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    Condensed imidazopyridine derivatives useful as psychotropic agents
    3.
    发明授权
    Condensed imidazopyridine derivatives useful as psychotropic agents 失效
    用作精神药物的缩合咪唑并吡啶衍生物

    公开(公告)号：US4753951A

    公开(公告)日：1988-06-28

    申请号：US920162

    申请日：1986-10-17

    申请人： Susumu Takada ,  Toshio Fujishita ,  Takashi Sasatani ,  Akira Matsushita ,  Masami Eigyo

    发明人： Susumu Takada ,  Toshio Fujishita ,  Takashi Sasatani ,  Akira Matsushita ,  Masami Eigyo

    IPC分类号： C07D471/04 ,  C07D495/14 ,  A61K31/47 ,  C07D471/14

    CPC分类号： C07D471/04 ,  C07D495/14

    摘要： A compound of the formula: ##STR1## (wherein R is phenyl optionally substituted by one or two members selected from the group consisting of trifluoromethyl, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 alkylthio, nitro, amino C.sub.1 -C.sub.5 alkanoylamino and C.sub.1 -C.sub.5 alkoxycarbonyl or 5- or 6-membered heterocyclic group optionally substituted by one or two members selected from the group consisting of halogen, C.sub.1 -C.sub.5 alkyl and C.sub.1 -C.sub.5 alkoxy,Q is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.10 acyl, C.sub.1 -C.sub.5 alkylsulfonyl or C.sub.6 -C.sub.10 arylsulfonyl, ##STR2## R.sup.1, R.sup.2, R.sup.3, and R.sup.4 each is hydrogen, halogen C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.5 alkoxy or C.sub.1 -C.sub.5 haloalkyl,Q is present on the nitrogen atom of the 1,3 or 5-position, and the dotted line indicates the presence of three double bonds at the position of 2, 3; 3a, 3b; 4, 5 / 1, 3b; 2, 3; 3a, 4 / or 1, 2; 3a, 3b; 4, 5)or its salt, being useful as psychostimulants or anxiolytics, is provided.

    摘要翻译： 下式的化合物：其中R是任选被一个或两个选自三氟甲基，C 1 -C 5烷基，C 1 -C 5烷氧基，C 1 -C 5烷硫基，硝基，氨基， 任选被一个或两个选自卤素，C 1 -C 5烷基和C 1 -C 5烷氧基的成员取代的C 1 -C 5烷酰基氨基和C 1 -C 5烷氧基羰基或5或6元杂环基，Q是氢，C 1 -C 5 烷基，C 1 -C 10酰基，C 1 -C 5烷基磺酰基或C 6 -C 10芳基磺酰基，R 1，R 2，R 3和R 4各自为氢，卤素C 1 -C 5烷基，C 1 -C 5烷氧基或C 1 -C 5烷氧基， C5卤代烷基，Q存在于1,3或5位的氮原子上，虚线表示在2,3,3a，3b; 4,5 / 1,3b的位置存在三个双键 ; 2,3,3a，4 /或1,2; 3a，3b; 4,5）或其盐，可用作精神兴奋剂或抗焦虑剂。

    Tetrahydrothiopyrano[2,3-b]indole derivatives
    6.
    发明授权
    Tetrahydrothiopyrano[2,3-b]indole derivatives 失效
    四氢噻喃并[2,3-b]吲哚衍生物

