CN115175893A - 2-((4-((S)-2-(5-氯吡啶-2-基)-2-甲基苯并[d][1,3]二氧杂环戊烯-4-基)哌啶-1-基)甲基)-1-(((S)-氧杂环丁烷-2-基)甲基)-1H-苯并[d]咪唑-6-甲酸, 1,3-二羟基-2-(羟基甲基)丙烷-2-胺盐的固体形式 - Google Patents

2-((4-((S)-2-(5-氯吡啶-2-基)-2-甲基苯并[d][1,3]二氧杂环戊烯-4-基)哌啶-1-基)甲基)-1-(((S)-氧杂环丁烷-2-基)甲基)-1H-苯并[d]咪唑-6-甲酸, 1,3-二羟基-2-(羟基甲基)丙烷-2-胺盐的固体形式 Download PDF

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CN115175893A
CN115175893A CN202080095964.2A CN202080095964A CN115175893A CN 115175893 A CN115175893 A CN 115175893A CN 202080095964 A CN202080095964 A CN 202080095964A CN 115175893 A CN115175893 A CN 115175893A
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compound
methyl
crystalline form
disease
salt
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Chinese (zh)
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G·E·阿斯普内斯
S·W·巴利
W·D·克拉克
J·M·库尔托
D·J·埃蒙兹
M·E·弗拉纳根
二木建太郎
D·A·格里菲斯
K·华德
连亚静
C·林贝拉基斯
A·T·龙雷根
A·M·马蒂奥维茨
D·W·皮奥特罗夫斯基
R·B·鲁格里
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Pfizer Corp SRL
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Pfizer Corp SRL
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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
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    • 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
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    • 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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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN202080095964.2A 2019-12-10 2020-12-07 2-((4-((S)-2-(5-氯吡啶-2-基)-2-甲基苯并[d][1,3]二氧杂环戊烯-4-基)哌啶-1-基)甲基)-1-(((S)-氧杂环丁烷-2-基)甲基)-1H-苯并[d]咪唑-6-甲酸, 1,3-二羟基-2-(羟基甲基)丙烷-2-胺盐的固体形式 Pending CN115175893A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962946084P 2019-12-10 2019-12-10
US62/946084 2019-12-10
PCT/IB2020/061585 WO2021116874A1 (en) 2019-12-10 2020-12-07 Solid forms of 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, 1,3-dihydroxy-2-(hydroxymethyl)propan-2-amine salt

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Publication Number Publication Date
CN115175893A true CN115175893A (zh) 2022-10-11

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CN202080095964.2A Pending CN115175893A (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]二氧杂环戊烯-4-基)哌啶-1-基)甲基)-1-(((S)-氧杂环丁烷-2-基)甲基)-1H-苯并[d]咪唑-6-甲酸, 1,3-二羟基-2-(羟基甲基)丙烷-2-胺盐的固体形式

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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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CN116217522A (zh) * 2023-02-22 2023-06-06 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
WO2024217553A1 (zh) * 2023-04-21 2024-10-24 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

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MA54555A (fr) 2018-11-22 2021-09-29 Qilu Regor Therapeutics Inc Agonistes de glp-1r et leurs utilisations
US10954221B2 (en) 2019-04-12 2021-03-23 Qilu Regor Therapeutics Inc. GLP-1R agonists and uses thereof
US12065434B2 (en) 2020-12-15 2024-08-20 Pfizer Inc. Metabolites of GLP1R agonists
US20220193063A1 (en) * 2020-12-15 2022-06-23 Pfizer Inc. Metabolites of glp1r agonists
US20230150998A1 (en) 2021-09-27 2023-05-18 Terns Pharmaceuticals, Inc. Compounds as glp-1r agonists
WO2023057414A1 (en) 2021-10-05 2023-04-13 Astrazeneca Ab Certain octahydrofuro[3,4- b]pyrazines as glp-1 receptor modulators
MX2024004131A (es) 2021-10-05 2024-04-22 Astrazeneca Ab Ciertos 2,5-diazabiciclo[4.2.0]octanos como moduladores del receptor de glp-1.
US20250115612A1 (en) 2021-10-05 2025-04-10 Astrazeneca Ab Certain 2,5-diazabicyclo[4.2.0]octanes and octahydrofuro[3,4-b]pyrazines as glp-1 receptor modulators
US12024507B2 (en) 2021-10-25 2024-07-02 Terns Pharmaceuticals, Inc. Compounds as GLP-1R agonists
WO2023111144A1 (en) 2021-12-16 2023-06-22 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
WO2023111145A1 (en) 2021-12-16 2023-06-22 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
KR20240150488A (ko) 2022-02-23 2024-10-15 테른스 파마슈티칼스, 인크. Glp-1r 작용제로서의 화합물
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
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
CN117362282A (zh) * 2022-07-07 2024-01-09 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
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
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
US12291530B1 (en) 2023-11-24 2025-05-06 Ascletis Pharma (China) Co., Limited GLP-1R agonist and therapeutic method thereof

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WO2018109607A1 (en) * 2016-12-16 2018-06-21 Pfizer Inc. Glp-1 receptor agonists and uses thereof
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WO2008012623A1 (en) * 2006-07-25 2008-01-31 Pfizer Products Inc. Benzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor
WO2018109607A1 (en) * 2016-12-16 2018-06-21 Pfizer Inc. Glp-1 receptor agonists and uses thereof
WO2019239319A1 (en) * 2018-06-13 2019-12-19 Pfizer Inc. Glp-1 receptor agonists and uses thereof

Cited By (2)

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Publication number Priority date Publication date Assignee Title
CN116217522A (zh) * 2023-02-22 2023-06-06 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
WO2024217553A1 (zh) * 2023-04-21 2024-10-24 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

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JP2021091683A (ja) 2021-06-17
WO2021116874A1 (en) 2021-06-17
ZA202207589B (en) 2023-04-26
CA3163979A1 (en) 2021-06-17
TWI809334B (zh) 2023-07-21
AU2020402177A1 (en) 2022-06-16
TW202136247A (zh) 2021-10-01
US20230045419A1 (en) 2023-02-09
BR112022010599A2 (pt) 2022-08-16
AR120703A1 (es) 2022-03-09
EP4073028A1 (en) 2022-10-19
KR20220112811A (ko) 2022-08-11

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