公开(公告)号：US20120101068A1

公开(公告)日：2012-04-26

申请号：US13382011

申请日：2010-07-08

申请人： Yasushi Kohno ,  Kiyoshi Fujii ,  Momoko Taru ,  Keita Miyoshi

发明人： Yasushi Kohno ,  Kiyoshi Fujii ,  Momoko Taru ,  Keita Miyoshi

IPC分类号： A61K31/661 ,  C07F9/38 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P19/04 ,  A61P35/00 ,  A61P31/16 ,  A61P31/14 ,  A61P9/10 ,  A61P7/00 ,  A61P27/02 ,  A61P29/00 ,  A61P9/04 ,  A61P7/02 ,  A61P9/06 ,  A61P27/06 ,  A61P37/00 ,  C07F9/09

CPC分类号： A61K31/662 ,  C07F9/091 ,  C07F9/3808 ,  C07F9/4006 ,  C07F9/4015

摘要： Provided are diphenyl sulfide derivatives which have excellent S1P3 antagonistic activity and are useful as drugs. Intensive studies have been made for the purpose of creating a compound having S1P3 antagonistic activity. As a result of the intensive studies, it has been found that diphenyl sulfide derivatives represented by general formula (1) have excellent S1P3 antagonistic activity. In general formula (1), R1 is a hydrogen atom or the like; R2 is an optionally substituted alkyl group having 1 to 6 carbon atoms, or the like; X is a methylene group which may be substituted with one or two fluorine atoms, or the like; Y is a hydrogen atom or the like; and Z is a halogen atom.

摘要翻译： 提供具有优异的S1P3拮抗活性并可用作药物的二苯硫醚衍生物。 为了制备具有S1P3拮抗活性的化合物，已进行了深入研究。 作为深入研究的结果，已经发现由通式（1）表示的二苯硫醚衍生物具有优异的S1P3拮抗活性。 通式（1）中，R 1为氢原子等; R2是任选取代的碳原子数为1〜6的烷基等; X是可被一个或两个氟原子取代的亚甲基等; Y是氢原子等; Z为卤素原子。

公开(公告)号：US08569270B2

公开(公告)日：2013-10-29

申请号：US13382011

申请日：2010-07-08

申请人： Yasushi Kohno ,  Kiyoshi Fujii ,  Momoko Taru ,  Keita Miyoshi

发明人： Yasushi Kohno ,  Kiyoshi Fujii ,  Momoko Taru ,  Keita Miyoshi

IPC分类号： A61K31/663 ,  C07F9/09

CPC分类号： A61K31/662 ,  C07F9/091 ,  C07F9/3808 ,  C07F9/4006 ,  C07F9/4015

摘要： Provided are diphenyl sulfide derivatives which have excellent S1P3 antagonistic activity and are useful as drugs. Intensive studies have been made for the purpose of creating a compound having S1P3 antagonistic activity. As a result of the intensive studies, it has been found that diphenyl sulfide derivatives represented by general formula (1) have excellent S1P3 antagonistic activity. In general formula (1), R1 is a hydrogen atom or the like; R2 is an optionally substituted alkyl group having 1 to 6 carbon atoms, or the like; X is a methylene group which may be substituted with one or two fluorine atoms, or the like; Y is a hydrogen atom or the like; and Z is a halogen atom.

摘要翻译： 提供具有优异的S1P3拮抗活性并可用作药物的二苯硫醚衍生物。 为了制备具有S1P3拮抗活性的化合物，已进行了深入研究。 作为深入研究的结果，已经发现由通式（1）表示的二苯硫醚衍生物具有优异的S1P3拮抗活性。 通式（1）中，R 1为氢原子等; R2是任选取代的碳原子数为1〜6的烷基等; X是可被一个或两个氟原子取代的亚甲基等; Y是氢原子等; Z为卤素原子。

公开(公告)号：US20120142932A1

公开(公告)日：2012-06-07

申请号：US13386698

申请日：2010-09-07

申请人： Koji Kawamura ,  Keita Miyoshi ,  Emi Kobayashi

发明人： Koji Kawamura ,  Keita Miyoshi ,  Emi Kobayashi

IPC分类号： C07D401/12

CPC分类号： C07D401/12

摘要： A novel method for manufacturing 5-methyl-2-(piperidin-4-ylamino)pyridine is established. This method can be used as an industrial manufacturing method to produce a 4-(5-methylpyridin-2-ylamino)piperidine-1-carboxylic acid derivative represented by the general formula, (wherein R represents a linear or branched alkyl group having 1 to 6 carbon atoms or an aralkyl group having 7 to 12 carbon atoms) in a reaction solution having an aromatic monocyclic hydrocarbon as a reaction medium, in the presence of sodium triacetoxyborohydride as a reducing agent, or after adding sodium borohydride and acetic acid to the reaction solution in advance.

摘要翻译： 建立了一种制备5-甲基-2-（哌啶-4-基氨基）吡啶的新方法。 该方法可以用作工业制造方法来制备由通式表示的4-（5-甲基吡啶-2-基氨基）哌啶-1-羧酸衍生物（其中R表示具有1〜 6个碳原子或具有7〜12个碳原子的芳烷基）在具有芳香族单环烃作为反应介质的反应溶液中，在三乙酰氧基硼氢化钠作为还原剂的存在下，或在将硼氢化钠和乙酸加入反应中 提前解决。