摘要:
The present invention relates to a method of producing a hydroxyalkyl starch derivative, said hydroxyalkyl starch having a structure according to formula (I)
comprising reacting - hydroxyalkyl starch of formula (I) at its optionally oxidized reducing end or - a hydroxyalkyl starch derivative, obtainable by reacting hydroxyalkyl starch of formula (I) at its optionally oxidized reducing end with a compound (D), said compound (D) comprising -- at least one functional group Z 1 capable of being reacted with the optionally oxidized reducing end of the hydroxyalkyl starch, and -- at least one functional group W,
with a compound (L) comprising - at least one functional group Z 1 capable of being reacted with said hydroxyalkyl starch, or at least one functional group Z 2 capable of being reacted with functional group W comprised in said hydroxyalkyl starch derivative, and - at least one functional group X capable of being reacted with a functional group Y of a further compound (M),
wherein said functional group Y is selected from the group consisting of an aldehyd group, a keto group, a hemiacetal group, an acetal group, and a thio group. The present invention further relates to the hydroxyalkyl starch derivatives as such ans a pharmaceutical composition comprising the hydroxyalkyl starch derivatives.
摘要:
The present invention relates to conjugates of hydroxyalkyl starch and a protein wherein these conjugates are formed by a covalent linkage between the hydroxyalkyl starch or a derivative of the hydroxyalkyl starch and the protein. The present invention also relates to the method of producing these conjugates and the use of these conjugates.
摘要:
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-R" (II)
wherein R 1 , R 2 and R 3 are independently hydrogen or a linear or branched hydroxyalkyl group, wherein compound (II) is reacted via the NH group bridging R' and R" with compound (I) at its reducing end which is not oxidized.
摘要:
The present invention relates to hydroxyalkylstarch (HAS)-polypeptide-conjugate (HAS-polypeptide) comprising one or more HAS moecules, 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).
摘要:
The present invention relates to hydroxyalkylstarch (HAS)-polypeptide-conjugate (HAS-polypeptide) comprising one or more HAS moecules, 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).
摘要:
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-R" (II)
wherein R 1 , R 2 and R 3 are independently hydrogen or a linear or branched hydroxyalkyl group, and wherein either R' or R" or R' and R" 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.
摘要:
The present invention relates to hydroxyalkylstarch (HAS)-polypeptide-conjugate (HAS-polypeptide) comprising one or more HAS moecules, 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).
摘要:
Die vorliegende Erfindung betrifft die Kopplung von niedermolekularen Substanzen an ein von Stärke abgeleitetes modifiziertes Polysaccharid, wobei die bindende Wechselwirkung zwischen dem modifizierten Polysaccharid und der niedermolekularen Substanz auf einer kovalenten Bindung beruht, welche das Ergebnis einer Kopplungsreaktion zwischen der endständigen Aldehydgruppe oder einer aus dieser Aldehydgruppe durch chemische Umsetzung hervorgegangenen funktionellen Gruppe des modifizierten Polysaccharidmoleküls und einer mit dieser Aldehydgruppe oder daraus hervorgegangenen funktionellen Gruppe des Polysaccharidmoleküls reaktionsfähigen funktionellen Gruppe der niedermolekularen Substanz ist, wobei die bei der Kopplungsreaktion unmittelbar resultierende Bindung gegebenenfalls durch eine weitere Reaktion zur obengenannten kovalenten Bindung modifiziert sein kann. Die Erfindung betrifft ferner pharmazeutische Zusammensetzungen, welche die bei der Kopplung gebildeten Konjugate umfassen, und die Verwendung dieser Konjugate und Zusammensetzungen zur prophylaktischen oder therapeutischen Behandlung des menschlichen oder tierischen Körpers.