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    Carboxamide derivatives having tetrazole and thiazole rings and their use
    1.
    发明授权
    Carboxamide derivatives having tetrazole and thiazole rings and their use 失效
    具有四唑和噻唑环的羧甲酰胺衍生物及其用途

    公开(公告)号：US4946855A

    公开(公告)日：1990-08-07

    申请号：US276953

    申请日：1988-11-28

    申请人： Junji Yoshinaga ,  Takeshi Shogaki ,  Takao Kakita ,  Hiromi Ozeki ,  Yoshiko Kato

    发明人： Junji Yoshinaga ,  Takeshi Shogaki ,  Takao Kakita ,  Hiromi Ozeki ,  Yoshiko Kato

    IPC分类号： C07D417/12 ,  C07D417/14

    CPC分类号： C07D417/12 ,  C07D417/14

    摘要： A compound of the formula: ##STR1## wherein the free valency of the groups A-, R- and --X--Y-- is attached to any of 2-, 4- and 5- positions of the thiazol ring, A is a C.sub.1-6 alkyl group, an aryl group which is unsubstituted or substituted with at least one substituent selected from the group consisting of hydroxy C.sub.1-6 alkoxy, aryl-(C.sub.1-6)alkoxy, halo-(C.sub.1-6)alkyl, halogen, and nitro,or 5- or 6-membered heterocyclic group containing at least one hetero atom selected from oxygen, nitrogen and sulfur, or a condensed heterocyclic group consisting of a heterocycle as defined above and a benzene nucleus, these two heterocyclic groups being unsubstituted or substituted with at least one substituent selected from halogen,R is hydrogen or a C.sub.1-6 alkyl group,X is --CO--or --NH--, andY is --NH--or --CO--, with the proviso that(a) X and Y cannot be the same group, and(b) when X is --CO--and Y is --NH--, the group --X--Y--is attached to 2- or 5-position,or a pharmaceutically acceptable salt thereof are nobel and useful as antiallergic.

    Process for preparation of voglibose
    2.
    发明申请
    Process for preparation of voglibose 审中-公开
    伏格列博糖的制备方法

    公开(公告)号：US20050165257A1

    公开(公告)日：2005-07-28

    申请号：US10509059

    申请日：2002-10-15

    申请人： Takeshi Shogaki ,  Takao Kakita ,  Suguru Yagi

    发明人： Takeshi Shogaki ,  Takao Kakita ,  Suguru Yagi

    IPC分类号： C07C213/00 ,  C07C213/02 ,  C07C215/44 ,  C07C217/52

    CPC分类号： C07C217/52 ,  C07C213/00 ,  C07C213/02 ,  C07C2601/14 ,  Y02P20/55 ,  C07C215/44

    摘要： A process capable of conveniently preparing voglibose at a low cost in a safe process, and an intermediate which can be suitably used in the process and a process for preparing the intermediate are provided. An inositol derivative represented by the formula (VI): wherein Prt is a protecting group of hydroxyl group; a process for preparing the inositol derivative, wherein a cyclohexanone compound represented by the formula (IV): wherein Prt is as defined above, is dihydroxyaminated using a dihydroxyaminating agent and a reducing agent; and a process for preparing voglibose represented by the formula (VIII): wherein the inositol derivative is oxidized to give an inositol compound, and the protecting group, Prt of the inositol compound is deprotected.

    摘要翻译： 提供了一种能够在安全的方法中以低成本方便地制备伏格列波糖的方法，以及可以在该方法中适当使用的中间体和制备该中间体的方法。 由式（VI）表示的肌醇衍生物：其中Prt是羟基的保护基; 制备肌醇衍生物的方法，其中由式（IV）表示的环己酮化合物：其中Prt如上所定义，使用二羟基胺化剂和还原剂进行二羟基胺化; 以及由式（VIII）表示的伏格列溴糖的制备方法：其中所述肌醇衍生物被氧化得到肌醇化合物，肌醇化合物的保护基Prt被去保护。

    Carbostyril derivatives and antiallergic agent
    3.
    发明授权
    Carbostyril derivatives and antiallergic agent 失效
    卡波他汀衍生物和抗过敏剂

    公开(公告)号：US5457099A

    公开(公告)日：1995-10-10

    申请号：US81021

    申请日：1993-06-22

    申请人： Takeshi Shogaki ,  Hiromu Toyoda ,  Takao Kakita ,  Masumi Furukawa ,  Seiichi Nakatsugi ,  Emi Masai ,  Tsuyako Yashima ,  Ikuo Ueda

    发明人： Takeshi Shogaki ,  Hiromu Toyoda ,  Takao Kakita ,  Masumi Furukawa ,  Seiichi Nakatsugi ,  Emi Masai ,  Tsuyako Yashima ,  Ikuo Ueda

    IPC分类号： A61K31/47 ,  C07D215/22 ,  C07D215/227 ,  C07D401/06 ,  C07D401/14 ,  C07D407/12 ,  C07D409/14

    CPC分类号： C07D215/227 ,  A61K31/47 ,  C07D401/06 ,  C07D401/14 ,  C07D407/12 ,  C07D409/14

    摘要： 1. A compound of the formula: ##STR1## wherein the symbol of a solid line with a broken line means a single bond or a double bond,R and R' are independently selected from the group consisting of hydrogen atom, halogen atom, lower alkyl, nitro, unsubstituted amino and substituted amino,A and B are independently selected from the group consisting of hydrogen atom, lower alkyl optionally substituted with a lower cycloalkyl, aryl optionally substituted with one or more halogen atoms and the group: -Y-R.sup.2wherein Y is lower alkylene and R.sup.2 is the group: ##STR2## wherein m is integer of 1 to 3, n is 0 or 1, Z is >N-, >CH-- or >C=, R.sup.3 is diaryl (lower) alkyl optionally substituted with one or more halogen atoms or is condensed heterocyclic group optionally substituted with oxo, with the proviso that(a) at least one of A and B is the group -Y-R.sup.2 and(b) when A is hydrogen atom and B is the group -Y-R.sup.2, then Z is >CH-- or >C= if R.sup.3 is condensed heterocyclic group optionally substituted with oxo and n is Oor a pharmaceutically acceptable salt thereof. The compounds of the above formula have antiallergic activity.

    摘要翻译： 1.下式的化合物：其中虚线的实线的符号表示单键或双键，R和R'独立地选自氢原子，卤原子，低级 烷基，硝基，未取代的氨基和取代的氨基，A和B独立地选自氢原子，任选被低级环烷基取代的低级烷基，任选被一个或多个卤素原子取代的基团和-Y-R 2 其中Y为低级亚烷基且R2为基团：其中m为1至3的整数，n为0或1，Z为> N-，> CH-或> C =，R3为二芳基（低级）烷基 任选地被一个或多个卤素原子取代或是被氧代取代的稠合杂环基，条件是（a）A和B中的至少一个是基团-Y-R 2和（b）当A是氢原子和B 是基团-Y-R 2，则Z是> CH-或> C =，如果R 3是任选被氧代a取代的稠合杂环基 nd n是O或其药学上可接受的盐。 上述化合物具有抗过敏活性。