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1. 发明授权

US08865731B2 Inhibitor of analgesic tolerance 有权
标题翻译：止痛耐受抑制剂
公开(公告)号：US08865731B2
公开(公告)日：2014-10-21
申请号：US12994923
申请日：2009-05-29
申请人： Jun Ouchi , Shunji Kunori , Yozo Kojima , Katsumi Shinoda , Katsutoshi Sasaki , Shiro Shirakura
发明人： Jun Ouchi , Shunji Kunori , Yozo Kojima , Katsumi Shinoda , Katsutoshi Sasaki , Shiro Shirakura
IPC分类号： A01N43/90 , A61K31/522 , A61K31/52 , A01N43/64 , A61K31/41 , A01N43/78 , A61K31/425 , A01N43/54 , A61K31/517 , A61K31/519 , C07D471/04 , C07D471/22 , C07D487/04 , C07D473/00 , C07D273/00 , C07D239/02 , C07D249/16 , C07D403/00 , A61K31/4439 , C07D473/34 , C07D473/06 , C07D487/14 , C07D417/04 , C07D417/14 , A61K31/506 , A61K45/06 , A61K31/343 , A61K31/427 , A61K31/485
CPC分类号： 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
摘要： 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.
摘要翻译：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。

2. 发明申请

US20110105465A1 INHIBITOR OF ANALGESIC TOLERANCE 有权
标题翻译：耐药性抑制剂
公开(公告)号：US20110105465A1
公开(公告)日：2011-05-05
申请号：US12994923
申请日：2009-05-29
申请人： Jun Ouchi , Shunji Kunori , Yozo Kojima , Katsumi Shinoda , Katsutoshi Sasaki , Shiro Shirakura
发明人： Jun Ouchi , Shunji Kunori , Yozo Kojima , Katsumi Shinoda , Katsutoshi Sasaki , Shiro Shirakura
IPC分类号： 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分类号： 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
摘要： 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.
摘要翻译：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。

3. 发明申请

US20070185168A1 Piperidine derivatives 审中-公开
标题翻译：哌啶衍生物
公开(公告)号：US20070185168A1
公开(公告)日：2007-08-09
申请号：US11547810
申请日：2005-04-07
申请人： Haruki Takai , Shunji Kunori , Shiro Shirakura , Katsumi Shinoda , Atsuko Mizutani , Koji Yamada , Shinichiro Toki , Tomoyuki Nishikawa
发明人： Haruki Takai , Shunji Kunori , Shiro Shirakura , Katsumi Shinoda , Atsuko Mizutani , Koji Yamada , Shinichiro Toki , Tomoyuki Nishikawa
IPC分类号： A61K31/4439
CPC分类号： C07D409/14
摘要： 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.
摘要翻译：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。

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