JPWO2022017338A5 - - Google Patents
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- JPWO2022017338A5 JPWO2022017338A5 JP2023504008A JP2023504008A JPWO2022017338A5 JP WO2022017338 A5 JPWO2022017338 A5 JP WO2022017338A5 JP 2023504008 A JP2023504008 A JP 2023504008A JP 2023504008 A JP2023504008 A JP 2023504008A JP WO2022017338 A5 JPWO2022017338 A5 JP WO2022017338A5
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- JP
- Japan
- Prior art keywords
- alkyl
- present
- compound
- alkoxy
- pharma
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 90
- 150000003839 salts Chemical class 0.000 claims description 33
- -1 carrier Substances 0.000 claims description 15
- 239000008194 pharmaceutical composition Substances 0.000 claims description 13
- 239000003085 diluting agent Substances 0.000 claims description 10
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 10
- 125000000217 alkyl group Chemical group 0.000 description 101
- 125000003545 alkoxy group Chemical group 0.000 description 54
- 125000001188 haloalkyl group Chemical group 0.000 description 47
- 125000004438 haloalkoxy group Chemical group 0.000 description 46
- 229910052736 halogen Inorganic materials 0.000 description 43
- 150000002367 halogens Chemical class 0.000 description 43
- 125000000753 cycloalkyl group Chemical group 0.000 description 36
- 125000001424 substituent group Chemical group 0.000 description 35
- 229910052760 oxygen Inorganic materials 0.000 description 25
- 229910052717 sulfur Inorganic materials 0.000 description 25
- 125000005842 heteroatom Chemical group 0.000 description 23
- 125000001072 heteroaryl group Chemical group 0.000 description 20
- 125000000623 heterocyclic group Chemical group 0.000 description 13
- 125000004432 carbon atom Chemical group C* 0.000 description 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 10
- 102000007446 Glucagon-Like Peptide-1 Receptor Human genes 0.000 description 7
- 108010086246 Glucagon-Like Peptide-1 Receptor Proteins 0.000 description 7
- 229910052799 carbon Inorganic materials 0.000 description 7
- 239000000651 prodrug Substances 0.000 description 7
- 229940002612 prodrug Drugs 0.000 description 7
- 239000012453 solvate Substances 0.000 description 7
- 201000010099 disease Diseases 0.000 description 6
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 description 5
- 208000035475 disorder Diseases 0.000 description 4
- 230000001404 mediated effect Effects 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 description 3
- 208000008589 Obesity Diseases 0.000 description 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 2
- 206010012601 diabetes mellitus Diseases 0.000 description 2
- 229910052739 hydrogen Inorganic materials 0.000 description 2
- 208000019423 liver disease Diseases 0.000 description 2
- 235000020824 obesity Nutrition 0.000 description 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 201000001320 Atherosclerosis Diseases 0.000 description 1
- 206010007559 Cardiac failure congestive Diseases 0.000 description 1
