公开(公告)号：US07122173B2

公开(公告)日：2006-10-17

申请号：US10473348

申请日：2002-03-29

Applicant: Tsuyoshi Yamagata ,  Kaoru Atsuki ,  Tetsuji Ohno ,  Shiro Shirakura ,  Akira Karasawa ,  William C. de Groat ,  Naoki Yoshimura ,  Adrian Sculptoreanu

Inventor： Tsuyoshi Yamagata ,  Kaoru Atsuki ,  Tetsuji Ohno ,  Shiro Shirakura ,  Akira Karasawa ,  William C. de Groat ,  Naoki Yoshimura ,  Adrian Sculptoreanu

IPC: A61K10/00 ,  A61K49/00

CPC classification number: A61K31/55 ,  A61K31/38 ,  A61K31/44

Abstract: The present invention provides an agent for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia, comprising, as an active ingredient, a compound having a slowly-inactivating A-type K+ channel opening activity or a pharmaceutically acceptable salt thereof, and a method for screening agents for the treatment of bladder irritative symptoms accompanied by benign prostatic hyperplasia, comprising measuring a slowly-inactivating A-type K+ channel opening activity as an index.

公开(公告)号：US20060160887A1

公开(公告)日：2006-07-20

申请号：US10562635

申请日：2004-07-16

Applicant: Tsuyoshi Yamagata ,  Shiro Shirakura

Inventor： Tsuyoshi Yamagata ,  Shiro Shirakura

IPC: A61K31/381

CPC classification number: C07D495/04 ,  A61K31/137 ,  A61K31/216 ,  A61K31/38 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention provides a pharmaceutical composition which is useful in the treatment for overactive bladder and the like, and comprises 3,3,3-trifluoro-2-hydroxy-2-methyl-N-(5,5,10-trioxo-4,10-d ihydrothieno[3,2-c][1]benzothiepin-9-yl)propanamide or a pharmaceutically acceptable salt thereof, and an anticholinergic agent.

Abstract translation: 本发明提供一种药物组合物，其可用于治疗膀胱过度活动症等，并且包含3,3,3-三氟-2-羟基-2-甲基-N-（5,5,10-三氧代-4 ，10-二氢噻吩并[3,2-c] [1]苯并硫代-9-基）丙酰胺或其药学上可接受的盐，和抗胆碱剂。

公开(公告)号：US07354949B2

公开(公告)日：2008-04-08

申请号：US10472148

申请日：2002-03-29

Applicant: Tsuyoshi Yamagata ,  Kaoru Atsuki ,  Tetsuji Ohno ,  Shiro Shirakura ,  Akira Karasawa

Inventor： Tsuyoshi Yamagata ,  Kaoru Atsuki ,  Tetsuji Ohno ,  Shiro Shirakura ,  Akira Karasawa

IPC: A61K31/38 ,  A61K31/44 ,  A61K31/42

CPC classification number: C07D495/04 ,  A61K31/55

Abstract: The present invention provides a therapeutic agent for bladder irritative symptoms associated with benign prostatic hyperplasia comprising, as an active ingredient, a tricyclic compound represented by formula (I): [wherein R1 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy or halogen; X1-X2-X3 represents CR5═CR6—CR7═CR8, N(O)m═CR6—CR7═CR8, CR5═CR6—N(O)m═CR8, CR5═CR6—CR7═N(O)m, CR5═CR6—O, CR5═CR6—S, O—CR7═CR8, S—CR7═CR8 or O—CR7═N; Y represents 13 CH2S—, —CH2SO—, —CH2SO2—, —CH2O—, —CH═CH—, —(CH2)p—, —SCH2—, —SOCH2—, —SO2CH2— or —OCH2—; and R2 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted lower alkoxy, amino, mono(substituted or unsubstituted lower alkyl)-substituted amino, di(substituted or unsubstituted lower alkyl)-substituted amino, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted aralkylamino, substituted or unsubstituted arylamino or a substituted or unsubstituted heteroalicyclic group] or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20070149555A1

公开(公告)日：2007-06-28

申请号：US10594684

申请日：2005-03-30

Applicant: Hiroshi Kase ,  Isami Takahashi ,  Shunji Kunori ,  Minoru Kobayashi ,  Shizuo Shiozaki ,  Shiro Shirakura

Inventor： Hiroshi Kase ,  Isami Takahashi ,  Shunji Kunori ,  Minoru Kobayashi ,  Shizuo Shiozaki ,  Shiro Shirakura

IPC: A61K31/522

CPC classification number: A61K31/522 ,  C07D473/06 ,  Y02A50/401

Abstract: A prophylactic and/or therapeutic agent for diseases accompanied by chronic musculoskeletal pain comprising as an active ingredient a compound having an adenosine A2A receptor antagonistic action, for example, represented by the following formula (I) (wherein R1, R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl, lower alkenyl or lower alkynyl; R4 represents cycloalkyl, —(CH2)n—R5 or the following formula (II); and X1 and X2 are the same or different, each representing an oxygen atom or a sulfur atom) or a pharmaceutically acceptable salt thereof.

