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    Isoprenoid pathway inhibitors for stimulating cartilage growth
    1.
    发明申请
    Isoprenoid pathway inhibitors for stimulating cartilage growth 审中-公开
    用于刺激软骨生长的异戊二醛途径抑制剂

    公开(公告)号：US20050272801A1

    公开(公告)日：2005-12-08

    申请号：US11167054

    申请日：2005-06-24

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

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

    IPC分类号： A23L1/30 ,  A61K31/00 ,  A61K31/192 ,  A61K31/22 ,  A61K31/225 ,  A61K31/366 ,  A61K31/40 ,  A61K31/404 ,  A61K31/405 ,  A61K31/4409 ,  A61K31/47 ,  A61K31/505 ,  A61K45/06 ,  A61P1/02 ,  A61P3/14 ,  A61P5/20 ,  A61P19/08 ,  A61P19/10 ,  C07D207/416 ,  C07D213/54 ,  C07D215/14

    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X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是下式或其立体异构体，其中R 1是取代或未取代的烷基; 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具有下式：其中每个n是1，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）所示的连接位置间隔1-2- ，或式（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）中，R 5是H或直链，支链或环状的烷基，R'表示阳离子，H或1-6C的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，整形外手术，假体后关节手术和牙后植入术。 还公开了一种鉴定另外的化合物的方法，该化合物是类异戊二烯方案中尤其是HMG-CoA还原酶中的酶的抑制剂，其导致蛋白质的异戊烯化，以及合成类固醇或其生产抑制剂，其可用于治疗骨骼疾病。

    Method to ameliorate osteolysis and metastasis
    3.
    发明申请
    Method to ameliorate osteolysis and metastasis 审中-公开
    改善骨质溶解和转移的方法

    公开(公告)号：US20050244414A1

    公开(公告)日：2005-11-03

    申请号：US11109470

    申请日：2005-04-18

    申请人： Gregory Mundy ,  Yoshiyuki Yoneda ,  Theresa Guise

    发明人： Gregory Mundy ,  Yoshiyuki Yoneda ,  Theresa Guise

    IPC分类号： C12N15/09 ,  A61K9/08 ,  A61K31/66 ,  A61K31/675 ,  A61K38/00 ,  A61K39/395 ,  A61K45/06 ,  A61P35/00 ,  A61P43/00 ,  C07K16/22 ,  C07K16/24 ,  C07K16/26 ,  C12P21/08 ,  A61K31/663

    CPC分类号： C07K16/244 ,  A61K38/00 ,  A61K45/06 ,  C07K16/22 ,  C07K16/241 ,  C07K16/26

    摘要： A therapeutically effective amount of an antibody for a compound selected from the group consisting of PTHrp, TGFα, IL-1α, IL-1β, IL-6, Lymphotoxin, TNF, PGE; 1,25 dihydroxy vitamin D3 and an antigenic fragment thereof used in the treatment of cancer metastasis to bone and cancer cell growth in bone as well as osteolysis and symptomatic sequelae thereof. An antibody immunoreactive with parathyroid hormone-related protein (PTHrp) is particularly preferred. Antibodies with human characteristics are included in the invention for application of the invention method to human subjects. Also, the antibody can be administered in an injectable is formulation in combination with a therapeutically effective amount of a bisphosphonate or pyrophosphate having the general structure formula wherein X is a linking moiety allowing for the interconnection of the phosphonate groups, and pharmaceutically acceptable salts, hydrates and partial hydrates thereof. The antibody and bisphosphonate act synergistically in the treatment of cancer metastases to bone and symptomatic sequelae thereof and particularly as regards bone resorption.

    摘要翻译： 治疗有效量的选自PTHrp，TGFα，IL-1α，IL-1β，IL-6，淋巴毒素，TNF，PGE的化合物的抗体; 1,25二羟基维生素D 3及其抗原性片段用于治疗癌症转移至骨骼和骨细胞中的癌细胞，以及骨溶解及其症状后遗症。 与甲状旁腺激素相关蛋白（PTHrp）免疫反应的抗体是特别优选的。 具有人类特征的抗体包括在本发明中，用于将本发明方法应用于人类受试者。 此外，抗体可以以可注射的制剂与治疗有效量的具有以下通式结构式的二膦酸盐或焦磷酸盐组合施用：其中X是允许膦酸酯基团互连的连接部分，以及药学上可接受的盐，水合物 和其部分水合物。 抗体和双膦酸盐协同作用于治疗癌症转移至骨骼及其有症状的后遗症，特别是关于骨吸收。