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    Isoprenoid pathway inhibitors for stimulating cartilage growth
    3.
    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。

    Isoprenoid pathway inhibitors for stimulating bone growth
    5.
    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。

    Compositions and methods for stimulating bone growth
    8.
    发明授权
    Compositions and methods for stimulating bone growth 失效
    用于刺激骨骼生长的组合物和方法

    公开(公告)号：US6080779A

    公开(公告)日：2000-06-27

    申请号：US96957

    申请日：1998-06-12

    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： A61K31/22 ,  A61K31/366 ,  A61K31/404 ,  A61K31/335 ,  A61K31/33 ,  A61K31/66

    CPC分类号： A61K31/404 ,  A61K31/22 ,  A61K31/366

    摘要： Compounds of the formula ##STR1## wherein X in each of formulas (1) and (2) represents a substituted or unsubstituted alkylene, alkenylene, or alkynylene linker of 2-6 C;Y represents one or more carbocyclic or heterocyclic rings; when two or more rings are present in Y, they may optionally be fused; andR' represents a cation, H or a substituted or unsubstituted alkyl group of 1-6 C; andthe dotted lines represent optional .pi.-bonds,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. These compounds can be used in combination with other bone growth-promoting compounds and/or estrogens and/or bisphosphonates for this purpose.

    摘要翻译： 式（1）和（2）各自表示X为2-6的取代或未取代的亚烷基，亚烯基或亚炔基连接基的式 Y表示一个或多个碳环或杂环; 当Y中存在两个或更多个环时，它们可以任选地稠合; R'表示1-6个C的阳离子，H或取代或未取代的烷基; 虚线表示可选的pi-键，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，牙周病或缺陷，转移性骨病，溶骨性骨病，整形外手术 假体关节手术和牙植入后。 为了此目的，这些化合物可以与其它骨生长促进化合物和/或雌激素和/或二膦酸盐组合使用。

    Compositions and methods for treating bone deficit conditions
    10.
    发明授权
    Compositions and methods for treating bone deficit conditions 失效
    用于治疗骨缺损病症的组合物和方法

    公开(公告)号：US6153631A

    公开(公告)日：2000-11-28

    申请号：US806768

    申请日：1997-02-26

    申请人： Charles Petrie ,  Mark W. Orme ,  Nand Baindur ,  Kirk G. Robbins ,  Gregory R. Mundy

    发明人： Charles Petrie ,  Mark W. Orme ,  Nand Baindur ,  Kirk G. Robbins ,  Gregory R. Mundy

    IPC分类号： A61K31/428 ,  A61K31/425

    CPC分类号： A61K31/428

    摘要： Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or "linker" defined as including a covalent bond per se so as to space the aromatic systems at a distance 1.5-15 .ANG., are effective in treating conditions associated with bone deficits. The compounds can be administered to vertebrate subjects alone or in combination with additional agents that promote bone growth or that inhibit bone resorption. They can be screened for activity prior to administration by assessing their ability to effect the transcription of a reporter gene coupled to a promoter associated with a bone morphogenetic protein and/or their ability to stimulate calvarial growth in model animal systems.

    摘要翻译： 包含通过含有一个或多个原子的接头共价连接的两个芳族体系的化合物或定义为包含共价键本身的“连接体”，以使芳族体系在距离为1.5-15安培的范围内空间有效地处理与 骨缺损。 化合物可以单独施用于脊椎动物，或者与促进骨生长或抑制骨吸收的其它试剂组合施用。 可以通过评估其在影响与骨形态发生蛋白相关的启动子相关的报告基因的转录和/或刺激模型动物系统中颅骨生长的能力的能力来筛选其给药前的活性。