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    11-(Piperazin- or homopiperazin-1-yl)-5H-imidazo-(2,1-C)(1,4)benzodiazepines useful as anti-allergics
    1.
    发明授权
    11-(Piperazin- or homopiperazin-1-yl)-5H-imidazo-(2,1-C)(1,4)benzodiazepines useful as anti-allergics 失效
    可用作抗过敏剂的11-（哌嗪或高哌嗪-1-基）-5H-咪唑并 - （2,1-C）（1,4）苯并二氮杂

    公开(公告)号：US4686219A

    公开(公告)日：1987-08-11

    申请号：US827849

    申请日：1986-02-07

    申请人： Gerhard Walther ,  Claus Schneider ,  Karl-Heinz Weber ,  Armin Fugner

    发明人： Gerhard Walther ,  Claus Schneider ,  Karl-Heinz Weber ,  Armin Fugner

    IPC分类号： A61K31/55 ,  A61P25/02 ,  A61P25/04 ,  A61P25/20 ,  A61P37/08 ,  A61P43/00 ,  C07D233/90 ,  C07D487/04 ,  A61K31/33 ,  C07D487/14

    CPC分类号： C07D487/04 ,  C07D233/90

    摘要： Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, trifluoromethyl, hydroxyl, nitro, amino, cyano, methylsulfonamido, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 3 carbon atoms, (alkyl of 1 to 3 carbon atoms)thio or (alkanoyl of 2 to 4 carbon atoms)amino;R.sub.3 is hydrogen, fluorine, chlorine, bromine or alkyl of 1 to 3 carbon atoms;R.sub.4 is hydrogen, alkyl of 1 to 4 carbon atoms, hydroxy(alkyl of 2 to 4 carbon atoms), (alkoxy of 1 to 2 carbon atoms)-(alkyl of 2 to 4 carbon atoms), alkenyl of 3 to 6 carbon atoms, alkynyl of 3 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, (cycloalkyl of 3 to 7 carbon atoms)-(alkyl of 1 to 3 carbon atoms) or (unsubstituted or substituted phenyl)-(alkyl of 1 to 3 carbon atoms) where the substituent is fluorine, chlorine, bromine, methyl, methoxy, hydroxyl or trifluoromethyl; andn is 1 or 2;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiallergic.

    摘要翻译： 其中R 1和R 2可以相同或不同，各自为氢，氟，氯，溴，三氟甲基，羟基，硝基，氨基，氰基，甲基亚磺酰氨基，1至4的烷基 碳原子，1至3个碳原子的烷氧基，（1至3个碳原子的烷基）硫代或（2至4个碳原子的烷酰基）氨基; R3是氢，氟，氯，溴或1至3个碳原子的烷基; R4为氢，1至4个碳原子的烷基，羟基（2至4个碳原子的烷基），（1至2个碳原子的烷氧基） - （2至4个碳原子的烷基），3至6个碳原子的链烯基 3〜6个碳原子的炔基，3〜7个碳原子的环烷基，3〜7个碳原子的环烷基，1〜3个碳原子的烷基或（未取代或取代的苯基） - （1〜3的烷基） 碳原子），其中取代基是氟，氯，溴，甲基，甲氧基，羟基或三氟甲基; n为1或2; 和无毒的，药学上可接受的酸加成盐。 化合物及其盐可用作抗过敏药。

    4-Aminocarbonylaminomethyl-1-benzylpyrrolidin-2-ones as nootropic agents and as agents for treating cerebral insufficiency
    3.
    发明授权
    4-Aminocarbonylaminomethyl-1-benzylpyrrolidin-2-ones as nootropic agents and as agents for treating cerebral insufficiency 失效
    4-氨基羰基氨基甲基-1-苄基吡咯烷-2-酮作为助推剂和作为治疗脑功能不全的药物

    公开(公告)号：US4670456A

    公开(公告)日：1987-06-02

    申请号：US738152

    申请日：1985-05-24

    申请人： Karl-Heinz Weber ,  Claus Schneider ,  Gerhard Walther ,  Dieter Hinzen ,  Franz J. Kuhn ,  Erich Lehr ,  Helmut Ensinger ,  Wolfgang Troger

