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Generated: December 13, 2017

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Title:Spacer moiety for poly(ethylene glycol) modified peptide based compounds
Abstract: The present invention relates to a compound comprising a peptide moiety, a spacer moiety and a water-soluble polymer moiety such as a poly(ethylene glycol) moiety. The spacer moiety is between the peptide moiety and the water-soluble polymer moiety. The spacer moiety has the structure: --NH--(CH.sub.2).sub..alpha.--[O--(CH.sub.2).sub..beta.].sub..gamma.--O.s- ub..delta.--(CH.sub.2).sub..epsilon.--Y-- wherein .alpha., .beta., .gamma., .delta., and .epsilon. are each integers whose values are independently selected.
Inventor(s): Holmes; Christopher P. (Saratoga, CA), Tumelty; David (Sunnyvale, CA), Yin; Qun (Palo Alto, CA)
Assignee: Affymax, Inc. (Palo Alto, CA)
Filing Date:Apr 04, 2011
Application Number:13/079,615
Claims:1. A compound comprising a peptide moiety, a spacer moiety, and a water-soluble polymer moiety wherein: the peptide moiety comprises at least one peptide monomer; the spacer moiety is between the peptide moiety and the water-soluble polymer moiety, and has the structure: --NH--(CH.sub.2).sub..alpha.--[O--(CH.sub.2).sub..beta.].sub..gamma.--O.s- ub..delta.--(CH.sub.2).sub..epsilon.--Y--; .alpha. is an integer, 1.ltoreq..alpha..ltoreq.6; .beta. is an integer, 1.ltoreq..beta..ltoreq.6; .epsilon. is an integer, 1.ltoreq..epsilon..ltoreq.6; .delta. is 0 or 1; .gamma. is an integer, 0.ltoreq..gamma..ltoreq.10; and Y is either NH or CO.

2. The compound of claim 1, wherein the peptide moiety is a peptide monomer comprising a single peptide.

3. The compound of claim 1, wherein the peptide moiety comprises two peptide monomers linked by a linker moiety.

4. The compound of claim 1, wherein the peptide moiety comprises one or more peptides which bind to thrombopoietin-receptors.

5. A pharmaceutical composition comprising (a) a compound comprising a peptide moiety, a spacer moiety and a water-soluble polymer moiety; and (b) one or more pharmaceutically acceptable diluents, preservatives, solubilizers, emulsifiers, adjuvants or carriers wherein: the peptide moiety comprises at least one peptide monomer, the spacer moiety is between the peptide moiety and the water-soluble polymer moiety and has the structure: --NH--(CH.sub.2).sub..alpha.--[O--(CH.sub.2).sub..beta.].sub..gamma.--O.s- ub..delta.--(CH.sub.2).sub..epsilon.--Y-- .alpha. is an integer, 1.ltoreq..alpha..ltoreq.6; .beta. is an integer, 1.ltoreq..beta..ltoreq.6; .epsilon. is an integer, 1.ltoreq..epsilon..ltoreq.6; .delta. is 0 or 1; .gamma. is an integer, 0.ltoreq..gamma..ltoreq.10; and Y is either NH or CO.

6. The composition of claim 5, wherein the peptide moiety is peptide monomer comprising a single peptide.

7. The composition of claim 5, wherein the peptide moiety comprises two peptide monomers linked by a linker moiety.

8. The composition of claim 5, wherein the peptide moiety comprises one or more peptides which bind to thrombopoietin-receptors.

9. The compound according to claim 3, wherein the linker moiety has the structure ##STR00005## N of the linker moiety is covalently attached to Y of the spacer moiety, Y of the spacer moiety is CO, and .eta. and .phi. are integers whose values are independently selected.

10. The composition according to claim 7, wherein the linker moiety has the structure ##STR00006## N of the linker moiety is covalently attached to Y of the spacer moiety, Y of the spacer moiety is CO, and .eta. and .phi. are integers whose values are independently selected.
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