2,3-Dihydro-6,7-disubstituted-5-(acyl)benzofuran-2-carboxylic acids
AssigneeMerck & Co., Inc.
InventorsEdward J. Cragoe, Jr., Otto W. Woltersdorf, Jr.
Life of this patent
Estimating the term…
Abstract
2,3-Dihydro-6,7-disubstituted-5-(acyl)benzofuran-2-carboxylic acids, the pharmaceutically acceptable salt, ester and amide derivatives thereof and combinations of these compounds with antikaluretic agents are disclosed having diuretic-saluretic, uricosuric and antihypertensive activity.
Claims13
A compound having the formula:
- ##STR7## wherein X is halo, methyl or hydrogen;
- Y is halo or methyl and
- X and Y can be combined to form a hydrocarbylene radical of from 3 to 4 carbon atoms;
- R is phenyl or mono or disubstituted phenyl wherein the substituent is halo, methyl, trifluoromethyl or methoxy;
- and
- the non-toxic pharmaceutically acceptable salt, ester and amide derivative thereof.
A compound of the formula ##STR8## wherein X is halo, methyl or hydrogen;
- Y is halo or methyl;
- X and Y can be combined to form a hydrocarbylene radical of from 3 to 4 carbon atoms;
- R is selected from the group consisting of phenyl, p-methoxy phenyl, p-chlorophenyl, and
- the non-toxic pharmaceutically acceptable salt, ester and amide derivative thereof.
A pharmaceutical composition useful in the treatment of edema associated with hypertension comprising a therapeutically effective amount of a compound of the formula of ##STR9## wherein X is halo, methyl or hydrogen;
- Y is halo or methyl,
- X and Y can be combined to form a hydrocarbylene radical of from 3 or 4 carbon atoms,
- R is phenyl or mono or disubstituted phenyl wherein the substituent is halo, methyl, trifluoromethyl or methoxy and
- the non-toxic pharmaceutically acceptable salt, ester and amide derivative thereof and a pharmaceutically acceptable carrier.
A pharmaceutical composition useful in the treatment of edema associated with hypertension comprising a therapeutically effective amount of a compound of the formula:
- ##STR10## wherein X is chloro;
- Y is chloro;
- and R is selected from the group consisting of phenyl, p-methoxy phenyl, p-chlorophenyl, and
- the non-toxic pharmaceutically acceptable salt, ester and amide derivative thereof and a pharmaceutically acceptable carrier.
A method of treatment of edema associated with hypertension comprising the administration of a therapeutically effective amount in unitary dosage form of a compound having the formula of:
- ##STR11## wherein X is halo, methyl or hydrogen;
- Y is halo or methyl;
- X and Y can be combined to form a hydrocarbylene radical of from 3 to 4 carbon atoms;
- R is phenyl or mono or disubstituted phenyl wherein the substituent is halo, methyl, trifluoromethyl or methoxy and
- the non-toxic pharmaceutically acceptable salt, ester and amide derivative thereof.
A method of treatment of edema associated with hypertension comprising the administration to a patient of from 0.01 mg. to 10 mg./kg of body weight of the patent of a compound having the formula:
- ##STR12## wherein X is chloro;
- Y is chloro;
- and
- R is selected from the group consisting of phenyl, p-methoxy phenyl, p-chlorphenyl, benzyl and p-chlorobenzyl and
- the non-toxic pharmaceutically acceptable salt, ester and amide derivative thereof.
Dependencies are inferred from the claim text.