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    Indazole based compounds and associated methods of use
    2.
    发明专利
    Indazole based compounds and associated methods of use 未知

    公开(公告)号：AU2021244180A1

    公开(公告)日：2022-11-03

    申请号：AU2021244180

    申请日：2021-03-19

    Applicant: ARVINAS OPERATIONS INC

    Inventor： ARAUJO ERIKA ,  SPARKS STEVEN M ,  BERLIN MICHAEL ,  ZHANG WEI ,  WANG JING

    IPC: C07D401/14 ,  A61K31/506 ,  A61P25/00 ,  A61P35/00 ,  A61P37/00 ,  C07D413/14

    Abstract: Bifunctional compounds, which find utility as modulators of leucine-rich repeat kinase 2 (LRRK2), are described herein. In particular, the hetero-bifunctional compounds of the present disclosure contain on one end a moiety that binds to the cereblon E3 ubiquitin ligase and on the other end a moiety which binds LRRK2, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The hetero-bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aberrant regulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

    BRM targeting compounds and associated methods of use
    4.
    发明专利
    BRM targeting compounds and associated methods of use 未知

    公开(公告)号：AU2019249849B2

    公开(公告)日：2022-03-17

    申请号：AU2019249849

    申请日：2019-04-01

    Applicant: ARVINAS OPERATIONS INC ,  GENENTECH INC

    Inventor： CREW ANDREW P ,  WANG JING ,  BERLIN MICHAEL ,  DRAGOVICH PETER ,  CHEN HUIFEN ,  STABEN LEANNA

    IPC: C07D413/14 ,  A61K31/427 ,  A61P35/00 ,  C07D417/14

    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

    MODULADORES DE LA PROTEOLISIS BCL6 Y METODOS DE USO ASOCIADOS
    10.
    发明专利
    MODULADORES DE LA PROTEOLISIS BCL6 Y METODOS DE USO ASOCIADOS 未知

    公开(公告)号：PE20240639A1

    公开(公告)日：2024-04-04

    申请号：PE2023002843

    申请日：2022-04-15

    Applicant: ARVINAS OPERATIONS INC

    Inventor： BERLIN MICHAEL ,  DONG HANQING ,  SHERMAN DAN ,  SNYDER LAWRENCE B ,  WANG JING ,  ZHANG WEI

    IPC: C07D401/14 ,  A61K31/45 ,  A61P35/00 ,  C07D471/04 ,  C07D487/10

    Abstract: La presente invencion se refiere a compuestos bifuncionales, que tienen la estructura quimica CLM-L-PTM o una sal farmaceuticamente aceptable, enantiomero, estereoisomero, y forma deuterada de estos, en donde: (a) el CLM es un resto de union a la ligasa de ubiquitina E3 cereblon, b) el PTM es una molecula pequena que comprende un resto de direccionamiento a la proteina 6 de linfoma de linfocitos B (BCL6) y c) el L es un grupo enlazador quimico que conecta covalentemente el CLM y el PTM. Estos compuestos bifuncionales encuentran utilidad como moduladores de la proteina 6 del linfoma de linfocitos B (BCL6; proteina diana), se describen en la presente invencion. En particular, los compuestos bifuncionales de la presente descripcion contienen en un extremo un ligando cereblon que se une a la ligasa de ubiquitina E3 respectiva y en el otro extremo un resto que se une a la proteina diana, de manera que la proteina diana se coloca cerca de la ligasa de ubiquitina para efectuar la degradacion (e inhibicion) de la proteina diana. Los compuestos bifuncionales de la presente descripcion exhiben una amplia gama de actividades farmacologicas asociadas con la degradacion/inhibicion de la proteina diana. Las enfermedades o trastornos que resultan de la agregacion o acumulacion de la proteina diana se tratan o evitan con compuestos y composiciones de la presente invencion.

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