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    SELECTIVE ANDROGEN RECEPTOR COVALENT ANTAGONISTS (SARCAS) AND METHODS OF USE THEREOF
    2.
    发明申请
    SELECTIVE ANDROGEN RECEPTOR COVALENT ANTAGONISTS (SARCAS) AND METHODS OF USE THEREOF 审中-公开

    公开(公告)号：WO2021173731A1

    公开(公告)日：2021-09-02

    申请号：PCT/US2021/019490

    申请日：2021-02-24

    Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

    Inventor： NARAYANAN, Ramesh ,  PONNUSAMY, Thamarai ,  MILLER, Duane D. ,  HE, Yali ,  HWANG, Dong-Jin

    IPC: A61K31/325 ,  A61K45/06 ,  C07C271/02

    Abstract: This invention relates to selective androgen receptor covalent antagonists, synthetic intermediates and by-products, and related compounds, and compositions comprising the same, and uses thereof in treating androgen receptor dependent diseases and conditions such as hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR.

    SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
    5.
    发明申请
    SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开

    公开(公告)号：WO2020243373A1

    公开(公告)日：2020-12-03

    申请号：PCT/US2020/035015

    申请日：2020-05-28

    Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

    Inventor： NARAYANAN, Ramesh ,  MILLER, Duane D. ,  PONNUSAMY, Thamarai ,  HWANG, Dong-Jin ,  HE, Yali

    IPC: C07C237/20 ,  A61K31/167 ,  A61P5/28

    Abstract: This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including cyclic and heterocyclic anilide rings and their synthetic precursors, and mono-, di-, or multi-substituted N-heterocyclic rings, R-isomers, non-hydroxylated and/or non-chiral propanamides in treating androgen receptor dependent diseases and conditions such as hyperproliferations of the prostate including pre-malignancies and benign prostatic hyperplasia, prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

    SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF
    6.
    发明申请
    SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF 审中-公开
    选择性雄激素受体降解物（SARD）配体及其使用方法

    公开(公告)号：WO2017214634A1

    公开(公告)日：2017-12-14

    申请号：PCT/US2017/037063

    申请日：2017-06-12

    Applicant: UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION

    Inventor： NARAYANAN, Ramesh ,  MILLER, Duane ,  PONNUSAMY, Thamarai ,  HWANG, Dong-Jin ,  HE, Yali

    IPC: A61K31/325 ,  C07C271/02

    Abstract: This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R -isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.

    Abstract translation: 本发明涉及吡咯，吡唑，咪唑，三唑和基于吗啉的选择性雄激素受体降解剂（SARD）化合物，包括杂环酰苯胺环及其合成前体，R- 异构体和非羟基化和/或非手性丙酰胺，以及其在治疗前列腺癌，晚期前列腺癌，去势抵抗性前列腺癌，三阴性乳腺癌，表达雄激素受体的其他癌症，雄激素性脱发或其他 高雄激素性皮肤病，肯尼迪氏病，肌萎缩性侧索硬化症（ALS），腹主动脉瘤（AAA）和子宫肌瘤，以及降低包括致病性或抗性突变在内的雄激素受体全长（AR-FL） （AR-SV）和AR的致病性聚谷氨酰胺（polyQ）多态性。

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