PE20231309A1 - Agonistas duales glp-1/gip - Google Patents
Agonistas duales glp-1/gipInfo
- Publication number
- PE20231309A1 PE20231309A1 PE2023000804A PE2023000804A PE20231309A1 PE 20231309 A1 PE20231309 A1 PE 20231309A1 PE 2023000804 A PE2023000804 A PE 2023000804A PE 2023000804 A PE2023000804 A PE 2023000804A PE 20231309 A1 PE20231309 A1 PE 20231309A1
- Authority
- PE
- Peru
- Prior art keywords
- lys
- absent
- aib
- polypeptide
- gln
- Prior art date
Links
- 239000000556 agonist Substances 0.000 title abstract 2
- 230000009977 dual effect Effects 0.000 title abstract 2
- 102100025101 GATA-type zinc finger protein 1 Human genes 0.000 title 1
- 101710198884 GATA-type zinc finger protein 1 Proteins 0.000 title 1
- DTHNMHAUYICORS-KTKZVXAJSA-N Glucagon-like peptide 1 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 title 1
- 229920001184 polypeptide Polymers 0.000 abstract 3
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 3
- 102000004196 processed proteins & peptides Human genes 0.000 abstract 3
- 239000003626 gastrointestinal polypeptide Substances 0.000 abstract 2
- FUOOLUPWFVMBKG-UHFFFAOYSA-N 2-Aminoisobutyric acid Chemical group CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 abstract 1
- 125000001433 C-terminal amino-acid group Chemical group 0.000 abstract 1
- SNDPXSYFESPGGJ-SCSAIBSYSA-N D-2-aminopentanoic acid Chemical group CCC[C@@H](N)C(O)=O SNDPXSYFESPGGJ-SCSAIBSYSA-N 0.000 abstract 1
- 101000886868 Homo sapiens Gastric inhibitory polypeptide Proteins 0.000 abstract 1
- SNDPXSYFESPGGJ-BYPYZUCNSA-N L-2-aminopentanoic acid Chemical group CCC[C@H](N)C(O)=O SNDPXSYFESPGGJ-BYPYZUCNSA-N 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 150000001413 amino acids Chemical group 0.000 abstract 1
- 210000004899 c-terminal region Anatomy 0.000 abstract 1
- 125000002843 carboxylic acid group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 201000001421 hyperglycemia Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- GCYXWQUSHADNBF-AAEALURTSA-N preproglucagon 78-108 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 GCYXWQUSHADNBF-AAEALURTSA-N 0.000 abstract 1
- 150000003140 primary amides Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
-
- 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
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K4/00—Peptides having up to 20 amino acids in an undefined or only partially defined sequence; Derivatives thereof
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Diabetes (AREA)
- Engineering & Computer Science (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- General Chemical & Material Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Toxicology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Theoretical Computer Science (AREA)
- Physics & Mathematics (AREA)
- General Physics & Mathematics (AREA)
- Software Systems (AREA)
- Sewing Machines And Sewing (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Data Mining & Analysis (AREA)
Abstract