    公开(公告)号：US4256640A

    公开(公告)日：1981-03-17

    申请号：US39382

    申请日：1979-05-15

    申请人： Yasuo Makisumi ,  Susumu Takada ,  Takashi Sasatani ,  Natsuki Ishizuka

    发明人： Yasuo Makisumi ,  Susumu Takada ,  Takashi Sasatani ,  Natsuki Ishizuka

    IPC分类号： A61K31/40 ,  A61K31/445 ,  A61P25/04 ,  A61P29/00 ,  C07D209/30 ,  C07D495/04

    CPC分类号： C07D495/04 ,  C07D209/30

    摘要： Tetrahydrothiopyrano[2,3-b]indole derivative represented by the formula I: ##STR1## wherein R.sup.1 is hydrogen, alkyl, hydroxyalkyl, alkenyl, aralkyl, aryl, --COR.sup.5 (wherein R.sup.5 is alkyl, alkenyl, aryl or alkoxy) or ##STR2## (wherein Y is alkylene, oxoalkylene, hydroxyalkylene and R.sup.6 and R.sup.7 are each hydrogen or alkyl): R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen, alkyl, hydroxyalkyl, alkenyl, aralkyl, aryl or dialkylaminoalkyl or ##STR3## is pyrrolidino, piperidino, piperazino, 4-alkylpiperazino, 4-arylpiperazino or morpholino; R.sup.4 is hydrogen or alkyl; A is methylene, alkylmethylene, ethylene, alkylethylene; X is hydrogen or one or two groups selected from the group consisting of halogen, alkyl, alkoxy, hydroxy and halogenoalkyl; and n is an integer of 0 to 2 and its pharmaceutically acceptacle salts; synthesized from 2-propargylthioindole or 2-(4-hydroxy-2-butynylthio)-indole; useful as analgesic and anti-inflammatory agent.

    摘要翻译： 由式I表示的四氢噻喃[2,3-b]吲哚衍生物：其中R 1是氢，烷基，羟烷基，烯基，芳烷基，芳基，-COR 5（其中R 5是烷基，烯基，芳基或烷氧基）或 （其中Y是亚烷基，氧代亚烷基，羟基亚烷基，R 6和R 7各自是氢或烷基）：R 2是氢或烷基; R 3是氢，烷基，羟基烷基，烯基，芳烷基，芳基或二烷基氨基烷基，或者是吡咯烷子基，哌啶子基，哌嗪子基，4-烷基哌嗪基，4-芳基哌嗪基或吗啉代; R4是氢或烷基; A是亚甲基，烷基亚甲基，亚乙基，烷基亚乙基; X是氢或选自卤素，烷基，烷氧基，羟基和卤代烷基的一个或两个基团; n为0〜2的整数及其药学上可接受的盐; 由2-炔丙基硫吲哚或2-（4-羟基-2-丁炔硫基） - 吲哚合成; 用作镇痛和抗炎剂。

    Tricyclic indole compounds having an affinity against serotonin receptors
    7.
    发明申请
    Tricyclic indole compounds having an affinity against serotonin receptors 审中-公开
    对5-羟色胺受体具有亲和力的三环吲哚化合物

    公开(公告)号：US20050043387A1

    公开(公告)日：2005-02-24

    申请号：US10947172

    申请日：2004-09-23

    申请人： Yoshikazu Fukui ,  Makoto Adachi ,  Takashi Sasatani

    发明人： Yoshikazu Fukui ,  Makoto Adachi ,  Takashi Sasatani

    IPC分类号： A61P5/28 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D491/06 ,  A61K31/55 ,  A61K31/407 ,  A61K31/454 ,  C07D491/02

    CPC分类号： C07D491/06

    摘要： Having an affinity against serotonine receptors, compound (I) shown below is useful as a therapeutic agent against various kinds of diseases of central nervous systems. (wherein R1 is hydrogen; R2 is hydrogen or lower alkyl; R3 is hydrogen, —COOR12 and so on; R4 is hydrogen, lower alkyl and so on, or R3 and R4 taken together may form ═O or ═S; R5 is hydrogen, or R3 and R5 taken together may form a bond; R6 is hydrogen, —COOR24 and so on; R7 is hydrogen, halogen, lower alkyl and so on; R8 is hydrogen, lower alkyl, cycloalkyl and so on; R9, R10 and R11 are each independently hydrogen, halogen, lower alkyl and so on)

    摘要翻译： 对于5-羟色胺受体具有亲和性，下文所示的化合物（I）可用作抗各种中枢神经系统疾病的治疗剂。 （其中R 1为氢; R 2为氢或低级烷基; R 3为氢，-COOR 12等; R 4为氢，低级烷基等，或R R 3和R 4一起可以形成= O或= S; R 5是氢，或者R 3和R 5一起可以形成键; R 6是氢， COOR 24等; R 7是氢，卤素，低级烷基等; R 8是氢，低级烷基，环烷基等; R 9，R 10和R 10， 11>各自独立地为氢，卤素，低级烷基等）

