C07F9/653

3,3,3′,3′-tetramethyl-1,1′-spirobiindane-based phosphinooxazoline ligand compound, preparation method and uses of the same
11111258 · 2021-09-07 · ·

The invention discloses a tetramethyl-7,7′-spirobiindane-based phosphinooxazoline ligand compound and its preparation method and use. The phosphinooxazoline ligand compound is a compound having a structure shown in general formula I or an enantiomer, a raceme or a diastereoisomer thereof. The phosphinooxazoline ligand obtained through a series of reaction steps using cheap and easily available 3,3,3′,3′-tetramethyl-1,1′-spirobiindane-6,6′-diol as a starting material. The novel phosphinooxazoline ligand developed in the invention can be used to organic catalytic reactions, especially as a chiral phosphinooxazoline ligand widely used in metal-asymmetric catalytic reactions, having economical practicality and industrial application prospects. ##STR00001##

NOVEL OXAZOLIDINONE DERIVATIVES
20210121449 · 2021-04-29 ·

The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.

NOVEL OXAZOLIDINONE DERIVATIVES
20210121449 · 2021-04-29 ·

The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.

Method to treat lipid dysregulation by modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9) protein activity with small molecule ligands

This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.

Heterocyclic bridged biphenyls

The present invention relates electroluminescent devices, comprising a compound of the formula ##STR00001##
especially as host for phosphorescent compounds. The hosts may function with phosphorescent materials to provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices.

3,3,3',3'-TETRAMETHYL-1,1'-SPIROBIINDANE-BASED PHOSPHINOOXAZOLINE LIGAND COMPOUND, PREPARATION METHOD AND USES OF THE SAME
20210079030 · 2021-03-18 ·

The invention discloses a tetramethyl-7,7-spirobiindane-based phosphinooxazoline ligand compound and its preparation method and use. The phosphinooxazoline ligand compound is a compound having a structure shown in general formula I or an enantiomer, a raceme or a diastereoisomer thereof. The phosphinooxazoline ligand obtained through a series of reaction steps using cheap and easily available 3,3,3,3-tetramethyl-1,1-spirobiindane-6,6-diol as a starting material. The novel phosphinooxazoline ligand developed in the invention can be used to organic catalytic reactions, especially as a chiral phosphinooxazoline ligand widely used in metal-asymmetric catalytic reactions, having economical practicality and industrial application prospects.

##STR00001##

3,3,3',3'-TETRAMETHYL-1,1'-SPIROBIINDANE-BASED PHOSPHINOOXAZOLINE LIGAND COMPOUND, PREPARATION METHOD AND USES OF THE SAME
20210079030 · 2021-03-18 ·

The invention discloses a tetramethyl-7,7-spirobiindane-based phosphinooxazoline ligand compound and its preparation method and use. The phosphinooxazoline ligand compound is a compound having a structure shown in general formula I or an enantiomer, a raceme or a diastereoisomer thereof. The phosphinooxazoline ligand obtained through a series of reaction steps using cheap and easily available 3,3,3,3-tetramethyl-1,1-spirobiindane-6,6-diol as a starting material. The novel phosphinooxazoline ligand developed in the invention can be used to organic catalytic reactions, especially as a chiral phosphinooxazoline ligand widely used in metal-asymmetric catalytic reactions, having economical practicality and industrial application prospects.

##STR00001##

OXAZOLIDINONE-QUINOLONE HYBRID ANTIBACTERIAL FOR THE PARENTERAL TREATMENT OF PROPHYLAXIS OF BACTERIAL DISEASES
20200392168 · 2020-12-17 ·

The present invention relates to the use of oxazolidinone-quinolone hybrids for the parenteral (especially intravenous) treatment or prophylaxis of bacterial diseases. The present invention relates moreover to improved methods of administering oxazolidinone-quinolone hybrid antibacterials.

OXAZOLIDINONE-QUINOLONE HYBRID ANTIBACTERIAL FOR THE PARENTERAL TREATMENT OF PROPHYLAXIS OF BACTERIAL DISEASES
20200392168 · 2020-12-17 ·

The present invention relates to the use of oxazolidinone-quinolone hybrids for the parenteral (especially intravenous) treatment or prophylaxis of bacterial diseases. The present invention relates moreover to improved methods of administering oxazolidinone-quinolone hybrid antibacterials.

ADDITIVE FOR NON-AQUEOUS ELECTROLYTE SOLUTION, ELECTROLYTE SOLUTION FOR NON-AQUEOUS ELECTROLYTE SOLUTION BATTERY, AND NON-AQUEOUS ELECTROLYTE SOLUTION BATTERY

An additive for a non-aqueous electrolyte solution that can suppress the initial gas generation amount when used in a non-aqueous electrolyte solution battery. The additive for a non-aqueous electrolyte solution is represented by any one of formulae [1] to [4]:

##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2 and Y are as defined in the specification.