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US 6,673,789 B2Granted
2-pyridinylguanidine urokinase inhibitors
AssigneePfizer Inc.
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.
Claims4
A compound named N″-(5-methyl-2-pyridinyl)guanidine, or a pharmaceutically acceptable salt thereof.
A compound of formula
- selected from:
- said compound wherein R1 is Cl, R2 is H, and R3 is H;
- said compound wherein R1 is Br, R2 is H, and R3 is H;
- said compound wherein R1 is H, R2 is Ph, and R3 is H;
- said compound wherein R1 is H, R2 is CONHCH2Ph, and R3 is H;
- said compound wherein R1 is Cl, R2 is H, and R3 is Cl;
- said compound wherein R1 is Cl, R2 is H, and R3 is Br;
- said compound wherein R1 is Br, R2 is H, and R3 is Cl;
- said compound wherein R1 is Cl, R2 is H, and R3 is E—CH═CHCO2H;
- said compound wherein R1 is Cl, R2 is H, and R3 is CH2CH2CO2H;
- said compound wherein R1 is Cl, R2 is H, and R3 is E—CH═CHCONHMe;
- said compound wherein R1 is Cl, R2 is H, and R3 is E—CH═CHCONHCH2Ph;
- said compound wherein R1 is Cl, R2 is H, and R3 is E—CH═CHCO-(3-hydroxypiperidino);
- said compound wherein R1 is Cl, R2 is H, and R3 is E—CH═CHCON(Me)CH2Ph;
- said compound wherein R1 is Cl, R2 is H, and R3 is E—CH═CHCO(morpholino);
- said compound wherein R1 is Cl, R2 is H, and R3 is E—CH═CHSO2NHMe;
- said compound wherein R1 is Cl, R2 is H, and R3 is E—CH═CHPh;
- said compound wherein R1 is Cl, R2 is H, and R3 is E—CH═CH(4-MeOC6H4);
- said compound wherein R1 is Cl, R2 is H, and R3 is E—CH═CH2(2-pyridyl);
- said compound wherein R1 is Cl, R2 is H, and R3 is E—CH═CH-cyclohexyl;
- said compound wherein R1 is Cl, R2 is H, and R3 is E—CH═CH-(3,4-methylenedioxyphenyl);
- said compound wherein R1 is Cl, R2 is H, and R3 is E—CH═CH(3-CN—C6H4);
- said compound wherein R1 is Cl, R2 is H, and R3 is C≡CPh;
- said compound wherein R1 is Cl, R2 is H, and R3 is OPh;
- said compound wherein R1 is Cl, R2 is H, and R3 is OCH2Ph;
- said compound wherein R1 is Cl, R2 is H, and R3 is OCH2CH2OH;
- said compound wherein R1 is Cl, R2 is H, and R3 is OCH2CH2OMe;
- said compound wherein R1 is Cl, R2 is H, and R3 is OCH2CONHCH2Ph;
- said compound wherein R1 is Cl, R2 is H, and R3 is OCH2(3-CO2Me—C6H4);
- said compound wherein R1 is Cl, R2 is H, and R3 is CH2OPh;
- said compound wherein R1 is Cl, R2 is Cl, and R3 is Cl;
- said compound wherein R1 is Cl, R2 is Me, and R3 is Cl;
- said compound wherein R1 is Cl, R2 is CH2OPh, and R3 is Cl;
- said compound wherein R1 is Cl, R2 is CH2NMeBn, and R3 is Cl;
- and
- said compound wherein R1 is Cl, R2 is CH2N(CH2)4, and R3 is Cl;
- or
- a pharmaceutically acceptable salt thereof or solvate of either entity.
35 more elements
A pharmaceutical composition comprising a compound, salt or solvate, as defined in any preceding claim, in admixture with a pharmaceutically compatible adjuvant, diluent or carrier.
Dependencies are inferred from the claim text.