    发明人： Karl-Heinz Weber ,  Claus Schneider ,  Gerhard Walther ,  Dieter Hinzen ,  Franz J. Kuhn ,  Erich Lehr ,  Helmut Ensinger ,  Wolfgang Troger

    IPC分类号： A61K31/40 ,  A61K31/4015 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61P25/00 ,  A61P25/28 ,  C07D207/26 ,  C07D401/12 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08 ,  C07D207/12

    CPC分类号： C07D207/26 ,  C07D401/12 ,  C07D413/12 ,  C07D451/02

    摘要： The invention relates to new substituted pyrrolidinones of general formula ##STR1## wherein R.sub.1 represents a phenyl group which may be mono- or di-substituted by methyl, methoxy, fluorine, chlorine, bromine or trifluoromethyl, or a pyridyl group;R.sub.2 represents hydrogen or a straight-chained or branched alkyl group with 1-4 carbon atoms;R.sub.3 represents a straight-chained or branched alkyl group with 1-3 carbon atoms, a hydroxyalkyl group with 2-3 carbon atoms, a phenyl group which can be mono- or di-substituted by chlorine, bromine, methyl or methoxy, a cyclohexyl group or a dialkylamino alkyl group, where in each alkyl group can contain from 1-3 carbon atoms;R.sub.4 represents hydrogen or a straight-chained or branched alkyl group with 1-3 carbon atoms; orR.sub.3 and R.sub.4 together with the nitrogen atom represent a piperidine, morpholine or piperazine ring, while the ring may be substituted by 1 or 2 methyl groups and the piperazine ring at the nitrogen atom in 4-position may also carry a phenyl, chlorophenyl or benzyl group, or they may represent the nortropanyl group, processes for preparing them and pharmaceutical compositions.The new compounds have proved effective in animal trials in alleviating or remedying conditions or restricted cerebral performance.

    摘要翻译： 本发明涉及通式为（I）的新的取代的吡咯烷酮，其中R 1表示可被甲基，甲氧基，氟，氯，溴或三氟甲基或吡啶基单取代或二取代的苯基; R 2表示氢或具有1-4个碳原子的直链或支链烷基; R3表示具有1-3个碳原子的直链或支链烷基，具有2-3个碳原子的羟烷基，可被氯，溴，甲基或甲氧基单取代或二取代的苯基，环己基 基团或二烷基氨基烷基，其中在每个烷基中可以含有1-3个碳原子; R4表示氢或具有1-3个碳原子的直链或支链烷基; 或者R3和R4与氮原子一起代表哌啶，吗啉或哌嗪环，而环可以被1或2个甲基取代，4-位氮原子上的哌嗪环也可以带有苯基，氯苯基或 或它们可以代表异丙基丙基，其制备方法和药物组合物。 新化合物已被证明在动物试验中有效减轻或补救病症或限制脑部表现。

    4-Phenyl-4,5,6,7-tetrahydro-thieno[2,3-c]pyridines and salts thereof, compositions and use
    4.
    发明授权
    4-Phenyl-4,5,6,7-tetrahydro-thieno[2,3-c]pyridines and salts thereof, compositions and use 失效
    4-苯基-4,5,6,7-四氢 - 噻吩并[2,3-c]吡啶及其盐，组合物和用途

    公开(公告)号：US4550106A

    公开(公告)日：1985-10-29

    申请号：US630376

    申请日：1984-07-23

    申请人： Claus Schneider ,  Gerhard Walther ,  Karl-Heinz Weber ,  Wolf D. Bechtel ,  Karin Boke-Kuhn

    发明人： Claus Schneider ,  Gerhard Walther ,  Karl-Heinz Weber ,  Wolf D. Bechtel ,  Karin Boke-Kuhn

    IPC分类号： A61K31/435 ,  A61P25/24 ,  A61P25/26 ,  C07D495/04 ,  A61K31/44 ,  A61K31/535

    CPC分类号： C07D495/04

    摘要： Compounds of the formula ##STR1## wherein R.sub.1 is amino, acetylamino, hydroxymethyl, methoxymethyl or ##STR2## R.sub.2 and R.sub.3, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, trifluoromethyl, hydroxyl, methoxy, methyl or ethyl;R.sub.4 is straight or branched alkyl of 1 to 3 carbon atoms; andR.sub.5 and R.sub.6, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms or, together with each other and the nitrogen atom to which they are attached, form a 5-, 6- or 7-membered heterocyclic ring where, in the case of a 6-membered ring, a --CH.sub.2 -group in the ring may be replaced by an oxygen atom,and non-toxic, pharmacologically acceptable salts thereof. The compounds as well as their salts are useful as antidepressants.

