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1. 发明授权

US06734187B1 Purine derivatives and medicaments comprising the same as active ingredient 失效
标题翻译：嘌呤衍生物和包含与活性成分相同的药物
公开(公告)号：US06734187B1
公开(公告)日：2004-05-11
申请号：US10200576
申请日：2002-07-23
申请人： Toshihiko Tanaka , Eiichirou Iwashita , Akiko Tarao , Akira Amenomori , Yuya Ono
发明人： Toshihiko Tanaka , Eiichirou Iwashita , Akiko Tarao , Akira Amenomori , Yuya Ono
IPC分类号： C07D47332
CPC分类号： C07D473/30
摘要： Purine derivatives represented by the following formula and salts thereof: wherein R1 represents a C1-C4 alkyl group or difluoromethyl group; R2 represents tetrahydrofuranyl group, a C1-C7 alkyl group and the like; X represents hydrogen atom, a halogen atom or nitro group; and A represents a group represented by the following formula: wherein R3 represents hydrogen atom, a halogen atom and the like; R4 and R5 represent hydrogen atom, a halogen atom, a C1-C4 alkyl group, a C1-C4 alkoxyl group and the like, which are useful as active ingredients of medicaments such as antiasthmatic agents.
摘要翻译：由下式表示的嘌呤衍生物及其盐：其中R 1表示C1-C4烷基或二氟甲基; R 2表示四氢呋喃基，C 1 -C 7烷基等; X表示氢原子，卤素原子或硝基; A表示由下式表示的基团：其中R 3表示氢原子，卤素原子等; R 4和R 5表示氢原子，卤素原子，C 1 -C 4烷基，C 1 -C 4烷氧基等，其可用作药物如抗哮喘药的活性成分。

2. 发明授权

US06437125B1 Process for the production of purine derivatives 有权
标题翻译：嘌呤衍生物生产工艺
公开(公告)号：US06437125B1
公开(公告)日：2002-08-20
申请号：US09623700
申请日：2000-11-01
申请人： Graham Richard Geen , Andrew Colin Share
发明人： Graham Richard Geen , Andrew Colin Share
IPC分类号： C07D47332
CPC分类号： C07D473/40 , C07D473/32
摘要： The invention provides a method of rearranging a compound of formula (I), wherein R and R′ are selected independently from hydrogen and C1-12alkyl; and R1 and R2 are selected independently from hydrogen, hydroxy, halo, C1-12alkyl- or aryl carbonate, amino, mono- or di-C1-12alkylamino, C1-12alkyl or arylamido, C1-12alkyl- or arylcarbonyl, C1-12alkyl- or arylcarboxy, C1-12alkyl- or arylcarbamoyl, C1-12alkyl, C2-12alkenyl, C2-12alkynyl, aryl, heteroaryl, C1-12alkoxy, aryloxy, azido, C1-12alkyl- or arylthio, C1-12alkyl- or arylsulfonyl, C1-12alkyl- or arylsilyl, C1-12alkyl- or arylphosphoryl, and phosphato; to form a compound of formula (II), wherein R, R′, R1 and R2 are as defined for formula (I); said method comprising treating the compound of formula (I) with a palladium (0) catalyst and a (diphenylphosphino)nC1-6 alkane, wherein n is an integer of 1-6. The invention also provides methods of R making penciclovir and famciclovir using this rearrangement reaction.
摘要翻译：本发明提供了一种重排式（I）化合物的方法，其中R和R'独立地选自氢和C 1-12烷基; R 1和R 2独立地选自氢，羟基，卤素，C 1-12烷基 - 或芳基碳酸酯，氨基，单或二-C 1-12烷基氨基，C 1-12烷基或芳基酰氨基，C 1-12烷基 - 或芳基羰基，或芳基羧基，C 1-12烷基或芳基氨基甲酰基，C 1-12烷基，C 12-12烯基，C 12-12炔基，芳基，杂芳基，C 1-12烷氧基，芳氧基，叠氮基，C 1-12烷基 - 或芳硫基，C 1-12烷基 - 或芳基磺酰基， C 1-6烷基 - 或芳基磷酰基和磷酸酯; 形成式（II）化合物，其中R，R'，R 1和R 2如式（I）所定义; 所述方法包括用钯（0）催化剂和（二苯基膦基）nC1-6烷烃处理式（I）化合物，其中n为1-6的整数。本发明还提供使用这种重排反应制备喷昔洛韦和泛昔洛韦的方法。

3. 发明授权

US06172224B2 Process for isolating 2-amino-6-chloro-9-[(1'S,2'R)-1'2'-bis(hydroxymethyl)-cyclopropane-1'-YL]methylpurine and an optical isomer thereof 有权
标题翻译：分离2-氨基-6-氯-9 - [（1'S，2'R）-1'2'-双（羟甲基） - 环丙烷-1'-YL]甲基嘌呤及其旋光异构体的方法
公开(公告)号：US06172224B2
公开(公告)日：2001-01-09
申请号：US09263999
申请日：1999-03-08
申请人： Noriyasu Kataoka , Toshihiro Matsuzawa , Masanobu Yatagai
发明人： Noriyasu Kataoka , Toshihiro Matsuzawa , Masanobu Yatagai
IPC分类号： C07D47332
CPC分类号： C07D473/00
摘要： A process for purifying 2-amino-6-chloro-9-[(1′S,2′R)-1′,2′-bis(hydroxymethyl) cycdopropane-1′-yl]methylpurine represented by the following formula (5) comprises the step of selectively isolating 2-amino-6-chloro-9-[(1′S,2′R)-1′,2′-bis(hydroxymethyl) cyclopropane-1′-yl]methylpurine from a mixture of 2-amino-6-chloro-9-[(1′S,2′R)-1′,2′-bis(hydroxymethyl)cyclopropane-1′-yl]methylpurine and 2-amino-6-chloro-7-[(1′S,2′R)-1′,2′-bis(hydroxymethyl)cyclopropane-1′-yl]methylpurine represented by the following formula (6) by the crystallization. This process has a satisfactory medicinal quality on an industrial scale without necessitating complicated operations such as chromatographic purification.
摘要翻译：用于纯化由下式（5）表示的2-氨基-6-氯-9 - [（1'S，2'R）-1'，2'-双（羟甲基）环丙烷-1'-基]甲基嘌呤的方法包括从2-氨基-6-氯-9 - [（1'S，2'R）-1'，2'-双（羟甲基）环丙烷-1'-基]甲基嘌呤的2-氨基-6- 6-氯-9 - [（1'S，2'R）-1'，2'-双（羟甲基）环丙烷-1'-基]甲基嘌呤和2-氨基-6-氯-7 - [（1'S，2' R）-1'，2'-双（羟甲基）环丙烷-1'-基]甲基嘌呤通过结晶表示。该方法在工业规模上具有令人满意的药用质量，而不需要色谱纯化等复杂操作。

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