# US 8,772,232 B2 · Protracted exendin-4 compounds > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,772,232 B2 - Document ID: US8772232B2 - Status: Granted - Kind: B2 - Application number: 13/212,439 - Filed: 2011-08-18 - Published: 2011-12-08 - Granted: 2014-07-08 - Earliest claimed: 2004-10-07 - Assignees: Novo Nordisk A/S - Applicants: Jesper Lau; Thomas Kruse Hansen - Inventors: Jesper Lau; Thomas Kruse Hansen - Web page: https://patentgrep.com/patent/US8772232B2 ## CPC - C07K 14/57563: {Vasoactive intestinal peptide [VIP]; Related peptides} - A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants - A61P 1/14: Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents - A61P 3/04: Anorexiants; Antiobesity agents - A61P 3/06: Antihyperlipidemics - A61P 3/10: for hyperglycaemia, e.g. antidiabetics - A61P 5/50: for increasing or potentiating the activity of insulin - A61P 9/00: Drugs for disorders of the cardiovascular system - A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis - A61P 9/12: Antihypertensives - 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) - C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) ## Abstract Novel protracted exendin-4 compounds and therapeutic uses thereof. ## Claims ### Claim 1 A derivative of an exendin-4 (1-39)amide comprising an exendin-4 (1-39)amide comprising an amino acid sequence having no more than ten amino acid residues which have been exchanged, added or deleted as compared to SEQ ID NO: 1 wherein the derivative is substituted at position 32 with a lysine residue that is acylated with a diacid. ### Claim 2 (depends on 1) A derivative according to claim 1, wherein said diacid is a dicarboxylic acid. ### Claim 3 (depends on 1) A derivative according claim 1, wherein said diacid is a straight-chain or branched alkane α,ω-dicarboxylic acid. ### Claim 4 (depends on 1) A derivative according to claim 1, wherein said diacid has the structure HOOC—(CH2)nCO—, wherein n is 12 to 20. ### Claim 5 (depends on 1) A derivative according to claim 1, wherein said diacid has a structure selected from HOOC—(CH2)14CO—, HOOC—(CH2)15CO—, HOOC—(CH2)16CO—, HOOC—(CH2)17CO—, and HOOC—(CH2)18CO—. ### Claim 6 (depends on 1) A derivative according to claim 1, wherein said diacid has the structure HOOC—(CH2)16CO—. ### Claim 7 (depends on 1) A derivative according to claim 1, wherein said derivative comprises no more than six amino acid residues which have been exchanged, added or deleted as compared to exendin-4(1-39) (SEQ ID No: 1). ### Claim 8 (depends on 1) A derivative according to claim 1, wherein said derivative comprises no more than 4 amino acid residues which are not encoded by the genetic code. ### Claim 9 (depends on 1) A derivative according to claim 1, wherein said derivative comprises only one lysine residue. ### Claim 10 (depends on 1) A derivative according to claim 1, which is N-epsilon32-(17-carboxy-heptadecanoyl)[Lys32]exendin-4(1-39)amide or N-epsilon32-(17-carboxy-heptadecanoyl)[Lys32]exendin-4(1-39)amide or Arg12,27 NLe14, lys32 N-epsilon32-(17-carboxy-heptadecanoyl)[Lys32]exendin-4(1-9)amide ### Claim 11 (depends on 1) A pharmaceutical composition comprising a derivative according to claim 1, and a pharmaceutically acceptable excipient. ### Claim 12 (depends on 10) A pharmaceutical composition comprising a derivative according to claim 10, and a pharmaceutically acceptable excipient. ### Claim 13 (depends on 11) A method for treating type 2 diabetes, said method comprising administering to a subject in need of such treatment an effective amount of a pharmaceutical composition according to claim 11. ### Claim 14 (depends on 12) A method for treating type 2 diabetes, said method comprising administering to a subject in need of such treatment an effective amount of a pharmaceutical composition according to claim 12.