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    Indazole derivatives
    1.
    发明授权
    Indazole derivatives 失效
    吲唑衍生物

    公开(公告)号：US07919517B2

    公开(公告)日：2011-04-05

    申请号：US12275614

    申请日：2008-11-21

    Applicant: Yoshihisa Ohta ,  Fumihiko Kanai ,  Shinji Nara ,  Yutaka Kanda ,  Hiroshi Umehara ,  Yukimasa Shiotsu ,  Tomoki Naoe ,  Hitoshi Kiyoi ,  Keiko Kawashima ,  Hiromi Ando ,  Motoki Miyama

    Inventor： Yoshihisa Ohta ,  Fumihiko Kanai ,  Shinji Nara ,  Yutaka Kanda ,  Hiroshi Umehara ,  Yukimasa Shiotsu ,  Tomoki Naoe ,  Hitoshi Kiyoi ,  Keiko Kawashima ,  Hiromi Ando ,  Motoki Miyama

    IPC: A61K31/416 ,  C07D231/56

    CPC classification number: C07D231/56

    Abstract: The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroaroyl, substituted or unsubstituted ararkyl, substituted or unsubstituted lower alkylsulfonyl or substituted or unsubstituted lower arylsulfonyl) or the like].

    Abstract translation: 本发明提供由式（I）表示的化合物：[其中R1表示CONR1aR1b（其中R1a和R1b可以相同或不同，各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的 芳基或取代或未取代的杂环基，或者R1a和R1b与相邻的氮原子一起形成取代或未取代的杂环基）等，R2表示氢原子，CONR2aR2b（其中R2a和R2b可以是 各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳基或取代或未取代的杂环基，或者R 2a和R 2b与相邻的氮原子一起形成取代基 或未取代的杂环基），NR2cR2d（其中R2c和R2d可以相同或不同 取代或未取代的杂芳酰基，取代或未取代的芳酰基，取代或未取代的低级烷基磺酰基或取代或未取代的低级芳基磺酰基）等，其中R 1表示氢原子，取代或未取代的低级烷基，取代或未取代的低级烷酰基，取代或未取代的芳酰基， 。

    Tricyclic compounds
    3.
    发明授权
    Tricyclic compounds 失效
    三环化合物

    公开(公告)号：US5478840A

    公开(公告)日：1995-12-26

    申请号：US294978

    申请日：1994-08-24

    Applicant: Etsuo Ohshima ,  Fumihiko Kanai ,  Hideyuki Sato ,  Hiroyuki Obase ,  Toshiaki Kumazawa ,  Shiho Takahara ,  Tetsuji Ohno ,  Tomoko Ishikawa ,  Koji Yamada

    Inventor： Etsuo Ohshima ,  Fumihiko Kanai ,  Hideyuki Sato ,  Hiroyuki Obase ,  Toshiaki Kumazawa ,  Shiho Takahara ,  Tetsuji Ohno ,  Tomoko Ishikawa ,  Koji Yamada

    IPC: C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D471/04 ,  C07D521/00 ,  A61K31/44

    CPC classification number: C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D471/04

    Abstract: A tricyclic compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, halogen or lower alkyl; A represents cyano, carboxyl, tetrazolyl, cyano-substituted phenyl, carboxyl-substituted phenyl or tetrazolyl-substituted phenyl; V represents --(CH.sub.2).sub.m --(wherein m is an integer of 0 to 2); W represents ##STR2## (wherein R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, halogen, lower alkyl, cycloalkyl, halogenated lower alkyl, hydroxy, lower alkoxy, amino, lower alkylamino, carboxyl or lower alkoxycarbonyl; and Q.sup.1 --Q.sup.2 --Q.sup.3 --Q.sup.4 represents N.dbd.CH--CH.dbd.CH; X.sup.1 --X.sup.2 --X.sup.3 represents CH.dbd.CH--CH.dbd.CH, S--CH.dbd.CH or CH.dbd.CH--S; Y represents a single bond, CH.sub.2, O, S, CH.sub.2 O, OCH.sub.2, CH.sub.2 S, SCH.sub.2, CH.sub.2 CH.sub.2 or CH.dbd.CH; and Z.sup.1 --Z.sup.2 represents C.dbd.CH, CH--CH.sub.2 or CH--CH(COOH)-- or a pharmaceutically acceptable salt thereof. The compound of the present invention exhibits antagonism to angiotensin II receptors.

