CN115348863A - 以2-[(4-{6-[(4-氰基-2-氟苄基)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-甲酸或其药学上的盐治疗2型糖尿病或肥胖症或体重过重 - Google Patents

以2-[(4-{6-[(4-氰基-2-氟苄基)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-甲酸或其药学上的盐治疗2型糖尿病或肥胖症或体重过重 Download PDF

Info

Publication number
CN115348863A
CN115348863A CN202180024485.6A CN202180024485A CN115348863A CN 115348863 A CN115348863 A CN 115348863A CN 202180024485 A CN202180024485 A CN 202180024485A CN 115348863 A CN115348863 A CN 115348863A
Authority
CN
China
Prior art keywords
compound
pharmaceutical composition
fluorobenzyl
ylmethyl
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
CN202180024485.6A
Other languages
English (en)
Chinese (zh)
Inventor
K·T·李
S·曼泰纳
A·R·萨克塞纳
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 CN115348863A publication Critical patent/CN115348863A/zh
Pending legal-status Critical Current

Links

Images

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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (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)
CN202180024485.6A 2020-03-27 2021-03-24 以2-[(4-{6-[(4-氰基-2-氟苄基)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-甲酸或其药学上的盐治疗2型糖尿病或肥胖症或体重过重 Pending CN115348863A (zh)

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
CN115348863A true CN115348863A (zh) 2022-11-15

Family

ID=75252595

Family Applications (1)

Application Number Title Priority Date Filing Date
CN202180024485.6A Pending CN115348863A (zh) 2020-03-27 2021-03-24 以2-[(4-{6-[(4-氰基-2-氟苄基)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-甲酸或其药学上的盐治疗2型糖尿病或肥胖症或体重过重

Country Status (13)

Country Link
US (1) US20230201185A1 (https=)
EP (2) EP4537816A3 (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=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116675680A (zh) * 2023-08-02 2023-09-01 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
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

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA54555A (fr) 2018-11-22 2021-09-29 Qilu Regor Therapeutics Inc Agonistes de glp-1r et leurs utilisations
EP3953344A4 (en) 2019-04-12 2023-08-09 Qilu Regor Therapeutics Inc. GLP-IR AGONISTS AND THEIR USES
EP4048664A1 (en) 2019-10-25 2022-08-31 Gilead Sciences, Inc. Glp-1r modulating compounds
ES3016132T3 (en) 2020-01-29 2025-05-08 Gilead Sciences Inc Glp-1r modulating compounds
EP4247804A1 (en) 2020-11-20 2023-09-27 Gilead Sciences, Inc. Polyheterocyclic glp-1 r modulating compounds
EP4304712A1 (en) 2021-03-11 2024-01-17 Gilead Sciences, Inc. Glp-1r modulating compounds
WO2022192428A1 (en) 2021-03-11 2022-09-15 Gilead Sciences, Inc. Glp-1r modulating compounds
IL306110A (en) 2021-04-21 2023-11-01 Gilead Sciences Inc Carboxy-benzimidazole glp-1r modulating compounds
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
US20250214968A1 (en) * 2022-03-25 2025-07-03 Ildong Pharmaceutical Co., Ltd. Novel Salt of GLP-1 Receptor Agonist Compound, Preparation Method Thereof and Pharmaceutical Composition Comprising Thereof
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
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
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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013117963A1 (en) * 2012-02-09 2013-08-15 Piramal Enterprises Limited Stable oral tablet dosage form of an antidiabetic compound
CN110325530A (zh) * 2016-12-16 2019-10-11 辉瑞大药厂 Glp-1受体激动剂及其用途

