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公开(公告)号:US20110118281A9
公开(公告)日:2011-05-19
申请号:US12572079
申请日:2009-10-01
申请人: Gary Bohnert , Zhiqiang Xia , Shoujun Chen , Lijun Sun
发明人: Gary Bohnert , Zhiqiang Xia , Shoujun Chen , Lijun Sun
IPC分类号: C07D401/04 , A61K31/497 , A61K31/4436 , C07D417/04 , C12N5/00 , A61P29/00 , A61P37/00 , A61P19/02 , A61P17/00 , A61P37/08
CPC分类号: C07D401/04 , A61K31/497 , A61K45/06 , C07D211/96 , C07D401/14 , C07D417/04 , C07D417/14
摘要: The invention relates to certain compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
摘要翻译: 本发明涉及可用作免疫抑制剂并用于治疗和预防炎性病症,过敏性疾病和免疫疾病的某些化合物或其药学上可接受的盐,溶剂化物,包合物或前药。
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公开(公告)号:US20100279410A1
公开(公告)日:2010-11-04
申请号:US12768164
申请日:2010-04-27
申请人: Zachary Demko , Christopher Borella , Shoujun Chen , Lijun Sun
发明人: Zachary Demko , Christopher Borella , Shoujun Chen , Lijun Sun
IPC分类号: C12N5/09
CPC分类号: C07F9/6518 , A61K31/4192 , A61K31/422 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/501 , A61K31/506 , A61K31/675 , C07D249/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D413/10
摘要: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
摘要翻译: 本发明涉及结构式(I)的化合物或其药学上可接受的盐,溶剂化物,包合物和前药,其中R a,R b和R 2在本文中定义。 这些化合物抑制微管蛋白聚合和/或靶向脉管系统,并且可用于治疗增殖性疾病如癌症。
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公开(公告)号:US07795313B2
公开(公告)日:2010-09-14
申请号:US12503661
申请日:2009-07-15
申请人: Keizo Koya , Lijun Sun , Elena Kostik , Farid Vaghefi , Shoujun Chen , Noriaki Tatsuta , Guiqing Liang , Takayo Inoue , Zhi-Qiang Xia
发明人: Keizo Koya , Lijun Sun , Elena Kostik , Farid Vaghefi , Shoujun Chen , Noriaki Tatsuta , Guiqing Liang , Takayo Inoue , Zhi-Qiang Xia
IPC分类号: A61K31/16
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.
摘要翻译: 公开了由结构式(I)表示的双(硫代 - 酰肼酰胺)二醛:Y是共价键或取代或未取代的直链烃基。 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。 Z是-O或-S。 M +是药学上可接受的一价阳离子,M2 +是药学上可接受的二价阳离子。 还公开了包含上述双(硫代 - 酰肼酰胺)二盐的药物组合物。 进一步公开的是用癌症治疗受试者的方法。 所述方法包括施用有效量的上述双(硫代 - 酰肼酰胺)二盐的步骤。
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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。
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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。
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公开(公告)号:US07579503B2
公开(公告)日:2009-08-25
申请号:US12148312
申请日:2008-04-18
申请人: Keizo Koya , Lijun Sun , Elena Kostik , Farid Vaghefi , Shoujun Chen , Noriaki Tatsuta , Guiqing Liang , Takayo Inoue , Zhi-Qiang Xia
发明人: Keizo Koya , Lijun Sun , Elena Kostik , Farid Vaghefi , Shoujun Chen , Noriaki Tatsuta , Guiqing Liang , Takayo Inoue , Zhi-Qiang Xia
IPC分类号: C07C327/38 , A61K31/16
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.
摘要翻译: 公开了由结构式(I)表示的双(硫代 - 酰肼酰胺)二醛:Y是共价键或取代或未取代的直链烃基。 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。 Z是-O或-S。 M +是药学上可接受的一价阳离子,M2 +是药学上可接受的二价阳离子。 还公开了包含上述双(硫代 - 酰肼酰胺)二盐的药物组合物。 进一步公开的是用癌症治疗受试者的方法。 所述方法包括施用有效量的上述双(硫代 - 酰肼酰胺)二盐的步骤。
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公开(公告)号:US20080242702A1
公开(公告)日:2008-10-02
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: A61K31/265 , C07C327/18 , C07D209/04 , A61K31/444 , A61P35/00 , A61K31/404 , C07D213/02
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。
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公开(公告)号:US07368473B2
公开(公告)日:2008-05-06
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: A61K31/16 , A61K31/335
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。
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公开(公告)号:US20070238699A1
公开(公告)日:2007-10-11
申请号:US11492692
申请日:2006-07-24
申请人: Zachary Demko , Christopher Borella , Shoujun Chen , Lijun Sun
发明人: Zachary Demko , Christopher Borella , Shoujun Chen , Lijun Sun
IPC分类号: A61K31/724 , A61K31/506 , A61K31/501 , A61K31/4439 , A61K31/4192 , C07D403/04
CPC分类号: C07F9/6518 , A61K31/4192 , A61K31/422 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/501 , A61K31/506 , A61K31/675 , C07D249/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D413/10
摘要: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
摘要翻译: 本发明涉及结构式(I)的化合物或其药学上可接受的盐,溶剂化物,包合物和前药,其中R a,R b,R b, SUB> 2 SUB>在本文中定义。 这些化合物抑制微管蛋白聚合和/或靶向脉管系统,并且可用于治疗增殖性疾病如癌症。
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公开(公告)号:US07081466B2
公开(公告)日:2006-07-25
申请号:US10802292
申请日:2004-03-16
申请人: Keizo Koya , Lijun Sun , Mitsunori Ono , David James , Weiwen Ying , Shoujun Chen
发明人: Keizo Koya , Lijun Sun , Mitsunori Ono , David James , Weiwen Ying , Shoujun Chen
IPC分类号: A61K31/44 , A61K31/445 , A61K31/415 , C07D471/02 , C07D209/04
CPC分类号: C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D471/04
摘要: Disclosed is a compound represented by Structural Formula (I): R1 is a substituted or unsubstituted 2-imidazolyl group which is optionally fused to a substituted or unsubstituted aryl group. Z1 is ═O, ═S, ═NOR11. R is represented by a Structural Formula selected from (II)–(VII): The variables in Structural Formulas (II)–(VII) are described herein.
摘要翻译: 公开了由结构式(I)表示的化合物:R 1是任选与取代或未取代的芳基稠合的取代或未取代的2-咪唑基。 Z 1是-O,-S,-NOR 11。 R由选自(II) - (VII)的结构式表示:本文描述了结构式(II) - (VII)中的变量。
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