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    Triazoles as farnesyl transferase inhibitors
    1.
    发明授权
    Triazoles as farnesyl transferase inhibitors 有权
    三唑作为法呢基转移酶抑制剂

    公开(公告)号：US07511061B2

    公开(公告)日：2009-03-31

    申请号：US11143814

    申请日：2005-06-02

    申请人： Ashis Kumar Saha ,  David William End ,  Bart Lieven Daniel De Corte ,  Henry Joseph Breslin ,  Li Liu

    发明人： Ashis Kumar Saha ,  David William End ,  Bart Lieven Daniel De Corte ,  Henry Joseph Breslin ,  Li Liu

    IPC分类号： A61K31/4196 ,  A61K31/47 ,  C07D215/00 ,  C07D249/06

    CPC分类号： C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

    摘要： A prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(═O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; =Z1-Z2=Z3- represents a radical of formula ═N—N═CH— (a-1), ═N—CH═N— (a-2), ═CH—N═N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(═O), C(═S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, —NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.

    摘要翻译： 前药，N-氧化物，加成盐，季胺或其立体化学异构形式，其中L 1和L 2是R 1 -Y-，其中每个（R 1 -Y） - 取代基独立地彼此定义; Y是C1-4烷二基，C2-4亚烯基，C2-4炔二基，C（-O）或直接键; R1是氢，氰基，芳基或取代或未取代的C1-14杂环; = Z1-Z2 = Z3-表示式-N-N-CH-（a-1），-N-CH-N-（a-2），-CH-N-N-（a-3） X是SO 2，（CH 2）n，其中n是1至4，C（-O），C（-S）或直接键; R 2是芳基，C 3-7环烷基，被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，羟基C 1-6烷基，羟基C 1-6烷基， 被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷氧基羰基，C 1-6烷硫基， 羟基C 1-6烷基，羟基C 1-6烷氧基，羟基C 1-6烷硫基和芳基C 1-6烷硫基; R3是芳基，-NR5R6，取代或未取代的C1-14杂环，或被取代或未取代的C1-14杂环或芳基取代的C2-4亚烯基; R4是氢，芳基，C3-7环烷基，C1-6烷基或被C3-7环烷基取代的C1-6烷基，羟基羰基，C1-4烷氧基羰基或芳基; R 5和R 6各自独立地选自氢，取代或未取代的C 1-14杂环，芳基，C 1-12烷基和被一个或多个选自羟基，芳基，芳氧基或取代或未取代的C 1-14杂环的取代基取代的C 1-12烷基。

    Triazoles as farnesyl transferase inhibitors
    2.
    发明授权
    Triazoles as farnesyl transferase inhibitors 有权

    公开(公告)号：US07049324B1

    公开(公告)日：2006-05-23

    申请号：US10130322

    申请日：2000-11-15

    申请人： Ashis Kumar Saha ,  David William End ,  Bart Lieven Daniel De Corte ,  Henry Joseph Breslin ,  Li Liu

    发明人： Ashis Kumar Saha ,  David William End ,  Bart Lieven Daniel De Corte ,  Henry Joseph Breslin ,  Li Liu

    IPC分类号： A61K31/47 ,  C07D215/38 ,  C07D249/08

    CPC分类号： C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D487/14

    摘要： a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(═O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; ═Z1—Z2═Z3— represents a radical of formula ═N—N═CH— (a-1), ═N—CH═N— (a-2), ═CH—N═N— (a-3); X is SO2, (CH2)n wherein n is 1 to 4, C(═O), C(═S), or a direct bond, R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, —NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.

    Triazoles as farnesyl transferase inhibitors
    3.
    发明授权
    Triazoles as farnesyl transferase inhibitors 有权
    三唑作为法呢基转移酶抑制剂

    公开(公告)号：US07592356B2

    公开(公告)日：2009-09-22

    申请号：US11926858

    申请日：2007-10-29

    申请人： Ashis Kumar Saha ,  David William End ,  Bart Lieven Daniel De Corte ,  Henry Joseph Breslin ,  Li Liu

    发明人： Ashis Kumar Saha ,  David William End ,  Bart Lieven Daniel De Corte ,  Henry Joseph Breslin ,  Li Liu

    IPC分类号： A61K31/47 ,  C07D249/08

    CPC分类号： C07D249/08 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

    摘要： a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L1 and L2 are R1—Y— wherein each (R1—Y)— substituent is defined independently of the other; Y is C1-4alkanediyl, C2-4alkenediyl, C2-4alkynediyl, C(═O), or a direct bond; R1 is hydrogen, cyano, aryl or a substituted or unsubstituted C1-14heterocycle; ═Z1—Z2═Z3— represents a radical of formula ═N—N═CH— (a-1), ═N—CH═N— (a-2), ═CH—N═N— (a-3); X is SO2, (CH2), wherein n is 1 to 4, C(═O), C(═S), or a direct bond; R2 is aryl, C3-7cycloalkyl, C3-7cycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio, C1-12alkyl or C1-12alkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted C1-14heterocycle, C3-7cycloalkyl, hydroxycarbonyl, C1-6alkyloxycarbonyl, hydroxyC1-6alkyl, hydroxyC1-6alkyloxy, hydroxyC1-6alkylthio and arylC1-6alkylthio; R3 is aryl, —NR5R6, a substituted or unsubstituted C1-14heterocycle, or C2-4alkenediyl substituted with a substituted or unsubstituted C1-14heterocycle or aryl; R4 is hydrogen, aryl, C3-7cycloalkyl, C1-6alkyl or C1-6alkyl substituted with C3-7cycloalkyl, hydroxycarbonyl, C1-4alkyloxycarbonyl or aryl; R5 and R6 are each independently selected from hydrogen, a substituted or unsubstituted C1-14heterocycle, aryl, C1-12alkyl and C1-12alkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted C1-14heterocycle.

    摘要翻译： 前药，N-氧化物，加成盐，季胺或其立体化学异构形式，其中L 1和L 2是R 1 -Y-，其中每个（R 1 -Y） - 取代基独立地彼此定义; Y是C1-4烷二基，C2-4亚烯基，C2-4炔二基，C（-O）或直接键; R1是氢，氰基，芳基或取代或未取代的C1-14杂环; -Z1-Z2-Z3-表示式-N-N-CH-（a-1），-N-CH-N-（a-2），-CH-N-N-（a-3） X是SO 2，（CH 2），其中n是1至4，C（-O），C（-S）或直接键; R 2是芳基，C 3-7环烷基，被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，羟基C 1-6烷基，羟基C 1-6烷基， 被一个或多个独立地选自羟基，芳基，芳氧基，取代或未取代的C 1-14杂环，C 3-7环烷基，羟基羰基，C 1-6烷氧基羰基，C 1-6烷氧基羰基，C 1-6烷硫基， 羟基C 1-6烷基，羟基C 1-6烷氧基，羟基C 1-6烷硫基和芳基C 1-6烷硫基; R3是芳基，-NR5R6，取代或未取代的C1-14杂环，或被取代或未取代的C1-14杂环或芳基取代的C2-4亚烯基; R4是氢，芳基，C3-7环烷基，C1-6烷基或被C3-7环烷基取代的C1-6烷基，羟基羰基，C1-4烷氧基羰基或芳基; R 5和R 6各自独立地选自氢，取代或未取代的C 1-14杂环，芳基，C 1-12烷基和被一个或多个选自羟基，芳基，芳氧基或取代或未取代的C 1-14杂环的取代基取代的C 1-12烷基。