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1. 发明授权

EP0420763B1 6-Substituted acyclopyrimidine nucleoside derivatives and antiviral agent containing the same as active ingredient thereof 失效
标题翻译： 6-取代嘧啶核苷和非环含有它们作为活性成分的抗病毒剂衍生物
公开(公告)号：EP0420763B1
公开(公告)日：1999-07-28
申请号：EP90402693.7
申请日：1990-09-28
申请人： Mitsubishi Chemical Corporation
发明人： Miyasaka, Tadashi , Tanaka, Hiromichi , De Clercq, Erik Desire Alice , Baba, Masanori , Walker, Richard Thomas , Ubasawa, Masaru
IPC分类号： C07D239/60 , C07D239/54 , C07D239/56 , C07D239/47 , A61K31/505
CPC分类号： C07D239/47 , C07D239/54 , C07D239/545 , C07D239/56 , C07D239/58 , C07D239/60

2. 发明公开

EP0420763A2 6-Substituted acyclopyrimidine nucleoside derivatives and antiviral agent containing the same as active ingredient thereof 失效
标题翻译： 6-取代嘧啶核苷和非环含有它们作为活性成分的抗病毒剂的衍生物。
公开(公告)号：EP0420763A2
公开(公告)日：1991-04-03
申请号：EP90402693.7
申请日：1990-09-28
申请人： Mitsubishi Chemical Corporation
发明人： Miyasaka, Tadashi , Tanaka, Hiromichi , De Clercq, Erik Desire Alice , Baba, Masanori , Walker, Richard Thomas , Ubasawa, Masaru
IPC分类号： C07D239/60 , C07D239/54 , C07D239/56 , C07D239/47 , A61K31/505
CPC分类号： C07D239/47 , C07D239/54 , C07D239/545 , C07D239/56 , C07D239/58 , C07D239/60
摘要： 6-substituted acyclopyrimidine nucleoside derivative represented by the following general formula I or I';
wherein R 1 represents a hydrogen atom, halogen atom, alkyl, cycloalkyl, alkenyl, alkynyl, alkylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylthio or aralkyl group; R 2 represents an arylthio, alkylthio, cycloalkylthio, arylsulfinyl, alkylsulfinyl, cycloalkylsulfinyl, alkenyl, alkynyl, aralkyl, arylcarbonyl, arylcarbonylalkyl or aryloxy group, those groups optionally substituted by one or more of substituents selected from a haloger atom, alkyl, halogenated alkyl, alkoxy, hydroxyl, nitro, amino, cyano and acyl groups;

R 3 represents a hydrogen atom, methyl, branched alkyl or -CH 2 -Z-(CH 2 ) n -R 5 group where R 5 represents a hydrogen atom, halogen atom, hydroxyl, heterocyclic carbonyloxy, formyloxy, alkylcarbonyloxy, cycloalkylcarbonyloxy, aralkylcarbonyloxy, arylcarbonyloxy, azido, alkoxycarbonyloxy, N-alkylcarbamoyloxy, N-arylcarbamoyloxy, N-alkylthiocarbamoyloxy, N-arylthiocarbamoyloxy, alkoxy, aralkyloxy, branched alkyl, cycloalkyl or aryl group, the alkoxycarbonyloxy to aryl groups mentioned above as R 5 optionally substituted by one or more substituents selected from a halogen atom, aryl, alkyl, alkoxy and halogenated alkyl groups, Z represents an oxygen, sulfur atom or methylene group, and n represents 0 or an integer of 1 to 5,
R4- represents a hydrogen atom, alkyl or aralkyl group,
X represents an oxygen or sulfur atom,
Y represents an oxygen or sulfur atom,
provided that when R 4 and Z represent a hydrogen atom and oxygen atom respectively in the formula I R 5 does not represent a hydroxyl group,

