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    GLUTAMINASE INHIBITORS
    5.
    发明申请
    GLUTAMINASE INHIBITORS 审中-公开
    谷氨酰胺酶抑制剂

    公开(公告)号：WO2016054388A1

    公开(公告)日：2016-04-07

    申请号：PCT/US2015/053514

    申请日：2015-10-01

    申请人： UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION ,  CORNELL UNIVERSITY

    发明人： MCDERMOTT, Lee A. ,  IYER, Prema, C. ,  CERIONE, Rick ,  KATT, William

    IPC分类号： C07D417/14 ,  C07D417/12 ,  C07D401/14 ,  A61K31/495 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/40 ,  A61P35/00

    CPC分类号： A61K31/433 ,  A61K31/4535 ,  C07D285/135 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14

    摘要： A compound, or a pharmaceutically acceptable salt thereof, having a structure of: Formula A wherein A is a ring; Y 1 and Y 2 are each independently N or C with the proper valency; X 1 and X 2 are each independently -NH-, -0-, -CH 2 -0-, -NH-CH 2 -, or -N(CH 3 )-CH 2 -, provided that when at least one of X 1 and X 2 is -CH 2 -0-, -NH-CH 2 -, or -N(CH 3 )-CH 2 - then the - CH 2 - is directly connected to A; a and b are each independently 0 or 1; c and d are each independently 0 or 1; Z 1 and Z 2 are each independently a heterocyclic; and R 1 and R 2 are each independently optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, amino, optionally substituted heteroaralkyl, optionally substituted alkylalkoxy, optionally substituted alkylaryloxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl; provided that if Y 1 and Y 2 are each C, then a is 1 and b is 1; provided that if Y 1 and Y 2 are each N, then a is 0 and b is 0; provided that if Y 1 is N and Y 2 is C, then a=0 and b=l; provided that if Y 1 is C and Y 2 is N, then a=l and b=0; provided that if c=0 and d=0, then R 1 and R 2 are both amino; provided that if c is 1 and d is 1, then both R 1 and R 2 are not amino; provided that if c is 0 and d is 1, then R 1 is amino and R 2 is optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted heteroaralkyl, optionally substituted alkylalkoxy, optionally substituted alkylaryloxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl; and provided that if c is 1 and d is 0, then R 2 is amino and R 1 is optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted heteroaralkyl, optionally substituted alkylalkoxy, optionally substituted alkylaryloxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocycloalkyl.

    摘要翻译： 具有以下结构的化合物或其药学上可接受的盐：式A其中A是环; Y1和Y2各自独立地为N或C，具有合适的化合价; X 1和X 2各自独立地为-NH-，-O-，-CH 2 O-，-NH-CH 2 - 或-N（CH 3）-CH 2 - ，条件是当X 1和X 2中的至少一个为-CH 2 - 0-，-NH-CH 2 - 或-N（CH 3）-CH 2 - ，则-CH 2 - 直接与A连接; a和b各自独立地为0或1; c和d各自独立地为0或1; Z 1和Z 2各自独立地为杂环; 任选取代的杂芳烷基，任选取代的烷基烷氧基，任选取代的烷基芳基氧基，任选取代的芳基，任选取代的杂芳基或任选取代的杂环烷基; R 1和R 2各自独立地为任选取代的烷基，任选取代的芳烷基，任选取代的环烷基， 条件是如果Y1和Y2各自为C，则a为1，b为1; 条件是如果Y1和Y2各自为N，则a为0且b为0; 条件是如果Y1是N，Y2是C，那么a = 0和b = 1; 条件是如果Y1为C且Y2为N，则a = 1和b = 0; 条件是如果c = 0和d = 0，那么R1和R2都是氨基; 条件是如果c为1且d为1，那么R1和R2都不是氨基; 条件是如果c为0且d为1，则R1为氨基，R2为任选取代的烷基，任选取代的芳烷基，任选取代的环烷基，任选取代的杂芳烷基，任选取代的烷基烷氧基，任选取代的烷基芳氧基，任选取代的芳基，任选取代的杂芳基， 或任选取代的杂环烷基; 并且条件是如果c为1且d为0，则R2为氨基，R1为任选取代的烷基，任选取代的芳烷基，任选取代的环烷基，任选取代的杂芳烷基，任选取代的烷基烷氧基，任选取代的烷基芳氧基，任选取代的芳基，任选取代的杂芳基 ，或任选取代的杂环烷基。