C07C211/10

Biodegradable lipids for the delivery of active agents

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

Biodegradable lipids for the delivery of active agents

The present invention relates to a cationic lipid having one or more biodegradable groups located in a lipidic moiety (e.g., a hydrophobic chain) of the cationic lipid. These cationic lipids may be incorporated into a lipid particle for delivering an active agent, such as a nucleic acid. The invention also relates to lipid particles comprising a neutral lipid, a lipid capable of reducing aggregation, a cationic lipid of the present invention, and optionally, a sterol. The lipid particle may further include a therapeutic agent such as a nucleic acid.

Process for converting cyclic alkylene ureas into their corresponding alkylene amines

A process is provided for converting one or more cyclic ethylene ureas into corresponding ethylene amines and carbon dioxide. The process may include contacting water with one or more cyclic alkylene urea compounds comprising one or more cyclic alkylene urea moieties in a reaction vessel at a temperature of 150 to 400° C., optionally in the presence of an amine compound selected from the group of primary amines, cyclic secondary amines and bicyclic tertiary amines. The mole ratio of water to cyclic alkylene urea moieties is in the range of from about 0.1 to about 20. In the reaction, at least a portion of the cyclic alkylene urea moieties are converted to corresponding alkylenediamine moieties and carbon dioxide. The process may further include removing the carbon dioxide from the liquid reaction mixture in a stripping vessel by feeding a stripping fluid to the stripping vessel. Further, the process may include removing a carbon dioxide-containing stripping fluid.

CANNABIGEROL QUINONE ACID AND SALTS THEREOF

A compound of formula I

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or a pharmaceutical salt thereof of formula II,

##STR00002##

as well as a process to obtain said compound and a process to obtain said salt. Additionally, disclosed is the use of said compound of formula I or said pharmaceutical salt thereof of formula II as a medicament, in particular as a peroxisome proliferator-activated receptor gamma (PPARγ) agonist, for use in the treatment or prevention of a disease responsive to PPARγ agonists. Also disclosed is a pharmaceutical composition comprising said compound or said salt, as well as a method of treating or preventing a disease with said compound of formula I or said salt thereof of formula II, or with a composition comprising said compound or said salt.

COMPOUNDS AND COMPOSITIONS FOR TREATING HIV WITH DERIVATIVES OF BETULIN
20170252356 · 2017-09-07 ·

The present invention relates to compounds characterized by having a structure according to the following Formula I:

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or a pharmaceutically acceptable salt thereof. Compounds of the present invention are useful for the treatment or prevention of HIV.

PRODUCTS OBTAINED BY THE CONVERSION OF GLYCOLALDEHYDE DERIVATIVES AND AMINATING AGENTS AND THEIR CONVERSION TO ETHYLENEAMINES AND ETHANOLAMINES

A process for the manufacture of ethyleneamines and ethanolamines, comprising the steps of (i) converting a glycolaldehyde derivative of formula (II), in which R.sup.2, R.sup.3 are—the same or different—hydrogen, alkyl, such as C.sub.1-6-alkyl, or cycloalkyl such as Cs-e-cycloalkyl; and an animating agent of formula (III); in which R1 is hydrogen (H), alkyl, such as C.sub.1-6-alkyl, or cycloalkyl such as C.sub.3-6-cycloalkyl, in the gas or liquid phase; (ii) feeding the reaction products obtained in step (i) into a hydrogenation reactor, where the reaction products are converted with hydrogen in the presence of a hydrogenation catalyst.

##STR00001##

PRODUCTS OBTAINED BY THE CONVERSION OF GLYCOLALDEHYDE DERIVATIVES AND AMINATING AGENTS AND THEIR CONVERSION TO ETHYLENEAMINES AND ETHANOLAMINES

A process for the manufacture of ethyleneamines and ethanolamines, comprising the steps of (i) converting a glycolaldehyde derivative of formula (II), in which R.sup.2, R.sup.3 are—the same or different—hydrogen, alkyl, such as C.sub.1-6-alkyl, or cycloalkyl such as Cs-e-cycloalkyl; and an animating agent of formula (III); in which R1 is hydrogen (H), alkyl, such as C.sub.1-6-alkyl, or cycloalkyl such as C.sub.3-6-cycloalkyl, in the gas or liquid phase; (ii) feeding the reaction products obtained in step (i) into a hydrogenation reactor, where the reaction products are converted with hydrogen in the presence of a hydrogenation catalyst.

##STR00001##

Method for the production of ethyleneamines

The present invention relates to a process for preparing alkanolamines and/or ethyleneamines in the liquid phase, by reacting ethylene glycol and/or monoethanolamine with ammonia in the presence of an amination catalyst comprising Co, Ru and Sn.

Method for the production of ethyleneamines

The present invention relates to a process for preparing alkanolamines and/or ethyleneamines in the liquid phase, by reacting ethylene glycol and/or monoethanolamine with ammonia in the presence of an amination catalyst comprising Co, Ru and Sn.

Methods for extraction, processing, and purification of a selected family of target compounds from cannabis

Disclosed are methods for separating, recovering, and purifying tetrahydrocannabinolic acid (THCA) salts from an organic solvent solution comprising a mixture of cannabinoids. The methods comprise solubilizing the mixture of cannabinoids in a selected C5-C7 hydrocarbon solvent, adding thereto a selected amine to thereby precipitate a THCA-amine salt therefrom, dissolving the recovered THCA-amine salt in a selected solvent and then adding thereto a selected antisolvent to thereby recrystallize a purified THCA-amine salt therefrom. The recrystallized THCA-amine salt may be decarboxylated to form a mixture of Δ9-tetrahydrocannabinol (Δ9-THC) and amine. The Δ9-THC amine mixture may be acidified to separate the amine from Δ9-THC. The recovered Δ9-THC may be concentrated to produce a highly purified Δ9-THC. Also disclosed are THCA-amine salts produced with amines selected from groups of diamines, amino alcohols, and tertiary amines.