C07D213/50

Curcumin analogues as zinc chelators and their uses

This invention provides a compound having the structure ##STR00001##
wherein α, β, X, Y, and R.sub.1-R.sub.11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NFκ-B activation in a population of cells.

Curcumin analogues as zinc chelators and their uses

This invention provides a compound having the structure ##STR00001##
wherein α, β, X, Y, and R.sub.1-R.sub.11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NFκ-B activation in a population of cells.

ARYLMETHYLENE AROMATIC COMPOUNDS AS Kv1.3 POTASSIUM SHAKER CHANNEL BLOCKERS

A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.

##STR00001##

ARYLMETHYLENE AROMATIC COMPOUNDS AS Kv1.3 POTASSIUM SHAKER CHANNEL BLOCKERS

A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is described, wherein the substituents are as defined herein. Pharmaceutical compositions comprising the same and method of using the same are also described.

##STR00001##

Complexes

The present invention provides a palladium(II) complex of formula (1). ##STR00001## R.sub.12, m, and X are described in the specification. The invention also provides a process for the preparation of the complex, and its use in carbon-carbon and carbon-heteroatom coupling reactions.

Complexes

The present invention provides a palladium(II) complex of formula (1). ##STR00001## R.sub.12, m, and X are described in the specification. The invention also provides a process for the preparation of the complex, and its use in carbon-carbon and carbon-heteroatom coupling reactions.

Arylcyclohexylamine derivatives and process for preparing same
20230139975 · 2023-05-04 ·

The present invention relates to the technical field of pharmaceutical synthesis and development of drugs, and to a process for preparing cyclic 2-amino-1-one derivatives and to the reaction products and intermediates obtainable by this process. The present invention further relates to pharmaceutical compositions, in particular drugs or medicaments, comprising the cyclic 2-amino-1-one derivatives and to their use as medicaments, in particular in the prophylactic or therapeutic treatment of diseases of the human or animal body, preferably of neurodegenerative diseases or psychiatric disorders.

ARYL SULFONAMIDES

Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.

ARYL SULFONAMIDES

Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.

Slow release of organoboronic acids in cross-coupling reactions

A method of performing a chemical reaction includes reacting a compound selected from the group consisting of an organohalide and an organo-pseudohalide, and a protected organoboronic acid represented by formula (I) in a reaction mixture:
R.sup.1—B-T  (I);
where R.sup.1 represents an organic group, T represents a conformationally rigid protecting group, and B represents boron having sp.sup.3 hybridization. When unprotected, the corresponding organoboronic acid is unstable by the boronic acid neat stability test. The reaction mixture further includes a base having a pK.sub.B of at least 1 and a palladium catalyst. The method further includes forming a cross-coupled product in the reaction mixture.