or a pharmaceutically acceptable salt thereof, and an antiviral agent containing the derivative or the salt thereof as an active ingredient.
摘要翻译： 6-取代acyclopyrimidine核苷衍生物由以下通式I或I MIN代表的; 其中，R <1>代表氢原子，卤素原子，烷基，环烷基，烯基，炔基，烷基羰基，芳基羰基，芳基羰基，芳硫基或芳烷基; [R <2> darstellt由一个或多个从一个haloger原子的取代基的对芳硫基，烷硫基，环烷硫基，芳基亚磺酰基，烷基亚磺酰基，环烷，烯基，炔基，芳烷基，芳基羰基，芳基羰基或芳氧基，这些基团可任意substituiertem，烷基，卤代烷基，烷氧基，羟基，硝基，氨基，氰基和酰基; [R <3>代表氢原子，甲基，支链烷基或-CH 2 -Z-（CH 2）NR <5>团，其中R <5>代表氢原子，卤原子，羟基，杂环基羰氧基，甲酰氧基，烷基羰基氧基，环烷基羰，芳烷基羰氧基，芳基羰基，叠氮基，烷氧基羰氧基，N-烷基氨基甲酰氧基，N-芳，N- alkylthiocarbamoyloxy，N- arylthiocarbamoyloxy，烷氧基，芳烷氧基，支化烷基，环烷基或芳基，烷氧基羰上述为R的芳基<5> OPTIONALLY 被选自卤原子，芳基，烷基，烷氧基和卤代烷基，氧，硫原子或亚甲基的ždarstellt选择的一个或多个取代基取代，并且n darstellt 0或1整数5 substituiertem，R <4> darstellt 氢原子，烷基或芳烷基，X darstellt到氧或硫原子，Y darstellt于氧或硫原子，条件做当R <4>和Z式中分别代表氢原子和氧原子的IR <5>确实不代表水电 XYL基，或其药学上可接受的盐，和活性在抗病毒剂含有该衍生物或其盐作为成分。

3. 发明授权

EP0829476B1 6-Substituted acyclopyrimidine nucleoside derivatives and antiviral agent containing the same as active ingredient thereof 失效
标题翻译： 6-取代的Acylopyrimidin核苷衍生物和抗病毒剂含有作为活性物质的
公开(公告)号：EP0829476B1
公开(公告)日：2002-08-28
申请号：EP97110658.8
申请日：1990-09-28
申请人： MITSUBISHI CHEMICAL CORPORATION
发明人： Miyasaka, Tadashi , Tanaka, Hiromichi , De Clercq, Erik Desire Alice , Baba, Masanori , Walker, Richard Thomas , Ubasawa, Masaru
IPC分类号： C07D239/60 , C07D239/54 , C07D401/12 , C07D239/56 , C07D239/58 , A61K31/505
CPC分类号： C07D239/47 , C07D239/54 , C07D239/545 , C07D239/56 , C07D239/58 , C07D239/60

4. 发明公开

EP0829476A2 6-Substituted acyclopyrimidine nucleoside derivatives and antiviral agent containing the same as active ingredient thereof 失效
标题翻译： 6-取代基Acylopyrimidin-Nucleoside-Derivate und diese als wirksamen Stoff enthaltende Antivirusmittel
公开(公告)号：EP0829476A2
公开(公告)日：1998-03-18
申请号：EP97110658.8
申请日：1990-09-28
申请人： Mitsubishi Chemical Corporation
发明人： Miyasaka, Tadashi , Tanaka, Hiromichi , De Clercq, Erik Desire Alice , Masanori, Baba , Walker, Richard Thomas , Ubasawa, Masaru
IPC分类号： C07D239/46 , C07D239/54 , C07D239/56 , C07D239/58 , C07D239/60 , A61K31/505
CPC分类号： C07D239/47 , C07D239/54 , C07D239/545 , C07D239/56 , C07D239/58 , C07D239/60
摘要： A 6-substituted acyclopyrimidine nucleoside derivative represented by the following general formula I or I';