Referido a un polipeptido o una sal farmaceuticamente aceptable de este que comprende la secuencia de aminoacidos: Y-X1-E-G-T-F-T-S-D-Y-S-I-X2-L-Xaa15-K-I-A-Xaa19-X3-Xaa21-F-V-Xaa24-W-L-X4-A-G-G-P-S-S-G-A-P-P-P-S-X5-X6-X7-X8-X9-X10-X11 (Seq. ID 1); en donde X1 es Aib, (L)-norvalina o (D)-norvalina; X2 se selecciona de Aib, Leu, (D)-Leu, Val, entre otros; X3 es Gln o Lys; X4 es Leu, Ile o Glu; X5 esta ausente, Arg o Lys; X6 esta ausente o es Lys; X7 esta ausente o es Lys; X8 esta ausente o es Lys; X9 esta ausente o es Lys; X10 esta ausente o es Lys; X11 esta ausente o es Lys; Xaa15 es Asp o Glu; Xaa19 es Gln o Ala; Xaa21 es Ala o Glu; Xaa24 es Gln o Asn; en donde el grupo acido del aminoacido del extremo C es un grupo acido carboxilico libre o esta amidado como una amida primaria del extremo C y al menos uno de X3 y X5 es Lys; y siempre que cuando X1 es Aib, X2 no es Aib. Este polipeptido es de accion prolongada dual, agonista del peptido 1 similar al glucagon (GLP-1) y del polipeptido insulinotropico dependiente de la glucosa humano/ peptido gastrointestinal (GIP). Tambien se refiere a metodos de preparacion de dicho polipeptido, una composicion farmaceutica y su uso en el tratamiento de enfermedades tales como hiperglucemia, diabetes tipo 2, obesidad, entre otros.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN202021045240 | 2020-10-17 | ||
| IN202121002837 | 2021-01-20 | ||
| PCT/IB2021/059420 WO2022079639A1 (en) | 2020-10-17 | 2021-10-13 | Glp-1/gip dual agonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20231309A1 true PE20231309A1 (es) | 2023-08-24 |
Family
ID=78302859
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2023000804A PE20231309A1 (es) | 2020-10-17 | 2021-10-13 | Agonistas duales glp-1/gip |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US20240020543A1 (es) |
| EP (1) | EP4204440A1 (es) |
| JP (1) | JP2023545662A (es) |
| KR (1) | KR20230088337A (es) |
| CN (1) | CN116171164A (es) |
| AU (1) | AU2021361263A1 (es) |
| BR (1) | BR112023003668A2 (es) |
| CA (1) | CA3195155A1 (es) |
| CL (1) | CL2023000960A1 (es) |
| CO (1) | CO2023001960A2 (es) |
| IL (1) | IL301109A (es) |
| MX (1) | MX2023002906A (es) |
| PE (1) | PE20231309A1 (es) |
| TW (1) | TW202229323A (es) |
| WO (1) | WO2022079639A1 (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2022159395A1 (en) | 2021-01-20 | 2022-07-28 | Viking Therapeutics, Inc. | Compositions and methods for the treatment of metabolic and liver disorders |
| CR20230530A (es) | 2021-05-13 | 2024-02-19 | Carmot Therapeutics Inc | Moduladores de los receptores acoplados a proteínas g. |
| EP4259647A4 (en) | 2021-09-15 | 2025-03-26 | Viking Therapeutics, Inc. | COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC AND LIVER DISEASES |
| AU2023305663A1 (en) * | 2022-07-13 | 2025-02-20 | Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. | Glp-1/gip dual agonist, and preparation method therefor and use thereof |
| IL318334A (en) * | 2022-07-20 | 2025-03-01 | Viking Therapeutics Inc | Pharmaceutical formulations and methods for treating metabolic and liver disorders |
| CN117756913B (zh) * | 2022-11-07 | 2025-05-09 | 内蒙古博睿精创科技有限公司 | 一种新型长效多肽化合物、组合物及其应用 |
| CN115651075B (zh) * | 2022-12-12 | 2023-04-11 | 杭州信海医药科技有限公司 | 一种Tirzepatide的合成方法 |
| WO2024152259A1 (zh) * | 2023-01-18 | 2024-07-25 | 上海民为生物技术有限公司 | 具有三重活性的融合蛋白及其应用 |
| WO2024165571A2 (en) | 2023-02-06 | 2024-08-15 | E-Therapeutics Plc | Inhibitors of expression and/or function |
| CN121398835A (zh) * | 2023-05-21 | 2026-01-23 | 卡莫特治疗学股份有限公司 | 患有或未患有体重相关合并症的超重或肥胖成年人的治疗 |
| CN121285571A (zh) | 2023-06-09 | 2026-01-06 | 太阳医药工业有限公司 | Glp-1/gip双重、glp-1/gcg双重和glp-1/gip/gcg三重受体激动剂 |
| CN116693652B (zh) * | 2023-08-02 | 2024-01-05 | 北京惠之衡生物科技有限公司 | 一种glp-1/gip受体双重激动剂衍生物及其制备方法和应用 |
| WO2025125576A2 (en) | 2023-12-15 | 2025-06-19 | E-Therapeutics Plc | Inhibitors of expression and/or function |
| EP4686757A1 (en) | 2024-07-31 | 2026-02-04 | e-therapeutics PLC | Inhibitors of expression and/or function |
