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    BICYCLIC COMPOUNDS
    42.
    发明申请
    BICYCLIC COMPOUNDS 审中-公开
    双酚化合物

    公开(公告)号：WO2005115984A2

    公开(公告)日：2005-12-08

    申请号：PCT/JP2005/010287

    申请日：2005-05-30

    Applicant: TANABE SEIYAKU CO., LTD. ,  HIRAI, Miki ,  KUSAMA, Mari ,  HOSAKA, Toshihiro ,  KOHNOMI, Shuntarou

    Inventor： HIRAI, Miki ,  KUSAMA, Mari ,  HOSAKA, Toshihiro ,  KOHNOMI, Shuntarou

    IPC: C07D213/61

    CPC classification number: C07D213/55 ,  C07D213/56 ,  C07D213/57 ,  C07D213/61 ,  C07D213/64 ,  C07D239/26 ,  C07D239/30 ,  C07D239/34 ,  C07D239/42 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D409/04

    Abstract: The present invention is to provide a bicyclic compound represented by the following formula: wherein Ring Q is pyridine or pyrimidine; Ring A is benzene or a heterocyclic ring; G is Ring B optionally having a substituent(s) R 3 , or an amino optionally substituted by one or two selected from the group consisting of alkyl(s), aralkyl(s) and cycloalkyl(s); Ring B is benzene, a heterocyclic ring, a cycloalkane or a cycloalkene; R 1 is a group selected from the following formulae: R 2 and R 3 may be the same or different from each other, and each is cyano, nitro, etc.; m is 0, 1 or 2; R 4 is hydrogen, a halogen, etc.; and R 5 and R 6 may be the same or different from each other, and each is hydrogen, an optionally substituted alkyl, etc., or a pharmaceutically acceptable salt thereof, which is a large conductance calcium-activated K channel opener useful for treatment of pollakiuria, urinary incontinence, etc.

    Abstract translation: 本发明提供由下式表示的双环化合物：其中环Q是吡啶或嘧啶; 环A是苯或杂环; G是任选具有取代基R 3的环B，或任选被一个或两个选自烷基，芳烷基和环烷基的一个或两个取代基的氨基; 环B是苯，杂环，环烷烃或环烯烃; R 1是选自下式的基团：R 2和R 3可以相同或不同，各自为氰基，硝基等; m为0,1或2; R 4是氢，卤素等; R 5和R 6可以彼此相同或不同，各自为氢，任选取代的烷基等，或其药学上可接受的盐，其是大电导钙激活的K通道 开胃器可用于治疗尿频，尿失禁等

    NOVEL COMPOUNDS HAVING INHIBITORY ACTIVITY AGAINST SODIUM-DEPENDANT TRANSPORTER
    46.
    发明申请
    NOVEL COMPOUNDS HAVING INHIBITORY ACTIVITY AGAINST SODIUM-DEPENDANT TRANSPORTER 审中-公开
    具有抗依赖性运输机构的抑制活性的新型化合物

    公开(公告)号：WO2005012326A1

    公开(公告)日：2005-02-10

    申请号：PCT/JP2004/011312

    申请日：2004-07-30

    Applicant: TANABE SEIYAKU CO., LTD. ,  NOMURA, Sumihiro ,  KAWANISHI, Eiji ,  UETA, Kiichiro

    Inventor： NOMURA, Sumihiro ,  KAWANISHI, Eiji ,  UETA, Kiichiro

    IPC: C07H19/06

    CPC classification number: C07H19/048 ,  A61K45/06 ,  C07D405/04 ,  C07D409/04 ,  C07D409/10 ,  C07H19/06

    Abstract: A compound of the formula (I) wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is -(CH2)n- (n is 1 or 2); a pharmaceutically acceptable salt thereof, or a prodrug thereof.

    Abstract translation: 式（I）的化合物，其中环A和环B是：（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环， 或任选取代的苯环，（2）环A是任选取代的苯环，并且环B是任选取代的不饱和单环杂环或任选取代的不饱和稠合杂双环，或（3）环A是任选取代的不饱和 稠环杂双环和环B独立地是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环; X是碳原子或氮原子; Y为 - （CH 2）n - （n为1或2）; 其药学上可接受的盐或其前药。

    NOVEL COMPOUNDS
    47.
    发明申请
    NOVEL COMPOUNDS 审中-公开
    新型化合物

    公开(公告)号：WO2005012321A1

    公开(公告)日：2005-02-10

    申请号：PCT/JP2004/011311

    申请日：2004-07-30

    Applicant: TANABE SEIYAKU CO., LTD. ,  NOMURA, Sumihiro ,  SAKAMOTO, Toshiaki ,  UETA, Kiichiro

    Inventor： NOMURA, Sumihiro ,  SAKAMOTO, Toshiaki ,  UETA, Kiichiro

    IPC: C07H15/203

    CPC classification number: C07H15/203 ,  C07H5/04 ,  C07H17/02

    Abstract: A compound of the formula (I): wherein Ring A and Ring B are (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, wherein -NR- group and -CH2- group are both on the same ring of the unsaturated fused heterobicyclic ring, and Ring B is an optionally substituted monocyclic unsaturated heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; and R is a hydrogen atom, a lower alkyl group, a lower alkanoyl group or a lower alkoxycarbonyl group, or a pharmaceutically acceptable salt thereof, or a prodrug thereof.

