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    • 1. 发明授权
    • Dual molecules containing a peroxide derivative, synthesis and therapeutic applications thereof
    • 含有过氧化物衍生物的双分子,其合成和治疗应用
    • US07566710B2
    • 2009-07-28
    • US11196979
    • 2005-08-04
    • Bernard MeunierAnne RobertOdile Dechy-CabaretFrancoise Benoit-Vical
    • Bernard MeunierAnne RobertOdile Dechy-CabaretFrancoise Benoit-Vical
    • C07D215/38A61K31/4745A61K31/4709
    • C07D405/12C07D323/04C07D471/04
    • The invention relates to dual molecules formed from coupling products complying with the formula wherein A represents a residue of molecule with anti-malarial activity, Y1 and Y2, represent a linear or branched alkylene chain at C1 to C5, or either Y1 or Y2 is absent, U is an amine, amide, sulphonamide, carboxyl, ether or thioether function, said function linking Y1 and Y2, Z1 and Z2, represent a linear arylene or alkylene, or either Z1 or Z2 is absent, or Z1+Z2 together represent a cyclic or polycyclic structure including the junction carbons Ci and Cj, R1 and R2, represent a hydrogen atom or a functional group capable of increasing the hydrosolubility of the dual molecule, Rx and Ry form a cyclic peroxide with 4 to 8 chain links, Cj being one of the peaks of said cyclic peroxide, or -Rx or Ry is a cyclic peroxide with 4 to 8 chain links, which may comprise 1 or 2 additional oxygen atoms in the cyclic structure, and one or more substituents R3, identical or different, at least one R3 representing a halogen atom, an —OH group, a —CF3 group, an aryl, an alkyl or alkoxy at C1 to C5, —NO2, the other substituent(s) having one of these correspondences or a hydrogen, and their addition salts with pharmacological acceptable acids.
    • 本发明涉及由符合下式的偶联产物形成的双分子:其中A代表具有抗疟疾活性的分子的残基,Y1和Y2代表C1至C5的直链或支链亚烷基链,或Y1或Y2不存在 ,U是胺,酰胺,磺酰胺,羧基,醚或硫醚的功能,所述连接Y1和Y2,Z1和Z2的功能代表线性亚芳基或亚烷基,或不存在Z1或Z2,或Z1 + Z2一起代表 包括连接碳C 1和C 1的环状或多环结构,R 1和R 2表示氢原子或能够增加双分子的水溶性的官能团,Rx和Ry形成具有4至8个链键的环状过氧化物,C j为 所述环状过氧化物的一个峰,或-Rx或Ry是具有4至8个链节的环状过氧化物,其可以在环状结构中包含1或2个另外的氧原子,以及一个或多个相同或不同的取代基R 3, 至少一个R3 代表卤素原子,-OH基团,-CF 3基团,C 1 -C 5的芳基,烷基或烷氧基,-NO 2,具有这些对应关系的其它取代基或氢,以及它们与 药理学可接受的酸。
    • 3. 发明申请
    • Dual molecules containing a peroxide derivative, synthesis and therapeutic applications thereof
    • 含有过氧化物衍生物的双分子,其合成和治疗应用
    • US20050288315A1
    • 2005-12-29
    • US11196979
    • 2005-08-04
    • Bernard MeunierAnne RobertOdile Dechy-CabaretFrancoise Benoit-Vical
    • Bernard MeunierAnne RobertOdile Dechy-CabaretFrancoise Benoit-Vical
    • A61K20060101A61K9/08A61K9/10A61K9/20A61K9/48A61K31/397A61K31/435A61K31/47A61K31/4709A61K31/4745A61K31/513A61P20060101A61P33/06C07D20060101C07D215/00C07D323/04C07D405/12C07D407/12C07D453/04C07D471/02C07D471/04C07D43/02
    • C07D405/12C07D323/04C07D471/04
    • The invention relates to dual molecules formed from coupling products complying with the formula wherein A represents a residue of molecule with anti-malarial activity, Y1 and Y2, represent a linear or ramified alkylene chain at C1 to C5, with the possibility of either Y1 or Y2 being absent, U is an amine, amide, sulphonamide, carboxyl, ether or thioether function, said function linking Y1 and Y2, Z1 and Z2, represent a linear arylene or alkylene, with the possibility of either Z1 or Z2 being absent, or Z1+Z2 together represent a polycyclic structure including the junction carbons Ci and Cj, R1 and R2, represent a hydrogen atom or a functional group capable of increasing the hydrosolubility of the dual molecule, Rx and Ry form a cyclic peroxide with 4 to 8 chain links, Cj being one of the peaks of said cyclic peroxide, or Rx or Ry is a cyclic peroxide with 4 to 8 chain links, which may comprise 1 or 2 additional oxygen atoms in the cyclic structure, and one or more substituents R3, identical or different, at least one representing a halogen atom, an —OH group, a —CF3 group, an aryl, an alkyl or alkoxy at C1 to C5, —NO2, the other substituent(s) having one of these correspondences or a hydrogen, and their addition salts with pharmacological acceptable acids. Application as medicinal products with anti-malarial activity.
    • 本发明涉及由符合下式的偶联产物形成的双分子:其中A表示具有抗疟疾活性的分子的残基Y 1和Y 2 2代表线性 或在C1至C5处带有分支的亚烷基链,其中不存在Y 1或Y 2的可能性,U是胺,酰胺,磺酰胺,羧基,醚或硫醚 功能,所述连接Y 1和Y 2,Z 1和Z 2的功能代表线性亚芳基或 亚烷基,Z 1或Z 2 2个不存在的可能性,或Z 1 + Z 2 2一起 表示包括连接碳C 1和C 1,R 1和R 2的多环结构表示氢原子或能够增加双分子的水溶性的官能团, R x和R y y形成具有4至8个链节的环状过氧化物,C j是所述环状过氧化物的峰之一 氧化物或R x x或R y y是具有4至8个链节的环状过氧化物,其可以在环状结构中包含1或2个另外的氧原子,并且一个或 更多的取代基R 3 3相同或不同,表示卤素原子,-OH基团,-CF 3 N 3基团,芳基,烷基或烷氧基中的至少一个 C 1〜C 5,-NO 2 2,其它取代基具有这些对应之一或氢,以及它们与药理学上可接受的酸的加成盐。 作为具有抗疟活性的药用产品。