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。

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。

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。

公开(公告)号：US07345094B2

公开(公告)日：2008-03-18

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： A61K31/16 ,  C07C327/00 ,  C07C233/00

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.

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。

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。

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。

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。

公开(公告)号：US09107955B2

公开(公告)日：2015-08-18

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： A61K31/16 ,  A61K31/165 ,  A61K47/48 ,  A61K31/381 ,  A61K31/277 ,  A61K31/337 ,  A61K31/44 ,  A61K31/505 ,  A61K31/53 ,  C07C327/56 ,  C07D209/42 ,  C07D209/44 ,  C07D213/83 ,  C07D261/18 ,  C07D305/14 ,  C07D307/68 ,  C07D333/38 ,  C07D333/68 ,  C07D407/12

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。

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。