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US 5,382,657 AGranted
Peg-interferon conjugates
AssigneeHoffmann-La Roche Inc.
InventorsRobert Karasiewicz, Carlo Nalin, Perry Rosen
Life of this patent
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Abstract
Substituted PEG-interferon conjugates of formulae IA and IB where PEG is linked by means of activated linking reagents of formulae IIA, IIB, or IIB-1 to an amino group in the interferon, and activated linking reagents of formulae IIA, IIB, or IIB-1. The conjugates are not readily susceptible to in vivo hydrolytic cleavage, have enhanced in vivo half life, and reduce the immunogenicity of the interferon while maintaining biological activity.
Claims20
A physiologically active interferon conjugate having the formula:
- ##STR6## wherein R is lower alkyl;
- R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are H or lower alkyl;
- m is a number up to the number of accessible amino groups in the protein;
- and x, y and z are selected from any combination of numbers such that the conjugate has at least a portion of the biological activity of the interferons which forms the conjugate, with the proviso that at least one of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 is lower alkyl.
1 more element
A reagent of the formula:
- ##STR7## wherein R is lower alkyl, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are H or lower alkyl;
- and x, y, and z are selected from any combination of numbers such that the reagent when conjugated to a protein allows said protein to retain an activity at least equivalent to a portion of its biological activity when not conjugated, with the proviso that at least one of R.sub.1, R.sub.2, R.sub.3, and R.sub.4 is lower alkyl.
A reagent of the formula:
- ##STR8## wherein R is lower alkyl;
- R'.sub.1, R'.sub.2, R'.sub.3, R'.sub.4, are H or methyl;
- R.sub.5 is H or lower alkyl;
- and x, y, and z are selected from any combination of numbers such that the reagent when conjugated to a protein allows said protein to retain an activity at least equivalent to its biological activity when not conjugated.
1 more element
Dependencies are inferred from the claim text.