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US 2026/0226031 A1Published application
Novel compounds
AssigneeNRG Therapeutics Ltd
InventorsNeil MILLER, Gilles OUVRY, Richard RUTTER, Tammy LADDUWAHETTY, Christopher THOMSON, Jan KULAGOWSKI, Michael ROWLEY, Susan BOYD
Life of this patent
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Abstract
The invention relates to compounds of formula (I), and related aspects.
Claims24
A compound according to formula (I):
- wherein:
- R1a is H or C1-4alkyl;
- R1b is H or C1-4alkyl;
- R2a is H, halo, C1-4alkyl or C1-4haloalkyl;
- R3a is H, halo or C1-4alkyl;
- R4a is H or C1-4alkyl;
- R5a is C1-6alkyl, C1-6haloalkyl, C1-6alkoxy, C1-6haloalkoxy, C2-6alkenyl, C2-6haloalkenyl, C0-6alkylene(C3-6cycloalkyl), C0-6alkylene(OH);
- or R4a and R5a together with the carbon atom to which they are attached form a C3-6cycloalkyl wherein said cycloalkyl may be optionally substituted by one or more groups selected from C1-4alkyl, C1-4haloalkyl and halo;
- R6a is H, halo, C1-4alkyl, C1-4haloalkyl, C1-4alkoxy or C1-4haloalkoxy;
- x is 0, 1 or 2;
- AA is a phenyl or phenyl fused to C5-6cycloalkyl, wherein said phenyl or phenyl fused to C5-6cycloalkyl may be optionally substituted by one or more AA1;
- AA1 is halo, C2-6alkynyl, C1-6alkyl C1-6haloalkyl, C1-6alkoxy, C1-6haloalkoxy, C3-6cycloalkyl, CN, OH, NRqRr, or NHSO2Rt;
- Rq is H or C1-4alkyl;
- Rr is H or C1-4alkyl;
- Rt is C1-4alkyl;
- BA is a monocyclic or bicyclic heterocycle or a monocyclic or bicyclic heteroaryl, wherein said heterocycle or heteroaryl may be optionally substituted by one or more B1A;
- and
- B1A is halo, C1-6alkyl, C1-6haloalkyl, oxo (=O), C1-6alkoxy, C1-6haloalkoxy, or C0-6alkylene(OH);
- or a salt and/or solvate thereof,
- and provided that the compound of formula (I) is not 5-hydroxypyridin-3-yl)(8-phenyl-6-azaspiro[3.4]octan-6-yl)methanone:
17 more elements
(canceled)
(canceled)
A compound or salt and/or solvate thereof, which is selected from the group consisting of:
- (6-hydroxypyrazin-2-yl)(8-phenyl-6-azaspiro[3.4]octan-6-yl)methanone;
- (4-hydroxypyridin-2-yl)(8-phenyl-6-azaspiro[3.4]octan-6-yl)methanone;
- (3,3-dimethyl-4-phenylpyrrolidin-1-yl)(5-hydroxypyridin-3-yl)methanone;
- 2-methyl-5-(8-phenyl-6-azaspiro[3.4]octane-6-carbonyl)-2,4-dihydro-3H-1,2,4-triazol-3-one;
- (6-hydroxypyrazin-2-yl)(8-phenyl-6-azaspiro[3.4]octan-6-yl)methanone;
- 6-(8-(2-fluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)pyrazin-2(1H)-one;
- 6-(3,3-dimethyl-4-phenylpyrrolidine-1-carbonyl)pyrazin-2(1H)-one;
- 6-(3,3-dimethyl-4-phenylpiperidine-1-carbonyl)pyrazin-2(1H)-one;
- 6-(3,3-dimethyl-4-phenylpyrrolidine-1-carbonyl)pyrazin-2(1H)-one;
- 5-(8-(2-fluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)-2-methyl-2,4-dihydro-3H-1,2,4-triazol-3-one;
- 6-(3-methyl-4-phenylpyrrolidine-1-carbonyl)pyrazin-2(1H)-one;
- 8-Phenyl-6-(3H-1,2,3-triazole-4-carbonyl)-6-azaspiro[3.4]octane;
- 6-(3-ethyl-4-phenylpyrrolidine-1-carbonyl)pyrazin-2(1H)-one;
