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1. 发明申请

WO2007031803A3 MOLECULAR RESISTS BASED ON FUNCTIONALIZED POLYCARBOCYCLES 审中-公开
公开(公告)号：WO2007031803A3
公开(公告)日：2007-03-22
申请号：PCT/GR2006/000050
申请日：2006-09-18
申请人： NATIONAL CENTER FOR SCIENTIFIC RESEARCH (NCSR) ''DEMOKRITOS'' , ARGITIS, Panagiotis , GOGOLIDES, Evangelos , COULADOUROS, Elias , NIAKOULA, Dimitra , VIDALI, Veroniki , GAUTAM, Daman, R.
发明人： ARGITIS, Panagiotis , GOGOLIDES, Evangelos , COULADOUROS, Elias , NIAKOULA, Dimitra , VIDALI, Veroniki , GAUTAM, Daman, R.
IPC分类号： G03F7/039
摘要： The present invention refers to new organic molecules, derived from the class of polycarbocycle derivatives, and their application as components of photoresists, and in particular as components of photoresist compositions where no polymer is comprised as one of the photoresists components. In these photoresist formulations the new molecule(s) is/are the main component(s) (i.e. percentage higher than 50 % w/w).

2. 发明公开

EP1941324A2 MOLECULAR RESISTS BASED ON FUNCTIONALIZED POLYCARBOCYCLES 审中-公开
标题翻译：分子抗蚀BASED功能化polycarbocycles
公开(公告)号：EP1941324A2
公开(公告)日：2008-07-09
申请号：EP06779677.1
申请日：2006-09-18
申请人： National Center for Scientific Research Demokritos , Argitis, Panagiotis , Gogolidis, Evangelos , Couladouros, Elias Andreas
发明人： ARGITIS, Panagiotis , GOGOLIDES, Evangelos , COULADOUROS, Elias , NIAKOULA, Dimitra , VIDALI, Veroniki , GAUTAM, Daman, R.
IPC分类号： G03F7/039
CPC分类号： G03F7/0397 , G03F7/0392
摘要： The present invention refers to new organic molecules, derived from the class of polycarbocycle derivatives, and their application as components of photoresists, and in particular as components of photoresist compositions where no polymer is comprised as one of the photoresists components. In these photoresist formulations the new molecule(s) is/are the main component(s) (i.e. percentage higher than 50 % w/w).

3. 发明申请

WO2020039097A1 2,6-BIS(((1H-BENZO[D]IMIDAZOL-2-YL)THIO)METHYL)PYRIDINE AND N2,N6-DIBENZYLPYRIDINE-2,6-DICARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE (PI3K) INHIBITORS FOR TREATING CANCER 审中-公开
公开(公告)号：WO2020039097A1
公开(公告)日：2020-02-27
申请号：PCT/EP2019/072648
申请日：2019-08-23
申请人： BIOMEDICAL RESEARCH FOUNDATION OF THE ACADEMY OF ATHENS (BRFAA) , AGRICULTURAL UNIVERSITY OF ATHENS (AUA) , FOUNDATION FOR RESEARCH AND TECHNOLOGY- HELLAS (FORTH) , COURNIA, Zoe , EFSTRATIADIS, Argiris , KAPELLA, Anna , COULADOUROS, Elias
发明人： COURNIA, Zoe , EFSTRATIADIS, Argiris , KAPELLA, Anna , COULADOUROS, Elias , CHRISTOFORIDIS, Savvas
IPC分类号： C07D401/14 , C07D213/81 , A61K31/4439 , A61P35/00
摘要： 2,6-bis(((lH-benzo[d]imidazol-2-yl)thio)methyl)pyridine and N2, N6-dibenzylpyridine-2, 6-dicarboxamide derivatives and related compounds as phosphoinositide 3-kinase (PI3K) inhibitors for treating cancer. The present invention relates to pharmaceutically active 2,6- bis(((lH-benzo[d]imidazol-2-yl)thio)methyl)pyridine, N2,N6- dibenzylpyridine-2, 6-dicarboxamide and N2,N6-bis(3-hydroxyphenyl) pyridine-2, 6-dicarboxamide, as well as to derivatives thereof, and to structurally related compounds. These compounds are phosphoinositide 3-kinase inhibitors (PI3K) and useful in treating or preventing cancerous diseases. The invention further relates methods of manufacturing such compounds as well as to pharmaceutical compositions and formulations comprising such compounds, optionally together with other pharmaceutically active compounds. The invention further relates to a method for determining the activity of PI3Kalpha or PI3Kalpha mutants, which method includes: a) providing a solid phase which is functionalized by immobilization of GST-GRPl-molecules onto the solid phase, b) performing a PI3Kalpha or PI3Kalpha mutant catalyzed enzyme reaction to convert PIP2 to PIP3, c) adding competitor PIP3 carrying a detectable label or reporter molecule, and d) determining enzyme activity based on the amount of PIP3 obtained in step b) which competes with competitor PIP3 for binding to the functionalized solid phase.

