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    6,7-unsaturated-7-carbamoyl substituted morphinan derivative
    1.
    发明授权
    6,7-unsaturated-7-carbamoyl substituted morphinan derivative 有权
    6,7-不饱和-7-氨甲酰基取代的吗啡喃衍生物

    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 。

    6,7-unsaturated-7-carbamoyl substituted morphinan derivative
    2.
    发明申请
    6,7-unsaturated-7-carbamoyl substituted morphinan derivative 有权
    6,7-不饱和-7-氨甲酰基取代的吗啡喃衍生物

    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 。

    6,7-UNSATURATED-7-CARBAMOYL SUBSTITUTED MORPHINAN DERIVATIVE
    3.
    发明申请
    6,7-UNSATURATED-7-CARBAMOYL SUBSTITUTED MORPHINAN DERIVATIVE 有权
    6,7-不饱和的7-羧基取代的摩尔衍生物

    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 。

    6,7-unsaturated-7-carbamoyl substituted morphinan derivative
    4.
    发明授权
    6,7-unsaturated-7-carbamoyl substituted morphinan derivative 有权
    6,7-不饱和-7-氨甲酰基取代的吗啡喃衍生物

    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 。

    Method for producing benzylidene derivatives
    7.
    发明授权
    Method for producing benzylidene derivatives 失效
    亚苄基衍生物的制备方法

    公开(公告)号：US5463052A

    公开(公告)日：1995-10-31

    申请号：US246494

    申请日：1994-05-20

    申请人： Nobuhiro Haga ,  Masanao Inagaki ,  Saichi Matsumoto ,  Susumu Kamata

    发明人： Nobuhiro Haga ,  Masanao Inagaki ,  Saichi Matsumoto ,  Susumu Kamata

    IPC分类号： C07D207/26 ,  C07D265/02 ,  C07D275/02 ,  C07D279/02 ,  C07D281/02 ,  C07D281/18 ,  C07D291/00 ,  C07D291/04 ,  C07D291/06

    CPC分类号： C07D275/02 ,  C07D265/02 ,  C07D291/06 ,  Y02P20/55

    摘要： A selective and high-yield method is described for producing stereoisomeric benzylidene derivatives of the formula III: ##STR1## wherein R.sup.1 and R.sup.2 each independently is lower alkyl, lower alkoxy or halogen; Y is SO.sub.2, SO or CO; --A-- is optionally substituted lower alkylene; --B-- is --CH.sub.2 -- or --O--; or --A-- and --B-- taken together may form optionally substituted phenylene or optionally substituted lower alkenylene; and R is hydrogen, optionally substituted lower alkyl, cycloalkyl, lower alkoxy, hydroxy, optionally substituted aryl, optionally substituted arylalkyl; optionally substituted arylalkyloxy, heterocyclic ring or N-protecting groups, which comprises reacting a compound of the formula I: ##STR2## wherein R.sup.1 and R.sup.2 are as defined above and X is lower alkoxy or halogen with a compound of the formula II: ##STR3## wherein Y, --A--, --B-- and R are as defined above in the presence of a base.

    摘要翻译： 描述了用于制备式III的立体异构亚苄基衍生物的选择性和高产率方法：其中R 1和R 2各自独立地为低级烷基，低级烷氧基或卤素; Y是SO2，SO或CO; -A-是任选取代的低级亚烷基; -B-是-CH 2 - 或-O-; 或-A-和-B-可以一起形成任选取代的亚苯基或任选取代的低级亚烯基; 并且R是氢，任选取代的低级烷基，环烷基，低级烷氧基，羟基，任选取代的芳基，任选取代的芳基烷基; 任选取代的芳基烷氧基，杂环或N-保护基，其包括使式I化合物：其中R 1和R 2如上所定义，X是低级烷氧基或卤素与式II化合物反应： 图像II其中Y，-A-，-B-和R如上所定义，在碱的存在下。

    3-benzylidene-1-carbamoyl-2-pyrrolidone analogues
    8.
    发明授权
    3-benzylidene-1-carbamoyl-2-pyrrolidone analogues 失效
    3-亚苄基-1-氨基甲酰基-2-吡咯烷酮类似物

    公开(公告)号：US5319100A

    公开(公告)日：1994-06-07

    申请号：US33342

    申请日：1993-03-18

    申请人： Susumu Kamata ,  Takeshi Shiota ,  Nobuhiro Haga ,  Toshihiko Okada ,  Hirokuni Jyoyama ,  Saichi Matsumoto

    发明人： Susumu Kamata ,  Takeshi Shiota ,  Nobuhiro Haga ,  Toshihiko Okada ,  Hirokuni Jyoyama ,  Saichi Matsumoto

    IPC分类号： C07D207/36 ,  C07D207/38 ,  C07D261/12 ,  C07D263/40 ,  C07D263/46 ,  C07D275/02 ,  C07D275/03 ,  C07D277/34 ,  C07D207/12

    CPC分类号： C07D275/03 ,  C07D207/36 ,  C07D207/38 ,  C07D261/12 ,  C07D263/40 ,  C07D263/46 ,  C07D277/34

    摘要： The present invention relates to novel 3-benzylidene-1-carbamoyl-2-pyrroridone analogues having advantage anti-inflammatory activities, which is represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is independently hydrogen, alkyl, alkoxy, or halogen; R.sup.3 is hydrogen or acyl; R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, cyano, or halogen; R.sup.5 and R.sup.6 each is independently hydrogen, alkyl, aryl, aralkyl, heterocyclic group, substituted or unsubstituted amino, or OR.sup.7 wherein R.sup.7 is hydrogen, alkyl, aryl, acyl, or aralkyl, or taken together with the adjacent nitrogen atom may form heterocyclic group which may contain N, O, and/or S, and X and Y each is independently O, S, substituted or unsubstituted imino, or substituted or unsubstituted methylene. In more detail, the present invention provides an anti-inflammatory agent which is useful for the treatment of chronic inflammation and has little side effect, e.g., stomach disease.

    摘要翻译： 本发明涉及具有抗炎活性优势的新型3-亚苄基-1-氨基甲酰基-2-吡咯酮类似物，其由下式表示：其中R 1和R 2各自独立地为氢，烷基，烷氧基或卤素 ; R3是氢或酰基; R4是氢，烷基，羟基，烷氧基，氰基或卤素; R 5和R 6各自独立地为氢，烷基，芳基，芳烷基，杂环基，取代或未取代的氨基或OR 7，其中R 7为氢，烷基，芳基，酰基或芳烷基，或与相邻氮原子一起形成杂环基 其可以含有N，O和/或S，X和Y各自独立地为O，S，取代或未取代的亚氨基，或取代或未取代的亚甲基。 更详细地，本发明提供一种抗炎剂，其可用于治疗慢性炎症并且具有很小的副作用，例如胃病。