JP2025505198A - 肥満の治療のためのglp1受容体の活性化因子としての2-((4-((s)-2-(4-クロロ-2-フルオロフェニル)-2-メチルベンゾ[d][1,3]ジオキソール-4-イル)ピペリジン-1-イル)メチル)-1-(((s)-オキセタン-2-イル)メチル)-1h-イミダゾール誘導体 - Google Patents

肥満の治療のためのglp1受容体の活性化因子としての2-((4-((s)-2-(4-クロロ-2-フルオロフェニル)-2-メチルベンゾ[d][1,3]ジオキソール-4-イル)ピペリジン-1-イル)メチル)-1-(((s)-オキセタン-2-イル)メチル)-1h-イミダゾール誘導体 Download PDF

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JP2025505198A
JP2025505198A JP2024546402A JP2024546402A JP2025505198A JP 2025505198 A JP2025505198 A JP 2025505198A JP 2024546402 A JP2024546402 A JP 2024546402A JP 2024546402 A JP2024546402 A JP 2024546402A JP 2025505198 A JP2025505198 A JP 2025505198A
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methyl
alkyl
halo
oxetan
chloro
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JP2025505198A5 (enExample
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アラン,マーティン
カーソン,マシュー
カヤ,トーマス
ファザル,タンジナ
スミス,トロイ
ス,リャンシェン
ヤン,リファ
ツァン,ピン
キャン,ミン
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ノバルティス アーゲー
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Priority claimed from PCT/IB2022/053367 external-priority patent/WO2022219495A1/en
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P25/00Drugs for disorders of the nervous system
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    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

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  • Animal Behavior & Ethology (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
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  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
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  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2024546402A 2022-02-10 2023-02-10 肥満の治療のためのglp1受容体の活性化因子としての2-((4-((s)-2-(4-クロロ-2-フルオロフェニル)-2-メチルベンゾ[d][1,3]ジオキソール-4-イル)ピペリジン-1-イル)メチル)-1-(((s)-オキセタン-2-イル)メチル)-1h-イミダゾール誘導体 Pending JP2025505198A (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US202263308843P 2022-02-10 2022-02-10
US63/308,843 2022-02-10
US202263323401P 2022-03-24 2022-03-24
US63/323,401 2022-03-24
PCT/IB2022/053367 WO2022219495A1 (en) 2021-04-12 2022-04-11 2-((4-((s)-2-(4-chloro-2-fluorophenyl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-imidazole derivatives as activators of the glp1 receptor for the treatment of obesity
IBPCT/IB2022/053367 2022-04-11
US202263378749P 2022-10-07 2022-10-07
US63/378,749 2022-10-07
PCT/IB2023/051207 WO2023152698A1 (en) 2022-02-10 2023-02-10 2-((4-((s)-2-(4-chloro-2-fluorophenyl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-imidazole derivatives as activators of the glp1 receptor for the treatment of obesity

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JP2025505198A true JP2025505198A (ja) 2025-02-21
JP2025505198A5 JP2025505198A5 (enExample) 2025-03-03

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JP2024546402A Pending JP2025505198A (ja) 2022-02-10 2023-02-10 肥満の治療のためのglp1受容体の活性化因子としての2-((4-((s)-2-(4-クロロ-2-フルオロフェニル)-2-メチルベンゾ[d][1,3]ジオキソール-4-イル)ピペリジン-1-イル)メチル)-1-(((s)-オキセタン-2-イル)メチル)-1h-イミダゾール誘導体

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EP (1) EP4476212A1 (enExample)
JP (1) JP2025505198A (enExample)
TW (1) TW202342014A (enExample)
WO (1) WO2023152698A1 (enExample)

Families Citing this family (8)

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Publication number Priority date Publication date Assignee Title
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
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
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2020200308A (ja) * 2019-05-20 2020-12-17 ファイザー・インク Nash/nafldおよび関連疾患治療のための組合せ
JP2021521265A (ja) * 2018-06-13 2021-08-26 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

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200303742A (en) 2001-11-21 2003-09-16 Novartis Ag Organic compounds
CA2525764C (en) 2003-05-20 2012-07-17 Novartis Ag N-acyl nitrogen heterocycles as ligands of peroxisome proliferator-activated receptors
EP2694092B1 (en) 2011-04-08 2017-01-04 Amgen Inc. Method of treating or ameliorating metabolic disorders using growth differentiation factor 15 (gdf-15)
EP3683228A3 (en) 2012-01-26 2020-07-29 Amgen Inc. Growth differentiation factor 15 (gdf-15) polypeptides
CA2862516C (en) 2012-03-27 2023-02-14 Ngm Biopharmaceuticals, Inc. Compositions and methods of use for treating metabolic disorders
US9161966B2 (en) 2013-01-30 2015-10-20 Ngm Biopharmaceuticals, Inc. GDF15 mutein polypeptides
KR101993714B1 (ko) 2013-01-30 2019-06-28 엔지엠 바이오파마슈티컬스, 아이엔씨. 대사 장애를 치료하는데 이용하기 위한 조성물과 방법
US9862752B2 (en) 2013-07-31 2018-01-09 Amgen Inc. Growth differentiation factor 15 (GDF-15) constructs
EP3157947A1 (en) 2014-06-23 2017-04-26 Novartis AG Hsa-gdf-15 fusion polypeptide and use thereof
US10588980B2 (en) 2014-06-23 2020-03-17 Novartis Ag Fatty acids and their use in conjugation to biomolecules
RU2017101436A (ru) 2014-06-24 2018-07-24 Ново Нордиск А/С Mic-1 слитные белки и их применение
JP6946304B2 (ja) 2015-12-22 2021-10-06 ノバルティス アーゲー 増殖分化因子15(gdf−15)を使用して代謝障害を処置するまたは軽快させる方法
JP2023537501A (ja) * 2020-08-06 2023-09-01 ガシャーブラム・バイオ・インコーポレイテッド ヘテロ環glp-1アゴニスト

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021521265A (ja) * 2018-06-13 2021-08-26 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
JP2020200308A (ja) * 2019-05-20 2020-12-17 ファイザー・インク Nash/nafldおよび関連疾患治療のための組合せ

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