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1. 发明授权

US06858644B2 Paclitaxel solvates 失效
标题翻译：紫杉醇溶剂化物
公开(公告)号：US06858644B2
公开(公告)日：2005-02-22
申请号：US10304615
申请日：2002-11-26
申请人： Daniel A. Benigni , Jack Z. Gougoutas , John D. DiMarco
发明人： Daniel A. Benigni , Jack Z. Gougoutas , John D. DiMarco
IPC分类号： A61K31/337 , A61P35/00 , C07C233/03 , C07C233/05 , C07C255/03 , C07C317/04 , C07D305/14 , C07D409/12 , A61K31/335
CPC分类号： C07D409/12 , A61K31/337 , C07D305/14
摘要： Biologically active crystalline solvates of paclitaxel are precipitated using polar, aprotic, organic solvents. A pharmaceutical composition is also disclosed, as well as the preparation of the novel solvates and their uses as anti-tumor agents.
摘要翻译：使用极性，非质子，有机溶剂沉淀紫杉醇的生物活性结晶溶剂合物。还公开了药物组合物，以及新溶剂合物的制备及其作为抗肿瘤剂的用途。

2. 发明授权

US5011774A Dideoxyinosine by enzymatic deamination of dideoxyadenosine 失效
标题翻译：双脱氧肌苷通过双脱氧腺苷的酶脱氨作用
公开(公告)号：US5011774A
公开(公告)日：1991-04-30
申请号：US486701
申请日：1990-02-28
申请人： Vittorio Farina , Daniel A. Benigni , Paul R. Brodfuehrer
发明人： Vittorio Farina , Daniel A. Benigni , Paul R. Brodfuehrer
IPC分类号： C07H19/16 , C12P19/40
CPC分类号： C07H19/16 , C12P19/40
摘要： A novel process utilizing adenosine deaminase to selectively produce .beta.-(D)-2',3'-dideoxyinosine in high yields from an .alpha.,.beta.-anomeric mixture. .beta.-(D)-2',3'-Dideoxyinosine so produced is useful as an antiviral and antibiotic agent.
摘要翻译：一种利用腺苷脱氨酶以α，β-异构体混合物高产率选择性产生β-（D）-2'，3'-二脱氧肌苷的新方法。所产生的β-（D）-2'，3'-二脱氧肌苷可用作抗病毒和抗生素。

3. 发明授权

US5175303A Preparation of 7-(diphenylmethyl)oxy-9A-methoxymitosane 失效
标题翻译： 7-（二苯基甲基）氧基-9a-甲氧基甲烷的制备
公开(公告)号：US5175303A
公开(公告)日：1992-12-29
申请号：US766299
申请日：1991-09-27
申请人： Daniel A. Benigni , Kenton L. Shultis , Henry S. L. Wong
发明人： Daniel A. Benigni , Kenton L. Shultis , Henry S. L. Wong
IPC分类号： C07D487/14
CPC分类号： C07D487/14
摘要： 7-(Diphenylmethyl)oxy-9a-methoxymitosane is a novel intermediate for conversion into 7-amino and 7-oxy-9a-methoxymitosanes and is also useful for inhibiting mammalian tumor growth. The compound is prepared by reacting 7-hydroxy-9a-methoxymitosane with diazodiphenylmethane. In a preferred reaction, the compound is prepared from mitomycin C via 7-hydroxy-9a-methoxymitosane without drying (water removal). The intermediate is advantageously converted to the very effective anti-tumor agent 7-[2-(4-nitrophenyldithio) ethylamino]-9a-methoxymitosane in unexpectedly high yields using a two step process where the first step constitutes conversion to 7-[2-(2-pyridyldithio) ethylamino]-9a-methoxymitosane. or 7-[2-(3-nitro-2-pyridyldithio)ethylamino]-9a-methoxymitosane.
摘要翻译： 7-（二苯基甲基）氧基-9a-甲氧基甲烷是用于转化为7-氨基和7-氧-9a-甲氧基
二烷硅烷的新型中间体，也可用于抑制哺乳动物肿瘤生长。该化合物通过使7-羟基-9a-甲氧基甲烷与重氮二苯基甲烷反应来制备。在优选的反应中，化合物由丝裂霉素C通过7-羟基-9a-甲氧基甲烷不经干燥（除水）制备。有利地使用两步法将中间体转化为非常有效的抗肿瘤剂7- [2-（4-硝基苯基二硫代）乙基氨基] -9a-甲氧基甲硅烷，其中第一步构成转化为7- [2- （2-吡啶基二硫代）乙基氨基] -9a-甲氧基甲烷。或7- [2-（3-硝基-2-吡啶基二硫代）乙基氨基] -9a-甲氧基甲烷烷。

