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公开(公告)号:US06743919B2
公开(公告)日:2004-06-01
申请号:US10233371
申请日:2002-08-29
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: C07D47102
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, or ═NR11. R is represented by a Structural Formula selected from (II)-(VII): The variables in Structural Formulas (II)-(VII) are described below.
摘要翻译: 公开了由结构式(I)表示的化合物:R1是任选地与取代或未取代的芳基稠合的取代或未取代的2-咪唑基.Z1 = O,= S,= NOR11或= NR11.R 由选自(II) - (VII)的结构式表示:结构式(II) - (VII)中的变量如下所述。
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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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公开(公告)号:US08598366B2
公开(公告)日:2013-12-03
申请号:US13558886
申请日:2012-07-26
申请人: Lijun Sun , Christopher Borella , Hao Li , Jun Jiang , Shoujun Chen , Keizo Koya , Takayo Inoue , Zhenjian Du , Kevin Foley , Yaming Wu , Mei Zhang , Weiwen Ying
发明人: Lijun Sun , Christopher Borella , Hao Li , Jun Jiang , Shoujun Chen , Keizo Koya , Takayo Inoue , Zhenjian Du , Kevin Foley , Yaming Wu , Mei Zhang , Weiwen Ying
IPC分类号: C07D261/02
CPC分类号: C07D413/14 , A61K31/42 , A61K31/426 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/675 , A61K45/06 , C07D261/08 , C07D413/04 , C07D413/10 , C07F9/653
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.
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公开(公告)号:US07884094B2
公开(公告)日:2011-02-08
申请号:US11355922
申请日:2006-02-16
申请人: Lijun Sun , Christopher Borella , Hao Li , Jun Jiang , Shoujun Chen , Keizo Koya , Takayo Inoue , Zhenjian Du , Kevin Foley , Yaming Wu , Mei Zhang , Weiwen Ying
发明人: Lijun Sun , Christopher Borella , Hao Li , Jun Jiang , Shoujun Chen , Keizo Koya , Takayo Inoue , Zhenjian Du , Kevin Foley , Yaming Wu , Mei Zhang , Weiwen Ying
IPC分类号: A61K31/33 , C07D261/02
CPC分类号: C07D413/14 , A61K31/42 , A61K31/426 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/675 , A61K45/06 , C07D261/08 , C07D413/04 , C07D413/10 , C07F9/653
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.
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公开(公告)号:US20060217389A1
公开(公告)日:2006-09-28
申请号:US11355922
申请日:2006-02-16
申请人: Lijun Sun , Christopher Borella , Hao Li , Jun Jiang , Shoujun Chen , Keizo Koya , Takayo Inoue , Zhenjian Du , Kevin Foley , Yaming Wu , Mei Zhang , Weiwen Ying
发明人: Lijun Sun , Christopher Borella , Hao Li , Jun Jiang , Shoujun Chen , Keizo Koya , Takayo Inoue , Zhenjian Du , Kevin Foley , Yaming Wu , Mei Zhang , Weiwen Ying
IPC分类号: A61K31/506 , A61K31/501 , A61K31/497 , A61K31/4709 , A61K31/4439 , A61K31/426 , A61K31/42
CPC分类号: C07D413/14 , A61K31/42 , A61K31/426 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/675 , A61K45/06 , C07D261/08 , C07D413/04 , C07D413/10 , C07F9/653
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, 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:US20120289483A1
公开(公告)日:2012-11-15
申请号:US13558886
申请日:2012-07-26
申请人: Lijun Sun , Christopher Borella , Hao Li , Jun Jiang , Shoujun Chen , Keizo Koya , Takayo Inoue , Zhenjian Du , Kevin Foley , Yaming Wu , Mei Zhang , Weiwen Ying
发明人: Lijun Sun , Christopher Borella , Hao Li , Jun Jiang , Shoujun Chen , Keizo Koya , Takayo Inoue , Zhenjian Du , Kevin Foley , Yaming Wu , Mei Zhang , Weiwen Ying
IPC分类号: A61K31/42 , C07D261/08 , C07F9/653 , C07D413/04 , A61P35/00 , A61K31/4439 , A61K31/4725 , A61K31/4709 , A61K31/422 , A61K31/675 , C07D413/10
CPC分类号: C07D413/14 , A61K31/42 , A61K31/426 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/675 , A61K45/06 , C07D261/08 , C07D413/04 , C07D413/10 , C07F9/653
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.
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公开(公告)号:US08269017B2
公开(公告)日:2012-09-18
申请号:US12883883
申请日:2010-09-16
申请人: Lijun Sun , Christopher Borella , Hao Li , Jun Jiang , Shoujun Chen , Keizo Koya , Takayo Inoue , Zhenjian Du , Kevin Foley , Yaming Wu , Mei Zhang , Weiwen Ying
发明人: Lijun Sun , Christopher Borella , Hao Li , Jun Jiang , Shoujun Chen , Keizo Koya , Takayo Inoue , Zhenjian Du , Kevin Foley , Yaming Wu , Mei Zhang , Weiwen Ying
IPC分类号: C07D261/02 , A61K31/42
CPC分类号: C07D413/14 , A61K31/42 , A61K31/426 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/675 , A61K45/06 , C07D261/08 , C07D413/04 , C07D413/10 , C07F9/653
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:US20110059893A1
公开(公告)日:2011-03-10
申请号:US12883883
申请日:2010-09-16
申请人: Lijun Sun , Christopher Borella , Hao Li , Jun Jiang , Shoujun Chen , Keizo Koya , Takayo Inoue , Zhenjian Du , Kevin Foley , Yaming Wu , Mei Zhang , Weiwen Ying
发明人: Lijun Sun , Christopher Borella , Hao Li , Jun Jiang , Shoujun Chen , Keizo Koya , Takayo Inoue , Zhenjian Du , Kevin Foley , Yaming Wu , Mei Zhang , Weiwen Ying
IPC分类号: A61K38/06 , A61K31/675 , A61K31/501 , A61K31/4725 , A61K31/4709 , A61K31/4439 , A61K31/42 , C07K5/08 , C07F9/09 , C07D261/08 , C07D413/10 , C07D413/04 , A61K31/422 , A61P35/00 , A61P7/00 , A61P27/02
CPC分类号: C07D413/14 , A61K31/42 , A61K31/426 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/675 , A61K45/06 , C07D261/08 , C07D413/04 , C07D413/10 , C07F9/653
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: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。
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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.
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