Isoprenoid pathway inhibitors for stimulating bone growth
    4.
    发明授权
    Isoprenoid pathway inhibitors for stimulating bone growth 有权
    用于刺激骨生长的异戊二醛途径抑制剂

    公开(公告)号:US06642216B2

    公开(公告)日:2003-11-04

    申请号:US09848839

    申请日:2001-05-03

    IPC分类号: A61K31665

    摘要: Compounds of the formula wherein X in each of formulas (1) and (2) represents a substituted or unsubstituted alkylene, alkenylene, or alkynylene linker of 2-6C; Y is of the formula  or a stereoisomer thereof, wherein R1 is substituted or unsubstituted alkyl; each R2 is independently H, hydroxy, alkoxy (1-6C) or lower alkyl (1-4C); R3 is H, hydroxy, or alkoxy (1-6C); or Y is of the formula  wherein each n is 1, Z is N, K comprises a substituted or unsubstituted aromatic carbocyclic or heterocyclic ring system which may optionally be spaced from the linkage position shown in formula (7) by a linker of 1-2C, or in formula (7), Z may be spaced from the carbon bonded to X by ═CR6— wherein R6 is H or linear, branded or cyclic alkyl (1-6C), R5 is H or linear, branched or cyclic alkyl, and R′ represents a cation, H or a substituted or unsubstituted alkyl group of 1-6C, promote bone formation and are thus useful in treating osteoporosis, bone fracture or deficiency, primary or secondary hyperparathyroidism, periodontal disease or defect, metastatic bone disease, osteolytic bone disease, post-plastic surgery, post-prosthetic joint surgery, and post-dental implantation. Also disclosed is a method to identify additional compounds which are inhibitors of enzymes in the isoprenoid scheme especially of HMG-CoA reductase which results in prenylation of proteins and in the synthesis of steroids or of inhibitors of their production which are useful in treating bone disorders.

    摘要翻译: 式(1)和(2)中的式(Ⅳ)化合物表示取代或未取代的2-6C的亚烷基,亚烯基或亚炔基接头; Y为其立体异构体,其中R 1为取代或 每个R 2独立地是H,羟基,烷氧基(1-6C)或低级烷基(1-4C); R 3是H,羟基或烷氧基(1-6C); 或Y是每个n是1的烷基,其中Z是N,K包括取代或未取代的芳族碳环或杂环系统,其可以任选地与式(7)所示的连接位置与1-2C的连接体间隔开,或 在式(7)中,Z可以与通过= CR 6键合到X的碳隔开,其中R 6是H或直链的,有品牌的或环状的烷基(1-6C),R 5是H或 直链,支链或环状的烷基,R'表示1-6个C的阳离子H或取代或未取代的烷基,促进骨形成,因此可用于治疗骨质疏松症,骨折或缺陷,原发性或继发性甲状旁腺功能亢进,牙周病或 缺损,转移性骨病,溶骨性骨病,整形后手术,假体后关节手术和牙后植入术。还公开了一种鉴定作为特异性HMG-CoA的异戊二烯方案中的酶抑制剂的其它化合物的方法 导致蛋白质异戊烯化的还原酶 在合成类固醇或其制备的抑制剂中可用于治疗骨骼疾病。

    PAF synthesis modulators
    5.
    发明授权
    PAF synthesis modulators 失效
    PAF合成调节剂

    公开(公告)号:US5550148A

    公开(公告)日:1996-08-27

    申请号:US482248

    申请日:1995-06-07

    CPC分类号: C07D207/38

    摘要: Compounds that selectively modulate the remodeling pathway of platelet activating factor (PAF) are described. Related pharmaceutical compositions and methods are also disclosed. These compounds, pharmaceutical compositions and methods are useful for reducing or eliminating inflammation.

    摘要翻译: 描述了选择性调节血小板活化因子(PAF)重塑途径的化合物。 还公开了相关的药物组合物和方法。 这些化合物,药物组合物和方法可用于减少或消除炎症。

    PDGF antagonists III
    9.
    发明授权
    PDGF antagonists III 失效
    PDGF拮抗剂III

    公开(公告)号:US5618837A

    公开(公告)日:1997-04-08

    申请号:US483216

    申请日:1995-06-07

    CPC分类号: A61K31/19 A61K31/365

    摘要: Methods for inhibiting intimal hyperplasia in the vasculature of mammals, including primates, are disclosed. The methods comprise administering to the mammal an effective amount of Brefeldin A or a derivative of Brefeldin A. The methods are useful in reducing intimal hyperplasia due to, for example, vascular injuries resulting from angioplasty, endarterectomy, reduction atherectomy or anastomosis of a vascular graft. The non-peptide PDGF antagonists Brefeldin A and its derivatives may optionally be administered coordinately with heparin, whereby the coordinately administered of non-peptide PDGF antagonist and heparin are combinatorially effective in inhibiting intimal hyperplasia.

    摘要翻译: 公开了抑制哺乳动物(包括灵长类动物)脉管系统内膜增生的方法。 所述方法包括向哺乳动物施用有效量的布雷菲德菌素A或布雷菲德菌素A的衍生物。该方法可用于减少由于血管成形术,内膜切除术,血管移植术中的粥样斑块切除术或吻合口引起的血管损伤引起的内膜增生 。 非肽PDGF拮抗剂Brefeldin A及其衍生物可以任选地与肝素配位施用,由此协调施用非肽PDGF拮抗剂和肝素在抑制内膜增生中是组合有效的。

    Wind turbine system
    10.
    发明授权

    公开(公告)号:US11022095B2

    公开(公告)日:2021-06-01

    申请号:US16431805

    申请日:2019-06-05

    申请人: Robert R. West

    发明人: Robert R. West

    摘要: A wind turbine system to provide electrical power in areas not connected to the electrical power grid. The wind turbine system includes a frame and a rotatable shaft supported by the frame. A ring and idler gear assembly is coupled to the rotatable shaft. An upper rotor assembly is coupled to the rotatable shaft. The upper rotor assembly is configured to rotate in a first direction and thereby to rotate the rotatable shaft in a first direction. A lower rotor assembly is coupled to the ring and idler gear assembly. The lower rotor assembly is configured to rotate in a second direction which is opposite of the first direction and thereby to rotate the rotatable shaft in the first direction via the ring and idler gear assembly.