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US4485045A (en) 1981-07-06 1984-11-27 Research Corporation Synthetic phosphatidyl cholines useful in forming liposomes
US4544545A (en) 1983-06-20 1985-10-01 Trustees University Of Massachusetts Liposomes containing modified cholesterol for organ targeting
US5013556A (en) 1989-10-20 1991-05-07 Liposome Technology, Inc. Liposomes with enhanced circulation time
AU2001296000A1 (en) * 2000-10-24 2002-05-27 Ajinomoto Co., Inc. Nateglinide-containing hydrophilic drug preparations
CH702192A1 (de) 2009-11-04 2011-05-13 New Dent Ag Keramisches Implantat.
HRP20161178T1 (hr) 2010-09-30 2016-11-04 Pfizer Inc. N1-PIRAZOLOSPIROKETONSKI INHIBITORI ACETIL-CoA-KARBOKSILAZE
CU24152B1 (es) 2010-12-20 2016-02-29 Irm Llc 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr
TWI538748B (zh) * 2011-11-16 2016-06-21 鴻海精密工業股份有限公司 鏡頭除塵裝置
EP3091981B1 (en) * 2014-01-09 2021-03-10 Verastem, Inc. Compositions and methods for treatment of abnormal cell growth
JP5871294B1 (ja) * 2015-02-27 2016-03-01 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 即時放出経口錠剤
SI3397631T1 (sl) 2015-12-29 2022-01-31 Pfizer Inc. Substituirani 3-azabiciklo(3.1.0)heksani kot zaviralci ketoheksokinaze
BR112018069782A2 (pt) * 2016-03-31 2019-01-29 Lupin Ltd composição farmacêutica de dapagliflozina
AR109179A1 (es) 2016-08-19 2018-11-07 Pfizer Inhibidores de diacilglicerol aciltransferasa 2
CN106271089B (zh) 2016-09-30 2019-01-25 英诺激光科技股份有限公司 一种激光薄膜刻蚀装置及方法

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013117963A1 (en) * 2012-02-09 2013-08-15 Piramal Enterprises Limited Stable oral tablet dosage form of an antidiabetic compound
CN110325530A (zh) * 2016-12-16 2019-10-11 辉瑞大药厂 Glp-1受体激动剂及其用途

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN116675680A (zh) * 2023-08-02 2023-09-01 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
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
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

Also Published As

Publication number Publication date
WO2021191812A1 (en) 2021-09-30
TWI823072B (zh) 2023-11-21
AU2021244918A1 (en) 2022-09-29
EP4537816A3 (en) 2025-06-25
MX2022010811A (es) 2022-09-27
TW202202139A (zh) 2022-01-16
JP2025118943A (ja) 2025-08-13
JP2021155415A (ja) 2021-10-07
KR20220157486A (ko) 2022-11-29
CA3176569A1 (en) 2021-09-30
EP4537816A2 (en) 2025-04-16
US20230201185A1 (en) 2023-06-29
ES3031577T3 (en) 2025-07-09
EP4125896A1 (en) 2023-02-08
IL296694A (en) 2022-11-01
EP4125896B1 (en) 2025-05-07
BR112022017578A2 (pt) 2022-10-18

Similar Documents

Publication Publication Date Title
TWI823072B (zh) 以２－〔（４－｛６－〔（４－氰基－２－氟苄基）氧基〕吡啶－２－基｝哌啶－１－基）甲基〕－１－〔（２ｓ）－氧雜環丁烷－２－基甲基〕－１ｈ－苯並咪唑－６－甲酸或其藥學上的鹽治療第２型糖尿病或肥胖症或體重過重
JP2022001592A (ja) 代謝障害を治療するための組成物および方法
KR102856843B1 (ko) 시타글립틴, 다파글리플로진, 및 메트포르민을 포함하는 경구용 복합정제
CN104780915A (zh) 包含他汀、双胍和用于减小心脏代谢风险的其它药剂的组合物
RU2664422C2 (ru) Комбинированный препарат, содержащий гемиглиптин и метформин, и способ его получения
EP4197543A1 (en) Composition and use of sglt-2 inhibitor and angiotensin receptor blockers
AU2014207748B2 (en) Combinations of a GLP1R agonist and metformin and use thereof for the treatment of type 2 diabetes and other disorders
WO2023228023A1 (en) Treatment of type 2 diabetes or weight management control with 2-((4-((s)-2-(5-chloropyridin-2-yl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-benzo[d]imidazole-6-carboxylic acid or a pharmaceutically salt thereof
JP4408340B2 (ja) 速崩壊性固形製剤
JP2024524113A (ja) シタグリプチン、ダパグリフロジン及びメトホルミンを含む経口用複合錠剤
EP4456872A1 (en) Obicetrapib and sglt2 inhibitor combination
HK40078244A (en) 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
WO2010050422A1 (ja) 糖尿病治療剤
WO2025099561A1 (en) 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
WO2025224648A1 (en) 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
KR20160121190A (ko) 아나글립틴 또는 이의 약학적으로 허용 가능한 염 및 메트포르민 또는 이의 약학적으로 허용 가능한 염을 포함하는 약제학적 조성물 및 그의 제조 방법
HK40076733A (en) Oral complex tablet comprising sitagliptin, dapagliflozin, and metformin

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40078244

Country of ref document: HK

WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20221115

WD01 Invention patent application deemed withdrawn after publication