Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formula I-III: wherein, variables Q, R, X, X?, Y1, Y2, Y2?, Y3, Y4, Y5, m, and n are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I-III and at least one carrier, diluent or excipient.

Abstract: This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-Phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-III: wherein, variables Q, R, X, X?, Y1, Y2, Y2?, Y3, Y4, Y5, m, and n are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formulae I-III and at least one carrier, diluent or excipient.

Abstract: Disclosed herein is a method of producing an optically active thiophene-based compound using a simulated moving bed adsorption separation process, and more specifically, a method of continuously separating a racemic thiophene-based compound into its optically active thiophene-based compounds having high purity, through optical resolution using the simulated moving bed process. According to the method of the current invention, a racemic mixture of a thiophene-based compound can be continuously separated into its optically active thiophene-based compounds having high purity, which is an intermediate of optically active dorzolamide acting as a topical therapeutic agent for glaucoma, using a simulated moving bed adsorption separation technique, thereby increasing industrial usability.

Abstract: Disclosed herein is a method of producing an optically active thiophene-based compound using a simulated moving bed adsorption separation process, and more specifically, a method of continuously separating a racemic thiophene-based compound into its optically active thiophene-based compounds having high purity, through optical resolution using the simulated moving bed process. According to the method of the current invention, a racemic mixture of a thiophene-based compound can be continuously separated into its optically active thiophene-based compounds having high purity, which is an intermediate of optically active dorzolamide acting as a topical therapeutic agent for glaucoma, using a simulated moving bed adsorption separation technique, thereby increasing industrial usability.

Abstract: A method for preparing ketones has advantages of improving yields and reducing the time of the reactions due to high efficiency of catalysts. Ketones are prepared by reacting an aliphatic or an aromatic aldehyde with a vinyl olefin having an aliphatic or aromatic alkyl moiety in the presence of a transition metal catalyst, 2-aminopyridine catalyst, a primary amine and an acid, as catalysts and additives.

Abstract: An ortho-alkylation method of an aromatic ketone. In the method, as starting materials, the aromatic ketone is reacted with aliphatic or aromatic alkyl moiety-containing olefins in the presence of a primary amine and a transition metal catalyst as reaction catalysts, or ketimines resulting from a reaction of aromatic ketones with a primary amine are reacted with aliphatic or aromatic alkyl moiety-containing olefins in the presence of a transition metal catalyst, thereby introducing the alkyl moiety to the ortho-position of the aromatic ketone.