公开(公告)号：EP1846378B1

公开(公告)日：2011-04-06

申请号：EP06711426.4

申请日：2006-02-13

申请人： Politecnico Di Milano

发明人： ZANDA, Matteo ,  BRUCHE, Luca ,  FRIGERIO, Massimo ,  VIANI, Fiorenza ,  CHIAMENTI, Luca ,  PANZERI, Walter ,  ZAFFARONI, Nadia ,  FOLINI, Marco ,  GRECO, Maria Angela

IPC分类号： C07D251/54 ,  A61K31/53 ,  C12N15/00

CPC分类号： C07D251/44 ,  A61K48/0025 ,  C07D251/28 ,  C07D251/50 ,  C07D251/54 ,  Y10S977/773 ,  Y10S977/788 ,  Y10S977/792 ,  Y10S977/906 ,  Y10S977/915

摘要： The present invention relates to cationic lipids capable of forming complexes with nucleic acids and the use thereof for the transfection of eukaryotic cells. The cationic lipids according to the invention have general formulas (I) and (Ia): (see formulas (I) and (Ia), wherein E is a heteroaryl; Rl and R2 are selected from H, -R7-NH2, -CH-NH-NH2, alkyl; R7 is selected from alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl- (C0-C20) alkyl; R3 and R4 are selected from: H, -R8-SH, -R8-NH-NH2/ -R8-CO-R9 or - R8-NH2; R8 is selected from: alkyl, alkenyl, aryl, (C1- C20) alkyl-aryl- (C0 -C20 ) alkyl; R9 is selected from: H, alkyl; R5 and R6 are selected from: H, alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl.

公开(公告)号：EP1846378A2

公开(公告)日：2007-10-24

申请号：EP06711426.4

申请日：2006-02-13

申请人： Politecnico Di Milano

发明人： ZANDA, Matteo ,  BRUCHE, Luca ,  FRIGERIO, Massimo ,  VIANI, Fiorenza ,  CHIAMENTI, Luca ,  PANZERI, Walter ,  ZAFFARONI, Nadia ,  FOLINI, Marco ,  GRECO, Maria Angela

IPC分类号： C07D251/54 ,  A61K31/53 ,  C12N15/00

CPC分类号： C07D251/44 ,  A61K48/0025 ,  C07D251/28 ,  C07D251/50 ,  C07D251/54 ,  Y10S977/773 ,  Y10S977/788 ,  Y10S977/792 ,  Y10S977/906 ,  Y10S977/915

摘要： The present invention relates to cationic lipids capable of forming complexes with nucleic acids and the use thereof for the transfection of eukaryotic cells. The cationic lipids according to the invention have general formulas (I) and (Ia): (see formulas (I) and (Ia), wherein E is a heteroaryl; Rl and R2 are selected from H, -R7-NH2, -CH-NH-NH2, alkyl; R7 is selected from alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl- (C0-C20) alkyl; R3 and R4 are selected from: H, -R8-SH, -R8-NH-NH2/ -R8-CO-R9 or - R8-NH2; R8 is selected from: alkyl, alkenyl, aryl, (C1- C20) alkyl-aryl- (C0 -C20 ) alkyl; R9 is selected from: H, alkyl; R5 and R6 are selected from: H, alkyl, alkenyl, aryl, (C1-C20) alkyl-aryl.