JP2024516291A - ベンゾイミダゾイルｇｌｐ－１受容体アゴニスト、それを含む医薬組成物、及びそれらの使用方法 - Google Patents
ベンゾイミダゾイルｇｌｐ－１受容体アゴニスト、それを含む医薬組成物、及びそれらの使用方法 Download PDFInfo
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- JP2024516291A JP2024516291A JP2023567973A JP2023567973A JP2024516291A JP 2024516291 A JP2024516291 A JP 2024516291A JP 2023567973 A JP2023567973 A JP 2023567973A JP 2023567973 A JP2023567973 A JP 2023567973A JP 2024516291 A JP2024516291 A JP 2024516291A
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- Prior art keywords
- alkyl
- substituted
- methyl
- certain embodiments
- unsubstituted
- Prior art date
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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 (2)
| Publication Number | Publication Date |
|---|---|
| JP2024516291A true JP2024516291A (ja) | 2024-04-12 |
| JP2024516291A5 JP2024516291A5 (https=) | 2025-05-13 |
Family
ID=81750835
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023567973A Pending JP2024516291A (ja) | 2021-05-03 | 2022-05-03 | ベンゾイミダゾイルｇｌｐ－１受容体アゴニスト、それを含む医薬組成物、及びそれらの使用方法 |
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=) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023538408A (ja) * | 2020-08-21 | 2023-09-07 | ターンズ・ファーマシューティカルズ・インコーポレイテッド | Ｇｌｐ－１ｒ作動薬としての化合物 |
| US12486261B2 (en) | 2021-10-25 | 2025-12-02 | Terns Pharmaceuticals, Inc. | Compounds as GLP-1R agonists |
| US12485118B2 (en) | 2023-04-07 | 2025-12-02 | Terns Pharmaceuticals, Inc. | Combinations of GLP-1R and THRβ agonists and methods of use thereof |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20190382384A1 (en) * | 2018-06-13 | 2019-12-19 | Pfizer Inc. | GLP-1 Receptor Agonists and Uses Thereof |
| JP2020511411A (ja) * | 2016-12-16 | 2020-04-16 | ファイザー・インク | Ｇｌｐ−１受容体アゴニストおよびその使用 |
| WO2020103815A1 (en) * | 2018-11-22 | 2020-05-28 | Qilu Regor Therapeutics Inc. | Glp-1r agonists and uses thereof |
| US20200325121A1 (en) * | 2019-04-12 | 2020-10-15 | Qilu Regor Therapeutics Inc. | Glp-1r agonists and uses thereof |
| US20200407347A1 (en) * | 2019-06-28 | 2020-12-31 | Eli Lilly And Company | Glucagon-like peptide1 receptor agonists |
| WO2021112538A1 (en) * | 2019-12-02 | 2021-06-10 | Hyundai Pharm Co., Ltd. | Glp-1 receptor agonist |
Family Cites Families (5)
| 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 |
| 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 |
| WO2021096284A1 (ko) * | 2019-11-15 | 2021-05-20 | 일동제약(주) | Glp-1 수용체 작용제 및 이의 용도 |
-
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
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2020511411A (ja) * | 2016-12-16 | 2020-04-16 | ファイザー・インク | Ｇｌｐ−１受容体アゴニストおよびその使用 |
| US20190382384A1 (en) * | 2018-06-13 | 2019-12-19 | Pfizer Inc. | GLP-1 Receptor Agonists and Uses Thereof |
| WO2020103815A1 (en) * | 2018-11-22 | 2020-05-28 | Qilu Regor Therapeutics Inc. | Glp-1r agonists and uses thereof |
| US20200325121A1 (en) * | 2019-04-12 | 2020-10-15 | Qilu Regor Therapeutics Inc. | Glp-1r agonists and uses thereof |
| US20200407347A1 (en) * | 2019-06-28 | 2020-12-31 | Eli Lilly And Company | Glucagon-like peptide1 receptor agonists |
| WO2021112538A1 (en) * | 2019-12-02 | 2021-06-10 | Hyundai Pharm Co., Ltd. | Glp-1 receptor agonist |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2023538408A (ja) * | 2020-08-21 | 2023-09-07 | ターンズ・ファーマシューティカルズ・インコーポレイテッド | Ｇｌｐ－１ｒ作動薬としての化合物 |
| US12486261B2 (en) | 2021-10-25 | 2025-12-02 | Terns Pharmaceuticals, Inc. | Compounds as GLP-1R agonists |
| US12485118B2 (en) | 2023-04-07 | 2025-12-02 | Terns Pharmaceuticals, Inc. | Combinations of GLP-1R and THRβ agonists and methods of use thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| EP4334304A1 (en) | 2024-03-13 |
| CA3217720A1 (en) | 2022-11-10 |
| 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 |
| EP4461355A2 (en) | 2024-11-13 |
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