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    Synthetic antibody mimetic compounds (SyAMs) targeting cancer, especially prostate cancer
    1.
    发明授权
    Synthetic antibody mimetic compounds (SyAMs) targeting cancer, especially prostate cancer 有权

    公开(公告)号：US10912836B2

    公开(公告)日：2021-02-09

    申请号：US16180494

    申请日：2018-11-05

    申请人： YALE UNIVERSITY

    发明人： David A. Spiegel ,  Patrick McEnaney ,  Kelly Fitzgerald

    IPC分类号： A61K47/55 ,  C07D249/04 ,  C07D249/06 ,  A61K47/54 ,  A61K31/194 ,  A61K38/10 ,  A61K45/06

    摘要： The present invention relates to compounds which function as antibody mimetic compounds. These compounds are bifunctional/multifunctional compounds which contain at least one cancer cell binding moiety which selectively binds to prostate specific membrane antigen (PSMA) and a FC receptor binding moiety which modulates an FC immune receptor, preferably a FcγRI receptor. Compounds according to the present invention bind selectively to cancer cells which upregulate PSMA and through that interaction, place the Fc receptor binding moiety of the compound in proximity to a Fc receptor, preferably a FcγRI receptor, which can modulate (preferably, upregulate) a humoral response in a patient to cancer cells. Through this biological action of the compounds according to the present invention, cancer cells, including metastatic cancer cells, especially prostate cancer cells can be immune regulated, resulting in the favorable therapy of cancer in a patient. Methods of using these compounds to treat cancer and/or reduce the likelihood of metastasis of cancer are additional aspects of the present invention.

    REPROGRAMMING UROKINASE INTO AN ANTIBODY-RECRUITING ANTICANCER AGENT
    3.
    发明申请
    REPROGRAMMING UROKINASE INTO AN ANTIBODY-RECRUITING ANTICANCER AGENT 审中-公开
    将尿激酶转化成抗体受体反应剂

    公开(公告)号：US20140308342A1

    公开(公告)日：2014-10-16

    申请号：US14356820

    申请日：2012-11-07

    申请人： YALE UNIVERSITY

    发明人： David A. Spiegel ,  Charles E. Jakobsche

    IPC分类号： C12N9/96 ,  C07K5/062 ,  A61K38/05 ,  A61K38/48 ,  A61K45/06 ,  C07D491/107 ,  A61K31/352

    CPC分类号： C12N9/96 ,  A61K31/165 ,  A61K31/352 ,  A61K31/365 ,  A61K38/05 ,  A61K38/482 ,  A61K45/06 ,  A61K47/54 ,  A61K47/60 ,  C07C279/12 ,  C07D491/107 ,  C07D493/10 ,  C07K5/06026 ,  A61K2300/00

    摘要： The present invention relates to chimeric (preferably, bifunctional) compounds, compositions comprising those compounds and methods of treating cancer in a patient or subject, especially including metastatic cancer where cancer cells exhibit overexpression (heightened expression) of cell surface urokinase-type plasminogen activator receptor (urokinase receptor) compared to normal (non-cancerous) cells. The compounds preferably covalently bind to the urokinase receptor and recruit native antibodies of the patient or subject where the antibodies can selectively degrade and/or deactivate targeted cancer cells through antibody-dependent cellular phagocytosis and/or antibody-dependent cellular cytotoxicity (ADCC) against a large number and variety of cancers, thus providing cancer cell death and/or an inhibition of growth, elaboration and/or metastasis of the cancer, including remission and cure of the patient's cancer.

    摘要翻译： 本发明涉及嵌合（优选双官能）化合物，包含这些化合物的组合物和治疗患者或受试者中的癌症的方法，特别是包括转移性癌症，其中癌细胞表现出细胞表面尿激酶型纤溶酶原激活物受体的过表达（高表达） （尿激酶受体）与正常（非癌性）细胞相比。 化合物优选共价结合尿激酶受体并招募患者或受试者的天然抗体，其中抗体可以通过抗体依赖性细胞吞噬作用和/或抗体依赖性细胞毒性（ADCC）选择性降解和/或失活靶向癌细胞 大量和多种癌症，从而提供癌细胞死亡和/或抑制癌症的生长，修复和/或转移，包括缓解和治愈患者的癌症。

