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49 条记录 (耗时 0.036 秒)

    ANTI-PROLIFERATIVE COMPOUNDS AND USES THEREOF
    4.
    发明申请
    ANTI-PROLIFERATIVE COMPOUNDS AND USES THEREOF 有权
    抗增生化合物及其用途

    公开(公告)号：US20150191417A1

    公开(公告)日：2015-07-09

    申请号：US14413745

    申请日：2013-07-10

    申请人： Dana-Farber Cancer Institute, Inc. ,  The General Hospital Corporation d/b/a Massachusettls General Hospital

    发明人： Kenneth C. Anderson ,  Teru Hideshima ,  Ralph Mazitschek ,  Gullu Gorgun

    IPC分类号： C07C223/06 ,  C07D233/80 ,  C07C251/48 ,  C07C251/86 ,  C07D211/62

    CPC分类号： C07C223/06 ,  A61K31/136 ,  A61K31/15 ,  A61K31/164 ,  A61K31/165 ,  A61K31/216 ,  A61K31/395 ,  A61K31/4166 ,  A61K31/445 ,  A61K31/655 ,  A61K31/69 ,  A61K45/06 ,  C07C251/48 ,  C07C251/86 ,  C07D211/62 ,  C07D233/80 ,  A61K2300/00

    摘要： The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, tautomers, stereoisomers, solvates, hydrates, polymorphs, and compositions thereof. Also provided are methods and kits involving the inventive compounds for treating proliferative diseases (e.g., cancers (e.g., breast cancer, prostate cancer, lung cancer, and ovarian cancer), benign neoplasms, angiogenesis, inflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound of the invention may enhance the anti-tumor immune response by inhibiting or eliminating the immune suppression mediated by immune suppressor myeloid cells (MDSCs), inducing apoptosis, and/or inhibit or down-regulate proteins (e.g., epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), estrogen receptor (ER), X-linked inhibitor of apoptosis protein (XIAP), and heat shock protein 90 (Hsp90)) in the subject.

    摘要翻译： 本发明提供新的式（I）化合物及其药学上可接受的盐，互变异构体，立体异构体，溶剂合物，水合物，多晶型物及其组合物。 还提供了涉及用于治疗受试者的增殖性疾病（例如，癌症（例如，乳腺癌，前列腺癌，肺癌和卵巢癌），良性肿瘤，血管发生，炎性疾病和自身免疫性疾病）的本发明化合物的方法和试剂盒 。 使用本发明化合物治疗患有增殖性疾病的受试者可通过抑制或消除由免疫抑制骨髓细胞（MDSC）介导的免疫抑制，诱导凋亡和/或抑制或下调 蛋白质（例如表皮生长因子受体（EGFR），人表皮生长因子受体2（HER2），雌激素受体（ER），X连锁蛋白抑制剂（XIAP）和热休克蛋白90（Hsp90）） 学科。

    Histone deacetylase inhibitors
    8.
    发明授权
    Histone deacetylase inhibitors 有权
    组蛋白脱乙酰酶抑制剂

    公开(公告)号：US09199923B2

    公开(公告)日：2015-12-01

    申请号：US14198764

    申请日：2014-03-06

    申请人： President and Fellows of Harvard College ,  Dana-Farber Cancer Institute Inc.

    发明人： James Elliot Bradner ,  Ralph Mazitschek

    IPC分类号： A61K31/47 ,  A61K31/19 ,  C07C259/06 ,  A61K31/337 ,  A61K31/165 ,  C07D413/12 ,  C07C235/78 ,  C07D319/06

    CPC分类号： A61K31/231 ,  A61K9/0014 ,  A61K31/165 ,  A61K31/337 ,  C07C235/78 ,  C07C259/06 ,  C07D319/06 ,  C07D413/12

    摘要： In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.

    摘要翻译： 鉴于需要开发新的治疗剂，本发明提供了新的组蛋白脱乙酰酶抑制剂。 这些化合物包括酯键，使它们对酯酶的失活敏感。 因此，这些化合物特别可用于治疗皮肤病。 当化合物达到血流时，酯酶或具有酯酶活性的酶将化合物切割成具有大大降低的活性的生物活性片段或片段。理想地，这些降解产物表现出短的血清和/或全身半衰期并被快速消除。 这些化合物及其药物组合物例如特别可用于治疗皮肤T细胞淋巴瘤，神经纤维瘤病，牛皮癣，脱发，皮肤色素沉着和皮炎。 本发明还提供了制备本发明化合物及其中间体的方法。

    Histone deacetylase inhibitors
    10.
    发明授权
    Histone deacetylase inhibitors 有权

    公开(公告)号：US10172821B2

    公开(公告)日：2019-01-08

    申请号：US15637078

    申请日：2017-06-29

    申请人： President & Fellows of Harvard College ,  Dana-Farber Cancer Institute, Inc.

    发明人： James Elliot Bradner ,  Ralph Mazitschek

    IPC分类号： A61K31/165 ,  A61K31/231 ,  A61K31/337 ,  C07C259/06 ,  C07D413/12 ,  C07C235/78 ,  C07D319/06 ,  A61K9/00

    摘要： In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.