Monomeric analogues of human insulin

• US 6,800,606 B1
• Filed: 03/08/2002
• Issued: 10/05/2004
• Est. Priority Date: 09/08/1999
• Status: Expired due to Fees

• Current Assignee: Shanghai Institute of Biochemistry
• Original Assignee: Shanghai Institute of Biochemistry
• Inventors: You-Min, Feng, Zhang, You-Shang
• Primary Examiner(s): Brumback, Brenda
• Assistant Examiner(s): Gupta, Anish
• Application Number:
  US10/070,568
• Time in Patent Office: 942 Days
• Field of Search: 514/2, 514/3, 530/303, 530/304, 530/305
• US Class Current: 514/6.1
• CPC Class Codes: A61K 38/00 Medicinal preparations containing peptides peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: C07K 14/62 Insulins

Abstract

Monomeric analogues of human insulin have a single substitution of the amino acid in 12^th, 16^th or the 26^th position of the B chain of human insulin and may also have a terminal deletion in the B chain.

Claims

1. A method for treating an individual having an insulin deficiency wherein said method comprises administering to the individual an insulin analogue wherein the Tyr at the 16^th or 26^th position of the B chain of human insulin is substituted by Ala, and said analogue has a deletion at either one or both of Phe at position 1, B1, or Thr at position 30, B30, of the B-chain of human insulin.

2. The method, according to claim 1, wherein, at the 26^th amino acid, the analogue is substituted by Ala.

3. The method, according to claim 2, wherein said analogue has a deletion of B30.

4. The method according to claim 1, wherein at the 16^th amino acid the analogue is substituted by Ala.

5. The method, according to claim 4, wherein said analogue has a deletion at B30.

6. A pharmaceutical composition comprising an insulin analogue wherein the Tyr at the 16^th or 26^th position of the B chain of human insulin is substituted by Ala, and said analogue has a deletion at either one or both of Phe at position 1, B1, or Thr at position 30, B30, of the B chain of human insulin wherein said composition further comprises a pharmaceutical carrier.

7. The pharmaceutical composition, according to claim 6, wherein at the 26^th amino acid, the analogue is substituted by Ala.

8. The pharmaceutical composition, according to claim 7, wherein said analogue has a deletion of B30.

9. The pharmaceutical composition, according to claim 6, wherein at the 16^th amino acid, the analogue is substituted by Ala.

10. The pharmaceutical composition, according to claim 9, wherein said analogue has a deletion at B30.