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US 2010/0160409 A1Published application
Highly Branched Reagents For Modifying Biopharmaceuticals, Their Preparation And Use
OwnerRalf Krahmer, Frank Leendersinventors
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Abstract
The invention relates to compounds, which are suitable for coupling to pharmaceuticals, in particular biopharmaceuticals, in addition to conjugates from the compounds comprising biomolecules or pharmaceutically active substances. The inventive compounds are highly cross-linked and can be formed in a simple manner by using a central cross-linking module. The invention also relates to the use of conjugates as an improved formulation of pharmaceuticals and to the production thereof.
Claims27
A compound of the formula (I)
- where
- r is an integer between 1 and 20,
- P, L, T and Y are each independently of one another a hydrocarbon radical, wherein P exhibits at least one group of the formula (IIa)
- R1—(CH2—CH2—O)n—CH2—CH2— formula (IIa)
- in which
- R1 is H, OH or a hydrocarbon radical which has from 1 to 50 carbon atoms,
- n is, on each occasion independently, an integer of from 2 to 1000, and wherein group T exhibits the structure
- the compound containing in total at least three groups of the formula (IIa).
5 more elements
A compound of the formula (I)
- where
- r is an integer between 1 and 20,
- P, L, T and Y are each independently of one another a hydrocarbon radical,
- wherein group L has the structure
- where
- B is H, OH, C1-C4-alkyl, O—R2 or CO—R3,
- R1 is H, OH or a hydrocarbon radical which has from 1 to 50 carbon atoms,
- R2 is, on each occasion independently, a hydrocarbon radical having from 1 to 6 carbon atoms,
- R3 is OH or NR4R5,
- R4 and R5 are, in each case independently, H or a hydrocarbon radical, where R4 and R5 may also together form a ring system,
- r is an integer between 1 and 20,
- X is NR1, S, O or C═O, and
- h is 0 or 1.
10 more elements
Dependencies are inferred from the claim text.