Fresenius Kabi Deutschland Gmbh

Harald Conradt

Norbert Zander

Wolfram Eichner

Ronald Frank

Klaus Sommermeyer

Michele Orlando

Klaus Langer

Frank Hacket

Elmar Kraus

Martin Schimmel

Eckart Grabenhorst

Manfred Nimtz

Conjugates of hydroxyalkyl starch and a protein are provided herein. The conjugates are formed by a covalent linkage between the hydroxyalkyl starch or a derivative of the hydroxyalkyl starch and the protein. Methods of producing the conjugates and the use of the conjugates also are provided herein.

Conjugates of hydroxyalkyl starch and a protein

The present invention relates to hydroxyalkylstarch (HAS)-polypeptide-conjugate (HAS-polypeptide) comprising one or more HAS molecules, wherein each HAS is conjugated to the polypeptide via a carbohydrate moiety or a thioether as well as to methods for the production thereof. In a preferred embodiment, the polypeptide is erythropoietin (EPO).

Hasylated polypeptides

The present invention relates to a method of producing a hydroxyalkyl starch derivative comprising reacting hydroxyalkyl starch of formula (I) at its reducing end which is not oxidized prior to said reaction, with a compound of formula (II) R'NH&#x2014;R&#x2033; (II) wherein R-Rand Rare independently hydrogen or a linear or branched hydroxyalkyl group, and wherein either R&#x2032; or R&#x2033; or R&#x2032; and R&#x2033; comprise at least one functional group X capable of being reacted with at least one other compound prior to or after the reaction of (I) and (II), as well as to the hydroxyalkyl starch derivative as such, obtainable by said method, and to a pharmaceutical composition comprising said hydroxyalkyl starch derivative.

Hydroxyalkyl starch derivatives

Conjugates of hydroxyalkyl starch and a protein are provided. The conjugates are formed by a reductive amination reaction between at least one aldehyde group or keto group or hemiacetal group of the hydroxyalkyl starch or of a derivative of the hydroxyalkyl starch, and at least one amino group of the protein, so that the hydroxyalkyl starch or the derivative thereof is covalently linked to the protein via an azomethine linkage or a amino linkage. Methods of producing these conjugates and specific uses of the conjugates also are provided.

Conjugates of hydroxyalkyl starch and a protein, prepared by reductive amination

Conjugates of hydroxyalkyl starch and a protein are provided herein. The conjugates are formed by a convalent linkage between the hydroxyalkyl starch or a derivative of the hydroxyalkyl starch and the protein. Methods of producing the conjugates and the use of the conjugates also are provided herein.

The invention relates to starch derivatives of formula (I), in which: X represents a bromine or iodine atom; R&#x2033; represents a straight-chain or branched alkyl group, aryl group or aralkyl group, and; R&#x2014;CO&#x2014; represents an oxidized substituted or unsubstituted starch radical that is oxidized on the reducing terminal group to form a carboxylic acid. Starch derivatives of formula (I) can selectively couple to active substances containing SH groups and have a prolonged half-life period in the human body. The invention also relates to coupling products of compound (I) with active substances, to methods for the production thereof, and to their use as medicaments 

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Braunschweig, Germany

Harald Conradt