Patent classifications
C07C59/90
Process for the preparation of ethacrynic acid
The invention provides an improved process for preparing Ethacrynic acid of formula I, including the steps of: (a) reacting 4-butyryl-2,3-dichloro-phenoxy acetic acid of formula II with dimethylamine or its salt to obtain [2,3-dichloro-4-(2-dimethylaminomethylbutyryl)phenoxy] acetic acid of formula III or its salt; (b) hydrolyzing [2,3-dichloro-4-(2-dimethylaminomethylbutyryl)phenoxy] acetic acid hydrochloride of formula III obtained in step a) with t-butyl amine to obtain t-butyl amine salt of Ethacrynic acid; (c) acidifying the t-butyl amine salt of Ethacrynic acid formed in step b) to obtain Ethacrynic acid of formula I; and (d) optionally purifying the obtained Ethacrynic acid with a solvent mixture of alkyl acetate and hydrocarbon solvent. The invention also provides crystalline t-butylamine salt of Ethacrynic acid and process thereof. Also provide compound Ethacrynic acid having a purity of greater than or equal to 99% and a composition including the compound.
Co-crystals of NURR1-lbd in complex with a cyclopentenone prostaglandin and modulators of NURR1
Co-crystals comprising the Nuclear receptor related 1 protein-ligand binding domain (Nurr1-LBD) and a cyclopentenone prostaglandin are provided. Also provided are methods of identifying or designing Nurr1-modulating ligands and compounds based on the crystal structures described herein as well as the applications of said ligands and compounds as Nurr1 modulators or medicaments.
Co-crystals of NURR1-lbd in complex with a cyclopentenone prostaglandin and modulators of NURR1
Co-crystals comprising the Nuclear receptor related 1 protein-ligand binding domain (Nurr1-LBD) and a cyclopentenone prostaglandin are provided. Also provided are methods of identifying or designing Nurr1-modulating ligands and compounds based on the crystal structures described herein as well as the applications of said ligands and compounds as Nurr1 modulators or medicaments.
NEW VANILLIN AND OR ETHYLVANILLIN, PROCESS FOR THEIR PREPARATIONS AND USE THEREOF
The present invention relates to a new bio-sourced vanillin and/or ethylvanillin, containing specific impurities. The invention further relates to a process for their preparations and the use of such compounds.
NEW VANILLIN AND OR ETHYLVANILLIN, PROCESS FOR THEIR PREPARATIONS AND USE THEREOF
The present invention relates to a new bio-sourced vanillin and/or ethylvanillin, containing specific impurities. The invention further relates to a process for their preparations and the use of such compounds.
3′-alkynyl abscisic acid derivatives as ABA antagonists
The present application relates to novel 3-unsaturated abscisic acid (ABA) derivatives of Formula (I) as ABA antagonists. For example, the present application relates to methods of using compounds of Formula (I) for reducing adverse effects of an ABA response in plants such as lentil and promoting germination. (I) The present application also relates to methods of using 3-phenyl abscisic acid (ABA) derivatives of Formula (II) as ABA antagonists, for example, for reducing adverse effects of an ABA response in plants such as lentil and promoting germination. (II) ##STR00001##
3′-alkynyl abscisic acid derivatives as ABA antagonists
The present application relates to novel 3-unsaturated abscisic acid (ABA) derivatives of Formula (I) as ABA antagonists. For example, the present application relates to methods of using compounds of Formula (I) for reducing adverse effects of an ABA response in plants such as lentil and promoting germination. (I) The present application also relates to methods of using 3-phenyl abscisic acid (ABA) derivatives of Formula (II) as ABA antagonists, for example, for reducing adverse effects of an ABA response in plants such as lentil and promoting germination. (II) ##STR00001##
15-oxospiramilactone derivatives, preparation method and uses thereof
The invention relates to a derivative of 15-oxospiramilacton, particularly to a compound of Formula I or II, or an isomer, a solvate or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the compound as pharmaceutically active ingredient, a method for preparing the same, and use thereof in manufacture of an anti-tumor agent. The derivative of 15-oxospiramilactone of the invention have an activity against multiple tumor cell lines, and the anti-tumor activity is positively correlated to an activity inhibiting the Wnt signaling pathway. ##STR00001##
PROCESSES FOR PREPARING ACC INHIBITORS AND SOLID FORMS THEREOF
The present disclosure provides solid forms, including a salt or co-crystal, of Compound I:
##STR00001##
which exhibits Acetyl-CoA carboxylase (ACC) inhibitory activity and may be useful in treating ACC mediated diseases. Also provided herein are processes or steps for the preparation of a Compound I and intermediates useful for the processes or steps described herein.
PROCESSES FOR PREPARING ACC INHIBITORS AND SOLID FORMS THEREOF
The present disclosure provides solid forms, including a salt or co-crystal, of Compound I:
##STR00001##
which exhibits Acetyl-CoA carboxylase (ACC) inhibitory activity and may be useful in treating ACC mediated diseases. Also provided herein are processes or steps for the preparation of a Compound I and intermediates useful for the processes or steps described herein.