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公开(公告)号:US20090197901A1
公开(公告)日:2009-08-06
申请号:US12349813
申请日:2009-01-07
申请人: Modesto Remuinan , Juan Jose Gonzalez , Carlos del Pozo , Andres Francesh , Carmen Cuevas , Simon Munt , Ignacio Manzanares , Regan James Anderson , Jonathan Charles Morris
发明人: Modesto Remuinan , Juan Jose Gonzalez , Carlos del Pozo , Andres Francesh , Carmen Cuevas , Simon Munt , Ignacio Manzanares , Regan James Anderson , Jonathan Charles Morris
IPC分类号: A61K31/519 , A61K31/506 , C07D239/70 , A61P35/00 , C07D239/24
CPC分类号: C07D213/64 , C07D213/78 , C07D239/38 , C07D401/06 , C07D401/14 , C07D409/14 , C07D471/06 , C07D471/14
摘要: Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X2, R1, R2, R3, R6, R7, and R12 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHCOR′, NHSO2R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, SH, NO2, NH2, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups of R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.
摘要翻译: 提供了式(5)的衍生物,其中由X2,R1,R2,R3,R6,R7和R12定义的取代基各自独立地选自H,OH,OR',SH,SR' ,SOR',SO 2 R',NO 2,NH 2,NHR',N(R')2,NHCOR',NHSO 2 R',CN,卤素,-O,C(-O)H,C(-O)R' ,CO 2 R',羧基烷基,C 1 -C 12烷基,C 2 -C 12烯基,C 2 -C 12炔基,取代或未取代的芳基,取代或未取代的芳烷基和取代或未取代的杂芳族; 其中每个R'基团独立地选自H,OH,SH,NO 2,NH 2,CN,卤素,-O,C(-O)H,C(-O)CH 3,CO 2 H,CO 2 CH 3, C 1 -C 12烷基,C 2 -C 12烯基,C 2 -C 12炔基,芳基,芳烷基和杂芳族; 其中R 1和R 2,R 2和R 3,R 3和R 12,R 12和R 6,或R 6和R 7的这些基团可以连接成碳环或杂环系。
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公开(公告)号:US07410969B2
公开(公告)日:2008-08-12
申请号:US11045595
申请日:2005-01-26
申请人: Ignacio Manzanares , María Jesús Martin , Alberto Rodriguez , Simon Munt , Carmen Cuevas , Marta Perez
发明人: Ignacio Manzanares , María Jesús Martin , Alberto Rodriguez , Simon Munt , Carmen Cuevas , Marta Perez
IPC分类号: C07D471/22 , C07D487/22 , A61K31/496 , A61P35/00
CPC分类号: C07D491/18 , C07D471/18 , C07D471/22 , C07D491/22 , C07D497/22
摘要: Antitumor compounds have the five membered fused ring ecteinascidin structure of the formula (XIV). The present compounds lack a 1,4-bridging group as found in the ecteinascidins. They have at the C-1 position a substituent selected from an optionally protected or derivatised aminomethylene group or an optionally protected or derivatised hydroxymethylene group
摘要翻译: 抗肿瘤化合物具有式(XIV)的五元稠环环虫苷结构。 本发明化合物缺乏在ecteinascidins中发现的1,4桥连基团。 它们在C-1位具有选自任选保护或衍生的氨基亚甲基或任选保护或衍生的羟基亚甲基的取代基
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公开(公告)号:US07247629B2
公开(公告)日:2007-07-24
申请号:US10257857
申请日:2001-05-15
申请人: Ignacio Manzanares , María Jesús Martin , Alberto Rodriguez , Simon Munt , Carmen Cuevas , Marta Perez
发明人: Ignacio Manzanares , María Jesús Martin , Alberto Rodriguez , Simon Munt , Carmen Cuevas , Marta Perez
IPC分类号: C07D471/22 , C07D487/22 , A61K31/496 , A61P35/00
CPC分类号: C07D491/18 , C07D471/18 , C07D471/22 , C07D491/22 , C07D497/22
摘要: Antitumour compounds have the five membered fused ring ecteinascidin structure of the formula (XIV). The present compounds lack a 1,4-bridging group as found in the ecteinascidins. They have at the C-1 position a substituent selected from an optionally protected or derivatised aminomethylene group or an optionally protected or derivatised hydroxymethylene group.
