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1. 发明申请

WO2003040402A2 ALPHA-HELIX MIMICRY BY A CLASS OF ORGANIC MOLECULES 审中-公开
标题翻译： ALPHA-HELIX MIMICRY一系列有机分子
公开(公告)号：WO2003040402A2
公开(公告)日：2003-05-15
申请号：PCT/US2002/036680
申请日：2002-11-12
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , GUY, Rodney, K. , KUNTZ, Irwin, D. , LU, Felice
发明人： GUY, Rodney, K. , KUNTZ, Irwin, D. , LU, Felice
IPC分类号： C12Q
CPC分类号： C07D217/04 , C07D241/42
摘要： The present invention provides methods for making compounds and methods for using the compounds to disrupt or inhibit protein-protein interactions. Also provided are pharmaceutical compositions comprising the compounds of the current invention.
摘要翻译：本发明提供了制备化合物的方法和使用该化合物来破坏或抑制蛋白质 - 蛋白质相互作用的方法。还提供了包含本发明化合物的药物组合物。

2. 发明申请

WO2003040402A3 ALPHA-HELIX MIMICRY BY A CLASS OF ORGANIC MOLECULES 审中-公开
公开(公告)号：WO2003040402A3
公开(公告)日：2003-05-15
申请号：PCT/US2002/036680
申请日：2002-11-12
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA , GUY, Rodney, K. , KUNTZ, Irwin, D. , LU, Felice
发明人： GUY, Rodney, K. , KUNTZ, Irwin, D. , LU, Felice
IPC分类号： C07C237/40
摘要： The present invention provides methods for making compounds and methods for using the compounds to disrupt or inhibit protein-protein interactions. Also provided are pharmaceutical compositions comprising the compounds of the current invention.

3. 发明申请

WO1995018798A1 CHEMICAL SWITCHING OF TAXO-DITERPENOIDS BETWEEN LOW SOLUBILITY ACTIVE FORMS AND HIGH SOLUBILITY INACTIVE FORMS 审中-公开
标题翻译：低溶解度活性物质和高溶解度不活泼形式之间的TAXO-DITERPENOIDS的化学开关
公开(公告)号：WO1995018798A1
公开(公告)日：1995-07-13
申请号：PCT/US1995000481
申请日：1995-01-10
申请人： THE SCRIPPS RESEARCH INSTITUTE , NICOLAOU, K, C. , WRASIDLO, Wolfgang , GUY, Rodney, K. , PITSINOS, Emmanuel
发明人： THE SCRIPPS RESEARCH INSTITUTE
IPC分类号： C07D305/14
CPC分类号： C07D405/14 , C07D305/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07F7/1804
摘要： Cyclic chemical switching method is employed for solubilizing and desolubilizing taxo-diterpenoids with respect to aqueous solvents. 2-halogenated onium salts of aza-arenes are employed to derivatize taxo-diterpenoids so as to alter their solubility in aqueous solvents. The onium salt of aza-arene includes a delocalized charge which imparts polarity and aqueous solubility to taxo-diterpenoid derivatives. Solubilization is achieved in a one step derivatization with the onium salt of 2-halogenated aza-arenes. Desolubilization is achieved by contacting onium salts of taxo-diterpenoid-C ,2-O-aza-arenes with serum protein to displace the 2-O-aza-arene and form a soluble protein:taxo-diterpenoid intermediate. This protein:taxo-diterpenoid intermediate then dissociates over time to provide a bioactive taxo-diterpenoid. Preferred taxo-diterpenoids include taxol, C-2 substituted taxol, and Taxotere . These same onium salts of taxo-diterpenoid-C ,2-O-aza-arenes are employed as water soluble prodrugs. For example, taxol-2'-methylpyridinium tosylate (MPT) is characterized by an elevated aqueous solubility, rapid activation by serum protein, good stability in most other aqueous solutions, formation of a protein:taxol intermediate and good retention within the circulatory system. The toxicity of the activated form is comparable or greater than underivatized taxol. Furthermore, taxol-2'-MPT can be synthesized by a simple one step reaction between taxol and 2-fluoro-1-MPT. The invention is applicable to taxol and taxol mimetics having hydroxyls that are reactive with onium salts of 2-halogenated-aza-arenes. For example, taxol and Taxotere each have reactive hydroxyls at the 2' and 7 positions. The invention is also applicable to a wide array of 2-halogenated-aza-arenes.
摘要翻译：循环化学开关方法用于溶解和脱溶剂相对于含水溶剂的分子二萜类化合物。使用氮杂芳烃的2-卤代鎓盐衍生分子二萜类化合物，以改变其在含水溶剂中的溶解度。氮杂芳烃的鎓盐包括赋予紫杉醇衍生物极性和水溶性的离域电荷。用2-卤代氮杂芳烃的鎓盐在一步衍生化中实现溶解。通过使分子二萜-Cn，2-O-氮杂芳烃与血清蛋白质的盐接触来置换2-O-氮杂 - 芳烃并形成可溶性蛋白质：taxo-diterpenoid中间体来实现脱醇。该蛋白质：taxo-diterpenoid中间体随后随着解离以提供生物活性的taxo-diterpenoid。优选的分子二萜类化合物包括紫杉醇，C-2取代的紫杉醇和Taxotere TM。使用这些相同的二 - p enoid enoid enoid--，，ium ium nes nes nes nes nes。。。。。。。。。。例如，紫杉醇-2'-甲基吡啶甲苯磺酸盐（MPT）的特征在于水溶性升高，通过血清蛋白快速活化，在大多数其他水溶液中具有良好的稳定性，形成蛋白质：紫杉醇中间体和在循环系统内具有良好的保留性。活性形式的毒性与未衍生的紫杉醇相当或更大。此外，紫杉醇-2-MPT可以通过紫杉醇和2-氟-1-MPT之间的简单的一步反应合成。本发明适用于具有与2-卤代 - 氮杂芳烃的鎓盐反应的羟基的紫杉醇和紫杉醇模拟物。例如，紫杉醇和泰索帝各自在2'和7个位置具有反应性羟基。本发明也适用于广泛的2-卤代 - 氮杂芳烃。

