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US 2001/0056074 A1Published application
Novel lipophilic compounds having affinity with nucleic acids and therapeutical uses thereof
OwnerJean-Jacques Yaouanc, Erwann Guenin +5inventors
InventorsJean-Jacques Yaouanc, Erwann Guenin, Jean-Claude Clement, Anne-Cecile Herve, Claude Ferec, Virginie Floch, Herve des Abbayes
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Abstract
The invention consists of a compound of the general formula (I) below: 1 Wherein A, R1, R2, R3, R4 and X are as disclosed in the specification. The invention also relates to the therapeutical uses of this compound, particularly for gene therapy.
Claims31
A compound of the general formula (I) below:
- 11
- Wherein A is a phosphorus or an arsenic atom;
- X− is an anion;
- and
- wherein R1 is selected from the group consisting of:
- a) the radical of formula (II) below:
- 12
- wherein R5 represents a lipid moiety and R6 is a linear or branched alkyl chain from 1 to 4 carbon atoms,
- Provided that R2, R3 and R4 of formula (I) represent each a methyl group;
- b) the radical of formula (III) below:
- 13
- wherein R5 represents a lipid moiety and R6 is a linear or branched alkyl chain from 1 to 4 carbon atoms,
- provided that R2, R3 and R4 of formula (I) represent each a methyl group;
- c) the radical of formula (IV) below:
- 14
- wherein Chol means a cholesteryl radical and R6 is a linear or branched alkyl chain from 1 to 4 carbon atoms,
- provided that R2 and R3 of formula (I) represent each a methyl group;
- and
- d) the radical of formula (V) below:
- 15
- wherein R5 represents a lipid moiety and R6 is a linear or branched alkyl chain from 1 to 4 carbon atoms,
- provided that R2 and R4 are alkyl chains from 1 to 4 carbon atoms;
- and
- R3 is selected from the group consisting of:
- an alkyl chain as defined for R2 and R4,
- the functional group CH2—CH2—P+ (R6R7R8), wherein R6, R7 and R8 have the same meaning as R2 and R4;
- and
- —CH2—CO2R9, wherein R9 has the same meaning as R2.
25 more elements
Dependencies are inferred from the claim text.