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US 4,229,456 AGranted
Substituted naphthyridinones and processes for their preparations
AssigneeMerck & Co., Inc.
InventorsWilliam A. Bolhofer, Edward J. Cragoe, Jr., Jacob M. Hoffman, Jr.
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Abstract
Organic chemical compounds based upon the naphthyridine molecule are disclosed which have potent gastric secretion inhibitory properties. The naphthyridinone is substituted with a substituted amino alkyl group at the 1-position, and variously substituted at the remaining positions. The compounds have profound effects on the inhibition of gastric secretions in the gastro-intestinal tract, and compositions for such uses are also disclosed.
Claims7
A compound having the formula:
- ##STR14## wherein X is oxygen;
- n is an integer of from 2 to 6 such that the length of the carbon chain connecting the two nitrogen atoms is not less than 2;
- R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently hydrogen, loweralkyl, loweralkoxy, amino, haloloweralkyl, or phenyl;
- or any two adjacent substituents may be joined to form a benzo substituent;
- R.sub.6 and R.sub.7 are independently N-loweralkylthiocarbamoyl;
- or R.sub.6 and R.sub.7 may be joined to form a morpholino ring or R.sub.6 and R.sub.7 may be an alkylene linkage of 4 or 5 carbon atoms to form a pyrrolidine or piperidine group which may be substituted with loweralkyl, oxo or benzo substituents;
- and the broken line in the 3,4 position of the naphthyridine molecule indicates that the bond may be either a single or a double bond;
- and the acid addition and quaternary ammonium salts thereof;
- and those compounds wherein
- X is sulfur,
- n is an integer of from 2 to 6 such that the length of the carbon chain connecting the two nitrogen atoms is not less than 2;
- R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently hydrogen, loweralkyl, loweralkoxy, amino, haloloweralkyl, or phenyl;
- or any two adjacent substituents may be joined to form a benzo substituent;
- R.sub.6 and R.sub.7 are independently hydrogen, phenylloweralkyl, N-loweralkylcarbamoyl, N-loweralkylthiocarbamoyl;
- or R.sub.6 and R.sub.7 may be joined to form a morpholino ring or R.sub.6 and R.sub.7 may be an alkylene linkage of 4 or 5 carbon atoms to form a pyrrolidine or piperidine group which may be substituted with loweralkyl, oxo or benzo substituents;
- and the broken line in the 3,4 position of the naphthyridine molecule indicates that the bond may be either a single or a double bond;
- and the acid addition and quaternary ammonium salts thereof.
14 more elements
Dependencies are inferred from the claim text.