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19 条记录 (耗时 0.024 秒)

    Butyrophenone derivatives
    2.
    发明授权
    Butyrophenone derivatives 失效
    丁酰苯衍生物

    公开(公告)号：US4009173A

    公开(公告)日：1977-02-22

    申请号：US617730

    申请日：1975-09-29

    申请人： Kikuo Sasajima ,  Masaru Nakao ,  Isamu Maruyama ,  Keiichi Ono ,  Shigenari Katayama ,  Shigeho Inaba ,  Hisao Yamamoto

    发明人： Kikuo Sasajima ,  Masaru Nakao ,  Isamu Maruyama ,  Keiichi Ono ,  Shigenari Katayama ,  Shigeho Inaba ,  Hisao Yamamoto

    IPC分类号： C07D211/64 ,  C07D403/04

    CPC分类号： C07D211/64

    摘要： Novel butyrophenone derivatives of the formula: ##STR1## wherein R.sub.1 represents a hydroxyl group or ##STR2## (wherein R.sub.6 and R.sub.7 are each a hydrogen atom or a lower alkyl group or, when taken together with the adjacent nitrogen atom, may form a heterocyclic group), R.sub.2 represents an optionally substituted phenyl group or ##STR3## (wherein R.sub.8 and R.sub.9 are each a hydrogen atom or a lower alkyl group or, when taken together with the adjacent nitrogen atom, may form a heterocyclic group), R.sub.4 represents a hydrogen atom, a lower alkyl group or an optionally substituted phenyl group, R.sub.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a trifluoromethyl group, R.sub.10 represents a hydrogen atom or an acyl group represented by R.sub.3 CO- (wherein R.sub.3 is a hydrogen atom, a lower alkyl group or an optionally substituted phenyl group) and Z represents two hydrogen atoms or an oxygen atom, provided that when Z is an oxygen atom and R.sub.1 is ##STR4## R.sub.10 can not be a hydrogen atom, and their acid addition salts, which are useful as central and autonomic nervous system depressants.

    摘要翻译： 下式的新型丁基苯酚衍生物：其中R 1表示羟基或（其中R 6和R 7各自为氢原子或低级烷基，或者当与相邻的氮原子一起形成杂环时 基团），R 2表示任选取代的苯基或者其中R 8和R 9各自为氢原子或低级烷基，或者当与相邻的氮原子一起形成杂环基时，R 4表示 氢原子，低级烷基或任选取代的苯基，R 5表示氢原子，卤素原子，低级烷基，低级烷氧基或三氟甲基，R 10表示氢原子或R 3 CO 3表示的酰基 - （其中R 3是氢原子，低级烷基或任选取代的苯基），Z代表两个氢原子或氧原子，条件是当Z是氧原子且R 1不能是 氢原子， 和它们的酸加成盐，其可用作中枢神经系统抑制剂和自主神经系统抑制剂。

    1-Phenylthiopropyl-4-hydroxy-4-phenyl piperidines
    6.
    发明授权
    1-Phenylthiopropyl-4-hydroxy-4-phenyl piperidines 失效
    1-苯基硫丙基-4-羟基-4-苯基哌啶

    公开(公告)号：US3960873A

    公开(公告)日：1976-06-01

    申请号：US481796

    申请日：1974-06-21

    申请人： Isamu Maruyama ,  Hisao Yamamoto ,  Masaru Nakao ,  Shigeru Sakai ,  Kikuo Sasajima ,  Sumio Kitagawa ,  Shigeho Inaba

    发明人： Isamu Maruyama ,  Hisao Yamamoto ,  Masaru Nakao ,  Shigeru Sakai ,  Kikuo Sasajima ,  Sumio Kitagawa ,  Shigeho Inaba

    IPC分类号： C07D295/092 ,  C07D211/52

    CPC分类号： C07D295/088

    摘要： Novel N-substituted heterocyclic derivatives represented by the formula, ##SPC1##Wherein R.sub.1 is hydrogen atom, lower alkyl, lower alkoxy, nitro, halogen or trifluoromethyl group; R.sub.2 is hydrogen atom or lower alkyl group; X is sulfur atom, sulfinyl or sulfonyl group; Y is ##EQU1## group (wherein R.sub.3 is phenyl or substituted phenyl group; R.sub.4 is hydrogen atom, hydroxy, lower alkyl, lower alkoxy, lower alkanoyl, lower alkanoyloxy, carbamoyl, N-(lower alkyl)-carbamoyl or N,N-di(lower akyl)-carbamoyl group; R.sub.5 is hydrogen atom, morpholino, pyrrolidinyl, piperidinyl, hexamethylenimino, lower alkyl, cyclo(lower alkyl), cyclo(lower alkyl)-(lower alkyl), hydroxy-(lower alkyl), (lower alkoxy)-(lower alkyl), phenyl or substituted phenyl group; k is 0 or 1 and m is 0, 1 or 2); and n is 3 or 4, and pharmaceutically acceptable salts thereof, which have excellent tranquillizing, anti-psychotonic, anti-emotional, anti-convulsive, anti-psychosis, sedative, analgesic or anti-hypertensive activities.

    摘要翻译： 由式WHEREIN R1表示的新型N-取代的杂环衍生物是氢原子，低级烷基，低级烷氧基，硝基，卤素或三氟甲基; R2是氢原子或低级烷基; X是硫原子，亚磺酰基或磺酰基; Y是|| - （CH2）kN-（CH2）m-R3， - （CH2）kC-（CH2）m-R5或| R4 | -CH = C-（CH2）m-R5基（其中R3是苯基 或取代的苯基; R 4是氢原子，羟基，低级烷基，低级烷氧基，低级烷酰基，低级烷酰氧基，氨基甲酰基，N-（低级烷基） - 氨基甲酰基或N，N-二（低级烷基） - 氨基甲酰基; 氢原子，吗啉代，吡咯烷基，哌啶基，六亚甲基亚氨基，低级烷基，环（低级烷基），环（低级烷基） - （低级烷基），羟基 - （低级烷基），（低级烷氧基） - （低级烷基） 取代苯基; k为0或1，m为0,1或2）; 和n为3或4，及其药学上可接受的盐，其具有优异的镇静，抗心律失常，抗感觉，抗惊厥，抗精神病，镇静，止痛或抗高血压活性。

    N-substituted heterocyclic derivatives and preparation thereof
    8.
    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
    9.
    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; ：