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    Substituted 1,4-diazepines and uses thereof
    2.
    发明授权
    Substituted 1,4-diazepines and uses thereof 有权
    取代的1,4-二氮杂及其用途

    公开(公告)号：US07115598B2

    公开(公告)日：2006-10-03

    申请号：US10829040

    申请日：2004-04-21

    申请人： Tianbao Lu ,  Karen L. Milkiewicz ,  Pierre Raboisson ,  Maxwell David Cummings ,  Raul R. Calvo ,  Daniel J. Parks ,  Louis V. Lafrance, III ,  Juan Jose Marugan Sanchez ,  Joan Gushue ,  Kristi Leonard

    发明人： Tianbao Lu ,  Karen L. Milkiewicz ,  Pierre Raboisson ,  Maxwell David Cummings ,  Raul R. Calvo ,  Daniel J. Parks ,  Louis V. Lafrance, III ,  Juan Jose Marugan Sanchez ,  Joan Gushue ,  Kristi Leonard

    IPC分类号： C07D243/14 ,  A61K31/55

    CPC分类号： C07D243/14

    摘要： The present invention is directed to novel 1,4-diazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: R1, R2, R9, R10, Ra, Rd and M are defined herein;X is a bivalent radical of: an alkane, a cycloalkane, an optionally-substituted arene, an optionally-substituted heteroarene, an optionally-substituted arylalkane or an optionally-substituted heteroarylalkane; andR3 is —CO2Rd, —CO2M, —OH, —NHRd, —SO2Rd, —NHCONHRd, optionally-substituted amidino or optionally-substituted guanidino;or R3—X— is hydrogen or an electron pair;R4 is oxygen or —NR9R10;R5 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; andR6, R7 and R8 are independently hydrogen, alkyl, cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkylalkyl, aralkyl or heteroarylalkyl, each of which is optionally substituted; or R6 and R7, together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted 1 to 3 times with Ra.

    摘要翻译： 本发明涉及新的1,4-二氮杂，其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。 化合物具有式I：或其溶剂合物，水合物或其药学上可接受的盐; 其中：R 1，R 2，R 9，R 10，R a， >，R d和M在本文中定义; X是二价基团：烷烃，环烷烃，任选取代的芳烃，任选取代的杂芳烃，任选取代的芳基烷烃或任选取代的杂芳基烷烃; 和R 3是-CO 2 R 2，-CO 2 M，-OH，-NHR 0 任选取代的脒基或任选取代的胍基;其中R 1，R 2，R 3，R 4， 或R 3 -X-是氢或电子对; R 4是氧或-NR 9 R 10; R 5是环烷基，芳基，杂芳基，环烷基烷基，芳烷基，杂芳基烷基或饱和或部分不饱和的杂环，其各自任选被取代; R 6和R 8独立地是氢，烷基，环烷基，芳基，杂芳基，饱和或部分不饱和的杂环，环烷基烷基 ，芳烷基或杂芳基烷基，其各自任选被取代; 或R 6和R 7与它们所连接的碳原子一起形成3-至7-元碳环，任选地被R 1取代1至3倍， SUP> a 。