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    Pyrazinoisoquinolines as anthelmintic agents
    2.
    发明授权
    Pyrazinoisoquinolines as anthelmintic agents 失效
    吡嗪异喹啉作为驱肠剂

    公开(公告)号：US3993760A

    公开(公告)日：1976-11-23

    申请号：US481792

    申请日：1974-06-21

    申请人： Rolf Pohlke ,  Friedrich Loebich ,  Jurgen Seubert ,  Herbert Thomas ,  Peter Andrews

    发明人： Rolf Pohlke ,  Friedrich Loebich ,  Jurgen Seubert ,  Herbert Thomas ,  Peter Andrews

    IPC分类号： C07D217/14 ,  C07D471/04 ,  A61K31/495

    CPC分类号： C07D471/04 ,  C07D217/14

    摘要： (-)-2-Benzoyl-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline is prepared by benzoylation of (-)-4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline, or cyclization of a compound of the formula ##SPC1##Wherein X is F, Cl, Br, I or O-tosyl and which has the optical configuration of the final product, or cyclization of a compound of the formula ##SPC2## wherein Y is OH, alkoxy, F, Cl, Br or I under HY-removing reaction conditions and which has the optical configuration of the final product, which is an anthelmintic.

    摘要翻译： （ - ） - 2-苯甲酰基-4-氧代-1,2,3,6,7,11b-六氢-4H-吡嗪并[2,1-a]异喹啉线是通过（ - ） - 4-氧代 -1,2,3,6,7,11b-六氢-4H-吡嗪并[2,1-a]异喹啉，或式WHEREIN X的化合物与F，Cl，Br，I或O-甲苯磺酰基和 其具有最终产物的光学构型，或在HY-去除反应条件下环化下式化合物其中Y是OH，烷氧基，F，Cl，Br或I，并且具有最终产物的光学构型，其中 是一个驱魔。

    Ring substituted pyrazino-isoquinoline derivatives and their preparation
    5.
    发明授权
    Ring substituted pyrazino-isoquinoline derivatives and their preparation 失效
    环取代的吡嗪异喹啉衍生物及其制备方法

    公开(公告)号：US4120961A

    公开(公告)日：1978-10-17

    申请号：US817467

    申请日：1977-07-20

    申请人： Jurgen Seubert ,  Rolf Pohlke ,  Herbert Thomas ,  Peter Andrews

    发明人： Jurgen Seubert ,  Rolf Pohlke ,  Herbert Thomas ,  Peter Andrews

    IPC分类号： C07D217/14 ,  A61K31/495 ,  C07D241/36

    CPC分类号： C07D217/14

    摘要： Isoquinolines of the formula ##STR1## wherein R.sup.1 is H, OH, alkyl; R.sup.2 is H, or an unsubstituted or substituted carbonyl, carbonyloxy or thiocarbonyl group; R.sup.3 is H, alkyl or hydroxy alkyl; R.sup.4 is H, alkyl or phenyl; R.sup.5 is O, H,H or H and alkyl, phenyl, halo or hydroxy; R.sup.6 and R.sup.7 are optional substituents; and R.sup.8 is H or alkyl, R.sup.2 being a thiocarbonyl or carbonyloxy group when R.sup.1 and R.sup.3 to R.sup.8 are H and X is O; and their physiologically acceptable salts, are antihelmintics, especially against cestodes and trematodes; some also possessing CNS activity, e.g., psychotropic and blood pressure regulating activity.

    摘要翻译： 其中R 1是H，OH，烷基; R2是H或未取代或取代的羰基，羰基氧基或硫代羰基; R3是H，烷基或羟基烷基; R4是H，烷基或苯基; R5是O，H，H或H，烷基，苯基，卤素或羟基; R6和R7是任选的取代基; 当R 1和R 3至R 8为H且X为O时，R 8为H或烷基，R 2为硫代羰基或羰基氧基; 和它们的生理学上可接受的盐，是抗炎药，特别是针对绦虫和吸虫; 一些还具有CNS活性，例如精神病和血压调节活性。

    Process for the preparation of 4-oxo-hexahydro-pyrazinoisoquinoline derivatives
    6.
    发明授权
    Process for the preparation of 4-oxo-hexahydro-pyrazinoisoquinoline derivatives 失效
    制备4-氧代 - 六氢 - 吡嗪并异喹啉衍生物的方法

    公开(公告)号：US4049659A

    公开(公告)日：1977-09-20

    申请号：US662009

    申请日：1976-02-27

    申请人： Rolf Pohlke

    发明人： Rolf Pohlke

    IPC分类号： C07D217/06 ,  C07D471/04

    CPC分类号： C07D471/04 ,  C07D217/06

    摘要： 4-OXO-HEXAHYDRO-PYRAZINOISOQUINOLINE DERIVATIVES ARE OBTAINED IN GOOD YIELD BY A SINGLE-STEP PROCESS WHICH COMPRISES HYDROLYZING A 2-ACYL-4-OXO-1,2,3,6,7,11B-HEXAHYDRO-4H-pyrazino[2,1-a]isoquinoline with an oxygen-containing acid or acid salt of inorganic pentavalent phosphorus or hexavalent sulfur.

