The invention is related to boronate compds. of formula I with neuroprotective, antiplatelet, antitumor, and antimicrobial activities for the treatment of diseases and conditions assocd. to oxidative stress. Compds. of formula I wherein X1 and X2 are independently CH and CH2; X3 and X4 are independently S and SH; A is (CH2)n; n is 1 to 10; R is H, (un)substituted alkyl, (un)substituted aryl, etc.; R1 and R2 are independently H, CH3, alkyl, etc.; R1 and R2 can be taken together to in a cyclic compd.; and their pharmaceutically acceptable stereoisomers, enantiomers, conformers and racemic mixt. of different stereoisomers thereof, are claimed. Example compd. II was prepd. by amidation of 5-(S)-(1,2-dithiolanyl-3-yl)pentanoic acid with 3a,5,5-trimethylhexahydro-4,6-methanobenzo[d][1,3,2]dioxaborol-2-ylmethylamine hydrochloride. The compds. of formula I were evaluated for their antiplatelet activity (data given).
Preparation of boronate derivatives for the treatment of diseases and conditions associated to oxidative stress
DI STEFANO ANTONIO;CACCIATORE IVANA;
2018-01-01
Abstract
The invention is related to boronate compds. of formula I with neuroprotective, antiplatelet, antitumor, and antimicrobial activities for the treatment of diseases and conditions assocd. to oxidative stress. Compds. of formula I wherein X1 and X2 are independently CH and CH2; X3 and X4 are independently S and SH; A is (CH2)n; n is 1 to 10; R is H, (un)substituted alkyl, (un)substituted aryl, etc.; R1 and R2 are independently H, CH3, alkyl, etc.; R1 and R2 can be taken together to in a cyclic compd.; and their pharmaceutically acceptable stereoisomers, enantiomers, conformers and racemic mixt. of different stereoisomers thereof, are claimed. Example compd. II was prepd. by amidation of 5-(S)-(1,2-dithiolanyl-3-yl)pentanoic acid with 3a,5,5-trimethylhexahydro-4,6-methanobenzo[d][1,3,2]dioxaborol-2-ylmethylamine hydrochloride. The compds. of formula I were evaluated for their antiplatelet activity (data given).File | Dimensione | Formato | |
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