Lipophilic compounds and uses thereof

Organic compounds -- part of the class 532-570 series – Organic compounds – Phosphorus acids or salts thereof

Reexamination Certificate

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C546S022000

Reexamination Certificate

active

07667070

ABSTRACT:
The present invention has for an object a cationic lipophilic compound of the following general formula (I):wherein:a) R1and R′1each represent, independently from one another, an alkyl chain, an alkenyl chain or a polyalkenyl chain with from 10 to 24 carbon atoms, with the polyalkenyl chain having from 2 to 4 double links;b) R2is a hydrogen atom or an alkyl chain having from 1 to 4 carbon atoms; andR3is a group with the following formula (IIa) —(CH2)n— or following formula (IIb) —C(═NH)—NH—(CH2)n— wherein:n is an integer equal to 0, 1, 2, 3 or 4; andd) A+is an organic cation;e) X−is an anion.

REFERENCES:
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Lanham, 1953, CAS: 47: 41353.
Yasuda et al., 1995, CAS:124:18304.
Floch et al., “Cation substitution in cationic phosphonolipids: a new concept to improve transfection activity and decrease cellular toxicity,”J Medicinal Chemistry, 43:4617-4628, 2000.
Floch et al., “Phosphonolipids as non-viral vectors for gene therapy,”European Journal of Medicinal Chemistry, 33:923-934, 1998.
Guenin et al., “Cationic phosphonolipids containing quaternary phosphonium and arsonium groups for dna trasfection with good efficiency and low cellular toxicity,”Angewandte Chemie International Edition, 39:629-631, 2000.
Miller, “Cationic Liposomes for gene therapy,”Angewandte Chemie International Edition, 37:1768-1785, 1998.
Yasuda, “Phosphoric acid ester derivative for silber halide photographic material and it treating agent,”Chemical Abstracts, 124, 1996.

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