CAS: 21508-19-0; 5-Chlorofuran-2-Carbaldehyde

相似化合物

618-30-4 58235-81-7 57240-59-2

上下游产品

furfural 5-chlorofuran-2-carbonyl chloride (furan-2-yl)methylene diacetate carbon disulfide t-(5-chloro-[2]furyl)-acrylic acid3t-(5-chloro-[2]furyl)-acrylic acid N-(5-chloro-furan-2-ylmethylene)-4-methyl-anilineN-(5-chloro-furan-2-ylmethylene)-4-methyl-aniline bis-[(5-chloro-[2]furyl)-phenyl-methyl]-ether N-(5-chloro-furan-2-ylmethylene)-anilineN-(5-chloro-furan-2-ylmethylene)-aniline

(乙酰基氧基)(2-呋喃基)乙酸甲酯置于二硫化碳,磺酰氯体系中,化学反应生成5-氯-2-糠醛
参考文献:Gilman; Wright,Recueil Des Travaux Chimiques Des Pays-Bas,1931,Vol. 50,P. 833,835
标题:Gilman; Wright,Recueil Des Travaux Chimiques Des Pays-Bas,1931,Vol. 50,P. 833,835

专利信息

专利号:US-10377729-B2
优先权日:2015-06-15
标题 :Bis-furan derivatives as transthyretin (TTR) stabilizers and amyloid inhibitors for the treatment of familial amyloid polyneuropathy (FAP)
发明人：VIEIRA SIMÕES CARLOS JOSÉ; LOURENÇO DE ALMEIDA ZAIDA CATARINA; VASCONCELOS DIAS DE PINHO E MELO TERESA MARGARIDA; PONTES MEIRELES FERREIRA DE BRITO RUI MANUEL; SILVA COSTA DORA CRISTINA; CABRAL CARDOSO LOPES ANA LÚCIA
权利人:BSIM THERAPEUTICS S A
摘要:The design and synthesis of a novel bis-furan scaffold tailored for high efficiency at inhibiting transthyretin amyloid formation is reported. In vitro results show that the discovered compounds are more efficient inhibitors of amyloid formation than tafamidis, a drug currently used in the treatment of familial amyloid polyneuropathy (FAP), despite their lower molecular weight and lipophilicity. Moreover, ex vivo experiments with the strongest inhibitor in the series, conducted in human blood plasma from normal and FAP Val30Met-transthyretin carriers, disclose remarkable affinity and selectivity profiles. The promises and challenges facing further development of this compound are discussed under the light of increasing evidence implicating transthyretin stability as a key factor not only in transthyretin amyloidoses and several associated co-morbidities, but also in Alzheimer's disease.