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    Phenoxypropylamine derivatives
    4.
    发明授权
    Phenoxypropylamine derivatives 失效
    苯氧丙胺衍生物

    公开(公告)号：US4009275A

    公开(公告)日：1977-02-22

    申请号：US553932

    申请日：1975-02-28

    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： A61K31/445 ,  C07D401/04

    CPC分类号： C07D401/04 ,  A61K31/445

    摘要： Phenoxypropylamine derivatives of the formula: ##STR1## (in which R.sub.2 is a halogen atom or a trifluoromethyl group) and R.sub.1 is a halogen atom or a C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 alkenyl group, and their pharmaceutically acceptable salts, which are useful as neuroleptic agents and can be prepared by reacting a compound of the formula: ##STR2## wherein X is a halogen atom and R.sub.1 is as defined above with a compound of the formula:H-Ywherein Y is as defined above.

    摘要翻译： 下式的苯氧丙胺衍生物：其中R 2为卤原子或三氟甲基，R 1为卤素原子或C 1 -C 4烷基或C 2 -C 4烯基， 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：其中X是卤素原子，R 1如上定义;

    Phenoxyethylamine derivatives having central nervous system depressant and anti-hypertensive activity
    5.
    发明授权
    Phenoxyethylamine derivatives having central nervous system depressant and anti-hypertensive activity 失效
    具有中枢神经系统抑制剂和抗高血压活性的苯氧基乙胺衍生物

    公开(公告)号：US3993780A

    公开(公告)日：1976-11-23

    申请号：US515889

    申请日：1974-10-18

    申请人： Masaru Nakao ,  Kikuo Sasajima ,  Isamu Maruyama ,  Shigenari Katayama ,  Hisao Yamamoto

    发明人： Masaru Nakao ,  Kikuo Sasajima ,  Isamu Maruyama ,  Shigenari Katayama ,  Hisao Yamamoto

    IPC分类号： A61K31/135 ,  A61P25/20 ,  C07C67/00 ,  C07C213/00 ,  C07C217/48 ,  C07C217/72 ,  F28B1/00 ,  F28B1/02

    CPC分类号： F28B1/00 ,  F28B1/02

    摘要： Novel phenoxyethylamine derivatives of the formula: ##SPC1##Wherein R.sub.1 and R.sub.2 are each hydrogen, halogen, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl, R.sub.4 and R.sub.5 are each hydrogen or C.sub.1 -C.sub.4 alkoxy and R is alkyl or aralkyl, and non-toxic pharmaceutically acceptable salts thereof, which are useful as central nervous system depressants and anti-hypertensive agents and can be prepared by reducing a compound of the formula: ##SPC2##Wherein R.sub.1, R.sub.2, R.sub.4, R.sub.5 and R are each as defined above and A is ##EQU1## (wherein R.sub.3 is as defined above) with a reducing agent.

    摘要翻译： 式：+ q，10的新型苯氧基乙胺衍生物，其中R1和R2各自为氢，卤素，C1-C4烷基或C1-C4烷氧基，R3为氢或C1-C4烷基，R4和R5各自为氢或C1-C4 烷氧基和R是烷基或芳烷基，以及其无毒的药学上可接受的盐，其可用作中枢神经系统抑制剂和抗高血压药，并且可以通过还原下式化合物来制备：+ q，11，其中R1，R2 ，R4，R5和R各自如上所定义，A是-CO-N-CH 2 - 或-CH 2 -N-CO- || R3R 3（其中R 3如上定义）与还原剂反应。

    Phenylbutanol derivatives
    6.
    发明授权
    Phenylbutanol derivatives 失效
    苯丁醇衍生物

    公开(公告)号：US3936468A

    公开(公告)日：1976-02-03

    申请号：US332777

    申请日：1973-02-15

    申请人： Hisao Yamamoto ,  Masaru Nakao ,  Kikuo Sasajima ,  Isamu Maruyama ,  Shigenari Katayama

    发明人： Hisao Yamamoto ,  Masaru Nakao ,  Kikuo Sasajima ,  Isamu Maruyama ,  Shigenari Katayama

