TWI809334B - ２－（（４－（（Ｓ）－２－（５－氯吡啶－２－基）－２－甲基苯并〔ｄ〕〔１，３〕二氧呃－４－基）哌啶－１－基）甲基）－１－（（（Ｓ）－氧呾－２－基）甲基）－１Ｈ－苯并〔ｄ〕咪唑－６－羧酸１，３－二羥基－２－（羥基甲基）丙烷－２－胺鹽之固體形式 - Google Patents

２－（（４－（（Ｓ）－２－（５－氯吡啶－２－基）－２－甲基苯并〔ｄ〕〔１，３〕二氧呃－４－基）哌啶－１－基）甲基）－１－（（（Ｓ）－氧呾－２－基）甲基）－１Ｈ－苯并〔ｄ〕咪唑－６－羧酸１，３－二羥基－２－（羥基甲基）丙烷－２－胺鹽之固體形式 Download PDF

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TWI809334B
TWI809334B TW109143088A TW109143088A TWI809334B TW I809334 B TWI809334 B TW I809334B TW 109143088 A TW109143088 A TW 109143088A TW 109143088 A TW109143088 A TW 109143088A TW I809334 B TWI809334 B TW I809334B
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salt
compound
methyl
crystal form
torres
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TW202136247A (zh
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蓋瑞 艾斯柏尼斯
史考特 貝格里
衛斯理 克拉克
約翰 客托
大衛 艾德蒙
馬克 佛蘭根
二木建太郎
大衛 格利菲斯
金 華德
連亞靜
克里斯 林柏克斯
艾力 龍卓根
艾倫 馬西威茲
大衛 帕歐卓斯基
羅奇 路格理
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美商輝瑞股份有限公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/10—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW109143088A 2019-12-10 2020-12-07 ２－（（４－（（Ｓ）－２－（５－氯吡啶－２－基）－２－甲基苯并〔ｄ〕〔１，３〕二氧呃－４－基）哌啶－１－基）甲基）－１－（（（Ｓ）－氧呾－２－基）甲基）－１Ｈ－苯并〔ｄ〕咪唑－６－羧酸１，３－二羥基－２－（羥基甲基）丙烷－２－胺鹽之固體形式 TWI809334B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962946084P 2019-12-10 2019-12-10
US62/946,084 2019-12-10

Publications (2)

Publication Number Publication Date
TW202136247A TW202136247A (zh) 2021-10-01
TWI809334B true TWI809334B (zh) 2023-07-21

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TW109143088A TWI809334B (zh) 2019-12-10 2020-12-07 ２－（（４－（（Ｓ）－２－（５－氯吡啶－２－基）－２－甲基苯并〔ｄ〕〔１，３〕二氧呃－４－基）哌啶－１－基）甲基）－１－（（（Ｓ）－氧呾－２－基）甲基）－１Ｈ－苯并〔ｄ〕咪唑－６－羧酸１，３－二羥基－２－（羥基甲基）丙烷－２－胺鹽之固體形式

Country Status (13)

Country Link
US (1) US20230045419A1 (enExample)
EP (1) EP4073028A1 (enExample)
JP (1) JP2021091683A (enExample)
KR (1) KR20220112811A (enExample)
CN (1) CN115175893A (enExample)
AR (1) AR120703A1 (enExample)
AU (1) AU2020402177A1 (enExample)
BR (1) BR112022010599A2 (enExample)
CA (1) CA3163979A1 (enExample)
MX (1) MX2022007105A (enExample)
TW (1) TWI809334B (enExample)
WO (1) WO2021116874A1 (enExample)
ZA (1) ZA202207589B (enExample)

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AU2020256647B2 (en) 2019-04-12 2025-07-31 Qilu Regor Therapeutics Inc. GLP-1R agonists and uses thereof
US20220193063A1 (en) * 2020-12-15 2022-06-23 Pfizer Inc. Metabolites of glp1r agonists
US12065434B2 (en) 2020-12-15 2024-08-20 Pfizer Inc. Metabolites of GLP1R agonists
SI4408840T1 (sl) 2021-09-27 2025-12-31 Terns Pharmaceuticals, Inc. Benzimidazolne karboksilne kisline kot agonisti GLP-1R
WO2023057429A1 (en) 2021-10-05 2023-04-13 Astrazeneca Ab Certain 2,5-diazabicyclo[4.2.0]octanes and octahydrofuro[3,4- b]pyrazines as glp-1 receptor modulators
US20250236627A1 (en) 2021-10-05 2025-07-24 Astrazeneca Ab Certain octahydrofuro[3,4- b]pyrazines as glp-1 receptor modulators
WO2023057427A1 (en) 2021-10-05 2023-04-13 Astrazeneca Ab Certain 2,5-diazabicyclo[4.2.0]octanes as glp-1 receptor modulators
US12024507B2 (en) 2021-10-25 2024-07-02 Terns Pharmaceuticals, Inc. Compounds as GLP-1R agonists
US20250066338A1 (en) 2021-12-16 2025-02-27 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
US20250042882A1 (en) 2021-12-16 2025-02-06 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
AU2023224854A1 (en) 2022-02-23 2024-10-03 Terns Pharmaceuticals, Inc. Compounds as glp-1r agonists
CA3246495A1 (en) * 2022-03-25 2023-09-28 Ildong Pharmaceutical Co., Ltd. NEW GLP-1 RECEPTOR AGONIST COMPOUND SALT, ITS PREPARATION PROCESS AND PHARMACEUTICAL COMPOSITION INCLUDING IT
WO2023228023A1 (en) 2022-05-23 2023-11-30 Pfizer Inc. 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
CN117362282B (zh) * 2022-07-07 2026-04-21 杭州德睿智药科技有限公司 Glp-1r激动剂的盐及其制备方法和应用
CN116217522B (zh) * 2023-02-22 2025-06-24 广东莱佛士制药技术有限公司 Glp-1受体激动剂关键中间体的手性纯化方法
PE20252787A1 (es) 2023-04-07 2025-12-22 Terns Pharmaceuticals Inc Combinacion que comprende un agonista de thr-beta y un agonista de glp-1r para su uso en el tratamiento de un trastorno hepatico o una enfermedad cardiometabolica
CN118812522A (zh) * 2023-04-21 2024-10-22 苏州闻泰医药科技有限公司 一种glp-1r受体激动剂化合物盐、其晶型、其制备方法和应用
EP4777197A2 (en) 2023-09-14 2026-07-22 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof
WO2025109387A1 (en) 2023-11-24 2025-05-30 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof

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TWI707683B (zh) * 2018-06-13 2020-10-21 美商輝瑞股份有限公司 Ｇｌｐ－１受體促效劑及其用途

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TWI707683B (zh) * 2018-06-13 2020-10-21 美商輝瑞股份有限公司 Ｇｌｐ－１受體促效劑及其用途

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JP2021091683A (ja) 2021-06-17
TW202136247A (zh) 2021-10-01
BR112022010599A2 (pt) 2022-08-16
US20230045419A1 (en) 2023-02-09
CN115175893A (zh) 2022-10-11
CA3163979A1 (en) 2021-06-17
ZA202207589B (en) 2023-04-26
MX2022007105A (es) 2022-07-11
EP4073028A1 (en) 2022-10-19
AR120703A1 (es) 2022-03-09
AU2020402177A1 (en) 2022-06-16
WO2021116874A1 (en) 2021-06-17
KR20220112811A (ko) 2022-08-11

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