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US 12,630,516 B2Granted
Compounds
AssigneeNRG Therapeutics Ltd
InventorsNeil Miller, Richard Rutter, Jan Kulagowski, Richard Morphy, Tammy Ladduwahetty, John Maclean, Mustafa Moroglu, Eric Talbot, Michael Rowley
Life of this patent
Estimating the term…
Abstract
The invention relates to compounds of formula (I): and related aspects.
Claims20
A compound of formula (I):
- wherein:
- R1a is H or methyl;
- R1b is H or F;
- A is group (Aa), (Ab), (Ac) or (Ad):
- wherein group (Aa) is:
- wherein:
- R2 is H, C1-4alkyl, C1-4alkylene(aryl), C1-4alkylene(OH), C1-4alkylene(C3-6cycloalkyl), C1-4alkylene (4-7 membered heterocycloalkyl), C1-4alkoxy, OC1-4alkylene(aryl), C1-4alkyleneOC1-4alkyl, C1-4alkyleneOC3-6cycloalkyl, C1-4alkyleneO(4-7 membered heterocycloalkyl), C1-4alkyleneO(aryl), C3-6alkynyl or C1-4alkenylO(C3-6alkynyl);
- wherein said aryl, heterocycloalkyl and cycloalkyl are optionally substituted by 1, 2 or 3 substituents each independently selected from C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, halo, CN, OH, NR2aR2b, SO2R2c and NHSO2R2c;
- R2a is selected from H and C1-4alkyl;
- R2b is selected from H, C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, aryl and 4-7 membered heterocycloalkyl;
- R2c is selected from C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, aryl and 4-7 membered heterocycloalkyl;
- each R3 is independently halo, methyl, ethyl or n-propyl;
- m is 0, 1, 2, 3 or 4;
- wherein group (Ab) is:
- wherein:
- R4 is H, C1-4alkyl or C1-4alkylene(aryl);
- wherein said aryl is optionally substituted by 1, 2 or 3 substituents each independently selected from C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, halo, CN, OH, NR4aR4b, SO2R4c and NHSO2R4c;
- R4a is selected from H and C1-4alkyl;
- R4b is selected from H, C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, aryl and 4-7 membered heterocycloalkyl;
- R4c is selected from C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, aryl and 4-7 membered heterocycloalkyl;
- R5 is H or C1-4alkyl;
- each R6 is independently C1-4alkyl or halo;
- n is 0, 1, 2 or 3;
- wherein group (Ac) is:
- wherein:
- R7 is C1-4alkyl, C1-4alkylene(OH) or C1-4alkyleneOC1-4alkyl;
- is 1 or 2;
- wherein group (Ad) is:
- wherein:
- X is a bond, O or CH2;
- each R8 is independently halo, C1-4alkyl, C1-4alkoxy, OC1-4haloalkyl, OC1-4alkylene(C3-6cycloalkyl), OC1-4alkylene (4-7 membered heterocycloalkyl) or OH;
- wherein said heterocycloalkyl and cycloalkyl are optionally substituted by 1, 2 or 3 substituents independently selected from C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, halo, CN, OH, NR8aR8b, SO2R8c and NHSO2R8c;
- R8a is selected from H and C1-4alkyl;
- R8b is selected from H, C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, aryl and 4-7 membered heterocycloalkyl;
- R8c is selected from C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, aryl and 4-7 membered heterocycloalkyl;
- each R9 is independently halo or C1-4alkyl;
- p is 0, 1 or 2;
- q is 0, 1, 2, 3 or 4;
- wherein B is group (Ba), (Bb) or (Bc):
- wherein group (Ba) is:
- wherein:
- Y is C(R11)(R12), N(R13), O or S;
- each R10 is independently halo or C1-4alkyl;
- r is 0, 1, 2 or 3;
- R11 is H or C1-4alkyl;
- R12 is H or C1-4alkyl;
- or R11 and R12 together with the carbon atom to which they are attached form a C3-6cycloalkyl;
- R13 is H, C1-4alkyl or C3-6cycloalkyl;
- wherein said cycloalkyl is optionally substituted by 1, 2 or 3 substituents independently selected from C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, halo, CN, OH, NR13aR13b, SO2R13c and NHSO2R13c;
- R13a is selected from H and C1-4alkyl;
- R13b is selected from H, C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, aryl and 4-7 membered heterocycloalkyl;
- R13c is selected from C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, aryl and 4-7 membered heterocycloalkyl;
- wherein group (Bb) is:
- wherein:
- each R14 is independently halo or C1-4alkyl;
- sis 0, 1, 2 or 3;
- wherein group (Bc) is:
- wherein:
- R15 is C1-4alkyl, C1-4alkoxy, C3-6cycloalkyl, C1-4haloalkyl, halo or CN;
- wherein said cycloalkyl is optionally substituted by 1, 2 or 3 substituents independently selected from C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, halo, CN, OH, NR15aR15b, SO2R15c and NHSO2R15c;
- R15a is selected from H and C1-4alkyl;
- R15b is selected from H, C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, aryl and 4-7 membered heterocycloalkyl;
- R15c is selected from C1-4alkyl, C3-6cycloalkyl, C1-4alkoxy, C1-4haloalkyl, aryl and 4-7 membered heterocycloalkyl;
- R16 is H, halo or C1-4alkyl;
- and
- D, E and F are each independently C(R16);
- or one of D, E and F is N, and the two remaining D, E and F groups are independently C(R16);
- or a pharmaceutically acceptable salt and/or solvate thereof.
65 more elements
Dependencies are inferred from the claim text.