Compounds, their synthesis and their uses

摘要

The present invention discloses novel chemical compounds obtained by causing a covalent attachment of a modifying agent of the structure provided for formula 1, to a functional group or a heteroatom of a heterocyclic ring system in chemical compound with improved chemical and biological properties. Wherein: Y is DRUG-CO; DRUG-OCO; DRUG-NRCO, and X is selected from.

主权项

1. A method for modifying the properties of a drug, comprising
(i) converting the DRUG to DRUG-O—C(R1R2)G (ii) reacting the DRUG-O—C(G(R1R2)G with to give [Y—O—X]+G−, wherein: Y is the drug linked to through a carbonyl (—CO—), oxycarbonyl (—O—CO—), or amine carbonyl (—NR—CO—) X is selected from R, R1 and R2 are independently H; C1-C8 straight, or branched chain alkyl; C1-C8 straight or branched chain alkyl substituted with 1-3 heteroatoms selected from O, N, S, SO, or SO2; 3-7 membered cycloalkyl; 3-7 membered cyclo alkyl that has been substituted with 1-3 heteroatoms selected from O, N, S, SO, or SO2 and/or lower alkyl; straight or branched alkyl, alkoxy; alkaryl, aryl, heteroaryl, or alkheteroaryl; or is independently part of 3-7 membered ring optionally containing additional 1-2 heteroatoms selected from, O, N, S, SO, SO2 and optionally substituted with alkoxy, F or Cl; and G− is selected from iodide, chloride, bromide, mesylate, tosylate and tetra fluoroborate.