CA3176569A1 - Treatment of type 2 diabetes or obesity or overweight with 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl} piperidin-1-yl)methyl]-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid or a pharmaceutically salt thereof - Google Patents

Treatment of type 2 diabetes or obesity or overweight with 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl} piperidin-1-yl)methyl]-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid or a pharmaceutically salt thereof

Info

Publication number
CA3176569A1
CA3176569A1 CA3176569A CA3176569A CA3176569A1 CA 3176569 A1 CA3176569 A1 CA 3176569A1 CA 3176569 A CA3176569 A CA 3176569A CA 3176569 A CA3176569 A CA 3176569A CA 3176569 A1 CA3176569 A1 CA 3176569A1
Authority
CA
Canada
Prior art keywords
compound
pharmaceutical composition
oxetan
fluorobenzyl
benzimidazole
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
Application number
CA3176569A
Other languages
English (en)
French (fr)
Inventor
Kai Teck LEE
Sweta MANTHENA
Aditi Rao SAXENA
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Inc
Original Assignee
Pfizer Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Pfizer Inc filed Critical Pfizer Inc
Publication of CA3176569A1 publication Critical patent/CA3176569A1/en
Pending legal-status Critical Current

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Classifications

    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
CA3176569A 2020-03-27 2021-03-24 Treatment of type 2 diabetes or obesity or overweight with 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl} piperidin-1-yl)methyl]-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid or a pharmaceutically salt thereof Pending CA3176569A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US202063000787P 2020-03-27 2020-03-27
US63/000,787 2020-03-27
US202063126113P 2020-12-16 2020-12-16
US63/126,113 2020-12-16
US202163135870P 2021-01-11 2021-01-11
US63/135,870 2021-01-11
PCT/IB2021/052430 WO2021191812A1 (en) 2020-03-27 2021-03-24 Treatment of type 2 diabetes or obesity or overweight with 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl} piperidin-1-yl)methyl]-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid or a pharmaceutically salt thereof

Publications (1)

Publication Number Publication Date
CA3176569A1 true CA3176569A1 (en) 2021-09-30

Family

ID=75252595

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3176569A Pending CA3176569A1 (en) 2020-03-27 2021-03-24 Treatment of type 2 diabetes or obesity or overweight with 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl} piperidin-1-yl)methyl]-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid or a pharmaceutically salt thereof

Country Status (13)

Country Link
US (1) US20230201185A1 (enExample)
EP (2) EP4537816A3 (enExample)
JP (2) JP2021155415A (enExample)
KR (1) KR20220157486A (enExample)
CN (1) CN115348863A (enExample)
AU (1) AU2021244918A1 (enExample)
BR (1) BR112022017578A2 (enExample)
CA (1) CA3176569A1 (enExample)
ES (1) ES3031577T3 (enExample)
IL (1) IL296694A (enExample)
MX (1) MX2022010811A (enExample)
TW (1) TWI823072B (enExample)
WO (1) WO2021191812A1 (enExample)

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EA202191432A1 (ru) 2018-11-22 2021-10-14 Цилу Регор Терапьютикс Инк. Агонисты glp-1r и их применения
AU2020256647B2 (en) 2019-04-12 2025-07-31 Qilu Regor Therapeutics Inc. GLP-1R agonists and uses thereof
CR20220178A (es) 2019-10-25 2022-06-15 Gilead Sciences Inc Compuestos moduladores de glp-1r
SI4097097T1 (sl) 2020-01-29 2025-04-30 Gilead Sciences, Inc. Spojine, ki modulirajo glp-1r
EP4247804A1 (en) 2020-11-20 2023-09-27 Gilead Sciences, Inc. Polyheterocyclic glp-1 r modulating compounds
US12180197B2 (en) 2021-03-11 2024-12-31 Gilead Sciences, Inc. GLP-1R modulating compounds
EP4304711A1 (en) 2021-03-11 2024-01-17 Gilead Sciences, Inc. Glp-1r modulating compounds
LT4271672T (lt) 2021-04-21 2026-03-10 Gilead Sciences, Inc. Karboksibenzimidazolo junginiai, moduliuojantys glp-1r
US12024507B2 (en) 2021-10-25 2024-07-02 Terns Pharmaceuticals, Inc. Compounds as GLP-1R agonists
CA3246495A1 (en) * 2022-03-25 2023-09-28 Ildong Pharmaceutical Co., Ltd. NEW GLP-1 RECEPTOR AGONIST COMPOUND SALT, ITS PREPARATION PROCESS AND PHARMACEUTICAL COMPOSITION INCLUDING IT
KR20250036254A (ko) * 2022-07-22 2025-03-13 화이자 인코포레이티드 2-[(4-｛6-[(4-시아노-2-플루오로벤질)옥시]피리딘-2-일}피페리딘-1-일｝메틸]-1-[(2s)-옥세탄-2-일메틸]-1h-벤즈이미다졸-6-카복실산,1,3-다이하이드록시-2-(하이드록시메틸)프로판-2-아민 염의 제조를 위한 방법 및 중간체
PE20252787A1 (es) 2023-04-07 2025-12-22 Terns Pharmaceuticals Inc Combinacion que comprende un agonista de thr-beta y un agonista de glp-1r para su uso en el tratamiento de un trastorno hepatico o una enfermedad cardiometabolica
CN116675680B (zh) * 2023-08-02 2023-10-20 药康众拓(北京)医药科技有限公司 一种氘代化合物及其制备方法、药物和应用
EP4777197A2 (en) 2023-09-14 2026-07-22 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof
WO2025099561A1 (en) 2023-11-07 2025-05-15 Pfizer Inc. Oral controlled-release matrix formulations of 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid or a pharmaceutically salt thereof
WO2025109387A1 (en) 2023-11-24 2025-05-30 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof
WO2025224648A1 (en) * 2024-04-26 2025-10-30 Pfizer Inc. Oral compositions/formulations of 2-({4-[(2s)-2-(4-chloro-2-fluorophenyl)-2-methyl-1,3-benzodioxol-4-yl]piperidin-1-yl}methyl)-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid or a pharmaceutically salt thereof
TW202612693A (zh) * 2024-06-05 2026-04-01 大陸商杭州中美華東製藥有限公司 Glp-1受體激動劑的口服藥物組合物及其製備方法

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Also Published As

Publication number Publication date
ES3031577T3 (en) 2025-07-09
BR112022017578A2 (pt) 2022-10-18
EP4537816A2 (en) 2025-04-16
EP4125896B1 (en) 2025-05-07
TWI823072B (zh) 2023-11-21
AU2021244918A1 (en) 2022-09-29
EP4537816A3 (en) 2025-06-25
IL296694A (en) 2022-11-01
US20230201185A1 (en) 2023-06-29
WO2021191812A1 (en) 2021-09-30
CN115348863A (zh) 2022-11-15
MX2022010811A (es) 2022-09-27
JP2021155415A (ja) 2021-10-07
JP2025118943A (ja) 2025-08-13
EP4125896A1 (en) 2023-02-08
KR20220157486A (ko) 2022-11-29
TW202202139A (zh) 2022-01-16

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