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    Substituted 1,4-diazepines and uses thereof
    1.
    发明申请
    Substituted 1,4-diazepines and uses thereof 审中-公开
    取代的1,4-二氮杂及其用途

    公开(公告)号：US20060235007A1

    公开(公告)日：2006-10-19

    申请号：US11452861

    申请日：2006-06-14

    Applicant: Tianbao Lu ,  Karen Milkiewicz ,  Pierre Raboisson ,  Maxwell Cummings ,  Raul Calvo ,  Daniel Parks ,  Louis LaFrance ,  Juan Marugan Sanchez ,  Joan Gushue ,  Kristi Leonard

    Inventor： Tianbao Lu ,  Karen Milkiewicz ,  Pierre Raboisson ,  Maxwell Cummings ,  Raul Calvo ,  Daniel Parks ,  Louis LaFrance ,  Juan Marugan Sanchez ,  Joan Gushue ,  Kristi Leonard

    IPC: A61K31/5513 ,  C07D403/02 ,  C07D413/02 ,  C07D243/18

    CPC classification number: C07D243/14

    Abstract: 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; and R3 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; and R6, 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.

    Abstract translation: 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 SUP， >，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 。

    Substituted 1,4-benzodiazepines and uses thereof
    8.
    发明申请
    Substituted 1,4-benzodiazepines and uses thereof 审中-公开
    取代的1,4-苯并二氮杂及其用途

    公开(公告)号：US20060148792A1

    公开(公告)日：2006-07-06

    申请号：US11371964

    申请日：2006-03-09

    Applicant: Tianbao Lu ,  Louis LaFrance ,  Daniel Parks ,  Karen Milkiewicz ,  Raul Calvo ,  Maxwell Cummings ,  Alexander Kim ,  Bruce Grasberger ,  Theodore Carver

    Inventor： Tianbao Lu ,  Louis LaFrance ,  Daniel Parks ,  Karen Milkiewicz ,  Raul Calvo ,  Maxwell Cummings ,  Alexander Kim ,  Bruce Grasberger ,  Theodore Carver

    IPC: A61K31/551 ,  C07D243/12 ,  C07D243/18

    CPC classification number: C07D401/04 ,  C07D243/14 ,  C07D403/10 ,  C07D405/04 ,  C07D409/04

    Abstract: The present invention is directed to novel 1,4-benzodiazepines, 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: X and Y are independently —C(O)—, —CH2— or —C(S)—; R1, R2, R3, R4, R7, R8, Rb, Rc, Rd and M arm defined herein; R5 is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroaralkyl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl or alkylaminocarbonylalkyl; R6 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; R9 is cycloalkyl: aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkyl(alkyl), aralkyl or heteroarylalkyl, each of which is optionally substituted; and R10 is —(CH2)n—CO2Rb, —(CH2)m—CO2M, —(CH2)i—OH or —(CH2)j—CONRcRd n is 0-8, m is 0-8, i is 1-8 and j is 0-8.

    Abstract translation: 本发明涉及新的1,4-苯二氮卓类药物，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：X和Y独立地为-C（O） - ， - CH 2 - 或-C（S） - ; R 1，R 2，R 3，R 4，R 7， R 8，R b，R c，R d，R d和M臂; R 5是氢，烷基，环烷基，任选取代的芳基，任选取代的杂芳基，任选取代的芳烷基，任选取代的杂芳烷基，羧基烷基，烷氧基羰基，烷氧基羰基烷基，氨基羰基，氨基羰基烷基，烷基氨基羰基或烷基氨基羰基烷基; R 6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 9是环烷基：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; 和R 10是 - （CH 2）n - - - - - - （CH 2）n - ， - （CH 2）2 - ， - M 2 - ， - （CH 2） -OH或 - （CH 2 CH 2）n -CONR C n R n为0-8 ，m为0-8，i为1-8，j为0-8。

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