C07C327/22

PROCESS FOR THE PREPARATION OF A POLYUNSATURATED KETONE COMPOUND
20180009745 · 2018-01-11 ·

A process for the preparation of a polyunsaturated thiol comprising: (1) reacting a polyunsaturated alcohol in the presence of a compound of formula R.sub.2—SO.sub.2Hal wherein R.sub.2 is a C.sub.1-20 hydrocarbyl group, such an C.sub.1-10 alkyl group, to form a polyunsaturated sulphonyl ester; (2) converting the polyunsaturated sulphonyl ester to a polyunsaturated thioester by reacting with an anion of formula .sup.−SC(═O)R.sub.4 wherein R.sub.4 is a C.sub.1-20 hydrocarbyl group; (3) converting the polyunsaturated thioester to form a polyunsaturated thiol optionally in the presence of an antioxidant, e.g. using a metal carbonate. (4) reacting said polyunsaturated thiol with a compound (LG)R.sup.3COX wherein X is an electron withdrawing group and R.sup.3 is an alkylene group carrying a leaving group (LG), such as LG-CH.sub.2— forming

##STR00001## where X is an electron withdrawing group and LG is a leaving group; optionally in the presence of an antioxidant, so as to form a polyunsaturated ketone compound.

PROCESS FOR THE PREPARATION OF A POLYUNSATURATED KETONE COMPOUND
20180009745 · 2018-01-11 ·

A process for the preparation of a polyunsaturated thiol comprising: (1) reacting a polyunsaturated alcohol in the presence of a compound of formula R.sub.2—SO.sub.2Hal wherein R.sub.2 is a C.sub.1-20 hydrocarbyl group, such an C.sub.1-10 alkyl group, to form a polyunsaturated sulphonyl ester; (2) converting the polyunsaturated sulphonyl ester to a polyunsaturated thioester by reacting with an anion of formula .sup.−SC(═O)R.sub.4 wherein R.sub.4 is a C.sub.1-20 hydrocarbyl group; (3) converting the polyunsaturated thioester to form a polyunsaturated thiol optionally in the presence of an antioxidant, e.g. using a metal carbonate. (4) reacting said polyunsaturated thiol with a compound (LG)R.sup.3COX wherein X is an electron withdrawing group and R.sup.3 is an alkylene group carrying a leaving group (LG), such as LG-CH.sub.2— forming

##STR00001## where X is an electron withdrawing group and LG is a leaving group; optionally in the presence of an antioxidant, so as to form a polyunsaturated ketone compound.

Quaternary ammonium salt compound, preparation method therefor and use thereof

A compound is shown in formula I and can be in the form of a pharmaceutically acceptable salt, or a stereoisomer, or a solvate, or a prodrug, or a metabolite. The compound takes effect rapidly and has a long-time local anesthetic effect following a single dose, with the sensory nerve blocking time being greater than the motor nerve blocking time, has both a long-acting local anesthetic effect and a selective local anesthetic effect, significantly reduces side effects of the compositions QX314 and QX314 and a quaternary ammonium salt compound with surfactant structural characteristics, and is safer. The compound of formula I of the present invention and a pharmaceutically acceptable salt thereof can be used for preparing drugs that have a long-time local anesthetic effect and a selective local anesthetic effect.

METHODS AND MATERIALS FOR MODULATING NRF2 PATHWAY

The present application provides methods and compounds of modulating Nrf2 pathway. Methods for treating cancer and neurodegenerative conditions are also provided.

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.

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.

COMPOUNDS FOR OPTICALLY ACTIVE DEVICES
20230084690 · 2023-03-16 · ·

The present invention relates to novel ophthalmic devices comprising polymerized compounds comprising a photoactive unit, said polymerized compounds, and special monomer compounds being particularly suitable for compositions and ophthalmic devices.

COMPOUNDS FOR OPTICALLY ACTIVE DEVICES
20230084690 · 2023-03-16 · ·

The present invention relates to novel ophthalmic devices comprising polymerized compounds comprising a photoactive unit, said polymerized compounds, and special monomer compounds being particularly suitable for compositions and ophthalmic devices.