ZA202207589B - 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 - Google Patents

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
ZA202207589B
ZA202207589B ZA2022/07589A ZA202207589A ZA202207589B ZA 202207589 B ZA202207589 B ZA 202207589B ZA 2022/07589 A ZA2022/07589 A ZA 2022/07589A ZA 202207589 A ZA202207589 A ZA 202207589A ZA 202207589 B ZA202207589 B ZA 202207589B
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ZA
South Africa
Prior art keywords
methyl
methylbenzo
oxetan
chloropyridin
dioxol
Prior art date
Application number
ZA2022/07589A
Other languages
English (en)
Inventor
Gary E Aspnes
Scott W Bagley
Wesley Dewitt Clark
John M Curto
David James Edmonds
Mark E Flanagan
Kentaro Futatsugi
David Andrew Griffith
Kim Huard
Yajing Lian
Chris Limberakis
Allyn T Londregan
Alan M Mathiowetz
David Walter Piotrowski
Roger B Ruggeri
Original Assignee
Pfizer
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.)
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Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of ZA202207589B publication Critical patent/ZA202207589B/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02Compounds 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
    • C07C215/04Compounds 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
    • C07C215/06Compounds 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
    • C07C215/10Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
ZA2022/07589A 2019-12-10 2022-07-08 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 ZA202207589B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962946084P 2019-12-10 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
ZA202207589B true ZA202207589B (en) 2023-04-26

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Family Applications (1)

Application Number Title Priority Date Filing Date
ZA2022/07589A ZA202207589B (en) 2019-12-10 2022-07-08 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

Country Status (13)

Country Link
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=)

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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
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
PT4408840T (pt) 2021-09-27 2025-10-07 Terns Pharmaceuticals Inc Ácidos benzimidazolocarboxílicos como agonistas de glp-1r
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
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.
WO2023057414A1 (en) 2021-10-05 2023-04-13 Astrazeneca Ab Certain octahydrofuro[3,4- b]pyrazines as glp-1 receptor modulators
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
US20250042882A1 (en) 2021-12-16 2025-02-06 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
WO2023111144A1 (en) 2021-12-16 2023-06-22 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
CN119095843A (zh) 2022-02-23 2024-12-06 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
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
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
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
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
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

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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
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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
HRP20161178T1 (hr) 2010-09-30 2016-11-04 Pfizer Inc. N1-PIRAZOLOSPIROKETONSKI INHIBITORI ACETIL-CoA-KARBOKSILAZE
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AR109179A1 (es) 2016-08-19 2018-11-07 Pfizer Inhibidores de diacilglicerol aciltransferasa 2
KR102314286B1 (ko) * 2016-12-16 2021-10-21 화이자 인코포레이티드 Glp-1 수용체 작용제 및 이의 용도
US10934279B2 (en) * 2018-06-13 2021-03-02 Pfizer Inc. GLP-1 receptor agonists and uses thereof
WO2020234726A1 (en) * 2019-05-20 2020-11-26 Pfizer Inc. Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases

Also Published As

Publication number Publication date
TWI809334B (zh) 2023-07-21
JP2021091683A (ja) 2021-06-17
CA3163979A1 (en) 2021-06-17
AR120703A1 (es) 2022-03-09
TW202136247A (zh) 2021-10-01
AU2020402177A1 (en) 2022-06-16
BR112022010599A2 (pt) 2022-08-16
WO2021116874A1 (en) 2021-06-17
EP4073028A1 (en) 2022-10-19
CN115175893A (zh) 2022-10-11
MX2022007105A (es) 2022-07-11
KR20220112811A (ko) 2022-08-11
US20230045419A1 (en) 2023-02-09

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