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    • 3. 发明授权
    • Phospholipid compound
    • US4492659A
    • 1985-01-08
    • US395954
    • 1982-07-07
    • Elmar BosiesRudi GallGunter WeimannUwe BickerWulf Pahlke
    • Elmar BosiesRudi GallGunter WeimannUwe BickerWulf Pahlke
    • A61K31/66A61P35/00C07F9/09C07F9/10C07F9/02
    • C07F9/10C07F9/091
    • The present invention provides phospholipids of the general formula: ##STR1## wherein X is a valency bond, an oxygen or sulphur atom or a sulfonyl, sulfinyl, phenylene, cycloaklylene, carbonylamino, aminocarbonyl, ureido or carbonyl group, R.sub.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated aliphatic hydrocarbon radical containing up to 18 carbon atoms, which is optionally substituted one or more times by halogen, alkoxy, alkylthio, alkanesulfinyl, alkanesulfonyl, carbalkoxy or phenyl, R.sub.2 is a straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing up to 18 carbon atoms, which is optionally substituted one or more times by halogen, alkoxy, alkylthio, alkanesulphinyl, alkanesulphonyl, carbalkoxy or phenyl, Y is an oxygen atom or a --O--CO--O--, --O--CO--NH-- or --O--CS--NH-- group, R.sub.3 is a straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon radical containing 2 to 8 carbon atoms, which can also be part of a cycloalkane ring system and is optionally substituted one or more times by hydroxyl, halogen, alkylthio, alkanesulphinyl, alkanesulfonyl, nitrile, alkoxycarbonyl, carboxamido optionally substituted by alkyl radicals, cycoalkyl, optionally substituted phenyl or alkoxy, which in turn is optionally substituted by phenyl, hydroxyl, alkoxy, alkylthio, alkanesulfinyl, alkanesulfonyl, optionally acylated amino, alkoxycarbonyl, nitrile or carboxamido optionally substituted by alkyl radicals, Z is an oxygen or sulfur atom, R.sub.4 is a straight-chained or branched alkylene radical containing 2 to 5 carbon atoms and R.sub.5 is a hydrogen atom or a lower alkyl radical, with the proviso that when X is a valency bond, R.sub.1 and R.sub.2 together represent an unsubstituted, straight-chained or branched, saturated or unsaturated divalent aliphatic hydrocarbon chain containing up to 18 carbon atoms, Y, R.sub.4 and R.sub.5 have the above-given meanings and Z is an oxygen atom, R.sub.3 cannot be a propylene or 2-methylpropylene chain optionally substituted by hydroxyl, alkoxy or benzyloxy and with the proviso that when X is a valency bond, R.sub.1 and R.sub.2 together signify an alkyl radical containing up to 18 carbon atoms and substituted by halogen or phenyl, Y and Z are oxygen atoms and R.sub.4 and R.sub.5 have the above-given meanings, R.sub.3 cannot be a propylene or 2-hydroxypropylene chain; and the pharmacologically acceptable salts thereof.The invention also provides pharmaceutical compositions containing such compounds, having cancerostatic action without inducing thrombocyte aggregation.
    • 7. 发明授权
    • 3-Nitropyrazole compounds and anti-microbial compositions
    • 3-硝基吡唑化合物和抗微生物组合物
    • US4172136A
    • 1979-10-23
    • US889594
    • 1978-03-23
    • Herbert BergerRudi GallKurt Stach, deceasedMax ThielWolfgang Vomel
    • Herbert BergerRudi GallKurt Stach, deceasedMax ThielWolfgang Vomel
    • C07D231/16C07D401/02C07D403/02
    • C07D231/16
    • New 3-nitropyrazole compounds of the formula: ##STR1## wherein R.sub.1 is lower alkyl;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is cyano, carboxyl or lower alkoxycarbonyl or the radical --CO-NR.sub.4 R.sub.5, in whichR.sub.4 is hydrogen or hydroxyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, thiocarbamoyl, ureido, thioureido, hydroxyphenyl, picolyl or is a lower alkyl, alkenyl or cycloalkyl radical substituted, if desired, by a cyano, hydroxyl, pyrrolidino, piperidino, amino, lower alkylamino, lower dialkylamino or lower acylamino substituent andR.sub.5 is a hydrogen atom or a lower alkyl radical orR.sub.4 and R.sub.5 together represent a lower alkylene bridge;And the pharmacologically compatible salts thereof are outstandingly effective as anti-microbial agents, particularly systemically and in the urinary tract.
    • 新的具有下式的3-硝基吡唑化合物:其中R 1是低级烷基; R2是氢或低级烷基; R3是氰基,羧基或低级烷氧基羰基或基团-CO-NR4R5,其中R4是氢或羟基,氨基甲酰基,烷基氨基甲酰基,二烷基氨基甲酰基,硫代氨基甲酰基,脲基,硫脲基,羟基苯基,吡啶甲基或是低级烷基,烯基或环烷基取代 如果需要,通过氰基,羟基,吡咯烷子基,哌啶子基,氨基,低级烷基氨基,低级二烷基氨基或低级酰基氨基取代基,R 5是氢原子或低级烷基,或者R 4和R 5一起代表低级亚烷基桥; 并且其药理学兼容的药物作为抗微生物药剂,特别是在系统性和在尿道感染中是非常有效的。