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1. 发明授权

US06600044B2 Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers 失效
标题翻译：从所需的反式异构体中回收所需的顺式-1,3-氧硫杂环戊烷核苷的方法
公开(公告)号：US06600044B2
公开(公告)日：2003-07-29
申请号：US09881705
申请日：2001-06-18
申请人： K. S. Keshava Murthy , Gurijala V. Reddy , Zhi-xian Wang , Chandrawansha B. W. Senanayake
发明人： K. S. Keshava Murthy , Gurijala V. Reddy , Zhi-xian Wang , Chandrawansha B. W. Senanayake
IPC分类号： C07D41104
CPC分类号： C07D411/04
摘要： A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof, comprising: (i) treatment of the cis-/trans-1,3-oxathiolane nucleosides (or protected derivatives thereof) with a pyrimidine base (or it derivatives thereof) and an acid, (ii) adding a suitable acid to the obtained cis-/trans-mixture of isomers, (iii) selective crystallization of the desired cis-isomer salt from a solvent or combination of solvents, and (iv) treatment of the predominantly cis-isomer salt with a suitable base to offer the free 1,3-oxathiolane nucleosides, and thereafter optionally repeating steps (i) to (iv) inclusive.
摘要翻译：从顺式 - 反式-1,3-氧硫杂环戊烷核苷或其受保护的衍生物的混合物制备主要为顺式的1,3-氧硫杂环戊烷核苷类似物的方法，包括：（i）（或其衍生物）和酸，（ii）向得到的异构体的顺式 - 反式混合物中加入合适的酸，（iii）反式-1,3-氧硫杂环戊烷核苷（或其保护的衍生物）与嘧啶碱）从溶剂或溶剂组合中选择性结晶所需的顺式异构体盐，和（iv）用合适的碱处理主要为顺式异构体盐以提供游离的1,3-氧硫杂环戊烷核苷，然后任选重复步骤（i）至（iv）包括在内。

2. 发明授权

US06541631B1 Methods of separating FTC isomers and derivatives thereof 有权
标题翻译：分离FTC异构体及其衍生物的方法
公开(公告)号：US06541631B1
公开(公告)日：2003-04-01
申请号：US09579796
申请日：2000-05-26
申请人： Salah Zahr , David A. Swanson , Adel M. Moussa , Luning Han
发明人： Salah Zahr , David A. Swanson , Adel M. Moussa , Luning Han
IPC分类号： C07D41104
CPC分类号： C07D411/04 , B01D15/185 , B01D15/3833 , Y02P20/55
摘要： The present invention relates to a method of preparing enantiomers and diastereomers of a 2′,3′-dideoxy-5-fluoro-3′thiocytadine (FTC) or a derivative thereof as represented by the following structural formula: In Structural Formula I, R is H, a substituted or unsubstituted organic acid radical, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted heteroaralkyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted heterocycloalkyl group, a substituted or unsubstituted cycloalkylalkyl, a substituted or unsubstituted heterocycloalkylalkyl, a sugar or a protecting group.
摘要翻译：本发明涉及如下结构式所示的制备2'，3'-二脱氧-5-氟-3'-硫代胞嘧啶（FTC）或其衍生物的对映异构体和非对映体的方法：在结构式I中，R 是取代或未取代的有机酸基，取代或未取代的烷基，取代或未取代的芳基，取代或未取代的杂芳基，取代或未取代的芳烷基，取代或未取代的杂芳烷基，取代或未取代的取代或未取代的杂环烷基，取代或未取代的环烷基烷基，取代或未取代的杂环烷基烷基，糖或保护基。

3. 发明授权

US06831174B2 Processes for preparing substituted 1, 3-oxathiolanes with antiviral properties 失效
标题翻译：制备具有抗病毒性能的取代1,3-氧硫杂环戊烷的方法
公开(公告)号：US06831174B2
公开(公告)日：2004-12-14
申请号：US09760380
申请日：2001-01-16
申请人： Bernard Belleau , Tarek Mansour , Allan Tse , Colleen A. Evans , Haolun Jin , Boulos Zacharie , Nghe Nguyen-Ba
发明人： Bernard Belleau , Tarek Mansour , Allan Tse , Colleen A. Evans , Haolun Jin , Boulos Zacharie , Nghe Nguyen-Ba
IPC分类号： C07D41104
CPC分类号： C07D327/04 , C07D405/04 , C07D411/04 , C07D411/14 , C07D473/00 , C07D473/40
摘要： Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: wherein R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S═O or SO2. The invention also relates to intermediates of use in the preparation of these compounds.
摘要翻译：公开了制备式（I）化合物及其药学上可接受的盐或酯的方法：其中R2是嘌呤或嘧啶碱基或其类似物或衍生物; Z为S，S = O或SO 2。本发明还涉及用于制备这些化合物的中间体。

4. 发明授权

US06723728B2 Polymorphic and other crystalline forms cis-FTC 有权
标题翻译：多形态和其他结晶形式的顺式FTC
公开(公告)号：US06723728B2
公开(公告)日：2004-04-20
申请号：US10086830
申请日：2002-03-01
申请人： Yuerong Hu , Devalina Law , Kenneth R. Phares
发明人： Yuerong Hu , Devalina Law , Kenneth R. Phares
IPC分类号： C07D41104
CPC分类号： C07D411/04
摘要： Solid phases of (−)-cis-FTC, which are designated herein as amorphous (−)-FTC and Forms II and III (−)-cis-FTC) are provided that can be distinguished from Form I (−)-cis-FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. A hydrated crystalline form of (±)-cis-FTC (i.e. racemic cis-FTC), and a dehydrated form of the hydrate, are also provided, and can similarly be distinguished from other forms of FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These FTC forms can be used in the manufacture of other forms of FTC, or in pharmaceutical compositions. Particularly preferred uses of these forms are in the treatment of HIV or hepatitis B.
摘要翻译：提供了本文中称为无定形（ - ） - FTC和形式II和III（ - ） - 顺式 - FTC）的（ - ） - 顺式 - FTC的固相，其可以与I型（ - ） - 顺式 - FTC通过X射线粉末衍射图，热性能和制造方法。还提供了（±）-cis-FTC（即外消旋顺式FTC）的水合结晶形式和水合物的脱水形式，并且可以类似地通过X射线粉末衍射图与其它形式的FTC区分开，热性能和制造方法。这些FTC形式可用于制造其他形式的FTC或药物组合物。这些形式的特别优选的用途是治疗HIV或乙型肝炎。

5. 发明授权

US06518425B1 Method of manufacture of 1,3-oxathiolane nucleosides 有权
公开(公告)号：US06518425B1
公开(公告)日：2003-02-11
申请号：US09570885
申请日：2000-05-15
申请人： George R. Painter , Dennis C. Liotta , Merrick R. Almond , Darryl G. Cleary , Josè D. Soria , Marcos Sznaidman
发明人： George R. Painter , Dennis C. Liotta , Merrick R. Almond , Darryl G. Cleary , Josè D. Soria , Marcos Sznaidman
IPC分类号： C07D41104
CPC分类号： C07D473/00 , C07D327/04 , C07D411/04
摘要： Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.

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