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    Isoprenoid pathway inhibitors for stimulating bone growth
    10.
    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。