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1. 发明授权

US07772241B2 Variolin derivatives and their use as antitumor agents 失效
标题翻译：异喹啉衍生物及其作为抗肿瘤剂的用途
公开(公告)号：US07772241B2
公开(公告)日：2010-08-10
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 , C07D473/00
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'，SO2R'，NO2，NH2，NHR'，N（R'）2，NHCOR'，NHSO2R'，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。

2. 发明申请

US20090197901A1 VARIOLIN DERIVATIVES AND THEIR USE AS ANTITUMOR AGENTS 失效
标题翻译： VARIOLIN衍生物及其作为抗菌剂的用途
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。

3. 发明授权

US07495000B2 Variolin derivatives and their use as antitumor agents 失效
标题翻译：异喹啉衍生物及其作为抗肿瘤剂的用途
公开(公告)号：US07495000B2
公开(公告)日：2009-02-24
申请号：US10483525
申请日：2002-07-11
申请人： Modesto Remuiñan , Juan Jose Gonzalez , Carlos Del Pozo , Carmen Cuevas , Simon Munt , Regan James Anderson , Andres Francesh , Jonathan Charles Morris , Ignacio Manzanares
发明人： Modesto Remuiñan , Juan Jose Gonzalez , Carlos Del Pozo , Carmen Cuevas , Simon Munt , Regan James Anderson , Andres Francesh , Jonathan Charles Morris , Ignacio Manzanares
IPC分类号： A61K31/506 , C07D239/06
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-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 3，R 6，R 7和R 12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; 其中基团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的对可以连接成碳环或杂环系。

4. 发明申请

US20060235223A1 Variolin derivatives and their use as antitumor agents 失效
标题翻译：异喹啉衍生物及其作为抗肿瘤剂的用途
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。

5. 发明授权

US07947671B2 Synthesis of naturally occuring ecteinascidins and related compounds 有权
标题翻译：天然存在的ecteinascidins及相关化合物的合成
公开(公告)号：US07947671B2
公开(公告)日：2011-05-24
申请号：US12758182
申请日：2010-04-12
申请人： Valentin Martinez Barrasa , Pilar Gallego , Carmen Cuevas , Simon Munt , Ignacio Manzanares , Roberto Menchaca , Natividad Rodriguez , Alberto Rodriguez
发明人： Valentin Martinez Barrasa , Pilar Gallego , Carmen Cuevas , Simon Munt , Ignacio Manzanares , Roberto Menchaca , Natividad Rodriguez , Alberto Rodriguez
IPC分类号： A61K31/33 , C07D513/00
CPC分类号： C07D515/18 , C07D515/22
摘要： Ecteinascidin compounds with a quinone ring for ring E are active as anti-cancer agents. Related processes and compounds are provided.
摘要翻译：具有环E的醌环的白in素化合物作为抗癌剂是有活性的。提供相关方法和化合物。

6. 发明授权

US08012975B2 Antitumoral analogs of ET-743 有权
标题翻译： ET-743的抗肿瘤类似物
公开(公告)号：US08012975B2
公开(公告)日：2011-09-06
申请号：US11645356
申请日：2006-12-22
申请人： Ignacio Manzanares , Carmen Cuevas , Marta Perez , Maria Jesus Martin , Alberto Rodriguez , Simon Munt
发明人： Ignacio Manzanares , Carmen Cuevas , Marta Perez , Maria Jesus Martin , Alberto Rodriguez , Simon Munt
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。

