MX2022010811A - Tratamiento de la diabetes tipo 2 u obesidad o sobrepeso con el acido 2-[(4-{6-[(4-ciano-2-fluorobencil)oxi]piridin-2-il}piperidin -1-il)metil]-1-[(2s)-oxetan-2-ilmetil]-1h-bencimidazol-6-carboxil ico o una sal farmaceutica del mismo. - Google Patents

Tratamiento de la diabetes tipo 2 u obesidad o sobrepeso con el acido 2-[(4-{6-[(4-ciano-2-fluorobencil)oxi]piridin-2-il}piperidin -1-il)metil]-1-[(2s)-oxetan-2-ilmetil]-1h-bencimidazol-6-carboxil ico o una sal farmaceutica del mismo.

Info

Publication number
MX2022010811A
MX2022010811A MX2022010811A MX2022010811A MX2022010811A MX 2022010811 A MX2022010811 A MX 2022010811A MX 2022010811 A MX2022010811 A MX 2022010811A MX 2022010811 A MX2022010811 A MX 2022010811A MX 2022010811 A MX2022010811 A MX 2022010811A
Authority
MX
Mexico
Prior art keywords
oxetan
fluorobenzyl
overweight
piperidin
ylmethyl
Prior art date
Application number
MX2022010811A
Other languages
English (en)
Inventor
Kai Teck Lee
Sweta Manthena
Aditi Rao Saxena
Original Assignee
Pfizer
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 filed Critical Pfizer
Publication of MX2022010811A publication Critical patent/MX2022010811A/es

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2031Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, 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
    • A61K9/2086Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

La invención proporciona un método para tratar la T2DM, obesidad o sobrepeso o para el manejo de control del peso al administrar a un mamífero (por ejemplo, un humano) en necesidad del mismo una composición farmacéutica dos veces al día en una forma de dosificación oral, en donde la composición farmacéutica contiene ácido 2-[(4-{6-[(4-ciano-2-fluorobencil)oxi]piridin-2-il}piperidin -1-il)metil]-1-[(2S)-oxetan-2-ilmetil]-1H-bencimidazol-6-carboxíl ico o una sal farmacéuticamente del mismo [tal como su sal tris]. Más aún, la invención proporciona composiciones/formulaciones orales para los métodos de tratamiento descritos en la presente.
MX2022010811A 2020-03-27 2021-03-24 Tratamiento de la diabetes tipo 2 u obesidad o sobrepeso con el acido 2-[(4-{6-[(4-ciano-2-fluorobencil)oxi]piridin-2-il}piperidin -1-il)metil]-1-[(2s)-oxetan-2-ilmetil]-1h-bencimidazol-6-carboxil ico o una sal farmaceutica del mismo. MX2022010811A (es)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US202063000787P 2020-03-27 2020-03-27
US202063126113P 2020-12-16 2020-12-16
US202163135870P 2021-01-11 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
MX2022010811A true MX2022010811A (es) 2022-09-27

Family

ID=75252595

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2022010811A MX2022010811A (es) 2020-03-27 2021-03-24 Tratamiento de la diabetes tipo 2 u obesidad o sobrepeso con el acido 2-[(4-{6-[(4-ciano-2-fluorobencil)oxi]piridin-2-il}piperidin -1-il)metil]-1-[(2s)-oxetan-2-ilmetil]-1h-bencimidazol-6-carboxil ico o una sal farmaceutica del mismo.

Country Status (13)

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

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CN113227068B (zh) 2018-11-22 2023-06-13 上海齐鲁锐格医药研发有限公司 Glp-1r激动剂及其用途
US10954221B2 (en) 2019-04-12 2021-03-23 Qilu Regor Therapeutics Inc. GLP-1R agonists and uses thereof
JP7558267B2 (ja) 2019-10-25 2024-09-30 ギリアード サイエンシーズ, インコーポレイテッド Glp-1r調節化合物
CN120518596A (zh) 2020-01-29 2025-08-22 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
EP4304712A1 (en) 2021-03-11 2024-01-17 Gilead Sciences, Inc. Glp-1r modulating compounds
US12091404B2 (en) 2021-03-11 2024-09-17 Gilead Sciences, Inc. GLP-1R modulating compounds
IL306110A (en) 2021-04-21 2023-11-01 Gilead Sciences Inc Carboxy-benzimidazole glp-1r modulating compounds
WO2023076237A1 (en) 2021-10-25 2023-05-04 Terns Pharmaceuticals, Inc. Compounds as glp-1r agonists
CN119212991A (zh) * 2022-03-25 2024-12-27 日东制药株式会社 Glp-1受体激动剂化合物之新颖盐类、其制备方法以及包含其的药物组合物
CA3262491A1 (en) * 2022-07-22 2024-01-25 Pfizer Inc. PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF 1,3-DIHYDROXY-2-(HYDROXYMETHYL)PROPAN-2-AMINE SALT 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,
WO2024211898A1 (en) 2023-04-07 2024-10-10 Terns Pharmaceuticals, Inc. Combination comprising a thrbeta agonist anda glp-1r agonist for use in treating a liver disorder or a cardiometabolic disease
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
US12234236B1 (en) 2023-09-14 2025-02-25 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
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
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
WO2025252098A1 (zh) * 2024-06-05 2025-12-11 杭州中美华东制药有限公司 Glp-1受体激动剂的口服药物组合物及其制备方法

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Also Published As

Publication number Publication date
JP2021155415A (ja) 2021-10-07
EP4537816A2 (en) 2025-04-16
EP4125896B1 (en) 2025-05-07
WO2021191812A1 (en) 2021-09-30
BR112022017578A2 (pt) 2022-10-18
CN115348863A (zh) 2022-11-15
AU2021244918A1 (en) 2022-09-29
IL296694A (en) 2022-11-01
CA3176569A1 (en) 2021-09-30
ES3031577T3 (en) 2025-07-09
EP4537816A3 (en) 2025-06-25
TWI823072B (zh) 2023-11-21
EP4125896A1 (en) 2023-02-08
JP2025118943A (ja) 2025-08-13
TW202202139A (zh) 2022-01-16
US20230201185A1 (en) 2023-06-29
KR20220157486A (ko) 2022-11-29

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