# US 4,399,139 A · 5,6-Dihydro-11-alkylene-morphanthridin-6-ones, their pharmaceutical compositions and method of use

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- Number: US 4,399,139 A
- Document ID: US4399139A
- Status: Granted
- Kind: A
- Application number: 06/359,936
- Filed: 1982-03-19
- Granted: 1983-08-16
- Earliest claimed: 1981-04-01
- Assignees: BASF SE
- Inventors: Gerd Steiner; Ludwig Friedrich; Dieter Lenke
- Web page: https://patentgrep.com/patent/US4399139A

## CPC

- C07D 223/20: Dibenz [b, e] azepines; Hydrogenated dibenz [b, e] azepines
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- C07F 9/59: Hydrogenated pyridine rings
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)

## Abstract

Novel 5,6-dihydro-11-alkylene-morphanthridin-6-ones of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the meanings given in the description, their preparation and their use. The novel compounds are particularly useful in the treatment of gastric and duodenal ulcers.

## Claims

### Claim 1

A 5,6-dihydro-11-alkylene-morphanthridin-6-one of the formula I ##STR9## where R.sup.1 and R.sup.2 are hydrogen, chlorine or methyl and R.sup.3 and R.sup.4 together with nitrogen atom by which they are linked form a piperazine ring in which the carbon atoms are unsubstituted or substituted by one or more alkyl radicals of 1 to 3 carbon atoms and the nitrogen atom is substituted by alkyl of 1 to 3 carbon atoms, hydroxylalkyl of 2 or 3 carbon atoms or phenyl which is itself unsubstituted or substituted by fluorine, chlorine, methoxy or methyl, or is in the form of the N-oxide, and/or its physiologically tolerated acid addition salts.

### Claim 2 (depends on 1)

A compound of the formula I as set forth in claim 1, in the cis-form.

### Claim 3

11-(4-Methylpiperazinyl-1-yl)-carboxamidomethylene-5,6-dihydromorphanthr idin-6one.

### Claim 4

cis-11- (4-Methylpiperazinyl-1-yl)-carboxamidomethylene-5,6-dihydromorphanthridin-6 -one.

### Claim 5 (depends on 1)

A pharmaceutical composition for treating gastric and duodenal ulcers which comprises: a pharmaceutical auxillary and from 0.001 to 99% by weight of a compound of the formula I of claim 1.

### Claim 6 (depends on 1)

A process for treating disorders which are accompanied by pathologically increased gastric secretion which comprises: administering to the patient to be treated a composition as set forth in claim 1 in an amount sufficient to provide a daily dose of a compound of the formula I of from 5 to 100 mg.