C07D207/333

PROTEOSTASIS REGULATORS
20200299270 · 2020-09-24 ·

The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.

PROTEOSTASIS REGULATORS
20200299270 · 2020-09-24 ·

The present invention is directed to compounds having the Formulae (Ia-Ie), (II), (IIIa-IIId), (IVa-IVc), (Va-Vb), (VIa-VIe), (VII), (VIIIa-VIIIc), and (IX), pharmaceutically acceptable salts, prodrugs and solvates thereof, compositions of any of thereof and methods for the treatment of a condition associated with a dysfunction in proteostasis comprising an effective amount of these compounds.

ADDUCTS FORMED FROM PRIMARY AMINES, DICARBONYL DERIVATIVES, INORGANIC OXIDE HYDROXYDES AND SP2-HYBRIDIZED CARBON ALLOTROPES

Adducts are described, obtainable from the reaction product of a secondary amine and a diketone, with carbon allotropes in which the carbon is sp.sup.2 hybridized, such as graphene, graphite, fullerene, carbon nanotubes and the like, and an inorganic oxide-hy-droxide. A process for preparing said adducts is also described.

ADDUCTS FORMED FROM PRIMARY AMINES, DICARBONYL DERIVATIVES, INORGANIC OXIDE HYDROXYDES AND SP2-HYBRIDIZED CARBON ALLOTROPES

Adducts are described, obtainable from the reaction product of a secondary amine and a diketone, with carbon allotropes in which the carbon is sp.sup.2 hybridized, such as graphene, graphite, fullerene, carbon nanotubes and the like, and an inorganic oxide-hy-droxide. A process for preparing said adducts is also described.

Necrosis Inhibitors

The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.

PYRROLE COMPOUND, AROMA COMPOSITION, AND FOOD AND DRINK AND COSMETICS CONTAINING THE SAME

A compound represented by the following formula (1):

##STR00001## wherein, R.sub.1 is a linear or branched alkyl group having 1 to 3 carbon atoms or a hydroxyl group; and R.sub.2 is a 1-pyrrolyl group, a 2-pyrrolyl group, or a 3-pyrrolyl group. The present invention can provide a means highly effective in contributing to savory roasting flavor and capable of imparting fragrance with natural feeling.

PYRROLE COMPOUND, AROMA COMPOSITION, AND FOOD AND DRINK AND COSMETICS CONTAINING THE SAME

A compound represented by the following formula (1):

##STR00001## wherein, R.sub.1 is a linear or branched alkyl group having 1 to 3 carbon atoms or a hydroxyl group; and R.sub.2 is a 1-pyrrolyl group, a 2-pyrrolyl group, or a 3-pyrrolyl group. The present invention can provide a means highly effective in contributing to savory roasting flavor and capable of imparting fragrance with natural feeling.

PROCESS FOR PRODUCING PYRROLE COMPOUND

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

##STR00001##

PROCESS FOR PRODUCING PYRROLE COMPOUND

The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

##STR00001##

Markovnikov-selective palladium catalyst for carbonylation of alkynes with heteroarenes

Markovnikov-selective palladium catalyst for carbonylation of alkynes is formed from a bisphosphite having formula (1): ##STR00001## The carbonylation catalyst is suited for the preparation of a branched heteroarene-keto product from an alkyne substrate, CO and heterocycle in high yields with low amounts of the linear product.