公开(公告)号：US20120122923A1

公开(公告)日：2012-05-17

申请号：US12332633

申请日：2008-12-11

申请人： Frederic COSLEDAN ,  Bernard MEUNIER ,  Alain PELLET

发明人： Frederic COSLEDAN ,  Bernard MEUNIER ,  Alain PELLET

IPC分类号： A61K31/47 ,  A61P33/06 ,  C07D405/12

CPC分类号： C07D405/12

摘要： The invention concerns dual molecules corresponding to formula (I): in which: A represents a molecular residue with antimalarial activity of formula (IIa) or (IIIa) or a residue facilitating bioavailability; B represents a cycloalkyl group potentially substituted, or B represents a bi- or tricyclic group capable of being substituted, or B represents 2 cycloalkyl groups linked together through either a single bond or an alkylene chain; m and n represent independently of one another 0, 1 or 2; R5 represents a hydrogen atom, an alkyl, cycloalkyl or C1-3-alkylene-cycloakyl group; Z1 and Z2 represent an alkyl radical, the group Z1+Z2+Ci+Cj representing a mono- or polycyclic structure, with one of the Z1 or Z2 being able to represent a single bond; R1 and R2, identical or different, represent a hydrogen atom or a functional group capable of increasing hydrosolubility; Rx and Ry forming together a cyclic peroxide including 4 to 8 links and including 1 or 2 additional oxygen atoms in the cyclic structure, possibly substituted by one or more R3 groups; as a base or a salt to be added to an acid, as a hydrate or solvate, in racemic form, isomers and their mixtures, in addition to their diasteroisomers and their mixtures. Preparation method and use as medications with antimalarial activity.

摘要翻译： 本发明涉及对应于式（I）的双分子：其中：A表示具有式（IIa）或（IIIa）的抗疟活性的分子残基或促进生物利用度的残基; B表示可被取代的环烷基，或B表示可被取代的双环或三环基，或B表示通过单键或亚烷基链连接在一起的2个环烷基; m和n彼此独立地表示0,1或2; R5表示氢原子，烷基，环烷基或C1-3亚烷基 - 环烷基; Z 1和Z 2表示烷基，基团Z 1 + Z 2 + C 1 + C 1表示单环或多环结构，其中Z1或Z2之一能够表示单键; R1和R2相同或不同，表示氢原子或能够提高水溶性的官能团; Rx和Ry一起形成环状过氧化物，其包含4至8个连接并且在环状结构中包含1或2个另外的氧原子，可能被一个或多个R 3基团取代; 除了它们的非对映异构体及其混合物之外，还可以以外消旋体，异构体和它们的混合物作为水合物或溶剂合物加入到酸中的碱或盐。 制备方法和用作具有抗疟活性的药物。