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    AMINOQUINOLINE AND AMINOQUINAZOLINE KINASE MODULATORS
    4.
    发明申请
    AMINOQUINOLINE AND AMINOQUINAZOLINE KINASE MODULATORS 审中-公开
    氨基喹啉和氨基喹啉激酶调节剂

    公开(公告)号：US20070004763A1

    公开(公告)日：2007-01-04

    申请号：US11422355

    申请日：2006-06-06

    申请人： Nand Baindur ,  Michael Gaul ,  Kevin Kreutter ,  Christian Baumann ,  Alexander Kim ,  Guozhang Xu ,  Bao-Ping Zhao

    发明人： Nand Baindur ,  Michael Gaul ,  Kevin Kreutter ,  Christian Baumann ,  Alexander Kim ,  Guozhang Xu ,  Bao-Ping Zhao

    IPC分类号： A61K31/517 ,  C07D403/04 ,  C07D401/04 ,  A61K31/4709

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04

    摘要： The invention is directed to aminoquinoline and aminoquinazoline compounds of Formula I: where R1, R2, R3, B, Z, Q, p, q and X are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of FLT3 and/or TrkB, the use of such compounds to reduce or inhibit kinase activity of FLT3 and/or TrkB in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 and/or TrkB. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

    摘要翻译： 本发明涉及式I的氨基喹啉和氨基喹唑啉化合物：其中R 1，R 2，R 3，B，Z，Q， p，q和X如本文所定义，使用这些化合物如蛋白酪氨酸激酶调节剂，特别是FLT3和/或TrkB的抑制剂，使用这些化合物来降低或抑制细胞中FLT3和/或TrkB的激酶活性 或受试者，以及这些化合物在受试者中预防或治疗细胞增殖性疾病和/或与FLT3和/或TrkB相关的疾病的用途。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

    Isoprenoid pathway inhibitors for stimulating cartilage growth
    6.
    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。

    Compositions and methods for treating bone deficit conditions
    8.
    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。