4. 发明授权

US5075454A 7-(diphenylmethyl)oxy-9a-methoxymitosane 失效
标题翻译： 7-（二苯基甲基）氧基-9-甲氧基木糖苷
公开(公告)号：US5075454A
公开(公告)日：1991-12-24
申请号：US491380
申请日：1990-03-08
申请人： Daniel A. Benigni , Kenton L. Shultis , Henry S. L. Wong
发明人： Daniel A. Benigni , Kenton L. Shultis , Henry S. L. Wong
IPC分类号： A61K31/40 , A61K31/00 , A61K31/407 , A61P35/00 , C07D487/14
CPC分类号： C07D487/14
摘要： 7-(Diphenylmethyl)oxy-9a-methoxymitosane is a novel intermediate for conversion into 7-amino and 7-oxy-9a-methoxymitosanes and is also useful for inhibiting mammalian tumor growth. The compound is prepared by reacting 7-hydroxy-9a-methoxymitosane with diazodiphenylmethane. In a preferred reaction, the compound is prepared from mitomycin C via 7-hydroxy-9a-methoxymitosane without drying (water removal). The intermediate is advantageously converted to the very effective anti-tumor agent 7-[2-(4-nitrophenyldithio)ethylamino]-9a-methoxymitosane in unexpectedly high yields using a two step process where the first step constitutes conversion to 7-[2-(2-pyridyldithio)ethylamino]-9a-methoxymitosane or 7-[2-(3-nitro-2-pyridyldithio)ethylamino]-9a-methoxymitosane.

5. 发明授权

US07241899B2 Methods for the preparation, isolation and purification of epothilone B, and X-ray crystal structures of epothilone B 有权
标题翻译：埃坡霉素B的制备，分离和纯化方法以及埃坡霉素B的X射线晶体结构
公开(公告)号：US07241899B2
公开(公告)日：2007-07-10
申请号：US10805724
申请日：2004-03-22
申请人： Daniel A. Benigni , Jack Z. Gougoutas , John D. DiMarco
发明人： Daniel A. Benigni , Jack Z. Gougoutas , John D. DiMarco
IPC分类号： A61K31/724 , C12P17/14 , C07D417/02
CPC分类号： C07D493/04 , C12N1/20 , C12N1/38 , C12P17/181 , C12R1/01
摘要： The present invention relates to improved methods for the production, isolation and purification of epothilone B. These methods include, for example, a fermentation process for the production of epothilone B, isolation via adsorption onto a resin, and subsequent purification.
摘要翻译：本发明涉及埃坡霉素B的生产，分离和纯化的改进方法。这些方法包括例如用于生产埃坡霉素B的发酵方法，通过吸附到树脂上进行分离和随后的纯化。

6. 发明授权

US5352798A Process for preparing dithio-ethylanino 9A-methoxymitosanes 失效
标题翻译：二硫代乙基亚氨基-9a-甲氧基甲烷的制备方法
公开(公告)号：US5352798A
公开(公告)日：1994-10-04
申请号：US945793
申请日：1992-09-16
申请人： Daniel A. Benigni , Kenton L. Shultis
发明人： Daniel A. Benigni , Kenton L. Shultis
IPC分类号： A61K31/40 , A61K31/00 , A61K31/407 , A61P35/00 , C07D487/14
CPC分类号： C07D487/14
摘要： 7-(Diphenylmethyl)oxy-9a-methoxymitosane is a novel intermediate for conversion into 7-amino and 7-oxy-9a-methoxymitosanes and is also useful for inhibiting mammalian tumor growth. The compound is prepared by reacting 7-hydroxy-9a-methoxymitosane with diazodiphenylmethane. In a preferred reaction, the compound is prepared from mitomycin C via 7-hydroxy-9a-methoxymitosane without drying (water removal). The intermediate is advantageously converted to the very effective anti-tumor agent 7-[2-(4-nitrophenyldithio)ethylamino]-9a-methoxymitosane in unexpectedly high yields using a two step process where the first step constitutes conversion to 7-[2-(2-pyridyldithio)ethylamino]-9a-methoxymitosane or 7-[2-(3-nitro-2-pyridyldithio)ethylamino]-9a-methoxymitosane.
摘要翻译： 7-（二苯基甲基）氧基-9a-甲氧基甲烷是用于转化为7-氨基和7-氧-9a-甲氧基
二烷硅烷的新型中间体，也可用于抑制哺乳动物肿瘤生长。该化合物通过使7-羟基-9a-甲氧基甲烷与重氮二苯基甲烷反应来制备。在优选的反应中，化合物由丝裂霉素C通过7-羟基-9a-甲氧基甲烷不经干燥（除水）制备。有利地使用两步法将中间体转化为非常有效的抗肿瘤剂7- [2-（4-硝基苯基二硫代）乙基氨基] -9a-甲氧基甲硅烷，其中第一步构成转化为7- [2- （2-吡啶基二硫代）乙基氨基] -9a-甲氧基甲烷或7- [2-（3-硝基-2-吡啶基二硫代）乙基氨基] -9a-甲氧基甲烷烷。

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