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56 条记录 (耗时 0.031 秒)

    FAP-TARGETED RADIOPHARMACEUTICALS AND IMAGING AGENTS, AND USES RELATED THERETO
    1.
    发明申请
    FAP-TARGETED RADIOPHARMACEUTICALS AND IMAGING AGENTS, AND USES RELATED THERETO 有权

    公开(公告)号：US20220370647A1

    公开(公告)日：2022-11-24

    申请号：US17211481

    申请日：2021-03-24

    申请人： Trustees of Tufts College

    发明人： William W. Bachovchin ,  Hung-sen Lai ,  Wengen Wu

    IPC分类号： A61K51/04

    摘要： The tumor stroma, which accounts for a large part of the tumor mass, represents an attractive target for the delivery of diagnostic and therapeutic compounds. Here, the focus is notably on a subpopulation of stromal cells, known as cancer-associated fibroblasts, which are present in more than 90% of epithelial carcinomas, including pancreatic, colon, and breast cancer. Cancer-associated fibroblasts feature high expression of FAP, which is not detectable in adult normal tissue but is associated with a poor prognosis in cancer patients. The present invention provides small-molecule radiopharmaceutical and imaging agents based on a FAP-specific inhibitor.

    Non-flushing niacin analogues, and methods of use thereof
    7.
    发明授权
    Non-flushing niacin analogues, and methods of use thereof 有权
    非潮红烟酸类似物及其使用方法

    公开(公告)号：US08889720B2

    公开(公告)日：2014-11-18

    申请号：US13715242

    申请日：2012-12-14

    申请人： Trustees of Tufts College

    发明人： William W. Bachovchin ,  Hung-sen Lai

    IPC分类号： C07D213/02 ,  C07D401/06 ,  A61K31/44 ,  A61K31/4439 ,  C07D213/80 ,  A61K45/06 ,  C07D213/55

    CPC分类号： A61K31/4439 ,  A61K45/06 ,  C07D213/55 ,  C07D213/80 ,  C07D401/06

    摘要： One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.

    摘要翻译： 本发明的一个方面涉及对一系列哺乳动物疾病具有活性的取代吡啶及其药学上可接受的盐。 本发明的另一方面涉及包含本发明化合物或其药学上可接受的盐的药物组合物; 和药学上可接受的赋形剂。 本发明还涉及治疗一系列哺乳动物疾病或病症的方法，包括但不限于高脂血症，高胆固醇血症，动脉粥样硬化，冠状动脉疾病，充血性心力衰竭，心血管疾病，高血压，冠心病，心绞痛，皮癣，Hartnup's 综合征，类癌综合征，动脉闭塞性疾病，肥胖，甲状腺功能减退，血管收缩，骨关节炎，类风湿性关节炎，糖尿病，阿尔茨海默病，脂肪营养不良或血脂异常，提高血清高密度脂蛋白（HDL）水平，降低血清低密度脂蛋白 ）级别。