摘要翻译: 抗肿瘤化合物具有式(ⅩⅣ)的五元稠环甙元结构。 本发明化合物缺乏在ecteinascidins中发现的1,4桥连基团。 它们在C-1位具有选自任选保护或衍生的氨基亚甲基或任选保护或衍生的羟基亚甲基的取代基。
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公开(公告)号:US20060235223A1
公开(公告)日:2006-10-19
申请号:US10483525
申请日:2002-07-11
申请人: Modesto Remuiñan , Juan Gonzalez , Carlos Pozo , Carmen Cuevas , Simon Munt , Regan Anderson , Andres Francesh , Jonathan Morris , Ignacio Manzanares
发明人: Modesto Remuiñan , Juan Gonzalez , Carlos Pozo , Carmen Cuevas , Simon Munt , Regan Anderson , Andres Francesh , Jonathan Morris , Ignacio Manzanares
IPC分类号: C07D487/14
CPC分类号: C07D213/64 , C07D213/78 , C07D239/38 , C07D401/06 , C07D401/14 , C07D409/14 , C07D471/06 , C07D471/14
摘要: Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X2, R1, R2, R3, R6, R7 and R12 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHCOR′, NHSO2R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, SH, N02, NH2, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.
摘要翻译: 提供了式(5)的异喹啉衍生物,其中由X 2,R 1,R 2,R 2, R 3,R 6,R 7和R 12各自独立地选自H,OH,OR' ,SH,SR',SOR',SO 2 R',NO 2,NH 2,NHR',N(R' (O)H,C(-O)R',CO 2(OR 2)2,NHCOR',NHSO 2 R',CN,卤素, H,CO 2 R',羧基烷基,C 1 -C 12烷基,C 2 -C 12烷基,C 1 -C 12烷基, C 12 - 12链烯基,C 2 -C 12炔基,取代或未取代的芳基,取代或未取代的芳烷基和取代或未取代的杂芳族; 其中每个R'基团独立地选自H,OH,SH,N,O,NH 2,CN,卤素,-O,C (-O)H,C(-O)CH 3,CO 2 H,CO 2,CH 3, C 1 -C 12烷基,C 2 -C 12链烯基,C 2 -C 12烷基,C 1 -C 12烷基, 炔基,芳基,芳烷基和杂芳基; 其中基团R 1和R 2,R 2和R 3,R 3, R 12和R 12,R 12和R 6,或R 6和R 12, 7可以连接到碳环或杂环系中。
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公开(公告)号:US20060019960A1
公开(公告)日:2006-01-26
申请号:US11045595
申请日:2005-01-26
申请人: Ignacio Manzanares , Maria Martin , Alberto Rodriguez , Simon Munt , Carmen Cuevas , Marta Perez
发明人: Ignacio Manzanares , Maria Martin , Alberto Rodriguez , Simon Munt , Carmen Cuevas , Marta Perez
IPC分类号: A61K31/498 , C07D491/14
CPC分类号: C07D491/18 , C07D471/18 , C07D471/22 , C07D491/22 , C07D497/22
摘要: Antitumor compounds have the five membered fused ring ecteinascidin structure of the formula (XIV). The present compounds lack a 1,4-bridging group as found in the ecteinascidins. They have at the C-1 position a substituent selected from an optionally protected or derivatised aminomethylene group or an optionally protected or derivatised hydroxymethylene group.
摘要翻译: 抗肿瘤化合物具有式(XIV)的五元稠环环虫苷结构。 本发明化合物缺乏在ecteinascidins中发现的1,4桥连基团。 它们在C-1位具有选自任选保护或衍生的氨基亚甲基或任选保护或衍生的羟基亚甲基的取代基。
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公开(公告)号:US20080051407A1
公开(公告)日:2008-02-28
申请号:US11645356
申请日:2006-12-22
申请人: Ignacio Manzanares , Maria Martin , Alberto Rodriguez , Simon Munt , Carmen Cuevas , Marta Perez
发明人: Ignacio Manzanares , Maria Martin , Alberto Rodriguez , Simon Munt , Carmen Cuevas , Marta Perez
IPC分类号: A61K31/496 , A61P35/00 , C07D241/36
CPC分类号: C07D491/18 , C07D471/18 , C07D471/22 , C07D491/22 , C07D497/22
摘要: Antitumor compounds have the five membered fused ring ecteinascidin structure of the formula (XIV). The present compounds lack a 1,4-bridging group as found in the ecteinascidins. They have at the C-1 position a substituent selected from an optionally protected or derivatised aminomethylene group or an optionally protected or derivatised hydroxymethylene group.
摘要翻译: 抗肿瘤化合物具有式(XIV)的五元稠环环虫苷结构。 本发明化合物缺乏在ecteinascidins中发现的1,4桥连基团。 它们在C-1位具有选自任选保护或衍生的氨基亚甲基或任选保护或衍生的羟基亚甲基的取代基。
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