    摘要翻译： 其中R 1是氨基，乙酰氨基，羟甲基，甲氧基甲基或者R 2可以相同或不同的式（I）化合物分别是氢，氟，氯，溴，三氟甲基 ，羟基，甲氧基，甲基或乙基; R4是1〜3个碳原子的直链或支链烷基; 和可以相同或不同的R 5和R 6各自为氢或1至4个碳原子的烷基，或彼此连接并与它们相连的氮原子形成5-，6- 或7-元杂环，其中在6元环的情况下，环中的-CH 2 - 基可被氧原子取代，及其无毒的药学上可接受的盐。 化合物及其盐可用作抗抑郁药。

    N-heterocyclic substituted -pyrrolidin-2-ones
    5.
    发明授权
    N-heterocyclic substituted -pyrrolidin-2-ones 失效
    N-杂环取代的吡咯烷-2-酮

    公开(公告)号：US5149808A

    公开(公告)日：1992-09-22

    申请号：US755039

    申请日：1991-09-04

    申请人： Karl-Heinz Weber ,  Gerhard Walther ,  Claus Schneider ,  Dieter Hinzen ,  Franz J. Kuhn ,  Erich Lehr

    发明人： Karl-Heinz Weber ,  Gerhard Walther ,  Claus Schneider ,  Dieter Hinzen ,  Franz J. Kuhn ,  Erich Lehr

    IPC分类号： C07D207/26 ,  C07D401/06 ,  C07D521/00

    CPC分类号： C07D207/26 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/06

    摘要： Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms; R.sub.2 is 2-, 3- or 4-pyridyl, phenyl or mono- or di-substituted phenyl, where the substituents are each individually alkoxy of 1 to 2 carbon atoms, fluorine, chlorine, bromine, trifluoromethyl, alkyl or 1 to 4 carbon atoms, hydroxyl or nitro; andR.sub.3 and R.sub.4 are each independently hydrogen or alkyl of 1 to 4 carbon atoms; orR.sub.3 and R.sub.4, together with each other and the nitrogen atom to which they are attached, form an unsubstituted or methyl-substituted, saturated 5- or 6-membered heterocycle which may contain an additional oxygen or nitrogen heteroatom, or form an imidazole ring;where the aminomethyl substituent is attached to the 4- or 5-position or the pyrrolidine ring, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as nootropics and antihypoxics.

    摘要翻译： 其中R 1为氢或1至4个碳原子的烷基的式IMA化合物; R2是2-，3-或4-吡啶基，苯基或单取代或二取代的苯基，其中取代基各自为1至2个碳原子的烷氧基，氟，氯，溴，三氟甲基，烷基或1至4个碳 原子，羟基或硝基; 并且R 3和R 4各自独立地为氢或1至4个碳原子的烷基; 或R 3和R 4彼此连接并与它们所连接的氮原子形成未取代的或甲基取代的饱和的5-或6-元杂环，其可以含有另外的氧或氮杂原子，或形成咪唑环 ; 其中氨基甲基取代基连接到4-或5-位或吡咯烷环上，以及无毒的药学上可接受的酸加成盐。 这些化合物以及盐类可用作神经递质和抗缺氧剂。

    3-Imino-3H-dibenzo-[c,f]-imidazo-[1,5-a]azepine pharmaceuticals
    7.
    发明授权
    3-Imino-3H-dibenzo-[c,f]-imidazo-[1,5-a]azepine pharmaceuticals 失效
    3-亚氨基-3H-二苯并[c，f] - 咪唑并[1,5-a]吖庚因药物

