C07C251/24

Manganese based complexes and uses thereof for homogeneous catalysis

The present invention relates to novel manganese complexes and their use, inter alia, for homogeneous catalysis in (1) the preparation of imine by dehydrogenative coupling of an alcohol and amine; (2) C—C coupling in Michael addition reaction using nitriles as Michael donors; (3) dehydrogenative coupling of alcohols to give esters and hydrogen gas (4) hydrogenation of esters to form alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones), or polyesters); (5) hydrogenation of amides (including cyclic dipeptides, lactams, diamide, polypeptides and polyamides) to alcohols and amines (or diamine); (6) hydrogenation of organic carbonates (including polycarbonates) to alcohols or hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (7) dehydrogenation of secondary alcohols to ketones; (8) amidation of esters (i.e., synthesis of amides from esters and amines); (9) acylation of alcohols using esters; (10) coupling of alcohols with water and a base to form carboxylic acids; and (11) preparation of amino acids or their salts by coupling of amino alcohols with water and a hydrogenative coupling of alcohols and amines; (13) preparation of imides from diols. ##STR00001## ##STR00002##

ANALOGUES OF PENTAMIDINE AND USES THEREFOR

The present disclosure provides a group of aromatic (e.g., pyridinyl, pyrimidinyl, pyrazinyl, or phenyl) diamidine analogs and pharmaceutically acceptable salts that are useful for treating a proliferative disease. The proliferative disease may include solid cancer or blood cancer. Compositions, methods of synthesizing the same and methods for treating various cancer using the analogs are disclosed herein. The present disclosure also provides pharmaceutical formulations comprising at least one of the compounds with a pharmaceutically acceptable carrier, diluent or excipient therefor.

ANALOGUES OF PENTAMIDINE AND USES THEREFOR

The present disclosure provides a group of aromatic (e.g., pyridinyl, pyrimidinyl, pyrazinyl, or phenyl) diamidine analogs and pharmaceutically acceptable salts that are useful for treating a proliferative disease. The proliferative disease may include solid cancer or blood cancer. Compositions, methods of synthesizing the same and methods for treating various cancer using the analogs are disclosed herein. The present disclosure also provides pharmaceutical formulations comprising at least one of the compounds with a pharmaceutically acceptable carrier, diluent or excipient therefor.

METHOD FOR PREPARING 18F-BPA AND INTERMEDIATE
20230242555 · 2023-08-03 ·

A method for preparing .sup.18F-BPA and an intermediate, by which high-purity .sup.18F-BPA is obtained. The method simplifies the synthesis steps after .sup.18F labeling, and is easy to operate and efficient.

CRF1 RECEPTOR ANTAGONIST, PHARMACEUTICAL FORMULATIONS AND SOLID FORMS THEREOF FOR THE TREATMENT OF CONGENITAL ADRENAL HYPERPLASIA

Provided are methods related to treating congenital adrenal hyperplasia in a subject in need thereof comprising administering 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-prop-2-ynyl-1,3-thiazol-2-amine (Formula 1), or a pharmaceutically acceptable salt thereof. Further provided are pharmaceutical formulations and solid forms of 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-prop-2-ynyl-1,3-thiazol-2-amine, or a pharmaceutically acceptable salt thereof, and their use in the treatment of congenital adrenal hyperplasia (CAH).

CRF1 RECEPTOR ANTAGONIST, PHARMACEUTICAL FORMULATIONS AND SOLID FORMS THEREOF FOR THE TREATMENT OF CONGENITAL ADRENAL HYPERPLASIA

Provided are methods related to treating congenital adrenal hyperplasia in a subject in need thereof comprising administering 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-prop-2-ynyl-1,3-thiazol-2-amine (Formula 1), or a pharmaceutically acceptable salt thereof. Further provided are pharmaceutical formulations and solid forms of 4-(2-chloro-4-methoxy-5-methylphenyl)-N-[(1S)-2-cyclopropyl-1-(3-fluoro-4-methylphenyl)ethyl]-5-methyl-N-prop-2-ynyl-1,3-thiazol-2-amine, or a pharmaceutically acceptable salt thereof, and their use in the treatment of congenital adrenal hyperplasia (CAH).

Process for preparing safinamide

The present invention is related to a process for preparing safinamide and salts thereof, preferably safinamide methanesulfonate, with high yields and high enantiomeric and chemical purity without the need of using highly pure intermediates. The process of the present invention is suitable for the production of safinamide and its salts, preferably safinamide methanesulfonate, at industrial scale.

Process for preparing safinamide

The present invention is related to a process for preparing safinamide and salts thereof, preferably safinamide methanesulfonate, with high yields and high enantiomeric and chemical purity without the need of using highly pure intermediates. The process of the present invention is suitable for the production of safinamide and its salts, preferably safinamide methanesulfonate, at industrial scale.

Process for preparing safinamide

The present invention is related to a process for preparing safinamide and salts thereof, preferably safinamide methanesulfonate, with high yields and high enantiomeric and chemical purity without the need of using highly pure intermediates. The process of the present invention is suitable for the production of safinamide and its salts, preferably safinamide methanesulfonate, at industrial scale.

RESIN COMPOSITION, COATED AND DRIED PRODUCT, MELT-KNEADED PRODUCT, OPTICAL FILTER, IMAGE DISPLAY DEVICE, SOLID-STATE IMAGING ELEMENT, SQUARYLIUM COMPOUND, AND METHOD FOR PRODUCING THE SAME

Provided are a resin composition containing a squarylium compound and a resin, in which the squarylium compound includes at least one selected from squarylium compounds represented by specific formulae; a coated and dried product or a melt-kneaded product; an optical filter including these components; an image display device and a solid-state imaging element including the optical filter; and a squarylium compound represented by a specific formula and a method for producing the same.