CA3217720A1 - Benzimidazoyl glp-1 receptor agonists, pharmaceutical compositions comprising the same, and methods for their use - Google Patents
Benzimidazoyl glp-1 receptor agonists, pharmaceutical compositions comprising the same, and methods for their use Download PDFInfo
- Publication number
- CA3217720A1 CA3217720A1 CA3217720A CA3217720A CA3217720A1 CA 3217720 A1 CA3217720 A1 CA 3217720A1 CA 3217720 A CA3217720 A CA 3217720A CA 3217720 A CA3217720 A CA 3217720A CA 3217720 A1 CA3217720 A1 CA 3217720A1
- Authority
- CA
- Canada
- Prior art keywords
- methyl
- alkyl
- substituted
- compound
- certain embodiments
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic 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
- 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
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163183612P | 2021-05-03 | 2021-05-03 | |
| US63/183,612 | 2021-05-03 | ||
| US202163282686P | 2021-11-24 | 2021-11-24 | |
| US63/282,686 | 2021-11-24 | ||
| PCT/US2022/027535 WO2022235717A1 (en) | 2021-05-03 | 2022-05-03 | Benzimidazoyl glp-1 receptor agonists, pharmaceutical compositions comprising the same, and methods for their use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3217720A1 true CA3217720A1 (en) | 2022-11-10 |
Family
ID=81750835
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3217720A Pending CA3217720A1 (en) | 2021-05-03 | 2022-05-03 | Benzimidazoyl glp-1 receptor agonists, pharmaceutical compositions comprising the same, and methods for their use |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US20220396569A1 (https=) |
| EP (2) | EP4334304A1 (https=) |
| JP (1) | JP2024516291A (https=) |
| AU (1) | AU2022271223A1 (https=) |
| BR (1) | BR112023022836A2 (https=) |
| CA (1) | CA3217720A1 (https=) |
| MX (1) | MX2023012918A (https=) |
| WO (1) | WO2022235717A1 (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3192601A1 (en) * | 2020-08-21 | 2022-02-24 | Terns Pharmaceuticals, Inc. | Compounds as glp-1r agonists |
| WO2023029380A1 (zh) | 2021-08-30 | 2023-03-09 | 杭州德睿智药科技有限公司 | 作为glp1r激动剂的新型芳醚取代杂环类化合物 |
| PT4408840T (pt) | 2021-09-27 | 2025-10-07 | Terns Pharmaceuticals Inc | Ácidos benzimidazolocarboxílicos como agonistas de glp-1r |
| CN118401519A (zh) | 2021-10-25 | 2024-07-26 | 拓臻制药公司 | 作为glp-1r激动剂的化合物 |
| US20250042882A1 (en) | 2021-12-16 | 2025-02-06 | Astrazeneca Ab | Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators |
| WO2023111144A1 (en) | 2021-12-16 | 2023-06-22 | Astrazeneca Ab | Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators |
| CN119095843A (zh) | 2022-02-23 | 2024-12-06 | 拓臻制药公司 | 作为glp-1r激动剂的化合物 |
| CN117362282B (zh) * | 2022-07-07 | 2026-04-21 | 杭州德睿智药科技有限公司 | Glp-1r激动剂的盐及其制备方法和应用 |
| EP4562006A1 (en) * | 2022-07-27 | 2025-06-04 | Carmot Therapeutics, Inc. | N-heterocylic gpcr receptor agonists, pharmaceutical compositions comprising the same, and methods for their use |
| WO2024051700A1 (zh) * | 2022-09-05 | 2024-03-14 | 德睿智药(苏州)新药研发有限公司 | 作为glp1r激动剂的新型芳基氘代苄醚取代杂环类化合物 |
| EP4592285A1 (en) | 2022-09-22 | 2025-07-30 | Shionogi & Co., Ltd. | Fused ring compound having glp-1 receptor agonist effect |
| KR20250085816A (ko) | 2022-11-16 | 2025-06-12 | 일라이 릴리 앤드 캄파니 | 글루카곤-유사 펩티드 1 수용체 효능제 |
| CN116217522B (zh) * | 2023-02-22 | 2025-06-24 | 广东莱佛士制药技术有限公司 | Glp-1受体激动剂关键中间体的手性纯化方法 |
