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US 6,281,371 B1Granted
Lipopolyamines, and the preparation and use thereof
AssigneeBiontex Laboratories GmbH
InventorsRoland Klösel, Stephan König
Life of this patent
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Abstract
The present invention relates to new lipopolyamines (including salts thereof) characterised by a symmetrical, highly flexible lipophilic moiety having buffering capacity at physiological pH, and to the use thereof for the in vivo or in vitro introduction of biologically active materials, such as, for example, DNA, RNA, ribozymes, antisense DNA, PNA, peptides and proteins, into eukaryotic cells.
Claims14
A compound corresponding to the following formula (I):
- which, when a center of asymmetry is present, may occur in the D-, L- or DL-form,
- which includes salts thereof,
- wherein “R1” is a lipophilic radical of the following general formula:
- in which “R2” and “R3” are, independently, selected from the group consisting of dodecyl, dodecenyl, tetradecyl, tetradecenyl, hexadecyl, hexadecenyl, octadecyl, octadecenyl, and other alkyl radicals, and may be either saturated or unsaturated, branched or unbranched, fluorinated or non-fluorinated, and are constructed from 5 to 30 carbon atoms,
- wherein “X” is selected from one of the following formulae
- wherein, “m” is a number from 0 to 2, “n” is a number from 0 to 2, “g” is a number from 1 to 8, “a” is number from 0 to 6, “b” is a number from 0 to 6, “c” is a number from 0 to 6, “d”is a number from 0 to 6, “e” is a number from 0 to 6, “f” is a number from 0 to 6, “h” is a number from 0 to 6, “r” is a number from 0 to 6, “k” is a number from 0 to 6, and “1” is a number from 0 to 6,
- with the proviso that “b” is less than or equal to 1 whenever “a” equals 0, and “f” is less than or equal to 1 whenever “e” equals 0.
4 more elements
Dependencies are inferred from the claim text.