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1. 发明授权

US6037335A Phosphonate-nucleotide ester derivatives 失效
标题翻译：膦酸酯 - 核苷酸酯衍生物
公开(公告)号：US6037335A
公开(公告)日：2000-03-14
申请号：US942490
申请日：1997-10-02
申请人： Hideaki Takashima , Naoko Inoue , Masaru Ubasawa , Kouichi Sekiya , Shingo Yabuuchi
发明人： Hideaki Takashima , Naoko Inoue , Masaru Ubasawa , Kouichi Sekiya , Shingo Yabuuchi
IPC分类号： C07F9/6561 , A61K31/675 , C07F9/6512
CPC分类号： C07F9/6561 , C07F9/65616
摘要： Phosphonate-nucleotide ester compounds of the formula (I) have excellent antiviral activity and antineoplastic activity. Further, they can be orally administered. ##STR1## wherein ring A represents ##STR2## wherein R.sup.1 and R.sup.2 independently represent hydrogen, halogen, hydroxyl, mercapto, C.sub.6 -C.sub.10 arylthio or amino; R.sup.3 represents C.sub.1 -C.sub.4 alkyl or ethyl having one or more substituents selected from the group consisting of fluorine, C.sub.1 -C.sub.4 alkoxy, phenoxy, C.sub.7 -C.sub.10 phenylalkoxy and C.sub.2 -C.sub.5 acyloxy; R.sup.4 represents ethyl having one or more substituents selected from the group consisting of fluorine, C.sub.1 -C.sub.4 alkoxy, phenoxy, C.sub.7 -C.sub.10 phenylalkoxy and C.sub.2 -C.sub.5 acyloxy; X, Y and Z independently represent methyne or nitrogen atom; or a pharmaceutically acceptable salt thereof.
摘要翻译：式（I）的膦酸酯 - 核苷酸酯化合物具有优异的抗病毒活性和抗肿瘤活性。此外，它们可以口服给药。其中环A表示其中R1和R2独立地表示氢，卤素，羟基，巯基，C6-C10芳硫基或氨基; R 3表示具有一个或多个选自氟，C 1 -C 4烷氧基，苯氧基，C 7 -C 10苯基烷氧基和C 2 -C 5酰氧基的取代基的C 1 -C 4烷基或乙基; R4表示具有一个或多个选自氟，C 1 -C 4烷氧基，苯氧基，C 7 -C 10苯基烷氧基和C 2 -C 5酰氧基的取代基的乙基; X，Y和Z独立地表示甲炔或氮原子; 或其药学上可接受的盐。

2. 发明授权

US06197775B1 Phosphonate nucleotide derivatives 失效
标题翻译：磷酸核苷酸衍生物
公开(公告)号：US06197775B1
公开(公告)日：2001-03-06
申请号：US08973762
申请日：1997-12-11
申请人： Masaru Ubasawa , Hideaki Takashima , Kouichi Sekiya , Naoko Inoue , Satoshi Yuasa , Naohiro Kamiya
发明人： Masaru Ubasawa , Hideaki Takashima , Kouichi Sekiya , Naoko Inoue , Satoshi Yuasa , Naohiro Kamiya
IPC分类号： A01N4390
CPC分类号： C07F9/6561 , C07F9/65616
摘要： A compound represented by the following general formula (I) which has an antiviral activity: wherein R1 represents hydrogen atom, C1-C6 alkyl group, or C7-C10 aralkyl group; R2 represents C1-C6 alkyl group, C7-C10 aralkyl group, or phenyl group; R3 and R4 independently represent hydrogen atom, C1-C6 alkyl group, acyloxymethyl group, acylthioethyl group, or ethyl gorup substituted with at least one halogen atom; R5 represents hydrogen atom, C1-C4 alkyl gorup, C1-C4 hydroxyalkyl group, C1-C4 alkyl group substituted with at least one halogen atom; and X represents carbon atom or nitrogen atom.
摘要翻译：由具有抗病毒活性的以下通式（I）表示的化合物：其中R1表示氢原子，C1-C6烷基或C7-C10芳烷基; R2表示C1-C6烷基，C7-C10芳烷基或苯基; R3和R4独立地表示氢原子，C1-C6烷基，酰氧基甲基，酰基硫代乙基或被至少一个卤素原子取代的乙基; R5代表氢原子，C1-C4烷基羰基，C1-C4羟基烷基，被至少一个卤素原子取代的C1-C4烷基; X表示碳原子或氮原子。

