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US 2016/0311784 A1Published application
Cyclic triazo and diazo sodium channel blockers
AssigneeUniversity of Greenwich
InventorsMichael LEACH, Laurence HARBIGE, Dieter RIDDALL, Karl FRANZMANN
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Abstract
A method of treating a disorder. The method includes administering to a subject in need thereof a compound of general formula (I): Each of A, N*, X, Y, R1, and R2 is defined herein. Also disclosed are compounds of the formula and a pharmaceutical composition containing such a compound.
Claims17
A method of treating a disorder comprising administering to a subject in need thereof a compound of general formula (I), or a salt, solvate or tautomer thereof,
- in which:
- X and Y are each N;
- A is selected from ditrifluoromethylphenyl, methoxyphenyl, ethoxyphenyl, dimethoxyphenyl, diethoxyphenyl, trimethoxyphenyl, triethoxyphenyl, fluoromethoxyphenyl, fluoroethoxyphenyl, difluoromethoxyphenyl, difluoroethoxyphenyl, trifluoromethoxyphenyl, trifluoroethoxyphenyl, and tetrafluoroethoxyphenyl;
- R1 is hydrogen or a substituent group selected from C1-10 alkyl, C2-10 alkenyl, C1-3 alkyl-aryl, C1-3 alkyl-heterocyclyl and C3-10 cycloalkyl, optionally substituted by hydroxy, halogen, carboxamido, halo C1-6 alkyl, C1-6 alkyl or C1-6 alkoxy, or the Y nitrogen is unsubstituted;
- R2 is amino or a substituent group selected from C1-6 alkyl groups and phenyl groups, in which the substituent group is optionally substituted by hydroxy, halogen, halo-C1-6 alkyl, C1-6 alkyl or C1-6 alkoxy;
- and
- N* is ═NH when R1 is hydrogen or a substituent group;
- or
- N* is a group NRaRb where Ra and Rb are independently H or a C1-6 alkyl group;
- or
- N* is a piperazinyl ring optionally substituted by hydroxy, halogen, halo-C1-6 alkyl, C1-6 alkyl or C1-6 alkoxy;
- wherein the disorder is selected from those that are treatable by sodium channel blockers.
9 more elements
A compound of general formula (I), or a salt, solvate or tautomer thereof,
- in which:
- X and Y are each N;
- A is selected from ditrifluoromethylphenyl, methoxyphenyl, ethoxyphenyl, dimethoxyphenyl, diethoxyphenyl, trimethoxyphenyl, triethoxyphenyl, fluoromethoxyphenyl, fluoroethoxyphenyl, difluoromethoxyphenyl, difluoroethoxyphenyl, trifluoromethoxyphenyl, trifluoroethoxyphenyl, and tetrafluoroethoxyphenyl;
- R1 is hydrogen or a substituent group selected from C1-10 alkyl, C2-10 alkenyl, C1-3 alkyl-aryl, C1-3 alkyl-heterocyclyl and C3-10 cycloalkyl, optionally substituted by hydroxy, halogen, carboxamido, halo C1-6 alkyl, C1-6 alkyl or C1-6 alkoxy, or the Y nitrogen is unsubstituted;
- R2 is amino or a substituent group selected from C1-6 alkyl groups and phenyl groups, in which the substituent group is optionally substituted by hydroxy, halogen, halo-C1-6 alkyl, C1-6 alkyl or C1-6 alkoxy;
- and
- N* is ═NH when R1 is hydrogen or a substituent group;
- or
- N* is a group NRaRb where Ra and Rb are independently H or a C1-6 alkyl group;
- or
- N* is a piperazinyl ring optionally substituted by hydroxy, halogen, halo-C1-6 alkyl, C1-6 alkyl or C1-6 alkoxy.
8 more elements
Dependencies are inferred from the claim text.