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    Chromanone derivatives
    7.
    发明授权
    Chromanone derivatives 失效
    色酮衍生物

    公开(公告)号：US4261988A

    公开(公告)日：1981-04-14

    申请号：US20119

    申请日：1979-03-13

    申请人： Arno Widdig ,  Hans-Joachim Kabbe ,  Martin Scheer ,  Rudiger Sitt

    发明人： Arno Widdig ,  Hans-Joachim Kabbe ,  Martin Scheer ,  Rudiger Sitt

    IPC分类号： A61K31/35 ,  A61K31/352 ,  A61P19/06 ,  C07D311/22 ,  C07D311/24 ,  C07D311/32 ,  C07D311/92 ,  C07D311/96 ,  C07D405/04 ,  C07D491/10 ,  C07D491/107

    CPC分类号： C07D491/10 ,  C07D311/22 ,  C07D311/24 ,  C07D311/32 ,  C07D311/92 ,  C07D311/96

    摘要： Compounds useful in the treatment of cholesterolaemia are of the general formula ##STR1## or salts thereof in which R.sup.1 and R.sup.2 independently denote radicals including hydrogen, alkyl, aryl and heterocyclic radical or together complete a carbocyclic or heterocylic ring, R.sup.3 denotes a radical ##STR2## in which R.sup.9, R.sup.10 and R.sup.11 include hydrogen, cyano, nitro, alkyl and aryl or, in pairs, complete carbocyclic rings, X denotes cyano, nitro or substituted carbonyl, sulphonyl or phosphonyl group, R.sup.4 is hydrogen or a radical defined for R.sup.1 or R.sup.3, and R.sup.5, R.sup.6, R.sup.7 and R.sup.8 include hydrogen, nitro, cyano, carboxyl, alkyl and aryl or, in pairs, complete carbocyclic rings, with the proviso that R.sup.1 and R.sup.9 are not both phenyl if X denotes CO--C.sub.6 H.sub.6. The compounds exhibit considerably higher hypocholesterolaemic activity than the known clofibrate and in addition exhibit a pronounced nutritive effect, e.g., in a medicated fodder or premix.

    摘要翻译： 用于治疗胆固醇血症的化合物具有通式（I）或其盐，其中R 1和R 2独立地表示包括氢，烷基，芳基和杂环基团的基团，或者一起完成碳环或杂环，R3表示 其中R9，R10和R11包括氢，氰基，硝基，烷基和芳基，或成对地成为完全碳环，X表示氰基，硝基或取代的羰基，磺酰基或膦酰基，R4是氢或基团 对于R 1或R 3而言，R 5，R 6，R 7和R 8包括氢，硝基，氰基，羧基，烷基和芳基，或成对地成为完全碳环，条件是如果X表示CO，则R 1和R 9不是苯基 -C6H6。 化合物显示比已知的氯贝特明显更高的降血胆固醇血症活性，并且还显示出明显的营养作用，例如在药物饲料或预混物中。

    Possibly substituted 8-cyano-1-cyclopropyl-7-(2,8-diazabicyclo-[4.3.0]-nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolin carboxylic acids and their derivatives
    9.
    发明授权
    Possibly substituted 8-cyano-1-cyclopropyl-7-(2,8-diazabicyclo-[4.3.0]-nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolin carboxylic acids and their derivatives 有权
    可取代的8-氰基-1-环丙基-7-（2,8-二氮杂双环[4.3.0] - 壬烷-8-基）-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸 酸及其衍生物

    公开(公告)号：US06323213B1

    公开(公告)日：2001-11-27

    申请号：US09125191

    申请日：1998-08-13

    申请人： Stefan Bartel ,  Thomas Jaetsch ,  Thomas Himmler ,  Hans-Georg Rast ,  Werner Hallenbach ,  Ernst Heinen ,  Franz Pirro ,  Martin Scheer ,  Michael Stegemann ,  Hans-Peter Stupp ,  Heinz-Georg Wetzstein

    发明人： Stefan Bartel ,  Thomas Jaetsch ,  Thomas Himmler ,  Hans-Georg Rast ,  Werner Hallenbach ,  Ernst Heinen ,  Franz Pirro ,  Martin Scheer ,  Michael Stegemann ,  Hans-Peter Stupp ,  Heinz-Georg Wetzstein

    IPC分类号： A61K31407

    CPC分类号： C07D471/04 ,  A01N43/90

    摘要： The present invention relates to novel optionally substituted 8-cyano-1-cyclo-propyl-7-(2,8-diazabicyclo[4.3.0]nonan-8-yl)-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids and their derivatives, of the general formula (I) in which R1 represents hydrogen, C1-C4-alkyl which is optionally substituted by hydroxyl, methoxy, amino, methylamino or dimethylamino, or (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl, R2 represents hydrogen, benzyl, C1-C3-alkyl, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl, radicals having the structures —CH═CH—COOR3, —CH2CH2COOR3, —CH2CH2CN, —CH2CH2COCH3 or —CH2COCH3, in which R3 represents methyl or ethyl, or a radical of the general structure R4—(NH—CHR5—CO)n—, in which R4 represents hydrogen, C1-C3-alkyl or the radical —COO-tert-butyl, R5 represents hydrogen, C1-C4-alkyl, hydroxyalkyl, aminoalkyl, thioalkyl, carboxyalkyl or benzyl and n is 1 or 2, and Y is oxygen or sulfur, the process for their preparation and their use in antibacterial compositions.

    摘要翻译： 本发明涉及新的任选取代的8-氰基-1-环丙基-7-（2,8-二氮杂双环[4.3.0]壬烷-8-基）-6-氟-1,4-二氢-4- 甲氧基，氨基，甲基氨基或二甲基氨基取代的C 1 -C 4 - 烷基，或（5-甲基-2-羟基喹啉羧酸）或其衍生物，其中R 1表示氢， 氧代-1,3-二氧杂环戊烯-4-基）甲基，R 2表示氢，苄基，C 1 -C 3 - 烷基，（5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基）甲基， 结构-CH = CH-COOR 3，-CH 2 CH 2 COOR 3，-CH 2 CH 2 CN，-CH 2 CH 2 COCH 3或-CH 2 COCH 3，其中R 3表示甲基或乙基，或通式结构R4-（NH-CHR5-CO）n - 的基团，其中R4 代表氢，C 1 -C 3 - 烷基或-COO-叔丁基，R 5表示氢，C 1 -C 4 - 烷基，羟基烷基，氨基烷基，硫代烷基，羧基烷基或苄基，n是1或2，Y是氧或硫， 其制备方法及其在抗菌组合物中的应用。