    Abstract translation: 式（I）的化合物：其中环A和环B是（1）环A是任选取代的不饱和单环杂环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环， 或任选取代的苯环，（2）环A是任选取代的苯环，环B是任选取代的不饱和单环杂环，任选取代的不饱和稠合杂双环或任选取代的苯环，或（3） 环A是任选取代的不饱和稠合杂双环，其中-NR-基和-CH2-基都在不饱和稠合杂双环的相同环上，环B是任选取代的单环不饱和杂环，任选取代的不饱和杂环 稠合杂双环或任选取代的苯环; 或其前体药物，R为氢原子，低级烷基，低级烷酰基或低级烷氧基羰基，或其药学上可接受的盐。

    PLASMODIUM PROTOZOA PHOSPHODIESTERASE, NUCLEIC ACID ENCODING THE PHOSPHODIESTERASE, AND TREATMENT OF MALARIA USING INHIBITOR OF THE PHOSPHODIESTERASE
    50.
    发明申请
    PLASMODIUM PROTOZOA PHOSPHODIESTERASE, NUCLEIC ACID ENCODING THE PHOSPHODIESTERASE, AND TREATMENT OF MALARIA USING INHIBITOR OF THE PHOSPHODIESTERASE 审中-公开
    原卟啉磷酸二酯酶，核酸磷酸二酯酶的制备，以及用磷酸二酯酶抑制剂治疗疟疾

    公开(公告)号：WO2004044192A2

    公开(公告)日：2004-05-27

    申请号：PCT/JP2003/014422

    申请日：2003-11-13

    Applicant: TANABE SEIYAKU CO., LTD. ,  YUASA, Keizo ,  OMORI, Kenji ,  SAKURAI, Naoki ,  KITA, Kiyoshi

    Inventor： YUASA, Keizo ,  OMORI, Kenji ,  SAKURAI, Naoki ,  KITA, Kiyoshi

    IPC: C12N9/00

    CPC classification number: C12N9/16 ,  A61K38/00 ,  C12Y301/04017 ,  Y02A50/411

    Abstract: The present invention relates to a novel cyclic nucleotide phosphodiesterase (PDE) of Plasmodium protozoa and a nucleic acid encoding the cyclic nucleotide phosphodiesterase, more specifically, a polypeptide comprising the amino acid sequence as shown in SEQ ID NO: 2, 4, 6 or 8, or a conservative substitution variant or a naturally occurring allelic variant thereof. Also, there is provided a nucleic acid encoding the above polypeptide or a complement thereof. There are provided a recombinant vector comprising the above nucleic acid; a host cell into which the above recombinant vector has been introduced; a method of producing a polypeptide comprising culturing the above host cell. Further, there are provided a method of characterizing, identifying or selecting an inhibitor of a cyclic nucleotide phosphodiesterase using the above pollypeptide; a pharmaceutical composition for treatment of malaria comprising, as an active ingredient, a compound having an inhibitory activity against a cyclic nucleotide phosphodiesterase of Plasmodium protozoa; and a method of treating malaria using the compound. The novel PDE, the novel nucleic acid encoding the PDE and the like according to the present invention are useful for research of mechanisms of intracellular signal transduction or the like in Plasmodium. Also, the method of characterizing, identifying and selecting an inhibitor using the novel PDE and a gene thereof is useful for research and development for a highly selective inhibitor or an excellent pharmaceutical (for instance, a therapeutic agent for malaria) with a high therapeutic effect and little side effects.

    Abstract translation: 本发明涉及疟原虫原生动物的新型环核苷酸磷酸二酯酶（PDE）和编码环核苷酸磷酸二酯酶的核酸，更具体地，涉及包含氨基酸 序列如SEQ ID NO：2,4,6或8所示，或其保守置换变体或其天然存在的等位基因变体。 而且，提供了编码上述多肽或其互补物的核酸。 提供了包含上述核酸的重组载体; 导入了上述重组载体的宿主细胞; 包括培养上述宿主细胞的生产多肽的方法。 此外，提供了使用上述多肽表征，鉴定或选择环核苷酸磷酸二酯酶抑制剂的方法; 一种用于治疗疟疾的药物组合物，其包含作为活性成分的对疟原虫原核环状核苷酸磷酸二酯酶具有抑制活性的化合物; 以及使用该化合物治疗疟疾的方法。 根据本发明的新型PDE，编码PDE等的新型核酸可用于研究疟原虫中细胞内信号转导等的机制。 此外，使用新型PDE及其基因表征，鉴定和选择抑制剂的方法对于高选择性抑制剂或优异药物（例如疟疾治疗剂）的研究和开发是有用的，其中 疗效高，副作用小。

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