- 208000024172 Cardiovascular disease Diseases 0.000 description 1
- 206010012289 Dementia Diseases 0.000 description 1
- 208000002249 Diabetes Complications Diseases 0.000 description 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 description 1
- 206010012655 Diabetic complications Diseases 0.000 description 1
- 229940089838 Glucagon-like peptide 1 receptor agonist Drugs 0.000 description 1
- 208000002705 Glucose Intolerance Diseases 0.000 description 1
- 206010019280 Heart failures Diseases 0.000 description 1
- 208000035150 Hypercholesterolemia Diseases 0.000 description 1
- 208000031226 Hyperlipidaemia Diseases 0.000 description 1
- 206010020772 Hypertension Diseases 0.000 description 1
- 206010033307 Overweight Diseases 0.000 description 1
- 208000018737 Parkinson disease Diseases 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 206010003119 arrhythmia Diseases 0.000 description 1
- 230000006793 arrhythmia Effects 0.000 description 1
- 206010008118 cerebral infarction Diseases 0.000 description 1
- 208000026106 cerebrovascular disease Diseases 0.000 description 1
- 208000029078 coronary artery disease Diseases 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 1
- 208000033679 diabetic kidney disease Diseases 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 125000004857 imidazopyridinyl group Chemical group N1C(=NC2=C1C=CC=N2)* 0.000 description 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 description 1
- 125000001786 isothiazolyl group Chemical group 0.000 description 1
- 125000000842 isoxazolyl group Chemical group 0.000 description 1
- 208000017169 kidney disease Diseases 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 208000030159 metabolic disease Diseases 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 230000004770 neurodegeneration Effects 0.000 description 1
- 208000015122 neurodegenerative disease Diseases 0.000 description 1
- 125000001715 oxadiazolyl group Chemical group 0.000 description 1
- 125000002971 oxazolyl group Chemical group 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 201000009104 prediabetes syndrome Diseases 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024174734A JP7795064B2 (ja) | 2020-07-20 | 2024-10-04 | テトラヒドロピラゾロ－ピラジニル－ジヒドロイミダゾロンまたはテトラヒドロピラゾロ－ピリジニル－ジヒドロイミダゾロン化合物およびそれを使用する方法 |
| JP2025207454A JP2026035735A (ja) | 2020-07-20 | 2025-11-28 | テトラヒドロピラゾロ－ピラジニル－ジヒドロイミダゾロンまたはテトラヒドロピラゾロ－ピリジニル－ジヒドロイミダゾロン化合物およびそれを使用する方法 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2020/102955 | 2020-07-20 | ||
| CN2020102955 | 2020-07-20 | ||
| CNPCT/CN2021/070120 | 2021-01-04 | ||
| CN2021070120 | 2021-01-04 | ||
| PCT/CN2021/107216 WO2022017338A1 (en) | 2020-07-20 | 2021-07-20 | Tetrahydropyrazolo-pyrazinyl-dihydroimidazolone or tetrahydropyrazolo-pyridinyl-dihydroimidazolone compounds and methods of using same |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024174734A Division JP7795064B2 (ja) | 2020-07-20 | 2024-10-04 | テトラヒドロピラゾロ－ピラジニル－ジヒドロイミダゾロンまたはテトラヒドロピラゾロ－ピリジニル－ジヒドロイミダゾロン化合物およびそれを使用する方法 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2023534983A JP2023534983A (ja) | 2023-08-15 |