    公开(公告)号：US4503060A

    公开(公告)日：1985-03-05

    申请号：US410006

    申请日：1982-08-20

    申请人： Gerhard Walther ,  Claus Schneider ,  Karl-Heinz Weber ,  Armin F/u/ gner

    发明人： Gerhard Walther ,  Claus Schneider ,  Karl-Heinz Weber ,  Armin F/u/ gner

    IPC分类号： C07D491/04 ,  A61K31/55 ,  A61K31/553 ,  A61K31/554 ,  A61P37/08 ,  A61P43/00 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

    CPC分类号： C07D487/04 ,  C07D513/04

    摘要： Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each hydrogen, halogen, alkyl of 1 to 6 carbon atoms or alkoxy of 1 to 6 carbon atoms;R.sub.5 is hydrogen, alkyl of 1 to 6 carbon atoms or alkenyl of 3 to 6 carbon atoms;R.sub.6 is alkyl of 1 to 6 carbon atoms, alkenyl of 3 to 6 carbon atoms, phenyl, halo-phenyl, lower alkyl-phenyl, or lower alkoxy-phenyl or ##STR2## R.sub.7 and R.sub.8 are each hydrogen, halogen, alkyl of 1 to 6 carbon atoms or alkoxy or 1 to 6 carbon atoms;n is an integer from 0 to 4, inclusive;x is --O--, --S--, or --CH.sub.2 --; and the broken line between the 10 and 13b-positions indicates a single or double bond;and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as antiallergics and antithrombotics.

    摘要翻译： 其中R 1，R 2，R 3和R 4各自为氢，卤素，1至6个碳原子的烷基或1至6个碳原子的烷氧基的式IMA化合物; R5是氢，1〜6个碳原子的烷基或3〜6个碳原子的链烯基; R6为1-6个碳原子的烷基，3-6个碳原子的烯基，苯基，卤代苯基，低级烷基 - 苯基或低级烷氧基 - 苯基或R7和R8各自为氢，卤素， 至6个碳原子或烷氧基或1至6个碳原子; n是0至4的整数，包括0和4; x是-O-，-S-或-CH 2 - ; 10和13b位之间的虚线表示单键或双键; 和无毒的，药学上可接受的酸加成盐; 化合物及其盐可用作抗过敏药和抗血栓药。

    Morpholine containing pyrrolidinones pharmaceutical compositions and use
    8.
    发明授权
    Morpholine containing pyrrolidinones pharmaceutical compositions and use 失效
    含吡咯烷酮的吗啉药物组合物及用途

    公开(公告)号：US4762832A

    公开(公告)日：1988-08-09

    申请号：US943532

    申请日：1986-12-18

    申请人： Karl-Heinz Weber ,  Claus Schneider ,  Gerhard Walther ,  Dieter Hinzen ,  Franz J. Kuhn ,  Erich Lehr ,  Helmut Ensinger ,  Wolfgang Troger

    发明人： Karl-Heinz Weber ,  Claus Schneider ,  Gerhard Walther ,  Dieter Hinzen ,  Franz J. Kuhn ,  Erich Lehr ,  Helmut Ensinger ,  Wolfgang Troger

    IPC分类号： A61K31/40 ,  A61K31/4015 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61P25/00 ,  A61P25/28 ,  C07D207/26 ,  C07D401/12 ,  C07D413/12 ,  C07D451/02 ,  C07D487/08

