1,2-benzisoxazoloxyacetic acids and related compounds
AssigneeHoechst-Roussel Pharmaceuticals Inc.
InventorsGregory M. Shutske, Linda L. Setescak, Richard C. Allen
Life of this patent
Estimating the term…
Abstract
Novel 1,2-benzisoxazoloxyacetic acids and related compounds, methods for preparing same and methods of treatment by administering compositions containing such a compound are described. These compounds are useful as diuretic, uricosuric and antihypertensive agents.
Claims33
A method of producing diuresis comprising administering to a patient in need of diuresis a diuretically effective amount of a compound of the formula ##STR65## in which R is naphthyl, ##STR66## thienyl, furyl, pyrryl, pyridyl or pyridyl N-oxide;
- R.sup.1 is a free or esterified carboxyl group of from 1 to 8 atoms, ##STR67## R.sup.2, R.sup.3 and R.sup.4 are the same or different and each can be hydrogen, halogen, or loweralkyl;
- X is hydrogen, halogen, loweralkyl, loweralkoxy, loweralkylthio, hydroxy, trifluoromethyl, nitro, amino or acylamino;
- R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are the same or different and can be hydrogen or loweralkyl;
- A and A' are the same or different and can be O or S;
- and
- m and n are the same or different and each can be the integer 1, 2 or 3;
- or a physiologically acceptable salt thereof.
A method of increasing uric acid excretion comprising administering to a patient in need of such increased uric acid excretion a uricosurically effective amount of a compound of the formula ##STR70## in which R is naphthyl, ##STR71## thienyl, furyl, pyrryl, pyridyl or pyridyl N-oxide;
- R.sup.1 is a free or esterfied carboxyl group of from 1 to 8 carbon atoms, ##STR72## R.sup.2, R.sup.3 and R.sup.4 are the same or different and each can be hydrogen, halogen, or loweralkyl;
- X is hydrogen, halogen, loweralkyl, loweralkoxy, loweralkylthio, hydroxy, trifluoromethyl, nitro, amino or acylamino;
- R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are the same or different and can be hydrogen or loweralkyl;
- A and A' are the same or different and can be O or S;
- and
- m and n are the same or different and each can be the integer 1, 2 or 3;
- or a physiologically acceptable salt thereof.
A method of depressing blood pressure comprising administering to a patient having high blood pressure an antihypertensively effective amount of a compound of the formula ##STR75## in which R is naphthyl, ##STR76## thienyl, furyl, pyrryl, pyridyl or pyridyl N-oxide;
- R.sup.1 is a free or esterified carboxyl group of from 1 to 8 carbon atoms, ##STR77## R.sup.2, R.sup.3 and R.sup.4 are the same or different and each can be hydrogen, halogen or loweralkyl, X is hydrogen, halogen, loweralkyl, loweralkoxy, loweralkylthio, hydroxy, trifluoromethyl, nitro, amino or acylamino;
- R5, R6, R7 and R8 and are the same or different and can be hydrogen or loweralkyl;
- A and A' are the same or different and can be O or S;
- and
- m and n are the same or different and each can be the integer 1, 2 or 3;
- or a physiologically acceptable salt thereof.
A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of the formula ##STR80## in which R is naphthyl, ##STR81## thienyl, furyl, pyrryl, pyridyl or pyridyl N-oxide;
- R.sup.1 is a free or esterified carboxyl group of from 1 to 8 carbon atoms, ##STR82## R.sup.2, R.sup.3 and R.sup.4 are the same or different and each can be hydrogen, halogen or loweralkyl;
- X is hydrogen, halogen, loweralkyl, loweralkoxy, loweralkylthio, hydroxy, trifluoromethyl, nitro, amino or acylamino;
- R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are the same or different and can be hydrogen or loweralkyl;
- A and A' are the same or different and can be O or S;
- and
- m and n are the same or different and each can be the integer 1, 2 or 3;
- or a physiologically acceptable salt thereof and a pharmaceutically acceptable carrier therefor.
Dependencies are inferred from the claim text.