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公开(公告)号：EP1089998A2
公开(公告)日：2001-04-11
申请号：EP99931120.2
申请日：1999-06-21
申请人： Novartis AG , Novartis-Erfindungen Verwaltungsgesellschaft m.b.H. , The Scripps Research Institute
发明人： NICOLAOU, Kyriacos, Costa , KING, Nigel, Paul , FINLAY, Maurice, Raymond, Verschoyle , HE, Yun , ROSCHANGAR, Frank , VOURLOUMIS, Dionisios , VALLBERG, Hans , BIGOT, Antony
IPC分类号： C07D417/06 , C07D493/04 , A61K31/425
CPC分类号： C07D313/00 , C07D417/06 , C07D493/04 , Y02P20/55
摘要： The invention relates to epothilone analog represented by formula (I) wherein (i) R2 is absent or oxygen; 'a' can be either a single or double bond; 'b' can be either absent or a single bond; and 'c' can be either absent or a single bond, with the proviso that if R2 is oxygen then 'b' and 'c' are both a single bond and 'a' is a single bond; if R2 is absent then 'b' and 'c' are absent and 'a' is a double bond; and if 'a' is a double bond, then R2, 'b' and 'c' are absent; R3 is a radical selected from the group consisting of hydrogen; lower alkyl; -CH=CH2; -C CH; -CH2F; -CH2Cl; -CH2-OH; -CH2-O-(C1-C6-alkyl); and -CH2-S-(C1-C6-alkyl); R4 and R5 are independently selected from hydrogen, methyl or a protecting group; and R1 is as defined in the specification, or a salt of a compound of formula (I) where a salt-forming group is present. A further aspect of the invention is related to the synthesis of epothilone E. These compounds have inter alia microtubuli depolymerisation inhibiting activity and are e.g. useful against proliferative diseases.
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公开(公告)号：EP1089998B1
公开(公告)日：2006-10-25
申请号：EP99931120.2
申请日：1999-06-21
发明人： NICOLAOU, Kyriacos, Costa , KING, Nigel, Paul , FINLAY, Maurice, Raymond, Verschoyle , HE, Yun , ROSCHANGAR, Frank , VOURLOUMIS, Dionisios , VALLBERG, Hans , BIGOT, Antony
IPC分类号： C07D417/06 , C07D493/04 , A61K31/425
CPC分类号： C07D313/00 , C07D417/06 , C07D493/04 , Y02P20/55
摘要： The invention relates to epothilone analog represented by formula (I) wherein (i) R2 is absent or oxygen; 'a' can be either a single or double bond; 'b' can be either absent or a single bond; and 'c' can be either absent or a single bond, with the proviso that if R2 is oxygen then 'b' and 'c' are both a single bond and 'a' is a single bond; if R2 is absent then 'b' and 'c' are absent and 'a' is a double bond; and if 'a' is a double bond, then R2, 'b' and 'c' are absent; R3 is a radical selected from the group consisting of hydrogen; lower alkyl; -CH=CH2; -C CH; -CH2F; -CH2Cl; -CH2-OH; -CH2-O-(C1-C6-alkyl); and -CH2-S-(C1-C6-alkyl); R4 and R5 are independently selected from hydrogen, methyl or a protecting group; and R1 is as defined in the specification, or a salt of a compound of formula (I) where a salt-forming group is present. A further aspect of the invention is related to the synthesis of epothilone E. These compounds have inter alia microtubuli depolymerisation inhibiting activity and are e.g. useful against proliferative diseases.
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公开(公告)号：EP0944634A1
公开(公告)日：1999-09-29
申请号：EP97953808.0
申请日：1997-12-12
发明人： NICOLAOU, Costa, Kyriacos , HE, Yun , NINKOVIC, Sacha , PASTOR, Joaquin , ROSCHANGAR, Frank , SARABIA, Francisco , VALLBERG, Hans , VOURLOUMIS, Dionisios , WINSSINGER, Nicolas , YANG, Zhen , KING, Nigel, Paul , FINLAY, Maurice, Raymond, Verschoyle
CPC分类号： C07D417/06 , C07D313/00 , C07D493/04
摘要： Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubulin assembly. The analogs of epothilone are novel. Several of the analogs are demonstrated to have a superior cytotoxic activity as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.
摘要翻译： 埃坡霉素A，埃坡霉素B，埃坡霉素类似物和埃坡霉素类似物文库被合成。 埃坡霉素A和B是已知的抗癌剂，其通过诱导和稳定微管蛋白组装来预防有丝分裂来衍生它们的抗癌活性。 埃博霉素的类似物是新颖的。 证明几种类似物与埃坡霉素A或埃坡霉素B相比具有优异的细胞毒性活性，如它们增强的诱导聚合作用和稳定微管的能力所证明的。
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