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    METHYLENE DERIVATIVES
    5.
    发明申请
    METHYLENE DERIVATIVES 审中-公开
    甲基衍生物

    公开(公告)号：WO2006061715A2

    公开(公告)日：2006-06-15

    申请号：PCT/IB2005003769

    申请日：2005-12-05

    Applicant: WARNER LAMBERT CO ,  BOOTH RICHARD JOHN ,  O'BRIEN PATRICK MICHAEL

    Inventor： BOOTH RICHARD JOHN ,  O'BRIEN PATRICK MICHAEL

    IPC: C07D213/56 ,  A61K31/455 ,  A61P35/00

    CPC classification number: C07D213/81 ,  C07D213/56

    Abstract: This invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof; a pharmaceutical composition; a method of treating a disease mediated by an MMP-13 enzyme in a mammal; and a therapeutic combination containing at least two pharmaceutically active components, wherein R 1

    Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐; 药物组合物; 治疗哺乳动物中由MMP-13酶介导的疾病的方法; 和含有至少两种药物活性成分的治疗组合，其中R 1

    METHODS AND COMPOSITIONS FOR THE TREATMENT OF MYELOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES
    8.
    发明申请
    METHODS AND COMPOSITIONS FOR THE TREATMENT OF MYELOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES 审中-公开
    治疗失语性疾病和其他增殖性疾病的方法和组合

    公开(公告)号：WO2012019015A2

    公开(公告)日：2012-02-09

    申请号：PCT/US2011046609

    申请日：2011-08-04

    Applicant: DECIPHERA PHARMACEUTICALS LLC ,  FLYNN DANIEL L ,  PETILLO PETER A ,  KAUFMAN MICHAEL D ,  BOOTH RICHARD JOHN

    Inventor： FLYNN DANIEL L ,  PETILLO PETER A ,  KAUFMAN MICHAEL D ,  BOOTH RICHARD JOHN

    IPC: A61K39/395 ,  A61K31/454 ,  A61K31/506 ,  A61K31/519 ,  A61P11/00 ,  A61P19/00 ,  A61P35/00

    CPC classification number: A61K31/454 ,  A61K31/506 ,  A61K31/519

    Abstract: Compounds of the present invention find utility in the treatment of hyperproliferative diseases, including autoimmune diseases and other diseases characterized by hypervascularization or proliferation of myeloid, mast cells, fibroblasts, synoviocytes, or monocytes; mammalian cancers and especially human cancers including but not limited to melanomas; a disease caused by c-ABL kinase, oncogenic forms thereof, aberrant fusion proteins thereof including BCR-ABL kinase and polymorphs thereof; a disease caused by FLT-3 kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof; a disease caused by cMET kinase, oncogenic forms thereof, aberrant fusion proteins thereof including TPR-MET; a disease caused by KDR kinase or PDGFR kinases; a disease caused by HER kinases, oncogenic forms thereof and polymorphs thereof; a disease caused by RET kinase, oncogenic forms thereof, aberrant fusion proteins thereof; a disease caused by c-FMS kinase, oncogenic forms thereof and polymorphs thereof; a disease caused by a c-KIT kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof; and diseases caused by any of the foregoing kinases, oncogenic forms thereof, and aberrant fusion proteins thereof, including but not limited to, chronic myelogenous leukemia, acute lymphocytic leukemia, acute myeloid leukemia, other myeloproliferative disorders, a disease caused by metastasis of primary solid tumors to secondary sites, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, mesothelioma, hypereosinophilic syndrome, a disease caused or maintained by pathological vascularization, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, i.e. diabetic retinopathy and age-related macular degeneration, non small cell lung cancer, breast cancers, kidney cancers, colon cancers, cervical carcinomas, papillary thyroid carcinoma, melanomas, autoimmune diseases including rheumatoid arthritis, multiple sclerosis, lupus, asthma, human inflammation, rheumatoid spondylitis, ostero-arthritis, asthma, gouty arthritis, sepsis, septic shock, endotoxic shock, Gram-negative sepsis, toxic shock syndrome, adult respiratory distress syndrome, stroke, reperfusion injury, neural trauma, neural ischemia, psoriasis, restenosis, chronic obstructive pulmonary disease, bone resorptive diseases, bone cancer, graft-versus-host reaction, Chron's disease, ulcerative colitis, inflammatory bowel disease, pyresis, gastrointestinal stromal tumors, mastocytosis, mast cell leukemia, and combinations thereof.

    Abstract translation: 本发明的化合物可用于治疗过度增殖性疾病，包括自身免疫疾病和其它特征在于骨髓，肥大细胞，成纤维细胞，滑膜细胞或单核细胞的高血管形成或增殖的疾病; 哺乳动物癌症，特别是人类癌症，包括但不限于黑素瘤; 由c-ABL激酶，其致癌形式引起的疾病，异常融合蛋白，包括BCR-ABL激酶及其多态性; 由FLT-3激酶，其致癌形式，异常融合蛋白及其多态性引起的疾病; 由cMET激酶引起的疾病，其致癌形式，异常融合蛋白，包括TPR-MET; 由KDR激酶或PDGFR激酶引起的疾病; 由HER激酶，其致癌形式及其多晶型物引起的疾病; 由RET激酶，其致癌形式，异常融合蛋白引起的疾病; 由c-FMS激酶，其致癌形式及其多形体引起的疾病; 由c-KIT激酶，其致癌形式，异常融合蛋白及其多态性引起的疾病; 以及由上述激酶，其致癌形式及其异常融合蛋白引起的疾病，包括但不限于慢性骨髓性白血病，急性淋巴细胞性白血病，急性骨髓性白血病，其他骨髓增生性疾病，由原发性转移引起的疾病 肿瘤到继发部位，胶质母细胞瘤，卵巢癌，胰腺癌，前列腺癌，肺癌，间皮瘤，嗜酸性粒细胞综合征，由病理性血管形成引起或维持的疾病，以过度增生为特征的眼病，导致失明，包括各种视网膜病变，即糖尿病性视网膜病变和年龄 相关黄斑变性，非小细胞肺癌，乳腺癌，肾癌，结肠癌，宫颈癌，甲状腺乳头状癌，黑素瘤，自身免疫性疾病，包括类风湿性关节炎，多发性硬化症，狼疮，哮喘，人类炎症，类风湿性脊椎炎， 关节炎，哮喘，痛风 脓毒病，败血症，败血症休克，内毒素休克，革兰氏阴性败血症，中毒性休克综合征，成人呼吸窘迫综合征，中风，再灌注损伤，神经创伤，神经缺血，牛皮癣，再狭窄，慢性阻塞性肺病，骨吸收性疾病， ，移植物抗宿主反应，克隆氏病，溃疡性结肠炎，炎症性肠病，胃肠道间质瘤，肥大细胞增多症，肥大细胞白血病及其组合。

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