3. 发明授权

US5840716A Phosphonate nucleotide compounds 失效
标题翻译：磷酸核苷酸化合物
公开(公告)号：US5840716A
公开(公告)日：1998-11-24
申请号：US785606
申请日：1997-01-17
申请人： Masaru Ubasawa , Kouichi Sekiya , Hideaki Takashima , Naoko Ueda , Satoshi Yuasa , Naohiro Kamiya
发明人： Masaru Ubasawa , Kouichi Sekiya , Hideaki Takashima , Naoko Ueda , Satoshi Yuasa , Naohiro Kamiya
IPC分类号： C07F9/6561 , A01N57/00 , C07F9/02
CPC分类号： C07F9/6561 , C07F9/65616
摘要： A phosphonate nucleotide compound having antiviral activity and is useful for an orally available and highly safe antiviral agent, which is represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, a C.sub.1 -C.sub.6 alkoxy, a halogen-substituted C.sub.1 -C.sub.4 alkoxy, halogen, amino, or nitro; R.sup.2 and R.sup.3 independently represent hydrogen, a C.sub.1 -C.sub.22 alkyl, an acyloxymethy, an acylthioethyl, or a halogen-substituted ethyl; R.sup.4 represents hydrogen, a C.sub.1 -C.sub.4 alkyl, a C.sub.1 -C.sub.4 hydroxyalkyl, or a halogen-substituted C.sub.1 -C.sub.4 alkyl; and X represents carbon or nitrogen.
摘要翻译：具有抗病毒活性的膦酸酯核苷酸化合物，可用于口服可用和高度安全的抗病毒剂，其由下式（I）表示：其中R 1表示氢，C 1 -C 6烷氧基，卤素取代的C 1 -C 4烷氧基，卤素，氨基或硝基; R2和R3独立地表示氢，C1-C22烷基，酰氧基甲基，酰基硫代乙基或卤素取代的乙基; R4表示氢，C1-C4烷基，C1-C4羟基烷基或卤素取代的C1-C4烷基; X表示碳或氮。

4. 发明授权

US06194398B1 Phosphonate nucleotide compound 失效
标题翻译：磷酸核苷酸化合物
公开(公告)号：US06194398B1
公开(公告)日：2001-02-27
申请号：US09242111
申请日：1999-06-17
申请人： Masaru Ubasawa , Kouichi Sekiya , Hideaki Takashima , Naoko Ueda , Satoshi Yuasa , Naohiro Kamiya
发明人： Masaru Ubasawa , Kouichi Sekiya , Hideaki Takashima , Naoko Ueda , Satoshi Yuasa , Naohiro Kamiya
IPC分类号： C07D47324
CPC分类号： C07F9/6561 , C07F9/65616
摘要： A phosphonate nucleotide compound represented by formula (I): (wherein R1 is a C1-C6 alkyl group or the like, R2 is a hydrogen atom, a C1-C4 alkyl group substituted by one or more halogen atoms or the like, R3 is a hydrogen atom, a C1-C4 alkyl group substituted by one or more halogen atoms or the like, R4 is a hydrogen atom, a C1-C4 alkyl group substituted by one or more halogen atoms and X is a carbon atom or a nitrogen atom), a salt thereof, a hydrate thereof or a solvate thereof, as well as a medicament containing the same. It is useful as an antiviral agent for human immunodeficiency virus, herpes simplex virus, hepatitis B virus or the like and as an antitumor agent.
摘要翻译：由式（I）表示的膦酸酯核苷酸化合物:(其中R1是C1-C6烷基等，R2是氢原子，被一个或多个卤素原子取代的C1-C4烷基等，R3是氢原子，被一个或多个卤素原子等取代的C 1 -C 4烷基，R 4是氢原子，被一个或多个卤素原子取代的C 1 -C 4烷基，X是碳原子或氮原子），其盐，其水合物或其溶剂合物，以及含有它们的药物。作为人体免疫缺陷病毒，单纯疱疹病毒，乙型肝炎病毒等的抗病毒剂，作为抗肿瘤剂是有用的。

5. 发明授权

US06767900B2 Phosphonate nucleotide compound 失效
标题翻译：磷酸核苷酸化合物
公开(公告)号：US06767900B2
公开(公告)日：2004-07-27
申请号：US10220126
申请日：2002-11-04
申请人： Masaru Ubasawa , Kouichi Sekiya
发明人： Masaru Ubasawa , Kouichi Sekiya
IPC分类号： C07F96561
CPC分类号： A61K31/675 , A61K31/685 , C07F9/6561 , C07F9/65616
摘要： A phosphonate nucleotide compound represented by the following formula (I) or a salt thereof, or a hydrate or solvate thereof: wherein, R1 is a hydroxyl group; each of R2 and R3 is independently a hydrogen atom, a C1-C22 alkyl group, an alkanoyloxymethyl group, an alkanoylthioethyl group, or an ethyl group substituted by one or more halogen atoms; R4 is a hydrogen atom, a C1-C4 alkyl group, a C1-C4 hydroxyalkyl group, or a C1-C4 alkyl group substituted by one or more halogen atoms; and X is CH or a nitrogen atom.

