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US 4,845,242 AGranted
Isocoumarins with basic substituents as serine proteases inhibitors, anticoagulants and anti-inflammatory agents
AssigneeGeorgia Tech Research Corporation
InventorsJames C. Powers, Chih-Min Kam
Life of this patent
Estimating the term…
Abstract
Substituted isocoumarins, their preparation, their use in inhibiting serine proteases with trypsin-like, chymotrypsin-like and elastase-like specificity and their roles as anticoagulant agents, and anti-inflammatory agents.
Claims3
A compound of the formula:
- ##STR2## or a pharmaceutically acceptable salt thereof, wherein R is selected from the group consisting of --NH--C(.dbd.NH)--NH.sub.2, --C(.dbd.NH)NH.sub.2, amino-C.sub.1-6 alkyl, and isothiureido-C.sub.1-6 alkyl,
- Z is selected from the group consisting of H, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkyl with a phenyl group attached to the alkyl group, C.sub.1-6 fluorinated alkyl, C.sub.1-6 alkyl with an hydroxyl group attached to the alkyl group, C.sub.1-6 alkyl with a C.sub.1-6 alkoxy group attached to the alkyl group, C.sub.1-6 alkoxy, C.sub.1-6 fluorinated alkoxy, C.sub.1-6 alkoxy with a phenyl group attached to the alkoxy group, benzyloxy group wherein the phenyl group is unsubstituted or substituted by one or two substituents selected from halogen, trifluoromethyl, NO.sub.2, cyano, methyl, methoxy, acetyl, carbonyl, OH, and amino, and
- Y is selected from the group consisting of H, halogen, trifluoromethyl, methyl, OH, and methoxy.
A compound of the formula:
- ##STR3## or a pharmaceutically acceptable salt thereof, wherein Z is selected from the group consisting of C.sub.1-6 alkoxy with an amino group attached to the alkoxy group, C.sub.1-6 alkoxy with an isothiureido group attached to the alkoxy group, C.sub.1-6 alkoxy with a guanidino group attached to the alkoxy group, C.sub.1-6 alkoxy with an amidino group attached to the alkoxy group, C.sub.1-6 alkyl with an amino group attached to the alkyl group, C.sub.1-6 alkyl with an isothiureido group attached to the alkyl group, C.sub.1-6 alkyl with a guanidino group attached to the alkyl group, C.sub.1-6 alkyl with an amidino group attached to the alkyl group,
- R is selected from the group consisting of H, OH, NH.sub.2, NO.sub.2, halogen, C.sub.1-6 alkoxy, C.sub.1-6 fluorinated alkoxy, C.sub.1-6 alkyl, amino-C.sub.1-6 alkyl, and
- Y is selected from the group consisting of H, halogen, trifluoromethyl, methyl, OH and methoxy.
A compound of the formula:
- ##STR4## or a pharmaceutically acceptable salt thereof, wherein R is selected from the group consisting of --NH--C(.dbd.NH)--NH.sub.2, --C(.dbd.NH)NH.sub.2, amino-C.sub.1-6 alkyl, and isothiureido-C.sub.1-6 alkyl,
- Z is selected from the group consisting of C.sub.1-6 alkoxy with an amino group attached to the alkoxy group, C.sub.1-6 alkoxy with an isothiureido group attached to the alkoxy group, C.sub.1-6 alkoxy with a guanidino group attached to the alkoxy group, C.sub.1-6 alkoxy with an amidino group attached to the alkoxy group, C.sub.1-6 alkyl with an amino group attached to the alkyl group, C.sub.1-6 alkyl with an isothiureido group attached to the alkyl group, C.sub.1-6 alkyl with a guanidino group attached to the alkyl group, C.sub.1-6 alkyl with an amidino group attached to the alkyl group, and
- Y is selected from the group consisting of H, halogen, trifluoromethyl, methyl, OH and methoxy.
Dependencies are inferred from the claim text.