    Tricyclic indole compounds having affinity for serotonin receptor
    8.
    发明授权
    Tricyclic indole compounds having affinity for serotonin receptor 失效
    对5-羟色胺受体具有亲和力的三环吲哚化合物

    公开(公告)号：US06858640B2

    公开(公告)日：2005-02-22

    申请号：US10312818

    申请日：2001-09-17

    申请人： Yoshikazu Fukui ,  Makoto Adachi ,  Takashi Sasatani

    发明人： Yoshikazu Fukui ,  Makoto Adachi ,  Takashi Sasatani

    IPC分类号： A61P5/28 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P43/00 ,  C07D491/06 ,  A61K31/40 ,  C07D491/044

    CPC分类号： C07D491/06

    摘要： Having an affinity against serotonine receptors, compound (I) shown below is useful as a therapeutic agent against various kinds of diseases of central nervous systems; (wherein R1 is hydrogen; R2 is hydrogen or lower alkyl; R3 is hydrogen, —COOR12 and so on; R4 is hydrogen, lower alkyl and so on, or R3 and R4 taken together may form ═O or ═S; R5 is hydrogen, or R3 and R5 taken together may form a bond; R6 is hydrogen, —COOR24 and so on; R7 is hydrogen, halogen, lower alkyl and so on; R8 is hydrogen, lower alkyl, cycloalkyl and so on; R9, R10 and R11 are each independently hydrogen, halogen, lower alkyl and so on).

    摘要翻译： 对于5-羟色胺受体具有亲和力，下文所示的化合物（I）可用作抗各种中枢神经系统疾病的治疗剂;（其中R 1是氢; R 2是氢或低级烷基; 3>是氢，-COOR 12等; R 4是氢，低级烷基等，或者R 3和R 4一起可以形成= O或= S; R 5 >是氢，或R 3和R 5一起形成键; R 6是氢，-COOR 24等; R 7是氢，卤素，低级烷基等 R 8是氢，低级烷基，环烷基等; R 9，R 10和R 11各自独立地是氢，卤素，低级烷基等）。

    Process for the production of 3-aminoisoxazoles
    9.
    发明授权
    Process for the production of 3-aminoisoxazoles 失效
    生产3-氨基异恶唑的方法

    公开(公告)号：US4200757A

    公开(公告)日：1980-04-29

    申请号：US912252

    申请日：1978-06-05

    申请人： Yasuo Makisumi ,  Akira Murabayashi ,  Takashi Sasatani

    发明人： Yasuo Makisumi ,  Akira Murabayashi ,  Takashi Sasatani

    IPC分类号： C07D261/14 ,  C07D261/08

    CPC分类号： C07D261/14

    摘要： 3-Aminoisoxazoles of the formula: ##STR1## (wherein R is C.sub.1 -C.sub.6 alkyl, phenyl or halo-phenyl) are prepared by reacting a .beta.-ketonitrile of the formula:R--CO--CH.sub.2 CN(wherein R is as defined above) with a compound of the formula:HY(wherein Y is C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkylthio) in the presence of an acid in a solvent to give an iminium salt of the formula: ##STR2## (wherein X is the residue of said acid; R and Y are each as defined above) and further reacting the iminium salt with hydroxylamine in an inert solvent.

    摘要翻译： 下式的3-氨基异恶唑：其中R为C1-C6烷基，苯基或卤素 - 苯基）是通过使下式所示的β-甲酯与下式反应来制备的：式中R-CO-CH 2 CN（其中R如上定义） 与下式的化合物HY（其中Y是C 1 -C 6烷氧基或C 1 -C 6烷硫基）在酸的存在下在溶剂中反应，得到下式的亚铵盐：其中X是 所述酸; R和Y各自如上所定义），并进一步使亚胺盐与羟胺在惰性溶剂中反应。