On February 3, 2005, Cheng, Jie Fei; Nguyen, Bao Ngoc; Liu, Xuewei; Lopaschuk, Gary D.; Dyck, Jason R. published a patent.Product Details of 29735-85-1 The title of the patent was Preparation of heterocyclic compounds useful as malonyl-CoA decarboxylase inhibitors. And the patent contained the following:
The present invention provides methods for the use of compounds I [X1, X2, X3 = O, N, NH, NR5, S, C; R1, R2 = H, halogen, substituted C1-6-alkyl, substituted C1-6-alkenyl, substituted C1-6-alkynyl, alkoxy, (un)substituted Ph, aryl, (un)substituted heteroaryl, NHCONR5R6, COR5, CONR5R6, S(O)nR5, SO2NR5R6; R3, R4 = H, Br, Cl, F, I, OH, OMe, CO2H, CO2R5, CONR5R6, S(O)nR5, SO2NR5R6, substituted C1-6-alkyl, C1-6-alkoxy, (un)substituted Ph, aryl, heteroaryl; R5, R6 = H, (un)substituted C1-6-alkyl, (un)substituted Ph, aryl, heteroaryl], its enantiomers, diastereomers, tautomers, or physiol. acceptable salts or prodrugs, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. Thus, benzofuran I [X1 = CC(:O)NHC6H3(OMe)2-3,4, X2 = CH, X3 = O, R3 = 4-Br, R4 = 6-Br] was prepared from 5-methoxybenzofuran-2-carboxylic acid via regioselective bromination at C(3), decarboxylation, debromination-carboxylation at C(3), O-demethylation, regioselective dibromination and amidation with 3,4-dimethoxyaniline. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. The inhibitory activity of I vs. malonyl-CoA decarboxylase was determined [Ki = 31.6 – 4750.2 μM]. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity. The experimental process involved the reaction of 5-Hydroxybenzofuran-3-carboxylic acid(cas: 29735-85-1).Product Details of 29735-85-1
The Article related to heterocyclic compound preparation malonyl coa decarboxylase inhibitor, cardiovascular disease prophylaxis management treatment heterocyclic compound, diabetes prophylaxis management treatment heterocyclic compound, cancer prophylaxis management treatment heterocyclic compound, obesity prophylaxis management treatment heterocyclic compound and other aspects.Product Details of 29735-85-1
Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem