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    Tetralone and indanone compounds
    2.
    发明授权
    Tetralone and indanone compounds 失效
    四氢萘酮和茚酮化合物

    公开(公告)号：US4016281A

    公开(公告)日：1977-04-05

    申请号：US659132

    申请日：1976-02-18

    申请人： Rochus Jonas ,  Jurgen Uhl ,  Helmut Muller-Calgan ,  Klaus Irmscher

    发明人： Rochus Jonas ,  Jurgen Uhl ,  Helmut Muller-Calgan ,  Klaus Irmscher

    IPC分类号： C07D211/52

    CPC分类号： C07D211/52

    摘要： Tetralone and indanone compounds of the formula ##STR1## wherein R.sup.1 is H, OH, alkoxy of 1-4 carbon atoms, cycloalkoxy of 3-6 carbon atoms, F, Cl, Br, NO.sub.2, monoalkylamino or dialkylamino, wherein each alkyl is of 1-4 carbon atoms, alkanoyloxy of 1-6 carbon atoms or alkanoylamino of 1-4 carbon atoms; R.sup.2 is OH or alkoxy of 1-4 carbon atoms or R.sup.1 and R.sup.2 collectively are methylenedioxy; R.sup.3 is H or CH.sub.3 ; Ar is phenyl or phenyl substituted by up to 5 of alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, F, Cl, Br or CF.sub.3 ; n is 1 or 2, and physiologically acceptable acid addition salts thereof, are central nervous system depressants.

    摘要翻译： 其中R 1是H，OH，1-4个碳原子的烷氧基，3-6个碳原子的环烷氧基，F，Cl，Br，NO 2，一烷基氨基或二烷基氨基的四酮和茚酮化合物，其中每个烷基是 1-4个碳原子，1-6个碳原子的烷酰氧基或1-4个碳原子的烷酰氨基; R2是OH或1-4个碳原子的烷氧基或R1和R2统称为亚甲二氧基; R3是H或CH3; Ar是苯基或被至多5个1-4个碳原子的烷基，1-4个碳原子的烷氧基，F，Cl，Br或CF 3取代的苯基; n为1或2，其生理上可接受的酸加成盐为中枢神经系统抑制剂。

    Gaba-agonistic imidazo(4,5-c)pyridines useful as pharmaceuticals
    4.
    发明授权
    Gaba-agonistic imidazo(4,5-c)pyridines useful as pharmaceuticals 失效
    用作药物的Gaba-激动咪唑并（4,5-c）吡啶

    公开(公告)号：US4654350A

    公开(公告)日：1987-03-31

    申请号：US873560

    申请日：1986-06-12

    申请人： Klaus Irmscher ,  Otto Saiko ,  Klaus-Otto Minck ,  Hans-Peter Wolf

    发明人： Klaus Irmscher ,  Otto Saiko ,  Klaus-Otto Minck ,  Hans-Peter Wolf

    IPC分类号： A61K31/435 ,  A61P3/04 ,  A61P25/08 ,  A61P39/02 ,  C07D471/04 ,  A61K31/44

    CPC分类号： C07D471/04

    摘要： Imidazo(4,5-c)pyridines of the formula ##STR1## wherein X is O, S or NH;Y is --NR.sup.2 --CH.dbd.N-- or --N.dbd.CH--NR.sup.2 --;R.sup.1 is 1-benzothienylmethyl, naphthylmethyl, or benzyl which is mono- or di-substituted by F, Cl, NO.sub.2, CF.sub.3 or a combination thereof, and;R.sup.2 is alkyl of 1-4 C atoms or cyclopropylmethyl,or a physiologically acceptable acid addition salt thereof,have valuable pharmacological activity, e.g., as GABA agonists.