Abstract translation: 一种伴有慢性肌肉骨骼疼痛的疾病的预防和/或治疗剂，其包含作为活性成分的具有腺苷A 2A受体拮抗作用的化合物，例如由下式（I）表示的化合物（其中 R 1，R 2和R 3相同或不同，各自表示氢原子，低级烷基，低级烯基或低级炔基; R 4表示环烷基， - （CH 2）n - R 5 -R 5或下式（II）; 和X 1和X 2相同或不同，各自表示氧原子或硫原子）或其药学上可接受的盐。

公开(公告)号：US20110105465A1

公开(公告)日：2011-05-05

申请号：US12994923

申请日：2009-05-29

Applicant: Jun Ouchi ,  Shunji Kunori ,  Yozo Kojima ,  Katsumi Shinoda ,  Katsutoshi Sasaki ,  Shiro Shirakura

Inventor： Jun Ouchi ,  Shunji Kunori ,  Yozo Kojima ,  Katsumi Shinoda ,  Katsutoshi Sasaki ,  Shiro Shirakura

IPC: A61K31/55 ,  A61K31/506 ,  A61K31/519 ,  A61K31/522 ,  A61K31/505 ,  A61K31/4355 ,  A61K31/485 ,  A61K31/439 ,  A61K31/445 ,  A61K31/4245 ,  A61K31/4192 ,  A61K31/425 ,  A61P25/04

CPC classification number: C07D417/14 ,  A61K31/343 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/485 ,  A61K31/506 ,  A61K31/519 ,  A61K31/52 ,  A61K31/522 ,  A61K45/06 ,  C07D417/04 ,  C07D473/06 ,  C07D473/34 ,  C07D487/04 ,  C07D487/14 ,  A61K2300/00

Abstract: Provided are: an agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), which comprises a compound having adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof as an active ingredient; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance or constipation; the agent for suppressing an undesirable effect of an opioid-type analgesic (opioid), wherein the undesirable effect of the opioid-type analgesic (opioid) is analgesic tolerance; and the like.

Abstract translation: 提供：包含具有腺苷A 2A受体拮抗作用的化合物或其药学上可接受的盐作为活性成分的阿片类止痛剂（阿片样物质）的不良作用的药剂。 用于抑制阿片样镇痛药（阿片样物质）的不良作用的药剂，其中阿片类镇痛药（阿片样物质）的不良作用是镇痛耐受性或便秘性; 用于抑制阿片样镇痛药（阿片样物质）的不良作用的药剂，其中阿片类镇痛药（阿片样物质）的不良作用是止痛耐受性; 等等。

公开(公告)号：US20090181948A1

公开(公告)日：2009-07-16

申请号：US11814944

申请日：2006-01-31

Applicant: Setsuya Sasho ,  Takashi Seishi ,  Eri Atsumi ,  Mariko Osakada ,  Ryo Hirose ,  Shinichiro Toki ,  Katsuyoshi Tsukii ,  Shiro Shirakura

Inventor： Setsuya Sasho ,  Takashi Seishi ,  Eri Atsumi ,  Mariko Osakada ,  Ryo Hirose ,  Shinichiro Toki ,  Katsuyoshi Tsukii ,  Shiro Shirakura

IPC: A61K31/55 ,  C07D401/12 ,  C07D413/14 ,  A61K31/5377 ,  A61P37/08

CPC classification number: C07D295/13 ,  C07D211/26 ,  C07D211/58 ,  C07D233/20 ,  C07D233/26 ,  C07D233/36 ,  C07D233/48 ,  C07D233/52 ,  C07D235/16 ,  C07D239/06 ,  C07D295/145 ,  C07D401/06 ,  C07D401/14 ,  C07D417/06

Abstract: The present invention provides a diamine derivative or the like represented by the general formula (I): {wherein Q represents an oxygen atom or the like, RG represents a hydrogen atom or the like, RI represents (wherein p and r may be the same or different, and each represents 0 or the like, RA represents a hydrogen atom or the like, and RB and RC may be the same or different, and each represents a hydrogen atom or the like), RH represents a hydrogen atom or the like, and RJ represents: (wherein q and s may be the same or different, and each represents 0 or the like, RD represents a hydrogen atom or the like, and RE and RF may be the same or different, and each represents a hydrogen atom or the like) or the like}, etc.

