Lipidoids for nucleic acid transfection and use thereof

Compounds of general formula I

• wherein X is selected from a group consisting of —C(═O)NH—, —C(═O)O—, —C(═S)O—, —C(═O)S—, —C(═S)S—, —C(═O)NHNH—, —CH2—, —O—, —OC(═O)—, —S—, —SC(═O)—, —NH—, —NHNH—, —NHC(═O)—, —NHNHC(═O)—, —C≡C—, —CH═CH—, a five-membered heterocycle containing at least 2 nitrogen atoms, —CH2C(═O)NH—, —CH2C(═O)O—, —CH2C(═S)O—, —CH2C(═S)S—, —CH2C(═O)NHNH—, —N═CH—, and —CH═N—;
• Y is independently selected from the group consisting of C2-C10 alkylene chains wherein in the alkylene chain, one or more —CH2— groups may optionally be replaced with one or more 0 or S atoms;
• Z is selected from the group consisting of hydrogen, —OH, —CH2OH, —NH2, —N+(CH3)2—(CH2)3—SO3−, —N+(CH3)2—(CH2)2—COO—, and —NHCH3, —N(CH3)2, —N+(CH3)3, —OCH3, —OCH2CH3, —C(═O)R1,
• wherein R1 is selected from —NH2, —NH(CH2)nOH, —N[(CH2)nOH]2, —NHCH(CH2OH)2, —NHCH2CH(—OH)CH2OH, —NH(CH2) C(═O)NH2, —N[CH2C(═O)NH2]2, —NHCH[C(═O)NH2]2, —NH(CH2)2NHC(═O)NH2,
• wherein n is an integer within the range from 2 to 5;
• and R are the same or different from each other, each R being independently selected from the group consisting of C8-C20 alkyl, C8-C20 alkenyl, and C8-C20 alkynyl, wherein in the alkyl, alkenyl or alkynyl, one or more —CH2— groups may optionally be replaced with one or more groups selected from —CH(OH)—, —OC(═O)—, —C(═O)O—, —S—S—, —C(═O)NH—, —NHC(═O)—, —O—, and —S—;
• and pharmaceutically acceptable salts, addition salts and solvates thereof.