公开(公告)号：US08536192B2

公开(公告)日：2013-09-17

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： C07D489/00 ,  C07D489/08 ,  A01N43/42 ,  A61K31/44

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 。

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 。

公开(公告)号：US08084460B2

公开(公告)日：2011-12-27

申请号：US11920851

申请日：2006-05-25

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： C07D489/00 ,  C07D489/08 ,  A01N43/42 ,  A61K31/44

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，R 4是氢或低级烷基，R 5是氢，低级烷基，环烷基低级烷基或低级链烯基，或其药学上可接受的盐或溶剂合物 。

公开(公告)号：US20090203723A1

公开(公告)日：2009-08-13

申请号：US11920851

申请日：2006-05-25

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 ,  C07D489/08 ,  A61P1/08

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，R 4是氢或低级烷基，R 5是氢，低级烷基，环烷基低级烷基或低级链烯基，或其药学上可接受的盐或溶剂合物 。