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    THIADIAZOLEAMIDE DERIVATIVES AND THEIR APPLICATIONS
    65.
    发明申请
    THIADIAZOLEAMIDE DERIVATIVES AND THEIR APPLICATIONS 有权

    公开(公告)号：US20240376091A1

    公开(公告)日：2024-11-14

    申请号：US18292906

    申请日：2021-08-19

    Applicant: ZHEJIANG UNIVERSITY

    Inventor： TINGJUN HOU ,  DAN LI ,  RONG SHENG ,  WEITAO FU ,  CHENXIAN HU ,  HAO YANG ,  MINKUI ZHANG ,  JIANING LIAO

    IPC: C07D417/12 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61P35/00 ,  C07D417/14

    Abstract: This invention pertains to compounds of the general formula (I) and their applications. The invention introduces a novel class of compounds exhibiting androgen receptor (AR) antagonistic activity. In particular, these compounds target a binding pocket located in the dimer interface of AR ligand binding domain (AR-LBD). These compounds effectively disrupt AR dimerization, thereby suppressing AR signaling. The high AR antagonistic activity and favorable safety profile of the compounds provided by the present invention have been substantiated through biochemical assays and animal models. Therefore, these compounds can be utilized in the formulation of medications to treat diseases characterized by abnormal expression of AR, including but not limited to prostate cancer, metastatic prostate cancer, castration-resistant prostate cancer, breast cancer and ovarian cancer.

    TRICYCLIC GPR65 MODULATORS
    69.
    发明申请
    TRICYCLIC GPR65 MODULATORS 有权

    公开(公告)号：US20240368173A1

    公开(公告)日：2024-11-07

    申请号：US18699825

    申请日：2022-10-17

    Applicant: PATHIOS THERAPEUTICS LIMITED

    Inventor： Tom MCCARTHY ,  Alan NAYLOR ,  David MILLER ,  Gavin MILNE ,  Maria IEVA ,  Tobias MOECHEL ,  Yannick ESVAN ,  John FEUTRILL

    IPC: C07D487/18 ,  A61K31/439 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  C07D471/18 ,  C07D519/00

    Abstract: 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 CR10R10′, 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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