C07F9/653

NON-AQUEOUS LIQUID ELECTROLYTE, ELECTRICITY STORAGE DEVICE USING SAME, AND PHOSPHORUS COMPOUND USED THEREIN

The present invention is concerned with a nonaqueous electrolytic solution having an electrolyte salt dissolved in a nonaqueous solvent, the nonaqueous electrolytic solution containing a compound represented by the following general formula (X), in which a polar group (X) is bound to a phosphorus atom (P), and capable of improving electrochemical characteristics in a broad temperature range; an energy storage device using the same; and a novel compound.

##STR00001##

In the formula, R.sup.10 and R.sup.20 are each independently an organic group selected from the group consisting of an alkyl group having 1 to 8 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, an alkynyl group having 3 to 6 carbon atoms, and an aryl group having 6 to 12 carbon atoms, or a lithium atom; and X is a polar group (i) containing a —C(═O) group, a —P(═O) group, or an —S(═O).sub.2 group, a polar group (ii) containing a —CN group or an alkyl group having 1 to 6 carbon atoms, in which a part of hydrogen atoms is substituted with a fluorine atom, or a 4- to 7-membered ring polar group (iii) containing a —C(═O)—O— group or a —C(═O)—N— group, provided that when X is a 4- to 7-membered ring polar group (iii) containing a —C(═O)—N— group, at least one of R.sup.10 and R.sup.20 is a lithium atom.

COMPOSITION AND METHODS OF USE OF SMALL MOLECULES AS BINDING LIGANDS FOR THE MODULATION OF PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9(PCSK9) PROTEIN ACTIVITY

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.

Therapeutic bisphosphonates

The invention provides novel pyrophosphate synthase inhibitors of formula I and formula II as well salts thereof; the invention also provides compositions comprising such inhibitors and methods for their use. ##STR00001##

Therapeutic bisphosphonates

The invention provides novel pyrophosphate synthase inhibitors of formula I and formula II as well salts thereof; the invention also provides compositions comprising such inhibitors and methods for their use. ##STR00001##

N-(PHOSPHINOALKYL)-N-(THIOALKYL)AMINE DERIVATIVE, METHOD FOR PRODUCING SAME, AND METAL COMPLEX THEREOF

The purpose of the present invention is to provide: a ligand that is useful in a catalytic organic synthetic reaction; a method for producing said ligand; and a metal complex that is useful as a catalyst in an organic synthetic reaction. The present invention provides a compound represented by general formula (1.sup.A), a method for producing said compound, and a metal complex including said compound as a ligand. (In the formula, H, N, P, S, L, R.sup.1, R.sup.2, R.sup.3, Q.sup.1, and Q.sup.2 have the meaning as defined in the Description.)

##STR00001##

Synthesis of Phosphoramidates

A process for the preparation of a compound of formula (I) including all isomers, stereoisomers, enantiomers and diastereomers thereof (I), and salts thereof; the process comprising providing a mixture comprising a compound of formula (II) and a compound of formula (III) subjecting the mixture provided in a) to reaction conditions in the presence of one or more Lewis acids to the mixture provided in a), obtaining a mixture comprising the compound of formula (I).

##STR00001##

A PROCESS FOR THE PREPARATION OF NUCLEOSIDE PHOSPHORAMIDATE

The present invention pertains to process for preparing nucleoside phosphoramidate and its intermediate. The present invention provides novel intermediate, its process for preparation and its use for the preparation of Sofosbuvir.

A PROCESS FOR THE PREPARATION OF NUCLEOSIDE PHOSPHORAMIDATE

The present invention pertains to process for preparing nucleoside phosphoramidate and its intermediate. The present invention provides novel intermediate, its process for preparation and its use for the preparation of Sofosbuvir.

Aminopeptidase A inhibitors and pharmaceutical compositions comprising the same

The present invention relates to a novel compound, to a composition comprising the same, to methods for preparing the compound, and the use of this compound in therapy. In particular, the present invention relates to a compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma.