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8 条记录 (耗时 0.203 秒)

    Heterocyclic compounds containing an alkoxycarbonyl and a substituted methyl group
    2.
    发明授权
    Heterocyclic compounds containing an alkoxycarbonyl and a substituted methyl group 失效
    含有烷氧羰基和取代甲基的杂环化合物

    公开(公告)号：US4435322A

    公开(公告)日：1984-03-06

    申请号：US301191

    申请日：1981-09-11

    申请人： Karoly Lempert ,  Kalman Harsanyi ,  Gabor Doleschall ,  Gyula Hornyak ,  Jozsef Nyitrai ,  Karoly Zauer ,  Jozsef Fetter ,  Gyula Simig ,  Zsuzsanna Visky nee Gombos ,  Gizella Barta nee Szalai

    发明人： Karoly Lempert ,  Kalman Harsanyi ,  Gabor Doleschall ,  Gyula Hornyak ,  Jozsef Nyitrai ,  Karoly Zauer ,  Jozsef Fetter ,  Gyula Simig ,  Zsuzsanna Visky nee Gombos ,  Gizella Barta nee Szalai

    IPC分类号： C07D205/08 ,  C07D487/04

    CPC分类号： C07D205/08

    摘要： The invention relates to new heterocyclic compound containing an alkoxycarbonyl and a substituted methyl group a process for the preparation of these and analogeous compound and pharmaceutical compositions containing them.More particularly, the invention concerns compounds of the general formula (IVa) ##STR1## wherein R' is hydrogen, 2-ethoxycarbonylethyl, aryl or a group suitable for a temporary protection of amides andY' represents a group of the formula --COOZ or --CH.sub.2 M, in whichZ is lower alkyl andM is hydroxyl, halogen, cyano or a group of the formula --O--SO.sub.2 R.sup.2, in whichR.sup.2 is lower alkyl or aryl,with the proviso that if R' is phenyl, Y' cannot stand for the group --COOC.sub.2 H.sub.5.The invention further relates to a process for the preparation of compounds of the general formula (IV) ##STR2## in which R and Y are identical with R' and Y', respectively, except the proviso.According to a further aspect of the invention there are provided pharmaceutical compositions, first of all with antihypoxic activity, comprising compounds of the general formula (IVa) as active ingredient.

    摘要翻译： 本发明涉及含有烷氧基羰基和取代的甲基的新的杂环化合物，其制备这些和分解化合物的方法和含有它们的药物组合物。 更具体地说，本发明涉及通式（IVa）（IVa）的化合物，其中R'是氢，2-乙氧基羰基乙基，芳基或适于临时保护酰胺的基团，Y'代表式 -COOZ或-CH2M，其中Z是低级烷基，M是羟基，卤素，氰基或式-O-SO2R2的基团，其中R2是低级烷基或芳基，条件是如果R'是苯基， Y'不能代表组-COOC2H5。 本发明还涉及制备通式（IV）的化合物（IV）的方法，其中R和Y分别与R'和Y'相同，但条件是。 根据本发明的另一方面，提供首先具有抗缺氧活性的药物组合物，其包含通式（IVa）的化合物作为活性成分。

    Process for the preparation of aminolactone carboxylic acid
    6.
    发明授权
    Process for the preparation of aminolactone carboxylic acid 失效
    制备氨基内酯羧酸的方法

    公开(公告)号：US4559406A

    公开(公告)日：1985-12-17

    申请号：US508436

    申请日：1983-06-27

    申请人： Karoly Lempert ,  Gabor Doleschall ,  Jozsef Fetter ,  Gyula Hornyak ,  Jozsef Nyitrai ,  Gyula Simig ,  Karoly Zauer

    发明人： Karoly Lempert ,  Gabor Doleschall ,  Jozsef Fetter ,  Gyula Hornyak ,  Jozsef Nyitrai ,  Gyula Simig ,  Karoly Zauer

    IPC分类号： C07D205/08 ,  C07D207/26 ,  C07D207/277 ,  C07D207/28 ,  C07D309/30 ,  C07D405/04

    CPC分类号： C07D207/277 ,  C07D205/08 ,  C07D207/28 ,  C07D309/30 ,  C07D405/04 ,  Y02P20/55

    摘要： The invention relates to a process for the preparation of the compound of the formula I, ##STR1## which comprises (a.sub.1) splitting off the ethylene ketal protecting group from the azetidinone derivative of the formula IVa, ##STR2## reducing the compound of the formula III thus obtained, ##STR3## treating the resulting compound of the formula II ##STR4## with concentrated aqueous hydrogen chloride solution; or (a.sub.2) reducing the compound of the formula III, treating the compound of the formula II thus obtained with concentrated aqueous hydrogen chloride solution; or (a.sub.3) treating the compound of the formula II with concentrated aqueous hydrogen chloride solution; and isolating the compound of the formula I thus obtained from the reaction mixture. The compound of the formula I is useful as an intermediate in the production of thienamycin, a highly potent antibiotic.

    摘要翻译： 本发明涉及一种制备式I化合物的方法，其包括（a1）将亚乙基缩酮保护基从式IVa的氮杂环丁酮衍生物中分离出来， 由此获得的式III，使用浓缩的氯化氢水溶液处理所得式II的化合物; 或（a2）还原式III的化合物，用浓缩的氯化氢水溶液处理由此获得的式II化合物; 或（a3）用浓缩的氯化氢水溶液处理式II的化合物; 并从反应混合物中分离得到的式I化合物。 式I的化合物可用作生产高效抗生素的噻吩霉素的中间体。

    Azetidinone acetic acid derivatives and process for the preparation thereof
    7.
    发明授权
    Azetidinone acetic acid derivatives and process for the preparation thereof 失效
    氮杂环丁酮乙酸衍生物及其制备方法

    公开(公告)号：US4587049A

    公开(公告)日：1986-05-06

    申请号：US549681

    申请日：1983-11-07

    申请人： Karoly Lempert ,  Ferenc Bartha ,  Gabor Doleschall ,  Jozsef Fetter ,  Gyula Hornyak ,  Jozsef Nyitrai ,  Gyula Siming ,  Karoly Zauer

    发明人： Karoly Lempert ,  Ferenc Bartha ,  Gabor Doleschall ,  Jozsef Fetter ,  Gyula Hornyak ,  Jozsef Nyitrai ,  Gyula Siming ,  Karoly Zauer

    IPC分类号： C07D205/08

    CPC分类号： C07D205/08

    摘要： The invention relates to compounds of the general formula (X) ##STR1## wherein R is as a removable protecting substituent of the amido group a phenyl group or a benzyl group substituted by one or more alkoxy group(s) having 1-4 carbon atoms andR.sup.1 stands for a hydrogen atom or an alkyl group having 1-4 carbon atoms and a process for the preparation thereof.The compounds of the general formula (X) can be prepared from the starting materials of the general formula (V), wherein R and R.sup.1 are as stated above and Z is an alkyl group having 1-4 carbon atoms.The compounds of the general formula (X) are useful pharmaceutical intermediates which can be used in the preparation of known antibiotics (e.g. Thienamycin and PS-5).

    摘要翻译： 本发明涉及通式（X）的化合物（X）其中R为酰氨基的可除去保护取代基，苯基或被一个或多个具有1-羟基的烷氧基取代的苄基， 4个碳原子，R1代表氢原子或具有1-4个碳原子的烷基及其制备方法。 通式（X）的化合物可以由通式（V）的起始原料制备，其中R和R 1如上所述，Z是具有1-4个碳原子的烷基。 通式（X）的化合物是可用于制备已知抗生素（例如硫霉素和PS-5）的有用的药物中间体。

    2-(substituted imino)-thiazolidines and process for the preparation thereof
    8.
    发明授权
    2-(substituted imino)-thiazolidines and process for the preparation thereof 失效
    2-（取代的亚氨基） - 噻唑啉及其制备方法

    公开(公告)号：US5240918A

    公开(公告)日：1993-08-31

    申请号：US857067

    申请日：1992-03-24

    申请人： Karoly Lempert ,  Gyula Hornyak ,  Jozsef Fetter ,  Antal Feller ,  Klara Gaso ,  Gabor Gigler ,  Laszlo Kapolnai ,  Lujza Petocz ,  Katalin Szemeredi ,  Marton Fekete

    发明人： Karoly Lempert ,  Gyula Hornyak ,  Jozsef Fetter ,  Antal Feller ,  Klara Gaso ,  Gabor Gigler ,  Laszlo Kapolnai ,  Lujza Petocz ,  Katalin Szemeredi ,  Marton Fekete

    IPC分类号： C07D277/18

    CPC分类号： C07D277/18

    摘要： The invention relates to new 2-(substituted imino)-thiazolidines, a process for the preparation thereof, pharmaceutical compositions comprising the same, the use of the said 2-(substituted imino)thiazolidines for the treatment of diseases and for the preparation of pharmaceutical compositions suitable for the treatment of diseases.The new 2-(substituted imino)-thiazolidine derivatives provided by the present invention correspond to the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each represent halogen, nitro, C.sub.1-4 alkoxy or C.sub.1-4 alkyl, which latter may optionally carry one or more halogen substituent(s),R.sup.3 and R.sup.4 each represent hydrogen or C.sub.1-4 alkyl,Z denotes oxygen, sulfur or imino, which latter is substituted by a C.sub.1-6 alkyl or a C.sub.1-6 alkenyl group,R.sup.5 stands for hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkylthio or a group or the formula --NH--R, wherein R represents C.sub.1-6 alkyl, aryl, aralkyl or C.sub.1-6 alkenyl optionally carrying a halogen or a di-(C.sub.1-4 alkyl)-amino substituent; orZ and R.sup.5 together stand for a trivalent nitrogen atom, with the proviso that if Z denotes a substituted imino group, R.sup.5 stands for C.sub.1-4 alkylthio, and if R.sup.5 is C.sub.1-4 alkylthio, Z represents a substituted imino, and with the further proviso that if Z denotes sulfur, R.sup.5 is other than hydrogen or C.sub.1-4 alkyl,and possess valuable antianginal and analgesic properties.

    摘要翻译： 本发明涉及新的2-（取代的亚氨基） - 噻唑烷，其制备方法，包含该方法的药物组合物，所述2-（取代的亚氨基）噻唑烷用于治疗疾病和用于制备药物 适用于治疗疾病的组合物。 本发明提供的新的2-（取代亚氨基） - 噻唑烷衍生物对应于通式（I），其中R 1和R 2各自表示卤素，硝基，C 1-4烷氧基或C 1-4烷基 ，其可以任选地带有一个或多个卤素取代基，R 3和R 4各自表示氢或C 1-4烷基，Z表示氧，硫或亚氨基，后者被C 1-6烷基或C 1-6 烯基，R5代表氢，C1-4烷基，C1-4烷硫基或基团-NH-R，其中R表示C1-6烷基，芳基，芳烷基或任选携带卤素或 二（C 1-4烷基） - 氨基取代基; 或Z和R5一起代表三价氮原子，条件是如果Z表示取代的亚氨基，则R5表示C1-4烷硫基，如果R5是C1-4烷硫基，则Z表示取代的亚氨基，并且与 进一步的条件是，如果Z表示硫，R5不是氢或C1-4烷基，并且具有有价值的抗心绞痛和止痛特性。