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    Compositions and methods for treating bone deficit conditions
    44.
    发明授权
    Compositions and methods for treating bone deficit conditions 有权
    用于治疗骨缺损病症的组合物和方法

    公开(公告)号：US06413998B1

    公开(公告)日：2002-07-02

    申请号：US09453828

    申请日：1999-12-02

    申请人： Charles Petrie ,  Mark V. Craig ,  Nand Baindur ,  Kirk G. Robbins ,  Scott M. Harris ,  Maria Kontoyianni ,  Gregory R. Mundy

    发明人： Charles Petrie ,  Mark V. Craig ,  Nand Baindur ,  Kirk G. Robbins ,  Scott M. Harris ,  Maria Kontoyianni ,  Gregory R. Mundy

    IPC分类号： A61K3112

    CPC分类号： A61K31/47 ,  A61K31/549 ,  A61K31/655

    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 Å, 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连接体共价连接的两个芳族体系的化合物或定义为包含共价键的“连接体”本身以便使芳族体系间距离为1.5-15，在治疗与 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。

    Compositions and methods for treating bone deficit conditions
    47.
    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：US06251901B1

    公开(公告)日：2001-06-26

    申请号：US08806769

    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： A61K31495

    CPC分类号： A61K31/655 ,  A61K31/196 ,  A61K31/4184 ,  A61K31/428 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/498 ,  A61K31/517 ,  A61K31/53

    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 29 as to space the aromatic systems at a distance 1.5-15Å, 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”299将芳族体系间距离为1.5-15A，在治疗与骨骼相关的病症中是有效的 赤字。 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。

    Compositions and methods for stimulating bone growth
    48.
    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。