn-Asp;
Y is selected from the group consisting of Thr, Met, Leu, Nle, Val;
W is selected from the group consisting of Met, Nle, Leu.

### Claim 2 (depends on 1)

A method in accordance with claim 1 wherein the polypeptide is administered by parenteral route.

### Claim 3 (depends on 1, 2)

A method in accordance with claims 1 and 2, wherein the polypeptide used is ##STR14##

### Claim 4 (depends on 1, 2)

A method in accordance with claims 1 and 2, wherein the polypeptide used is ##STR15##

### Claim 5 (depends on 1, 2)

A method in accordance with claims 1 and 2, wherein the polypeptide used is ##STR16##

### Claim 6 (depends on 1, 2)

A method in accordance with claims 1 and 2, wherein the polypeptide used is ##STR17##

### Claim 7 (depends on 1, 2)

A method in accordance with claims 1 and 2, wherein the polypeptide used is ##STR18##

### Claim 8 (depends on 1)

A method in accordance with claim 1, wherein the polypeptide used is administered to the patient in need at the dose level of from 2 nanograms/kg body weight (i.v.) to 1500 nanograms/kg body weight (intra muscularly) in admixture with the usual carriers suitable for the parenteral administration.