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1. 发明授权

US08558019B2 Thiolated paclitaxels for reaction with gold nanoparticles as drug delivery agents 有权
标题翻译：硫化紫杉醇与金纳米粒子作为药物递送剂反应
公开(公告)号：US08558019B2
公开(公告)日：2013-10-15
申请号：US12373135
申请日：2008-11-10
申请人： David G. I. Kingston , Shugeng Cao , Jielu Zhao , Glullo F. Paciotti , Marja S. Hubta
发明人： David G. I. Kingston , Shugeng Cao , Jielu Zhao , Glullo F. Paciotti , Marja S. Hubta
IPC分类号： C07D305/14
CPC分类号： C07D305/14 , A61K47/6923 , B82Y5/00
摘要： Thioloated taxane derivatives are linked to colloidal metal particles such as gold nanoparticles for use as antitumor agents. The antitumor agents may be targeted to tumors.
摘要翻译：透射紫杉烷衍生物与胶体金属颗粒如金纳米颗粒连接，用作抗肿瘤剂。抗肿瘤剂可以靶向肿瘤。

2. 发明授权

US5296506A Rearranged taxol compounds and method of using in testing of in vivo activity 失效
标题翻译：重组的紫杉醇化合物和用于体内活性测试的方法
公开(公告)号：US5296506A
公开(公告)日：1994-03-22
申请号：US978713
申请日：1992-11-19
申请人： David G. I. Kingston , Gamini Samaranyake
发明人： David G. I. Kingston , Gamini Samaranyake
IPC分类号： C07D305/14 , C07D317/70 , A01N43/02 , C07D305/00 , C07D407/00
CPC分类号： C07D317/70 , C07D305/14
摘要： In a preferred embodiment, taxol is treated with mesyl chloride to prepare a taxol derivative with a contracted A-ring, which has comparable activity to taxol in a tubulin depolymerization assay, and which shows cytotoxicity against KB cells in a cell culture assay. In an alternate preferred embodiment, taxol is treated with triethyloxonium tetrafluoroborate (Meerwein's reagent) to produce a taxol derivative with an opened oxetane ring. In another alternate preferred embodiment, reaction of taxol with acetyl chloride yields a taxol derivative in which the oxetane ring is opened and the A-ring is contracted. All of the aforementioned products show in vivo activity in KB cell culture assays. Further, the preferred compounds have different in vivo activities, which makes them ideal to form a range of standards for use in biological testing of other compounds.
摘要翻译：在优选的实施方案中，紫杉醇用甲磺酰氯处理以制备具有收缩的A环的紫杉醇衍生物，其在微管蛋白解聚测定中具有与紫杉醇相当的活性，并且在细胞培养测定中显示出对KB细胞的细胞毒性。在替代的优选实施方案中，用三乙基氧鎓四氟硼酸盐（Meerwein's试剂）处理紫杉醇以产生具有开放的氧杂环丁烷环的紫杉醇衍生物。在另一个优选的实施方案中，紫杉醇与乙酰氯的反应产生紫杉酚衍生物，其中氧杂环丁烷环被打开并且A环收缩。所有上述产物在KB细胞培养测定中显示体内活性。此外，优选的化合物具有不同的体内活性，这使得它们成为形成用于其它化合物的生物测试的一系列标准品的理想选择。