Abstract translation: 本发明提供由通式（I）表示的二胺衍生物等：其中Q表示氧原子等，RG表示氢原子等，RI表示（其中p和r可以相同 或不同，各自表示0等，RA表示氢原子等，RB和RC可以相同或不同，表示氢原子等），RH表示氢原子等 ，并且RJ表示：（其中q和s可以相同或不同，并且各自表示0等，RD表示氢原子等，RE和RF可以相同或不同，并且各自表示氢 原子等）等}等

公开(公告)号：US07276532B2

公开(公告)日：2007-10-02

申请号：US10472143

申请日：2002-03-29

Applicant: Tsuyoshi Yamagata ,  Kaoru Atsuki ,  Tetsuji Ohno ,  Shiro Shirakura ,  Akira Karasawa

Inventor： Tsuyoshi Yamagata ,  Kaoru Atsuki ,  Tetsuji Ohno ,  Shiro Shirakura ,  Akira Karasawa

IPC: A61K31/38

CPC classification number: C07D495/04 ,  A61K31/55 ,  C07D337/12

Abstract: The present invention provides a therapeutic agent for overactive bladder comprising, as an active ingredient, a tricyclic compound represented by formula (I): [wherein R1 represents a hydrogen atom, substituted or unsubstituted lower alkyl, and the like; X1—X2—X3 represents CR5═CR6—CR7═CR8, CR5═CR6—S, and the like; Y represents —CH2S—, —SOCH2—, and the like; and R2 represents a hydrogen atom, and the like] or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明提供一种活性过氧化物的治疗剂，其包含作为活性成分的由式（I）表示的三环化合物：其中R 1表示氢原子，取代或未取代的低级烷基，和 类似; X 1 - 2 - - - - - - - - - - - - - - - - - - （3） CR 7 -CR 8，CR 5 -CR 6 -S等; Y表示-CH 2 -S-，-SOCH 2 - 等; 和R 2表示氢原子等]或其药学上可接受的盐。

公开(公告)号：US20070185168A1

公开(公告)日：2007-08-09

申请号：US11547810

申请日：2005-04-07

Applicant: Haruki Takai ,  Shunji Kunori ,  Shiro Shirakura ,  Katsumi Shinoda ,  Atsuko Mizutani ,  Koji Yamada ,  Shinichiro Toki ,  Tomoyuki Nishikawa

Inventor： Haruki Takai ,  Shunji Kunori ,  Shiro Shirakura ,  Katsumi Shinoda ,  Atsuko Mizutani ,  Koji Yamada ,  Shinichiro Toki ,  Tomoyuki Nishikawa

IPC: A61K31/4439

CPC classification number: C07D409/14

Abstract: For example, a piperidine derivative represented by following formula (I) (wherein, —C(═O)-Z- represents —C(═O)—CH2—, —C(═O)—C(CH3)2—, —C(═O)—NH—, —C(═O)—O—, —C(═O)—S—, —C(═O)—CH2CH2—, —C(═O)—CH═CH—, —C(═O)—CH2O—, —C(═O)—CH2S—, —C(═O)—CH2CH2CH2— or —C(═O)—NR8CH2—; R1 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R2 represents a hydrogen atom or hydroxy; R3 represents a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R5 represents a hydrogen atom, hydroxy, or the like; R6 represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkyl, or the like, etc.; R7 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like; n and k each independently represents an integer of 0 to 2; and ---- represents a single bond, or a double bond together with R4, where in case ---- is a single bond, R4 represents a hydrogen atom, hydroxy, or the like) or a pharmaceutically acceptable salt thereof and the like having an antagonistic activity for a glutamic acid receptor (NR2B/NMDA receptor) of an N-methyl-D-aspartic acid (NMDA) type containing an NR2B subunit are provided.

Abstract translation: 例如，由下式（I）表示的哌啶衍生物（其中，-C（-O）-Z-表示-C（-O）-CH 2 - ， - C（ - -C（= O）-NH-， - C（-O）-O - ， - C（-O） - S - ， - C（-O）-CH 2 CH 2 - ， - C（-O）-CH-CH - ， - C（-O）-CH O - ， - C（-O）-CH 2 S - ， - C（-O）-CH 2 CH 2 2-CH 2 - 或-C（ - ）-NR 8 CH 2 - ; R 1 - SUP>表示氢原子，取代或未取代的低级烷基等; R 2表示氢原子或羟基; R 3表示氢原子，取代或未取代的 低级烷基等; R 5表示氢原子，羟基等; R 6表示氢原子，羟基，取代或未取代的低级烷基，或 R 7表示氢原子，卤素，取代或未取代的低级烷基等; n和k各自独立地表示0〜2的整数;＆lt; U STYLE = “ SINGLE“> ----表示单键，或与R 4连接的双键，其中如果是单键，则R” 对于N-甲基-D-葡萄糖酸的谷氨酸受体（NR2B / NMDA受体）具有拮抗作用的氨基酸或其药学上可接受的盐等） 提供了含有NR2B亚基的天冬氨酸（NMDA）型。