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12 条记录 (耗时 0.026 秒)

    Therapeutic Targeting of Casein Kinase 1 Delta in Breast Cancer
    1.
    发明申请
    Therapeutic Targeting of Casein Kinase 1 Delta in Breast Cancer 审中-公开

    公开(公告)号：US20200163972A1

    公开(公告)日：2020-05-28

    申请号：US16694380

    申请日：2019-11-25

    申请人： The Scripps Research Institute

    发明人： William R. Roush ,  Derek R. Duckett ,  John L. Cleveland ,  Laura H. Rosenberg

    IPC分类号： A61K31/5377 ,  C12Q1/6886 ,  A61P35/00

    摘要： The invention provides a method of inhibiting casein kinase 1δ (CK1δ), comprising contacting the CK1δ with a compound of formula (I) as defined herein; such as compound SR-3029. We demonstrate that CSNK1D is amplified and/or overexpressed in human breast tumors and that CK1δ can be medically targeted in human breast cancer subtypes overexpressing this kinase. The invention further provides a method of treating cancer, such as a breast cancer, melanoma, glioblastoma, medulloblastoma, renal, bladder or colon cancer, or a cancer that metastasizes to the brain, lung, or bone provided that both elevated CK1δ and β-catenin dependence are involved in those metastatic diseases. The cancer can be a breast cancer of the triple negative subclass of breast cancers (TNBC), or can be an HER+ breast cancer.

    Therapeutic targeting of casein kinase 1δ in breast cancer
    2.
    发明授权
    Therapeutic targeting of casein kinase 1δ in breast cancer 有权

    公开(公告)号：US10603322B2

    公开(公告)日：2020-03-31

    申请号：US15768257

    申请日：2016-10-05

    申请人： The Scripps Research Institute

    发明人： William R. Roush ,  Derek R. Duckett ,  John L. Cleveland ,  Laura H. Rosenberg

    IPC分类号： A61K31/5377 ,  A61P35/00 ,  C12Q1/6886

    摘要： The invention provides a method of inhibiting casein kinase 1δ (CK1δ), comprising contacting the CK1δ with a compound of formula (I), as defined herein; such as compound SR-3029. We demonstrate that CSNK1D is amplified and/or overexpressed in human breast tumors and that CK1δ can be medically targeted in human breast cancer subtypes overexpressing this kinase. The invention further provides a method of treating cancer, such as a breast cancer, melanoma, glioblastoma, medulloblastoma, renal, bladder or colon cancer, or a cancer that metastasizes to the brain, lung, or bone provided that both elevated CK1δ and β-catenin dependence are involved in those metastatic diseases. The cancer can be a breast cancer of the triple negative subclass of breast cancers (TNBC), or can be an HER+ breast cancer.

    Therapeutic Targeting of Casein Kinase 1 Delta in Breast Cancer
    4.
    发明申请
    Therapeutic Targeting of Casein Kinase 1 Delta in Breast Cancer 审中-公开

    公开(公告)号：US20180311252A1

    公开(公告)日：2018-11-01

    申请号：US15768257

    申请日：2016-10-05

    申请人： The Scripps Research Institute

    发明人： William R. Roush ,  Derek R. Duckett ,  John L. Cleveland ,  Laura H. Rosenberg

    IPC分类号： A61K31/5377 ,  A61P35/00 ,  C12Q1/6886

    CPC分类号： C07D473/16

    摘要： The invention provides a method of inhibiting casein kinase 1δ (CK1δ), comprising contacting the CK1δ with a compound of formula (I), as defined herein; such as compound SR-3029. We demonstrate that CSNK1D is amplified and/or overexpressed in human breast tumors and that CK1δ can be medically targeted in human breast cancer subtypes overexpressing this kinase. The invention further provides a method of treating cancer, such as a breast cancer, melanoma, glioblastoma, medulloblastoma, renal, bladder or colon cancer, or a cancer that metastasizes to the brain, lung, or bone provided that both elevated CK1δ and β-catenin dependence are involved in those metastatic diseases. The cancer can be a breast cancer of the triple negative subclass of breast cancers (TNBC), or can be an HER+ breast cancer.

    SMALL MOLECULE INHIBITORS OF CDK12/CDK13
    7.
    发明申请
    SMALL MOLECULE INHIBITORS OF CDK12/CDK13 有权

    公开(公告)号：US20210186979A1

    公开(公告)日：2021-06-24

    申请号：US17053652

    申请日：2019-05-07

    申请人： The Scripps Research Institute

    发明人： William R. Roush ,  Derek R. Duckett ,  Andrii Monastyrskyi

    IPC分类号： A61K31/5377

    摘要： The invention provides compounds and methods of inhibiting a cyclin-dependent kinase, comprising contacting the cyclin-dependent kinase and an effective amount or concentration of a compound of formula (I) wherein variables are as defined herein. Compounds of formula (I) can be highly selective inhibitors of cyclin-dependent kinases such as CDK12/13, relative to other kinases such as casein kinases, such as CK1δ/ε. Compounds can be used in treatment of cancers, such as breast cancer, brain cancer and ovarian cancer.