Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing
Patent
1996-07-22
2000-02-01
Kumar, Shailendra
Organic compounds -- part of the class 532-570 series
Organic compounds
Amino nitrogen containing
562561, 562563, 564159, 564197, C07C23305
Patent
active
060205261
ABSTRACT:
The present invention provides novel amide-based cationic lipids of the general structure: ##STR1## or a salt, or solvate, or enantiomers thereof wherein; (a) Y is a direct link or an alkylene of 1 to about 20 carbon atoms; (b) R.sub.1 is H or a lipophilic moiety; (c) R.sub.2, R.sub.3, and R.sub.4 are positively charged moieties, or at least one but not all of R.sub.2, R.sub.3, or R.sub.4 is a positive moiety and the remaining are independently selected from H, an alkyl moiety of 1 to about 6 carbon atoms, or a heterocyclic moiety of about 5 to about 10 carbon atoms; (d) n and p are independently selected integers from 0 to 8, such that the sum of n and o is from 1 to 16; (e) X.sup.- is an anion or polyanion and (f) m is an integer from 0 to a number equivalent to the positive charge(s) present on the lipid; provided that if Y is a direct link and the sum of n and p is 1 then one of either R.sub.3 or R.sub.4 must have an alkyl moiety of at least 10 carbon atoms.
The present invention further provides compositions of these lipids with polyanionic macromolecules, methods for interfering with protein expression in a cell utilizing these compositions and a kit for preparing the same.
REFERENCES:
patent: 4897355 (1990-01-01), Eppstein et al.
patent: 5171678 (1992-12-01), Beher et al.
patent: 5264618 (1993-11-01), Felgner et al.
patent: 5334761 (1994-08-01), Gebeyehu et al.
Felgner et al., "Lipofection: A highly efficient, lipid-mediated DNA-transfection procedure," Proc. Natl. Acad. Sci. USA 84:7413-7414 (1987).
Remy et.al., Bioconjugate chem, vol. 5, pp. 647-654, 1994.
Brown Bob Dale
Daily William J.
Dwyer Brian Patrick
Schwartz David Aaron
Srinivasan Kumar
Genta Incorporated
Kumar Shailendra
LandOfFree
Amide-based cationic lipids does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Amide-based cationic lipids, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Amide-based cationic lipids will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-938963