6. 再颁专利

USRE37979E1 Pyrimidine derivatives and anti-viral agent containing the same as active ingredient thereof 失效
标题翻译：嘧啶衍生物和含有其活性成分的抗病毒剂
公开(公告)号：USRE37979E1
公开(公告)日：2003-02-04
申请号：US08957358
申请日：1997-10-23
申请人： Tadashi Miyasaka , Hiromichi Tanaka , Erik Desiré DeClercq , Masanori Baba , Richard Thomas Walker , Masaru Ubasawa
发明人： Tadashi Miyasaka , Hiromichi Tanaka , Erik Desiré DeClercq , Masanori Baba , Richard Thomas Walker , Masaru Ubasawa
IPC分类号： A61K31505
CPC分类号： C07D239/47 , C07D239/54 , C07D239/545 , C07D239/56 , C07D239/58 , C07D239/60
摘要： The disclosure concerns pyrimidine derivatives represented by the following general formulas [I] and [I′] and having antiviral activity, particularly antiretroviral activity such as anti-HIV activity: and pharmaceutical compositions having antiviral activity and comprising the above-described derivative(s) as an active ingredient.
摘要翻译：本发明涉及由以下通式[I]和[I']表示并具有抗病毒活性的特别是抗病毒活性如抗HIV活性的嘧啶衍生物：和具有抗病毒活性并含有上述衍生物的药物组合物，作为活性成分。

7. 发明授权

US5112835A 6-substituted acyclopyrimidine nucleoside derivatives and antiviral agents containing the same as active ingredient thereof 失效
标题翻译： 6-取代的环丙基嘧啶核苷衍生物和含有它的活性成分的抗病毒剂
公开(公告)号：US5112835A
公开(公告)日：1992-05-12
申请号：US449930
申请日：1989-11-21
申请人： Tadashi Miyasaka , Hiromichi Tanaka , Erik D. A. De Clercq , Masanori Baba , Richard T. Walker , Masaru Ubasawa
发明人： Tadashi Miyasaka , Hiromichi Tanaka , Erik D. A. De Clercq , Masanori Baba , Richard T. Walker , Masaru Ubasawa
IPC分类号： C07D239/54 , C07D239/60
CPC分类号： C07D239/54 , C07D239/60
摘要： 6-substitutted acyclopyrimidine nucleoside derivatives represented by the following general formula I: ##STR1## wherein R.sup.1 represents a hydrogen or halogen atom or a group of alkyl, alkenyl, alkynyl, alkylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylthio or aralkyl; R.sup.2 represents a group of arylthio, alkylthio, cycloalkylthio, aryl sulfoxide, alkyl sulfoxide, cycloalkyl sulfoxide, alkenyl, alkynyl, aralkyl, arylcarbonyl, arylcarbonylalkyl or aryloxy; R.sup.3 represents a hydroxyalkyl group of which alkyl portion may contain an oxygen atom; X represents an oxygen or sulfur atom or amino group; Y represents an oxygen or sulfur atom; and A represents .dbd.N-- or --NH-- or pharmaceutically acceptable salts thereof, processes for their preparation and antiviral agents containing them as active ingredients.
摘要翻译： PCT No.PCT / JP89 / 00347 Sec。 371日期：一九八九年十一月二十一日 102（e）1989年11月21日PCT PCT 1989年3月31日PCT公布。出版物WO89 / 09213 日期：1989年10月5日，由以下通式I表示的6-取代的阿卡吡啶核苷衍生物：其中R 1表示氢或卤原子或烷基，烯基，炔基，烷基羰基，芳基羰基，芳基羰基烷基，芳硫基或芳烷基 ; R2代表芳硫基，烷硫基，环烷硫基，芳基亚砜，烷基亚砜，环烷基亚砜，烯基，炔基，芳烷基，芳基羰基，芳基羰基烷基或芳氧基; R3表示烷基部分可含有氧原子的羟烷基; X表示氧或硫原子或氨基; Y表示氧或硫原子; 并且A表示= N-或-NH-或其药学上可接受的盐，其制备方法和含有它们作为活性成分的抗病毒剂。