- 6-[8-(4-Chlorophenyl)-6-azaspiro[3.4]octane-6-carbonyl]-1H-pyrazin-2-one;
- 6-[4-Phenyl-2-azaspiro[4.4]nonane-2-carbonyl]-1H-pyrazin-2-one;
- rac-2-{8-phenyl-6-azaspiro[3.4]octane-6-carbonyl}-3H-pyrimidin-4-one;
- 6-[(4-Ethynylphenyl)-6-azaspiro[3.4]octane-6-carbonyl]-1H-pyrazin-2-one;
- 4-[6-(6-oxo-1H-pyrazine-2-carbonyl)-6-azaspiro[3.4]octan-8-yl]benzonitrile;
- 2-[8-phenyl-6-azaspiro[3.4]octane-6-carbonyl]-3H-pyrimidin-4-one;
- (3-hydroxyisoxazol-5-yl)(8-phenyl-6-azaspiro[3.4]octan-6-yl)methanone;
- (3-hydroxyisoxazol-5-yl)(8-phenyl-6-azaspiro[3.4]octan-6-yl)methanone;
- 3-[8-Phenyl-6-azaspiro[3.4]octane-6-carbonyl]-4H-1,2,4-oxadiazol-5-one;
- 2-(2-fluoro-8-phenyl-6-azaspiro[3.4]octane-6-carbonyl)pyrimidin-4(3H)-one;
- 6-(8-phenyl-6-azaspiro[3.4]octane-6-carbonyl)pyridin-2(1H)-one;
- 6-(8-phenyl-6-azaspiro[3.4]octane-6-carbonyl)pyrimidin-2(1H)-one;
- 6-(8-(4-methoxyphenyl)-6-azaspiro[3.4]octane-6-carbonyl)pyrazin-2(1H)-one;
- 6-(8-(4-bromophenyl)-6-azaspiro[3.4]octane-6-carbonyl)pyrazin-2(1H)-one;
- 6-(8-(2-chlorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)pyrazin-2(1H)-one;
- 6-(8-(3-chlorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)pyrazin-2(1H)-one;
- 6-8-(5-chloro-2-fluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)pyrazin-2(1H)-one;
- 6-(8-(3-chloro-2-fluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)pyrazin-2(1H)-one;
- 3-(8-phenyl-6-azaspiro[3.4]octane-6-carbonyl)-1,2,4-oxadiazol-5(4H)-one;
- 6-(8-(4-fluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)pyrazin-2(1H)-one;
- (8-(4-fluorophenyl)-6-azaspiro[3.4]octan-6-yl)(3-hydroxyisoxazol-5-yl)methanone;
- 6-(8-(2,4-difluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)pyrazin-2(1H)-one;
- (8-(3-fluorophenyl)-6-azaspiro[3.4]octan-6-yl)(3-hydroxyisoxazol-5-yl)methanone;
- (8-(2,3-difluorophenyl)-6-azaspiro[3.4]octan-6-yl)(3-hydroxyisoxazol-5-yl)methanone;
- 6-(8-(3-fluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)pyrazin-2(1H)-one;
- 3-(8-(4-fluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)-1,2,4-oxadiazol-5(4H)-one;
- (8-(2,4-difluorophenyl)-6-azaspiro[3.4]octan-6-yl)(3-hydroxyisoxazol-5-yl)methanone;
- 6-(8-(2,3-difluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)pyrazin-2(1H)-one;
- 3-(8-(2,3-difluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)-1,2,4-oxadiazol-5(4H)-one 6-(8-(3,4-difluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)pyrazin-2(1H)-one;
- (8-(3,4-difluorophenyl)-6-azaspiro[3.4]octan-6-yl)(3-hydroxyisoxazol-5-yl)methanone;
- 3-(8-(3,4-difluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)-1,2,4-oxadiazol-5(4H)-one;
- 3-(8-(2,4-difluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)-1,2,4-oxadiazol-5(4H)-one;
- and
- 3-(8-(3-fluorophenyl)-6-azaspiro[3.4]octane-6-carbonyl)-1,2,4-oxadiazol-5(4H)-one;
- or a salt and/or solvate of any one thereof.
45 more elements
(canceled)
19-21. (canceled)
24-34. (canceled)
Dependencies are inferred from the claim text.