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    KETONES AND REDUCED KETONES AS THERAPEUTIC AGENTS FOR THE TREATMENT OF BONE CONDITIONS
    6.
    发明申请
    KETONES AND REDUCED KETONES AS THERAPEUTIC AGENTS FOR THE TREATMENT OF BONE CONDITIONS 审中-公开
    作为治疗骨质素的治疗药物的酮类和降低的克松顿

    公开(公告)号：WO2004098582A2

    公开(公告)日：2004-11-18

    申请号：PCT/GB2004/001958

    申请日：2004-05-06

    申请人： THE UNIVERSITY COURT OF THE UNIVERSITY OF ABERDEEN ,  RALSTON, Stuart, Hamilton ,  GREIG, Iain, Robert ,  MOHAMED, Aymen, Ibrahim, Idris ,  VAN'T HOF, Robert, Jurgen

    发明人： RALSTON, Stuart, Hamilton ,  GREIG, Iain, Robert ,  MOHAMED, Aymen, Ibrahim, Idris ,  VAN'T HOF, Robert, Jurgen

    IPC分类号： A61K31/12

    CPC分类号： C07C43/315 ,  A61K31/12 ,  A61K31/403 ,  C07C33/26 ,  C07C33/36 ,  C07C33/38 ,  C07C33/46 ,  C07C33/486 ,  C07C43/1782 ,  C07C45/004 ,  C07C45/46 ,  C07C45/567 ,  C07C45/673 ,  C07C49/784 ,  C07C49/796 ,  C07C49/813 ,  C07C59/84 ,  C07C69/007 ,  C07C205/19 ,  C07C205/45 ,  C07C251/48 ,  C07C259/10 ,  C07C2603/18 ,  C07C2603/26 ,  C07D309/12 ,  C07D339/08 ,  C07C49/84 ,  C07C49/83

    摘要： The present invention pertains to certain ketones and reduced ketones and derivatives thereof which, inter alia , inhibit osteoclast survival, formation, and/or activity; and/or inhibit bone resorption, and more particularly to compounds of the formulae: (1) (2) wherein: Ar 1 is independently a biphenyl, phenanthryl, fluorenyl, or carbazolyl, and is optionally substituted; R alk is independently a C 2-10 alkylene group, and is optionally substituted; -OR O , if present, is independently -OH or -OR K ; -OR K , if present, is independently selected from: -O-R K1 ; -O-C(=O)R K2 ; -O-C(=O)OR K3 ; -O-S(=O)2OR K4 ; Q is independently -OH or -OR OT ; wherein: -OR OT , if present, is independently selected from: -O-R E1 ; -O-C(=O)-R E2 ; -O-C(=O)-O-R E3 ; -O-C(=O)-O-SO 3 R E4 ; -O-C(=O)-O-(CH 2 ) n -COOR E5 ; -O-C(=O)-(CH 2 ) n -NR N1 R N2 ; -O-C(=O)-(CH 2 ) n -NH-C(=O)R E6 ; -O-C(=O)-(CH 2 ) n -C(=O)-NR N3 R N4 ; -O-P(=O)(OR E7 )(OR E8 ); -O-R PA ; R PA , if present, is an organic group which incorporates a phosphonic acid group; with the proviso that if -OR OT is -O-R E1 , then R E1 is not a phenyl group substituted with a sulfonyl group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, or prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to inhibit osteoclast survival, formation, and/or activity, and to inhibit conditions mediated by osteoclasts and/or characterised by bone resorption, in the treatment of bone disorders such as osteoporosis, rheumatoid arthritis, cancer associated bone disease, Paget's disease, aseptic loosening of prosthetic implants, and the like; and/or in the treatment of conditions associated with inflammation or activation of the immune system.

    摘要翻译： 本发明涉及某些酮和还原酮及其衍生物，其特别是抑制破骨细胞存活，形成和/或活性; 尤其涉及下式的化合物：（1）（2）其中：Ar 1独立地是联苯基，菲基，芴基或咔唑基，并且任选被取代; R a烷基独立地为C 2-10亚烷基，并且任选被取代; -ORO，如果存在，独立地是-OH或-ORK; -OR ，如果存在，独立地选自：-O-R ; -O-C（= O）R ; -O-C（= O）OR ; -O-S（= O）2 OR ; Q独立地为-OH或-ORO; 其中：-OR OT如果存在，独立地选自：-O-R E1; -O-C（= O）-R ; -O-C（= O）-O-R ; -O-C（= O）-O-SO 3 ; -O-C（= O）-O-（CH 2）N-COOR ; -O-C（= O） - （CH 2）N-NR - [R ; -O-C（= O） - （CH 2）N-NH-C（= O）R ; -O-C（= O） - （CH 2）N-C（= O）-NR - [R ; -O-P（= O）（OR ）（OR ）; -O-R ; 如果存在，R PA是含有膦酸基的有机基团; 条件是如果-OR OT是-O-R ，则R E1不是被磺酰基取代的苯基; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式或前药。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制破骨细胞存活，形成和/或活性，以及​​抑制破骨细胞介导的病症和/或 其特征在于骨吸收，治疗诸如骨质疏松症，类风湿性关节炎，癌症相关骨病，佩吉特氏病，假体植入物的无菌性松动等骨骼疾病; 和/或治疗与炎症或免疫系统的激活相关的病症。