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    Heterocyclic compound, composition and method for inhibiting adenosine deaminase
    1.
    发明授权
    Heterocyclic compound, composition and method for inhibiting adenosine deaminase 失效
    杂环化合物，抑制腺苷脱氨酶的组合物和方法

    公开(公告)号：US06596738B1

    公开(公告)日：2003-07-22

    申请号：US09926134

    申请日：2001-09-07

    申请人： Tadashi Terasaka ,  Nobuo Seki ,  Kiyoshi Tsuji ,  Isao Nakanishi ,  Takayoshi Kinoshita ,  Katsuya Nakamura

    发明人： Tadashi Terasaka ,  Nobuo Seki ,  Kiyoshi Tsuji ,  Isao Nakanishi ,  Takayoshi Kinoshita ,  Katsuya Nakamura

    IPC分类号： A61K314164

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D233/90 ,  C07D249/10 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04 ,  C07F7/1804 ,  Y02P20/55

    摘要： Heterocyclic compounds of the following formula: wherein B is  [wherein R1 is hydrogen or lower alkyl; R2 is hydrogen or lower alkyl; and X is hydrogen or hydroxy protective group], lower alkanoyl or hydroxyimino(lower)alkyl A is lower alkylene; W is heterocyclic or carbocyclic group, each of which may have one or more substituent(s); Z is heterocyclic group selected from the group consisting of imidazolyl, triazolyl,imidazopyridyl and adenyl, each of which may have one or more substituent(s); or a salt thereof, provided that when W is aryl which may have one or more substituent(s), then (i) Z is triazolyl, imidazopyridyl or adenyl, each of which may have one or more substituent(s); (ii) Z is imidazolyl which may have one or more substituent(s) and B is lower alkanoyl or hydroxyimino(lower)alkyl; or (iii) Z is imidazolyl which may have one or more substituent(s) and R1 and R2 are both lower alkyl. or pharmaceutically acceptable salts thereof, which are useful as a medicament.

    摘要翻译： 下式的杂环化合物：其中B是[其中R 1是氢或低级烷基; R 2是氢或低级烷基; 和X是氢或羟基保护基]，低级烷酰基或羟基亚氨基（低级）烷基A是低级亚烷基; W是杂环或碳环基，每一个可以具有一个或多个取代基; Z是选自 咪唑基，三唑基，咪唑并吡啶基和腺嘌呤，其各自可以具有一个或多个取代基;或其盐，条件是当W是可以具有一个或多个取代基的芳基时，则（i）Z是 三唑基，咪唑并吡啶基或腺苷酸，其各自可以具有一个或多个取代基; （ii）Z是可以具有一个或多个取代基的咪唑基，B是低级烷酰基或羟基亚氨基（低级）烷基; 或（iii）Z是可具有一个或多个取代基的咪唑基，R 1和R 2均为低级烷基或其药学上可接受的盐，其可用作药物。

    Imidazole compounds
    2.
    发明授权
    Imidazole compounds 失效
    咪唑化合物

    公开(公告)号：US06359145B1

    公开(公告)日：2002-03-19

    申请号：US09764995

    申请日：2001-03-09

    申请人： Tadashi Terasaka ,  Katsuya Nakamura ,  Nobuo Seki ,  Masako Kuno ,  Susumu Tsujimoto ,  Akihiro Sato ,  Isao Nakanishi ,  Takayoshi Kinoshita ,  Nobuya Nishio ,  Hiroyuki Okumura ,  Kiyoshi Tsuji

    发明人： Tadashi Terasaka ,  Katsuya Nakamura ,  Nobuo Seki ,  Masako Kuno ,  Susumu Tsujimoto ,  Akihiro Sato ,  Isao Nakanishi ,  Takayoshi Kinoshita ,  Nobuya Nishio ,  Hiroyuki Okumura ,  Kiyoshi Tsuji

    IPC分类号： C07D23366

    CPC分类号： C07D403/04 ,  C07D233/90 ,  C07D405/06 ,  C07F7/1804

    摘要： Imidazole compounds having adenosine deaminase inhibitory activity represented by formula (I) wherein R1 is hydrogen, hydroxy, protected hydroxy, or aryl optionally substituted with suitable substituent(s); R2 is hydrogen or lower alkyl; R3 is hydroxy or protected hydroxy; R4 is cyano, (hydroxy)iminoamino(lower)alkyl, carboxy, protected carboxy, heterocyclic group optionally substituted with amino, or carbamoyl optionally substituted with suitable substituent(s); and —A— is —Q— or —O—Q—, wherein Q is single bond or lower alkylene, provided that when R2 is lower alkyl, then R1 is hydroxy, protected hydroxy, or aryl optionally substituted with suitable substituent(s), its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective.

