# US 4,397,845 A · Lincomycin 3-(5'-adenylate) as anesthetic

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- Number: US 4,397,845 A
- Document ID: US4397845A
- Status: Granted
- Kind: A
- Application number: 06/379,529
- Filed: 1982-05-19
- Granted: 1983-08-09
- Earliest claimed: 1982-05-19
- Assignees: The Upjohn Company
- Inventors: Harry R. Allen
- Web page: https://patentgrep.com/patent/US4397845A

## CPC

- C07H 19/20: with the saccharide radical esterified by phosphoric or polyphosphoric acids
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)

## Abstract

The 3-(5'-adenylate) of lincomycin- and clindamycin-type compounds in which the propyl hygric acid moiety has been replaced by different cyclic amino acids can be used as a local anesthetic in humans and animals.

## Claims

### Claim 1

A method for treating a human or animal subject in need of a local anesthetic which comprises administering to said subject an effective local anesthetic dose of a compound of the formula
R.sub.1 is H, C.sub.1 -C.sub.8 -alkyl; R.sub.11 is OH, OCH.sub.3, halogen (Cl, Br, I), --SCH.sub.2 CH.sub.2 OH, --SCH.sub.2 CH.sub.2 CH.sub.2 OH, SCH.sub.3 ; R.sub.12 is CH.sub.3, CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 OH, ##STR3## or the pharmaceutically acceptable acid addition salts thereof, selected from the group consisting of hydrochloride, sulfate, phosphoric, sodium, potassium, calcium, and lithium, as an essential active ingredient in combination with a pharmaceutical carrier.

### Claim 2 (depends on 1)

A method, according to claim 1, wherein said effective local anesthetic dose is from about 0.05 to about 50 mg/dose.

### Claim 3 (depends on 1)

A method, according to claim 1, wherein said administered compound has the formula ##STR4##