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 审中-公开
    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:US20110028452A1

    公开(公告)日:2011-02-03

    申请号:US12894525

    申请日:2010-09-30

    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R1,R2,R3,R4和R5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。

    Laser peening for reducing hydrogen embrittlement
    3.
    发明授权
    Laser peening for reducing hydrogen embrittlement 有权
    用于减少氢脆的激光喷丸

    公开(公告)号:US07723643B2

    公开(公告)日:2010-05-25

    申请号:US11400618

    申请日:2006-04-06

    IPC分类号: B23K26/00

    CPC分类号: B23K26/356

    摘要: A laser peening process for the densification of metal surfaces and sub-layers and for changing surface chemical activities provides retardation of the up-take and penetration of atoms and molecules, particularly Hydrogen, which improves the lifetime of such laser peened metals. Penetration of hydrogen into metals initiates an embrittlement that leaves the material susceptible to cracking.

    摘要翻译: 用于金属表面和亚层的致密化和用于改变表面化学活性的激光喷丸方法提供了原子和分子(特别是氢)的上升和穿透的延迟,这提高了这种激光喷丸金属的寿命。 氢气渗透到金属中会导致脆化,使得材料易于破裂。

    Pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as calcium receptor antagonists
    6.
    发明授权
    Pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as calcium receptor antagonists 失效
    吡啶并[4,3-d]嘧啶-4(3H) - 酮衍生物作为钙受体拮抗剂

    公开(公告)号:US07829572B2

    公开(公告)日:2010-11-09

    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R1,R2,R3,R4和R5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。

    Glucocorticoid receptor modulators
    8.
    发明授权
    Glucocorticoid receptor modulators 失效
    糖皮质激素受体调节剂

    公开(公告)号:US06852719B2

    公开(公告)日:2005-02-08

    申请号:US10012274

    申请日:2001-10-26

    摘要: The present invention provides non-steroidal compounds of Formula I, including prodrugs and pharmaceutically acceptable salts thereof, which are selective modulators (e.g., agonists, partial agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to treat diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides processes for preparing these compounds

    摘要翻译: 本发明提供式I的非类固醇化合物,包括其前体药物和药学上可接受的盐,其是类固醇受体的特异性调节剂(例如激动剂,部分激动剂和拮抗剂),特别是糖皮质激素受体。 本发明还提供含有这些化合物的药物组合物和使用这些化合物治疗需要糖皮质激素受体激动剂或拮抗剂治疗的动物的方法。 糖皮质激素受体调节剂可用于治疗如下所述的疾病,例如肥胖,糖尿病,炎症等。 本发明还提供了制备这些化合物的方法

    Glucocorticoid receptor modulators
    10.
    发明授权
    Glucocorticoid receptor modulators 有权
    糖皮质激素受体调节剂

    公开(公告)号:US07713989B2

    公开(公告)日:2010-05-11

    申请号:US11580996

    申请日:2006-10-13

    IPC分类号: A61K31/44 C07D471/12

    摘要: The present invention provides non-steroidal compounds of formula I which are selective modulators (i.e., agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to the diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides intermediates and processes for preparing these compounds.

    摘要翻译: 本发明提供了类固醇受体的选择性调节剂(即激动剂和拮抗剂),特别是糖皮质激素受体的式I的非类固醇化合物。 本发明还提供含有这些化合物的药物组合物和使用这些化合物治疗需要糖皮质激素受体激动剂或拮抗剂治疗的动物的方法。 糖皮质激素受体调节剂可用于如下所述的疾病,例如肥胖,糖尿病,炎症等。 本发明还提供了制备这些化合物的中间体和方法。