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    Kinase inhibitors useful for the treatment of proliferative diseases
    6.
    发明授权
    Kinase inhibitors useful for the treatment of proliferative diseases 失效
    可用于治疗增殖性疾病的激酶抑制剂

    公开(公告)号：US07897762B2

    公开(公告)日：2011-03-01

    申请号：US11854293

    申请日：2007-09-12

    申请人： Daniel L. Flynn ,  Peter A. Petillo ,  Michael D. Kaufman ,  William C. Patt

    发明人： Daniel L. Flynn ,  Peter A. Petillo ,  Michael D. Kaufman ,  William C. Patt

    IPC分类号： A61K31/519 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

    摘要翻译： 本发明涉及可用于治疗各种疾病的新型激酶抑制剂和调节剂化合物。 更具体地，本发明涉及这样的化合物，激酶/化合物加合物，治疗疾病的方法和化合物的合成方法。 优选地，所述化合物可用于调节Raf激酶及其疾病多形体的激酶活性。 本发明的化合物可用于治疗哺乳动物癌症，特别是人类癌症，包括但不限于恶性黑素瘤，结肠直肠癌，卵巢癌，甲状腺乳头状癌，非小细胞肺癌和间皮瘤。 本发明的化合物还可用于治疗类风湿性关节炎和视网膜病变，包括糖尿病性视网膜神经病变和黄斑变性。

    CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES
    8.
    发明申请
    CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES 有权
    环丙沙星和类似物展示抗癌和抗增生活性

    公开(公告)号：US20100120806A1

    公开(公告)日：2010-05-13

    申请号：US12608578

    申请日：2009-10-29

    申请人： Daniel L. Flynn ,  Peter A. Petillo ,  Michael D. Kaufman

    发明人： Daniel L. Flynn ,  Peter A. Petillo ,  Michael D. Kaufman

    IPC分类号： A61K31/4439 ,  C07D401/04 ,  C07D413/04 ,  C07D401/14 ,  C07D403/04 ,  A61K31/444 ,  A61K31/506 ,  A61P35/00 ,  A61P35/02 ,  A61P25/00 ,  A61P3/00

    CPC分类号： C07D413/04 ,  A61K31/555 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04

    摘要： Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-α kinase, PDGFR-β kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.

    摘要翻译： 本发明的化合物可用于治疗哺乳动物癌症，特别是人类癌症，包括但不限于恶性黑素瘤，实体瘤，成胶质细胞瘤，卵巢癌，胰腺癌，前列腺癌，肺癌，乳腺癌，肾癌， 肝癌，宫颈癌，原发性肿瘤部位转移，骨髓增生性疾病，慢性骨髓性白血病，白血病，甲状腺乳头状癌，非小细胞肺癌，间皮瘤，嗜酸性粒细胞综合征，胃肠道间质瘤，结肠癌，以过度增生为特征的眼部疾病 包括各种视网膜病变，糖尿病性视网膜病变，类风湿性关节炎，哮喘，慢性阻塞性肺疾病，肥大细胞增多症，肥大细胞白血病和由PDGFR-α激酶引起的疾病，PDGFR-＆bgr; 激酶，c-KIT激酶，cFMS激酶，c-MET激酶和致癌形式，异常融合蛋白和任何前述激酶的多态性。