3. 发明授权

US5059699A Water soluble derivatives of taxol 失效
标题翻译：紫杉醇的水溶性衍生物
公开(公告)号：US5059699A
公开(公告)日：1991-10-22
申请号：US573731
申请日：1990-08-28
申请人： David G. I. Kingston , Zhi-Yang Zhao
发明人： David G. I. Kingston , Zhi-Yang Zhao
IPC分类号： A61K31/335 , A61K31/337 , A61P35/00 , C07D305/14
CPC分类号： C07D305/14
摘要： Sulfonated 2'-acryloyltaxol and sulfonated 2'-O-acyl acid taxol derivatives are synthesized which have improved water solubility and stability while maintaining bio-activity. In particular, 2'-[(3-sulfo-1-oxopropyl)oxy]taxol sodium salt is synthesized by reacting taxol with acrylic acid, and subsequently reacting the 2'-acryloyltaxol with bisulfite in a Michael reaction. 2'-{[4-((2-sulfoethyl)amino)-1,4-dioxobutyl]oxy}taxol sodium salt and 2'-{[4-((3-sulfopropyl)amino-1,4-dioxobutyl]oxy}taxol sodium salt are synthesized by reacting 2'-succinyltaxol with the tetrabutylammonium salts of taurine and 3-aminopropyl sulfonic acid, respectively, and subsequently exchanging the ammonium with sodium. Glycol derivatives of 2'-O-acyl acid taxols with improved water solubility are synthesized by reaction of a glycol with 2'-O-acyl acid taxol.

4. 发明授权

US5739359A Methods for preparing 1-deoxy paclitaxels 失效
标题翻译： 1-脱氧紫杉醇的制备方法
公开(公告)号：US5739359A
公开(公告)日：1998-04-14
申请号：US840171
申请日：1997-04-14
申请人： David G. I. Kingston , Mahendra D. Chordia , Prakash G. Jagtap
发明人： David G. I. Kingston , Mahendra D. Chordia , Prakash G. Jagtap
IPC分类号： A61K31/335 , A61K31/337 , A61P35/00 , C07D305/14 , C07D493/08 , C07D309/08
CPC分类号： C07D493/08 , C07D305/14 , Y02P20/55
摘要： The present invention provides methods for making a novel class of 1-deoxy paclitaxel derivatives. These derivatives include 1-deoxy paclitaxel. The derivatives of the present invention are potent cytotoxic agents.
摘要翻译：本发明提供了制备新型1-脱氧紫杉醇衍生物的方法。这些衍生物包括1-脱氧紫杉醇。本发明的衍生物是有效的细胞毒性剂。

5. 发明授权

US5703247A 2-Debenzoyl-2-acyl taxol derivatives and methods for making same 失效
标题翻译： 2-脱苯甲酰基-2-酰基紫杉醇衍生物及其制备方法
公开(公告)号：US5703247A
公开(公告)日：1997-12-30
申请号：US202108
申请日：1994-02-25
申请人： David G. I. Kingston , Ashok Gopal Chaudhary , Milind Moreshwar Gharpure , John Matthew Rimoldi , A. A. Leslie Gunatilaka
发明人： David G. I. Kingston , Ashok Gopal Chaudhary , Milind Moreshwar Gharpure , John Matthew Rimoldi , A. A. Leslie Gunatilaka
IPC分类号： A61K31/335 , A61K31/337 , A61P35/00 , C07D305/14 , C07D405/12 , C07D409/12 , C07F7/18
CPC分类号： C07D405/12 , C07D305/14 , C07D409/12 , C07F7/1856 , Y02P20/55
摘要： Compounds having the general formula: ##STR1## wherein R.sub.1 is an alkyl or substituted alkyl; R.sub.2 is selected from the group consisting of H and C(O)R.sub.a ; R.sub.3 is selected from the group consisting of H, protecting groups, R.sub.b, and C(O)R.sub.b ; R.sub.4 is selected from the group consisting of H and C(O)R.sub.c, and wherein R.sub.a, R.sub.b, and R.sub.c are independently selected from the group consisting of alkyls, substituted alkyls, alkenyls, alkynyls, aryls, and substituted aryls; provided that R.sub.a is other than phenyl and 3-hydroxyphenyl.
摘要翻译：具有以下通式的化合物：其中R 1是烷基或取代的烷基; R2选自H和C（O）Ra; R3选自H，保护基，Rb和C（O）Rb; R 4选自H和C（O）R c，其中R a，R b和R c独立地选自烷基，取代的烷基，烯基，炔基，芳基和取代的芳基; 条件是Ra不是苯基和3-羟基苯基。

