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US 6,284,796 B1Granted
Ukokinase inhibitors
AssigneeAbbott Laboratories
InventorsAndrew G. Geyer, William J. McClellan, Todd W. Rockway, Kent D. Stewart, Moshe Weitzberg, Michael D. Wendt
Life of this patent
Estimating the term…
Abstract
Compounds having the formula are inhibitors of urokinase and are useful in the treatment of diseases in which urokinase plays a role. Also disclosed are urokinase-inhibiting compositions and a method of inhibiting urokinase in a mammal.
Claims14
A compound having the formula
- or a pharmaceutically acceptable salt or prodrug thereof, wherein LA is —NR2C(X)—, wherein X is O or S, and R2 is selected from the group consisting of
- (a) hydrogen
- (b) alkyl of one to six carbon atoms,
- (c) alkenyl of two to six carbon atoms,
- (d) alkynyl of two to six carbon atoms,
- (e) aryl,
- (f) arylalkyl, wherein the alkylene group is of one to six carbon atoms,
- (g) cycloalkyl of three to eight carbon atoms, and
- (h) cycloalkylalkyl, wherein the cycloalkyl group is of three to eight carbon atoms, and the alkylene group is of one to ten carbon atoms,
- wherein LA is depicted with the right end being the end which is attached to the naphthyl ring and the left end being the end which is attached to RA, and RA is aryl, wherein the aryl is optionally substituted with one or two substituents independently selected from the group consisting of
- (a) alkyl of one to six carbon atoms,
- (b) alkoxy of one to six carbon atoms,
- (c) aminoalkyl of one to six carbon atoms, and
- (d) cycloalkylalkyl wherein the cycloalkyl group is of three to eight carbon atoms and the alkyl group is of one to ten carbon atoms.
11 more elements
A compound selected from the group consisting of
- N-[4-(aminomethyl)phenyl]-6-aminoiminomethyl-2-naphthalenecarboxamide bis(trifluoroacetate);
- 6-(aminoiminomethyl)-N-[4-(hydroxymethyl)phenyl]-2-naphthalenecarboxamide;
- mono(trifluoroacetate);
- 6-(aminoiminomethyl)-N-[3-(1-methylethoxy)phenyl]-2-naphthalenecarboxamide, mono(trifluoroacetate);
- 6-(aminoiminomethyl)-N-(3-propoxyphenyl)-2-naphthalenecarboxamide, mono(trifluoroacetate);
- 6-(aminoiminomethyl)-N-[3-(1-ethylpropoxy)phenyl]-2-naphthalenecarboxamide, mono(trifluoroacetate);
- 6-(aminoiminomethyl)-N-[3-(cyclopentyloxy)phenyl]-2-naphthalenecarboxamide, mono(trifluoroacetate);
- 6-(aminoiminomethyl)-N-(3-ethoxyphenyl)-2-naphthalenecarboxamide, mono(trifluoroacetate);
- 6-(aminoiminomethyl)-N-(3,5-dimethoxyphenyl)-2-naphthalenecarboxamide;
- 6-(aminoiminomethyl)-N-3-((2-methylpropyl)phenyl)-2-naphthalenecarboxamide, monohydrochloride mono(trifluoroacetate);
- and
- 6-(aminoiminomethyl)-N-(3-(cyclopentylmethyl)phenyl)-2-naphthalenecarboxamide, monohydrochloride mono(trifluoroacetate).
9 more elements
The compound N-[4-(aminomethyl)phenyl]-6-aminoiminomethyl-2-naphthalenecarboxamide, or a pharmaceutically acceptable salt or prodrug thereof.
Dependencies are inferred from the claim text.