PYRIDO [4,3-d] PYRIMIDIN-4 (3H) -ONE DERIVATIVES AS CALCIUM RECEPTOR ANTAGONISTS
    2.
    发明申请
    PYRIDO [4,3-d] PYRIMIDIN-4 (3H) -ONE DERIVATIVES AS CALCIUM RECEPTOR ANTAGONISTS 失效
    吡咯并[4,3-d]嘧啶-4(3H) - 酮衍生物作为钙受体拮抗剂

    公开(公告)号:US20080085887A1

    公开(公告)日:2008-04-10

    申请号:US11867255

    申请日:2007-10-04

    CPC分类号: C07D471/04

    摘要: The present invention is directed to novel pyrido[4,3-d]pyrimidin-4(3H)-one derivatives and pharmaceutically acceptable salts thereof of structural formula I wherein the variables R1, R2, R3, R4 and R5 are as described herein. Also provided are pharmaceutical compositions comprising the compounds of formula I as well as methods of treatment employing compounds of formula I to treat a disease or disorder characterized by abnormal bone or mineral homeostasis such as hypoparathyroidism, osteoporosis, osteopenia, periodontal disease, Paget's disease, bone fracture, osteoarthritis, rheumatoid arthritis, and humoral hypercalcemia of malignancy.

    摘要翻译: 本发明涉及结构式I的新型吡啶并[4,3-d]嘧啶-4(3H) - 酮衍生物及其药学上可接受的盐,其中变量R 1,R 2, 2,R 3,R 4和R 5如本文所述。 还提供了包含式I化合物的药物组合物以及使用式I化合物治疗以异常骨或矿物质稳态为特征的疾病或病症的方法,例如甲状旁腺功能减退症,骨质疏松症,骨质减少症,牙周病,佩吉特氏病,骨骼 骨折,骨关节炎,类风湿关节炎和恶性肿瘤的体液性高钙血症。

    Methods for Augmenting Bone
    8.
    发明申请
    Methods for Augmenting Bone 审中-公开
    增强骨的方法

    公开(公告)号:US20090118316A1

    公开(公告)日:2009-05-07

    申请号:US11570815

    申请日:2005-06-10

    CPC分类号: A61K31/506 A61K31/00

    摘要: The present invention relates to methods of stimulating osteoblast function with a PYK2 inhibitor in subjects with osteoporosis, bone fractures, non-unions, pseudoarthroses, periodontal disease or other disorders of bone metabolism. Optionally, the method further comprises administration of a second therapeutic bone agent. The present invention also relates to methods to identify a PYK2 inhibitor effective as a therapeutic bone agent comprising administering a test agent to an osteoblast-like cell and determining if osteoblast function is stimulated. Optionally, the identifying method further comprises contacting the test agent with PYK2 and determining if PYK2 activity is inhibited.

    摘要翻译: 本发明涉及在具有骨质疏松症,骨折,非联合,假性关节炎,牙周病或其他骨代谢紊乱的受试者中用PYK2抑制剂刺激成骨细胞功能的方法。 任选地,所述方法还包括施用第二治疗骨剂。 本发明还涉及鉴定有效作为治疗性骨质的PYK2抑制剂的方法,其包括向成骨细胞样细胞施用测试试剂并确定是否刺激成骨细胞功能。 任选地,识别方法还包括使测试试剂与PYK2接触并确定PYK2活性是否被抑制。