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US 10,160,730 B2Granted
Triazoles as KV3 inhibitors
AssigneeAutifony Therapeutics Limited
InventorsAgostino Marasco, Giuseppe Alvaro, Anne Dècor, Dieter Hamprecht, Paolo Dambruoso, Simona Tommasi
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I) are of use in the modulation of Kv3.1, Kv.3.2 and Kv3.3 channels and have utility in the treatment or prevention of related disorders.
Claims30
A compound of formula (I):
- wherein:
- W is group (Wa), group (Wb) or group (Wc):
- wherein:
- R1 is H, C1-4alkyl, halo, haloC1-4alkyl, CN, C1-4alkoxy, or haloC1-4 alkoxy;
- R2 is H, C1-4alkyl, C3-5spiro carbocyclyl, haloC1-4alkyl or halo;
- R3 is H, C1-4alkyl, haloC1-4alkyl, halo;
- or R3 is absent;
- R13 is H, C1-4alkyl, haloC1-4alkyl, halo;
- or R13 is absent;
- R14 is H, C1-4alkyl, haloC1-4alkyl, halo;
- or R14 is absent;
- A is a 5 or 6 membered saturated or unsaturated heterocycle, with at least one O atom;
- which heterocycle is optionally fused with a cyclopropyl group, or a cyclobutyl group, or a cyclopentyl group to form a tricycle when considered together with the phenyl;
- X is CH or N;
- Y is CR15 or N;
- wherein R15 is H or C1-4alkyl;
- R22 is H, Cl, F, or C1-4alkyl;
- R23 is H, C1-4alkyl, CI, CF3, O-C1-4alkyl, OCF3 or N(CH3)2;
- R24 is H, Cl, F, C1-4alkyl, O-C1-4alkyl, CN, OCF3 or CF3;
- R25 is H, Cl, F, O-C1-4alkyl or C1-4alkyl;
- and
- R26 is H or C1-4alkyl;
- wherein for R22 to R26, C1-4alkyl may be substituted by O-methyl;
- with the provisos that:
- not all of R22 to R26 may be H;
- when R4 is H, then R23 is methyl or CF3 and R22, R24, R25 and R26 are all H;
- when one of R22, R24, R25 or R26 is F, then at least one of R22 to R26 cannot be H or F;
- and
- when R24 is not H, at least one of R22 or R23 is not H,
- R4 is H or C1-4alkyl;
- wherein R2 and R3 may be attached to the same or a different ring atom;
- R2 may be attached to a fused ring atom;
- and wherein R13 and R14 may be attached to the same or a different ring atom;
- or a pharmaceutically acceptable salt thereof.
31 more elements
A compound of formula (I):
- wherein:
- W is group Wb:
- R1 is H, C1-4alkyl, halo, haloC1-4alkyl, CN, C1-4alkoxy, or haloC1-4 alkoxy;
- R2 is H, C1-4alkyl, C3-5spiro carbocyclyl, haloC1-4alkyl, or halo;
- wherein R2 may be attached to a fused ring atom;
- R3 is H, C1-4alkyl, haloC1-4alkyl, halo;
- or R3 is absent;
- wherein R2 and R3 may be attached to the same or a different ring atom:
- R4 is H or C1-4alkyl;
- R13 is H, C1-4alkyl, haloC1-4alkyl, halo;
- or R13 is absent;
- R14 is H, C1-4alkyl, haloC1-4alkyl, halo;
- or R14 is absent;
- wherein R13 and R14 may be attached to the same or a different ring atom;
- A is a 5 or 6 membered saturated or unsaturated heterocycle, with at least one O atom;
- which heterocycle is optionally fused with a cyclopropyl group, or a cyclobutyl group, or a cyclopentyl group to form a tricycle when considered together with the phenyl;
- X is CH or N;
- Y is CR15 or N;
- wherein R15 is H or C1-4alkyl;
- or a pharmaceutically acceptable salt thereof.
17 more elements
Dependencies are inferred from the claim text.