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40 条记录 (耗时 0.029 秒)

    4-(Polyalkoxy phenyl)-2-pyrrolidones
    3.
    发明授权
    4-(Polyalkoxy phenyl)-2-pyrrolidones 失效
    4-（聚烷氧基苯基）-2-吡咯烷酮

    公开(公告)号：US4193926A

    公开(公告)日：1980-03-18

    申请号：US659082

    申请日：1976-02-18

    申请人： Ralph Schmiechen ,  Reinhard Horowski ,  Dieter Palenschat ,  Gert Paschelke ,  Helmut Wachtel ,  Wolfgang Kehr

    发明人： Ralph Schmiechen ,  Reinhard Horowski ,  Dieter Palenschat ,  Gert Paschelke ,  Helmut Wachtel ,  Wolfgang Kehr

    IPC分类号： C07D207/24 ,  C07D207/26 ,  C07D207/277 ,  C07D405/12 ,  C07D409/12

    CPC分类号： C07D207/277 ,  C07D207/24 ,  C07D207/26

    摘要： 4-(Polyalkoxyphenyl)-2-pyrrolidones of the formula ##STR1## wherein R.sub.1 and R.sub.2 each are hydrocarbon of up to 18 carbon atoms at least one being other than methyl, a heterocyclic ring, or alkyl of 1-5 carbon atoms substituted by halogen, OH, COOH, alkoxy, alkoxycarbonyl or an amino group; R' is H, alkyl, aryl or acyl; and X is O or S; possess neuropsychotropic activity. The compounds wherein X is O can be produced by saponifying and decarboxylating a corresponding 2-pyrrolidone-3-carboxylic acid alkyl ester or cyclizing a corresponding 3-phenyl-4-amino-butyric acid or alkyl ester thereof. The pyrrolidones can be converted to the corresponding thiopyrrolidones by reaction with phosphorous pentasulfide in the presence of base.

    摘要翻译： 式（IMAGE）的4-（聚烷氧基苯基）-2-吡咯烷酮，其中R 1和R 2各自是至多18个碳原子的烃，至少一个不同于甲基，杂环或1-5个碳原子的烷基被 卤素，OH，COOH，烷氧基，烷氧基羰基或氨基; R'是H，烷基，芳基或酰基; X为O或S; 具有神经食物活性。 其中X为O的化合物可通过皂化和脱羧相应的2-吡咯烷酮-3-羧酸烷基酯或环化相应的3-苯基-4-氨基 - 丁酸或其烷基酯来制备。 吡咯烷酮可以通过在碱存在下与五硫化二磷反应而转化为相应的硫代吡咯烷酮。

    Diacylapomorphines
    5.
    发明授权
    Diacylapomorphines 失效

    公开(公告)号：US4080456A

    公开(公告)日：1978-03-21

    申请号：US633650

    申请日：1975-11-20

    申请人： Dieter Seidelmann ,  Ralph Schmiechen ,  Reinhard Horowski ,  Wolfgang Kehr ,  Dieter Palenschat ,  Gert Paschelke

    发明人： Dieter Seidelmann ,  Ralph Schmiechen ,  Reinhard Horowski ,  Wolfgang Kehr ,  Dieter Palenschat ,  Gert Paschelke

    IPC分类号： C07D221/18 ,  A61K31/47 ,  C07D215/06

    CPC分类号： C07D221/18

    摘要： Diacylapomorphines of the formula ##STR1## wherein R.sub.1 and R.sub.2 are both acyl of 1-17 carbons are symptomatically effective agents in the treatment of motor disorders of the type associated with a dopamine deficiency of the extrapyramidal system of the central nervous system, e.g. Parkinson's disease. Pharmaceutical compositions containing these compounds as an active ingredient are described, as well as new compunds of the above formula wherein R.sub.1 and R.sub.2 are formyl or acyl of 3-17 carbon atoms.