| WO2025133348A1 (en) | 2023-12-22 | 2025-06-26 | E-Therapeutics Plc | Inhibitors of expression and/or function |
| TW202535911A (zh) * | 2024-01-12 | 2025-09-16 | 大陸商杭州中美華東製藥有限公司 | 長效glp-1/gip雙激動劑的藥物組合物 |
| WO2025163615A1 (en) | 2024-01-31 | 2025-08-07 | Sun Pharmaceutical Industries Ltd. | High level production of glp1 analogues |
| WO2025196502A1 (en) | 2024-03-20 | 2025-09-25 | North Carolina Agricultural & Technical State University | Choline kinase inhibitors as a therapeutic treatment for obesity |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2504521T3 (es) * | 2006-03-03 | 2014-10-08 | California Institute Of Technology | Incorporación específica del sitio de aminoácidos en moléculas |
| EA028665B1 (ru) | 2012-05-03 | 2017-12-29 | Зилэнд Фарма А/С | Соединения - двойные агонисты gip-glp-1 и способы |
| EP2864351B1 (en) * | 2012-06-21 | 2016-08-10 | Indiana University Research and Technology Corporation | Glucagon analogs exhibiting gip receptor activity |
| US10093713B2 (en) | 2013-11-06 | 2018-10-09 | Zealand Pharma A/S | GIP-GLP-1 dual agonist compounds and methods |
| JOP20200119A1 (ar) * | 2015-01-09 | 2017-06-16 | Lilly Co Eli | مركبات مساعد مشترك من gip وglp-1 |
| TWI622596B (zh) | 2015-10-26 | 2018-05-01 | 美國禮來大藥廠 | 升糖素受體促效劑 |
| PL4122954T3 (pl) * | 2018-04-05 | 2024-08-12 | Sun Pharmaceutical Industries Limited | Nowe analogi GLP-1 |
| TWI705820B (zh) * | 2018-06-22 | 2020-10-01 | 美商美國禮來大藥廠 | Gip/glp1促效劑組合物 |
| KR20210031533A (ko) | 2018-07-23 | 2021-03-19 | 일라이 릴리 앤드 캄파니 | Gip/glp1 공효능제 화합물 |
| EP3826662B9 (en) * | 2018-07-23 | 2025-02-19 | Eli Lilly and Company | Method of using a gip/glp1 co-agonist for diabetes |
| TW202216746A (zh) * | 2020-06-22 | 2022-05-01 | 印度商太陽製藥工業有限公司 | 長效型ｇｌｐ－１／ｇｉｐ雙重促效劑 |
-
2021
- 2021-10-13 AU AU2021361263A patent/AU2021361263A1/en active Pending
- 2021-10-13 JP JP2023519770A patent/JP2023545662A/ja active Pending
- 2021-10-13 PE PE2023000804A patent/PE20231309A1/es unknown
- 2021-10-13 CA CA3195155A patent/CA3195155A1/en active Pending
- 2021-10-13 MX MX2023002906A patent/MX2023002906A/es unknown
- 2021-10-13 IL IL301109A patent/IL301109A/en unknown
- 2021-10-13 WO PCT/IB2021/059420 patent/WO2022079639A1/en not_active Ceased
- 2021-10-13 US US18/249,055 patent/US20240020543A1/en active Pending
- 2021-10-13 TW TW110137941A patent/TW202229323A/zh unknown
- 2021-10-13 EP EP21795004.7A patent/EP4204440A1/en active Pending
- 2021-10-13 BR BR112023003668A patent/BR112023003668A2/pt unknown
- 2021-10-13 CN CN202180051573.5A patent/CN116171164A/zh active Pending
- 2021-10-13 KR KR1020237006545A patent/KR20230088337A/ko active Pending
-
2023
- 2023-02-22 CO CONC2023/0001960A patent/CO2023001960A2/es unknown
- 2023-03-31 CL CL2023000960A patent/CL2023000960A1/es unknown
-
2024
- 2024-08-22 US US18/812,797 patent/US20240400613A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| AU2021361263A1 (en) | 2023-02-16 |
| KR20230088337A (ko) | 2023-06-19 |
| CN116171164A (zh) | 2023-05-26 |
| CA3195155A1 (en) | 2022-04-21 |
| US20240020543A1 (en) | 2024-01-18 |
| TW202229323A (zh) | 2022-08-01 |
| MX2023002906A (es) | 2023-04-05 |
| US20240400613A1 (en) | 2024-12-05 |
| BR112023003668A2 (pt) | 2023-04-25 |
| CL2023000960A1 (es) | 2023-11-10 |
| JP2023545662A (ja) | 2023-10-31 |
| CO2023001960A2 (es) | 2023-05-08 |
| EP4204440A1 (en) | 2023-07-05 |
| IL301109A (en) | 2023-05-01 |
| WO2022079639A1 (en) | 2022-04-21 |
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