[EN] BI- OR TETRA-GUANIDINO-BIPHENYL COMPOUNDS AS SMALL MOLECULE CARRIERS<br/>[FR] COMPOSES BI-GUANIDINO-BIPHENYLE OU TETRA-GUANIDINO-BIPHENYLE SERVANT DE PETITES MOLECULES PORTEUSES
申请人:UNIV LONDON
公开号:WO2005123676A1
公开(公告)日:2005-12-29
The invention relates to compounds of formula: I, or pharmaceutically acceptable a salts thereof, I wherein X1 X2 and X3 are each independently where Y is an alkylene, alkenylene or alkynylene group, each of which may be optionally substituted with one or more substituents selected from alkyl, halo, CF3, OH, alkoxy, NH2, CN, NO2 and COOH; W is absent or is O, S or NH; Rl, R2, R3 and R4 are each independently selected from H, alkyl, aryl and a protecting group Pl; R7, R8 and R9 are each independently selected from H, alkyl, halo, CF3, OH, alkoxy, NH2, CN, NO2 and COOH; q and r are each independently 1, 2, 3 or 4; q' and r' are each independently 0, 1, 2 or 3, where q + q' and r + r' each equal 4; p is 1, 2, 3, 4 or 5, and p' is 0, 1, 2, 3 or 4, where p + p' is 5; n is 0, 1, 2, 3....6; L is (Z)mNR5R6 where Z is a hydrocarbyl group and m is 0 or 1; where R5 and R6 are each independently H, CO(CH2)jQ1 or C=S(NH)(CH2)kQ2 where j and k are each independently 0, 1, 2, 3, 4 or 5, and Q1 and Q2 are each independently selected from COOH, a chromophore or R5, R6 and the nitrogen to which they are attached together form.
该发明涉及以下结构的化合物:I,或其药学上可接受的盐,其中X1、X2和X3各自独立,其中Y是一个烷基,烯烃或炔烃基团,每个基团可能选择性地被一个或多个从烷基、卤素、CF3、羟基、烷氧基、NH2、CN、NO2和COOH中选择的取代基所取代;W不存在或是O、S或NH;R1、R2、R3和R4各自独立地选择自H、烷基、芳基和一个保护基Pl;R7、R8和R9各自独立地选择自H、烷基、卤素、CF3、羟基、烷氧基、NH2、CN、NO2和COOH;q和r各自独立地为1、2、3或4;q'和r'各自独立地为0、1、2或3,其中q + q'和r + r'分别等于4;p为1、2、3、4或5,p'为0、1、2、3或4,其中p + p'为5;n为0、1、2、3....6;L为(Z)mNR5R6,其中Z为一个烃基团,m为0或1;其中R5和R6各自独立地为H、CO(CH2)jQ1或C=S(NH)(CH2)kQ2,其中j和k各自独立地为0、1、2、3、4或5,Q1和Q2各自独立地选择自COOH、一个色团或R5、R6和它们所连接的氮共同形成。