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1. 发明申请

WO2023067322A1 TRICYCLIC GPR65 MODULATORS 审中-公开
公开(公告)号：WO2023067322A1
公开(公告)日：2023-04-27
申请号：PCT/GB2022/052644
申请日：2022-10-17
申请人： PATHIOS THERAPEUTICS LIMITED
发明人： MCCARTHY, Tom , NAYLOR, Alan , MILLER, David , MILNE, Gavin , IEVA, Maria , MOCHEL, Tobias , ESVAN, Yannick , FEUTRILL, John
IPC分类号： A61P11/00 , A61P11/06 , A61P35/00 , A61P43/00 , C07D471/18 , A61K31/439
摘要： 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.

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