    摘要翻译： 其中X为O，S或NH的咪唑（4,5-c）吡啶， Y是-NR 2 -CH = N-或-N = CH-NR 2 - ; R1是被F，Cl，NO2，CF3或它们的组合单取代或二取代的1-苯并噻吩基甲基，萘甲基或苄基， R2是1-4C原子的烷基或环丙基甲基或其生理上可接受的酸加成盐，具有有价值的药理活性，例如作为GABA激动剂。

    Sulfur-containing 6-ketoprostaglandins
    6.
    发明授权
    Sulfur-containing 6-ketoprostaglandins 失效
    含硫6孔松脂腺苷

    公开(公告)号：US4680288A

    公开(公告)日：1987-07-14

    申请号：US692490

    申请日：1985-01-18

    申请人： Klaus Irmscher ,  Hans-Eckart Radunz ,  Ernst Schulze ,  Bernhard Riefling

    发明人： Klaus Irmscher ,  Hans-Eckart Radunz ,  Ernst Schulze ,  Bernhard Riefling

    IPC分类号： C07D333/18 ,  A61K31/557 ,  A61K31/5575 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D213/70 ,  C07D309/12 ,  C07F7/18 ,  C07C177/00

    CPC分类号： C07C405/0033

    摘要： Sulfur-containing 6-ketoprostaglandins of the formula I ##STR1## in which D is a bond, alkylene having 1-3 C atoms, cis-alkenylene having 2-5 C atoms or alkinylene having 2-5 C atoms,R.sup.1 is H, alkyl having 1-4 C atoms, aryl having 6-12 C atoms or --C.sub.6 H.sub.4 NHCOC.sub.6 H.sub.5,R.sup.2 is alkyl having 1-7 C atoms, alkyl having 1-7 C atoms which is substituted by halogen, cycloalkyl having 5-6 C atoms, cycloalkyl having 5-6 C atoms which is substituted by alkyl having 1-4 C atoms, phenyl, phenyl which is substituted by F, Cl, Br, alkyl having 1-4 C atoms, OH, OCH.sub.3 or CF.sub.3, pyridyl, naphthyl, thienyl or, if D is alkylene having 1-3 C atoms, also is alkoxy having 1-4 C atoms, alkylthio having 1-4 C atoms, phenoxy or phenoxy which is substituted by F, Cl, Br, alkyl having 1-4 C atoms, OH, OCH.sub.3 or CF.sub.3,R.sup.3 and R.sup.4 each are H, alkyl having 1-7 C atoms, tetrahydro-2-pyranyl, trialkylsilyl having a total of 3-12 C atoms, aryldialkylsilyl having a total of 8-18 C atoms, alkoxymethyl having 2-5 C atoms, aryloxymethyl having 7-11 C atoms or acyl having 1-10 C atoms, andR.sup.5 is H or alkyl having 1-3 C atoms, and.... indicates that this bond is .alpha., indicates that this bond is .beta.,and, where R.sub.1 is H, their salts, show effects on the circulation, in particular hypotensive effects, as well as effects on the force of myocardial contraction.

    摘要翻译： 其中D为键的式I化合物I-I，含有1-3个C原子的亚烷基，具有2-5个C原子的顺式亚烯基或具有2-5个C原子的亚炔基的含硫的6-酮基前列腺素，R1为H 具有1-4个C原子的烷基，具有6-12个碳原子的芳基或-C6H4NHCOC6H5的芳基，R2是具有1-7个C原子的烷基，具有1-7个C原子的被卤素取代的烷基，具有5-6个C原子的环烷基 由具有1-4个C原子的烷基取代的具有5-6个碳原子的环烷基，苯基，被F，Cl，Br，具有1-4个C原子的烷基取代的苯基，OH，OCH3或CF3，吡啶基，萘基 ，噻吩基或如果D是具有1-3个C原子的亚烷基，也是具有1-4个C原子的烷氧基，具有1-4个C原子的烷硫基，被F，Cl，Br取代的苯氧基或苯氧基， 4个C原子，OH，OCH 3或CF 3，R 3和R 4各自为H，具有1-7个C原子的烷基，四氢-2-吡喃基，总共3-12个C原子的三烷基甲硅烷基，共有8-18个芳基二烷基甲硅烷基 C原子，具有2-5个C原子的烷氧基甲基，芳氧基甲基 具有1-10个碳原子的7-11个C原子或酰基，R5是H或具有1-3个C原子的烷基，...表示该键为α，表示该键为β，并且其中 R1是H，它们的盐，对循环有显着影响，特别是降压作用，以及对心肌收缩力的影响。