GLP-1 ANALOG USEFUL FOR TREATING DIABETES

• Main Authors: MALLORY JOANNE B, MOJSOV SVETLANA, HABENER JOEL F, BUCKLEY DOUGLAS I
• Format: Patent
• Language: English
• Published: 05.06.2001
• Edition: 7
• Subjects: CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PEPTIDES; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PROBLEM TO BE SOLVED: To solve problems that a conventional GLP-1 peptide analog has a short circulation half-life and it is not clear by what effects on characteristics an improvement in effectiveness is obtained. SOLUTION: Effective analogs of active GLP-1 peptides 7-34, 7-35, 7-36 and 7-37 having an improved characteristic for treatment of type II diabetes are obtained to solve the problems. The analogs contain an amino acid substituted at the 7-10 positions and the cleaved C-terminal and/or various other amino acid substitutions in the basic peptide and is improved in ability to stimulate the insulin production as compared with glucagon and capable of improving the stability in plasmas as compared with the GLP-1 (7-37) or both. The ability of the analogs as a therapeutic agent is improved by the characteristic. Analogs having a D-form amino acid substitution at the 7- and the 8-positions and/or an N-alkylated or an N-acylated amino acid at the 7-position are especially resistant to degradation in vivo.