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US 5,098,924 AGranted
Diol sulfonamide and sulfinyl renin inhibitors
AssigneeE. R. Squibb & Sons, Inc.
InventorMichael A. Poss
Life of this patent
Estimating the term…
Abstract
Compounds of the formula ##STR1## wherein Z is SO or SO.sub.2 possess renin inhibition activity and are useful in treating hypertension and other diseases where the reduction of the levels of circulating angiotensin II are beneficial.
Claims11
A compound of the formula:
- ##STR218## or a pharmaceutically acceptable salt thereof wherein:
- Z is SO or SO.sub.2 ;
- R.sub.1 and R.sub.2 are independently selected from the group consisting of hydrogen, alkyl of 1 to 7 carbons, alkenyl of 2 to 7 carbons, --(CH.sub.2).sub.m -aryl, --(CH.sub.2).sub.m -cycloalkyl, halo substituted alkyl of 1 to 7 carbons, --(CH.sub.2).sub.g --O--R.sub.15, ##STR219## R.sub.3, R.sub.7, R.sub.8, and R.sub.14 are independently selected from the group consisting of hydrogen, alkyl of 1 to 7 carbons, halo substituted alkyl of 1 to 7 carbons, --(CH.sub.2).sub.m -aryl, --(CH.sub.2).sub.m -cycloalkyl, --(CH.sub.2).sub.n --O--R.sub.15, --(CH.sub.2).sub.n --S--R.sub.15, ##STR220## R.sub.4 is hydrogen or alkyl of 1 to 7 carbons;
- R.sub.5 and R.sub.6 are independently selected from the group consisting of hydrogen, alkyl of 1 to 7 carbons, halo substituted alkyl of 1 to 7 carbons, --(CH.sub.2).sub.m -aryl, --(CH.sub.2)hd m-cycloalkyl;
- ##STR221## R.sub.15 and R.sub.16 are independently selected from the group consisting of hydrogen, alkyl of 1 to 7 carbons, --(CH.sub.2).sub.m -cycloalkyl, and --(CH.sub.2).sub.m -aryl;
- ##STR222## R.sub.17 and R.sub.17', are independently selected from the group consisting of hydrogen, alkyl of 1 to 7 carbons, aryl, cycloalkyl, and ##STR223## R.sub.18 R.sub.18' are independently selected from the group consisting of alkyl of 1 to 7 carbons, --(CH.sub.2).sub.m -aryl, --(CH.sub.2).sub.m -cycloalkyl, ##STR224## m and m' are independently selected from zero and an integer from 1 to 5;
- n and n' are independently selected from an integer from 1 to 5;
- p is zero or one;
- g is an integer from 2 to 5;
- the term "alkyl of 1 to 7 carbons" refers to straight or branched chain radicals having up to seven carbon atoms;
- the term "lower alkyl" refers to straight or branched chain radicals having up to four carbon atoms;
- the terms "lower alkoxy" and "lower alkylthio" refer to such lower alkyl groups as defined above attached to an oxygen or sulfur;
- the term "alkenyl" refers to straight or branched chain radicals of 2 to 7 carbons containing at least one double bond;
- the term "cycloalkyl" refers to saturated rings of 4 to 7 carbons;
- the term "halo" refers to chloro, bromo, fluoro, and iodo;
- the term "halo substituted alkyl" refers to such an alkyl group in which one or more hydrogens have been replaced by chloro, bromo, or fluoro groups;
- and
- the term "aryl" refers to phenyl, diphenylmethyl, 1-naphthyl, 2-naphthyl, mono substituted phenyl, diphenylmethyl, 1-naphthyl, or 2-naphthyl wherein said substituent is lower alkyl of 1 to 4 carbons, lower alkylthio of 1 to 4 carbons, lower alkoxy of 1 to 4 carbons, halogen, hydroxy, amino, --NH--alkyl wherein alkyl is of 1 to 4 carbons, or --N(alkyl).sub.2 wherein alkyl is of 1 to 4 carbons, di or tri substituted phenyl, diphenylmethyl, 1-naphthyl or 2-naphthyl wherein said substituents are selected from methyl, methoxy, methylthio, halogen, hydroxy and amino.
15 more elements
Dependencies are inferred from the claim text.