Claims for Patent: 6,146,658

Summary for Patent: 6,146,658

Title:	Prodrugs, their preparation and use as pharmaceuticals
Abstract:	Glycosyl-spacer-drugs compounds (prodrugs), their preparation and their use as pharmaceuticals are described.
Inventor(s):	Bosslet; Klaus (Marburg, DE), Czech; Jorg (Marburg, DE), Hoffmann; Dieter (Marburg-Elnhausen, DE), Kolar; Cenek (Marburg, DE), Tillequin; Fran.cedilla.ois (Paris, FR), Florent; Jean-Claude (Les Ulis, FR), Azoulay; Michel (Paris, FR), Monneret; Claude (Paris, FR), Jacquesy; Jean-Claude (Buxerolles, FR), Gesson; Jean-Pierre (Chansseneuil du Poitou, FR), Koch; Michel (La Celle Saint Cloud, FR)
Assignee:	Hoechst Aktiengesellschaft (Frankfurt am Main, DE)
Application Number:	08/859,084
Patent Claims:	1. A method for the treatment of diseases in which intracellular enzymes are released or are made accessible by cell damage, which method comprises administering to a host in need of said treatment an effective amount of a glycosyl-spacer-drug compound; wherein the glycosyl radical is a mono-, oligo- or polysaccharide which can be cleaved off enzymatically; wherein the drug is a compound which has antitumor or antiinflammatory or immunosuppressant properties, and the drug contains an OH or NH.sub.2 group which is capable of coupling; and wherein the spacer is self-eliminating and is bonded via O or N to the glycosyl radical and via O or N to the drug. 2. The method as claimed in claim 1, wherein the compound is present in a liposome or bound to a carrier protein. 3. The method as claimed in claim 1, wherein the compound is present in combination with a compound which breaks multiple drug resistance. 4. The method as claimed in claim 3, wherein the compound which breaks multiple drug resistance is cyclosporin A, R-verapamil, pentoxifylline or rapamycin. 5. The method as claimed in claim 3, wherein the carrier protein is human serum albumin or human acid alpha-1 glycoprotein. 6. The method as claimed in claim 1 wherein the glycosyl radical is a mono-, oligo- or polysaccharide which is cleaved off by enzymatic hydrolysis and then the spacer is spontaneously cleaved off by chemical hydrolysis. 7. The method as claimed in claim 1 wherein the spacer is an aromatic or heteroaromatic or aliphatic group with conjugated double bonds or an amino-acid derivative which cyclizes after elimination of the glycosyl radical. 8. The method as claimed in claim 1 in which the glycosyl-spacer-drug compound is administered in the form of a pharmaceutical composition also comprising a pharmaceutically acceptable carrier.

Details for Patent 6,146,658

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Grifols Therapeutics Llc	ALBUKED, PLASBUMIN-20, PLASBUMIN-25, PLASBUMIN-5	albumin (human)	For Injection	101138	10/21/1942		2012-10-27
Baxalta Us Inc.	BUMINATE, FLEXBUMIN	albumin (human)	Injection	101452	03/03/1954		2012-10-27
Csl Behring Ag	ALBURX	albumin (human)	Injection	102366	07/23/1976		2012-10-27
Grifols Biologicals Llc	ALBUTEIN	albumin (human)	Injection	102478	08/15/1978		2012-10-27
Instituto Grifols, S.a.	HUMAN ALBUMIN GRIFOLS	albumin (human)	Injection	103352	02/17/1995		2012-10-27
Instituto Grifols, S.a.	HUMAN ALBUMIN GRIFOLS	albumin (human)	Injection	103352	06/11/2003		2012-10-27
Csl Behring Llc	ALBUMINAR, ALBUMINAR-20, ALBUMINAR-25, ALBUMINAR-5	albumin (human)	Injection	103955	03/17/2000		2012-10-27