| JP2023534983A5 JP2023534983A5 (https=) | 2024-07-29 |
| JPWO2022017338A5 true JPWO2022017338A5 (https=) | 2024-07-29 |
| JP7569443B2 JP7569443B2 (ja) | 2024-10-17 |
Family
ID=77167918
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023504008A Active JP7569443B2 (ja) | 2020-07-20 | 2021-07-20 | テトラヒドロピラゾロ－ピラジニル－ジヒドロイミダゾロンまたはテトラヒドロピラゾロ－ピリジニル－ジヒドロイミダゾロン化合物およびそれを使用する方法 |
| JP2024174734A Active JP7795064B2 (ja) | 2020-07-20 | 2024-10-04 | テトラヒドロピラゾロ－ピラジニル－ジヒドロイミダゾロンまたはテトラヒドロピラゾロ－ピリジニル－ジヒドロイミダゾロン化合物およびそれを使用する方法 |
| JP2025207454A Pending JP2026035735A (ja) | 2020-07-20 | 2025-11-28 | テトラヒドロピラゾロ－ピラジニル－ジヒドロイミダゾロンまたはテトラヒドロピラゾロ－ピリジニル－ジヒドロイミダゾロン化合物およびそれを使用する方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024174734A Active JP7795064B2 (ja) | 2020-07-20 | 2024-10-04 | テトラヒドロピラゾロ－ピラジニル－ジヒドロイミダゾロンまたはテトラヒドロピラゾロ－ピリジニル－ジヒドロイミダゾロン化合物およびそれを使用する方法 |
| JP2025207454A Pending JP2026035735A (ja) | 2020-07-20 | 2025-11-28 | テトラヒドロピラゾロ－ピラジニル－ジヒドロイミダゾロンまたはテトラヒドロピラゾロ－ピリジニル－ジヒドロイミダゾロン化合物およびそれを使用する方法 |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US12037339B2 (https=) |
| EP (1) | EP4182020A1 (https=) |
| JP (3) | JP7569443B2 (https=) |
| KR (2) | KR102936860B1 (https=) |
| CN (1) | CN116390926A (https=) |
| AU (2) | AU2021311567B2 (https=) |
| BR (1) | BR112023000932A2 (https=) |
| CA (1) | CA3186217A1 (https=) |
| CL (1) | CL2023000196A1 (https=) |
| CO (1) | CO2023001407A2 (https=) |
| IL (1) | IL299704A (https=) |
| MX (1) | MX2023000943A (https=) |
| PE (1) | PE20230854A1 (https=) |
| PH (1) | PH12023550130A1 (https=) |
| WO (1) | WO2022017338A1 (https=) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20190060A1 (ar) | 2016-09-26 | 2019-03-26 | Chugai Pharmaceutical Co Ltd | مشتق بيرازولو بيريدين له تأثير مساعد لمستقبل glp-1 |
| EP4211139A4 (en) * | 2020-09-10 | 2024-12-18 | Gasherbrum Bio, Inc. | HETEROCYCLIC GLP-1 AGONISTS |
| US12479854B2 (en) | 2021-07-29 | 2025-11-25 | Enanta Pharmaceuticals, Inc. | Spiropyrrolidine derived antiviral agents |
| US20240366639A1 (en) * | 2021-08-12 | 2024-11-07 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
| KR20240068737A (ko) | 2021-09-27 | 2024-05-17 | 테른스 파마슈티칼스, 인크. | Glp-1r 효능제로서의 벤즈이미다졸 카복실산 |
| AU2022375634A1 (en) | 2021-10-25 | 2024-06-06 | Terns Pharmaceuticals, Inc. | Compounds as glp-1r agonists |
| KR20240150488A (ko) | 2022-02-23 | 2024-10-15 | 테른스 파마슈티칼스, 인크. | Glp-1r 작용제로서의 화합물 |
| IL316478A (en) * | 2022-05-11 | 2024-12-01 | Lilly Co Eli | GLP1 tablet preparations |
| CN116003403B (zh) * | 2022-11-20 | 2024-07-23 | 药康众拓(北京)医药科技有限公司 | 一种氘代吲唑类化合物、药物组合物及其应用 |
| EP4634156A1 (en) * | 2022-12-15 | 2025-10-22 | Sironax Ltd | Sarm1 modulators, preparations, and uses thereof |
| EP4652167A1 (en) * | 2023-01-17 | 2025-11-26 | Fochon Biosciences, Ltd. | Glp-1r agonists and uses thereof |
| AU2024222719A1 (en) | 2023-02-16 | 2025-08-21 | Gasherbrum Bio, Inc. | Heterocyclic glp-1 agonists |
