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US 2019/0161479 A1Published application
Novel compounds
AssigneeAutifony Therapeutics Limited
InventorsGiuseppe ALVARO, Agostino MARASCO, Guido MARCONI
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds of the formula (I) and their use as Kv3 modulators.
Claims33
A compound of formula (I):
- wherein:
- X is H or CH3;
- Y is H or CH3;
- wherein at least one of X and Y is H;
- W is group (Wa), group (Wb) or group (Wc):
- wherein group (Wa) and group (Wb) are:
- wherein:
- R1 is H, C1-4alkyl, halo, haloC1-4alkyl, CN, C1-4alkoxy or haloC1-4alkoxy;
- R2 is H, C1-4alkyl, C3-5 spiro 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;
- 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;
- wherein group (Wc) is:
- wherein:
- R16 is halo, C1-4alkyl, C1-4alkoxy, haloC1-4alkyl, haloC1-4alkoxy or CN;
- R17 is H, halo, CN, C1-4alkyl, C1-4alkoxy or haloC1-4alkoxy;
- R18 is H, halo, CN, C1-4alkyl or C1-4alkoxy;
- Z is group (Za) or (Zb):
- wherein group (Za) is:
- wherein:
- R4 is H or C1-4 alkyl;
- R5 is H or C1-4 alkyl;
- or
- R4 and R5 can be fused to form a C3-5 spiro carbocyclyl or a C2-5 spiro heterocyclyl;
- and wherein group (Zb) is:
- wherein:
- R19 is C1-4 alkyl;
- or a pharmaceutically acceptable salt and/or solvate thereof and/or derivative thereof.
33 more elements
-6. (canceled)
-17. (canceled)
-25. (canceled)
-30. (canceled)
(canceled)
(canceled)
The compound according to claim 41, wherein ring A is selected from the group consisting of:
(canceled)
(canceled)
(canceled)
-53. (canceled)
-58. (canceled)
-75. (canceled)
A compound of formula (II):
- wherein:
- X is H or CH3;
- Y is H or CH3;
- wherein at least one of X and Y is H;
- and W is group (Wa), group (Wb), group (Wc) or group (Wc-b):
- wherein group (Wa) and group (Wb) are:
- wherein:
- R1 is H, C1-4alkyl, halo, haloC1-4alkyl, CN, C1-4alkoxy or haloC1-4alkoxy;
- R2 is H, C1-4alkyl, C3-5 spiro 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;
- 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;
- wherein group (Wc) is:
- wherein:
- R16 is CN;
- R17 is H, halo, CN, C1-4alkyl, C1-4alkoxy or haloC1-4alkoxy:
- R18 is H, halo, CN, C1-4alkyl or C1-4alkoxy;
- and wherein group (Wc-b) is:
- wherein:
- R16 is C1-4alkyl;
- and
- R17 is C1-4alkoxy or haloC1-4alkoxy;
- or a salt and/or solvate thereof,
- wherein the compound of formula (II) may have a syn or anti configuration;
- or
- a compound of formula (XII):
- wherein:
- X is H or CH3;
- Y is H or CH3;
- wherein at least one of X and Y is H;
- and W is group (Wa), group (Wb) or group (Wc-b):
- wherein group (Wa) and group (Wb) are:
- wherein:
- R1 is H, C1-4alkyl, halo, haloC1-4alkyl, CN, C1-4alkoxy or haloC1-4alkoxy:
- R2 is H, C1-4alkyl, C3-5 spiro 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;
- 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;
- wherein group (Wc-b) is:
- wherein:
- R16 is CN or C1-4alkyl;
- and
- R17 is C1-4alkoxy or haloC1-4alkoxy;
- or a salt and/or solvate thereof,
- wherein the compound of formula (XII) may have a syn or anti configuration.
58 more elements
77-90. (canceled)
Dependencies are inferred from the claim text.