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8 条记录 (耗时 0.017 秒)

    Process for the production of 3-aminoisoxazoles
    1.
    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。

    Process for the production of urea derivatives
    2.
    发明授权
    Process for the production of urea derivatives 失效
    尿素衍生物生产工艺

    公开(公告)号：US4183856A

    公开(公告)日：1980-01-15

    申请号：US895105

    申请日：1978-04-10

    申请人： Yasuo Makisumi ,  Takashi Sasatani ,  Akira Murabayashi

    发明人： Yasuo Makisumi ,  Takashi Sasatani ,  Akira Murabayashi

    IPC分类号： C07D275/02 ,  C07D213/75 ,  C07D261/14 ,  C07D263/48 ,  C07D275/03 ,  C07D277/20 ,  C07D277/38 ,  C07D277/46 ,  C07D277/48 ,  C07D277/82

    CPC分类号： C07D213/75 ,  C07D261/14 ,  C07D275/03 ,  C07D277/48 ,  C07D277/82

    摘要： Urea derivatives of the formula ##STR1## (wherein Ar represents a residue of 5- or 6-membered heteroaromatic ring; R represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.1 represents a C.sub.1 -C.sub.6 alkyl group; and R.sup.2 represents a C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.1 -C.sub.6 alkoxy group) are produced by reacting an amine of the formulaAr--NH--R(wherein Ar and R have the significance given above) with a carbamoyl halogenide of the formula ##STR2## (wherein X represents a halogen atom, and R.sup.1 and R.sup.2 have the significance given above) in the presence of a Lewis acid in an inert solvent.

    摘要翻译： 下式的脲衍生物（其中Ar表示5或6元杂芳环的残基; R表示氢原子或C1-C6烷基; R1表示C1-C6烷基; R2表示 C 1 -C 6烷基，C 2 -C 6烯基或C 1 -C 6烷氧基）通过使式Ar-NH-R（其中Ar和R具有上述含义）具有下式的氨基甲酰卤化物： 图像（其中X表示卤原子，R1和R2具有上述含义）在路易斯酸存在下在惰性溶剂中反应。

    Tetrahydrothiopyrano[2,3-b]indole derivatives
    4.
    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。

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

    公开(公告)号：US4910318A

    公开(公告)日：1990-03-20

    申请号：US633686

    申请日：1984-07-25

    申请人： Yasuo Makisumi ,  Takashi Sasatani

    发明人： Yasuo Makisumi ,  Takashi Sasatani

    IPC分类号： A61K31/40 ,  A61K31/445 ,  A61K31/495 ,  A61P25/04 ,  A61P29/00 ,  C07D209/30 ,  C07D495/04

    CPC分类号： C07D495/04 ,  C07D209/30

    摘要： Tetrahydrothiopyrano[3,2-b]indole derivatives represented by the formula I: ##STR1## wherein R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, phenyl-C.sub.1-4 alkyl, C.sub.2-5 alkanoyl, or ##STR2## wherein Y is C.sub.1-4 alkylene or C.sub.1-4 oxoalkylene and R.sup.5 and R.sup.6 each is hydrogen or C.sub.1-4 alkyl;R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.3-6 cycloalkyl;R.sup.3 is hydrogen, C.sub.1-4 alkyl or ##STR3## wherein Y, R.sup.5 and R.sup.6 each is as defined above; or ##STR4## is pyrrolidino, piperdinyl, piperazinyl, 4-C.sub.1-4 alkylpiperazinyl or morpholino;R.sup.4 is hydrogen or C.sub.1-4 alkyl; andn is 0 or an integer of 1 or 2and the pharmaceutically acceptable salts being useful as analgesic and anti-inflammatory agents as well as psychoanaleptic and nootropic drug.

    摘要翻译： 由式I表示的四氢噻喃并[3,2-b]吲哚衍生物：其中R 1是氢，C 1-4烷基，C 2-4烯基，C 2-4炔基，苯基-C 1-4烷基，C 2-5 烷酰基或者其中Y是C 1-4亚烷基或C 1-4亚氧基亚烷基，R 5和R 6各自是氢或C 1-4烷基; R2是氢，C1-4烷基或C3-6环烷基; R 3是氢，C 1-4烷基或者其中Y，R 5和R 6各自如上所定义; 或是吡咯烷子基，哌啶基，哌嗪基，4-C 1-4烷基哌嗪基或吗啉代; R4是氢或C1-4烷基; 并且n为0或1或2的整数，并且其药学上可接受的盐可用作镇痛和抗炎剂以及精神无菌和益智药。