4. 发明申请

WO2005121077A1 PREPARATION AND APPLICATIONS OF POLYMER-SUPPORTED HALOGENATED BENZOQUINONES AS OXIDATIVE AGENTS 审中-公开
标题翻译：聚合物支持的氢化苯甲酸酯作为氧化剂的制备和应用
公开(公告)号：WO2005121077A1
公开(公告)日：2005-12-22
申请号：PCT/GR2004/000033
申请日：2004-06-10
申请人： COULADOUROS, Elias , STRONGILOS, Alexandros
发明人： COULADOUROS, Elias , STRONGILOS, Alexandros
IPC分类号： C07C255/46
CPC分类号： C07C255/57 , C07B2200/11 , C07C255/53 , C07C255/54 , C07C255/55 , C07C317/44 , C07C2601/16 , C07J75/00 , Y02P20/55
摘要： This invention provides a general method for the synthesis of polymer-supported benzoquinones described by the following generic structure I: wherein: •, X, R 1 , R 2 and R 3 are described in the main text . The general concept of the method consists of the use of a halogenated starting material of the general structure II (Figure 1) which by an nucleophilic substitution reaction (NSR) or a palladium mediated coupling (PMC) is either directly loaded on a resin to afford IIIa (Path A) or transformed to intermediate IIIb (Path B) which is subsequently (with or without modification) loaded on a resin to afford once again IIIa. Deprotection and/or oxidation of IIIa, if needed, afford target solid-supported oxidants I The polymer-supported benzoquinones I are used for the oxidation of hydroquinones to quinones, for the oxidation of benzylic alcohols the aldehydes, for the removal of p -methoxybenzyl and related protective groups, for the dehydrogenation of tetrahydronaphthalene derivatives and for the dehydrogenation of steroid 4-en-3-ones. The polymer-supported reagent after its use is regenerated upon treatment with an oxidative agent.
摘要翻译：本发明提供了通过以下通用结构I描述的合成聚合物负载的苯醌的一般方法：其中：。，X，R 1，R 2和R 3在正文中描述。该方法的一般概念包括使用一般结构II（图1）的卤化起始材料，其通过亲核取代反应（NSR）或钯介导的偶联（PMC）直接负载在树脂上以提供 IIIa（路径A）或转化成中间体IIIb（路径B），其随后（有或没有改性）负载在树脂上以再次提供IIIa。如果需要，IIIa的脱保护和/或氧化提供目标固体负载的氧化剂I聚合物负载的苯醌I用于将氢醌氧化成醌，用于苄基醇的氧化醛，用于除去对甲氧基苄基和相关的保护基团，用于四氢萘衍生物的脱氢和类固醇4-烯-3-酮的脱氢。使用后的聚合物负载的试剂在用氧化剂处理时再生。

5. 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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