发明名称 |
EPOTHILONE DERIVATIVES AND THEIR SYNTHESIS AND USE |
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; -CCH; -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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申请公布号 |
CA2334342(C) |
申请公布日期 |
2012.07.17 |
申请号 |
CA19992334342 |
申请日期 |
1999.06.21 |
申请人 |
NOVARTIS AG;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 |
分类号 |
C07D417/06;A61K31/335;A61K31/34;A61K31/365;A61K31/381;A61K31/4178;A61K31/422;A61K31/425;A61K31/427;A61K31/4427;A61P35/00;A61P35/04;A61P43/00;C07D303/00;C07D313/00;C07D405/06;C07D407/06;C07D409/06;C07D413/06;C07D417/14;C07D493/00;C07D493/04 |
主分类号 |
C07D417/06 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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