| EP4568664B1 (en) | 2023-04-07 | 2026-04-01 | Terns Pharmaceuticals, Inc. | Combination comprising a thr-beta agonist and a glp-1r agonist for use in treating obesity |
| CN120981457A (zh) | 2023-09-14 | 2025-11-18 | 歌礼制药(中国)有限公司 | Glp-1r激动剂及其治疗方法 |
| TW202521534A (zh) | 2023-11-24 | 2025-06-01 | 香港商歌禮製藥(中國)有限公司 | Glp-1r 激動劑及其治療方法 |
| WO2025158275A1 (en) | 2024-01-24 | 2025-07-31 | Pfizer Inc. | Combination therapy using glucose-dependent insulinotropic polypeptide receptor antagonist compounds and glp-1 receptor agonist compounds |
| TW202600132A (zh) | 2024-03-08 | 2026-01-01 | 美商安尼波那生物公司 | 用於治療肥胖症及提高減重之方法 |
| WO2026073030A1 (en) | 2024-09-27 | 2026-04-02 | Carmot Therapeutics Inc. | Combination therapy of peptide tyrosine-tyrosine (pyy) analogues and glp-1r agonists |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060275288A1 (en) | 2005-01-20 | 2006-12-07 | Grihalde Nelson D | GLP-1 receptor agonist and allosteric modulator monoclonal antibodies and uses thereof |
| US20120148586A1 (en) | 2009-08-27 | 2012-06-14 | Joyce Ching Tsu Chou | Glucagon-like protein-1 receptor (glp-1r) agonists for treating autoimmune disorders |
| US20120021979A1 (en) | 2010-06-24 | 2012-01-26 | Vanderbilt University | GLP-1 receptor modulation of addiction, neuropsychiatric disorders and erectile dysfunction |
| KR102314286B1 (ko) * | 2016-12-16 | 2021-10-21 | 화이자 인코포레이티드 | Glp-1 수용체 작용제 및 이의 용도 |
| US10934279B2 (en) * | 2018-06-13 | 2021-03-02 | Pfizer Inc. | GLP-1 receptor agonists and uses thereof |
| MA54555A (fr) * | 2018-11-22 | 2021-09-29 | Qilu Regor Therapeutics Inc | Agonistes de glp-1r et leurs utilisations |
| EP3953344A4 (en) * | 2019-04-12 | 2023-08-09 | Qilu Regor Therapeutics Inc. | GLP-IR AGONISTS AND THEIR USES |
| WO2020234726A1 (en) * | 2019-05-20 | 2020-11-26 | Pfizer Inc. | Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases |
| TWI751585B (zh) * | 2019-06-28 | 2022-01-01 | 美商美國禮來大藥廠 | 類升糖素肽1受體促效劑 |
| WO2021096284A1 (ko) * | 2019-11-15 | 2021-05-20 | 일동제약(주) | Glp-1 수용체 작용제 및 이의 용도 |
| CN114761395B (zh) * | 2019-12-02 | 2024-11-15 | 现代药品株式会社 | Glp-1受体激动剂 |
-
2022
- 2022-05-03 EP EP22725069.3A patent/EP4334304A1/en active Pending
- 2022-05-03 AU AU2022271223A patent/AU2022271223A1/en not_active Abandoned
- 2022-05-03 MX MX2023012918A patent/MX2023012918A/es unknown
- 2022-05-03 BR BR112023022836A patent/BR112023022836A2/pt unknown
- 2022-05-03 JP JP2023567973A patent/JP2024516291A/ja active Pending
- 2022-05-03 US US17/736,070 patent/US20220396569A1/en not_active Abandoned
- 2022-05-03 WO PCT/US2022/027535 patent/WO2022235717A1/en not_active Ceased
- 2022-05-03 EP EP24203388.4A patent/EP4461355A3/en not_active Withdrawn
- 2022-05-03 US US18/558,647 patent/US20240262811A1/en active Pending
- 2022-05-03 CA CA3217720A patent/CA3217720A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP4334304A1 (en) | 2024-03-13 |
| WO2022235717A1 (en) | 2022-11-10 |
| BR112023022836A2 (pt) | 2024-01-16 |
| US20240262811A1 (en) | 2024-08-08 |
| EP4461355A3 (en) | 2025-01-15 |
| MX2023012918A (es) | 2024-03-13 |
| US20220396569A1 (en) | 2022-12-15 |
| AU2022271223A1 (en) | 2023-11-02 |
| JP2024516291A (ja) | 2024-04-12 |
| EP4461355A2 (en) | 2024-11-13 |
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