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OwnerBeat Amrein, Stefan Foser +7inventors
InventorsBeat Amrein, Stefan Foser, Kurt Lang, Friedrich Metzger, Joerg Regula, Andreas Schaubmar, Friederike Hesse, Klaus-Peter Kuenkele, Martin Lanzendoerfer
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A conjugate consisting of an insulin-like growth factor-1 (IGF-I) variant and one or two poly(ethylene glycol) group(s), characterized in that said IGF-I variant has an amino acid alteration at up to three amino acid positions 27, 37, 65, 68 of the wild-type IGF-I amino acid sequence so that one or two of said amino acids is/are lysine and amino acid 27 is a polar amino acid but not lysine, is conjugated via the primary amino group(s) of said lysine(s) and said poly(ethylene glycol) group(s) have an overall molecular weight of from 20 to 100 kDa is disclosed. This conjugate is useful for the treatment of neurodegenerative disorders like Alzheimer's Disease.
A conjugate comprising an IGF-I variant and poly(ethylene glycol), wherein the IGF-I variant has at least one amino acid alteration selected from the group consisting of alterations at amino acid positions 27, 37, 65, and 68 of the wild-type IGF-I amino acid sequence wherein one or more of amino acids selected from the group consisting of 37, 65, and 68 is lysine, wherein amino acid 27 is a polar amino acid but is not lysine, and wherein said poly(ethylene glycol) is conjugated to said IGF-I variant via one or more primary amino groups.
An IGF-I variant selected from the group consisting of RRKK, RRRK, RRKR, and RKRR wherein up to three amino acids at the N-terminus are truncated.
An IGF-I variant having at least one amino acid alteration selected from the group consisting of alterations at amino acid positions 27, 37, 65, and 68 of the wild-type IGF-I amino acid sequence wherein one or more of amino acids selected from the group consisting of 37, 65, and 68 is lysine, wherein amino acid 27 is a polar amino acid but is not lysine.
A composition comprising a conjugate comprising an IGF-I variant and poly(ethylene glycol), wherein the IGF-I variant has at least one amino acid alteration selected from the group consisting of alterations at amino acid positions 27, 37, 65, and 68 of the wild-type IGF-I amino acid sequence wherein one or more of amino acids selected from the group consisting of 37, 65, and 68 is lysine, wherein amino acid 27 is a polar amino acid but is not lysine, and wherein said poly(ethylene glycol) is conjugated to said IGF-I variant via one or more primary amino groups) and an IGF-I variant which is conjugated to poly(ethylene glycol) at its N-terminus.
A pharmaceutical composition comprising a conjugate comprising an IGF-I variant and poly(ethylene glycol), wherein the IGF-I variant has at least one amino acid alteration selected from the group consisting of alterations at amino acid positions 27, 37, 65, and 68 of the wild-type IGF-I amino acid sequence wherein one or more of amino acids selected from the group consisting of 37, 65, and 68 is lysine, wherein amino acid 27 is a polar amino acid but is not lysine, and wherein said poly(ethylene glycol) is conjugated to said IGF-I variant via one or more primary amino groups, an IGF-I variant which is conjugated to poly(ethylene glycol) at its N-terminus, and a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.