    IPC分类号： C07D295/08 ,  C07D401/04 ,  C07D413/04 ,  C07D211/52

    CPC分类号： C07D401/04 ,  C07D295/08 ,  C07D413/04 ,  Y10S514/96

    摘要： Butyrophenone derivatives having excellent psychotropic activity and represented by the formula, ##SPC1##Wherein A represents a single or double bond linkage; R.sub.1 represents a hydrogen atom or a C.sub.1 - C.sub.4 alkyl group; R.sub.2, which is present only in case A represents a single bond linkage, represents a hydrogen atom, or a hydroxyl, C.sub.1 - C.sub.4 alkyl, or C.sub.1 - C.sub.4 alkoxy group; R.sub.3 represents a hydrogen atom, or a piperidino, pyrrolidino, morpholino, furyl, thienyl, C.sub.1 - C.sub.4 alkylamino, benzylamino, unsubstituted or halogen-substituted phenyl group, etc.; and X represents a hydrogen or halogen atom, or a C.sub.1 - C.sub.4 alkyl, C.sub.1 - C.sub.4 alkoxy, or trifluoromethyl group, can be prepared by reducing a benzoylpropionamide derivative of the formula, ##SPC2##Wherein A, R.sub.1, R.sub.2, R.sub.3 and X have the same meanings as defined above, to a phenylbutanol derivative of the formula, ##SPC3##

    摘要翻译： 丁基苯酚衍生物具有优良的精神活性，由下式表示，WHEREIN A表示单键或双键键; R1表示氢原子或C1-C4烷基; 仅在A表示单键连接的情况下存在的R 2表示氢原子或羟基，C 1 -C 4烷基或C 1 -C 4烷氧基; R3表示氢原子，哌啶子基，吡咯烷子基，吗啉代，呋喃基，噻吩基，C1-C4烷基氨基，苄基氨基，未取代或卤素取代的苯基等。 X代表氢或卤素原子，或C 1 -C 4烷基，C 1 -C 4烷氧基或三氟甲基可以通过还原下式的苯甲酰基丙酰胺衍生物，其中WHEREIN A，R1，R2，R3和X具有相同的 对于下式的苯基丁醇衍生物，

    Piperazinobutyrophenone derivatives
    7.
    发明授权
    Piperazinobutyrophenone derivatives 失效
    哌嗪丙基丙酮衍生物

    公开(公告)号：US3933824A

    公开(公告)日：1976-01-20

    申请号：US325372

    申请日：1973-01-22

    申请人： Hisao Yamamoto ,  Masaru Nakao ,  Kikuo Sasajima ,  Isamu Maruyama ,  Shigenari Katayama

    发明人： Hisao Yamamoto ,  Masaru Nakao ,  Kikuo Sasajima ,  Isamu Maruyama ,  Shigenari Katayama

    IPC分类号： C07D295/135 ,  C07D295/12

    CPC分类号： C07D295/135

    摘要： Central nervous system active butyrophenone derivatives in which .gamma. -piperazinobutyrophenone derivatives of the formula, ##SPC1##Wherein R.sup.1 is hydrogen, amino, C.sub.1 -C.sub.5 alkanoylamino, C.sub.1 -C.sub.4 alkylamino or N-(C.sub.1 -C.sub.4 alkyl)(C.sub.1 -C.sub.5 alkanoyl) amino; R.sup.2 is hydrogen or halogen; R.sup.3 is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or trifluoromethyl; and m is 0, 1 or 2, and acid addition salts thereof, can be prepared by reacting an indole derivative of the formula, ##SPC2##Wherein R.sup.2, R.sup.3 and m are the same as defined above, and R.sup.4 and R.sup.5 are hydrogen or C.sub.1 -C.sub.4 alkyl respectively, with an oxidizing agent to yield an o-alkanoylamino-.gamma.-piperazinobutyrophenone derivative of the formula, ##SPC3##Wherein R.sup.2, R.sup.3, R.sup.4, R.sup.5 and m are the same as defined above, and further, if necessary, hydrolyzing the product to yield an o-amino-.gamma.-piperazinobutyrophenone derivative of the formula, ##SPC4##Wherein R.sup.2, R.sup.3, R.sup.5 and m are the same as defined above, and further diazotizing, if desired, in case R.sup.5 is hydrogen, the obtained o-amino-.gamma.-piperazinobutyrophenone derivative and subsequently decomposing the resultant diazonium compound to replace the diazonium group by hydrogen. Among the butyrophenone derivatives thus obtained, those in which R.sup.1 is amino, alkanoylamino, alkylamino or N-alkylalkanoylamino and those in which R.sup.1 is hydrogen and R.sup.2 is halogen substituted at meta-position to carbonyl group are novel compounds.

