NZ765268B2 - Incretin analogs and uses thereof - Google Patents
Incretin analogs and uses thereof Download PDFInfo
- Publication number
- NZ765268B2 NZ765268B2 NZ765268A NZ76526818A NZ765268B2 NZ 765268 B2 NZ765268 B2 NZ 765268B2 NZ 765268 A NZ765268 A NZ 765268A NZ 76526818 A NZ76526818 A NZ 76526818A NZ 765268 B2 NZ765268 B2 NZ 765268B2
- Authority
- NZ
- New Zealand
- Prior art keywords
- incretin analog
- incretin
- analog
- amef
- ethoxy
- Prior art date
Links
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/26—Glucagons
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/605—Glucagons
Abstract
Incretin analogs are provided that have activity at each of the GIP, GLP-1 and glucagon receptors. The incretin analogs have structural features resulting in balanced activity and extended duration of action at each of these receptors. In particular, residue X17 is a K residue with a side chain of (2-[2-(2-amino-ethoxy)-ethoxy]-acetyl)a-(?Glu)b-CO-(CH2)c-CO2H. Methods also are provided for treating diseases such as diabetes mellitus, dyslipidemia, fatty liver disease, metabolic syndrome, non-alcoholic steatohepatitis and obesity.
Claims (19)
1. An incretin analog comprising: 5 YX X GTX TSDYSIX LDKX AQX AFIEYLLEGGPSSGAPPPS, 2 3 6 13 17 20 wherein: X is Aib, X is Q or H, X is aMeF or aMeF(2F), 10 X is L or aMeL, X is K chemically modified through conjugation to an epsilon-amino group of a K side-chain with the following structure: (2-[2-(2-amino-ethoxy)-ethoxy]-acetyl) -(?Glu) -CO-(CH ) -CO H, a b 2 c 2 wherein a is 0, 1 or 2; b is 1 or 2; and c is an integer between 16 to 18, 15 X is Aib, Q or H, and the C-terminal amino acid is optionally amidated; or a pharmaceutically acceptable salt thereof.
2. The incretin analog of Claim 1, wherein a is 1.
3. The incretin analog of Claim 1, wherein a is 2.
4. The incretin analog of any one of Claims 1 to 3, wherein b is 1. 25
5. The incretin analog of any one of Claims 1 to 3, wherein b is 2.
6. The incretin analog of any one of Claims 1 to 5, wherein c is 18.
7. The incretin analog of any one of Claims 1 to 6, wherein X is aMeL.
8. The incretin analog of any one of Claims 1 to 6, wherein X is L.
9. The incretin analog of any one of Claims 1 to 8, wherein X is Q.
10. The incretin analog of any one of Claims 1 to 8, wherein X is H. 5
11. The incretin analog of any one of Claims 1 to 10, wherein X is aMeF.
12. The incretin analog of any one of Claims 1 to 10 wherein X is aMeF(2F).
13. An incretin analog having a formula selected from the group consisting of SEQ ID 10 NOS:6-11.
14. A pharmaceutical composition comprising: an incretin analog of any one of Claims 1 to 13; and a pharmaceutically acceptable carrier, diluent, or excipient.
15. Use of an incretin analog of any one of Claims 1 to 13 in the manufacture of a medicament for treating a disease selected from the group consisting of diabetes mellitus, dyslipidemia, fatty liver disease, metabolic syndrome, non-alcoholic steatohepatitis and obesity.
16. Use of an incretin analog of any one of Claims 1 to 13 in the manufacture of a medicament for treating type II diabetes mellitus.
17. An incretin analog of any one of Claims 1 to 13 substantially as herein described 25 with reference to any example thereof.
18. A pharmaceutical composition of Claim 14 substantially as herein described with reference to any example thereof. 30
19. Use of claim 15 or 16 substantially as herein described with reference to any example thereof.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762608644P | 2017-12-21 | 2017-12-21 | |
| PCT/US2018/065605 WO2019125929A1 (en) | 2017-12-21 | 2018-12-14 | Incretin analogs and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NZ765268A NZ765268A (en) | 2024-07-05 |
| NZ765268B2 true NZ765268B2 (en) | 2024-10-08 |
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