| US20240398794A1 (en) | 2023-04-07 | 2024-12-05 | Terns Pharmaceuticals, Inc. | COMBINATIONS OF GLP-1R AND THRß AGONISTS AND METHODS OF USE THEREOF |
| JP2025538520A (ja) * | 2023-06-29 | 2025-11-28 | ウェイン バイオテクノロジー カンパニー，リミテッド | Ｇｌｐ－１受容体アゴニスト並びにその調製方法及び使用 |
| CN120574224A (zh) * | 2023-06-30 | 2025-09-02 | 正大天晴药业集团股份有限公司 | 含多稠环结构的化合物 |
| WO2025011664A1 (zh) | 2023-07-12 | 2025-01-16 | 歌礼制药(中国)有限公司 | Glp-1r激动剂的制剂及其制备方法 |
| CN121712771A (zh) * | 2023-07-28 | 2026-03-20 | 上海翰森生物医药科技有限公司 | 一种苯并含氮杂环类衍生物调节剂、其制备方法和应用 |
| WO2025026436A1 (zh) * | 2023-08-02 | 2025-02-06 | 韦恩生物科技有限公司 | 一种含氮并环化合物及其制备方法和用途 |
| WO2025045208A1 (en) * | 2023-08-31 | 2025-03-06 | Gasherbrum Bio, Inc. | Heteroaryl-heterocycloalkyl-based glp-1 agonists |
| TW202521533A (zh) * | 2023-09-14 | 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 |
| WO2025097835A1 (zh) | 2023-11-10 | 2025-05-15 | 重庆医药工业研究院有限责任公司 | 一种glp-1r激动剂化合物及其应用 |
| TW202527933A (zh) * | 2023-11-16 | 2025-07-16 | 大陸商西藏海思科製藥有限公司 | 咪唑-2-酮衍生物及其在醫藥上的應用 |
| WO2025108361A1 (zh) * | 2023-11-21 | 2025-05-30 | 江苏恒瑞医药股份有限公司 | 杂环类化合物、其制备方法及其在医药上的应用 |
| US12291530B1 (en) | 2023-11-24 | 2025-05-06 | Ascletis Pharma (China) Co., Limited | GLP-1R agonist and therapeutic method thereof |
| WO2025119206A1 (en) * | 2023-12-05 | 2025-06-12 | Fortvita Biologics Inc. | Glp-1 receptor targeting compounds and uses thereof |
| WO2025124357A1 (zh) * | 2023-12-14 | 2025-06-19 | 广东众生睿创生物科技有限公司 | 一种杂环glp-1受体激动剂及其应用 |
| TW202527937A (zh) * | 2023-12-22 | 2025-07-16 | 大陸商石藥集團百克（山東）生物製藥股份有限公司 | 多環化合物及其用途 |
| CN117447493A (zh) * | 2023-12-25 | 2024-01-26 | 药康众拓(北京)医药科技有限公司 | 氘代吲哚嗪类化合物、药物组合物及其应用 |
| CN117777111A (zh) * | 2023-12-26 | 2024-03-29 | 上海苏博医药科技有限公司 | 一种Orforglipron关键中间体的合成方法及其中间体 |
| WO2025148997A1 (zh) * | 2024-01-10 | 2025-07-17 | 海思科医药集团股份有限公司 | 一种四氢吡啶并吡唑衍生物及其在医药上的应用 |
| 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 |
| CN120813584A (zh) * | 2024-01-30 | 2025-10-17 | 海创药业股份有限公司 | 一种具有glp-1受体激动剂作用的小分子化合物及其用途 |
| WO2025175249A1 (en) | 2024-02-14 | 2025-08-21 | Olema Pharmaceuticals, Inc. | Estrogen receptor modulators and uses thereof |
| WO2025176130A1 (zh) * | 2024-02-19 | 2025-08-28 | 上海壹迪生物技术有限公司 | 一种含吡唑并环类化合物、其药物组合物及其用途 |
| WO2025189141A1 (en) | 2024-03-08 | 2025-09-12 | Annapurna Bio, Inc. | Methods for treating obesity and increasing weight loss |
| WO2025208111A1 (en) * | 2024-03-29 | 2025-10-02 | Biomea Fusion, Inc. | Heterocyclic glp-1r agonists |
| WO2025209515A1 (zh) * | 2024-04-03 | 2025-10-09 | 广州市联瑞制药有限公司 | 一种glp-1受体激动剂及其制备方法和应用 |
| WO2025237355A1 (zh) * | 2024-05-17 | 2025-11-20 | 成都地奥九泓制药厂 | 一种glp-1受体激动剂化合物、其制备方法及其应用 |
| WO2025247390A1 (zh) * | 2024-05-31 | 2025-12-04 | 福佑泰生物制药公司 | 可用作glp-1r激动剂的杂双环化合物 |
| WO2025259825A1 (en) | 2024-06-12 | 2025-12-18 | Eli Lilly And Company | Glp-1 npa therapies for maintaining body weight loss or reduced hba1c levels following a prior glp-1 ra treatment |
| WO2025261454A1 (zh) * | 2024-06-19 | 2025-12-26 | 上海翰森生物医药科技有限公司 | 一种含氮大环化合物衍生物调节剂及其制备方法和应用 |
| WO2025264023A1 (en) * | 2024-06-19 | 2025-12-26 | Chong Kun Dang Pharmaceutical Corp. | Glp-1 receptor agonist, and uses thereof |
