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US 6,583,162 B1Granted
2-pyridinylguanidine urokinase inhibitors
AssigneeWarner-Lambert Company
InventorsRoger Peter Dickinson, Christopher Gordon Barber
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I): or a pharmaceutically acceptable salt thereof, or solvate of either entity, wherein R4 is a guanidinyl moiety and the other substituents are as defined in the text, are urokinase inhibitors.
Claims12
A compound of formula (I):
- or a pharmaceutically acceptable salt thereof, or solvate of either entity,
- wherein
- R1 is H, halogen, CN, C1-6 alkyl optionally substituted by one or more halogen, or C1-6 alkoxy optionally substituted by one to three halogens,
- R2 and R3 are each independently H, halogen, C1-6 alkyl optionally substituted by one or more halogen or C1-6 alkoxy, (Cn-alkylene)CO2H, (Cn-alkylene)CO2(C1-6 alkyl), (Cn-alkylene)CONR5R6, CH═CHR7, CH═CHCO2H, CH═CHCONR5R6, CH═CHSO2NR5R6, C═CR7, O(Cm-alkylene)OH, O(Cm-alkylene)OR8, OR8, O(Cm-alkylene)CONR5R6, CH2OR8 or CH2NR5R6,
- R4 is N═C(NH2)2 or NHC(═NH)NH2,
- R5 and R6 are each independently H, C1-6 alkyl optionally substituted by OH or CO2H
- R7 is C1-6 alkyl;
- R8 is C1-6 alkyl;
- n is 0, 1 or 2;
- m is 1 or 2;
- and wherein the “C-alkylene” linking groups in the definitions above are optionally substituted by one or more C1-6 alkyl;
- with the proviso that R1, R2 and R3 are not all H.
9 more elements
A pharmaceutical composition comprising a compound, salt or solvate, as defined in any preceding claim, in admixture with a diluent or carrier.
Dependencies are inferred from the claim text.