KR20220157486A - 2-[(4-(6-[(4-시아노-2-플루오로벤질)옥시]피리딘-2-일)피페리딘-1-일)메틸]-1-[(2s)-옥세탄-2-일메틸]-1h-벤즈이미다졸-6-카르복실산 또는 그의 제약상 염을 사용한 제2형 당뇨병 또는 비만 또는 과체중의 치료 - Google Patents

2-[(4-(6-[(4-시아노-2-플루오로벤질)옥시]피리딘-2-일)피페리딘-1-일)메틸]-1-[(2s)-옥세탄-2-일메틸]-1h-벤즈이미다졸-6-카르복실산 또는 그의 제약상 염을 사용한 제2형 당뇨병 또는 비만 또는 과체중의 치료 Download PDF

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KR20220157486A
KR20220157486A KR1020227036905A KR20227036905A KR20220157486A KR 20220157486 A KR20220157486 A KR 20220157486A KR 1020227036905 A KR1020227036905 A KR 1020227036905A KR 20227036905 A KR20227036905 A KR 20227036905A KR 20220157486 A KR20220157486 A KR 20220157486A
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pharmaceutical composition
compound
pyridin
oxy
fluorobenzyl
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English (en)
Korean (ko)
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카이 테크 리
스웨타 만테나
아디티 라오 사세나
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화이자 인코포레이티드
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    • 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

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Obesity (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (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)
KR1020227036905A 2020-03-27 2021-03-24 2-[(4-(6-[(4-시아노-2-플루오로벤질)옥시]피리딘-2-일)피페리딘-1-일)메틸]-1-[(2s)-옥세탄-2-일메틸]-1h-벤즈이미다졸-6-카르복실산 또는 그의 제약상 염을 사용한 제2형 당뇨병 또는 비만 또는 과체중의 치료 Withdrawn KR20220157486A (ko)

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

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KR20220157486A true KR20220157486A (ko) 2022-11-29

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KR1020227036905A Withdrawn KR20220157486A (ko) 2020-03-27 2021-03-24 2-[(4-(6-[(4-시아노-2-플루오로벤질)옥시]피리딘-2-일)피페리딘-1-일)메틸]-1-[(2s)-옥세탄-2-일메틸]-1h-벤즈이미다졸-6-카르복실산 또는 그의 제약상 염을 사용한 제2형 당뇨병 또는 비만 또는 과체중의 치료

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US (1) US20230201185A1 (https=)
EP (2) EP4125896B1 (https=)
JP (2) JP2021155415A (https=)
KR (1) KR20220157486A (https=)
CN (1) CN115348863A (https=)
AU (1) AU2021244918A1 (https=)
BR (1) BR112022017578A2 (https=)
CA (1) CA3176569A1 (https=)
ES (1) ES3031577T3 (https=)
IL (1) IL296694A (https=)
MX (1) MX2022010811A (https=)
TW (1) TWI823072B (https=)
WO (1) WO2021191812A1 (https=)

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US10954221B2 (en) 2019-04-12 2021-03-23 Qilu Regor Therapeutics Inc. GLP-1R agonists and uses thereof
CA3157525A1 (en) 2019-10-25 2021-04-29 Gilead Sciences, Inc. Glp-1r modulating compounds
WO2021154796A1 (en) 2020-01-29 2021-08-05 Gilead Sciences, Inc. Glp-1r modulating compounds
EP4247804A1 (en) 2020-11-20 2023-09-27 Gilead Sciences, Inc. Polyheterocyclic glp-1 r modulating compounds
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WO2022192430A1 (en) 2021-03-11 2022-09-15 Gilead Sciences, Inc. Glp-1r modulating compounds
PH12023552860A1 (en) 2021-04-21 2024-05-20 Gilead Sciences Inc Carboxy-benzimidazole glp-1r modulating compounds
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WO2023182869A1 (en) * 2022-03-25 2023-09-28 Ildong Pharmaceutical Co., Ltd. Novel salt of glp-1 receptor agonist compound, preparation method thereof and pharmaceutical composition comprising thereof
JP2025523949A (ja) * 2022-07-22 2025-07-25 ファイザー・インク ２－［（４－｛６－［（４－シアノ－２－フルオロベンジル）オキシ］ピリジン－２－イル｝ピペリジン－１－イル）メチル］－１－［（２ｓ）－オキセタン－２－イルメチル］－１ｈ－ベンズイミダゾール－６－カルボン酸、１，３－ジヒドロキシ－２－（ヒドロキシメチル）プロパン－２－アミン塩を調製するための方法および中間体
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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
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
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US20230201185A1 (en) 2023-06-29
IL296694A (en) 2022-11-01
JP2025118943A (ja) 2025-08-13
MX2022010811A (es) 2022-09-27
EP4537816A2 (en) 2025-04-16
WO2021191812A1 (en) 2021-09-30
TWI823072B (zh) 2023-11-21
JP2021155415A (ja) 2021-10-07
EP4125896B1 (en) 2025-05-07
EP4125896A1 (en) 2023-02-08
EP4537816A3 (en) 2025-06-25
CA3176569A1 (en) 2021-09-30
CN115348863A (zh) 2022-11-15
ES3031577T3 (en) 2025-07-09
BR112022017578A2 (pt) 2022-10-18
AU2021244918A1 (en) 2022-09-29
TW202202139A (zh) 2022-01-16

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