| WO2026001866A1 (zh) * | 2024-06-24 | 2026-01-02 | 联邦生物科技(珠海横琴)有限公司 | 一种glp-1受体激动剂及其应用 |
| WO2026007995A1 (zh) * | 2024-07-03 | 2026-01-08 | 成都地奥九泓制药厂 | 一种杂环类glp-1受体激动剂化合物、其制备方法及其应用 |
| WO2026012416A1 (zh) * | 2024-07-11 | 2026-01-15 | 江苏德源药业股份有限公司 | 杂环类化合物、药物组合物及其应用 |
| WO2026012449A1 (zh) * | 2024-07-12 | 2026-01-15 | 联邦生物科技(珠海横琴)有限公司 | 一种具有glp-1受体激动剂效应的杂环化合物及其应用 |
| WO2026031819A1 (en) * | 2024-08-06 | 2026-02-12 | Insilico Medicine Ip Limited | Novel compounds as glp-1r agonists and uses thereof |
| WO2026041075A1 (en) * | 2024-08-21 | 2026-02-26 | Gasherbrum Bio, Inc. | Gpl-1 agonists |
| CN119100966B (zh) * | 2024-09-02 | 2025-09-09 | 上海毕得医药科技股份有限公司 | 一种溴代吡咯甲酸甲酯的合成方法 |
| WO2026055512A1 (en) * | 2024-09-05 | 2026-03-12 | Biomea Fusion, Inc. | Combination of a menin inhibitor with a pyrazolopiperidine glp-1 receptor agonist for treating diabetes and obesity |
| WO2026052129A1 (zh) * | 2024-09-09 | 2026-03-12 | 中国科学院上海药物研究所 | 多环杂芳烃类glp-1受体激动剂 |
| CN120309500B (zh) * | 2025-06-19 | 2025-08-15 | 南昌大学 | 奥格列龙原料中间体及合成方法与奥格列龙原料合成方法 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| EP2963013A4 (en) * | 2013-02-27 | 2016-09-14 | Shionogi & Co | INDOLE AND AZAINDOLE DERIVATIVES HAVING AMPK ACTIVATION ACTIVITY EACH |
| JOP20190060A1 (ar) * | 2016-09-26 | 2019-03-26 | Chugai Pharmaceutical Co Ltd | مشتق بيرازولو بيريدين له تأثير مساعد لمستقبل glp-1 |
| JP7461104B2 (ja) * | 2017-11-29 | 2024-04-03 | 中外製薬株式会社 | Ｇｌｐ－１受容体アゴニスト作用を持つピラゾロピリジン誘導体を含有する医薬組成物 |
| CN111801331A (zh) * | 2018-02-28 | 2020-10-20 | 诺华股份有限公司 | 吲哚-2-羰基化合物及其用于治疗乙型肝炎的用途 |
-
2021
- 2021-07-20 WO PCT/CN2021/107216 patent/WO2022017338A1/en not_active Ceased
- 2021-07-20 JP JP2023504008A patent/JP7569443B2/ja active Active
- 2021-07-20 US US17/380,084 patent/US12037339B2/en active Active
- 2021-07-20 KR KR1020237005845A patent/KR102936860B1/ko active Active
- 2021-07-20 PH PH1/2023/550130A patent/PH12023550130A1/en unknown
- 2021-07-20 AU AU2021311567A patent/AU2021311567B2/en active Active
- 2021-07-20 CN CN202180063652.8A patent/CN116390926A/zh active Pending
- 2021-07-20 BR BR112023000932A patent/BR112023000932A2/pt unknown
- 2021-07-20 IL IL299704A patent/IL299704A/en unknown
- 2021-07-20 KR KR1020267006827A patent/KR20260040657A/ko active Pending
- 2021-07-20 MX MX2023000943A patent/MX2023000943A/es unknown
- 2021-07-20 EP EP21749074.7A patent/EP4182020A1/en active Pending
- 2021-07-20 CA CA3186217A patent/CA3186217A1/en active Pending
- 2021-07-20 PE PE2023000103A patent/PE20230854A1/es unknown
- 2021-11-02 US US17/516,932 patent/US11584751B1/en active Active
-
2023
- 2023-01-19 CL CL2023000196A patent/CL2023000196A1/es unknown
- 2023-02-09 CO CONC2023/0001407A patent/CO2023001407A2/es unknown
-
2024
- 2024-05-14 US US18/663,450 patent/US20250059192A1/en active Pending
- 2024-10-04 JP JP2024174734A patent/JP7795064B2/ja active Active
-
2025
- 2025-09-24 AU AU2025237942A patent/AU2025237942A1/en active Pending
- 2025-11-28 JP JP2025207454A patent/JP2026035735A/ja active Pending
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