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1. 发明申请

WO2002074776A2 HIGHLY PURIFIED AND CRYSTALLINE FORM OF HARRINGTONINES, THEIR PROCESS OF PREPARATION BY PURIFICATION OF CRUDE ALKALOIDS FROM NATURAL, SYNTHETIC OR SEMI-SYNTHETIC SOURCES, ALLOWING THEIR USE FOR BLENDING IN PHARMACEUTICAL COMPOSITION PARTICULARLY USEFUL FOR TREATMENT OF CANCER IN USING ORAL MODE OF ADMINISTRATION 审中-公开
标题翻译： HARRYTONINES的高纯度和结晶形式，它们通过从天然，合成或半合成来源中纯化原核生物的方法制备的方法，允许其在药物组合物中混合使用，特别是用于治疗癌症使用口服管理模式
公开(公告)号：WO2002074776A2
公开(公告)日：2002-09-26
申请号：PCT/IB2002/002054
申请日：2002-03-21
申请人： ONCOPHARM CORPORATION , ROBIN, Jean-Pierre , BLANCHARD, Julie , DHAL, Robert , MARIE, Jean-Pierre , RADOSEVIC, Nina
发明人： ROBIN, Jean-Pierre , BLANCHARD, Julie , DHAL, Robert , MARIE, Jean-Pierre , RADOSEVIC, Nina
IPC分类号： C07D491/20
CPC分类号： C07D491/20
摘要： The invention concerns a natural, synthetic or semi-synthetic harringtonines including their tautomeric forms and their salts of the following formula: wherein n = 2 (i.e. harringtonine) or n = 3(i.e. homoharringtonine), in which the total content of impurities, possibly including enantiomeric forms, is lower than 1%, and/or the content of the major impurity is lower than 0.9%, and/or the chromatographic assay exhibits a harringtonines content higher than 97,5%.
摘要翻译：本发明涉及天然的，合成的或半合成的harringtonine，包括它们的互变异构形式及其下式的盐：其中n = 2（即，Harringtonine）或n = 3（即homoharringtonine），其中杂质的总含量可能包括对映异构体形式，低于1％，和/或主要杂质含量低于0.9％，和/或色谱测定显示哈林顿含量高于97.5％。

2. 发明申请

WO2015101628A1 WATER SOLUBLE CRYSTALLIN SALTS OF CERTAIN HARRINGTONINES UNAMBIGUOUSLY PROTONATED ON THEIR ALKALOID NITROGEN AND THEIR USE AS CHEMOTHERAPEUTIC DRUGS 审中-公开
标题翻译：水溶性结晶蛋白钠在其碱性氮化合物上不可预测地使用某些苦参碱，并作为化学药物使用
公开(公告)号：WO2015101628A1
公开(公告)日：2015-07-09
申请号：PCT/EP2014/079456
申请日：2014-12-30
申请人： ROBIN, Jean-Pierre , RADOSEVIC, Nina , BLANCHARD, Julie , ROISNEL, Thierry , BATAILLE, Thierry
发明人： ROBIN, Jean-Pierre , RADOSEVIC, Nina , BLANCHARD, Julie , ROISNEL, Thierry , BATAILLE, Thierry
IPC分类号： C07D491/14 , A61K31/55 , A61P35/00
CPC分类号： C07D491/147 , C07D491/14
摘要： The present invention concerns harringtonine salts at the solid state exhibiting a protonated nitrogen seen in solid state analysis and having formula (1), comprising solvate, made by reacting a cephalotaxine ester having formula (2), in which R 1 is, but not limited to, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl or heterocycloalkyl, and R 2 is, independently, but not limited to H, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl or heterocycloalkyl, with an acid having general formula AH in a crystallization solvent, wherein the said salt has a water or alkohol solubility ranged approximately from 5 mg/mL to approximately 100 mg/Ml. The invention also related to a process for preparing these salts and their use as chemotherapeutic drugs.
摘要翻译：本发明涉及在固态分析中看到的呈质子化氮的固态的哈林顿盐，并且具有式（1），其包含通过使具有式（2）的头孢噻肟酯反应制备的溶剂合物，其中R1是但不限于烷基，芳基，环烷基，杂烷基，杂芳基或杂环烷基，并且R 2独立地但不限于H，烷基，芳基，环烷基，杂烷基，杂芳基或杂环烷基，与具有通式AH 其中所述盐具有约5mg / mL至约100mg / Ml的水或烷醇溶解度。本发明还涉及制备这些盐的方法及其作为化学治疗药物的用途。

