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Claims for Patent: 7,919,118

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Claims for Patent: 7,919,118

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), Yin; Qun (Palo Alto, CA), Tumelty; David (Sunnyvale, CA)
Assignee: Affymax, Inc. (
Application Number:10/555,860
Patent Claims: 1. A compound which comprises: (a) a peptide moiety comprising at least two peptide monomers, (b) a linker moiety connecting the two peptide monomers and having the structure ##STR00005## (c) a spacer moiety having the structure --NH--(CH.sub.2).sub..alpha.--[O--(CH.sub.2).sub..beta.].gamma.--O.sub..d- elta.--(CH.sub.2).sub..epsilon.--Y-- in which Y of the spacer moiety is CO attached to N of the linker moiety; and (d) a water-soluble polymer moiety attached to the spacer moiety; wherein .alpha., .beta., .gamma., .delta., and .epsilon. are each integers whose values are independently selected.

2. The compound of claim 1, wherein .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; and .gamma. is an integer, 0.ltoreq.y.ltoreq.10.

3. The compound of claim 2, wherein .gamma.>1 and .beta.=2.

4. The compound of claim 1 wherein .alpha.=.beta.=.epsilon.=2; and .gamma.=.delta.=1.

5. The compound of claim 1 wherein the water-soluble polymer moiety is a poly(ethylene glycol) moiety.

6. The compound of claim 5 wherein the molecular weight of the poly(ethylene glycol) moiety is 20 KDalton or more.

7. The compound of claim 5, wherein the poly(ethylene glycol) moiety is linear.

8. The compound of claim 5, wherein the poly(ethylene glycol) moiety has a molecular weight from 20 to 40 KDalton.

9. The compound of claim 5, wherein the poly(ethylene glycol) moiety has polydispersity value (M.sub.w/M.sub.n) of less than 1.20.

10. The compound of claim 1, wherein each peptide monomer comprises no more than 50 amino acid monomers.

11. The compound of claim 10, wherein each peptide monomer comprises between about 10 and 25 amino acid monomers.

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

13. The compound of claim 1, wherein .alpha.=2; and .gamma.=.delta.=.beta.=.epsilon.=0.

14. The compound of claim 5 wherein the poly(ethylene glycol) moiety comprises at least one monomeric poly(ethylene glycol) chain.

15. The compound of claim 14 wherein each poly(ethylene glycol) chain has a molecular weight from 20 to 40 KDaltons.

16. The compound of claim 5, wherein the poly(ethylene glycol) moiety comprises two monomeric poly(ethylene glycol) chains.

17. The compound of claim 16, wherein each monomeric poly(ethylene glycol) chain has a molecular weight from 20 to 40 KDaltons.

18. The compound of claim 16, wherein the two monomeric poly(ethylene glycol) chains are linked together through a lysine residue.

19. The compound of claim 16, wherein the two monomeric poly(ethylene glycol) chains are linked together through a lysine amide.

20. The compound of claim 1, wherein .eta. is an integer 1.ltoreq..eta..ltoreq.6; and .phi. is an integer 1.ltoreq..phi..ltoreq.6.

21. The compound of claim 20, wherein .eta.=.phi.=1.

22. The compound of claim 1, wherein (i) one or both peptide monomers comprise a lysine residue having an .epsilon.-amino group, and (ii) one or both CO linkages of the linker moiety form an amide bond with the .epsilon.-amino group.

23. A pharmaceutical composition comprising a compound and one or more pharmaceutically acceptable diluents, preservatives, solubilizers, emulsifiers, adjuvants or carriers, wherein the compound comprises (a) a peptide moiety comprising at least two peptide monomers, (b) a linker moiety connecting the two peptide monomers and having the structure ##STR00006## (c) a spacer moiety having 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-- in which Y of the spacer moiety is a CO attached to N of the linker moiety, and (d) a water-soluble polymer moiety attached to the spacer moiety wherein .alpha., .beta., .gamma., .delta. and .epsilon. are each integers whose values are independently selected.

24. The composition of claim 23, wherein .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.c.ltoreq.6; .delta. 0 or 1; and .gamma. is an integer, 0.ltoreq..gamma..ltoreq.10.

25. The composition of claim 24, wherein .gamma.>1 and .beta.=2.

26. The composition of claim 23 wherein .alpha.=.beta.=.epsilon.+2; and .gamma.=.delta.=1.

27. The composition of claim 23 wherein the water-soluble polymer moiety is a poly(ethylene glycol) moiety.

28. The composition of claim 27 wherein the molecular weight of the poly(ethylene glycol) moiety is 20 KDalton or more.

29. The composition of claim 27, wherein the poly(ethylene glycol) moiety is linear.

30. The composition of claim 27, wherein the poly(ethylene glycol) moiety has a molecular weight from 20 to 40 KDalton.

31. The composition of claim 27, wherein the poly(ethylene glycol) moiety has polydispersity value (M.sub.w/M.sub.n) of less than 1.20.

32. The composition of claim 23, wherein each peptide monomer comprises no more than 50 amino acid monomers.

33. The composition of claim 32, wherein each peptide monomer comprises between about 10 and 25 amino acid monomers.

34. The composition of claim 23, wherein the peptide moiety comprises one or more peptides which bind to erythropoietin-receptors.

35. The composition of claim 23, wherein .alpha.=2; and .gamma.=.delta.=.beta.=.epsilon.0.

36. The composition of claim 27 wherein the poly(ethylene glycol) moiety comprises at least one monomeric poly(ethylene glycol) chain.

37. The compound of claim 36 wherein each poly(ethylene glycol) chain has a molecular weight from 20 to 40 KDaltons.

38. The composition of claim 27, wherein the poly(ethylene glycol) moiety comprises two monomeric poly(ethylene glycol) chains.

39. The composition of claim 38, wherein each monomeric poly(ethylene glycol) chain has a molecular weight from 20 to 40 KDaltons.

40. The composition of claim 38, wherein the two monomeric poly(ethylene glycol) chains are linked together through a lysine residue.

41. The composition of claim 38, wherein the two monomeric poly(ethylene glycol) chains are linked together through a lysine amide.

42. The composition of claim 23, wherein .eta. is an integer 1.ltoreq..eta..ltoreq.6; and .phi. is an integer 1.ltoreq..phi..ltoreq.6.

43. The composition of claim 42, wherein .eta.=.phi.=1.

44. The composition of claim 23, wherein: (i) one or both peptide monomers comprise a lysine residue having an .epsilon.-amino group, and (ii) one or both CO linkages of the linker moiety form an amide bond with the .epsilon.-amino group.
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