IL320810A - Glucagon-like peptide 1 agonists - Google Patents
Glucagon-like peptide 1 agonistsInfo
- Publication number
- IL320810A IL320810A IL320810A IL32081025A IL320810A IL 320810 A IL320810 A IL 320810A IL 320810 A IL320810 A IL 320810A IL 32081025 A IL32081025 A IL 32081025A IL 320810 A IL320810 A IL 320810A
- Authority
- IL
- Israel
- Prior art keywords
- methoxy
- oxetan
- methyl
- carboxylic acid
- ylmethyl
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
-
- 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
- A61P3/08—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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (9)
1. A compound of the formula: wherein is phenyl, a 5 or 6-membered heteroaryl or pyridone, which phenyl, heteroaryl or pyridone is optionally substituted with one or two R; R at each occurrence is independently CN, halo, C1-C3alkyl, C1-C3alkoxy, -C(O)NH2 or 5-membered heteroaryl; R at each occurrence is independently halo or methyl; R is C1-C4alkoxy optionally substituted with C1-C2alkoxy; or a pharmaceutically acceptable salt thereof.
2. The compound according to claim 1, which is of the formula: wherein R is F or OCH3; R is F or CH3; and R is -OCH3, or -OCH2CH2OCH3, or a pharmaceutically acceptable salt thereof.
3. The compound according to claim 1, which is selected from: 2-[[4-[6-[(4-Cyano-2-fluoro-phenyl)methoxy]-2-pyridyl]-2-fluoro-5-methyl- phenyl]methyl]-7-methoxy-3-[[oxetan-2-yl]methyl]benzimidazole-5-carboxylic acid; 2-(4-(6-((4-Cyano-2-fluorobenzyl)oxy)pyridin-2-yl)-2,5-difluorobenzyl)-4-methoxy-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid; 30435_OUS -44- 2-(4-(6-((5-Cyanopyridin-2-yl)methoxy)pyridin-2-yl)-2,5-difluorobenzyl)-4-methoxy-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid; 2-(4-(6-((6-Cyanopyridin-3-yl)methoxy)pyridin-2-yl)-2,5-difluorobenzyl)-4-methoxy-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid; 2-(4-(6-((4-Cyano-2-fluorobenzyl)oxy)pyridin-2-yl)-2,5-difluorobenzyl)-4-(2- methoxyethoxy)-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid; 2-[[4-[6-[(6-Cyano-2-methyl-3-pyridyl)methoxy]-2-pyridyl]-2,5-difluoro-phenyl]methyl]-7-methoxy-3-[[oxetan-2-yl]methyl]benzimidazole-5-carboxylic acid; 2-[[4-[6-[(6-carbamoyl-2-methyl-3-pyridyl)methoxy]-2-pyridyl]-2,5-difluoro-phenyl]methyl]-7-methoxy-3-[[oxetan-2-yl]methyl]benzimidazole-5-carboxylic acid; 2-[[2,5-Difluoro-4-[6-[(1-methyl-6-oxo-3-pyridyl)methoxy]-2-pyridyl]phenyl]methyl]-7-(2-methoxyethoxy)-3-[[oxetan-2-yl]methyl]benzimidazole-5-carboxylic acid; 2-(4-(6-((5-cyanothiophen-2-yl)methoxy)pyridin-2-yl)-2,5-difluorobenzyl)-4-methoxy-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid; 2-(4-(6-((4-cyano-2-methylbenzyl)oxy)pyridin-2-yl)-2,5-difluorobenzyl)-4-methoxy-1- (oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid; 2-(2,5-difluoro-4-(6-((2-methyl-2H-1,2,3-triazol-4-yl)methoxy)pyridin-2-yl)benzyl)-4-methoxy-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid; 2-(4-(6-((4-(1H-1,2,4-triazol-1-yl)benzyl)oxy)pyridin-2-yl)-2,5-difluorobenzyl)-4-methoxy-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid; 2-(2,5-difluoro-4-(6-(isoxazol-3-ylmethoxy)pyridin-2-yl)benzyl)-4-methoxy-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid; 2-(4-(6-((4-cyano-2-methoxybenzyl)oxy)pyridin-2-yl)-2,5-difluorobenzyl)-4-methoxy-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid; 2-(2,5-difluoro-4-(6-((1-methyl-1H-pyrazol-3-yl)methoxy)pyridin-2-yl)benzyl)-4- methoxy-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid; 2-(2,5-difluoro-4-(6-((2-methyl-2H-tetrazol-5-yl)methoxy)pyridin-2-yl)benzyl)-4-methoxy-1-(oxetan-2-ylmethyl)-1H-benzo[d]imidazole-6-carboxylic acid; or a pharmaceutically acceptable salt thereof. 30435_OUS -45-
4. A pharmaceutical composition comprising a compound, or a pharmaceutically acceptable salt thereof, according to any one of claims 1 to 3 and at least one pharmaceutically acceptable carrier, diluent, or excipient.