8. 发明授权

US5604209A Synergistic antiviral compositions 失效
标题翻译：协同抗病毒组合物
公开(公告)号：US5604209A
公开(公告)日：1997-02-18
申请号：US253274
申请日：1994-06-02
申请人： Masaru Ubasawa , Satoshi Yuasa
发明人： Masaru Ubasawa , Satoshi Yuasa
IPC分类号： A61K31/505 , A61K31/52 , A61K31/66 , A61K31/70 , A61P31/12 , A61P31/18
CPC分类号： A61K31/70 , Y10S514/885
摘要： Antiviral agents which comprises as active ingredients one or more 2',3'-dideoxyribonucleosides or phosphoric esters thereof and 6-benzyl-1-ethoxymethyl-5-substituted uracil derivative of the formula (I): ##STR1## wherein X is oxygen or sulfur atom; R.sup.1 is ethyl or isopropyl; R.sup.2 and R.sup.3 are independently hydrogen atom, C.sub.1 -C.sub.3 alkyl or halogen atom, which compounds can inhibit HIV reverse transcriptase through different mechanisms and are synergistic in combination.
摘要翻译：包含作为活性成分的一种或多种2'，3'-脱氧核糖核苷或其磷酸酯和式（I）的6-苄基-1-乙氧基甲基-5-取代的尿嘧啶衍生物的抗病毒剂：其中X 是氧或硫原子; R1是乙基或异丙基; R2和R3独立地是氢原子，C1-C3烷基或卤原子，这些化合物可以通过不同的机理抑制HIV逆转录酶，并且是组合的协同作用。

9. 发明授权

US5318972A Pyrimidine nucleoside derivative and antiviral agent containing the derivative as active ingredient 失效
标题翻译：嘧啶核苷衍生物和含有该衍生物作为活性成分的抗病毒剂
公开(公告)号：US5318972A
公开(公告)日：1994-06-07
申请号：US676912
申请日：1991-03-28
申请人： Tadashi Miyasaka , Hiromichi Tanaka , Erik D. A. De Clercq , Masanori Baba , Richard T. Walker , Masaru Ubasawa
发明人： Tadashi Miyasaka , Hiromichi Tanaka , Erik D. A. De Clercq , Masanori Baba , Richard T. Walker , Masaru Ubasawa
IPC分类号： C07D239/54 , C07D239/56 , C07D239/58 , C07D239/60 , A61K31/505 , C07D239/10
CPC分类号： C07D239/54 , C07D239/56 , C07D239/58 , C07D239/60
摘要： A pyrimidine nucleoside derivative and pharmaceutically acceptable salt thereof specified by the presence of ethyl group or isopropyl group at 5-position of the pyrimidine ring and the presence of a (substituted) phenylthio or a (substituted) benzyl group at 6-position of the pyrimidine ring is provided. The pyrimidine nucleoside derivative and pharmaceutically acceptable salt thereof show a markedly higher anti-retroviral activity than conventional analogous compounds and have a relatively low toxicity against the host cells, and therefore, are useful as an active ingredient of antiviral agent.
摘要翻译：嘧啶核苷衍生物及其药学上可接受的盐，其特征在于在嘧啶环的5-位存在乙基或异丙基，以及在嘧啶的6位存在（取代的）苯硫基或（取代的）苄基提供戒指。嘧啶核苷衍生物及其药学上可接受的盐显示比常规类似化合物显着更高的抗逆转录病毒活性，并且对宿主细胞具有相对低的毒性，因此可用作抗病毒剂的活性成分。

10. 发明授权

US5461060A Pyrimidine derivatives and anti-viral agent containing the same as active ingredient thereof 失效
标题翻译：嘧啶衍生物和含有其活性成分的抗病毒剂
公开(公告)号：US5461060A
公开(公告)日：1995-10-24
申请号：US222071
申请日：1993-09-03
申请人： Tadashi Miyasaka , Hiromichi Tanaka , Erik D. A. De Clercq , Masanori Baba , Richard T. Walker , Masaru Ubasawa
发明人： Tadashi Miyasaka , Hiromichi Tanaka , Erik D. A. De Clercq , Masanori Baba , Richard T. Walker , Masaru Ubasawa
IPC分类号： C07D239/46 , C07D239/54 , C07D239/545 , C07D239/56 , C07D239/58 , C07D239/60 , A61K31/505 , C07D239/02
CPC分类号： C07D239/47 , C07D239/54 , C07D239/545 , C07D239/56 , C07D239/58 , C07D239/60
摘要： The disclosure concerns pyrimidine derivatives represented by the following general formulas [I] and [I'] and having antiviral activity, particularly antiretroviral activity such as anti-HIV activity: ##STR1## and pharmaceutical compositions having antiviral activity and comprising the above-described derivative(s) as an active ingredient.
摘要翻译：本公开涉及由以下通式[I]和[I']表示的具有抗病毒活性的特异性抗转录病毒活性如抗HIV活性：抗病毒活性并包含上述衍生物作为活性的嘧啶衍生物成分。

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