7. 发明授权

US07763615B2 Ecteinascidin analogs for use as antitumour agents 有权
标题翻译：用作抗肿瘤剂的抗坏血酸类抗生素
公开(公告)号：US07763615B2
公开(公告)日：2010-07-27
申请号：US10485536
申请日：2002-08-06
申请人： Pilar Gallego , Carmen Cuevas , Simon Munt , Ignacio Manzanares , Valentin Martinez
发明人： Pilar Gallego , Carmen Cuevas , Simon Munt , Ignacio Manzanares , Valentin Martinez
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D487/00 , C07D491/00 , C07D513/00
CPC分类号： C07D515/22
摘要： Derivatives of ecteinascidin 736 of general formula (I) wherein the groups R1, R2, R3, R4 and R5 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, C(═O)R′, C(═O)OR′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′, CN, halogen, ═O, substituted or unsubstituted C1-C25 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclic; wherein X is independently selected of OR′, CN, (═O), or H; wherein each of the R′ groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, substituted or unsubstituted C1-C25 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl; wherein m is 0, 1 or 2; and wherein n is 0, 1, 2, 3, or 4, and their use as antitumoral agent.
摘要翻译：基团R 1，R 2，R 3，R 4和R 5各自独立地选自H，OH，OR'，SH，SR'，SOR'，SO 2 R'，C的通式（I）的抗坏血酸素736衍生物（= O）R'，C（= O）OR'，NO 2，NH 2，NHR'，N（R'）2，NHC（O）R'，CN，卤素，= O，取代或未取代的C 1 -C 25烷基取代或未取代的C 2 -C 18烯基，取代或未取代的C 2 -C 18炔基，取代或未取代的芳基，取代或未取代的杂环基; 其中X独立地选自OR'，CN，（= O）或H; 其中每个R'基团独立地选自H，OH，NO 2，NH 2，SH，CN，卤素，= O，C（= O）H，C（= O）CH 3，CO 2 H，未取代的C 1 -C 25烷基，取代或未取代的C 2 -C 18烯基，取代或未取代的C 2 -C 18炔基，取代或未取代的芳基; 其中m为0,1或2; 并且其中n为0,1,2,3或4，并且其用作抗肿瘤剂。

8. 发明申请

US20060106021A1 New antitumoral derivatives of et-743 有权
标题翻译： et-743的新抗肿瘤衍生物
公开(公告)号：US20060106021A1
公开(公告)日：2006-05-18
申请号：US10484060
申请日：2002-07-17
申请人： Valentin Martinez , Maria Flores , Pilar Gallego , Carmen Cuevas , Simon Munt , Ignacio Manzanares
发明人： Valentin Martinez , Maria Flores , Pilar Gallego , Carmen Cuevas , Simon Munt , Ignacio Manzanares
IPC分类号： A61K31/519 , C07D498/14
CPC分类号： C07D515/22
摘要： Derivatives of Et-743 or Et-770 or Et-729 are provided. The derivatives are of the general formula (Ia) wherein the substituent groups take various permitted meanings.
摘要翻译：提供Et-743或Et-770或Et-729的衍生物。衍生物具有通式（Ia），其中取代基具有各种允许的含义。

9. 发明授权

US08076337B2 Antitumoral derivatives of ET-743 有权
标题翻译： ET-743的抗肿瘤衍生物
公开(公告)号：US08076337B2
公开(公告)日：2011-12-13
申请号：US12755218
申请日：2010-04-06
申请人： Valentin Martinez , Maria Flores , Pilar Gallego , Carmen Cuevas , Simon Munt , Ignacio Manzanares
发明人： Valentin Martinez , Maria Flores , Pilar Gallego , Carmen Cuevas , Simon Munt , Ignacio Manzanares
IPC分类号： A01N43/58 , A01N43/60 , A61K31/50 , A61K31/495 , C07D241/36
CPC分类号： C07D515/22
摘要： Derivatives of Et-743 or Et-770 or Et-729 are provided. The derivatives are of the general formula Ia.: wherein the substituent groups take various permitted meanings.
摘要翻译：提供Et-743或Et-770或Et-729的衍生物。衍生物具有通式Ia：其中取代基具有各种允许的含义。

10. 发明授权

US07767659B2 Synthesis of naturally occurring ecteinascidins and related compounds 失效
标题翻译：天然存在的脑电泳和相关化合物的合成
公开(公告)号：US07767659B2
公开(公告)日：2010-08-03
申请号：US10503106
申请日：2003-02-04
申请人： Valentin Martinez Barrasa , Pilar Gallego , Carmen Cuevas , Simon Munt , Ignacio Manzanares , Roberto Menchaca , Natividad Rodriguez , Alberto Rodriguez
发明人： Valentin Martinez Barrasa , Pilar Gallego , Carmen Cuevas , Simon Munt , Ignacio Manzanares , Roberto Menchaca , Natividad Rodriguez , Alberto Rodriguez
IPC分类号： A01N43/00 , A61K31/33 , C07D487/00 , C07D491/00 , C07D513/00
CPC分类号： C07D515/18 , C07D515/22
摘要： Ecteinascidin compounds with a quinone ring for ring E are active as anti-cancer agents. Related processes and compounds are provided.
摘要翻译：具有环E的醌环的白in素化合物作为抗癌剂是有活性的。提供相关方法和化合物。

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