    摘要翻译： 其中R 1和R 2都是1-17个碳的酰基的二酰基基吗啡是用于治疗与中枢神经系统的锥体外系统的多巴胺缺乏有关的类型的运动障碍的症状有效的药剂。 帕金森病 描述了含有这些化合物作为活性成分的药物组合物，以及上述式的新型化合物，其中R 1和R 2是3-17个碳原子的甲酰基或酰基。

    Pharmacologically active 3-substituted beta-carbolines
    7.
    发明授权
    Pharmacologically active 3-substituted beta-carbolines 失效

    公开(公告)号：US4435403A

    公开(公告)日：1984-03-06

    申请号：US331740

    申请日：1981-12-17

    申请人： Claus T. Braestrup ,  Jogen A. Christensen ,  Mogens Engelstoft ,  Gunter Neef ,  Ulrich Eder ,  Ralph Schmiechen ,  Andreas Huth ,  Dieter Rahtz ,  Dieter Seidelmann ,  Wolfgang Kehr ,  Dieter Palenschat

    发明人： Claus T. Braestrup ,  Jogen A. Christensen ,  Mogens Engelstoft ,  Gunter Neef ,  Ulrich Eder ,  Ralph Schmiechen ,  Andreas Huth ,  Dieter Rahtz ,  Dieter Seidelmann ,  Wolfgang Kehr ,  Dieter Palenschat

    IPC分类号： A61K31/435 ,  A61K31/44 ,  A61K31/445 ,  A61K31/675 ,  A61P25/00 ,  A61P25/20 ,  C07D209/08 ,  C07D209/20 ,  C07D471/04 ,  C07F9/6561 ,  C07D487/14

    CPC分类号： C07D471/04 ,  C07D209/08 ,  C07D209/20 ,  C07F9/6561

    摘要： 3-substituted beta-carbolines of the formula ##STR1## wherein R.sup.C is hydrogen, lower alkyl, alkoxyalkyl of up to 6 C-atoms, cycloalkyl of 3-6 C-atoms, aralkyl of up to 8 C-atoms, or (CH.sub.2).sub.n OR.sup.20wherein R.sup.20 is alkyl of up to 6 C-atoms, cycloalkyl of 3-6 C-atoms or aralkyl of up to 8 C-atoms and n is an integer of 1 to 3;Y is oxygen, two hydrogen atoms or NOR.sup.1,wherein R.sup.1 is hydrogen, lower alkyl, aryl or aralkyl of up to 6 C-atoms, COR.sup.2, wherein R.sup.2 is lower alkyl of up to 6 C-atoms,or Y is CHCOOR.sup.3, wherein R.sup.3 is hydrogen or lower alkylor Y is NNR.sup.4 R.sup.5,wherein R.sup.4 and R.sup.5 can be the same or different and each is hydrogen, lower alkyl, C.sub.6-10 -aryl, C.sub.7-10 -aralkyl or CONR.sup.6 R.sup.7,wherein R.sup.6 and R.sup.7 can be the same or different and each is hydrogen or lower alkyl or R.sup.4 and R.sup.5 together with the connecting N-atom, for a 5- or 6-membered heterocyclic ring which optionally may also contain an O-atom or up to 3 N-atoms and which optionally may be substituted by a lower alkyl group;Z is hydrogen, or alkoxy or aralkoxy each of up to 10 C-atoms and each optionally substituted by hydroxy, or Z is alkyl of up to 6 C-atoms, C.sub.6-10 -aryl or C.sub.7-10 -aralkyl each of which may optionally be substituted by a COOR.sup.8 -- or a CONR.sup.9 R.sup.10 group,wherein R.sup.8 is alkyl of up to 6 C-atoms, and R.sup.9 and R.sup.10 can be the same or different and each is hydrogen or alkyl of up to 6 C-atoms;or Z is NR.sup.9 R.sup.10, wherein R.sup.9 and R.sup.10 are as defined above;or Z is NR.sup.11 CHR.sup.12 R.sup.13,wherein R.sup.11 and R.sup.12 each is hydrogen or together form a N.dbd.C double bond,wherein R.sup.13 is C.sub.1-10 -alkyl or NR.sup.14 R.sup.15,wherein R.sup.14 and R.sup.15 are the same or different and each is hydrogen, OH or alkyl or alkoxy each of up to 6 C-atoms,or wherein R.sup.12 and R.sup.13 together are oxygen, in which case, R.sup.11 is hydrogen;or Z is COOR.sup.2 wherein R.sup.2 is as defined above;or Y and Z, together with the connecting C-atom, may form a 5- or 6-membered heterocyclic ring which contains an O-atom, adjoining O- and N-atoms or up to 4 N atoms and which optionally may be substituted by a lower alkyl group, hydroxy or oxo have valuable psychotropic properties which make them useful for example as tranquilizers.

