Back to results
US 4,067,980 AGranted
Spirobenzoxazinium salts, method of use and compositions thereof as antihypertensive agents
AssigneeMerck & Co., Inc.
InventorsEdward J. Cragoe, Jr., Gerald E. Stokker, Everett M. Schultz
Life of this patent
Estimating the term…
Abstract
Quaternary salts of 3,4-dihydrospiro-2H-1,3-benzoxazines are prepared by treating 3,4-dihydrospiro-2H-1,3-benzoxazines with an alkylating agent. The products are antihypertensive agents.
Claims10
A compound of the formula:
- ##STR9## wherein R.sup.1 is hydrogen, methyl or methoxy;
- R.sup.2 is halo or lower alkyl;
- R.sup.3 is hydrogen, lower alkyl or lower alkoxy;
- R.sup.4 is halo, lower alkyl or trifluoromethyl;
- R.sup.5 is lower alkyl;
- ##STR10## is spiro-cyclohexane, spiro-cyclopentane spiro-4'-piperidine or spiro-4'-piperidine wherein the nitrogen heteroatom is substituted by lower alkanoyl and
- X is halo or lower alkanoyloxy.
4 more elements
A method of treating hypertension which comprises administration to a patient in need of such treatment a therapeutically effective amount of a compound of the formula:
- ##STR17## wherein R.sup.1 is hydrogen, methyl or methoxy,
- R.sup.2 is halo or lower alkyl;
- R.sup.3 is hydrogen, lower alkyl or lower alkoxy;
- R.sup.4 is halo, lower alkyl or trifluoromethyl;
- R.sup.5 is lower alkyl;
- ##STR18## is spiro-cyclohexane, spiro-cyclopentane spiro-4'piperidine or spiro-4'-piperidine wherein the nitrogen heteroatom is substituted by lower alkanoyl and
- X is halo or lower alkanoyloxy.
4 more elements
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of the formula for use in treating hypertension:
- ##STR19## wherein R.sup.1 is hydrogen, methyl or methoxy;
- R.sup.2 is halo or lower alkyl;
- R.sup.3 is hydrogen, lower alkyl or lower alkoxy;
- R.sup.4 is halo, lower alkyl or trifluoromethyl;
- R.sup.5 is lower alkyl;
- ##STR20## is spiro-cyclohexane, spiro-cyclopentane spiro-4'-piperidine or spiro-4'-piperidine wherein the nitrogen heteroatom is substituted by lower alkanoyl;
- and
- X is halo or lower alkanoyloxy.
5 more elements
Dependencies are inferred from the claim text.