3. 发明申请

WO2010103405A2 PROCESS FOR PREPARING CEPHALOTAXINE ESTERS 审中-公开
标题翻译：制备西酞菁酯的方法
公开(公告)号：WO2010103405A2
公开(公告)日：2010-09-16
申请号：PCT/IB2010/000835
申请日：2010-03-11
申请人： ROBIN, Jean-Pierre , RADOSEVIC, Nina , BLANCHARD, Julie
发明人： ROBIN, Jean-Pierre , RADOSEVIC, Nina , BLANCHARD, Julie
CPC分类号： C07D491/056 , C07D263/44 , C07D307/58 , C07D307/60 , C07D491/147 , C07D498/08 , C07D498/22
摘要： A process for preparing cephalotaxine esters corresponding to the following general formula I which comprises the cephalotaxine backbone: C(R 1 ) (R 2 ) (XH)COO[CTX] wherein CTX represents the cephalotaxine backbone, being optionally substituted and/or dehydrogenated, in which formula I, X is a heteroatom, preferably an oxygen, a sulfur or a nitrogen, R 1 and R 2 , taken separately, may be alkyl, cycloalkyl, heteroalkyl, aryl, heteroaryl, heterocycloalkyl or aralkyl groups, said groups being optionally interrupted by ester functions, or groups that can form one or more rings or a heterocycle together, consisting in bringing the corresponding cephalotaxine compound, or salts, isomers or tautomeric forms thereof, which is free or which is in the form of a metal alkoxide corresponding to the following general formula CTXOM, wherein CTX represents the cephalotaxine backbone, being optionally substituted and/or dehydrogenated, in which M is a hydrogen atom or a metal atom, into contact with a heterocyclic side chain precursor having both a bifunctional protected (bidentate) and activated (acylating) form of an acid bearing a hydrogenated heteroatom, in the alpha (α) position with respect to the carboxyl group, and corresponding to the following general formula: in which case W is a carbon, sulfur, silicon or bore atom, X, R 1 and R 2 have respectively the same meaning as above, it being possible for R 1 and R 2 to form a ring or a heterocycle together, and Y and Z are alkyl or heteroalkyl radicals, or monovalent heteroatoms, which may be identical or different, in an independent manner, or may fuse so as to give a divalent heteroatom, it being possible for the X-W bond to be covalent or ionic.
摘要翻译：一种制备对应于以下通式I的头孢噻肟酯的方法，其包含头孢噻肟主链：C（R 1）（R 2）（X H）COO [CTX]，其中CTX代表头孢噻肟主链任选被取代和/或脱氢，其中式I，X是杂原子，优选氧，硫或氮，R 1和R 2分别独立地可以是烷基，环烷基，杂烷基，芳基，杂芳基，杂环烷基或芳烷基，所述基团任选被酯官能，或可以一起形成一个或多个环或杂环的基团，其包括使相应的头孢噻肟化合物或其盐，异构体或互变异构体形式，其为与下列一般相对应的金属醇盐形式，式CTXOM，其中CTX代表头孢噻肟骨架，任选地被取代和/或脱氢，其中M是氢原子或金属原子与一个连接体接触在相对于羧基的α（a）位上具有双功能保护（二齿）和活化（酰化）形式的含有氢化杂原子的酸的环状侧链前体，并且对应于以下通式：其中情况W是碳，硫，硅或孔原子，X，R 1和R 2分别具有与上述相同的含义，R 1和R 2可以一起形成环或杂环，Y和Z是烷基或杂烷基基团或单价杂原子，其可以相同或不同，以独立的方式，或可以融合以产生二价杂原子，XW键可以是共价键或离子型。

