TWI823072B - 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 - 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 Download PDF

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TWI823072B
TWI823072B TW110110639A TW110110639A TWI823072B TW I823072 B TWI823072 B TW I823072B TW 110110639 A TW110110639 A TW 110110639A TW 110110639 A TW110110639 A TW 110110639A TW I823072 B TWI823072 B TW I823072B
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compound
salt
methyl
oxy
fluorobenzyl
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TW110110639A
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TW202202139A (zh
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李開德
史威塔 曼特納
艾迪蒂 薩克塞納
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美商輝瑞股份有限公司
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    • 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
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    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
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    • 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
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    • A—HUMAN NECESSITIES
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    • 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
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    • 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
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    • 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
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    • 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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  • Obesity (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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TW110110639A 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 TWI823072B (zh)

Applications Claiming Priority (6)

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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

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TW202202139A TW202202139A (zh) 2022-01-16
TWI823072B true TWI823072B (zh) 2023-11-21

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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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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
PL4097097T3 (pl) 2020-01-29 2025-05-12 Gilead Sciences, Inc. Związki modulujące glp-1r
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
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IL306110A (en) 2021-04-21 2023-11-01 Gilead Sciences Inc Carboxy-benzimidazole glp-1r modulating compounds
JP2024541920A (ja) 2021-10-25 2024-11-13 ターンズ・ファーマシューティカルズ・インコーポレイテッド Ｇｌｐ－１ｒ作動薬としての化合物
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
KR20250166323A (ko) 2023-04-07 2025-11-27 테른스 파마슈티칼스, 인크. 간 장애 또는 심장대사 질환의 치료에 사용하기 위한 thr베타 효현제 및 glp-1r 효현제를 포함하는 조합
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
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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KR20220157486A (ko) 2022-11-29
CN115348863A (zh) 2022-11-15
EP4125896A1 (en) 2023-02-08
TW202202139A (zh) 2022-01-16
US20230201185A1 (en) 2023-06-29
AU2021244918A1 (en) 2022-09-29
CA3176569A1 (en) 2021-09-30
MX2022010811A (es) 2022-09-27
WO2021191812A1 (en) 2021-09-30
EP4537816A2 (en) 2025-04-16
JP2021155415A (ja) 2021-10-07
EP4125896B1 (en) 2025-05-07
BR112022017578A2 (pt) 2022-10-18
EP4537816A3 (en) 2025-06-25
ES3031577T3 (en) 2025-07-09
JP2025118943A (ja) 2025-08-13
IL296694A (en) 2022-11-01

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