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    Benzisoxazole derivatives
    2.
    发明授权
    Benzisoxazole derivatives 失效
    苯并异恶唑衍生物

    公开(公告)号：US4217349A

    公开(公告)日：1980-08-12

    申请号：US919221

    申请日：1978-06-26

    申请人： Junki Katsube ,  Tsuyoshi Kobayashi ,  Katsumi Tamoto ,  Yoshiaki Takebayashi ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

    发明人： Junki Katsube ,  Tsuyoshi Kobayashi ,  Katsumi Tamoto ,  Yoshiaki Takebayashi ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

    IPC分类号： C07D261/20 ,  A61K31/535 ,  C07D413/06

    CPC分类号： C07D261/20

    摘要： Novel benzisoxazole compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, ar(C.sub.1 -C.sub.3)alkoxy or halogen or, when taken together, they form C.sub.1 -C.sub.2 alkylenedioxy, Alk is C.sub.1 -C.sub.4 alkylene and A is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each C.sub.1 -C.sub.4 alkyl or, when taken together with the adjacent nitrogen atom, they represent a 5-6 membered nitrogen-containing heterocyclic ring which may contain any additional hetero atom and R.sub.5 is C.sub.1 -C.sub.4 alkyl or aryl), and non-toxic salts thereof, which possess various pharmaceutical activities.

    摘要翻译： 新的苯并恶唑化合物，其结构式如下：其中R 1和R 2各自为氢，C 1 -C 4烷基，C 1 -C 4烷氧基，芳（C 1 -C 3）烷氧基或卤素，或者一起形成C 1 -C 2亚烷基二氧基， Alk是C 1 -C 4亚烷基，A是下式的基团：其中R 3和R 4各自是C 1 -C 4烷基，或者当与相邻的氮原子一起时，它们代表5-6元含氮的 可含有任何另外的杂原子的杂环，R 5为C 1 -C 4烷基或芳基）及其无毒盐，其具有各种药物活性。

    3-(Piperazinoalkyl)-benz-2,1-isoxazoles
    3.
    发明授权
    3-(Piperazinoalkyl)-benz-2,1-isoxazoles 失效
    3-（哌嗪基烷基） - 苯并-2,1 - 异恶唑

    公开(公告)号：US4122176A

    公开(公告)日：1978-10-24

    申请号：US755139

    申请日：1976-12-29

    申请人： Junki Katsube ,  Tsuyoshi Kobayashi ,  Katsumi Tamoto ,  Yoshiaki Takebayashi ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

    发明人： Junki Katsube ,  Tsuyoshi Kobayashi ,  Katsumi Tamoto ,  Yoshiaki Takebayashi ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

    IPC分类号： C07D261/20 ,  A61K31/495 ,  C07D413/06 ,  C07D413/14

    CPC分类号： C07D261/20 ,  Y10S514/826

    摘要： Novel benzisoxazole compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, ar(C.sub.1 14 C.sub.3) alkoxy or halogen or, when taken together, they form C.sub.1 -C.sub.2 alkylenedioxy, Alk is C.sub.1 -C.sub.4 alkylene and A is a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each C.sub.1 -C.sub.4 alkyl or, when taken together with the adjacent nitrogen atom, they represent a 5-6 membered nitrogen-containing heterocyclic ring which may contain any additional hetero atom and R.sub.5 is C.sub.1 -C.sub.4 alkyl or aryl), and non-toxic salts thereof, which possess various pharmaceutical activities.

