公开(公告)号：US20120208813A1

公开(公告)日：2012-08-16

申请号：US13407520

申请日：2012-02-28

申请人： Natsuki ISHIZUKA ,  Takashi SASATANI ,  Yoshiharu HIRAMATSU ,  Masanao INAGAKI ,  Masahide ODAN ,  Hiroshi HASHIZUMI ,  Susumu MITSUMORI ,  Yasuhiko FUJII ,  Yoshikazu FUKUI ,  Hideaki WATANABE ,  Jun SATO

发明人： Natsuki ISHIZUKA ,  Takashi SASATANI ,  Yoshiharu HIRAMATSU ,  Masanao INAGAKI ,  Masahide ODAN ,  Hiroshi HASHIZUMI ,  Susumu MITSUMORI ,  Yasuhiko FUJII ,  Yoshikazu FUKUI ,  Hideaki WATANABE ,  Jun SATO

IPC分类号： A61K31/435 ,  C07D495/04 ,  A61K31/4365 ,  A61P17/00 ,  A61K31/496 ,  A61K31/506 ,  C07D413/12 ,  A61K31/5377 ,  C07D221/04 ,  C07D401/12

CPC分类号： C07D213/82

摘要： The present invention provides compounds having an agonistic activity to the cannabinoid receptor, which is represented by the formula (I): wherein R1, R2, R3, R4, and G are defined as herein, a pharmaceutically acceptable salt or a solvate thereof, and pharmaceutical compositions, atopic dermatitis treating agents, and anti-pruritus agents, especially anti-pruritus agents for oral used and for external application, which each contains the said compound as an active ingredient.

摘要翻译： 本发明提供对大麻素受体具有激动作用的化合物，其由式（I）表示：其中R 1，R 2，R 3，R 4和G如本文所定义，其药学上可接受的盐或溶剂合物，以及 药物组合物，特应性皮炎治疗剂和抗瘙痒剂，特别是用于口服和外用的抗瘙痒剂，其各自含有所述化合物作为活性成分。

公开(公告)号：US20120135978A1

公开(公告)日：2012-05-31

申请号：US13308483

申请日：2011-11-30

申请人： Masanao INAGAKI ,  Shin-ichiro Hara ,  Nobuhiro Haga ,  Yoshinori Tamura ,  Yoshihisa Goto ,  Tsuyoshi Hasegawa

发明人： Masanao INAGAKI ,  Shin-ichiro Hara ,  Nobuhiro Haga ,  Yoshinori Tamura ,  Yoshihisa Goto ,  Tsuyoshi Hasegawa

IPC分类号： A61K31/485 ,  A61K31/5377 ,  A61K31/506 ,  A61P25/04 ,  A61K31/519 ,  C07D491/18 ,  A61P1/08 ,  A61P1/00 ,  C07D489/08 ,  C07D491/22

CPC分类号： C07D489/08

摘要： A novel compound which is useful as an agent for treating and/or preventing emesis, vomiting and/or constipation.A compound represented by the formula (I): wherein R1 and R2 are each independently hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted cycloalkyl, optionally substituted aryl etc., R3 is hydrogen, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkynyl, optionally substituted lower alkoxy etc., R4 is hydrogen or lower alkyl, R5 is hydrogen, lower alkyl, cycloalkyl lower alkyl or lower alkenyl, or a pharmaceutically acceptably salt, or a solvate thereof is provided.

摘要翻译： 可用作治疗和/或预防呕吐，呕吐和/或便秘的药剂的新型化合物。 由式（I）表示的化合物：其中R 1和R 2各自独立地为氢，任选取代的低级烷基，任选取代的低级烯基，任选取代的环烷基，任选取代的芳基等，R 3为氢，羟基，任选取代的低级烷基， 提供任选取代的低级烯基，任选取代的低级炔基，任选取代的低级烷氧基等，R4是氢或低级烷基，R5是氢，低级烷基，环烷基低级烷基或低级烯基，或其药学上可接受的盐或其溶剂化物 。