4. 发明申请

WO2015162217A2 CRYSTALLINE SALTS OF CEPHALOTAXINE AND THEIR USE FOR ITS PURIFICATION INCLUDING ENANTIOMERS 审中-公开
标题翻译：西酞红质的晶体盐及其用于纯化的用途，包括纯化剂
公开(公告)号：WO2015162217A2
公开(公告)日：2015-10-29
申请号：PCT/EP2015/058833
申请日：2015-04-23
申请人： ROBIN, Jean-Pierre , BLANCHARD, Julie , RADOSEVIC, Nina
发明人： ROBIN, Jean-Pierre , BLANCHARD, Julie , RADOSEVIC, Nina , ROISNEL, Thierry , BATAILLE, Thierry
IPC分类号： C07D491/04
CPC分类号： C07D491/04 , C07B2200/13
摘要： The present invention concerns crystalline salts of (2S,3S,4R)-cephalotaxine and of (2R,3R,4S)-cephalotaxine defined by their solid state analysis patterns, their process of preparation allowing their use for crude cephalotaxine purification including for resolution of racemic or partially racemized cephalotaxine.
摘要翻译：本发明涉及（2S，3S，4R） - 头孢噻肟和由其固态分析模式定义的（2R，3R，4S） - 头孢噻肟的结晶盐，其制备方法允许其用于粗头孢噻肟纯化，包括用于外消旋或部分消旋化的头孢噻肟。

5. 发明申请

WO2015128463A1 WATER SOLUBLE SALTS OF HARRINGTONINE AND THEIR PHARMACEUTICAL APPLICATIONS 审中-公开
标题翻译：哈灵顿水溶性盐及其药物应用
公开(公告)号：WO2015128463A1
公开(公告)日：2015-09-03
申请号：PCT/EP2015/054135
申请日：2015-02-27
申请人： ROBIN, Jean-Pierre , BLANCHARD, Julie , RADOSEVIC, Nina
发明人： ROBIN, Jean-Pierre , BLANCHARD, Julie , RADOSEVIC, Nina , ROISNEL, Thierry , BATAILLE, Thierry
IPC分类号： C07D491/20 , A61K31/55 , A61P35/00
CPC分类号： C07D491/20
摘要： A isolated harringtonines solid salt having formula 1, made by reacting a cephalotaxine ester having formula 2 in which R is, but not limited to, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl or heterocycloalkyi, with an acid having general formula AH in a crystallization solvent, wherein the salt has a water or methanol solubility of approximately 5 mg/mL to approximately 100 mg/mL, and its pharmaceutical applications.
摘要翻译：具有式1的分离的哈林顿固体盐，其通过使具有式2的头孢噻肟酯与其中R是但不限于烷基，芳基，环烷基，杂烷基，杂芳基或杂环烷基的酸与具有通式AH的酸反应制备在结晶溶剂中，其中盐具有约5mg / mL至约100mg / mL的水或甲醇溶解度及其药物应用。

6. 发明申请

WO2018055136A1 UTILISATION DES HARRINGTONINES DANS LE TRAITEMENT DU CANCER DU SEIN, NOTAMMENT TRIPLE-NÉGATIF 审中-公开
标题翻译：黄芩苷在治疗乳腺癌中的用途，特别是三阴性
公开(公告)号：WO2018055136A1
公开(公告)日：2018-03-29
申请号：PCT/EP2017/074135
申请日：2017-09-22
申请人： ROBIN, Jean-Pierre
发明人： ROBIN, Jean-Pierre , RADOSEVIC, Nina , ROBIN, Jean-Pierre , PENAULT-LLORCA, Frédérique
IPC分类号： A61K31/55 , A61P35/00
摘要： La présente invention concerne l'harringtonine, l'homoharringtonine et/ouses dérivés, notamment les composés de formule Ia à Ig tels que définis dans le tableau 1, plus particulièrement sous forme de sel, de préférence cristallin, pour utilisation dans le traitement ou la prévention du cancer du sein, en particulier le cancer du sein «triple- négatif» (CSTN).
摘要翻译：本发明涉及三尖杉酯碱，高三尖杉酯碱和从头开始，特别是式Ia化合物。如表1中所定义的Ig，更具体地以盐晶体透明的形式用于治疗或预防乳腺癌，特别是乳腺癌＆laquo 三重否定的＆raquo; （CSTN）。

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