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
tris 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 Inc
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Pfizer Inc
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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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  • 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)
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

Publications (1)

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 (https=)
EP (1) EP4073028A1 (https=)
JP (1) JP2021091683A (https=)
KR (1) KR20220112811A (https=)
CN (1) CN115175893A (https=)
AR (1) AR120703A1 (https=)
AU (1) AU2020402177A1 (https=)
BR (1) BR112022010599A2 (https=)
CA (1) CA3163979A1 (https=)
MX (1) MX2022007105A (https=)
TW (1) TWI809334B (https=)
WO (1) WO2021116874A1 (https=)
ZA (1) ZA202207589B (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
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

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CR20210341A (es) 2018-11-22 2021-11-25 Qilu Regor Therapeutics Inc Agonistas de glp-ir y usos de los mismos
US10954221B2 (en) 2019-04-12 2021-03-23 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
KR20240068737A (ko) 2021-09-27 2024-05-17 테른스 파마슈티칼스, 인크. Glp-1r 효능제로서의 벤즈이미다졸 카복실산
AU2022358915A1 (en) 2021-10-05 2024-05-09 Astrazeneca Ab Certain 2,5-diazabicyclo[4.2.0]octanes as glp-1 receptor modulators
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
WO2023057414A1 (en) 2021-10-05 2023-04-13 Astrazeneca Ab Certain octahydrofuro[3,4- b]pyrazines as glp-1 receptor modulators
AU2022375634A1 (en) 2021-10-25 2024-06-06 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
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
WO2023182869A1 (en) * 2022-03-25 2023-09-28 Ildong Pharmaceutical Co., Ltd. Novel salt of glp-1 receptor agonist compound, preparation method thereof and pharmaceutical composition comprising thereof
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
US20240398794A1 (en) 2023-04-07 2024-12-05 Terns Pharmaceuticals, Inc. COMBINATIONS OF GLP-1R AND THRß AGONISTS AND METHODS OF USE THEREOF
TW202521533A (zh) 2023-09-14 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
US12291530B1 (en) 2023-11-24 2025-05-06 Ascletis Pharma (China) Co., Limited GLP-1R agonist and therapeutic method thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (8)

* 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
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
SI3397631T1 (sl) 2015-12-29 2022-01-31 Pfizer Inc. Substituirani 3-azabiciklo(3.1.0)heksani kot zaviralci ketoheksokinaze
AR109179A1 (es) 2016-08-19 2018-11-07 Pfizer Inhibidores de diacilglicerol aciltransferasa 2

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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)

* Cited by examiner, † Cited by third party
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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KR20220112811A (ko) 2022-08-11
BR112022010599A2 (pt) 2022-08-16
AU2020402177A1 (en) 2022-06-16
EP4073028A1 (en) 2022-10-19
AR120703A1 (es) 2022-03-09
US20230045419A1 (en) 2023-02-09
MX2022007105A (es) 2022-07-11
TWI809334B (zh) 2023-07-21
TW202136247A (zh) 2021-10-01
WO2021116874A1 (en) 2021-06-17
JP2021091683A (ja) 2021-06-17
ZA202207589B (en) 2023-04-26

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