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    Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors
    61.
    发明申请
    Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors 有权
    正电子缩合吡啶和嘧啶衍生物（如嘌呤）作为蛋白激酶抑制剂

    公开(公告)号：US20140107137A1

    公开(公告)日：2014-04-17

    申请号：US14017814

    申请日：2013-09-04

    Applicant: ASTEX THERAPEUTICS LIMITED ,  CANCER RESEARCH TECHNOLOGY LIMITED ,  THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL

    Inventor： Valerio BERDINI ,  Robert George BOYLE ,  Gordon SAXTY ,  David Winter WALKER ,  Steven John WOODHEAD ,  Paul Graham WYATT ,  Alistair DONALD ,  John CALDWELL ,  Ian COLLINS ,  Tatiana Faria DA FONSECA

    IPC: C07D487/04

    CPC classification number: C07D471/04 ,  A61K31/4545 ,  A61K31/519 ,  A61K31/52 ,  A61K31/522 ,  C07D473/34 ,  C07D487/04

    Abstract: The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q2 is other than a bond; G is hydrogen, NR2R3, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R1 is hydrogen and G is NR2R3, then Q2 is a bond; and R2, R3, R4, R6 and R8 are as defined in the claims.

    Abstract translation: 本发明提供用作蛋白激酶B抑制剂的化合物，该化合物为式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T为N或CR 5; J1-J2是N = C（R6），（R7）C = N，（R8）N-C（O），（R8）2C-C（O），N = N或（R7）C = C ）; E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q1是键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选被氧或氮原子代替，或者相邻的一对碳原子可被CONRq或NRqCO代替，其中Rq 是氢或甲基，或Rq是与R1或Q1的碳原子连接的C 1-4亚烷基链，形成环状部分; 并且其中所述连接基团Q1的碳原子可任选地具有一个或多个选自氟和羟基的取代基; Q2是含有1至3个碳原子的键或饱和烃连接基团，其中连接基团中的一个碳原子可任选被氧或氮原子取代; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q2不是键; G为氢，NR2R3，OH或SH，条件是当E为芳基或杂芳基且Q2为键时，则G为氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢且G是NR 2 R 3时，则Q2是一个键; 并且R 2，R 3，R 4，R 6和R 8如权利要求中所定义。

    Anti-cancer combinations
    62.
    发明申请
    Anti-cancer combinations 失效
    抗癌组合

    公开(公告)号：US20040204480A1

    公开(公告)日：2004-10-14

    申请号：US10790943

    申请日：2004-03-02

    Applicant: Cancer Research Technology Limited

    Inventor： William R. Wilson ,  Bronwyn G. Siim

    IPC: A61K031/353 ,  A61K031/7072 ,  A61K031/7048 ,  A61K031/704

    CPC classification number: A61K31/66 ,  A61K31/352 ,  A61K31/4353 ,  A61K31/475 ,  A61K31/505 ,  A61K31/65 ,  A61K31/70 ,  A61K31/7034 ,  A61K33/24 ,  A61K2300/00

    Abstract: The present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and a compound selected from platinum compounds, vinca alkaloids, alkylating agents, anthracyclines, topoisomerase I inhibitors, antimetabolites and topoisomerase II inhibitors, which have anti-tumour activity. Preferably, the present invention relates to synergistic combinations of the compound 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and a compound selected from carboplatin, gemcitabine, cisplatin, 5-fluorouracil, cyclophosphamide, etoposide, vincristine, doxorubicin and irinotecan. More particularly, the invention is concerned with the use of such combinations in the treatment of cancer and pharmaceutical compositions containing such combinations. The invention further provides for methods of preparing the combinations of the invention.

    Abstract translation: 本发明涉及化合物5,6-二甲基呫吨酮-4-乙酸（DMXAA）与选自铂化合物，长春花生物碱，烷化剂，蒽环类，拓扑异构酶I抑制剂，抗代谢物和拓扑异构酶II抑制剂的化合物的协同组合，其中 具有抗肿瘤活性。 优选地，本发明涉及化合物5,6-二甲基呫吨酮-4-乙酸（DMXAA）和选自卡铂，吉西他滨，顺铂，5-氟尿嘧啶，环磷酰胺，依托泊苷，长春新碱，多柔比星和伊立替康的化合物的协同组合。 更具体地，本发明涉及这样的组合在治疗癌症中的用途以及含有这些组合的药物组合物。 本发明进一步提供了制备本发明组合的方法。

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