Methods for Augmenting Bone
    4.
    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。

    Arachidonic acid analogs
    5.
    发明授权
    Arachidonic acid analogs 失效
    花生四烯酸类似物

    公开(公告)号:US4670465A

    公开(公告)日:1987-06-02

    申请号:US866177

    申请日:1986-05-21

    摘要: Long chain unsaturated hydrocarbon derivatives, having from 13 to 21 carbon atoms, which are substituted at the 1-position by a phenoxy, phenylthio or a phenyl that bear a carboxylic acid group at the ortho, meta or para positions, and up to 4 carbon-carbon triple bonds, methods of preparing them, and pharmaceutical preparations containing them. These compounds are useful as lipoxygenase inhibitors, and therefore as antiinflammatory agents.

    摘要翻译: 具有13至21个碳原子的长链不饱和烃衍生物,其在1-位被苯邻,苯硫基或在邻位,间位或对位具有羧酸基的苯基和至多4个碳所取代 碳三键,其制备方法和含有它们的药物制剂。 这些化合物可用作脂氧合酶抑制剂,因此可用作抗炎剂。

    Substituted prostaglandin derivatives
    6.
    发明授权
    Substituted prostaglandin derivatives 失效
    取代前列腺素衍生物

    公开(公告)号:US3953470A

    公开(公告)日:1976-04-27

    申请号:US487504

    申请日:1974-07-11

    摘要: Prostaglandin analogs of the PGF.sub.2.sub..alpha., PGE.sub.2, PGF.sub.1.sub..alpha. and PGE.sub.1 series substituted at C-10.alpha. by a hydroxyl group, the derivatives of the PGF.sub.1.sub..alpha. and PGE.sub.1 series further substituted at C-5,6 by a methylene or dihalomethylene group, and the 10,11-ketals thereof and methods of preparing such compounds. 9.alpha.,15.alpha.-Dihydroxy-10.alpha.,11.alpha.-isopropylidenedioxyprosta-5,13-dienoic acid, 9-keto-10.alpha.,11.alpha.-isopropylidenedioxy-15.alpha.-hydroxyprosta-5,13-dienoic acid and 5,6-methylene-9.alpha.,15.alpha.-dihydroxy-10.alpha.,11.alpha.-isopropylidenedioxyprost-13-enoic acid are representative of the class. Also included are the corresponding esters, ethers, pharmaceutically acceptable salts and amides. These compounds possess prostaglandin-like activity and thus are useful in the treatment of mammals, where prostaglandins are indicated.

    摘要翻译: 在C-10α被羟基取代的PGF2α,PGE2,PGF1α和PGE1系列的前列腺素类似物,P-Aα和PGE1序列的衍生物在C-5,6上被亚甲基或二卤代亚甲基取代,以及 其10,11缩酮及其制备方法。 9α,15α-二羟基-10α,11α-异亚丙基二氧基孕甾-5,13-二烯酸,9-酮-10α,11α-异亚丙基二氧基-15α-羟基孕甾-5,13-二烯酸和5,6 - 亚甲基-9α,15α-二羟基-10α,11α-异亚丙基二氧代孕甾-6-烯酸是该类的代表。 还包括相应的酯,醚,药学上可接受的盐和酰胺。 这些化合物具有前列腺素样活性,因此可用于治疗表达前列腺素的哺乳动物。

    PYRIDO [4,3-d] PYRIMIDIN-4 (3H) -ONE DERIVATIVES AS CALCIUM RECEPTOR ANTAGONISTS
    8.
    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。