5. A compound, or a pharmaceutically acceptable salt thereof, according to any one of claims 1 to 3 for use in therapy.
6. A compound, or a pharmaceutically acceptable salt thereof, according to any one of claims 1 to 3 for use in the treatment of type II diabetes mellitus.
7. A compound, or a pharmaceutically acceptable salt thereof, according to any one of claims 1 to 3 for use in lowering blood glucose levels.
8. A compound, or a pharmaceutically acceptable salt thereof, according to any one of claims 1 to 3 for use in the treatment of hyperglycemia.
9. A compound, or a pharmaceutically acceptable salt thereof, according to any one of claims 1 to 3 for use in the treatment of obesity.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202263425751P | 2022-11-16 | 2022-11-16 | |
| PCT/US2023/079720 WO2024107781A1 (en) | 2022-11-16 | 2023-11-15 | Glucagon-like peptide 1 receptor agonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL320810A true IL320810A (en) | 2025-07-01 |
Family
ID=89378473
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL320810A IL320810A (en) | 2022-11-16 | 2023-11-15 | Glucagon-like peptide 1 agonists |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP4619098A1 (en) |
| JP (1) | JP2025538389A (en) |
| KR (1) | KR20250085816A (en) |
| CN (1) | CN120344520A (en) |
| AU (1) | AU2023379473A1 (en) |
| CL (1) | CL2025001423A1 (en) |
| CO (1) | CO2025005958A2 (en) |
| CR (1) | CR20250178A (en) |
| DO (1) | DOP2025000110A (en) |
| IL (1) | IL320810A (en) |
| JO (1) | JOP20250110A1 (en) |
| MX (1) | MX2025005718A (en) |
| WO (1) | WO2024107781A1 (en) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FI4408840T3 (en) | 2021-09-27 | 2025-11-04 | Terns Pharmaceuticals Inc | BENZIMIDAZOLE CARBOXYLIC ACIDS AS GLP-1R AGONISTS |
| IL312364A (en) | 2021-10-25 | 2024-06-01 | Luehr Gary W | Compounds as glp-1r agonists |
| US12410163B2 (en) | 2022-02-23 | 2025-09-09 | Terns Pharmaceuticals, Inc. | Compounds as GLP-IR agonists |
| WO2024211898A1 (en) | 2023-04-07 | 2024-10-10 | Terns Pharmaceuticals, Inc. | Combination comprising a thrbeta agonist anda glp-1r agonist for use in treating a liver disorder or a cardiometabolic disease |
| AU2024340407A1 (en) | 2023-09-14 | 2026-04-23 | Ascletis Pharma (China) Co., Limited | Glp-1r agonist and therapeutic method thereof |
| WO2025109387A1 (en) | 2023-11-24 | 2025-05-30 | Ascletis Pharma (China) Co., Limited | Glp-1r agonist and therapeutic method thereof |
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| SG11202011704XA (en) | 2018-06-15 | 2020-12-30 | Pfizer | Glp-1 receptor agonists and uses thereof |
| CU20210042A7 (en) | 2018-11-22 | 2022-01-13 | Qilu Regor Therapeutics Inc | Glp-1r agonists |
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| TWI751585B (en) | 2019-06-28 | 2022-01-01 | 美商美國禮來大藥廠 | Glucagon-like peptide 1 receptor agonists |
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-
2023
- 2023-11-15 EP EP23828849.2A patent/EP4619098A1/en active Pending
- 2023-11-15 KR KR1020257015415A patent/KR20250085816A/en active Pending
- 2023-11-15 CR CR20250178A patent/CR20250178A/en unknown
- 2023-11-15 AU AU2023379473A patent/AU2023379473A1/en active Pending
- 2023-11-15 JP JP2025528178A patent/JP2025538389A/en active Pending
- 2023-11-15 CN CN202380079819.9A patent/CN120344520A/en active Pending
- 2023-11-15 IL IL320810A patent/IL320810A/en unknown
- 2023-11-15 WO PCT/US2023/079720 patent/WO2024107781A1/en not_active Ceased
-
2025
- 2025-05-08 CO CONC2025/0005958A patent/CO2025005958A2/en unknown
- 2025-05-13 CL CL2025001423A patent/CL2025001423A1/en unknown
- 2025-05-13 JO JOJO/P/2025/0110A patent/JOP20250110A1/en unknown
- 2025-05-14 DO DO2025000110A patent/DOP2025000110A/en unknown
- 2025-05-15 MX MX2025005718A patent/MX2025005718A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| MX2025005718A (en) | 2025-06-02 |
| EP4619098A1 (en) | 2025-09-24 |
| JP2025538389A (en) | 2025-11-28 |
| WO2024107781A1 (en) | 2024-05-23 |
| AU2023379473A1 (en) | 2025-05-15 |
| CL2025001423A1 (en) | 2025-08-08 |
| DOP2025000110A (en) | 2025-06-15 |
| JOP20250110A1 (en) | 2025-05-13 |
| CR20250178A (en) | 2025-06-06 |
| CN120344520A (en) | 2025-07-18 |
| KR20250085816A (en) | 2025-06-12 |
| CO2025005958A2 (en) | 2025-05-29 |
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