[go: up one dir, main page]

AR120703A1 - Formas sólidas de sal de 1,3-dihidroxi-2-(hidroximetil)propan-2-amina 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 - Google Patents

Formas sólidas de sal de 1,3-dihidroxi-2-(hidroximetil)propan-2-amina 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

Info

Publication number
AR120703A1
AR120703A1 ARP200103424A ARP200103424A AR120703A1 AR 120703 A1 AR120703 A1 AR 120703A1 AR P200103424 A ARP200103424 A AR P200103424A AR P200103424 A ARP200103424 A AR P200103424A AR 120703 A1 AR120703 A1 AR 120703A1
Authority
AR
Argentina
Prior art keywords
methyl
methylbenzo
oxetan
chloropyridin
dioxol
Prior art date
Application number
ARP200103424A
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.)
Filing date
Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of AR120703A1 publication Critical patent/AR120703A1/es

Links

Classifications

    • 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

Landscapes

  • 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)

Abstract

Formas cristalinas de la sal 1,3-dihidroxi-2-(hidroximetil)propan-2-amina del 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; composiciones farmacéuticas que las comprenden y el uso de las mismas para el tratamiento de la diabetes, obesidad y otros trastornos modulados por GLP-1R. Reivindicación 1: Una forma cristalina caracterizada por el hidrato 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-dihidroxi-2-(hidroximetil)propan-2-amina. Reivindicación 3: La forma cristalina de hidrato de acuerdo con la reivindicación 2, caracterizada porque la forma cristalina es la Forma 2, y en donde la Forma 2 tiene un patrón de difracción de rayos X en polvo (PXRD) que comprende al menos dos picos, en términos de 2q, a 7,1 ± 0,2º, 7,6 ± 0,2º, 10,7 ± 0,2º y 19,4 ± 0,2º. Reivindicación 6: Una forma cristalina de monohidrato (Forma 3) 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-dihidroxi-2-(hidroximetilo)propan-2-amina, caracterizada porque la Forma 3 tiene un PXRD que comprende al menos dos picos, en términos de 2q, a 3,7 ± 0,2º, 7,4 ± 0,2º, 9,9 ± 0,2º, 14,8 ± 0,2º y 20,6 ± 0,2º. Reivindicación 22: Una forma amorfa caracterizada por ser el 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-dihidroxi-2-(hidroximetil)propan-2-amina.
ARP200103424A 2019-12-10 2020-12-09 Formas sólidas de sal de 1,3-dihidroxi-2-(hidroximetil)propan-2-amina 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 AR120703A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201962946084P 2019-12-10 2019-12-10

Publications (1)

Publication Number Publication Date
AR120703A1 true AR120703A1 (es) 2022-03-09

Family

ID=73835650

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP200103424A AR120703A1 (es) 2019-12-10 2020-12-09 Formas sólidas de sal de 1,3-dihidroxi-2-(hidroximetil)propan-2-amina 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

Country Status (13)

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

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2019382642B2 (en) 2018-11-22 2025-05-29 Qilu Regor Therapeutics Inc. GLP-1R agonists and uses thereof
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
HRP20251161T1 (hr) 2021-09-27 2025-11-21 Terns Pharmaceuticals, Inc. Benzimidazol karboksilne kisele kao agonisti glp-1r
US20240417393A1 (en) 2021-10-05 2024-12-19 Astrazeneca Ab Certain 2,5-diazabicyclo[4.2.0]octanes as glp-1 receptor modulators
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
WO2023057414A1 (en) 2021-10-05 2023-04-13 Astrazeneca Ab Certain octahydrofuro[3,4- b]pyrazines as glp-1 receptor modulators
TW202334129A (zh) 2021-10-25 2023-09-01 美商拓臻製藥公司 作為ｇｌｐ—１ｒ促效劑的化合物
US20250042882A1 (en) 2021-12-16 2025-02-06 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
US20250066338A1 (en) 2021-12-16 2025-02-27 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
WO2023164050A1 (en) 2022-02-23 2023-08-31 Terns Pharmaceuticals, Inc. Compounds as glp-1r agonists
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
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
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
TW202506131A (zh) 2023-04-07 2025-02-16 美商拓臻製藥公司 ＧＬＰ－１Ｒ及ＴＨＲβ激動劑之組合以及其使用方法
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
WO2025057134A2 (en) 2023-09-14 2025-03-20 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof
US12291530B1 (en) 2023-11-24 2025-05-06 Ascletis Pharma (China) Co., Limited GLP-1R agonist and therapeutic method thereof