    摘要翻译： 中枢神经系统活性丁酰苯衍生物，其中下式的γ-哌嗪基丙酰苯衍生物，其中R1是氢，氨基，C1-C5烷酰基氨基，C1-C4烷基氨基或N-（C1-C4烷基）（C1-C5烷酰基）氨基; R2是氢或卤素; R3是氢，卤素，C1-C4烷基，C1-C4烷氧基或三氟甲基; 并且m为0,1或2及其酸加成盐可以通过使下式的吲哚衍生物WHEREIN R2，R3和m与上述定义相同而制备，R4和R5是氢或C1-C4 烷基，分别与氧化剂反应，得到下式的邻 - 链烷酰氨基-γ-哌嗪基丙酰苯衍生物，其中，R 2，R 3，R 4，R 5和m与上述定义相同，此外，如果需要，水解产物 下式的邻氨基-γ-哌嗪基丙酰苯衍生物WHEREIN R2，R3，R5和m与上述定义相同，如果需要，在R5为氢的情况下进一步重氮化，得到的邻氨基-γ-哌嗪基丙酰苯 衍生并随后分解所得重氮化合物以用氢代替重氮基团。 在这样得到的丁酰苯衍生物中，R 1为氨基，烷酰基氨基，烷基氨基或N-烷基烷酰基氨基以及其中R 1为氢且R 2为卤素在间位被羰基取代的那些为新化合物。

    Butyrophenone compounds
    8.
    发明授权
    Butyrophenone compounds 失效
    丁基苯酚化合物

    公开(公告)号：US4303663A

    公开(公告)日：1981-12-01

    申请号：US795145

    申请日：1977-05-09

    申请人： Kikuo Sasajima ,  Keiichi Ono ,  Masaru Nakao ,  Hisao Yamamoto

    发明人： Kikuo Sasajima ,  Keiichi Ono ,  Masaru Nakao ,  Hisao Yamamoto

    IPC分类号： C07D295/10 ,  A61K31/435 ,  A61K31/443 ,  A61K31/445 ,  A61K31/451 ,  A61P9/12 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/20 ,  A61P29/00 ,  C07D211/14 ,  C07D211/52 ,  C07D405/06 ,  C07D471/10

    CPC分类号： C07D211/52

    摘要： Butyrophenone compounds having excellent psychotropic activities represented by the formula: ##STR1## wherein R.sup.1 is a halogen atom, R.sup.2 is a lower alkyl group, and Z is a group of either one of the formulae: ##STR2## (wherein the dotted line indicates the optional presence of an additional single bond linkage, R.sup.3 is a hydrogen atom or a hydroxyl group but only when said additional single bond linkage is not present and R.sup.4 is a hydrogen atom or a phenyl or benzyl group optionally substituted with one or two substituents selected from the group consisting of halogen, lower alkyl, lower alkoxy and trifluoromethyl on the benzene ring (except monohalophenyl)), ##STR3## (wherein the dotted line indicates the optional presence of an additional single bond linkage, R.sup.5 is a hydrogen atom or a lower alkyl group and R.sup.6 and R.sup.7 are each a hydrogen atom, a halogen atom or a lower alkyl group), ##STR4## (wherein R.sup.8 is a hydrogen atom or a lower alkyl group and R.sup.9 is a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group), ##STR5## (wherein R.sup.10 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a trifluoromethyl group), or ##STR6##

    3-(Piperazinoalkyl)-benz-2,1-isoxazoles
    9.
    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。