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US 6,258,822 B1Granted
Urokinase 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.
Claims5
A compound having the formula
- or a pharmaceutically acceptable salt, ester, or prodrug thereof, wherein
- A is —LARA, wherein LA is —NR2C(X)— wherein X is O and R2 is selected from the group consisting of
- (a) hydrogen,
- (b) alkyl of one to six carbon atoms,
- (c) alkenyl of three to six carbon atoms,
- (d) alkynyl of three 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 selected from the group consisting of aryl and heterocycle, wherein the aryl or the heterocycle are optionally substituted;
- B is hydrogen;
- and
- C is —LCRC, wherein LC is selected from the group the group consisting of
- (a) a covalent bond and
- (b) —NR1—, wherein R1 is selected from the group consisting of
- (i) hydrogen and
- (ii) alkyl of one to six carbon atoms,
- and RC is heterocycle,
- wherein the heterocycle is optionally substituted.
18 more elements
A compound selected from the group consisting of
- 6-(aminoiminomethyl)-4-(3-furanyl)-N-[4-(trifluoromethyl)phenyl]-2-naphthalenecarboxamide, mono(trifluoroacetate) salt;
- 6-(aminoiminomethyl)-4-(3-furanyl)-N-(4-pyridinyl)-2-naphthalenecarboxamide, dihydrochloride;
- 6-(aminoiminomethyl)-4-(3-furanyl)-N-(1H-pyrazol-3-yl)-2-naphthalenecarboxamide, dihydrochloride;
- 6-(aminoiminomethyl)-4-(3-furanyl)-N-(3-pyridinyl)-2-naphthalenecarboxamide, dihydrochloride;
- 6-(aminoiminomethyl)-4-(3-furanyl)-N-(2-pyridinyl)-2-naphthalenecarboxamide, dihydrochloride;
- 6-(aminoiminomethyl)-4-(3-furanyl)-N-phenyl-2-naphthalenecarboxamide, monohydrochloride;
- 6-(aminoiminomethyl)-4-[1-(methylsulfonyl)-1H-pyrazol-4-yl]-N-phenyl-2-naphthalenecarboxamide, monohydrochloride;
- 6-(aminoiminomethyl)-4-[5-(methylthio)-3-furanyl)]-N-phenyl-2-naphthalenecarboxamide, monohydrochloride;
- 6-(aminoiminomethyl)-N-[4-(aminomethyl)phenyl]-4-(2-pyrimidinylamino)-2-naphthalenecarboxamide, tris(trifluoroacetate) salt;
- 6-(aminoiminomethyl)-N-phenyl-4-(2-pyrimidinylamino)-2naphthalenecarboxamide, mono(trifluoroacetate) salt;
- N-[(4-(aminomethyl)phenyl]-6-[amino(hydroxyimino)methyl]-4-(2-pyrimidinylamino)-2-naphthalenecarboxamide, bis(trifluoroacetate) salt;
- 6-(aminoiminomethyl)-N-[4-(hydroxymethyl)phenyl]-4-(2-pyrimidinylamino)-2-naphthalenecarboxamide, mono(trifluoroacetate) salt;
- 6-(aminoiminomethyl)-N-phenyl-4-(tetrahydro-3-furanyl)-2-naphthalenecarboxamide, monohydrochloride;
- 6-[amino(hydroxyimino)methyl]-N-phenyl-4-(2-pyrimidinylamino)-2-naphthalenecarboxamide;
- 6-(aminoiminomethyl)-4-[5-(ethylthio)-3-furanyl]-N-phenyl-2-naphthalenecarboxamide, monohydrochloride;
- 6-(aminoiminomethyl)-4-[5-(propylthio)-3-furanyl]-N-phenyl-2-naphthalenecarboxamide, monohydrochloride;
- 6-(aminoiminomethyl)-N-phenyl-4-(2-pyrrolidinyl)-2-naphthalenecarboxamide, mono(trifluoroacetate) salt;
- 6-(aminoiminomethyl)-4-[5-(ethylsulfonyl)-3-furanyl]-N-phenyl-2-naphthalenecarboxamide, monohydrochloride;
- 6-(aminoiminomethyl)-4-[5-(propylsulfonyl)-3-furanyl]-N-phenyl-2-naphthalenecarboxamide, monohydrochloride;
- 6-(aminoiminomethyl)-4-[5-[methylthio)methyl]-3-furanyl]-N-phenyl-2-naphthalenecarboxamide, monohydrochloride;
- 6-(aminoiminomethyl)-4-[5-(methoxymethyl)-3-furanyl]-N-phenyl-2-naphthalenecarboxamide, monohydrochloride;
- 6-(aminoiminomethyl)-4-[5-(methylsulfonyl)-3-furanyl]-N-phenyl-2-naphthalenecarboxamide, mono(trifluoroacetate) salt;
- and
- 6-(aminoiminomethyl)-4-[5-(ethythio)tetrahydro-3-furanyl]-N-phenyl-2-naphthalenecarboxamide, monohydrochloride.
21 more elements
A compound, or a pharmaceutically acceptable salt or prodrug thereof, which is 6-(aminoiminomethyl)-N-[4-(aminomethyl)phenyl]-4-(2-pyrimidinylamino)-2-naphthalenecarboxamide.
Dependencies are inferred from the claim text.