利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

20 条记录 (耗时 0.015 秒)

    Isoprenoid pathway inhibitors for stimulating bone growth
    8.
    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

    申请人： Shirley R. Gasper ,  Robert R. West ,  Theresa Martinez ,  Kirk G. Robbins ,  Patricia A. McKernan ,  Nand Baindur ,  Virender M. Labroo ,  Gregory R. Mundy

    发明人： Shirley R. Gasper ,  Robert R. West ,  Theresa Martinez ,  Kirk G. Robbins ,  Patricia A. McKernan ,  Nand Baindur ,  Virender M. Labroo ,  Gregory R. Mundy

    IPC分类号： A61K31665

    CPC分类号： C07D215/14 ,  A23L33/10 ,  A61K31/00 ,  A61K31/192 ,  A61K31/22 ,  A61K31/225 ,  A61K31/366 ,  A61K31/40 ,  A61K31/404 ,  A61K31/405 ,  A61K31/505 ,  A61K45/06 ,  A61K2300/00

    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。