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    Synthesis of taxol enhancers
    41.
    发明申请
    Synthesis of taxol enhancers 失效
    紫杉醇增强剂的合成

    公开(公告)号：US20060281811A1

    公开(公告)日：2006-12-14

    申请号：US11440429

    申请日：2006-05-24

    申请人： Shoujun Chen ,  Lijun Sun ,  Zhi-Qiang Xia ,  Keizo Koya ,  Mitsunori Ono

    发明人： Shoujun Chen ,  Lijun Sun ,  Zhi-Qiang Xia ,  Keizo Koya ,  Mitsunori Ono

    IPC分类号： A61K31/235 ,  A61K31/195

    CPC分类号： C07D213/77 ,  C07C327/56 ,  C07C2601/14 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D307/54 ,  C07D333/38 ,  Y02P20/55

    摘要： Disclosed is a method of preparing a thiohydrazide product compound from a hydrazide starting compound. The hydrazide starting compound is represented by Structural Formula (I): The thiohydrazide product compound is represented by Structural Formula (II): In Structural Formulas (I)-(II), R1 and R2 are independently an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R2 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. When R2 is an aryl group or a substituted aryl group, then R5 is a hydrazine protecting group; and when R2 is an aliphatic or substituted aliphatic group, then R5 is —H or a hydrazine protecting group. R10 is —H or a substituted or unsubstituted alkyl group. The method comprising the step of reacting the starting compound with a thionylating reagent.

    摘要翻译： 公开了从酰肼起始化合物制备硫代酰肼产物化合物的方法。 酰肼起始化合物由结构式（I）表示：硫代酰肼产物化合物由结构式（II）表示：在结构式（I） - （II）中，R 1和R 2 > 2 独立地是脂族基团，取代的脂族基团，芳基或取代的芳基，或R 1和R 2与 与它们键合的碳原子和氮原子形成任选地与芳环稠合的非芳族杂环。 当R 2是芳基或取代的芳基时，R 5是肼保护基; 当R 2是脂族或取代的脂族基团时，R 5是-H或肼保护基。 R 10是-H或取代或未取代的烷基。 该方法包括使起始化合物与亚硫酰化试剂反应的步骤。

    Taxol enhancer compounds
    43.
    发明授权
    Taxol enhancer compounds 失效
    紫杉醇增强剂化合物

    公开(公告)号：US06924312B2

    公开(公告)日：2005-08-02

    申请号：US10345885

    申请日：2003-01-15

    申请人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono

    发明人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono

    IPC分类号： A45D8/00 ,  A45D8/12 ,  A45D8/20 ,  A45D8/36 ,  A61K31/337 ,  C07C327/56 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D307/68 ,  C07D333/38 ,  C07D333/68 ,  A61K31/16 ,  C07C241/00

    CPC分类号： C07D307/68 ,  A45D2008/006 ,  A61K31/337 ,  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： 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（I）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。 此外，Y与它所键合的两个> 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和R 2分别独立地是芳基或取代的芳基，R 3和R 4是 独立的-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 R 5 -R 6独立地是-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， 8是取代或未取代的芳基，或者R 7和R 8一起是C2-C6取代或未取代的亚烷基。 Z是-O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的类似物组合治疗患有癌症的受试者的方法。

    Paclitaxel enhancer compound
    45.
    发明授权
    Paclitaxel enhancer compound 失效
    紫杉醇增强剂化合物

    公开(公告)号：US07750042B2

    公开(公告)日：2010-07-06

    申请号：US12077729

    申请日：2008-03-20

    申请人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

    发明人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

    IPC分类号： A61K31/335 ,  A61K31/20 ,  C07C327/38 ,  C07C243/18

    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 the Structural Formula (I): 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 heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic 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 ═O 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：Y是取代或未取代的直链烃基的共价键。 此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。 优选Y为共价键或-C（R 7 R 8） - 。 R1是脂肪族基团，取代脂肪族基团，非芳族杂环基团或取代的非芳族杂环基团，R2-R4独立地是-H，脂肪族基团，取代的脂肪族基团，非芳香族杂环基 ，取代的非芳族杂环基，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与碳和氮原子一起 形成与芳环稠合的非芳族杂环。 R5-R6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 7和R 8各自独立地为-H，脂族或取代的脂族基团，或者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C 2 -C 6取代或未取代的亚烷基 。 Z为═O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。

