BR112022010599A2 - Formas sólidas de ácido 2-((4-((s)-2-(5-cloropiridin-2-il)-2-metilbenzo[d][1,3]dioxol-4-il)piperidin-1-il)metil)-1-(((s)-oxetan-2-il)metil)-1h-benzo[d]imidazol-6-carboxílico, sal de 1,3-dihidróxi-2-(hidroximetil)propan-2-amina - Google Patents

Formas sólidas de ácido 2-((4-((s)-2-(5-cloropiridin-2-il)-2-metilbenzo[d][1,3]dioxol-4-il)piperidin-1-il)metil)-1-(((s)-oxetan-2-il)metil)-1h-benzo[d]imidazol-6-carboxílico, sal de 1,3-dihidróxi-2-(hidroximetil)propan-2-amina

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Publication number
BR112022010599A2
BR112022010599A2 BR112022010599A BR112022010599A BR112022010599A2 BR 112022010599 A2 BR112022010599 A2 BR 112022010599A2 BR 112022010599 A BR112022010599 A BR 112022010599A BR 112022010599 A BR112022010599 A BR 112022010599A BR 112022010599 A2 BR112022010599 A2 BR 112022010599A2
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BR
Brazil
Prior art keywords
methyl
methylbenzo
oxetan
chloropyridin
dioxol
Prior art date
Application number
BR112022010599A
Other languages
English (en)
Inventor
E Aspnes Gary
W Bagley Scott
Dewitt Clark Wesley
M Curto John
James Edmonds David
e flanagan Mark
Futatsugi Kentaro
Andrew Griffith David
Huard Kim
Lian Yajing
Limberakis Chris
T Londregan Allyn
M Mathiowetz Alan
Walter Piotrowski David
B Ruggeri Roger
Original Assignee
Pfizer
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Filing date
Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of BR112022010599A2 publication Critical patent/BR112022010599A2/pt

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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)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

FORMAS SÓLIDAS DE ÁCIDO 2-((4-((S)-2-(5- CLOROPIRIDIN-2-IL)-2-METILBENZO[D][1,3]DIOXOL-4-IL)PIPERIDIN1IL)METIL)-1-(((S)-OXETAN-2-IL)METIL)-1H-BENZO[D]IMIDAZOL-6- CARBOXÍLICO, SAL DE 1,3-DIHIDRÓXI-2-(HIDROXIMETIL)PROPAN2-AMIN. A presente invenção refere-se a formas sólidas de ácido 2-((4-((S)-2-(5-cloropiridin-2-il)-2-metilbenzo[d][1,3]dioxol-4-il)piperidin-1-il)metil)-1-(((S)-oxetan-2-il)metil)-1H-benzo[d]imidazol-6-carboxílico, sal de 1,3-dihidróxi-2-(hidroximetil)propan-2-amina, por exemplo, uma forma cristalina de hidrato (por exemplo, um mono-hidrato) (por exemplo, Forma 2 ou Forma 3) ou uma forma amorfa; bem como composições farmacêuticas, e usos das mesmas no tratamento de doenças, condições ou distúrbios modulados por GLP-1R em um mamífero, tal como um ser humano.
BR112022010599A 2019-12-10 2020-12-07 Formas sólidas de ácido 2-((4-((s)-2-(5-cloropiridin-2-il)-2-metilbenzo[d][1,3]dioxol-4-il)piperidin-1-il)metil)-1-(((s)-oxetan-2-il)metil)-1h-benzo[d]imidazol-6-carboxílico, sal de 1,3-dihidróxi-2-(hidroximetil)propan-2-amina BR112022010599A2 (pt)

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
BR112022010599A2 true BR112022010599A2 (pt) 2022-08-16

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Family Applications (1)

Application Number Title Priority Date Filing Date
BR112022010599A BR112022010599A2 (pt) 2019-12-10 2020-12-07 Formas sólidas de ácido 2-((4-((s)-2-(5-cloropiridin-2-il)-2-metilbenzo[d][1,3]dioxol-4-il)piperidin-1-il)metil)-1-(((s)-oxetan-2-il)metil)-1h-benzo[d]imidazol-6-carboxílico, sal de 1,3-dihidróxi-2-(hidroximetil)propan-2-amina

Country Status (13)

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

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10954221B2 (en) 2019-04-12 2021-03-23 Qilu Regor Therapeutics Inc. GLP-1R agonists and uses thereof
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
CA3233131A1 (en) 2021-10-05 2023-04-13 Astrazeneca Ab Certain 2,5-diazabicyclo[4.2.0]octanes 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
WO2023111145A1 (en) 2021-12-16 2023-06-22 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
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

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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
US5013556A (en) 1989-10-20 1991-05-07 Liposome Technology, Inc. Liposomes with enhanced circulation time
WO2008012623A1 (en) * 2006-07-25 2008-01-31 Pfizer Products Inc. Benzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor
PL2621493T3 (pl) 2010-09-30 2017-01-31 Pfizer Inc. N1-pirazolospiroketonowe inhibitory karboksylazy acetylo-CoA
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
SG11201804363UA (en) 2015-12-29 2018-07-30 Pfizer Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors
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

Also Published As

Publication number Publication date
TW202136247A (zh) 2021-10-01
TWI809334B (zh) 2023-07-21
US20230045419A1 (en) 2023-02-09
JP2021091683A (ja) 2021-06-17
MX2022007105A (es) 2022-07-11
AR120703A1 (es) 2022-03-09
WO2021116874A1 (en) 2021-06-17
CN115175893A (zh) 2022-10-11
CA3163979A1 (en) 2021-06-17
KR20220112811A (ko) 2022-08-11
AU2020402177A1 (en) 2022-06-16
EP4073028A1 (en) 2022-10-19
ZA202207589B (en) 2023-04-26

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