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    Therapeutic acridone and acridine compounds
    65.
    发明授权
    Therapeutic acridone and acridine compounds 失效

    公开(公告)号：US07300930B2

    公开(公告)日：2007-11-27

    申请号：US11157977

    申请日：2005-06-22

    申请人： Stephen Neidle ,  Richard John Harrison ,  Lloyd Royston Kelland ,  Sharon Michele Gowan ,  Martin Anthony Read ,  Anthony Reszka

    发明人： Stephen Neidle ,  Richard John Harrison ,  Lloyd Royston Kelland ,  Sharon Michele Gowan ,  Martin Anthony Read ,  Anthony Reszka

    IPC分类号： A61K31/5377 ,  A61K31/435 ,  C07D413/14 ,  C07D219/10

    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: J1 is a 2- or 3-substituent; J2 is a 6- or 7-substituent; J1 and J2 are each independently a group of the formula —NHCO(CH2)nNR1R2, wherein: n is an integer from 1 to 5; and, R1 and R2 are independently hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl, or R1 and R2, 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(RN)Q, wherein: RN 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 proliferation, and in the treatment of proliferative conditions, such as cancer.

    Acridone inhibitors of IMPDH enzyme
    70.
    发明申请
    Acridone inhibitors of IMPDH enzyme 有权
    IMPDH酶的吖啶酮抑制剂

    公开(公告)号：US20040053955A1

    公开(公告)日：2004-03-18

    申请号：US10324306

    申请日：2002-12-20

    发明人： Edwin J. Iwanowicz ,  Scott H. Watterson ,  Ping Chen ,  T. G. Murali Dhar ,  Henry H. Gu ,  Yufen Zhao

    IPC分类号： A61K031/473 ,  C07F007/02 ,  C07D219/04

    CPC分类号： C07D401/12 ,  C07D219/06 ,  C07D401/14 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

    摘要： Compounds having the formula (I), 1 wherein R3 is selected from H, OH and NH2; R30 is selected from nullO and nullS; W is nullC(nullO)null, nullS(nullO)null, or nullS(O)2null; or W may be nullCH2null if X is nullC(nullO)null; X is selected from nullCH2null, nullN(R4)null, and nullOnull, except that when W is nullCH2null, X is nullC(nullO)null; Y is a bond or nullC(R40)(R45)null; Q is a linker; Z is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl; and R1, R2, R24, and R25 are as defined in the specification.

    摘要翻译： 具有式（I）的化合物，其中R 3选自H，OH和NH 2; R 30选自= O和= S; W是-C（= O） - ， - S（= O） - 或-S（O）2 - ; 或者如果X是-C（= O） - ，则W可以是-CH 2 - ; X选自-CH 2 - ， - N（R 4） - 和-O-，但是当W是-CH 2 - 时，X是-C（= O） - ; Y是键或-C（R 40）（R 45） - ; Q是一个连接符; Z是任选取代的烷基，烯基，炔基，环烷基，芳基，杂芳基或杂环基; 和R 1，R 2，R 24和R 25如说明书中所定义。