Patent classifications
C07C229/06
CATIONIC SULFONAMIDE AMINO LIPIDS AND AMPHIPHILIC ZWITTERIONIC AMINO LIPIDS
The present disclosure provides one or more amino lipids such as an amino lipids containing a sulfonic acid or sulfonic acid derivative of the formulas:
##STR00001##
wherein the variables are as defined herein. These amino lipids may be used in compositions with one or more helper lipids and a nucleic acid therapeutic agent. These compositions may be used to treat a disease or disorder such as cancer, cystic fibrosis, or other genetic diseases.
CATIONIC SULFONAMIDE AMINO LIPIDS AND AMPHIPHILIC ZWITTERIONIC AMINO LIPIDS
The present disclosure provides one or more amino lipids such as an amino lipids containing a sulfonic acid or sulfonic acid derivative of the formulas:
##STR00001##
wherein the variables are as defined herein. These amino lipids may be used in compositions with one or more helper lipids and a nucleic acid therapeutic agent. These compositions may be used to treat a disease or disorder such as cancer, cystic fibrosis, or other genetic diseases.
Nucleic acid-containing lipid nanoparticles
The present invention provides nucleic acid-containing lipid nanoparticles containing a lipid (lipid A) which has a hydrophilic unit having a single quaternary ammonium group, and three independent, optionally substituted hydrocarbon groups, a lipid derivative or fatty acid derivative of a water-soluble polymer, and a nucleic acid.
Nucleic acid-containing lipid nanoparticles
The present invention provides nucleic acid-containing lipid nanoparticles containing a lipid (lipid A) which has a hydrophilic unit having a single quaternary ammonium group, and three independent, optionally substituted hydrocarbon groups, a lipid derivative or fatty acid derivative of a water-soluble polymer, and a nucleic acid.
CATIONIC LIPID
The present invention provides a technique capable of transferring an active ingredient, particularly, a nucleic acid, to a cell with excellent efficiency and a cationic lipid for use in this technique, etc. The cationic lipid of the present invention is a compound represented by the formula (I) or a salt thereof. n1 represents an integer of 2 to 6, n2 represents an integer of 0 to 2, n3 represents an integer of 0 to 2, L represents —C(O)O— or —NHC(O)O—, Ra represents a linear C.sub.5-13 alkyl group, a linear C.sub.13-17 alkenyl group or a linear C.sub.17 alkadienyl group, Rb represents a linear C.sub.2-9 alkyl group, Rc represents a hydrogen atom or a linear C.sub.2-9 alkyl group, Rd represents a hydrogen atom or a linear C.sub.2-9 alkyl group, Re represents a linear C.sub.2-9 alkyl group, and Rf represents a linear C.sub.2-9 alkyl group.
##STR00001##
QUATERNARY AMMONIUM SALTS OF NICOTINIC ACID AND NICOTINAMIDE MONONUCLOETIDES AND RIBOSIDES AS ANTI-AGING AGENTS
The present invention relates to amino acid salts of nicotinic acid and nicotinamide and compositions thereof of Formula I, useful in the treatment of disorders and diseases associated with deficiencies in NAD.sup.+:
##STR00001##
wherein A, L, M.sup.1, M.sup.2, R.sup.1, R.sup.2, and R.sup.3 are as described herein.
QUATERNARY AMMONIUM SALTS OF NICOTINIC ACID AND NICOTINAMIDE MONONUCLOETIDES AND RIBOSIDES AS ANTI-AGING AGENTS
The present invention relates to amino acid salts of nicotinic acid and nicotinamide and compositions thereof of Formula I, useful in the treatment of disorders and diseases associated with deficiencies in NAD.sup.+:
##STR00001##
wherein A, L, M.sup.1, M.sup.2, R.sup.1, R.sup.2, and R.sup.3 are as described herein.
ESTERS OF AMINO CARBOXYLIC ACIDS AND A PROCESS TO PREPARE THEM
A process to prepare an amine-functional ester of an amino carboxylic acid includes the step of reacting a polyol of the formula (I)
HO-A-OH (I)
where A is a carbon chain with about 2 to about 36 carbon atoms that is aliphatic linear or branched, saturated or unsaturated, or aromatic, or CH.sub.2CH(OH)CH.sub.2, CH.sub.2C(CH.sub.2OH).sub.2CH.sub.2, CH.sub.2C(CH.sub.2OH)(CH.sub.3)CH.sub.2, CH.sub.2C(CH.sub.2OH)(CH.sub.2CH.sub.3)CH.sub.2, p-tetrahydrofuran, erythritol or an ester of di- or tricarboxylic acids with ethylene or propylene glycol, and wherein A can optionally be alkoxylated or reacted with hydroxy carboxylic acids, with an aminocarboxylic acid of formula II or its cyclic amide of the formula III, where m is an integer of about 1 to about 8 in formula II and about 3 to about 8 in formula III, each R independently is hydrogen or a C1-C4 alkyl group, or CH.sub.2CH.sub.2COOH, or CH.sub.2COOH, or (CH.sub.2).sub.4NH.sub.2, in the presence of a Brønsted-Lowry acid.
COMPOSITIONS AND METHODS FOR THE MODULATION OF CYTOKINES
A method for modulating production of a cytokine, or molecule upregulated or down regulated by a cytokine, in a patient in need thereof, including administering to a patient a composition comprising at least one of a strontium-containing compound, a cysteine-based antioxidant, a polyhydroxyphenol and beta hydroxybutyric acid to the patient, whereby an amount of a cytokine in the patient is modulated.
COMPOSITIONS AND METHODS FOR THE MODULATION OF CYTOKINES
A method for modulating production of a cytokine, or molecule upregulated or down regulated by a cytokine, in a patient in need thereof, including administering to a patient a composition comprising at least one of a strontium-containing compound, a cysteine-based antioxidant, a polyhydroxyphenol and beta hydroxybutyric acid to the patient, whereby an amount of a cytokine in the patient is modulated.