# US 5,348,940 A · Cyclohexapeptidyl hydroxypropionitrile compounds

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- Number: US 5,348,940 A
- Document ID: US5348940A
- Status: Granted
- Kind: A
- Application number: 07/936,434
- Filed: 1992-09-03
- Granted: 1994-09-20
- Earliest claimed: 1991-10-01
- Assignees: Merck & Co., Inc.
- Inventors: James M. Balkovec; Robert A. Zambias
- Web page: https://patentgrep.com/patent/US5348940A

## CPC

- C07K 7/56: the cyclisation not occurring through 2,4-diamino-butanoic acid
- A61P 31/04: Antibacterial agents
- A61P 31/10: Antimycotics
- A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00)
- Y10S 930/27: Cyclic peptide or cyclic protein
- 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)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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)
- Y10S: TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS

## Abstract

Certain propionitrile compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for use in therapeutic compositions are described. A novel process for their preparation is also described. ##STR1##

## Claims

### Claim 1

A compound having the formula: ##STR11## wherein R.sub.1 is H or OH
R.sub.2 is H or OH
R.sub.3 is H, OH or OR where R is C.sub.1 -C.sub.4 alkyl or benzyl
R.sub.4 is H or OH
R.sub.5 is H, OH or CH.sub.3
R.sub.6 is H or CH.sub.3, and
R.sup.I is C.sub.9 -C.sub.21 alkyl, C.sub.9 -C.sub.21 alkenyl, C.sub.1 -C.sub.10 alkoxyphenyl, or C.sub.1 -C.sub.10 alkoxynaphthyl.

### Claim 2 (depends on 1)

A compound according to claim 1 having the formula ##STR12##
3.

### Claim 3 (depends on 1)

A compound according to claim 1 having the formula: ##STR13##

### Claim 4 (depends on 1)

A compound according to claim 1 having the formula: ##STR14##

### Claim 5 (depends on 1)

A compound according to claim 1 having the formula ##STR15##

### Claim 6 (depends on 1)

A compound according to claim 1 having the formula ##STR16##

### Claim 7 (depends on 1)

A compound according to claim 1 having the formula ##STR17##

### Claim 8 (depends on 1)

An antibiotic composition comprising a therapeutic amount of a compound of claim 1 in a pharmaceutically acceptable carrier.

### Claim 9 (depends on 1, 8)

A composition according to claim 8 in unit dosage form wherein the compound of claim 1 is present in an amount of 100 to 200 milligrams.