公开(公告)号：US06660745B1

公开(公告)日：2003-12-09

申请号：US09926477

申请日：2002-01-09

申请人： Kouichi Sekiya ,  Akihiro Takemiya ,  Masahiro Ohshima

发明人： Kouichi Sekiya ,  Akihiro Takemiya ,  Masahiro Ohshima

IPC分类号： C07D47318

CPC分类号： C07D473/00 ,  A61K31/52 ,  C07D473/28 ,  C07D473/36 ,  C07D473/40

摘要： Dihydrate of 4-[[9-[(3-cyclopentyloxy-4-methoxy)benzyl]-6,8-dimethylpurin]-2-yl-3-oxypropyl]pyridine N-oxide, drugs containing the same and a compound useful as an intermediate in the production of this dihydrate. Because of having a phosphodiesterase IV inhibitory effect, this dihydrate is useful as a preventive and/or remedy for asthma, chronic obstructive lung disease and/or other inflammatory diseases.

摘要翻译： 4 - [[9 - [（3-环戊基氧基-4-甲氧基）苄基] -6,8-二甲基嘌呤] -2-基-3-氧代丙基]吡啶N-氧化物的二水合物，含有它们的药物和可用于 由于具有磷酸二酯酶IV抑制作用，因此该二水合物可用作哮喘，慢性阻塞性肺病和/或其它炎性疾病的预防和/或补救。

公开(公告)号：US06919455B2

公开(公告)日：2005-07-19

申请号：US10631795

申请日：2003-08-01

申请人： Kouichi Sekiya ,  Akihiro Takemiya

发明人： Kouichi Sekiya ,  Akihiro Takemiya

IPC分类号： A61K31/52 ,  A61P11/00 ,  A61P11/06 ,  A61P29/00 ,  A61P43/00 ,  C07D473/00 ,  C07D473/28 ,  C07D473/36 ,  C07D473/40 ,  C07F9/6561

CPC分类号： C07D473/00 ,  A61K31/52 ,  C07D473/28 ,  C07D473/36 ,  C07D473/40

摘要： A compound represented by the following formula (I), or a salt thereof: where X is a halogen atom or a group represented by —S—(CH2)n—A, —SO—(CH2)m—B, —SO2—(CH2)m —B, —OSO2—(CH2)m—B, —OCO—(CH2)m—B or —OPO(OR)—(CH2)m—B, wherein n represents an integer of 0-4, A represents an optionally substituted aromatic hydrocarbon group or an optionally substituted heterocyclic residue having 1 to 4 hetero atoms selected from an oxygen atom, sulfur atom and nitrogen atom and having 5 to 10 ring-constituent atoms, m represents an integer of 0-4, B represents an optionally substituted alkyl group, an optionally substituted aromatic hydrocarbon group or an optionally substituted heterocyclic residue having 1 to 4 hetero atoms selected from an oxygen atom, sulfur atom and nitrogen atom and having 5 to 10 ring-constituent atoms, and R represents an optionally substituted alkyl group.

摘要翻译： 由下式（I）表示的化合物或其盐：其中X是卤素原子或由-S-（CH 2）n - 表示的基团） A，-SO-（CH 2 CH 2）m -B，-SO 2 - （CH 2 CH 2） （CH 2）m -B，-OCO-（CH

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.

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。

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。

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。

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。