CAS: 247184-89-0; Kalkitoxin

专利信息

专利号:US-11912647-B2
优先权日:2020-05-22
标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation
发明人：CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS
权利人:UNIV GEORGIA
摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.

专利号:US-2021363098-A1
优先权日:2020-05-22
标题 :Diversity-oriented synthesis of n,n,o-trisubstituted hydroxylamines from alcohols and amines by n-o bond formation

专利号:US-8816095-B2
优先权日:2008-08-15
标题:Na channels, disease, and related assays and compositions
发明人：BROWN MILTON L; GRINDROD SCOTT; WALLS THOMAS H; HANSEN TODD; SUY SIMENG; PAIGE MIKELL A
权利人:BROWN MILTON L; GRINDROD SCOTT; WALLS THOMAS H; HANSEN TODD; SUY SIMENG; PAIGE MIKELL A; UNIV GEORGETOWN
摘要:Disclosed are molecules and their synthesis, for use in blocking gated ion channels such as voltage-gated sodium channels (VGSCs) and prostate voltage sodium channels (PVSCs). These inhibitors have superior blocking efficacy, for instance in displacing the radioligand [ 3 H]-Batrachotoxin-B ([ 3 H]-BTX-B) that binds to site 2 of a VGSC. The molecules of the invention comprise a moiety which increases the binding affinity of molecules for the protein binding site in prostate cancer cells (PCs), and which is also fluorescent. In one embodiment the invention molecules are an inhibition system that can be used to target over-abundant or hyperactive VGSCs selectively in pain, epilepsy or prostate cancer, inhibiting the proliferation of PCs. The fluorescent moiety also facilitates screening, tracking, and pharmacodynamic studies of the drug in a biological system both in vitro and in vivo.