wherein R 1 represents a hydrogen atom, halogen atom, alkyl, cycloalkyl, alkenyl, alkynyl, alkylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylthio or aralkyl group;
R 2 represents an arylthio, alkylthio, cycloalkylthio, arylsulfinyl, alkylsulfinyl, cycloalkylsulfinyl, alkenyl, alkynyl, aralkyl, arylcarbonyl, arylcarbonylalkyl or aryloxy group, those groups optionally substituted by one or more of substituents selected from a halogen atom, alkyl, halogenated alkyl, alkoxy, hydroxyl, nitro, amino, cyano and acyl groups;
R 3 represents a hydrogen atom, methyl, branched alkyl or -CH 2 -Z-(CH 2 ) n -R 5 group where R 5 represents a hydrogen atom, halogen atom, hydroxyl, heterocyclic carbonyloxy, formyloxy, alkylcarbonyloxy, cycloalkylcarbonyloxy, aralkylcarbonyloxy, arylcarbonyloxy, azido, alkoxycarbonyloxy, N-alkylcarbamoyloxy, N-arylcarbamoyloxy, N-alkylthiocarbamoyloxy, N-arylthiocarbamoyloxy, alkoxy, aralkyloxy, branched alkyl, cycloalkyl or aryl group, the alkoxycarbonyloxy to aryl groups mentioned above as R 5 optionally substituted by one or more substituents selected from a halogen atom, aryl, alkyl, alkoxy and halogenated alkyl groups, Z represents an oxygen, sulfur atom or methylene group, and n represents 0 or an integer of 1 to 5,
R 4 represents a hydrogen atom, alkyl or aralkyl group,
X represents an oxygen or sulfur atom,
Y represents an oxygen or sulfur atom,
provided that when R 4 and Z represent a hydrogen atom and oxygen atom respectively in the formula I R 5 does not represent a hydroxyl group,
or a pharmaceutically acceptable salt thereof, and an antiviral agent containing the derivative or the salt thereof as an active ingredient.
摘要翻译：由以下通式I或I'表示的6-取代的环磷酰嘧啶核苷衍生物; 其中R 1表示氢原子，卤素原子，烷基，环烷基，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。 R 2表示芳硫基，烷硫基，环烷基硫基，芳基亚磺酰基，烷基亚磺酰基，环烷基亚磺酰基，烯基，炔基，芳烷基，芳基羰基，芳基羰基烷基或芳氧基，这些基团任选被一个或多个选自卤素原子，烷基，烷氧基，羟基，硝基，氨基，氰基和酰基; R 3表示氢原子，甲基，支链烷基或-CH 2 -Z-（CH 2）n R 5基团，其中R 5表示氢原子，卤素原子，羟基，杂环羰氧基，甲酰氧基，烷基羰基氧基，环烷基羰基氧基，芳烷基羰基氧基，芳基羰基氧基，叠氮基，烷氧基羰基氧基，N-烷基氨基甲酰氧基，N-芳基氨基甲酰氧基，N-烷基硫代氨基甲酰氧基，N-芳硫基氨基甲酰氧基，烷氧基，芳烷氧基，支链烷基，环烷基或芳基，上述作为R 5烷氧基羰基氧基至芳基被一个或多个选自卤素原子，芳基，烷基，烷氧基和卤代烷基的取代基取代，Z表示氧，硫原子或亚甲基，n表示0或1〜5的整数，R 4表示氢原子，烷基或芳烷基，X表示氧或硫原子，Y表示氧或硫原子，条件是当R 4和Z分别代表式IR 5中的氢原子和氧原子时，不代表水电甲基或其药学上可接受的盐，以及含有其衍生物或其盐作为活性成分的抗病毒剂。

5. 发明公开

EP0449726A1 Pyrimidine nucleoside derivative and antiviral agent containing the derivative as active ingredient 失效
标题翻译： Pyrimidin-Nukleosid-Derivate und antivirale Mittel，die diese Derivate als aktiven Bestandteil enthalten。
公开(公告)号：EP0449726A1
公开(公告)日：1991-10-02
申请号：EP91400819.8
申请日：1991-03-26
申请人： Mitsubishi Chemical Corporation
发明人： Miyasaka, Tadashi , Tanaka, Hiromichi , De Clercq, Erik Desire Alice , Baba, Masanori , Walker, Richard Thomas , Ubasawa, Masaru
IPC分类号： C07D239/60 , C07D239/54 , A61K31/505
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-位上存在乙基或异丙基，并且在嘧啶的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。