6. 发明授权

US5278324A Water soluble derivatives of taxol 失效
标题翻译：紫杉醇的水溶性衍生物
公开(公告)号：US5278324A
公开(公告)日：1994-01-11
申请号：US774107
申请日：1991-10-15
申请人： David G. I. Kingston , Zhi-Yang Zhao
发明人： David G. I. Kingston , Zhi-Yang Zhao
IPC分类号： A61K31/335 , C07D305/14
CPC分类号： C07D305/14
摘要： Sulfonated 2'-acryloyltaxol and sulfonated 2'-O-acyl acid taxol derivatives are synthesized which have improved water solubility and stability while maintaining bioactivity. In particular, 2'-[(3-sulfo-1-oxopropyl)oxy]taxol sodium salt is synthesized by reacting taxol with acrylic acid, and subsequently reacting the 2'-acryloyltaxol with bisulfite in a Michael reaction. 2'-{[4-((2-sulfoethyl)amino)-1,4-dioxobutyl]oxy}taxol sodium salt and 2'-{[4-((3-sulfopropyl)amino)-1,4-dioxobutyl]oxy}taxol sodium salt are synthesized by reacting 2'-succinyltaxol with the tetrabutylammonium salts of taurine and 3-aminopropyl sulfonic acid, respectively, and subsequently exchanging the ammonium with sodium. Glycol derivatives of 2'-O-acyl acid taxols with improved water solubility are synthesized by reaction of a glycol with 2'-O-acyl acid taxol.
摘要翻译：合成了磺化的2'-丙烯酰基紫杉醇和磺化的2'-O-酰基紫杉酚衍生物，其具有改善的水溶性和稳定性，同时保持生物活性。特别地，通过使紫杉醇与丙烯酸反应合成2' - （（3-磺基-1-氧代丙基）氧基）紫杉酚钠盐，随后在迈克尔反应中使2'-丙烯酰基紫杉醇与亚硫酸氢盐反应。 2' - （（4 - （（2-磺乙基）氨基）-1,4-二氧代丁基）氧基）紫杉醇钠盐和2' - （（4 - （（3-磺丙基）氨基）-1,4-二氧代丁基）氧基）紫杉醇钠盐分别通过使2'-琥珀酰基紫杉醇与牛磺酸和3-氨基丙基磺酸的四丁基铵盐反应，然后将铵与钠交换而合成。通过二醇与2'-O-酰基紫杉醇的反应合成具有改善的水溶性的2'-O-酰基丁二酸的二醇衍生物。

7. 发明申请

US20110144163A1 THIOLATED PACLITAXELS FOR REACTION WITH GOLD NANOPARTICLES AS DRUG DELIVERY AGENTS 有权
标题翻译：用于与金纳米颗粒作为药物递送剂反应的硫化PACLITAXEL
公开(公告)号：US20110144163A1
公开(公告)日：2011-06-16
申请号：US12373135
申请日：2008-11-10
申请人： David G. I. Kingston , Shugeng Cao , Jielu Zhao , Mathis Hodge , Giulio F. Paciotti , Marja S. Huhta
发明人： David G. I. Kingston , Shugeng Cao , Jielu Zhao , Mathis Hodge , Giulio F. Paciotti , Marja S. Huhta
IPC分类号： A61K31/4427 , C07D405/12 , C07D409/12 , C07D305/14 , A61K31/337 , A61K31/385 , A61P35/00 , C07F1/12 , C07K14/525 , C07K16/00 , B82Y5/00
CPC分类号： C07D305/14 , A61K47/6923 , B82Y5/00
摘要： Thioloated taxane derivatives are linked to colloidal metal particles such as gold nanoparticles for use as antitumor agents. The antitumor agents may be targeted to tumors.
摘要翻译：透射紫杉烷衍生物与胶体金属颗粒如金纳米颗粒连接，用作抗肿瘤剂。抗肿瘤剂可以靶向肿瘤。