    Taxol enhancer compounds
    47.
    发明申请
    Taxol enhancer compounds 有权
    紫杉醇增强剂化合物

    公开(公告)号：US20060116374A1

    公开(公告)日：2006-06-01

    申请号：US11244427

    申请日：2005-10-05

    申请人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

    发明人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono ,  Zhi-Qiang Xia

    IPC分类号： A61K31/5377 ,  A61K31/53 ,  A61K31/505 ,  A61K31/337

    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 the Structural Formula (I): 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 heterocyclic group, or a substituted non-aromatic heterocyclic group, R2-R4 are independently —H, an aliphatic group, a substituted aliphatic group, a non-aromatic heterocyclic group, a substituted non-aromatic heterocyclic 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 ═O 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：Y是取代或未取代的直链烃基的共价键。 此外，Y与它所键合的两个> 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是脂族基团，取代的脂族基团，非芳族杂环基团或取代的非芳香族杂环基团，R 2 -R 4 独立地，-H，脂族基团，取代的脂族基团，非芳香族杂环基，取代的非芳族杂环基，芳基或取代的芳基，或R 1， SUB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结合在一起 与其键合的碳原子和氮原子形成任选地稠合到芳香环的非芳族杂环。 R 5 -R 6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 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， 8是取代或未取代的芳基，或者R 7和R 8一起是C2-C6取代或未取代的亚烷基。 Z是-O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。

    Treatment for cancers
    49.
    发明授权
    Treatment for cancers 失效
    癌症治疗

    公开(公告)号：US07763658B2

    公开(公告)日：2010-07-27

    申请号：US10758589

    申请日：2004-01-15

    申请人： Keizo Koya ,  Lijun Sun ,  Yaming Wu ,  Timothy Korbut ,  Dan Zhou ,  Zhenjian Du ,  Shoujun Chen ,  Noriaki Tatsuta ,  Guiqing Liang ,  Mitsunori Ono

    发明人： Keizo Koya ,  Lijun Sun ,  Yaming Wu ,  Timothy Korbut ,  Dan Zhou ,  Zhenjian Du ,  Shoujun Chen ,  Noriaki Tatsuta ,  Guiqing Liang ,  Mitsunori Ono

    IPC分类号： A61K31/16

    CPC分类号： A61K31/165 ,  A61K31/16 ,  A61K31/277

    摘要： One embodiment of the present invention is a method of treating a subject with a multi-drug resistant cancer. The method comprises administering to the subject an effective amount of a compound represented by Structural Formula (I): Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group, or, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic 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. Preferably R1 and R2 are the same and R3 and R4 are the same. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. Z is ═O or ═S.

    摘要翻译： 本发明的一个实施方案是用多药耐药性癌症治疗受试者的方法。 该方法包括向受试者施用有效量的由结构式（I）表示的化合物：Y是共价键或取代或未取代的直链烃基，或Y与两个> C = Z基团一起加到 其是键合的，是取代或未取代的芳基。 R 1 -R 4独立地为-H，脂族基团，取代的脂族基团，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 与它们所键合的碳原子和氮原子一起形成任选地与芳环稠合的非芳族杂环。 优选地，R 1和R 2相同，并且R 3和R 4相同。 R5-R6独立地是-H，脂族基团，取代的脂族基团，芳基或取代的芳基。 Z为═O或═S。

    Paclitaxel enhancer compounds
    50.
    发明授权
    Paclitaxel enhancer compounds 失效
    紫杉醇增强剂化合物

    公开(公告)号：US07671092B2

    公开(公告)日：2010-03-02

    申请号：US12009641

    申请日：2008-01-18

    申请人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono

    发明人： Keizo Koya ,  Lijun Sun ,  Shoujun Chen ,  Noriaki Tatsuta ,  Yaming Wu ,  Mitsunori Ono

    IPC分类号： A61K31/16 ,  C07D285/00 ,  C07D417/00

    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 Paclitaxel or an analog of Paclitaxel.

    摘要翻译： 公开了由结构式（I）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。 此外，Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。 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。 R5-R6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 7和R 8各自独立地为-H，脂族或取代的脂族基团，或者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C 2 -C 6取代或未取代的亚烷基 。 Z为═O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合式（I）的化合物与紫杉醇或紫杉醇的类似物组合来治疗患有癌症的受试者的方法。