    摘要翻译： 通过包含水解2-羟基-4-氧代-1,2,3,6,7,11B-十六氢-4H-吡嗪并[2]的单步方法获得良好的4-OXO-十六氢吡喃衍生物衍生物 ，1-a]异喹啉与无机五价磷或六价硫的含氧酸或酸盐反应。

    Isoquinolines and anti-depressants containing them
    8.
    发明授权
    Isoquinolines and anti-depressants containing them 失效
    含有异喹啉和抗抑郁剂

    公开(公告)号：US4122180A

    公开(公告)日：1978-10-24

    申请号：US806240

    申请日：1977-06-13

    申请人： Rolf Pohlke ,  Wighard Strehlow ,  Helmut Mueller-Calgan ,  Christoph Seyfried

    发明人： Rolf Pohlke ,  Wighard Strehlow ,  Helmut Mueller-Calgan ,  Christoph Seyfried

    IPC分类号： C07D401/04 ,  A61K20060101 ,  A61K31/47 ,  A61P25/24 ,  A61P25/26 ,  C07D20060101 ,  C07D211/04 ,  C07D211/06 ,  C07D217/04

    CPC分类号： C07D401/12

    摘要： Isoquinolines of the formula ##STR1## wherein R.sup.1 is H or alkyl of 1 - 4 carbon atoms, R.sup.2 is H and R.sup.3 is OH or R.sup.2 and R.sup.3 collectively are a C--C bond, and physiologically acceptable acid addition salts thereof have anti-depressant activity and can be prepared by solvolyzing or hydrogenolyzing a compound of the formula ##STR2## or an acid addition salt thereof, wherein R.sup.4 is R.sup.1 or R.sup.6, R.sup.5 is OR.sup.7 or, when R.sup.4 is R.sup.6, R.sup.3 ; R.sup.6 and R.sup.7 are radicals which can be split off solvolytically or hydrogenolytically and R.sup.1 and R.sup.2 are as above; and the optional step of dehydrating a resulting carbinol (R.sup.2 is H, R.sup.3 is OH) and/or treating a resulting compound (R.sup.1 is H) with a N-alkylating agent and/or converting a resulting base to a physiologically acceptable acid addition salt by treatment with and acid.

    摘要翻译： 其中R 1为H或1-4个碳原子的烷基，R 2为H且R 3为OH或R 2和R 3为CC键，其生理学上可接受的酸加成盐具有抗抑郁活性， 可以通过溶剂化或氢解式IMA的化合物或其酸加成盐，其中R 4是R 1或R 6，R 5是OR 7，或者当R 4是R 6时，R 3; R6和R7是可以溶剂分解或氢解分解的自由基，R1和R2如上所述; 和将所得的甲醇（R2是H，R3是OH）脱水和/或用N-烷基化剂处理所得化合物（R1是H）和/或将得到的碱转化为生理上可接受的酸加成盐的任选步骤 通过处理和酸。

    1(3,4,5-Trimethoxybenzamido methyl) tetrahydro isoquinoline derivatives and a process for their production
    9.
    发明授权
    1(3,4,5-Trimethoxybenzamido methyl) tetrahydro isoquinoline derivatives and a process for their production 失效
    1（3,4,5-三甲氧基苯甲酰氨基甲基）四氢异喹啉衍生物及其制备方法

    公开(公告)号：US3985881A

    公开(公告)日：1976-10-12

    申请号：US530551

    申请日：1974-12-09

    申请人： Werner Mehrhof ,  Rolf Pohlke ,  Karl Heinz Becker ,  Hans-Jochen Schliep

    发明人： Werner Mehrhof ,  Rolf Pohlke ,  Karl Heinz Becker ,  Hans-Jochen Schliep

    IPC分类号： C07D217/12 ,  C07D217/14 ,  C07D217/26

    CPC分类号： C07D217/26 ,  C07D217/14

    摘要： Novel isoquinoline derivatives of the formula ##SPC1##Wherein R.sub.1 is H or, together with R.sub.2, a C--N bond; R.sub.2 is H, R.sub.8 or, together with R.sub.1, a C--N bond; R.sub.3 is H, methyl or ethyl; R.sub.4 and R.sub.5 each are H or collectively a C--C bond; and R.sub.6 and R.sub.7 each are H or methoxy; R.sub.8 being acyl of 1-10 carbon atoms or alkyl of 1-17 carbon atoms optionally mono- or polysubstituted by phenyl, OH, ArCOO--, ArCONH--, piperidino, 3,4-dehydropiperidino, morpholino, carboxy, carbomethoxy and/or carbethoxy, Ar being 3,4,5-trimethoxyphenyl; and the physiologically acceptable acid addition salts and quaternary ammonium salts thereof, have cardiovascular activity and can be prepared by acylating a corresponding primary amine lacking the COAr group with 3,4,5-trimethoxybenzoic acid or a functional derivative thereof.

    摘要翻译： 式WHEREIN R1的新型异喹啉衍生物是H或与R2一起形成C-N键; R2是H，R8或与R1一起形成C-N键; R3是H，甲基或乙基; R4和R5各自为H或共同为C-C键; R6和R7各自为H或甲氧基; R8是1-10个碳原子的酰基或1-17个碳原子的烷基，任选被苯基，OH，ArCOO - ，ArCONH-，哌啶子基，3,4-脱氢哌啶子基，吗啉代，羧基，甲酯基和/或乙氧基乙氧基 Ar为3,4,5-三甲氧基苯基; 并且其生理上可接受的酸加成盐和季铵盐具有心血管活性，并且可以通过用3,4,5-三甲氧基苯甲酸或其功能性衍生物酰化相应的缺少COAr基团的伯胺来制备。