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    PACLITAXEL ENHANCER COMPOUNDS
    5.
    发明申请
    PACLITAXEL ENHANCER COMPOUNDS 审中-公开
    PACLITAXEL增强化合物

    公开(公告)号：US20100280075A1

    公开(公告)日：2010-11-04

    申请号：US12692895

    申请日：2010-01-25

    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： A61K31/444 ,  A61K31/422 ,  A61K31/4045 ,  A61K31/381 ,  A61K31/337 ,  A61K31/341 ,  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 Rg are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and Rg 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。 R7和Rg各自独立地为-H，脂族或取代的脂族基团，或R7为-H，Rg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。

    Taxol enhancer compounds
    6.
    发明申请
    Taxol enhancer compounds 有权
    紫杉醇增强剂化合物

    公开(公告)号：US20060122183A1

    公开(公告)日：2006-06-08

    申请号：US11244324

    申请日：2005-10-05

    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： A61K31/53 ,  A61K31/505 ,  A61K31/44 ,  A61K31/337 ,  A61K31/277 ,  A61K31/16

    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（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。

    Taxol enhancer compounds
    7.
    发明授权
    Taxol enhancer compounds 失效
    紫杉醇增强剂化合物

    公开(公告)号：US06800660B2

    公开(公告)日：2004-10-05

    申请号：US10193075

    申请日：2002-07-10

    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： A61K3116

    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（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（R7R8） - ，R1和R2独立地是芳基或取代的芳基，R3和R4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是 -H和R8是取代或未取代的芳基，或者R 7和R 8一起是C 2 -C 6取代或未取代的亚烷基。Z = O或= S。还公开了药物组合物，其包含 本发明和药学上可接受的载体或稀释剂。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。

    Taxol enhancer compounds
    8.
    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
    9.
    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。