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    THERAPEUTIC ACRIDONE AND ACRIDINE COMPOUNDS
    2.
    发明申请
    THERAPEUTIC ACRIDONE AND ACRIDINE COMPOUNDS 审中-公开
    治疗阿司匹林和阿司匹林化合物

    公开(公告)号：WO0208193A3

    公开(公告)日：2003-10-02

    申请号：PCT/GB0103046

    申请日：2001-07-06

    申请人： CANCER REC TECH LTD ,  NEIDLE STEPHEN ,  HARRISON RICHARD JOHN ,  KELLAND LLOYD ROYSTON ,  GOWAN SHARON MICHELE ,  READ MARTIN ,  RESZKA TONY

    发明人： NEIDLE STEPHEN ,  HARRISON RICHARD JOHN ,  KELLAND LLOYD ROYSTON ,  GOWAN SHARON MICHELE ,  READ MARTIN ,  RESZKA TONY

    IPC分类号： A61K31/473 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/55 ,  A61P35/00 ,  C07D219/06 ,  C07D219/08 ,  C07D219/10 ,  C07D219/12 ,  C07D401/12

    CPC分类号： C07D219/08 ,  C07D219/06 ,  C07D219/10

    摘要： The present invention pertains to acridone and acridine compounds of formula (I), wherein either: (a) K is =O, L is -H, alpha is a single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J is a 2- or 3-substituent; J is a 6- or 7-substituent; J and J are each independently a group of the formula -NHCO(CH2)nNR R , wherein: n is an integer from 1 to 5; and, R and R are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R and R , taken together with the nitrogen atom to which they are attached, form a heterocyclic ring having from 3 to 8 ring atoms; and wherein, when K is a 9-substituent, K is a group of the formula -N(R )Q, wherein: R is an amino substituent and is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q is C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, and is optionally substituted; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms 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 telomerase, to regulate cell prol iferation, and in the treatment of proliferative conditions, such as cancer.

    摘要翻译： 本发明涉及式（I）的吖啶酮和吖啶化合物，其中：（a）K是= O，L是-H，α是单键，β是双键，γ是单键（吖啶酮 ）; 或（b）K是9取代基，L不存在，α是双键，β是单键，γ是双键（吖啶）; 并且其中：J 1是2-或3-取代基; J 2是6-或7-取代基; J 1和J 2各自独立地是式-NHCO（CH 2）n NRR R 2的基团，其中：n是1至5的整数; 和R 1和R 2独立地是氢，C 1-7烷基，C 3-20杂环基或C 5-20芳基，或R 1和R 2与它们所连接的氮原子一起 形成具有3至8个环原子的杂环; 并且其中当K是9-取代基时，K是式-N（R N）Q的基团，其中：R N是氨基取代基并且是氢，C 1-7烷基，C 3-20杂环基， 或C5-20芳基; 且Q为C 1-7烷基，C 3-20杂环基或C 5-20芳基，并且任选被取代; 和其药学上可接受的盐，酯，酰胺，溶剂合物，水合物及其保护形式。 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，以抑制端粒酶，调节细胞增殖和治疗增殖性疾病如癌症。