Claims for Patent: 7,199,098

Summary for Patent: 7,199,098

Title:	Copolymer-1 improvements in compositions of copolymers
Abstract:	The present invention relates to an improved composition of copolymer-1 comprising copolymer-1 substantially free of species having a molecular weight of over 40 kilodaltons.
Inventor(s):	Konfino; Eliezer (Ramat Gan, IL), Sela; Michael (Rehovot, IL), Teitelbaum; Dvora (Rehovot, IL), Arnon; Ruth (Rehovot, IL)
Assignee:	Yeda Research and Development Co., Ltd. (Rehovot, IL)
Application Number:	11/098,432
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,199,098
Patent Claims:	1. A copolymer-1 composition comprising a mixture of copolymers of alanine, glutamic acid, lysine and tyrosine, the copolymer species in the mixture being non-uniform with respect to molecular weight and sequence, wherein over 75% of the copolymers in the mixture, on a molar fraction basis, have a molecular weight in the range of 2 kDa to 20 kDa and less than 5% of the copolymers have a molecular weight above 40 kDa, and wherein the composition is suitable for treating multiple sclerosis. 2. The composition of claim 1, wherein the mixture has an average molecular weight of 7000 Da.+-.2000 Da. 3. The composition of claim 1, wherein the mixture has an average molecular weight of 4 to 8.6 kDa. 4. The composition of claim 1, wherein the mixture has an average molecular weight of 6.25 to 8.4 kDa. 5. The composition of claim 1, wherein the mixture has an average molecular weight of 4 to 8 kDa. 6. The composition of claim 1, wherein the mixture has an average molecular weight of 7 to 8 kDa. 7. The composition of claim 1, wherein the mixture has a molecular weight distribution as depicted in FIG. 1 for the mixture with an average molecular weight of 7.7 kDa. 8. The composition of claim 1, wherein less than 2.5% of the copolymers in the mixture have a molecular weight above 40 kDa. 9. The composition of claim 8, wherein the mixture has an average molecular weight of 7000 Da.+-.2000 Da. 10. The composition of claim 8, wherein the mixture has an average molecular weight of 4 to 8.6 kDa. 11. The composition of claim 8, wherein the mixture has an average molecular weight of 6.2 5 to 8.4 kDa. 12. The composition of claim 8, wherein the mixture has an average molecular weight of 4 to 8 kDa. 13. The composition of claim 8, wherein the mixture has an average molecular weight of 7 to 8 kDa. 14. The composition of claim 8, wherein the mixture has a molecular weight distribution as depicted in FIG. 1 for the mixture with an average molecular weight of 7.7 kDa. 15. A process for preparing a copolymer-1 composition having an average molecular weight of 4 to about 8.6 kDa comprising: polymerizing a mixture of an N-carboxyanhydride of tyrosine, an N-carboxyanhydride of alanine, .gamma.-benzyl glutamate and trifluoroacetyllysine in a molar ratio of 1:5:2:4 to form a mixture of protected polypeptides; deprotecting the protected polypeptides to form a mixture of unprotected polypeptides; and isolating a copolymer-1 composition of unprotected polypeptides composed of glutamic acid, lysine, alanine and tyrosine, wherein the copolymer-1 composition has an average molecular weight of 4 to 9 kDa. 16. The process of claim 15, wherein the copolymer-1 composition has an average molecular weight of 6.25 to 8.4 kilodaltons. 17. A copolymer-1 composition having an average molecular weight of about 4 to about 8.6 kDa preparable by a process comprising: polymerizing a mixture of an N-carboxyanhydride of tyrosine, an N-carboxyanhydride of alanine, .gamma.-benzyl glutamate and trifluoroacetyllysine in a molar ratio of 1:5:2:4 to form a mixture of protected polypeptides; deprotecting the protected polypeptides to form a mixture of unprotected polypeptides; and isolating a mixture of unprotected polypeptides composed of glutamic acid, lysine, alanine and tyrosine, wherein the mixture has an average molecular weight of 4 to 9 kDa. 18. The composition of claim 17, wherein the mixture has an average molecular weight of 6.25 to 8.4 kilodaltons. 19. A copolymer-1 composition comprising a mixture of polypeptides composed of glutamic acid, lysine, alanine and tyrosine, wherein the mixture has an average molecular weight of 4 to about 8.6 kilodaltons, wherein the mixture of polypeptides is non-uniform with respect to molecular weight and sequence, and wherein the composition exhibits lower toxicity than a copolymer-1 composition having an average molecular weight greater than about 8.6 kilodaltons. 20. The composition of claim 19, wherein the mixture has an average molecular weight of 6.25 to 8.4 kilodaltons.