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US 6,638,935 B2Granted
Heteroary1 derivatives and their use as medicaments
AssigneeZentaris AG
InventorsPeter Emig, Eckhard Günther, Bernhard Kutscher, Bernd Nickel, Jürgen Schmidt, Anita Storch
Life of this patent
Estimating the term…
Abstract
The invention relates to novel pyridine derivatives of formula 1, to their preparation and to their use as medicaments, in particular for treating tumors
Claims48
A compound of formula 1
- wherein
- R, R1, R2, R3 can be attached to any of the pyridine carbon atoms C2 to C8, and can be the same or different and independently of one another are hydrogen, hydroxyl, straight-chain or branched C1-8 alkyl, C3-7 cycloalkyl, straight-chain or branched C1-8 alkylcarbonyl, straight-chain or branched C1-8 alkoxy, halogen, aryl-C1-8 alkoxy, nitro, amino, mono-C1-4 alkylamino, di-C1-4 alkylamino, C1-8 alkoxycarbonylamino, C1-6 alkoxycarbonylamino-C1-8 alkyl, cyano, straight-chain or branched cyano-C1-6 alkyl, carboxyl, C1-8 alkoxycarbonyl, C1-4 alkyl which is substituted by one or more fluorine atoms, carboxy-C1-8 alkyl or C1-8 alkoxycarbonyl-C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, straight-chain or branched cyano-C1-6 alkyl, aryl, where the aryl radical can be unsubstituted or mono- or polysubstituted by the same or different substituents from the group consisting of halogen, straight-chain or branched C1-8 alkyl, C3-7 cycloalkyl, carboxyl, straight-chain or branched C1-8 alkoxycarbonyl, trifluoromethyl, hydroxyl, straight-chain or branched C1-8 alkoxy, benzyloxy, nitro, amino, mono-C1-4 alkylamino, di-C1-4 alkylamino, cyano, straight-chain or branched cyano-C1-6 alkyl
- R and R1 and/or R2 and R3 can form a fused aromatic 6-membered ring with the pyridine ring forming a quinoline or acridine ring which can be substituted at any C atom ring position by the radicals R, R1, R2 and R3 having the meanings mentioned above;
- R4 is a straight-chain or branched C4-20 alkyl radical which can be saturated or unsaturated, with one to three double and/or triple bonds, and which can be unsubstituted or can optionally be substituted at the same or different C atoms by one, two or more aryl, heteroaryl, halogen, C1-6 alkoxy, amino, mono-C1-4 alkylamino, cyano —C═NH(NH2) or di-C1-4 alkylamino;
- a C6-14 aryl radical, carboxy, C1-4 alkoxycarbonyl, C6-14 aryl-C2-4 alkyl radical, or a C2-10 heteroaryl, or C2-10 heteroaryl-C1-4 alkyl radical which contains one or more heteroatoms of N, O or S, where the C1-4 alkyl radical can be unsubstituted or mono- or polysubstituted by the same or different substituents from the group consisting of C1-6 alkyl, halogen or oxo (═O), and where the C6-14 aryl or C2-10 heteroaryl radical can be unsubstituted or mono- or polysubstituted by the same or different substituents from the group consisting of straight-chain or branched C1-8 alkyl, C3-7 cycloalkyl, halogen, cyano, C1-6 alkoxycarbonylamino, C1-6 alkoxy, carboxyl, C1-8 alkoxycarbonyl, straight-chain or branched C1-6 alkyl which is substituted by one or more fluorine atoms, hydroxyl, straight-chain or branched C1-8 alkoxy, where adjacent oxygen atoms can also be linked by C1-2 alkylene groups, benzyloxy, nitro, amino, mono-C1-4 alkylamino, di-C1-4 alkylamino, aryl, which can be unsubstituted or mono- or polysubstituted by the same or different substituents from the group of straight-chain or branched C1-8 alkyl, C3-7 cycloalkyl, carboxyl, straight-chain or branched C1-8 alkoxycarbonyl, trifluoromethyl, hydroxyl, straight-chain or branched C1-8 alkoxy, benzyloxy, nitro, amino, mono-C1-4 alkylamino, di-C1-4 alkylamino, cyano, straight-chain or branched cyano-C1-6 alkyl;
- or their structural isomers or stereoisomers, including tautomers, diastereomers or enantiomers, or their pharmaceutically acceptable salts.
3 more elements
Dependencies are inferred from the claim text.