    摘要翻译： 下式的新型苯并异恶唑化合物：其中R 1和R 2各自为氢，C 1 -C 4烷基，C 1 -C 4烷氧基，芳（C 11 43 C 3）烷氧基或卤素，或者当它们一起形成C 1 -C 2亚烷基二氧基，Alk 是C 1 -C 4亚烷基，A是下式的基团：其中R 3和R 4各自是C 1 -C 4烷基，或者当与相邻的氮原子一起时，它们代表5-6元含氮杂环 可以含有任何另外的杂原子的环，R 5是C 1 -C 4烷基或芳基）及其无毒盐，其具有各种药物活性。

    N-substituted heterocyclic derivatives and preparation thereof
    6.
    发明授权
    N-substituted heterocyclic derivatives and preparation thereof 失效
    N-取代的杂环衍生物及其制备

    公开(公告)号：US4080328A

    公开(公告)日：1978-03-21

    申请号：US484274

    申请日：1974-06-28

    申请人： Isamu Maruyama ,  Masaru Nakao ,  Kikuo Sasajima ,  Shigeho Inaba ,  Izumi Yanagihara ,  Hisao Yamamoto

    发明人： Isamu Maruyama ,  Masaru Nakao ,  Kikuo Sasajima ,  Shigeho Inaba ,  Izumi Yanagihara ,  Hisao Yamamoto

    IPC分类号： C07D401/04

    摘要： Novel N-substituted heterocyclic derivatives represented by the formula, ##STR1## wherein R is hydrogen or lower alkanoyl; R.sub.1 is hydrogen, lower alkyl, lower alkoxy, halogen, nitro, trifluoromethyl, amino or N-lower alkanoylamino; R.sub.2 is hydrogen, halogen, amino or N-lower alkanoylamino; W is oxygen, sulfur, sulfinyl or sulfonyl; and Y is ##STR2## (wherein R.sub.3 is hydrogen, lower alkyl or lower alkanoyl; and R.sub.4 is hydrogen, halogen or lower alkyl), and pharmaceutically acceptable salts thereof, which have excellent anti-inflammatory, analgesic, sedative, anti-convulsive or anti-hypertensive activities.

    摘要翻译： 由下式表示的新型N-取代的杂环衍生物，其中R是氢或低级烷酰基; R 1是氢，低级烷基，低级烷氧基，卤素，硝基，三氟甲基，氨基或N-低级烷酰基氨基; R2是氢，卤素，氨基或N-低级烷酰氨基; W是氧，硫，亚磺酰基或磺酰基; （其中R3为氢，低级烷基或低级烷酰基，R4为氢，卤素或低级烷基）及其药学上可接受的盐，其具有优异的抗炎，止痛，镇静作用 ，抗惊厥或抗高血压活动。

    N-(.omega.-Amino)alkylaniline derivatives
    8.
    发明授权
    N-(.omega.-Amino)alkylaniline derivatives 失效
    N - （{107 - 氨基）烷基苯胺衍生物

    公开(公告)号：US4017624A

    公开(公告)日：1977-04-12

    申请号：US603240

    申请日：1975-08-08

    申请人： Isamu Maruyama ,  Masaru Nakao ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

    发明人： Isamu Maruyama ,  Masaru Nakao ,  Kikuo Sasajima ,  Shigeho Inaba ,  Hisao Yamamoto

    IPC分类号： C07D211/52 ,  C07D295/12 ,  C07D401/04

    CPC分类号： C07D211/52 ,  C07D295/12

    摘要： An N-(.omega.-amino)alkylaniline derivative of the formula: ##STR1## and its pharmaceutically acceptable salts, which are useful as neuroleptic agents and can be prepared by reacting a compound of the formula: ##STR2## with a compound of the formula:H--A[wherein R is hydrogen, C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.7 alkanoyl or aroyl, R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.7 alkyl or C.sub.1 -C.sub.7 alkoxy,A is ##STR3## (wherein R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.7 alkyl, C.sub.1 -C.sub.7 alkoxy or trifluoromethyl), ##STR4## (wherein R.sub.2 is as defined above and R.sub.3 is hydrogen, C.sub.1 -C.sub.7 alkyl or C.sub.1 -C.sub.7 alkanoyl), ##STR5## (wherein R.sub.2 is as defined above or ##STR6## (wherein R.sub.2 and R.sub.3 are each as defined above) and n is 2, 3 or 4].

    摘要翻译： 下式的N-（ω-氨基）烷基苯胺衍生物及其药学上可接受的盐，其可用作抗精神病药，并且可以通过使下式化合物与下式化合物反应来制备：＆lt; IMAGE＆gt; ：