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72 条记录 (耗时 0.033 秒)

    Tripeptides acting on the central nervous system and a process for the preparation thereof
    62.
    发明授权
    Tripeptides acting on the central nervous system and a process for the preparation thereof 失效
    作用于中枢神经系统的三肽及其制备方法

    公开(公告)号：US4299821A

    公开(公告)日：1981-11-10

    申请号：US163829

    申请日：1980-06-27

    申请人： Lajos Kisfaludy ,  Tamas Szirtes ,  Lajos Balaspiri ,  Eva Palosi ,  Laszlo Szporny ,  Adam Sarkadi

    发明人： Lajos Kisfaludy ,  Tamas Szirtes ,  Lajos Balaspiri ,  Eva Palosi ,  Laszlo Szporny ,  Adam Sarkadi

    IPC分类号： C07K5/08 ,  A61K38/04 ,  A61K38/06 ,  A61P25/00 ,  C07K1/113 ,  C07K5/062 ,  C07K5/097 ,  C07K14/575 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K5/06034 ,  C07K5/06043 ,  C07K5/06104 ,  C07K5/0825

    摘要： The invention relates to new peptide derivatives which act on the central nervous system and correspond to the general formula (I),Glp--X--Y--NH--A (I)whereinX is L-norleucyl, L-leucyl, L-norvalyl, D-leucyl, L-prolyl, L-2-aminobutyryl, L-valyl, L-threonyl, L-isoleucyl, L-2-aminodecanoyl, L-cyclohexylalanyl or L-tert.-butyl-seryl group andY is L-prolyl group, orX is L-histidyl group andY is L-homoprolyl or D-pipecolyl group, furthermoreA is hydrogen, a C.sub.1-10 alkyl group or a C.sub.1-3 alkyl group having a dimethylamino substituent,with the proviso that if X is L-leucyl group, A is other than hydrogen, and pharmaceutically acceptable complexes thereof.These compounds are prepared by methods commonly applied in the peptide chemistry.

    摘要翻译： 本发明涉及作用于中枢神经系统且对应于通式（I）的Glp-XY-NH-A（I）的新型肽衍生物，其中X为L-正亮氨酰基，L-亮氨酰，L-缬氨酰基，D -L-脯氨酰基，L-苏氨酸，L-异亮氨酰基，L-2-氨基十一烷酰基，L-环己基丙氨酰基或L-叔丁基 - 丝氨酰基，Y是L-脯氨酰基，L-脯氨酰基，L-2-氨基丁酰基， 基团，或X为L-组氨酰基，Y为L-顺式或D-哌啶基，此外A为氢，C1-10烷基或具有二甲基氨基取代基的C1-3烷基，条件是如果X 是L-亮氨酰基，A不是氢，和其药学上可接受的复合物。 这些化合物通过肽化学中常用的方法制备。

    2,3-Dihydro-7-chlorothiazolo[3,2-a]benzimidazole and salt
    66.
    发明授权
    2,3-Dihydro-7-chlorothiazolo[3,2-a]benzimidazole and salt 失效
    2,3-二氢-7-氯噻唑并[8 3,2-a {9苯并咪唑和盐

    公开(公告)号：US4017507A

    公开(公告)日：1977-04-12

    申请号：US637978

    申请日：1975-12-05

    申请人： Kalman Hideg ,  Olga Hankovszky ,  Eva Palosi ,  Gyorgy Hajos ,  Laszlo Szporny

    发明人： Kalman Hideg ,  Olga Hankovszky ,  Eva Palosi ,  Gyorgy Hajos ,  Laszlo Szporny