    SYNTHETIC ANTIBODY MIMETIC COMPOUNDS (SYAMS) TARGETING CANCER, ESPECIALLY PROSTATE CANCER
    5.
    发明申请
    SYNTHETIC ANTIBODY MIMETIC COMPOUNDS (SYAMS) TARGETING CANCER, ESPECIALLY PROSTATE CANCER 有权

    公开(公告)号：US20220111060A1

    公开(公告)日：2022-04-14

    申请号：US17122319

    申请日：2020-12-15

    申请人： YALE UNIVERSITY

    发明人： David A. Spiegel ,  Patrick McEnaney ,  Kelly Fitzgerald

    IPC分类号： A61K47/55 ,  C07D249/04 ,  C07D249/06 ,  A61K47/54 ,  A61K31/194 ,  A61K38/10 ,  A61K45/06

    摘要： The present invention relates to compounds which function as antibody mimetic compounds. These compounds are bifuinctional/multifuinctional compounds which contain at least one cancer cell binding moiety which selectively binds to prostate specific membrane antigen (PSMA) and a FC receptor binding moiety which modulates an FC immune receptor, preferably a FcγRI receptor. Compounds according to the present invention bind selectively to cancer cells which upregulate PSMA and through that interaction, place the Fc receptor binding moiety of the compound in proximity to a Fc receptor, preferably a FcγRI receptor, which can modulate (preferably, upregulate) a humoral response in a patient to cancer cells. Through this biological action of the compounds according to the present invention, cancer cells, including metastatic cancer cells, especially prostate cancer cells can be immune regulated, resulting in the favorable therapy of cancer in a patient. Methods of using these compounds to treat cancer and/or reduce the likelihood of metastatis of cancer are additional aspects of the present invention.

    THERAPEUTIC DNP DERIVATIVES AND METHODS USING SAME
    8.
    发明申请
    THERAPEUTIC DNP DERIVATIVES AND METHODS USING SAME 审中-公开
    治疗DNP衍生物及其使用方法

    公开(公告)号：US20160207873A1

    公开(公告)日：2016-07-21

    申请号：US14914408

    申请日：2014-08-28

    申请人： YALE UNIVERSITY

    发明人： Gerald I. Shulman ,  David A. Spiegel

    IPC分类号： C07C205/37 ,  A61K31/085

    CPC分类号： C07C205/37 ,  A61K31/085 ,  C07J41/0055

    摘要： The present invention includes DNP derivatives of formula (I) that are useful for preventing or treating a metabolic disease or disorder in a subject in need thereof. In certain embodiments, the subject is further administered at least one additional therapeutic agent.

    摘要翻译： 本发明包括可用于预防或治疗有需要的受试者的代谢疾病或病症的式（I）的DNP衍生物。 在某些实施方案中，受试者进一步施用至少一种另外的治疗剂。

    Synthetic antibody mimetic compounds (SYAMS) targeting cancer, especially prostate cancer
    9.
    发明授权
    Synthetic antibody mimetic compounds (SYAMS) targeting cancer, especially prostate cancer 有权

    公开(公告)号：US12042542B2

    公开(公告)日：2024-07-23

    申请号：US17122319

    申请日：2020-12-15

    申请人： YALE UNIVERSITY

    发明人： David A. Spiegel ,  Patrick McEnaney ,  Kelly Fitzgerald

    IPC分类号： A61K47/55 ,  A61K31/194 ,  A61K38/10 ,  A61K45/06 ,  A61K47/54 ,  C07D249/04 ,  C07D249/06

    CPC分类号： A61K47/55 ,  A61K31/194 ,  A61K38/10 ,  A61K45/06 ,  A61K47/54 ,  C07D249/04 ,  C07D249/06

    摘要： The present invention relates to compounds which function as antibody mimetic compounds. These compounds are bifunctional/multifunctional compounds which contain at least one cancer cell binding moiety which selectively binds to prostate specific membrane antigen (PSMA) and a FC receptor binding moiety which modulates an FC immune receptor, preferably a FcγRI receptor. Compounds according to the present invention bind selectively to cancer cells which upregulate PSMA and through that interaction, place the Fc receptor binding moiety of the compound in proximity to a Fc receptor, preferably a FcγRI receptor, which can modulate (preferably, upregulate) a humoral response in a patient to cancer cells. Through this biological action of the compounds according to the present invention, cancer cells, including metastatic cancer cells, especially prostate cancer cells can be immune regulated, resulting in the favorable therapy of cancer in a patient. Methods of using these compounds to treat cancer and/or reduce the likelihood of metastatis of cancer are additional aspects of the present invention.