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US 2006/0233740 A1Published application
Conjugates of an hGH moiety and a polymer
OwnerMary Bossard, Ping Zhanginventors
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Abstract
Conjugates of an hGH moiety and one or more non-peptidic water-soluble polymers are provided. Typically, the non-peptidic water-soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided are compositions comprising such conjugates, methods of making the conjugates, and methods of administering compositions comprising such conjugates to a mammalian subject.
Claims51
A conjugate comprising the following structure:
- wherein POLY is a linear water-soluble polymer;
- (a) is either zero or one;
- X, when present, is a spacer moiety comprised of one or more atoms;
- R1 is an organic radical containing 1 to 3 carbon atoms;
- and hGH is a residue of a human growth hormone (“hGH”) moiety.
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A composition comprising:
- wherein:
- POLY is a water-soluble polymer;
- (a) is either zero or one;
- (b) is either 0 or an integer having a value from 1 to 10;
- (c) is an integer having a value from 1 to 10;
- (d) is either zero or one;
- (e) is either one or two;
- X, when present, is a spacer moiety comprised of one or more atoms;
- R1 is H or an organic radical containing from 1 to 3 carbon atoms;
- Either R2 and R3, when taken together with the carbon atom to which they are attached, in each occurrence considered separately, forms a carbonyl (C═O), or
- R2, in each occurrence, is independently H or an organic radical, and
- R3, in each occurrence, is independently H or an organic radical;
- and
- hGH is a residue of a human growth hormone residue,
- wherein the following provisos apply:
- (i) when R2 and R3, when taken together with the carbon atom to which they are attached form a carbonyl adjacent to the —NH—, and POLY is linear, then (d) equals one and R1 is an organic radical containing from 1 to 3 carbon atoms;
- (ii) when R2 and R3, in each occurrence, are each independently H or an organic radical, then (b) is a positive integer and (a) is one;
- (iii) when POLY is branched, POLY does not contain a lysine residue,
- and further wherein when (e) is one, the composition comprises 85% or greater monoconjugate with respect to all conjugate species contained in the composition, and when (e) is two, the composition comprises greater than 80% diconjugate with respect to all conjugate species contained in the composition, and said composition is bioactive.
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Dependencies are inferred from the claim text.