The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
May. 31, 1983

Filed:

Apr. 20, 1981
Applicant:
Inventors:

Mitree M Ponpipom, Branchberg, NJ (US);

Robert L Bugianesi, Colonia, NJ (US);

James C Robbins, Monmouth Junction, NJ (US);

Tsung-Ying Shen, Westfield, NJ (US);

Assignee:

Merck & Co., Inc., Rahway, NJ (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07C / ; C08B / ; C07H / ;
U.S. Cl.
CPC ...
2601 / ; 536 53 ; 536 187 ; 536 54 ; 536115 ;
Abstract

Cell-specific ligands comprising conjugates of saccharides and amino acids or peptides are synthesized from amino acids such as ornithine, lysine, peptides such as dilysine, diornithine or oligolysine and selected saccharides having reactive functional groups protected by appropriate blocking groups. Such glycopeptides are useful as tissue specific substances, which when coupled with bioactive materials through metabolizable or hydrolyzable linkages, deliver such bioactive materials to the selected site. In this manner, antiinflammatory drugs such as dexamethasone are linked through a metabolizable or hydrolyzable linkage and on administration to an animal suffering from inflammatory disease carries the drug to the site of inflammation for intracellular release. Other examples include the macrophage ligand N.sup.2 -N.sup.2, N.sup.6 -Bis-[3-(.alpha.-D-mannopyranosylthio)propionyl]-6-lysyl-N.sup.6 -[3-(.alpha.-D-mannopyranosylthio)propionyl]-L-lysine, 5, which when coupled to .beta.-glucocerebrosidase, can deliver the enzyme selectively to kupffer cells. This is useful in the enzyme replacement therapy of Gaucher's disease.


Find Patent Forward Citations

Loading…