JP2021155415A - 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−ベンゾイミダゾール−６−カルボン酸またはその薬学的な塩を用いた２型糖尿病、または肥満、または過体重の治療 - Google Patents

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−ベンゾイミダゾール−６−カルボン酸またはその薬学的な塩を用いた２型糖尿病、または肥満、または過体重の治療 Download PDF

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JP2021155415A
JP2021155415A JP2021049350A JP2021049350A JP2021155415A JP 2021155415 A JP2021155415 A JP 2021155415A JP 2021049350 A JP2021049350 A JP 2021049350A JP 2021049350 A JP2021049350 A JP 2021049350A JP 2021155415 A JP2021155415 A JP 2021155415A
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pharmaceutical composition
compound
methyl
piperidine
oxy
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JP2021155415A5 (enExample
Inventor
テック リー カイ
Kai Teck Lee
テック リー カイ
マンセナ スウェタ
Manthena Sweta
マンセナ スウェタ
ラオ サクセナ アディティ
Rao Saxena Aditi
ラオ サクセナ アディティ
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Pfizer Corp Belgium
Pfizer Inc
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Pfizer Corp Belgium
Pfizer Inc
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Publication of JP2021155415A publication Critical patent/JP2021155415A/ja
Publication of JP2021155415A5 publication Critical patent/JP2021155415A5/ja
Priority to JP2025083688A priority Critical patent/JP2025118943A/ja
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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)
JP2021049350A 2020-03-27 2021-03-24 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−ベンゾイミダゾール−６−カルボン酸またはその薬学的な塩を用いた２型糖尿病、または肥満、または過体重の治療 Pending JP2021155415A (ja)

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JP2025083688A JP2025118943A (ja) 2020-03-27 2025-05-20 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－ベンゾイミダゾール－６－カルボン酸またはその薬学的な塩を用いた２型糖尿病、または肥満、または過体重の治療

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US202063000787P 2020-03-27 2020-03-27
US63/000787 2020-03-27
US202063126113P 2020-12-16 2020-12-16
US63/126113 2020-12-16
US202163135870P 2021-01-11 2021-01-11
US63/135870 2021-01-11

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JP2025083688A Division JP2025118943A (ja) 2020-03-27 2025-05-20 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－ベンゾイミダゾール－６－カルボン酸またはその薬学的な塩を用いた２型糖尿病、または肥満、または過体重の治療

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JP2021049350A Pending JP2021155415A (ja) 2020-03-27 2021-03-24 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−ベンゾイミダゾール−６−カルボン酸またはその薬学的な塩を用いた２型糖尿病、または肥満、または過体重の治療
JP2025083688A Pending JP2025118943A (ja) 2020-03-27 2025-05-20 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－ベンゾイミダゾール－６－カルボン酸またはその薬学的な塩を用いた２型糖尿病、または肥満、または過体重の治療

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EP (2) EP4125896B1 (enExample)
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BR112022007627A2 (pt) 2019-10-25 2022-07-12 Gilead Sciences Inc Compostos moduladores do glp-1r
CN115335374B (zh) 2020-01-29 2025-05-27 吉利德科学公司 Glp-1r调节化合物
US11851419B2 (en) 2020-11-20 2023-12-26 Gilead Sciences, Inc. GLP-1R modulating compounds
US12091404B2 (en) 2021-03-11 2024-09-17 Gilead Sciences, Inc. GLP-1R modulating compounds
WO2022192430A1 (en) 2021-03-11 2022-09-15 Gilead Sciences, Inc. Glp-1r modulating compounds
AU2022263410B2 (en) 2021-04-21 2024-08-01 Gilead Sciences, Inc. Carboxy-benzimidazole glp-1r modulating compounds
TW202334129A (zh) 2021-10-25 2023-09-01 美商拓臻製藥公司 作為ｇｌｐ—１ｒ促效劑的化合物
CN119585249A (zh) * 2022-07-22 2025-03-07 辉瑞公司 用于制备2-[(4-{6-[(4-氰基-2-氟芐基)氧基]吡啶-2-基}哌啶-1-基)甲基]-1-[(2s)-氧杂环丁烷-2-基甲基]-1h-苯并咪唑-6-羧酸，1,3-二羟基-2-(羟基甲基)丙-2-胺盐的方法及中间体
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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
WO2025057134A2 (en) 2023-09-14 2025-03-20 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof
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US12291530B1 (en) 2023-11-24 2025-05-06 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

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EP4537816A3 (en) 2025-06-25
JP2025118943A (ja) 2025-08-13
AU2021244918A1 (en) 2022-09-29
CA3176569A1 (en) 2021-09-30
US20230201185A1 (en) 2023-06-29
TW202202139A (zh) 2022-01-16
BR112022017578A2 (pt) 2022-10-18
IL296694A (en) 2022-11-01
EP4125896A1 (en) 2023-02-08
ES3031577T3 (en) 2025-07-09
KR20220157486A (ko) 2022-11-29
EP4125896B1 (en) 2025-05-07
CN115348863A (zh) 2022-11-15
EP4537816A2 (en) 2025-04-16
MX2022010811A (es) 2022-09-27
WO2021191812A1 (en) 2021-09-30

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