    IPC分类号： C07D513/04

    CPC分类号： C07D513/04

    摘要： New tricyclic fused imidazole derivatives of the general formula (I), ##STR1## wherein R.sub.1 stands for hydrogen or hydroxy,n is equal to zero or one,m is equal to zero, one or two,A stands for a group of the general formula (II), ##STR2## wherein R.sub.2 represents hydrogen or hydroxy,R.sub.3 represents hydrogen or amino, orQ and Z each stand for nitrogen or a=C-- group, orA stands for a group of the general formula (III), ##STR3## wherein R.sub.4 and R.sub.5 each represent hydrogen, methyl, chlorine or nitro,Were prepared by reacting a compound of the general formula (IV) ##STR4## wherein A and n each have the same meanings as defined above, with a compound of the general formula (V), ##STR5## wherein X stands for halogen, R.sub.6 stands for hydrogen and R.sub.7 stands for a group of the general formula (VI),--(ch.sub.2).sub.m --X VI.in which m and X each have the same meanings as defined above, or R.sub.6 and R.sub.7 together stand for oxygen. The reaction is carried out optionally in the presence of a base. The compounds of the general formula (I) can be converted into their acid addition salts.The compounds of the general formula (I) as well as their acid addition salts exert antipyretic and antiphlogistic activities, inhibit the reproduction of viruses, and exert a protecting effect against albumine shock.

    摘要翻译： 通式（I）的新型三环稠合咪唑衍生物，其中R1代表氢或羟基，N等于零或一，M等于零，一或二，A代表一个基团 的通式（II），其中R 2表示氢或羟基，R 3表示氢或氨基，或Q和Z各自代表氮或a = C-基团，或A表示一个 通式（III），其中R 4和R 5各自代表氢，甲基，氯或硝基，通过反应通用化合物（IV）化合物（IV）制备其中A和n各自 具有与上述定义相同的含有通式（Ⅴ）的化合物，其中X代表卤素，R6代表氢，R7代表通式（Ⅵ）的基团， （CH2）mX VI。

    Tricyclic imidazole derivatives
    67.
    发明授权
    Tricyclic imidazole derivatives 失效
    三环咪唑衍生物

    公开(公告)号：US3932395A

    公开(公告)日：1976-01-13

    申请号：US473184

    申请日：1974-05-24

    申请人： Kalman Hideg ,  Olga Hankovszky ,  Eva Palosi ,  Gyorgy Hajos ,  Laszlo Szporny

    发明人： Kalman Hideg ,  Olga Hankovszky ,  Eva Palosi ,  Gyorgy Hajos ,  Laszlo Szporny

    IPC分类号： C07D513/16 ,  C07D513/04 ,  C07D513/14 ,  C07D279/08 ,  C07D279/14

    CPC分类号： C07D513/04 ,  C07D513/14 ,  Y10S514/916

    摘要： New tricyclic fused imidazole derivatives of the general formula (I), ##SPC1##whereinR.sub.1 stands for hydrogen or hydroxy,n is equal to zero or one,m is equal to zero, one or two,A stands for a group of the general formula (II), ##EQU1## wherein R.sub.2 represents hydrogen or hydroxy,R.sub.3 represents hydrogen or amino, orQ and Z each stand for nitrogen or a =C-- group, orA stands for a group of the general formula (III), ##EQU2## wherein R.sub.4 and R.sub.5 each represent hydrogen, methyl, chlorine or nitro,Were prepared by reacting a compound of the general formula (IV) ##SPC2##wherein A and n each have the same meanings as defined above, with a compound of the general formula (V), ##EQU3## wherein X stands for halogen, R.sub.6 stands for hydrogen and R.sub.7 stands for a group of the general formula (VI),--(CH.sub.2).sub.m --X (VI)in which m and X each have the same meanings as defined above, or R.sub.6 and R.sub.7 together stand for oxygen. The reaction is carried out optionally in the presence of a base. The compounds of the general formula (I) can be converted into their acid addition salts.The compounds of the general formula (I) as well as their acid addition salts exert antipyretic and antiphlogistic activities, inhibit the reproduction of viruses, and exert a protecting effect against albumine shock.

