公开(公告)号：US20110092703A1

公开(公告)日：2011-04-21

申请号：US12672818

申请日：2008-08-08

申请人： Shogo Sakuma ,  Tsuyoshi Endo ,  Noriko Kanakubo ,  Masahiko Arai ,  Toshihiro Takahashi ,  Toshiyasu Imai ,  Kumiko Taguchi ,  Eriko Nakata ,  Nobutaka Mochiduki ,  Masatoshi Ushioda ,  Makoto Tsuda ,  Kazuhide Inoue

发明人： Shogo Sakuma ,  Tsuyoshi Endo ,  Noriko Kanakubo ,  Masahiko Arai ,  Toshihiro Takahashi ,  Toshiyasu Imai ,  Kumiko Taguchi ,  Eriko Nakata ,  Nobutaka Mochiduki ,  Masatoshi Ushioda ,  Makoto Tsuda ,  Kazuhide Inoue

IPC分类号： C07D241/04

CPC分类号： A61K31/495 ,  A61K31/496 ,  C07D241/04 ,  C07D405/12

摘要： A P2X4 receptor antagonist is a compound represented by the formula (I) or a pharmacologically acceptable salt thereof, which is used as a preventive or therapeutic agent for neuropathic pains: Wherein B is aryl or the like that can have a substituent; Y is C1-5 alkylene that can have a double bond; Z is O, S or the like; each of R1, R2 and R3 independently is hydrogen, C1-8 alkyl or the like; R4 is hydrogen, C1-8 alkyl or the like; each of P and Q independently is hydrogen, halogen, C1-8 alkyl or the like; W is C1-8 alkyl or the like; and each of n and m independently is 1 or 2.

摘要翻译： P2X4受体拮抗剂是由式（I）表示的化合物或其药理学上可接受的盐，其用作神经性疼痛的预防或治疗剂：其中B是可以具有取代基的芳基等; Y是可具有双键的C 1-5亚烷基; Z是O，S等; R 1，R 2和R 3各自独立地为氢，C 1-8烷基等; R4是氢，C1-8烷基等; P和Q各自独立地是氢，卤素，C 1-8烷基等; W是C 1-8烷基等; n和m各自独立地为1或2。

公开(公告)号：US08952030B2

公开(公告)日：2015-02-10

申请号：US14343218

申请日：2012-09-07

申请人： Hiroshi Nagase ,  Hideaki Fujii ,  Eriko Nakata ,  Yoshikazu Watanabe ,  Toshihiro Takahashi

发明人： Hiroshi Nagase ,  Hideaki Fujii ,  Eriko Nakata ,  Yoshikazu Watanabe ,  Toshihiro Takahashi

IPC分类号： A61K31/485 ,  C07D491/18 ,  C07D487/08 ,  C07F7/18

CPC分类号： C07D491/18 ,  C07D471/08 ,  C07D471/22 ,  C07D487/08 ,  C07D491/22 ,  C07F7/1804

摘要： A morphinan derivative represented by the following general formula (I): (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like, R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like, R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like, X represents O or CH2, and Y represents C═O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.

摘要翻译： 由以下通式（I）表示的吗啡喃衍生物：（式中，R 1表示氢，C 1-6烷基，环烷基烷基（环烷基部分具有3〜6个碳原子，亚烷基部分具有1〜5个碳原子） ，芳烷基（芳基部分具有6〜10个碳原子，亚烷基部分具有1〜5个碳原子）等，R 2表示氢，C 1-6烷基，C 3-6环烷基，C 6-10芳基，芳烷基（ 芳基部分具有6至10个碳原子，亚烷基部分具有1至5个碳原子）等，R 3，R 4和R 5表示氢，羟基，氨基甲酰基，C 1-6烷氧基，C 6-10芳氧基等，R 6a ，R6b，R7，R8，R9和R10表示氢等，X表示O或CH2，Y表示C = O，SO2，原子键等）或其酸加成盐作为 镇痛药

公开(公告)号：US20140343015A1

公开(公告)日：2014-11-20

申请号：US14343218

申请日：2012-09-07

申请人： Hiroshi Nagase ,  Hideaki Fujii ,  Eriko Nakata ,  Yoshikazu Watanabe ,  Toshihiro Takahashi

发明人： Hiroshi Nagase ,  Hideaki Fujii ,  Eriko Nakata ,  Yoshikazu Watanabe ,  Toshihiro Takahashi

IPC分类号： C07D491/18 ,  C07F7/18 ,  C07D487/08

CPC分类号： C07D491/18 ,  C07D471/08 ,  C07D471/22 ,  C07D487/08 ,  C07D491/22 ,  C07F7/1804

摘要： A morphinan derivative represented by the following general formula (I) (in the formula, R1 represents hydrogen, C1-6 alkyl, cycloalkylalkyl (the cycloalkyl moiety has 3 to 6 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms), aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,R2 represents hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C6-10 aryl, aralkyl (the aryl moiety has 6 to 10 carbon atoms, and the alkylene moiety has 1 to 5 carbon atoms) and the like,R3, R4 and R5 represent hydrogen, hydroxy, carbamoyl, C1-6 alkoxy, C6-10 aryloxy and the like,R6a, R6b, R7, R8, R9, and R10 represent hydrogen and the like,X represents O or CH2, andY represents C═O, SO2, an atomic bond and the like), or an acid addition salt thereof is used as an analgesic.

摘要翻译： 由以下通式（I）表示的吗啡喃衍生物（式中，R 1表示氢，C 1-6烷基，环烷基烷基（环烷基部分具有3〜6个碳原子，亚烷基部分具有1〜5个碳原子） 芳烷基（芳基部分具有6至10个碳原子，亚烷基部分具有1至5个碳原子）等，R 2表示氢，C 1-6烷基，C 3-6环烷基，C 6-10芳基，芳烷基（芳基 部分具有6至10个碳原子，并且亚烷基部分具有1至5个碳原子）等，R3，R4和R5表示氢，羟基，氨基甲酰基，C1-6烷氧基，C6-10芳氧基等，R6a， R6b，R7，R8，R9和R10表示氢等，X表示O或CH2，Y表示C = O，SO2，原子键等）或其酸加成盐作为止痛剂 。