8. 发明授权

US5319112A Method for the conversion of cephalomannine to taxol and for the preparation of N-acyl analogs of taxol 失效
标题翻译：将头孢菌胺转化为紫杉醇和制备紫杉醇的N-酰基类似物的方法
公开(公告)号：US5319112A
公开(公告)日：1994-06-07
申请号：US931319
申请日：1992-08-18
申请人： David G. I. Kingston , Anthony A. Molinero
发明人： David G. I. Kingston , Anthony A. Molinero
IPC分类号： C07D305/14
CPC分类号： C07D305/14
摘要： The natural product cephalomannine can be converted to the important anticancer natural product taxol by a simple process involving the steps of hydrogenation, benzoylation at the C-2'-position, protection of the C-7 position, and reaction with oxalyl chloride, followed by reaction with diphenylcarbodiimide and deprotection. The same process can be applied to mixtures of taxol and cephalomannine, thus obviating the need for the separation of these closely related compounds. In addition, the selection of an acylating reagent other than the benzoyl group allows the preparation of taxol analogs with other N-acyl substituents.
摘要翻译：天然产物cephalomannine可以通过简单的方法转化成重要的抗癌天然产物紫杉醇，包括氢化，C-2位上的苯甲酰化，C-7位的保护和与草酰氯的反应，然后是与二苯基碳二亚胺反应并脱保护。相同的方法可以应用于紫杉醇和头孢麻黄碱的混合物，从而避免了分离这些紧密相关的化合物的需要。此外，除苯甲酰基以外的酰化试剂的选择允许制备具有其它N-酰基取代基的紫杉酚类似物。

9. 发明授权

US07560536B2 Morning glory-derived anticancer agents, and novel ipomoeassin compounds 有权
标题翻译：牵牛花衍生的抗癌药，以及新型的皮托松辛化合物
公开(公告)号：US07560536B2
公开(公告)日：2009-07-14
申请号：US11366806
申请日：2006-03-03
申请人： David G. I. Kingston , Shugeng Cao
发明人： David G. I. Kingston , Shugeng Cao
IPC分类号： C07H17/08
CPC分类号： C07H13/02
摘要： Ipomoeassin compounds derived from morning glory plant material (especially Ipomoea sp. from Suriname) are useful as anti-cancer agents. The novel compounds also are useful for treating neurodegenerative disorders (such as Alzheimer's disease) in human patients.
摘要翻译：衍生自牵牛花植物材料（特别是来自苏里南的洋番茄）的番茄红素化合物可用作抗癌剂。新型化合物还可用于治疗人类患者的神经变性疾病（如阿尔茨海默病）。

10. 发明授权

US5614645A Methods for making 2-debenzoyl and -2-acyl taxol derivatives 失效
标题翻译：制备2-脱苯甲酰基和-2-酰基紫杉醇衍生物的方法
公开(公告)号：US5614645A
公开(公告)日：1997-03-25
申请号：US471886
申请日：1995-06-07
申请人： David G. I. Kingston , Ashok G. Chaudhary , Milind M. Gharpure , John M. Rimoldi , A. A. Leslie Gunatilaka
发明人： David G. I. Kingston , Ashok G. Chaudhary , Milind M. Gharpure , John M. Rimoldi , A. A. Leslie Gunatilaka
IPC分类号： A61K31/335 , A61K31/337 , A61P35/00 , C07D305/14 , C07D405/12 , C07D409/12 , C07F7/18
CPC分类号： C07D405/12 , C07D305/14 , C07D409/12 , C07F7/1856 , Y02P20/55
摘要： The present invention relates a method of making to 2-debenzoyl-2-acyl taxol derivatives, and analogues thereof.
摘要翻译：本发明涉及制备2-脱苯甲酰基-2-酰基紫杉醇衍生物的方法及其类似物。

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