Substituted O6-benzylguanines
    51.
    发明授权
    Substituted O6-benzylguanines 失效
    取代的O6-苄基胍

    公开(公告)号:US06333331B1

    公开(公告)日:2001-12-25

    申请号:US09333047

    申请日:1999-06-15

    IPC分类号: C07D47318

    摘要: The present invention provides AGT inactivating compounds such as substituted O6-benzylguanines of the formula 7- or 9-substituted 8-aza-O6-benzylguanines, 7,8-disubstituted O6-benzylguanines, 7,9-disubstituted O6-benzylguanines, 4(6)-substituted 2-amino-5-nitro-6(4)-benzyloxypyrimidines, and 4(6)-substituted 2-amino-5-nitroso-6(4)-benzyloxypyrimidines, as well as pharmaceutical compositions comprising such compounds along with a pharmaceutically acceptable carrier. The present invention further provides a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lesions at the O6-position of guanine, by administering to a mammal an effective amount of one of the aforesaid compounds, 2,4-diamino-6-benzyloxy-s-triazine, 5-substituted 2,4-diamino-6-benzyloxypyrimidines, or 8-aza-O6-benzylguanine, and administering to the mammal an effective amount of an antineoplastic alkylating agent which causes cytotoxic lesions at the O6-position of guanine.

    摘要翻译: 本发明提供AGT灭活化合物,例如式7-或9-取代的8-氮杂-O6-苄基胍的取代的O6-苄基胍,7,8-二取代的O6-苄基胍,7,9-二取代的O6-苄基胍,4(6 ) - 取代的2-氨基-5-硝基-6(4) - 苄氧基嘧啶和4(6) - 取代的2-氨基-5-亚硝基-6(4) - 苄氧基嘧啶,以及包含这些化合物的药物组合物 药学上可接受的载体。 本发明还提供了通过向哺乳动物施用有效量的上述化合物之一来增强哺乳动物中肿瘤细胞的化学治疗方法,所述抗肿瘤烷化剂通过在鸟嘌呤的O6位引起细胞毒性损伤, 2,4-二氨基-6-苄氧基-s-三嗪,5-取代的2,4-二氨基-6-苄氧基嘧啶或8-氮杂-O6-苄基鸟嘌呤,并向哺乳动物施用有效量的抗肿瘤烷化剂, 在鸟嘌呤的O6位引起细胞毒性病变。

    Pharmaceutical composition comprising 2,4-diamino-6-benzyloxy-s-triazine and inactivation of O6-alkylguanine-DNA-alkyltransferase
    52.
    发明授权
    Pharmaceutical composition comprising 2,4-diamino-6-benzyloxy-s-triazine and inactivation of O6-alkylguanine-DNA-alkyltransferase 失效
    包含2,4-二氨基-6-苄氧基-s-三嗪和O6-烷基鸟嘌呤-DNA-烷基转移酶失活的药物组合物

    公开(公告)号:US06303604B1

    公开(公告)日:2001-10-16

    申请号:US09590187

    申请日:2000-06-09

    IPC分类号: A61K3153

    摘要: The present invention provides 8-substituted O6-benzylguanine, 4(6)-substituted 2-amino-5-nitro-6(4)-benzyloxypyrimidine, and 4(6)-substituted 2-amino-5-nitroso-6(4)-benzyloxypyrimidine derivatives which have been found to be effective AGT inactivators, as well as pharmaceutical compositions comprising such derivatives along with a pharmaceutically acceptable carrier. The present invention further provides a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lesions at the O6-position of quanine, by administering to a mammal an effective amount of one of the aforesaid derivatives, 2,4-diamino-6-benzyloxy-s-triazine, 5-substituted 2,4-diamino-6-benzyloxypyrimidines, or 8-aza-O6-benzylguanine, and administering to the mammal an effective amount of an antineoplastic alkylating agent which causes cytotoxic lesions at the O6-position of guanine.

    摘要翻译: 本发明提供8-取代的O6-苄基鸟嘌呤,4(6) - 取代的2-氨基-5-硝基-6(4) - 苄氧基嘧啶和4(6) - 取代的2-氨基-5-亚硝基-6(4 已经被发现是有效的AGT灭活剂的苄氧基嘧啶衍生物,以及包含这些衍生物以及药学上可接受的载体的药物组合物。 本发明进一步提供一种通过向哺乳动物施用有效量的上述衍生物之一,通过向哺乳动物施用有效量的上述衍生物之一来增强哺乳动物中肿瘤细胞对化学治疗性治疗药物的抗肿瘤烷化剂的方法,所述抗肿瘤性烷化剂通过在喹诺酮的O6位引起细胞毒性病变, 2,4-二氨基-6-苄氧基-s-三嗪,5-取代的2,4-二氨基-6-苄氧基嘧啶或8-氮杂-O6-苄基鸟嘌呤,并向哺乳动物施用有效量的抗肿瘤烷化剂, 在鸟嘌呤的O6位引起细胞毒性病变。

