1251845-63-2

Upstream product

• 1292369-99-3 methyl 2-benzyl-4-oxopiperidine-1-carboxylate 
• 1569102-03-9 methyl 2-benzyl-4-oxo-3,4-dihydropyridine-1(2H)-carboxylate 
• 620-08-6 4-methoxypyridine 
• 1251842-95-1 2-benzyl-1-(methoxycarbonyl)piperidine-4-carboxylic acid 

Downstream Products

• 1251841-46-9 5-[(2S,4S)-2-(2-phenylethyl)piperidin-4-yl]-2,3-dihydro-1,2-oxazol-3-one 

Relevant academic research and scientific papers

Discovery of the fibrinolysis inhibitor AZD6564, acting via interference of a protein-protein interaction

A class of novel oral fibrinolysis inhibitors has been discovered, which are lysine mimetics containing an isoxazolone as a carboxylic acid isostere. As evidenced by X-ray crystallography the inhibitors bind to the lysine binding site in plasmin thus preventing plasmin from binding to fibrin, hence blocking the protein-protein interaction. Optimization of the series, focusing on potency in human buffer and plasma clotlysis assays, permeability, and GABAa selectivity, led to the discovery of AZD6564 (19) displaying an in vitro human plasma clot lysis IC50 of 0.44 μM, no detectable activity against GABAa, and with DMPK properties leading to a predicted dose of 340 mg twice a day oral dosing in humans.

ISOXAZOL-3(2H)-ONE ANALOGS AS THERAPEUTIC AGENTS

or a pharmaceutically suitable salt thereof, wherein, R1 and R2 independently are hydrogen, deuterium, aryl, hetero aryl, C1-C8 alkyl, optionally being substituted with one or more substituents independently being R3,R3 is an aryl, hetero aryl, fluorine(s), a C1-C6 alkyl containing one or more fluorine, a C1-C6 alkyl containing one or more deuterium, a C1-C6 alkyl containing hydroxy, the aryl and heteroaryl optionally being substituted with one or more halogen, a fluorinated alkoxy, a fluorinated alkyl, a sulfonyl, one or more deuterium, a C1-6 alkyl, a C1-6 alkoxy, a nitrile,or R3 is a C1-6 alkyl optionally substituted with one or more of the following groups: COOR4, OCOR4, CONR5R6, NR5COR6, OR4;wherein, R4 is a C1-10 alkyl optionally substituted with one or more fluorine, deuterium, alkoxy, arylcarboxylate, alkyl carboxylate;R5 and R6 are independently selected from hydrogen, alkyl or they may together form a 4-8 membered carbon ring;or R1 and R2 form a 3-10 membered carbon ring optionally comprising O or N and optionally substituted with a C1-10 alkyl or aryl, hetero aryl optionally substituted with R3.