    Substituted 5H-pyrimido[5,4-b]indoles
    10.
    发明授权
    Substituted 5H-pyrimido[5,4-b]indoles 失效
    取代的5H-嘧啶并[5,4-b]吲哚

    公开(公告)号：US4564610A

    公开(公告)日：1986-01-14

    申请号：US562248

    申请日：1983-12-16

    申请人： Dieter Rahtz ,  Andreas Huth ,  Ralph Schmiechen ,  Dieter Seidelmann ,  Wolfgang Kehr ,  Herbert H. Schneider ,  Claus T. Braestrup

    发明人： Dieter Rahtz ,  Andreas Huth ,  Ralph Schmiechen ,  Dieter Seidelmann ,  Wolfgang Kehr ,  Herbert H. Schneider ,  Claus T. Braestrup

    IPC分类号： A61K31/505 ,  A61P25/00 ,  C07D209/42 ,  C07D487/04 ,  C07F9/6561

    CPC分类号： C07D487/04 ,  C07D209/42 ,  C07F9/6561

    摘要： Substituted 5H-pyrimido[5,4-b]indoles of Formula I ##STR1## wherein R.sup.2 is halogen; the oxadiazolyl group ##STR2## wherein R" is lower alkyl with up to 3 carbon atoms; C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, or ##STR3## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR4## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, C.sub.3-5 -alkenyl, cycloalkyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; andR.sup.A is hydrogen; the oxadiazolyl group ##STR5## wherein R" is lower alkyl with up to 3 carbon atoms; halogen, nitro, OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, ##STR6## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR7## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, cycloalkyl, C.sub.3-5 -alkenyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; orPO(OR).sub.2 wherein R is C.sub.1-5 -alkyl, exhibit strong affinity for binding to benzodiazepine receptors.The novel compounds are suitable for use in psychopharmaceutical preparations.

    摘要翻译： 取代的式I的5H-嘧啶并[5,4-b]吲哚其中R 2是卤素; 恶二唑基其中R“是具有至多3个碳原子的低级烷基; C 1-5 - 烷基，环烷基，芳烷基或芳基; ORI，nn为0,1或2，或其中R 1为氢，C 1-5 - 烷基，环烷基，芳烷基或芳基的SO nRI; 其中RII和RIII是氢，C1-5-烷基，C3-5-烯基，环烷基，芳烷基，芳基，或具有连接的N-原子的5-或6-元杂环; RA为氢; 恶二唑基其中R“是具有至多3个碳原子的低级烷基; 卤素，硝基，ORI，nn为0,1或2的SO nRI，其中R 1为氢，C 1-5 - 烷基，环烷基，芳烷基或芳基; 其中RII和RIII是氢，C1-5烷基，环烷基，C3-5-烯基，芳烷基，芳基，或具有连接的N-原子的5或6元杂环; 或其中R为C 1-5 - 烷基的PO（OR）2表现出对苯并二氮杂受体结合的强亲合力。 新型化合物适用于精神药物制剂。