    Substituted 06-benzylguanines and 6(4)-benzyloxypyrimidines
    53.
    发明授权
    Substituted 06-benzylguanines and 6(4)-benzyloxypyrimidines 失效
    取代的06-苄基胍和6(4) - 苄氧基嘧啶

    公开(公告)号:US5916894A

    公开(公告)日:1999-06-29

    申请号:US927846

    申请日:1997-09-11

    摘要: The present invention provides 8-substituted O.sup.6 -benzylguanine derivatives which have been found to be effective AGT inactivators, as well as pharmaceutical compositions comprising such derivatives along with a pharmaceutically acceptable carrier. Thus, for example, the present invention provides a compound of the formula ##STR1## wherein R.sub.1 is a substituent selected from the group consisting of amino, hydroxy, C.sub.1 -C.sub.4 alkylamino, C.sub.1 -C.sub.4 dialkylamino, and C.sub.1 -C.sub.4 acylamino, R.sub.2 is a substituent selected from the group consisting of C.sub.1 -C.sub.4 aminoalkyl, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 dialkylamino alkyl, and C.sub.1 -C.sub.4 pivaloylalkyl, and R.sub.3 is a C.sub.1 -C.sub.4 alkyl. The present invention further provides a method of enhancing the chemotherapeutic treatment of tumor cells in a mammal with an antineoplastic alkylating agent which causes cytotoxic lessons at the O.sup.6 -position of guanine by administering to a mammal an effective amount of one of the aforesaid derivatives and administering to the mammal an effective amount of an antineoplastic alkylating agent which causes cytotoxic lesions at the O.sup.6 -position of guanine.

    摘要翻译: 本发明提供已被发现是有效的AGT灭活剂的8-取代的O6-苄基鸟嘌呤衍生物,以及包含这种衍生物以及药学上可接受的载体的药物组合物。 因此,例如,本发明提供下式化合物其中R 1是选自氨基,羟基,C 1 -C 4烷基氨基,C 1 -C 4二烷基氨基和C 1 -C 4酰基氨基的取代基,R 2是选择的取代基 由C 1 -C 4氨基烷基,C 1 -C 4烷基,C 1 -C 4二烷基氨基烷基和C 1 -C 4新戊酰基烷基组成的组,R 3为C 1 -C 4烷基。 本发明进一步提供一种通过向哺乳动物施用有效量的上述衍生物之一并施用有效量的上述衍生物之一来增强哺乳动物中具有抗肿瘤性烷化剂的肿瘤细胞的化学治疗方法,所述抗肿瘤烷化剂在鸟嘌呤的O6位上引起细胞毒性课程 向哺乳动物施用有效量的在鸟嘌呤的O6位上引起细胞毒性损伤的抗肿瘤性烷化剂。

    Material for organic photoelectric device and organic photoelectric device including the same
    60.
    发明授权
    Material for organic photoelectric device and organic photoelectric device including the same 有权
    有机光电器件用的材料及包括其的有机光电器件

    公开(公告)号:US08470454B2

    公开(公告)日:2013-06-25

    申请号:US13033842

    申请日:2011-02-24

    IPC分类号: H01L51/54

    摘要: A material for an organic photoelectric device and an organic photoelectric device including the same, the material including an asymmetric compound represented by the following Chemical Formula 1: wherein, in Chemical Formula 1, Ar1 is hydrogen or a substituted or unsubstituted aryl, provided that when Ar1 is a substituted aryl having a substituent, Ar2 is not the same as the substituent of Ar1, Ar2 and Ar3 are each independently a substituted or unsubstituted carbazolyl, a substituted or unsubstituted C2 to C30 heteroaryl, a substituted or unsubstituted C2 to C30 arylamine, or a substituted or unsubstituted C2 to C30 heteroarylamine, L1 and L2 are each independently a substituted or unsubstituted phenylene, a substituted or unsubstituted naphthylene, or a substituted or unsubstituted anthracene, and m and n are each independently integers of 1 to 4.

    摘要翻译: 用于有机光电装置的材料和包含该有机光电装置的有机光电装置,该材料包括由以下化学式1表示的不对称化合物:其中在化学式1中,Ar 1为氢或取代或未取代的芳基,条件是当 Ar 1是具有取代基的取代芳基,Ar 2与Ar 1的取代基不同,Ar 2和Ar 3各自独立地为取代或未取代的咔唑基,取代或未取代的C 2至C 30杂芳基,取代或未取代的C 2至C 30芳基胺, 或取代或未取代的C2至C30杂芳基胺,L1和L2各自独立地为取代或未取代的亚苯基,取代或未取代的亚萘基或取代或未取代的蒽,m和n各自独立地为1至4的整数。