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    TAXOL ENHANCER COMPOUNDS
    1.
    发明公开
    TAXOL ENHANCER COMPOUNDS 有权
    VERBINDUNGEN MIT TAXOL-VERSTÄRKENDERWIRKUNG

    公开(公告)号：EP1406869A1

    公开(公告)日：2004-04-14

    申请号：EP02746947.7

    申请日：2002-07-10

    申请人： Synta Pharmaceuticals Corporation

    发明人： KOYA, Keizo ,  SUN, Lijun ,  CHEN, Shoujun ,  TATSUTA, Noriaki ,  WU, Yaming ,  ONO, Mitsunori

    IPC分类号： C07C327/56 ,  A61K31/337 ,  A61P35/00

    CPC分类号： A61K47/48176 ,  A61K31/16 ,  A61K31/165 ,  A61K31/277 ,  A61K31/337 ,  A61K31/381 ,  A61K31/44 ,  A61K31/505 ,  A61K31/53 ,  A61K47/58 ,  C07C327/56 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D305/14 ,  C07D307/68 ,  C07D333/38 ,  C07D333/68 ,  C07D407/12

    摘要： Disclosed is a compound represented by the Structural Formula (I); Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both ⊃C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or -C(R7R8)-. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently -H, an aliphatic or substituted aliphatic group, or R7 is -H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is =O or =S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with taxol or an analog of taxol.

    摘要翻译： 公开了由结构式（1）表示的化合物; Y是共价键，亚苯基或取代或未取代的直链烃基另外，Y与它们所键合的两个> C = Z基团一起是取代或未取代的芳基。 优选Y为共价键或-C（R 7 R 8） - 。 R 1和R 2独立地是芳基或取代的芳基，R 3和R 4独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R 5 -R 6独立地为-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R 7和R 8各自独立地为-H，脂族或取代的脂族基团，或R 7为-H且R 8为取代或未取代的芳基，或者R 7和R 8一起为C2- C6取代或未取代的亚烷基。 Z = 0或= S。 还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。 还公开了通过向受试者施用结构式（I）的化合物与紫杉醇或紫杉醇类似物组合治疗患有癌症的受试者的方法。

    BIS(THIO-HYDRAZIDE AMIDE) SALTS FOR TREATMENT OF CANCERS
    5.
    发明公开
    BIS(THIO-HYDRAZIDE AMIDE) SALTS FOR TREATMENT OF CANCERS 有权
    BIS（THIOHYDRAZIDAMID）的盐治疗癌症的

    公开(公告)号：EP1781604A1

    公开(公告)日：2007-05-09

    申请号：EP05762347.2

    申请日：2005-06-20

    申请人： Synta Pharmaceuticals Corporation

    发明人： KOSTIK, Elena ,  VAGHEFI, Farid ,  LIANG, Guiqing ,  KOYA, Keizo ,  SUN, Lijun ,  TATSUTA, Noriaki ,  CHEN, Shoujun ,  INOUE, Takayo ,  XIA, Zhi-Qiang

    IPC分类号： C07C327/56 ,  A61K31/16 ,  A61P35/00

    CPC分类号： C07D305/14 ,  C07C327/56 ,  C07C2601/02

    摘要： Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I) Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group. R1-R4 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Z is -O or -S. M+ is a pharmaceutically acceptable monovalent cation and M2+ is a pharmaceutically acceptable divalent cation. Also, disclosed are pharmaceutical compositions comprising a bis(thio-hydrazide amide) disalt described above. Further disclosed are methods of treating a subject with cancer. The methods comprise the step of administering an effective amount of a bis(thio-hydrazide amide) disalt described above.

    TAXOL ENHANCER COMPOUNDS
    9.
    发明公开
    TAXOL ENHANCER COMPOUNDS 有权
    紫杉醇增强剂化合物

    公开(公告)号：EP1406870A1

    公开(公告)日：2004-04-14

    申请号：EP02752238.2

    申请日：2002-07-10

    申请人： Synta Pharmaceuticals Corporation

    发明人： KOYA, Keizo ,  SUN, Lijun ,  CHEN, Shoujun ,  TATSUTA, Noriaki ,  WU, Yaming ,  ONO, Mitsunori ,  XIA, Zhi-Qiang

    IPC分类号： C07C327/56 ,  A61K31/337 ,  A61P35/00

    CPC分类号： C07D307/68 ,  A45D2008/006 ,  A61K31/337 ,  A61K31/505 ,  A61K31/53 ,  A61K31/5377 ,  A61K47/58 ,  C07C327/56 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D333/38 ,  C07D333/68

    摘要： One embodiment of the present invention is a compound represented by Structural Formula (I) wherein Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C=Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or -C(R7R8)-. R1 is an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, or a substituted non-aromatic hetereocyclic group, R2-R4 are independently -H, an aliphatic group, a substituted aliphatic group, a non-aromatic hetereocyclic group, a substituted non-aromatic hetereocyclic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. R5-R6 are independently -H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently -H, an aliphatic or substituted aliphatic group, or R7 is -H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is =0 or =S. Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.

    摘要翻译： 本发明的一个实施方案是由结构式（I）表示的化合物，其中Y是取代或未取代的直链烃基的共价键。 另外，Y与它所键合的> C = Z基团一起是取代或未取代的芳族基团。 优选地，Y是共价键或-C（R 7 R 8） - 。 R 1为脂族基团，取代的脂族基团，非芳族杂环基团或取代的非芳族杂环基团，R 2 -R 4独立地为-H，脂族基团，取代的脂族基团，非芳族杂环基团 ，取代的非芳族杂环基团，芳基或取代的芳基，或者R 1和R 3与它们所键合的碳原子和氮原子一起，和/或R 2和R 4与碳原子和氮原子一起 它们键合到一起形成任选与芳环稠合的非芳族杂环。 R5-R6独立地为-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R7和R8各自独立地为-H，脂族或取代的脂族基团，或R7为-H和R8为取代或未取代的芳基，或者R7和R8一起为C2-C6取代或未取代的亚烷基 。 Z是= 0或= S。 还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。