    摘要翻译： 式（I）表示的具有腺苷脱氨酶抑制活性的咪唑化合物，其中R 1为氢，羟基，保护的羟基或任选被合适的取代基取代的芳基; R2是氢或低级烷基; R3是羟基或被保护的羟基; R4是氰基，（羟基）亚氨基氨基（低级）烷基，羧基，受保护的羧基，任选被氨基取代的杂环基或任选被合适的取代基取代的氨基甲酰基; 并且-A-是-Q-或-OQ-，其中Q是单键或低级亚烷基，条件是当R 2是低级烷基时，则R 1是羟基，保护的羟基或任选地被合适的取代基取代的芳基，其 前药或其盐。 该化合物可用于治疗和/或预防腺苷有效的疾病。

    Imidazole derivatives as adenosine deaminase inhibitors
    5.
    发明授权
    Imidazole derivatives as adenosine deaminase inhibitors 失效
    咪唑衍生物作为腺苷脱氨酶抑制剂

    公开(公告)号：US07064144B2

    公开(公告)日：2006-06-20

    申请号：US10483336

    申请日：2002-07-10

    申请人： Tadashi Terasaka ,  Takeshi Kato ,  Kiyoshi Tsuji ,  Katsuya Nakamura

    发明人： Tadashi Terasaka ,  Takeshi Kato ,  Kiyoshi Tsuji ,  Katsuya Nakamura

    IPC分类号： A01N43/36 ,  A61K31/40 ,  C07D233/22 ,  C07D233/64

    CPC分类号： C07D401/12 ,  C07D233/90 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： Imidazole compounds having adenosine deaminase inhibitory activity represented by the formula (I) wherein R1 is aryl or heterocyclic group which is optionally substituted with substituent(s); R2 is lower alkyl; R3 is hydroxy or protected hydroxy; -A- is lower alkylene; and —X— is —O— or —S—; provided that when then R1 is aryl which is substituted with substituent(s), or heterocyclic group which is optionally substituted with substituent(s), its prodrug, or their salt. The compounds are useful for treating and/or preventing diseases for which adenosine is effective.

    摘要翻译： 具有由式（I）表示的腺苷脱氨酶抑制活性的咪唑化合物，其中R 1是任选被取代基取代的芳基或杂环基; R 2是低级烷基; R 3是羟基或被保护的羟基; -A-是低级亚烷基; 和-X-是-O-或-S-; 条件是当R 1是被取代基取代的芳基，或任选被取代基取代的杂环基时，其前药或其盐。 该化合物可用于治疗和/或预防腺苷有效的疾病。

    Thiophene derivatives
    6.
    发明授权
    Thiophene derivatives 失效
    噻吩衍生物

    公开(公告)号：US5571810A

    公开(公告)日：1996-11-05

    申请号：US422545

    申请日：1995-04-13

    申请人： Masaaki Matsuo ,  Kiyoshi Tsuji ,  Nobukiyo Konishi ,  Katsuya Nakamura

    发明人： Masaaki Matsuo ,  Kiyoshi Tsuji ,  Nobukiyo Konishi ,  Katsuya Nakamura

    IPC分类号： C07D333/12 ,  C07D333/22 ,  C07D333/24 ,  C07D333/32 ,  C07D333/34 ,  C07D333/36 ,  C07D333/38 ,  C07D409/12 ,  A61K31/535 ,  A61K31/38 ,  A61K31/42 ,  A61K31/495

    CPC分类号： C07D409/12 ,  C07D333/12 ,  C07D333/22 ,  C07D333/24 ,  C07D333/32 ,  C07D333/34 ,  C07D333/36 ,  C07D333/38

    摘要： This invention relates to new thiophene derivatives having antiinflammatory and analgesic activities and represented by the general formula [I]: ##STR1## wherein R.sup.1 is hydrogen, halogen, cyano, substituted lower alkyl, substituted or unsubstituted lower alkenyl, acyl, nitro, substituted or unsubstituted amino, sulfo, substituted or unsubstituted sulfamoyl, N-containing heterocyclicsulfonyl, hydoxy, substituted or unsubstituted heterocyclic group,R.sup.2 is substituted or unsubstituted aryl, andR.sup.3 is substituted or unsubstituted aryl, provided that R.sup.3 is aryl substituted with substituent(s) selected from the group consisting of amino, mono(lower)-alkylamino, acylamino, lower alkyl(acyl)amino and sulfamoyl when R.sup.1 is hydrogen, halogen or cyano, and pharmaceutically acceptable salts thereof, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.

    摘要翻译： 本发明涉及具有抗炎和止痛活性的新噻吩衍生物，由通式[I]表示：其中R 1是氢，卤素，氰基，取代的低级烷基，取代或未取代的低级烯基，酰基，硝基 取代或未取代的氨基，磺基，取代或未取代的氨磺酰基，含N杂环基磺酰基，羟基，取代或未取代的杂环基，R2为取代或未取代的芳基，R3为取代或未取代的芳基，条件是R3为被取代基取代的芳基 s）选自氨基，单（低级） - 烷基氨基，酰氨基，低级烷基（酰基）氨基和氨磺酰基，当R 1为氢时，卤素或氰基，及其药学上可接受的盐，其制备方法和 包含其的药物组合物。