C07D233/22

ALPHA1A-ADRENERGIC RECEPTOR AGONISTS AND METHODS OF USE
20230312524 · 2023-10-05 ·

The present disclosure relates generally to chemical compounds and, in some embodiments, to α1A-adrenergic receptor agonists and uses of such agonists in the treatment of diseases associated with an adrenergic receptor. Disclosed herein is a compound according to Formula (I) or an optically pure stereoisomer, pharmaceutically acceptable salt, solvate, or prodrug thereof.

ALPHA1A-ADRENERGIC RECEPTOR AGONISTS AND METHODS OF USE
20230312524 · 2023-10-05 ·

The present disclosure relates generally to chemical compounds and, in some embodiments, to α1A-adrenergic receptor agonists and uses of such agonists in the treatment of diseases associated with an adrenergic receptor. Disclosed herein is a compound according to Formula (I) or an optically pure stereoisomer, pharmaceutically acceptable salt, solvate, or prodrug thereof.

REVERSIBLE STREPTAVIDIN BASED ANALYTE ENRICHMENT SYSTEM FOR USE IN CROSSLINKING MASS SPECTROMETRY ANALYSIS

It is provided a reversible streptavidin based analyte enrichment system for use in crosslinking mass spectrometry analysis, in particular for enriching at least parts of crosslinked peptides pairs in mass spectrometry analysis, and a method of enriching at least parts of crosslinked peptides pairs, in particular for use in crosslinking mass spectroscopy analysis.

REVERSIBLE STREPTAVIDIN BASED ANALYTE ENRICHMENT SYSTEM FOR USE IN CROSSLINKING MASS SPECTROMETRY ANALYSIS

It is provided a reversible streptavidin based analyte enrichment system for use in crosslinking mass spectrometry analysis, in particular for enriching at least parts of crosslinked peptides pairs in mass spectrometry analysis, and a method of enriching at least parts of crosslinked peptides pairs, in particular for use in crosslinking mass spectroscopy analysis.

Process for the synthesis of lofexidine

Disclosed is a process for the synthesis of lofexidine of formula (I) and the hydrochloride salt thereof (II), from ethyl 2-(2,6-dichlorophenoxy)propionate (III) and ethylenediamine in the presence of tetravalent titanium alkoxides, preferably titanium isopropoxide, in an apolar solvent such as toluene. A further object of the present invention is a process for the preparation of the intermediate ethyl 2-(2,6-dichlorophenoxy)propionate (III) from 2,6-dichlorophenol and ethyl 2-chloropropionate in the presence of a polar aprotic solvent and an alkali or alkaline earth carbonate salt, preferably potassium carbonate. Both processes are more cost-effective and more easily industrially scalable than the known procedures, thus enabling the active ingredient to be obtained with high yields at a limited cost.

Process for the synthesis of lofexidine

Disclosed is a process for the synthesis of lofexidine of formula (I) and the hydrochloride salt thereof (II), from ethyl 2-(2,6-dichlorophenoxy)propionate (III) and ethylenediamine in the presence of tetravalent titanium alkoxides, preferably titanium isopropoxide, in an apolar solvent such as toluene. A further object of the present invention is a process for the preparation of the intermediate ethyl 2-(2,6-dichlorophenoxy)propionate (III) from 2,6-dichlorophenol and ethyl 2-chloropropionate in the presence of a polar aprotic solvent and an alkali or alkaline earth carbonate salt, preferably potassium carbonate. Both processes are more cost-effective and more easily industrially scalable than the known procedures, thus enabling the active ingredient to be obtained with high yields at a limited cost.

2- or 3-imidazolines as carbapenemases inhibitors

The present application relates to novel 3-imidazolines of formula (I′) and (I) below: (I′) (I) Wherein Ar.sub.1, Ar.sub.2, Ar.sub.3, and R.sub.1 to R.sub.6 are as defined in the claims. The 3-imidazolines of the invention are useful in antibiotic therapies, in particular as inhibitors of carbapenemases. They are also useful as antibiotics themselves. The present invention also concerns a method for preparing more specifically the 3-imidazolines of formula (I). The present invention further relates to conjugates of said compounds with known antibiotics. ##STR00001##

2- or 3-imidazolines as carbapenemases inhibitors

The present application relates to novel 3-imidazolines of formula (I′) and (I) below: (I′) (I) Wherein Ar.sub.1, Ar.sub.2, Ar.sub.3, and R.sub.1 to R.sub.6 are as defined in the claims. The 3-imidazolines of the invention are useful in antibiotic therapies, in particular as inhibitors of carbapenemases. They are also useful as antibiotics themselves. The present invention also concerns a method for preparing more specifically the 3-imidazolines of formula (I). The present invention further relates to conjugates of said compounds with known antibiotics. ##STR00001##

Acidic gas absorbent, acidic gas removal method and acidic gas removal apparatus

The embodiments provide an acidic gas absorbent, an acidic gas removal method using the absorbent, and an acidic gas removal apparatus using the absorbent. The absorbent absorbs an acidic gas in a large amount and is hardly diffused. The acidic gas absorbent according to the embodiment comprises an amine compound represented by the following formula (1): ##STR00001##

VASCULAR ADHESION PROTEIN-1 (VAP-1) MODULATORS AND THERAPEUTIC USES THEREOF

Disclosed herein are small molecule Vascular Adhesion Protein-1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.