Pyrazinyl-1,2,4-oxadiazole-5-ones, for treatment of edema, and processes for preparing same
AssigneeMerck & Co., Inc.
InventorsMark G. Bock, Robert L. Smith
Life of this patent
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Abstract
The case concerns novel pyrazinyl-1,2,4-oxadiazole-5-ones and processes for preparing the same. The compounds are useful in the treatment of edema and hypertension.
Claims11
A method of treatment of edema which comprises administering to a patient in need of such treatment a pharmaceutically effective dose of the formula ##STR3## wherein R is hydrogen or lower alkyl (C.sub.1-5),
- R.sup.1 is hydrogen or lower alkyl (C.sub.1-5),
- R and R.sup.1 can be joined to form an alkylene group of from 2-4 carbon atoms, and
- X is halo, cyano or phenyl.
A method for treatment of edema which comprises administering to a patient in need of such treatment a pharmaceutically effective dose of a compound of the formula:
- ##STR4## wherein R is hydrogen or methyl;
- R.sup.1 is hydrogen or methyl;
- and
- X is halo.
A pharmaceutical composition useful in the treatment of edema which comprises a compound of the formula ##STR5## wherein R is hydrogen or lower alkyl (C.sub.1-5),
- R.sup.1 is hydrogen or lower alkyl (C.sub.1-5),
- R and R.sup.1 can be joined to form an alkylene group of from 2-4 carbon atoms, and
- X is halo, cyano or phenyl.
- and a pharmaceutically acceptable carrier.
A pharmaceutical composition useful in the treatment of edema which comprises a compound of the formula ##STR6## wherein R is hydrogen or methyl;
- R.sup.1 is hydrogen or methyl;
- and
- X is halo.
A compound of the formula:
- ##STR7## wherein R is hydrogen or lower alkyl (C.sub.1-5),
- R.sup.1 is hydrogen or lower alkyl (C.sub.1-5),
- R and R.sup.1 can be joined to form an alkylene group of from 2-4carbon atoms, and
- X is halo, cyano or phenyl.
A compound of the formula:
- ##STR8## wherein R is hydrogen or methyl;
- R.sup.1 is hydrogen or methyl;
- and
- X is halo.
A process for preparing a compound of the Formula ##STR9## wherein R is hydrogen or lower alkyl (C.sub.1-5),
- R.sup.1 is hydrogen or lower alkyl (C.sub.1-5),
- R and R.sup.1 can be joined to form an alkylene group of from 2-4 carbon atoms, and
- X is halo, cyano or phenyl which comprises reacting a compound of the formula ##STR10## with hydroxylamine hydroxchloride to form an intermediate of the formula ##STR11## and then reacting said latter compound with a hot hydrochloric acid solution to produce the desired product.
Dependencies are inferred from the claim text.