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US 4,363,816 AGranted
Tricyclic pyrroles, their compositions and their use
AssigneeByk Gulden Lomberg Chemische Fabrik GmbH
InventorJorg Senn-Bilfinger
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Abstract
1,4,9,10-tetrahydropyrrolo[3,2-b][1,5]benzodiazepin-10-ones have been found o provide excellent protection for the stomach and intestines of warm-blooded animals. They are useful for the treatment and prophylaxis of such maladies as gastritis, acute and chronic ulcus ventriculi and hyperacid gastric irritation. The compounds are administered enterally or parenterally, usually in a standard dosage form. The disclosure includes key intermediates, methods of synthesis, compositions and use.
Claims17
A tricyclic pyrrole of the formula ##STR15## wherein R.sup.1 is --H or lower alkyl;
- R.sup.2 is --H or --CO--C.sub.n H.sub.2n --R.sup.3 ;
- R.sup.3 is halo or --N(R.sup.4)R.sup.5 ;
- R.sup.4 is --H, lower alkyl, alkenyl with from 3 to 5 carbon atoms or, together with R.sup.5 and the nitrogen atom to which both are bonded, pyrrolidino, piperidino, morpholino, perhydroazepino, 1-piperazinyl, 4-methyl-1-piperazinyl, 4-ethyl-1-piperazinyl, 4-benzyl-1-piperazinyl, 1-homopiperazinyl or 4-methyl-1-homopiperazinyl;
- R.sup.5 is alkenyl with from 3 to 5 carbon atoms, lower alkyl, di(lower)alkylamino(lower)alkyl or, together with R.sup.4 and the nitrogen atom to which both are bonded, pyrrolidino, piperidino, morpholino, perhydroazepino, 1-piperazinyl, 4-methyl-1-piperazinyl, 4-ethyl-1-piperazinyl, 4-benzyl-1-piperazinyl, 1-homopiperazinyl or 4-methyl-1-homopiperazinyl;
- each of R.sup.6, R.sup.7 and R.sup.8 is, independently, --H or lower alkyl;
- and
- n is a positive whole number of at most 2;
- or an acid-addition salt thereof.
5 more elements
Dependencies are inferred from the claim text.