6. 发明公开

EP0829476A3 6-Substituted acyclopyrimidine nucleoside derivatives and antiviral agent containing the same as active ingredient thereof 失效
标题翻译： 6-取代基Acylopyrimidin-Nucleoside-Derivate und diese als wirksamen Stoff enthaltende Antivirusmittel
公开(公告)号：EP0829476A3
公开(公告)日：1999-02-24
申请号：EP97110658.8
申请日：1990-09-28
申请人： Mitsubishi Chemical Corporation
发明人： Miyasaka, Tadashi , Tanaka, Hiromichi , De Clercq, Erik Desire Alice , Masanori, Baba , Walker, Richard Thomas , Ubasawa, Masaru
IPC分类号： C07D239/46 , C07D239/54 , C07D239/56 , C07D239/58 , C07D239/60 , A61K31/505
CPC分类号： C07D239/47 , C07D239/54 , C07D239/545 , C07D239/56 , C07D239/58 , C07D239/60
摘要： A 6-substituted acyclopyrimidine nucleoside derivative represented by the following general formula I or I';
wherein R 1 represents a hydrogen atom, halogen atom, alkyl, cycloalkyl, alkenyl, alkynyl, alkylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylthio or aralkyl group; R 2 represents an arylthio, alkylthio, cycloalkylthio, arylsulfinyl, alkylsulfinyl, cycloalkylsulfinyl, alkenyl, alkynyl, aralkyl, arylcarbonyl, arylcarbonylalkyl or aryloxy group, those groups optionally substituted by one or more of substituents selected from a halogen atom, alkyl, halogenated alkyl, alkoxy, hydroxyl, nitro, amino, cyano and acyl groups; R 3 represents a hydrogen atom, methyl, branched alkyl or -CH 2 -Z-(CH 2 ) n -R 5 group where R 5 represents a hydrogen atom, halogen atom, hydroxyl, heterocyclic carbonyloxy, formyloxy, alkylcarbonyloxy, cycloalkylcarbonyloxy, aralkylcarbonyloxy, arylcarbonyloxy, azido, alkoxycarbonyloxy, N-alkylcarbamoyloxy, N-arylcarbamoyloxy, N-alkylthiocarbamoyloxy, N-arylthiocarbamoyloxy, alkoxy, aralkyloxy, branched alkyl, cycloalkyl or aryl group, the alkoxycarbonyloxy to aryl groups mentioned above as R 5 optionally substituted by one or more substituents selected from a halogen atom, aryl, alkyl, alkoxy and halogenated alkyl groups, Z represents an oxygen, sulfur atom or methylene group, and n represents 0 or an integer of 1 to 5, R 4 represents a hydrogen atom, alkyl or aralkyl group, X represents an oxygen or sulfur atom, Y represents an oxygen or sulfur atom,
provided that when R 4 and Z represent a hydrogen atom and oxygen atom respectively in the formula I R 5 does not represent a hydroxyl group,
or a pharmaceutically acceptable salt thereof, and an antiviral agent containing the derivative or the salt thereof as an active ingredient.
摘要翻译：由以下通式I或I min表示的6-取代的环磷酰嘧啶核苷衍生物; 其中R 1表示氢原子，卤素原子，烷基，环烷基，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。 R 2表示芳硫基，烷硫基，环烷硫基，芳基亚磺酰基，烷基亚磺酰基，环烷基亚磺酰基，烯基，炔基，芳烷基，芳基羰基，芳基羰基烷基或芳氧基，任选被一个或多个选自卤素原子，烷基，卤代烷基，烷氧基，羟基，硝基，氨基，氰基和酰基; R 3表示氢原子，甲基，支链烷基或-CH 2 -Z-（CH 2）n R 5基团，其中R 5表示氢原子，卤素原子，羟基，杂环羰氧基，甲酰氧基，烷基羰基氧基，环烷基羰基氧基，芳烷基羰基氧基，芳基羰基氧基，叠氮基，烷氧基羰基氧基，N-烷基氨基甲酰氧基，N-芳基氨基甲酰氧基，N-烷基硫代氨基甲酰氧基，N-芳硫基氨基甲酰氧基，烷氧基，芳烷氧基，支链烷基，环烷基或芳基，上述作为R 5烷氧基羰基氧基至芳基被一个或多个选自卤素原子，芳基，烷基，烷氧基和卤代烷基的取代基取代，Z表示氧，硫原子或亚甲基，n表示0或1〜5的整数，R 4表示氢原子，烷基或芳烷基，X表示氧或硫原子，Y表示氧或硫原子，条件是当R 4和Z分别代表式IR 5中的氢原子和氧原子时，不代表水电甲基或其药学上可接受的盐，以及含有其衍生物或其盐作为活性成分的抗病毒剂。