4. 发明申请

WO1995018613A1 SELF-ASSEMBLED TAXO-DIPERPENOID NANOSTRUCTURES 审中-公开
标题翻译：自组装的紫杉醇 - 二烯酸纳结构
公开(公告)号：WO1995018613A1
公开(公告)日：1995-07-13
申请号：PCT/US1995000538
申请日：1995-01-11
申请人： THE SCRIPPS RESEARCH INSTITUTE , NICOLAOU, K., C. , WRASIDLO, Wolfgang , GUY, Rodney, K. , PITSINOS, Emmanuel
发明人： THE SCRIPPS RESEARCH INSTITUTE
IPC分类号： A61K31/44
CPC分类号： C07D405/14 , C07D305/14 , C07D409/14 , C07D411/12 , C07D411/14 , C07D413/12 , C07D417/14 , Y10S977/906
摘要： Onium salts of taxo-diterpenoid-C ,2-O-aza-arenes form water soluble self-assembling nanostructures above a critical aggregation concentration. The onium salt of aza-arene includes a delocalized charge which renders derivatized taxo-diterpenoids amphoteric, enhances their solubility in water, and promotes self-assembly of water soluble nanostructures, e.g., helical fibular structures and spherical micellular structures. These same onium salts of taxo-diterpenoid-C ,2-O-aza-arenes are employed as water soluble prodrugs. For example, taxol-2'-methylpyridinium tosylate (MPT) is characterized by an elevated aqueous solubility, rapid activation by serum protein, good stability in most other aqueous solutions, formation of a protein: taxol intermediate and good retention within the circulatory system. The toxicity of the activated form is comparable or greater than underivatized taxol. Furthermore, taxol-2'-MPT can be synthesized by a simple one step reaction between taxol and 2-fluoro-1-MPT. The invention is applicable to taxol and taxol memetics having hydroxyls that are reactive with onium salts of 2-halogenated-aza-arenes. For example, taxol, C-2 substituted taxol and Taxotere each have reactive hydroxyls at the 2' and 7 positions. The invention is also applicable to a wide array of 2-halogenated-aza-arenes.
摘要翻译：紫杉醇二价enoid enoid enoid nes nes nes nes nes nes nes nes。。。。。。。。。。。。。。。。。。。。。氮杂芳烃的鎓盐包括离域电荷，其使衍生的二元萜类化合物两性，增强其在水中的溶解度，并促进水溶性纳米结构的自组装，例如螺旋状腓骨结构和球形胶束结构。使用这些相同的二 - p enoid enoid enoid--，，ium ium nes nes nes nes nes。。。。。。。。。。例如，紫杉醇-2'-甲基吡啶甲苯磺酸盐（MPT）的特征在于水溶性升高，通过血清蛋白快速活化，在大多数其他水溶液中具有良好的稳定性，形成蛋白质：紫杉醇中间体和在循环系统内具有良好的保留性。活性形式的毒性与未衍生的紫杉醇相当或更大。此外，紫杉醇-2-MPT可以通过紫杉醇和2-氟-1-MPT之间的简单的一步反应合成。本发明适用于具有与2-卤代 - 氮杂 - 芳烃的鎓盐反应的羟基的紫杉醇和紫杉醇记忆。例如，紫杉醇，C-2取代的紫杉醇和泰索帝各自在2'和7个位置具有反应性羟基。本发明也适用于广泛的2-卤代 - 氮杂芳烃。