    Abstract translation: 由下式（I）表示的三环化合物：其中R 1表示氢，卤素或低级烷基; A代表氰基，羧基，四唑基，氰基取代的苯基，羧基取代的苯基或四唑基取代的苯基; V表示 - （CH 2）m - （其中m为0〜2的整数）; W表示（其中R2，R3和R4独立地表示氢，卤素，低级烷基，环烷基，卤代低级烷基，羟基，低级烷氧基，氨基，低级烷基氨基，羧基或低级烷氧基羰基;以及Q1-Q2-Q3-Q4 表示N = CH-CH = CH; X 1 -X 2 -X 3表示CH = CH-CH = CH，S-CH = CH或CH = CH-S; Y表示单键，CH 2，O，S，CH 2 O，OCH 2 ，CH2S，SCH2，CH2CH2或CH = CH; Z1-Z2表示C = CH，CH-CH2或CH-CH（COOH） - 或其药学上可接受的盐。本发明化合物显示对血管紧张素II受体的拮抗作用。

    Indazole derivatives
    6.
    发明申请
    Indazole derivatives 失效
    吲唑衍生物

    公开(公告)号：US20070117856A1

    公开(公告)日：2007-05-24

    申请号：US10548475

    申请日：2004-07-30

    Applicant: Yoshihisa Ohta ,  Fumihiko Kanai ,  Shinji Nara ,  Yutaka Kanda ,  Hiroshi Umehara ,  Yukimasa Shiotsu ,  Tomoki Naoe ,  Hitoshi Kiyoi ,  Keiko Kawashima ,  Hiromi Ando ,  Motoki Miyama

    Inventor： Yoshihisa Ohta ,  Fumihiko Kanai ,  Shinji Nara ,  Yutaka Kanda ,  Hiroshi Umehara ,  Yukimasa Shiotsu ,  Tomoki Naoe ,  Hitoshi Kiyoi ,  Keiko Kawashima ,  Hiromi Ando ,  Motoki Miyama

    IPC: A61K31/416 ,  C07D231/56

    CPC classification number: C07D231/56

    Abstract: The present invention provides a compound represented by Formula (I): [wherein R1 represents CONR1aR1b (wherein R1a and R1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R1a and R1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R2 represents a hydrogen atom, CONR2aR2b (wherein R2a and R2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R2a and R2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR2cR2d (wherein R2c and R2d may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroaroyl, substituted or unsubstituted ararkyl, substituted or unsubstituted lower alkylsulfonyl or substituted or unsubstituted lower arylsulfonyl) or the like].

    Abstract translation: 本发明提供由式（I）表示的化合物：[其中R 1表示CONR 1a 1b 1b（其中R 1a） R 1b和R 1b可以相同或不同，各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳烷基或取代或未取代的杂环基， 或R 1a和R 1b与相邻的氮原子一起形成取代或未取代的杂环基）等，R 2 O， >表示氢原子，其中R 2a，R 2b和R 2b可以相同或不同， 各自表示氢原子，取代或未取代的低级烷基，取代或未取代的芳基，取代或未取代的芳烷基或取代或未取代的杂环基，或R 2b和R 2b >与t结合在一起 它与氮原子相邻以形成取代或未取代的杂环基），NR 2c R 2d（其中R 2c和R 2d） 取代或未取代的低级烷酰基，取代或未取代的芳酰基，取代或未取代的杂芳酰基，取代或未取代的芳烷基，取代或未取代的低级烷基磺酰基或 取代或未取代的低级芳基磺酰基等）。

    Staurosporin derivatives
    10.
    发明授权
    Staurosporin derivatives 失效
    星孢菌素衍生物

    公开(公告)号：US06806266B1

    公开(公告)日：2004-10-19

    申请号：US10030618

    申请日：2002-01-11

    Applicant: Fumihiko Kanai ,  Nobuyoshi Amishiro ,  Yushi Kitamura ,  Chikara Murakata ,  Tadakazu Akiyama ,  Shiro Akinaga ,  Eiichi Fuse ,  Takashi Kuwabara ,  Kenichi Yasoshima

    Inventor： Fumihiko Kanai ,  Nobuyoshi Amishiro ,  Yushi Kitamura ,  Chikara Murakata ,  Tadakazu Akiyama ,  Shiro Akinaga ,  Eiichi Fuse ,  Takashi Kuwabara ,  Kenichi Yasoshima

    IPC: C07D49822

    CPC classification number: C07D498/22 ,  A61K31/553

    Abstract: The present invention provides an antitumor agent comprising a staurosporin derivative or a pharmaceutically acceptable salt thereof, as an active ingredient, which is represented by the general formula (I): wherein R1 represents hydrogen, hydroxy or lower alkoxy, R2 and R3 are the same or different and represent hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted aryl, a substituted or unsubstituted heterocyclic group, halogen, nitro, formyl, etc., R4 represents hydrogen, etc., R5 represents NR11AR12A (wherein R11A and R12A represent hydrogen, substituted or unsubstituted lower alkyl, etc.), provided that R2 and R3 are not simultaneously hydrogen.

    Abstract translation: 本发明提供包含星形孢菌素衍生物或其药学上可接受的盐作为活性成分的抗肿瘤剂，其由通式（I）表示：其中R 1表示氢，羟基或低级烷氧基，R 2 和R 3相同或不同，表示氢，取代或未取代的烷基，取代或未取代的低级烯基，取代或未取代的低级炔基，取代或未取代的芳基，取代或未取代的杂环基，卤素，硝基，甲酰基， 等等，R 4表示氢等，R 5表示NR 11A R 12A（其中R 11A和R 12A表示氢，取代或未取代的低级烷基等）， 条件是R 2和R 3不同时为氢。

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