# US 12,215,133 B2 · GIP and GLP-1 dual receptor agonist, pharmaceutical composition, and use > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 12,215,133 B2 - Document ID: US12215133B2 - Status: Granted - Kind: B2 - Application number: 18/540,219 - Filed: 2023-12-14 - Published: 2024-05-09 - Granted: 2025-02-04 - Earliest claimed: 2021-03-25 - Assignees: BrightGene Bio-Medical Technology Co., Ltd.; Brightgene Pharmaceutical (Suzhou) Co. Ltd. - Applicants: BrightGene Bio-Medical Technology Co., Ltd.; Brightgene Pharmaceutical (Suzhou) Co. Ltd. - Inventors: Jiandong Yuan; Yunsong Song; Wenteng Zhen; Yue Cai; Jianing Gu; Yangqing Huang - Web page: https://patentgrep.com/patent/US12215133B2 ## CPC - C07K 14/605: Glucagons - A61K 38/26: Glucagons - A61P 3/10: for hyperglycaemia, e.g. antidiabetics - 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) - 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) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract A GIP and GLP-1 dual receptor agonist, a pharmaceutical composition, and the use. In particular, the present application relates to a compound represented by formula I, a pharmaceutical composition comprising the compound, and the use of the compound as a GIP and GLP-1 dual receptor agonist in the field of medicine. The compound represented by formula I exhibits excellent GIPR and GLP-1R agonist activity and excellent pharmaceutical activity in reducing blood sugar and controlling body weight, is a therapeutic drug having a clinical application prospect, and can be used for preventing and treating diseases such as diabetes, diabetes complications, obesity, or obesity complications. ## Claims ### Claim 1 A compound represented by any one of the following formulas I-3 or I-4 or a pharmaceutically acceptable salt, ester, optical isomer, tautomer, isotopically labeled compound or prodrug thereof: ### Claim 2 A GIP and GLP-1 dual receptor agonist, wherein, the GIP and GLP-1 dual receptor agonist is a compound represented by formula I-3 or a pharmaceutically acceptable salt, ester, optical isomer, tautomer, isotopically labeled compound or prodrug thereof: ### Claim 3 (depends on 1) A pharmaceutical composition comprising the compound or the pharmaceutically acceptable salt, ester, optical isomer, tautomer, isotopically labeled compound or prodrug thereof according to claim 1; wherein the pharmaceutical composition further comprises one or more pharmaceutically acceptable carriers. ### Claim 4 (depends on 1) A method for preventing and/or treating diseases associated with metabolic disorders, comprising administering a prophylactically and/or therapeutically effective amount of the compound or the pharmaceutically acceptable salt, ester, optical isomer, tautomer, isotopically labeled compound or prodrug thereof according to claim 1 to a subject; wherein the diseases associated with metabolic disorders are diabetes or obesity. ### Claim 5 (depends on 2) A pharmaceutical composition comprising the GIP and GLP-1 dual receptor agonist according to claim 2; wherein the pharmaceutical composition further comprises one or more pharmaceutically acceptable carriers. ### Claim 6 (depends on 2) A method for preventing and/or treating diseases associated with metabolic disorders, comprising administering a prophylactically and/or therapeutically effective amount of the GIP and GLP-1 dual receptor agonist according to claim 2 to a subject; wherein the diseases associated with metabolic disorders are diabetes or obesity. ### Claim 7 (depends on 3) A method for preventing and/or treating diseases associated with metabolic disorders, comprising administering a prophylactically and/or therapeutically effective amount of the pharmaceutical composition according to claim 3 to a subject; wherein the diseases associated with metabolic disorders are diabetes or obesity. ### Claim 8 (depends on 5) A method for preventing and/or treating diseases associated with metabolic disorders, comprising administering a prophylactically and/or therapeutically effective amount of the pharmaceutical composition according to claim 5 to a subject; wherein the diseases associated with metabolic disorders are diabetes or obesity.