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13 条记录 (耗时 0.009 秒)

    Process for preparing 1-polyhaloalkyl-3,4-dihydro-2-(1H)-quinazolinones
    2.
    发明授权
    Process for preparing 1-polyhaloalkyl-3,4-dihydro-2-(1H)-quinazolinones 失效
    1-多卤代烷基-3,4-二氢-2-（1H） - 喹唑啉酮的制备方法

    公开(公告)号：US4048168A

    公开(公告)日：1977-09-13

    申请号：US754640

    申请日：1976-12-27

    申请人： Michihiro Yamamoto ,  Shigenari Katayama ,  Masao Koshiba ,  Hisao Yamamoto

    发明人： Michihiro Yamamoto ,  Shigenari Katayama ,  Masao Koshiba ,  Hisao Yamamoto

    IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P25/04 ,  A61P29/00 ,  C07D239/78 ,  C07D239/82 ,  C07D409/04 ,  C07D491/056

    CPC分类号： C07D239/78 ,  C07D239/82

    摘要： 3,4-Dihydro-2(1H)-quinazolinone derivatives of the formula, ##STR1## wherein R.sub.1 and R.sub.2 are each hydrogen, lower alkyl, lower alkylthio or lower alkoxy, or, when taken together, R.sub.1 and R.sub.2 may form methylenedioxy; R.sub.3 is polyhalo-lower alkyl; R.sub.4 is phenyl, halophenyl, lower alkoxyphenyl, lower alkylphenyl or thienyl; and X is oxygen or sulfur, which are known to be very useful intermediates for the preparation of anti-inflammatory and analgesic agents, are obtained in a high yield by reacting a compound of the formula, ##STR2## wherein R.sub.1, R.sub.2, R.sub.3 and X are as defined above, with a compound of the formula,R.sub.4 --CHOwherein R.sub.4 is as defined above, with heating in the presence of a zinc halide as a catalyst.

    摘要翻译： 3,4-二氢-2（1H） - 喹唑啉酮衍生物，其中R 1和R 2各自为氢，低级烷基，低级烷硫基或低级烷氧基，或者当R 1和R 2一起形成亚甲二氧基时; R3是多卤代低级烷基; R4是苯基，卤代苯基，低级烷氧基苯基，低级烷基苯基或噻吩基; 通过使下式化合物，其中R 1，R 2，R 3和R 3与式（I）化合物反应，可以高收率获得已知是用于制备抗炎和止痛剂的非常有用的中间体的X是氧或硫。 X如上所定义，与卤化锌作为催化剂的存在下，加热下式的化合物，其中R 4如上定义。

    .gamma.-Piperidinobutyrophenones
    4.
    发明授权
    .gamma.-Piperidinobutyrophenones 失效
    {65-哌啶基丁酰苯

    公开(公告)号：US4148796A

    公开(公告)日：1979-04-10

    申请号：US388561

    申请日：1973-08-15

    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： C07D211/48 ,  C07D401/06 ,  C07D401/04 ,  C07D211/50

    CPC分类号： C07D401/06 ,  C07D211/48

    摘要： Novel .gamma.-piperidinobutyrophenone derivatives of the formula, ##STR1## wherein R.sup.1 is halogen, amino, alkanoylamino, alkylamino or N-(alkanoyl)alkylamino;R.sup.2 is hydrogen or halogen, provided that when R.sup.1 is halogen, R.sup.2 must be halogen; andZ is a piperidino group having the formula (A), ##STR2## (wherein each of R.sub.a and R.sub.b is hydrogen, halogen, lower alkyl, lower alkoxy or trifluoromethyl; R.sup.3 is hydrogen or hydroxyl; and n is 1 or 2), or a piperidino group having the formula (B), ##STR3## (wherein R.sub.c is hydrogen or lower alkyl; and each of R.sub.d and R.sub.e is hydrogen, halogen, lower alkyl or lower alkoxy), provided that when R.sup.1 is amino and R.sup.2 is hydrogen, Z cannot be represented by the formula (A), and their pharmaceutically acceptable acid addition salts, which are useful as psychotropic, neuroleptic or analgesic agents.

    摘要翻译： 其中R1是卤素，氨基，烷酰基氨基，烷基氨基或N-（烷酰基）烷基氨基的新颖的γ-哌啶基丁酰苯衍生物， R2是氢或卤素，条件是当R1是卤素时，R2必须是卤素; Z为具有式（A），（A）的哌啶子基，其中R a和R b各自为氢，卤素，低级烷基，低级烷氧基或三氟甲基; R 3为氢或羟基; n为1或 2）或具有式（B）的哌啶子基，其中R c是氢或低级烷基;并且R d和R e各自是氢，卤素，低级烷基或低级烷氧基），条件是当 R1是氨基，R2是氢，Z不能由式（A）表示，它们的药学上可接受的酸加成盐可用作精神药物，精神抑制剂或止痛剂。

    Butyrophenone derivatives
    5.
    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。

    Phenoxyethylamine derivatives having central nervous system depressant and anti-hypertensive activity
    8.
    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
    9.
    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
    10.
    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。