On November 17, 2016, Foreman, Kenneth W.; Nguyen, Hanh Nho; Ofori, Leslie Odame; Wanner, Jutta; Werner, Douglas S. published a patent.Application In Synthesis of Benzyl 2-(((benzyloxy)carbonyl)amino)acrylate The title of the patent was Preparation of silicon based drug conjugates and therapeutic uses thereof. And the patent contained the following:
Described herein are silicon based conjugates capable of delivering one or more pay load moieties to a target cell or tissue. Contemplated conjugates may include a silicon-heteroatom core, one or more optional catalytic moieties, a targeting moiety that permits accumulation of the conjugate within a target cell or tissue, one or more pay load moieties (e.g., a therapeutic agent or imaging agent), and two or more non-interfering moieties covalently bound to the silicon-heteroatom core. The silicon based conjugates of formula I [wherein L is a targeting moiety; RP is P, H, or R5; P is a payload moiety or cassette; R5 is independently at each occurrence H, OH, C1-6 alkyl, etc.; Y independently at each occurrence is -LL-G-LL-; LL independently at each occurrence is bond or substituted C1-20 alkylene; G independently at each occurrence is optional catalytic moieties selected from -heteroaryl, -O-heteroaryl, Ph, etc.; R1, R2, R3, and R4 are independently at each occurrence OH, α- or β-amino acid, heterocyclyl, etc.] or pharmaceutically acceptable salt, cocrystal, stereoisomer, metabolite, tautomer, solvate, or hydrate thereof, are claimed and exemplified. Folate receptor targeting conjugate II comprised of two different fluorescent dyes, BODIPY and rhodamine, was prepared from a multistep procedure (preparation given) and used in an imaging study demonstrating endocytosis and Si-O bond cleavage. The study revealed intact II was bound to the surface of folate receptor α expressing KB cells at t = 0 min. At t = 30 min endocytosis of II inside the endosomes was detected and cleavage of the siloxane core was visualized by color separation of the two fluorescent dyes. The experimental process involved the reaction of Benzyl 2-(((benzyloxy)carbonyl)amino)acrylate(cas: 59524-07-1).Application In Synthesis of Benzyl 2-(((benzyloxy)carbonyl)amino)acrylate
The Article related to silicon drug conjugate preparation targeted payload delivery therapeutic, folate receptor targeting conjugate endocytosis hydrolysis fluorescent imaging, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Application In Synthesis of Benzyl 2-(((benzyloxy)carbonyl)amino)acrylate
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