Copolymer-1 improvements on compositions of copolymers

• US 6,362,161 B1
• Filed: 02/22/2000
• Issued: 03/26/2002
• Est. Priority Date: 05/24/1994
• Status: Expired due to Term

• Current Assignee: Yeda Research and Development Co. Ltd. (Weizmann Institute of Science)
• Original Assignee: Yeda Research and Development Co. Ltd. (Weizmann Institute of Science)
• Inventors: Arnon, Ruth, Sela, Michael, Teitelbaum, Dvora, Konfino, Eliezer
• Primary Examiner(s): KRASS, FREDERICK F
• Application Number:
  US09/510,466
• Time in Patent Office: 763 Days
• Field of Search: 514/2, 514/12, 514/903, 424/78.37
• US Class Current: 514/17.9
• CPC Class Codes: A61K 38/1703 from vertebrates
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07K 14/4713 Autoimmune diseases, e.g. Insulin-dependent diabetes mellitus, multiple sclerosis, rheumathoid arthritis, systemic lupus erythematosus; Autoantigens
• CPC Class Codes: C08G 69/10 Alpha-amino-carboxylic acids polysuccinimides C08G73/1092

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.

Claims

1. A composition for the treatment of multiple sclerosis comprising a pharmaceutically effective amount of a copolymer-1 fraction, wherein said fraction contains less than 5% of species of copolymer-1 having a molecular weight of over 40 kilodaltons;

and wherein over 75% of said copolymer-1 in said fraction is within a molecular weight range of about 2 kilodaltons to about 20 kilodaltons, wherein said copolymer-1 fraction is prepared by a process comprising the steps of;

reacting protected copolymer-1 with hydrobromic acid to form trifluoroacetyl copolymer-1 having over 75% of its molar fraction within the molecular weight range from about 2 kDa to about 20 kDa, wherein said reaction takes place for a time and at a temperature predetermined by test reaction, and

treating said trifluoroacetyl copolymer-1 having over 75% of its molar fraction within the molecular weight range from about 2 kDa to about 20 kDa with aqueous piperidine solution to form copolymer-1 having over 75% of its molar fraction within the molecular weight range from about 2 kDa to about 20 kDa.