C07C211/04

Low molecular weight cationic lipids for oligonucleotide delivery

The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.

GAS-PHASE PROCESS FOR THE CONVERSION OF GLYCOLALDEHYDE WITH AN AMINATING AGENT

A process for the conversion of glycolaldehyde with an aminating agent in the presence of hy-5 drogen and of a catalyst, wherein the conversion is carried out in the gas phase.

GAS-PHASE PROCESS FOR THE CONVERSION OF GLYCOLALDEHYDE WITH AN AMINATING AGENT

A process for the conversion of glycolaldehyde with an aminating agent in the presence of hy-5 drogen and of a catalyst, wherein the conversion is carried out in the gas phase.

METHODS OF USING EHMT2 INHIBITORS IN TREATING OR PREVENTING BLOOD DISORDERS

The present disclosure relates to a method of preventing or treating a blood disorder (e.g., sickle-cell disease) via administering an EHMT2 inhibitor compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.

PROCESS FOR THE PREPARATION OF 6-(CYCLOPROPANEAMIDO)-4-((2-METHOXY-3-(1-METHYL-1H-1,2,4-TRIAZOL-3-YL)PHENYL)AMINO)-N-(METHYL-D3)PYRIDAZINE-3-CARBOXAMIDE

The invention relates to an improved process for synthesizing 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide of the formula:

##STR00001##

Compound I is currently in clinical trials for the treatment of auto-immune and auto-inflammatory diseases such as psoriasis.

PROCESS FOR THE PREPARATION OF 6-(CYCLOPROPANEAMIDO)-4-((2-METHOXY-3-(1-METHYL-1H-1,2,4-TRIAZOL-3-YL)PHENYL)AMINO)-N-(METHYL-D3)PYRIDAZINE-3-CARBOXAMIDE

The invention relates to an improved process for synthesizing 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide of the formula:

##STR00001##

Compound I is currently in clinical trials for the treatment of auto-immune and auto-inflammatory diseases such as psoriasis.

Branched trialkyl amine oxides

The invention provides branched trialkylamine oxides with improved properties. The trialkylamine oxides of the invention produced from branched trialkylamines, in one embodiment, can be made using certain branched C10-12 enals and aldehydes. The invention also provides an trialkylamine oxide having the formula: ##STR00001##
wherein R5, R6 and R7 are independently at least one of C3H7, C2H5, CH3, or H, or mixtures thereof; and wherein R5 and R6 are not H at the same time. In one embodiment, the trialkylamine oxides of the invention can be useful in making various products, for example, as surfactants.

Branched trialkyl amine oxides

The invention provides branched trialkylamine oxides with improved properties. The trialkylamine oxides of the invention produced from branched trialkylamines, in one embodiment, can be made using certain branched C10-12 enals and aldehydes. The invention also provides an trialkylamine oxide having the formula: ##STR00001##
wherein R5, R6 and R7 are independently at least one of C3H7, C2H5, CH3, or H, or mixtures thereof; and wherein R5 and R6 are not H at the same time. In one embodiment, the trialkylamine oxides of the invention can be useful in making various products, for example, as surfactants.

Process for the preparation of 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide

The invention relates to an improved process for synthesizing 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide of the formula: [INSERT CHEMICAL STRUCTURE HERE] Compound I is currently in clinical trials for the treatment of auto-immune and auto-inflammatory diseases such as psoriasis. ##STR00001##

Process for the preparation of 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide

The invention relates to an improved process for synthesizing 6-(cyclopropaneamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide of the formula: [INSERT CHEMICAL STRUCTURE HERE] Compound I is currently in clinical trials for the treatment of auto-immune and auto-inflammatory diseases such as psoriasis. ##STR00001##