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1. 发明公开

EP1675835A1 METHODS OF PREPARATION OF DEHYDRO-DIKETOPIPERAZINES IN LIQUID PHASE OR OF SOLID SUPPORTED PHASE 有权
标题翻译：工艺用于液体相PRODUCING脱氢DIKETOPYPERAZINEN或通过固相合成
公开(公告)号：EP1675835A1
公开(公告)日：2006-07-05
申请号：EP03738352.8
申请日：2003-07-07
申请人： Couladouros, Elias Andrea , Magos, Alexandros , Strongilos, Alexandros
发明人： Couladouros, Elias Andrea , Magos, Alexandros , Strongilos, Alexandros
IPC分类号： C07D241/18 , C07D403/06 , A61K31/496 , A61P35/00 , C07K5/12
CPC分类号： A61K31/496 , C07D241/18 , C07D401/06 , C07D403/06 , C07D403/14 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14 , C07D487/04 , Y02P20/55
摘要： The preparation of any compound of the generic structure (I); wherein: R1 and R2 are substituents described in the main text. Cycl- is a group represented by either of the formulae (a) and (b); wherein: R3 to R8, X and Y are substituents described in the main text. The above described compounds may be used for the treatment of cancer. The preparation method consists of coupling of the amine group of phosphynilglycinate with the carboxylic group of an aminoacid, the successively coupling of the above formed compound with the formyl-Cycl derivative, the deprotection of the aminoacid and the formation of dehydro-diketopiperazine employing mild alkaline conditions. The method is extended for the preparation of individual derivatives or libraries of derivatives related to the above described compounds of the general formula (II), employing a solid supported phosphonate of the general formula (II), wherein: Res represents any polymer support (resin) with or without a linker, Prot represents any NH- protective group, R represents alkyl or alkyloxyalkyl groups.

2. 发明申请

WO2005003102A1 METHODS OF PREPARATION OF DEHYDRO-DIKETOPIPERAZINES IN LIQUID PHASE OR OF SOLID SUPPORTED PHASE 审中-公开
标题翻译：在液相或固体相中制备脱氢二哌啶子酸的方法
公开(公告)号：WO2005003102A1
公开(公告)日：2005-01-13
申请号：PCT/GR2003/000028
申请日：2003-07-07
申请人： COULADOUROS, Elias , MAGOS, Alexandros , STRONGILOS, Alexandros
发明人： COULADOUROS, Elias , MAGOS, Alexandros , STRONGILOS, Alexandros
IPC分类号： C07D241/18
CPC分类号： A61K31/496 , C07D241/18 , C07D401/06 , C07D403/06 , C07D403/14 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/06 , C07D417/14 , C07D487/04 , Y02P20/55
摘要： The preparation of any compound of the generic structure (I); wherein: R 1 and R 2 are substituents described in the main text. Cycl - is a group represented by either of the formulae (a) and (b); wherein: R 3 to R 8 , X and Y are substituents described in the main text. The above described compounds may be used for the treatment of cancer. The preparation method consists of coupling of the amine group of phosphynilglycinate with the carboxylic group of an aminoacid, the successively coupling of the above formed compound with the formyl- Cycl derivative, the deprotection of the aminoacid and the formation of dehydro-diketopiperazine employing mild alkaline conditions. The method is extended for the preparation of individual derivatives or libraries of derivatives related to the above described compounds of the general formula (II), employing a solid supported phosphonate of the general formula (II), wherein: Res represents any polymer support (resin) with or without a linker, Prot represents any NH- protective group, R represents alkyl or alkyloxyalkyl groups.
摘要翻译：制备通用结构（I）的任何化合物; 其中：R 1和R 2是本文中描述的取代基。 Cycl-是由式（a）和（b）中的任一个表示的基团; 其中：R 3至R 8，X和Y是主要文中描述的取代基。上述化合物可用于治疗癌症。制备方法由膦酰基甘氨酸的胺基与氨基酸的羧基的偶联，上述形成的化合物与甲酰基-Cly衍生物的连续偶联，氨基酸的脱保护和使用温和碱性的脱氢 - 二酮哌嗪的形成条件。该方法延伸用于制备与上述通式（II）化合物有关的衍生物或衍生物文库，使用通式（II）的固体支持的膦酸酯，其中：Res代表任何聚合物载体（树脂）具有或不具有连接基团，Prot代表任何NH-保护基团，R代表烷基或烷氧基烷基。

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