7. 发明授权

EP0449726B1 Pyrimidine nucleoside derivative and antiviral agent containing the derivative as active ingredient 失效
标题翻译：嘧啶核苷衍生物以及含有这些衍生物作为活性成分的抗病毒剂
公开(公告)号：EP0449726B1
公开(公告)日：1997-06-11
申请号：EP91400819.8
申请日：1991-03-26
申请人： Mitsubishi Chemical Corporation
发明人： Miyasaka, Tadashi , Tanaka, Hiromichi , De Clercq, Erik Desire Alice , Baba, Masanori , Walker, Richard Thomas , Ubasawa, Masaru
IPC分类号： C07D239/60 , C07D239/54 , A61K31/505
CPC分类号： C07D239/54 , C07D239/56 , C07D239/58 , C07D239/60

8. 发明公开

EP0420763A3 6-Substituted acyclopyrimidine nucleoside derivatives and antiviral agent containing the same as active ingredient thereof 失效
标题翻译： 6-取代的ACYCLOPYRIMIDIN核苷衍生物和含有它的活性成分的杀真菌剂作为其主要成分
公开(公告)号：EP0420763A3
公开(公告)日：1991-09-18
申请号：EP90402693.7
申请日：1990-09-28
申请人： Mitsubishi Chemical Corporation
发明人： Miyasaka, Tadashi , Tanaka, Hiromichi , De Clercq, Erik Desire Alice , Baba, Masanori , Walker, Richard Thomas , Ubasawa, Masaru
IPC分类号： C07D239/60 , C07D239/54 , C07D239/56 , C07D239/47 , A61K31/505
CPC分类号： C07D239/47 , C07D239/54 , C07D239/545 , C07D239/56 , C07D239/58 , C07D239/60
摘要： 6-substituted acyclopyrimidine nucleoside derivative represented by the following general formula I or I';
wherein R 1 represents a hydrogen atom, halogen atom, alkyl, cycloalkyl, alkenyl, alkynyl, alkylcarbonyl, arylcarbonyl, arylcarbonylalkyl, arylthio or aralkyl group; R 2 represents an arylthio, alkylthio, cycloalkylthio, arylsulfinyl, alkylsulfinyl, cycloalkylsulfinyl, alkenyl, alkynyl, aralkyl, arylcarbonyl, arylcarbonylalkyl or aryloxy group, those groups optionally substituted by one or more of substituents selected from a haloger atom, alkyl, halogenated alkyl, alkoxy, hydroxyl, nitro, amino, cyano and acyl groups;
R 3 represents a hydrogen atom, methyl, branched alkyl or -CH 2 -Z-(CH 2 ) n -R 5 group where R 5 represents a hydrogen atom, halogen atom, hydroxyl, heterocyclic carbonyloxy, formyloxy, alkylcarbonyloxy, cycloalkylcarbonyloxy, aralkylcarbonyloxy, arylcarbonyloxy, azido, alkoxycarbonyloxy, N-alkylcarbamoyloxy, N-arylcarbamoyloxy, N-alkylthiocarbamoyloxy, N-arylthiocarbamoyloxy, alkoxy, aralkyloxy, branched alkyl, cycloalkyl or aryl group, the alkoxycarbonyloxy to aryl groups mentioned above as R 5 optionally substituted by one or more substituents selected from a halogen atom, aryl, alkyl, alkoxy and halogenated alkyl groups, Z represents an oxygen, sulfur atom or methylene group, and n represents 0 or an integer of 1 to 5, R4- represents a hydrogen atom, alkyl or aralkyl group, X represents an oxygen or sulfur atom, Y represents an oxygen or sulfur atom, provided that when R 4 and Z represent a hydrogen atom and oxygen atom respectively in the formula I R 5 does not represent a hydroxyl group,
or a pharmaceutically acceptable salt thereof, and an antiviral agent containing the derivative or the salt thereof as an active ingredient.

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