5. 发明申请

WO1995018804A1 WATER SOLUBLE ONIUM SALT OF TAXO-DITERPENOID 审中-公开
标题翻译：水溶性硫酸钠的盐溶液
公开(公告)号：WO1995018804A1
公开(公告)日：1995-07-13
申请号：PCT/US1995000478
申请日：1995-01-10
申请人： THE SCRIPPS RESEARCH INSTITUTE , NICOLAOU, K., C. , WRASIDLO, Wolfgang , GUY, Rodney, K. , PITSINOS, Emmanuel
发明人： THE SCRIPPS RESEARCH INSTITUTE
IPC分类号： C07D405/12
CPC分类号： C07D405/12 , C07D405/14 , C07D409/14 , C07D411/12 , C07D411/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Onium salts of taxo-diterpenoid-C , 2-0-aza-arenes are employed as water soluble prodrugs. For example, taxol-2'-methylpyridinium tosylate (MPT) is characterized by an elevated aqueous solubility, rapid activation by serum protein, good stability in most other aqueous solutions, formation of a protein:taxol intermediate and good retension within the circulatory system. The toxicity of the activated form is comparable or greater than underivatized taxol. Furthermore, taxol-2'-MPT can be synthesized by a simple one step reaction between taxol and 2-fluoro-1-MPT. The invention is applicable to taxol and taxol mimetics having hydroxyls that are reactive with onium salts of 2-halogenated-aza-arenes. For example, taxol, C-2 substituted analogs of taxol, and Taxotere each have reactive hydroxyls at the 2' and 7 positions. The invention is also applicable to a wide array of 2-halogenated-aza-arenes.
摘要翻译：盐酸二萜-C 0，2-0-氮杂 - 芳烃的鎓盐用作水溶性前药。例如，紫杉醇-2'-甲基吡啶甲苯磺酸盐（MPT）的特征在于水溶性升高，通过血清蛋白快速活化，在大多数其他水溶液中具有良好的稳定性，形成蛋白质：紫杉醇中间体和在循环系统内具有良好的延迟。活性形式的毒性与未衍生的紫杉醇相当或更大。此外，紫杉醇-2-MPT可以通过紫杉醇和2-氟-1-MPT之间的简单的一步反应合成。本发明适用于具有与2-卤代 - 氮杂芳烃的鎓盐反应的羟基的紫杉醇和紫杉醇模拟物。例如，紫杉醇，紫杉醇的C-2取代的类似物和泰索帝各自在2'和7位具有反应性羟基。本发明也适用于广泛的2-卤代 - 氮杂芳烃。

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