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    • 1. 发明申请
    • TRICYCLIC GPR65 MODULATORS
    • WO2023067322A1
    • 2023-04-27
    • PCT/GB2022/052644
    • 2022-10-17
    • PATHIOS THERAPEUTICS LIMITED
    • MCCARTHY, TomNAYLOR, AlanMILLER, DavidMILNE, GavinIEVA, MariaMOCHEL, TobiasESVAN, YannickFEUTRILL, John
    • A61P11/00A61P11/06A61P35/00A61P43/00C07D471/18A61K31/439
    • One aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof, (I) wherein: ring B is: a monocyclic aromatic group; or a monocyclic or bicyclic heteroaromatic group, each of which is optionally substituted by halo, CN, OH, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, hydroxycycloalkyl, O-cycloalkyl, alkoxy, haloalkoxy, heterocycloalkyl, O- heterocycloalkyl, aryl, heteroaryl, O-aryl, NHCO-alkenyl, NHCO-aryl, -(CH2)q-O-heteroaryl, CONH-aryl, aryloxy-alkyl, O-aralkyl, and CO2-alkyl, wherein said aryl, heteroaryl, heterocycloalkyl, O-cycloalkyl, NHCO-aryl, -(CH2)q-O-heteroaryl, CONH-aryl, aryloxy-alkyl, O-aralkyl, and O-aryl groups are each optionally further substituted by one or more groups independently selected from halo, alkyl, haloalkyl, alkoxy, NHCO-alkyl, NR13R13', SO2-alkyl, CN, hydroxyalkyl, CONR14R14', alkyl-NR15R15', heterocycloalkyl, alkyl-heterocycloalkyl, alkyl- cycloalkyl, aryl, (CH2)m-NHSO2-alkyl, CO2R16, alkoxy-alkyl, haloalkoxy, O-heterocycloalkyl, heteroaryl, alkoxy-alkoxy, and O-(CH2)p-cycloalkyl, where in the latter group, said cycloalkyl group is optionally further substituted by one or more halo, haloalkyl, alkyl or alkoxy groups; m is an integer from 0 to 3; p and q are each independently 0 to 3; Z is CR12; Y is CR10 R10', wherein R10 and R10' are each independently selected from H, F, alkyl, and haloalkyl; Ra and Rb are each independently selected from H and alkyl; R6 is selected from H, alkyl, cycloalkyl and hydroxyalkyl; R12 is selected from H, alkyl, haloalkyl, halo, OH and O-alkyl; and R13, R13', R14, R14', R15, R15', and R16 are each independently selected from H, alkyl, and alkoxyalkyl. Further aspects of the invention relate to compounds of formula (I) for use as a medicament, particularly in the field of immuno-oncology, immunology, and related applications.