    摘要翻译： 新的通式（I）的三环稠合咪唑衍生物，其中R1代表氢或羟基，N等于零或一，M等于零，一或二，A代表通式（II ），-C = QC = Z- |（II）R2R3其中R2表示氢或羟基，R3表示氢或氨基，或Q和Z各自代表氮或a = C-基团，或A表示 通式（III）-CH = C-C = CH- |（III）R4R5其中R4和R5各自表示氢，甲基，氯或硝基，通过反应通用化合物（IV）的化合物制备， 其中A和n各自具有与上述相同的含义，与通式（V）的化合物，X-CH 2 -CH-CH 2 ||（V）R 6 R 7，其中X代表卤素，R6代表氢，R7 代表通式（VI）， - （CH 2）m X（VI）的基团，其中m和X各自具有与上述相同的含义，或者R6和R7一起代表氧。 任选地在碱的存在下进行反应。 通式（I）的化合物可以转化成它们的酸加成盐。

    1-cyclohexyl-3,4-dihydroisoquinoline derivatives and pharmaceutical compositions containing them
    68.
    发明授权
    1-cyclohexyl-3,4-dihydroisoquinoline derivatives and pharmaceutical compositions containing them 失效
    1-环己基-3,4-二氢异喹啉衍生物和含有它们的药物组合物

    公开(公告)号：US4622329A

    公开(公告)日：1986-11-11

    申请号：US721880

    申请日：1985-04-10

    申请人： Gabor Bernath ,  Jeno Kobor ,  Janos Lazar ,  Gabor Motika ,  Elemer Ezer ,  Gyorgy Hajos ,  Eva Palosi ,  Laszlo Denes ,  Laszlo Szporny

    发明人： Gabor Bernath ,  Jeno Kobor ,  Janos Lazar ,  Gabor Motika ,  Elemer Ezer ,  Gyorgy Hajos ,  Eva Palosi ,  Laszlo Denes ,  Laszlo Szporny

    IPC分类号： C07D217/16 ,  A61K31/47 ,  A61K31/472 ,  A61P1/04 ,  A61P25/04 ,  A61P25/08 ,  A61P25/20 ,  A61P25/30 ,  A61P39/02 ,  C07D217/14

    CPC分类号： C07D217/14

    摘要： The invention relates to new 1-cyclohexyl-3,4-dihydroisoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents hydrogen, hydroxyl or alkoxy having from 1 to 6 carbon atoms,X is oxygen andZ is a .dbd.CH.sub.2 or .dbd.CH--COOR.sup.3 group, in which R.sup.3 is hydrogen or alkyl having from 1 to 6 carbon atoms; orX represents an .dbd.NR.sup.4 group, in which R.sup.4 is hydrogen or hydroxyl, andZ is a .dbd.CH--CN, .dbd.CH.sub.2 or .dbd.CH--COOR.sup.3 group, in which R.sup.3 is as defined above,and acid addition salts thereof.The compounds of formula (I) are pharmaceutically active, in particular show antispasm, analgesic, gastric acid secretion inhibiting, sedative and hypnotic activity and effectively reduce the alcoholic narcosis time. According to a further aspect of the invention there is provided a process for the preparation of these compounds. The invention further relates to pharmaceutical compositions containing them as active ingredient.

    摘要翻译： 本发明涉及式（I）的新的1-环己基-3,4-二氢异喹啉衍生物其中R 1和R 2各自独立地表示氢，羟基或具有1至6个碳原子的烷氧基，X是氧 Z为a = CH 2或= CH-COOR 3基团，其中R 3为氢或具有1至6个碳原子的烷基; 或X表示= NR4基团，其中R4为氢或羟基，Z为a = CH-CN，= CH2或= CH-COOR3基团，其中R3如上定义，及其酸加成盐。 式（I）的化合物是药学活性的，特别是表现出痉挛，镇痛，胃酸分泌抑制，镇静和催眠活性，并有效降低酒精性麻醉时间。 根据本发明的另一方面，提供了制备这些化合物的方法。 本发明还涉及含有它们作为活性成分的药物组合物。