[EN] N-SUBSTITUTED MANNOSAMINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE<br/>[FR] DÉRIVÉS N-SUBSTITUÉS DE MANNOSAMINE, PROCÉDÉ POUR LEUR PRÉPARATION ET LEUR UTILISATION
申请人:GLYCOM AS
公开号:WO2012140576A1
公开(公告)日:2012-10-18
A compound of the formula (I) wherein R1 is a group removable by hydrogenolysis,and wherein R2 is OH or R2 is -NHR3 wherein R3 is a group removable by hydrogenolysis. The compound can be made from fructose by a Heyns-rearrangement. The compound can be used then to make - free D-mannosamine or its salts, - D-mannosamine building blocks and mannosamine containing oligo- or polysaccharides, - N-acetyl-D-mannosamine and its hydrates and solvates, - neuraminic acid derivatives and, - viral neuraminidase inhibitors.
Disclosed and claimed are prodrugs activated by catalytic proteins, such as enzymes and catalytic antibodies. The invention comprehends such prodrugs, as well as haptens, to elicit catalytic antibodies to activate the prodrugs. The prodrugs are useful as cytotoxic chemotherapeutic agents; e.g., as antitumor agents.
Disclosed are Mannich base N-oxides of drugs containing acidic N—H groups. Pharmaceutical compositions comprising a therapeutically effective amount of Mannich base N-oxides, or a N-oxide rearrangement product, pharmaceutically acceptable salt or prodrug thereof, are also disclosed. Further, disclosed are methods of using the compounds, alone or in combination with one or more other active agents or treatments.
N-SUBSTITUTED MANNOSAMINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE
申请人:Vrasidas Ioannis
公开号:US20140046051A1
公开(公告)日:2014-02-13
A compound of the formula (1) wherein R
1
is a group removable by hydrogenolysis, and wherein R
2
is OH or R
2
is —NHR
3
wherein R
3
is a group removable by hydrogenolysis. The compound can be made from fructose by a Heyns-rearrangement. The compound can be used then to make free D-mannosamine or its salts, D-mannosamine building blocks and mannosamine containing oligo- or polysaccharides, N-acetyl-D-mannosamine and its hydrates and solvates, neuraminic acid derivatives, and viral neuraminidase inhibitors.
Microencapsulation for controlled oral drug delivery system
申请人:KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
公开号:EP0480729A1
公开(公告)日:1992-04-15
The present invention provides a microencapsulation method of an oil droplet containing drugs for oral administration using polysaccharide which has metal-chelating capacity and the biocompatible and water-soluble polymer as a capsule material. The drug carrier system obtained in this invention using the microencapsulated emulsion represses the drug release from the system and protects the emulsion and drug from the strong acidic condition of gastric juice. The oil droplet and drug dispersed in the oil droplet was released rapidly in the small intestine with the disintegration of capsule material. The system obtained in this invention can reduce the gastric upset or damages on the stomach and protect drugs from the degradation in the gastric juice. At the same time, the degradation of drug caused by the hepatic first-pass metabolism can be lessened because the drug dispersed in oil droplet can be absorbed via lymphatic absorption.