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    • 3. 发明授权
    • Derivatives of 2-phenyl-3-hydroxyquinoline-4(1H)-one and methods of their preparation and utilization
    • 2-苯基-3-羟基喹啉-4(1H) - 酮的衍生物及其制备和利用方法
    • US08299092B2
    • 2012-10-30
    • US12439723
    • 2007-07-26
    • Petr KrejciPavel HradilJan HlavacMarian Hajduch
    • Petr KrejciPavel HradilJan HlavacMarian Hajduch
    • A61K31/4709C07D215/00
    • C07D215/233C07D401/04
    • Derivatives of 2-phenyl-3-hydroxyquinoline-4(1H)-one of the general formula (II), where X represents a nitro group, amino group, and Y represents an atom of halogen, oxygen or sulphur substituted by C1 to C6 alkyl or phenyl group, whereby both the alkyl and phenyl group may be further substituted and the substituents may be identical or different, or by nitrogen substituted independently by hydrogen, C1 to C6 alkyl, C1 to C6 alkyl, which may be substituted among others by halogen, hydroxy, C1 to C4 alkoxy or C1 to C4 alkylamino group, or may form a saturated or unsaturated heterocyclic ring with 5 to 7 atoms, where the individual ring atoms comprise atoms of carbon, and any of the carbon atoms may be substituted by an atom of nitrogen, sulphur or oxygen, X and Y together form an imidazo group, or imidazo group substituted by C1 to C6 alkyl, which may be substituted among others by halogen, hydroxy, C1 to C4 alkoxy or C1 to C4 alkylamino group, CHO or acetylgroup, or a heterocyclic ring with 5 to 6 atoms, where the ring atoms may be further substituted. Methods of preparation of these compounds are described. In addition, their cytostatic, cytotoxic, antiproliferation and immunosuppressive activity is described including examples of their potential pharmacological and pharmaceutical utilization.
    • 通式(II)的2-苯基-3-羟基喹啉-4(1H) - 酮的衍生物,其中X表示硝基,氨基,Y表示被C1-C6取代的卤素,氧或硫原子 烷基或苯基,其中烷基和苯基可以被进一步取代,取代基可以相同或不同,或者被氢独立地取代的氮,C1-C6烷基,C1-C6烷基,其可以被 卤素,羟基,C 1〜C 4烷氧基或C 1〜C 4烷基氨基,或者可以形成具有5〜7个原子的饱和或不饱和杂环,其中各个环原子包含碳原子,并且任何碳原子可以被 氮,硫或氧原子,X和Y一起形成咪唑基或被C1至C6烷基取代的咪唑基,其可以被卤素,羟基,C1-C4烷氧基或C1-C4烷基氨基取代, CHO或乙酰基,或杂环 具有5至6个原子,其中环原子可以被进一步取代。 描述了这些化合物的制备方法。 此外,还描述了它们的细胞生长抑制,细胞毒性,抗增殖和免疫抑制活性,包括其潜在的药理和药物利用的实例。
    • 5. 发明申请
    • DERIVATIVES OF 2-PHENYL-3-HYDROXYQUINOLINE-4(1H)-ONE AND METHODS OF THEIR PREPARATION AND UTILIZATION
    • 2-苯基-3-羟基喹啉-4(1H) - 酮的衍生物及其制备和利用方法
    • US20100022587A1
    • 2010-01-28
    • US12439723
    • 2007-07-26
    • Petr KrejciPavel HradilJan HlavacMarian Hajduch
    • Petr KrejciPavel HradilJan HlavacMarian Hajduch
    • A61K31/4709C07D215/00C07D401/02A61K31/47A61P35/00A61P37/00A61P31/00
    • C07D215/233C07D401/04
    • Derivatives of 2-phenyl-3-hydroxyquinoline-4(1H)-one of the general formula (II), where X represents a nitro group, amino group, and Y represents an atom of halogen, oxygen or sulphur substituted by C1 to C6 alkyl or phenyl group, whereby both the alkyl and phenyl group may be further substituted and the substituents may be identical or different, or by nitrogen substituted independently by hydrogen, C1 to C6 alkyl, C1 to C6 alkyl, which may be substituted among others by halogen, hydroxy, C1 to C4 alkoxy or C1 to C4 alkylamino group, or may form a saturated or unsaturated heterocyclic ring with 5 to 7 atoms, where the individual ring atoms comprise atoms of carbon, and any of the carbon atoms may be substituted by an atom of nitrogen, sulphur or oxygen, X and Y together form an imidazo group, or imidazo group substituted by C1 to C6 alkyl, which may be substituted among others by halogen, hydroxy, C1 to C4 alkoxy or C1 to C4 alkylamino group, CHO or acetylgroup, or a heterocyclic ring with 5 to 6 atoms, where the ring atoms may be further substituted. Methods of preparation of these compounds are described. In addition, their cytostatic, cytotoxic, antiproliferation and immunosuppressive activity is described including examples of their potential pharmacological and pharmaceutical utilization.
    • 通式(II)的2-苯基-3-羟基喹啉-4(1H) - 酮的衍生物,其中X表示硝基,氨基,Y表示被C1-C6取代的卤素,氧或硫原子 烷基或苯基,其中烷基和苯基可以被进一步取代,取代基可以相同或不同,或者被氢独立地取代的氮,C1-C6烷基,C1-C6烷基,其可以被 卤素,羟基,C 1〜C 4烷氧基或C 1〜C 4烷基氨基,或者可以形成具有5〜7个原子的饱和或不饱和杂环,其中各个环原子包含碳原子,并且任何碳原子可以被 氮,硫或氧原子,X和Y一起形成咪唑基或被C1至C6烷基取代的咪唑基,其可以被卤素,羟基,C1-C4烷氧基或C1-C4烷基氨基取代, CHO或乙酰基,或杂环 具有5至6个原子,其中环原子可以被进一步取代。 描述了这些化合物的制备方法。 此外,还描述了它们的细胞生长抑制,细胞毒性,抗增殖和免疫抑制活性,包括其潜在的药理和药物利用的实例。