US 2026/0216151 A1 · GPR65 MODULATORS

Abstract

The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, wherein: ring A is a 5- or 6-membered monocyclic aromatic or heteroaromatic ring, or a 9- or 10-membered bicyclic aromatic or heteroaromatic ring, each of which is optionally substituted with one or more substituents independently selected from halo, CN, alkoxy, NR11R11′, OH, SO2-alkyl, CO2-alkyl, alkyl, haloalkyl, aralkyl, aryl, and heteroaryl, and wherein said aryl and heteroaryl substituents are in turn optionally substituted with one or more substituents each independently selected from halo, CN, alkoxy, NR11R11′, OH, alkyl, haloalkyl, and aralkyl; Y and Z are each independently CR10R10′, wherein R10 and R10′ are each independently selected from H, F, alkyl, and haloalkyl; R1, R4, and R5 are each independently selected from H, alkyl, alkoxy, O-aralkyl halo and haloalkyl; at least one of R2 and R3 is a monocyclic or fused bicyclic aryl or a monocyclic or fused bicyclic heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, alkoxy, haloalkyl, haloalkoxy, halo, aryl, heteroaryl, CONR14R14′, (CH2)mNR11R11′, SO2-alkyl, CN, hydroxyalkyl, (CH2)m-heterocycloalkyl, (CH2)m-cycloalkyl, CO2R15, alkoxy-alkyl and O-cycloalkyl; the other of R2 and R3 is selected from halo, CN, and haloalkyl; each R11 and each R11′ is independently selected from H, alkyl, haloalkyl, COR12, and SO2R13, wherein R12 and R13 are both alkyl; R14, R14′ and Rw are each independently selected from H, alkyl and alkoxyalkyl; and each m is independently 0 to 3. Further aspects of the invention relate to such compounds for use in the field of immuno-oncology, immunology, and related applications.

Claims39

Dependent claims

A compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof,

wherein:
ring A is a 5- or 6-membered monocyclic aromatic or heteroaromatic ring, or a 9- or 10-membered bicyclic aromatic or heteroaromatic ring, each of which is optionally substituted with one or more substituents independently selected from halo, CN, alkoxy, NR11R11′, OH, SO2-alkyl, CO2-alkyl, alkyl, haloalkyl, aralkyl, aryl, and heteroaryl, and wherein said aryl and heteroaryl substituents are in turn optionally substituted with one or more substituents each independently selected from halo, CN, alkoxy, NR11R11′, OH, alkyl, haloalkyl, and aralkyl;
Y and Z are each independently CR10R10′, wherein R10 and R10′ are each independently selected from H, F, alkyl, and haloalkyl;
R1, R4, and R5 are each independently selected from H, halo, alkyl, alkoxy, O-aralkyl and haloalkyl;
at least one of R2 and R3 is a monocyclic or fused bicyclic aryl or a monocyclic or fused bicyclic heteroaryl group, each of which is optionally substituted by one or more substituents selected from alkyl, alkoxy, haloalkyl, haloalkoxy, halo, aryl, heteroaryl, CONR14R14′, (CH2)mNR11R11′, SO2-alkyl, CN, hydroxyalkyl, (CH2)m-heterocycloalkyl, (CH2)m-cycloalkyl, CO2R15, alkoxy-alkyl and O-cycloalkyl;
the other of R2 and R3 is selected from halo, CN, and haloalkyl;
each R11 and each R11′ is independently selected from H, alkyl, haloalkyl, COR12, and SO2R13, wherein R12 and R13 are both alkyl;
R14, R14′ and R15 are each independently selected from H, alkyl and alkoxyalkyl;
and
each m is independently 0 to 3;
with the proviso that the compound is other than:
N-(3-fluoro-4-(4-methyl-1H-imidazol-1-yl)phenyl)-6-methoxy-3,4-dihydroisoquinoline-2(1H)-carboxamide;
N-(3-fluoro-4-(4-methyl-1H-imidazol-1-yl)phenyl)-3,4-dihydroisoquinoline-2(1H)-carboxamide;
N-(3-fluoro-4-(4-methyl-1H-imidazol-1-yl)phenyl)-6,7-dimethoxy-3,4-dihydroisoquinoline-2(1H)-carboxamide.

11 more elements

Dependencies are inferred from the claim text.

Gpr65 modulators

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Gpr65 modulators

Life of this patent

Abstract

Claims39