    CPC分类号： C07D207/26 ,  C07D401/12 ,  C07D413/12 ,  C07D451/02

    摘要： The invention relates to new substituted pyrrolidinones of general formula ##STR1## wherein R.sub.1 represents a phenyl group which may be mono- or di-substituted by methyl, methoxy, fluorine, chlorine, bromine or trifluoromethyl, or a pyridyl group;R.sub.2 represents hydrogen or a straight-chained or branched alkyl group with 1-4 carbon atoms;R.sub.3 represents a straight-chained or branched alkyl group with 1-3 carbon atoms, a hydroxyalkyl group with 2-3 carbon atoms, a phenyl group which can be mono- or di-substituted by chlorine, bromine, methyl or methoxy, a cyclohexyl group or a dialkylamino alkyl group, where in each alkyl group can contain from 1-3 carbon atoms;R.sub.4 represents hydrogen or a straight-chained or branched alkyl group with 1-3 carbon atoms; orR.sub.3 and R.sub.4 together with the nitrogen atom represents a piperidine, morpholine or piperazine ring, while the ring may be substituted by 1 or 2 methyl groups and the piperazine ring at the nitrogen atom in 4-position may also carry a phenyl, chlorophenyl or benzyl group, or they may represent the nortropanyl group, processes for preparing them and pharmaceutical compositions.The new compounds have proved effective in animal trails in alleviating or remedying conditions or restricted cerebral performance.

    摘要翻译： 本发明涉及通式为（I）的新的取代的吡咯烷酮，其中R 1表示可被甲基，甲氧基，氟，氯，溴或三氟甲基或吡啶基单取代或二取代的苯基; R 2表示氢或具有1-4个碳原子的直链或支链烷基; R3表示具有1-3个碳原子的直链或支链烷基，具有2-3个碳原子的羟烷基，可被氯，溴，甲基或甲氧基单取代或二取代的苯基，环己基 基团或二烷基氨基烷基，其中在每个烷基中可以含有1-3个碳原子; R4表示氢或具有1-3个碳原子的直链或支链烷基; 或R 3和R 4与氮原子一起代表哌啶，吗啉或哌嗪环，而环可以被1或2个甲基取代，4-位氮原子上的哌嗪环也可以带有苯基，氯苯基或 或它们可以代表异丙基丙基，其制备方法和药物组合物。 新化合物已被证明在减轻或补救病症或限制性脑部表现方面在动物踪迹中是有效的。

    4-Phenyl-4,5,6,7-tetrahydro-thieno [2,3-c]pyridines, compositions and use
    9.
    发明授权
    4-Phenyl-4,5,6,7-tetrahydro-thieno [2,3-c]pyridines, compositions and use 失效
    4-苯基-4,5,6,7-四氢 - 噻吩并[2,3-c]吡啶，组合物和用途

    公开(公告)号：US4482559A

    公开(公告)日：1984-11-13

    申请号：US466100

    申请日：1983-02-14

    申请人： Claus Schneider ,  Gerhard Walther ,  Karl-Heinz Weber ,  Wolf D. Bechtel ,  Karin Boke-Kuhn

    发明人： Claus Schneider ,  Gerhard Walther ,  Karl-Heinz Weber ,  Wolf D. Bechtel ,  Karin Boke-Kuhn

    IPC分类号： A61K31/435 ,  A61P25/24 ,  A61P25/26 ,  C07D495/04 ,  A61K31/44

    CPC分类号： C07D495/04

    摘要： Compounds of the formula ##STR1## wherein R.sub.1 is amino, acetylamino, hydroxymethyl, methoxymethyl or ##STR2## R.sub.2 and R.sub.3, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, trifluoromethyl, hydroxyl, methoxy, methyl or ethyl;R.sub.4 is straight or branched alkyl of 1 to 3 carbon atoms; andR.sub.5 and R.sub.6, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms or, together with each other and the nitrogen atom to which they are attached, form a 5-, 6- or 7-membered heterocyclic ring where, in the case of a 6-membered ring, a --CH.sub.2 -group in the ring may be replaced by an oxygen atom, and non-toxic, pharmacologically acceptable salts thereof. The compounds as well as their salts are useful as antidepressants.

    摘要翻译： 其中R 1是氨基，乙酰氨基，羟甲基，甲氧基甲基或者R 2和R 3的式（I）化合物可以相同或不同，分别是氢，氟，氯，溴，三氟甲基 ，羟基，甲氧基，甲基或乙基; R4是1〜3个碳原子的直链或支链烷基; 和可以相同或不同的R 5和R 6各自为氢或1至4个碳原子的烷基，或彼此连接并与它们相连的氮原子形成5-，6- 或7-元杂环，其中在6元环的情况下，环中的-CH 2 - 基可被氧原子取代，及其无毒的药学上可接受的盐。 化合物及其盐可用作抗抑郁药。