# US 4,393,077 A · 1-Methylene-1-phenylguanidine compounds

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- Number: US 4,393,077 A
- Document ID: US4393077A
- Status: Granted
- Kind: A
- Application number: 06/280,072
- Filed: 1981-07-02
- Granted: 1983-07-12
- Earliest claimed: 1981-07-02
- Assignees: William H. Rorer, Inc.
- Inventors: George H. Douglas; Henry F. Campbell
- Web page: https://patentgrep.com/patent/US4393077A

## CPC

- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- 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)

## Abstract

Compounds having the formula: ##STR1## wherein X.sub.1, X.sub.2, R, R.sub.1, R.sub.2 and R.sub.3 are as set forth hereinafter, their preparation and uses as ganglionic blocking agents are disclosed.

## Claims

### Claim 1

A method for ganglionic blocking which comprises administering an effective amount of a compound of the formula ##STR4## and the pharmaceutically acceptable salts thereof, wherein X.sub.1 and X.sub.2 each represent a member selected from the group consisting of hydrogen, halo, trifluoromethyl, acyl, alkyl, hydroxy, alkoxy and amino,
R.sub.1, R.sub.2, and R.sub.3 each represent a member selected from the group consisting of hydrogen, lower alkyl and lower alkenyl and
R represents a member selected from the group consisting of cycloalkyl, cycloalkenyl and aryl,
also, R.sub.3 and either R.sub.1 or R.sub.2 can constitute a methylene bridge, --(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.3 --, resulting in the formation of a five- or six-membered ring.

### Claim 2 (depends on 1)

The method according to claim 1, wherein the compound is 1-cyclopropylmethyl-1-(2,6-dichlorophenyl) guanidine.

### Claim 3 (depends on 1)

The method according to claim 1, wherein the compound is 1-cyclobutylmethyl-1-(2,6-dichlorophenyl) guanidine.

### Claim 4 (depends on 1)

The method according to claim 1, wherein the compound is 1-cyclohexylmethyl-1-(2,6-dichlorophenyl) guanidine.