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1. 发明授权

US07193081B2 Process for preparation of cyclic prodrugs of PMEA and PMPA 有权
标题翻译：制备PMEA和PMPA的环状前药的方法
公开(公告)号：US07193081B2
公开(公告)日：2007-03-20
申请号：US10436799
申请日：2003-05-12
申请人： Joseph J. Kopcho , K. Raja Reddy , Michael C. Matelich , Bheemarao G. Ugarkar
发明人： Joseph J. Kopcho , K. Raja Reddy , Michael C. Matelich , Bheemarao G. Ugarkar
IPC分类号： C07F9/6574
CPC分类号： C07F9/657181
摘要： The method of preparing compounds of Formula I is described: wherein: M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, and (R)-9-(2-phosphonylmethoxypropyl)adenine; wherein V is phenyl, optionally substituted with 1–2 substituents selected from a group consisting of fluoro, chloro, and bromo; comprising: coupling a chiral 1-phenylpropane-1,3-diol, wherein the phenyl may be optionally substituted, with MPOCl2 or an N-6 substituted analogue thereof. Additionally, methods and salt forms are described that enable isolation and purification of the desired isomer.
摘要翻译：描述了制备式I化合物的方法：其中：M和V彼此是顺式的，MPO 3 H 2是选自以下的膦酸： 9-（2-膦酰基甲氧基乙基）腺嘌呤和（R）-9-（2-膦酰基甲氧基丙基）腺嘌呤; 其中V是苯基，任选被1-2个选自氟，氯和溴的取代基取代; 包括：将其中苯基可以任选取代的手性1-苯基丙烷-1,3-二醇与MPOCl 2 N或其N-6取代的类似物偶联。另外，描述了能够分离和纯化所需异构体的方法和盐形式。

2. 发明授权

US07214668B2 Phosphonic acid based prodrugs of PMEA and its analogues 有权
标题翻译：基于磷酸的前药PMEA及其类似物
公开(公告)号：US07214668B2
公开(公告)日：2007-05-08
申请号：US10436922
申请日：2003-05-12
申请人： K. Raja Reddy , Mark D. Erion , Michael C. Matelich , Joseph J. Kopcho
发明人： K. Raja Reddy , Mark D. Erion , Michael C. Matelich , Joseph J. Kopcho
IPC分类号： C07F9/6574 , A61K31/675 , A61P31/20 , A61P31/14 , A61P35/00
CPC分类号： C07F9/65742 , C07F9/65616
摘要： Prodrugs of Formula I, their uses, their intermediates, and their method of manufacture are described: wherein: M and V are cis to one another and MPO3H2 is a phosphonic acid selected from the group consisting of 9-(2-phosphonylmethoxyethyl)adenine, (R)-9-(2-phosphonylmethoxy propyl)adenine, 9-(2-phosphonylmethoxyethyl)guanine, 9-(2-phosphonylmethoxy ethyloxy)adenine, 9-(2-phosphonylmethoxyethyl)-2,6-diaminopurine, (S)-1-(3-hydroxy-2-phosphonylmethoxypropyl)cytosine, (S)-9-(3-hydroxy-2-phosphonylmethoxypropyl)adenine, 9-(3-hydroxy-2-phosphonylmethoxypropyl)guanine, and (S)-9-(3-fluoro-2-phosphonyl methoxypropyl)adenine; V is selected from a group consisting of phenyl, 2-pyridyl, 3-pyridyl, 4-pyridyl, 2-furanyl, 3-furanyl, 2-thienyl, and 3-thienyl, all optionally substituted with 1-3 substituents selected from a group consisting of F, Cl, Br, C1-C3 alkyl, CF3 and OR6; R6 is selected from the group consisting of C1-C3 alkyl, and CF3; and pharmaceutically acceptable salts thereof.
摘要翻译：描述了式I的前药，其用途及其中间体及其制备方法：其中：M和V彼此是顺式的，MPO 3 H 2是选自9-（2-膦酰基甲氧基乙基）腺嘌呤，（R）-9-（2-膦酰基甲氧基丙基）腺嘌呤，9-（2-膦酰基甲氧基乙基）鸟嘌呤，9-（2-膦酰基甲氧基乙氧基）腺嘌呤， 9-（3-膦酰基甲氧基乙基）-2,6-二氨基嘌呤，（S）-1-（3-羟基-2-膦酰基甲氧基丙基）胞嘧啶，（S）-9-（3-羟基-2-膦酰基甲氧基丙基）腺嘌呤，（3-羟基-2-膦酰基甲氧基丙基）鸟嘌呤和（S）-9-（3-氟-2-膦酰基甲氧基丙基）腺嘌呤; V选自苯基，2-吡啶基，3-吡啶基，4-吡啶基，2-呋喃基，3-呋喃基，2-噻吩基和3-噻吩基，全部任选被1-3个选自由F，Cl，Br，C 1 -C 3烷基，CF 3 3和OR 6构成的基团。 R 6选自C 1 -C 3烷基和CF 3 N; 及其药学上可接受的盐。

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