Family Cites Families (12)

* 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
WO2008012623A1 (en) * 2006-07-25 2008-01-31 Pfizer Products Inc. Benzimidazolyl compounds as potentiators of mglur2 subtype of glutamate receptor
PT2621493T (pt) 2010-09-30 2016-11-14 Pfizer Inibidores de n1-pirazolospirocetona acetil-coa carboxilase
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
EP3397631B1 (en) 2015-12-29 2021-04-07 Pfizer Inc Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors
AR109179A1 (es) 2016-08-19 2018-11-07 Pfizer Inhibidores de diacilglicerol aciltransferasa 2
AU2017374860B2 (en) * 2016-12-16 2021-09-02 Pfizer Inc. GLP-1 receptor agonists and uses thereof
US10934279B2 (en) * 2018-06-13 2021-03-02 Pfizer Inc. GLP-1 receptor agonists and uses thereof
CA3140972C (en) * 2019-05-20 2024-06-18 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
US20230045419A1 (en) 2023-02-09
JP2021091683A (ja) 2021-06-17
AU2020402177A1 (en) 2022-06-16
ZA202207589B (en) 2023-04-26
WO2021116874A1 (en) 2021-06-17
MX2022007105A (es) 2022-07-11
TW202136247A (zh) 2021-10-01
BR112022010599A2 (pt) 2022-08-16
CN115175893A (zh) 2022-10-11
EP4073028A1 (en) 2022-10-19
TWI809334B (zh) 2023-07-21
CA3163979A1 (en) 2021-06-17
KR20220112811A (ko) 2022-08-11

Similar Documents

Publication Publication Date Title
AR120703A1 (es) Formas sólidas de sal de 1,3-dihidroxi-2-(hidroximetil)propan-2-amina 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
PE20231438A1 (es) Proceso para hacer un inhibidor de pd-1/pd-l1 y sales y formas cristalinas del mismo
EP4563150A3 (en) New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl) isonicotinamide as raf inhibitors for the treatment of cancer
BRPI0718714B8 (pt) arilamidas substituídas por tiazol e oxazol, seu uso e composição farmacêutica que as compreende
PE20212067A1 (es) Forma cristalina de 1-(1-oxo-1,2-dihidroisoquinolin-5-il)-5-(trifluorometil)-n-(2- (trifluorometil)piridin-4-il)-1h-pirazol-4-carboxamida monohidratada
JP2010013443A5 (es)
PE20191406A1 (es) N-[4-fluoro-5-[[(2s, 4s)-2-metil-4-[(5-metil-1,2,4-oxadiazol-3-il)metoxi]-1-piperidil]metil]tiazol-2-il]acetamida como inhibidor de oga
AR084309A1 (es) Formas cristalinas de 5-cloro-n2-(2-isopropoxi-5-metil-4-piperidin-4-il-fenil)-n4-[2-(propan-2-sulfonil)-fenil]-pirimidin-2,4-diamina
RU2017127135A (ru) Терапевтическое средство против рака желчных протоков
AR106612A1 (es) Sales, formas cristalinas y composiciones farmacéuticas de 4-[2-(4-amino-piperidin-1-il)-5-(3-fluoro-4-metoxi-fenil)-1-metil-6-oxo-1,6-dihidro-pirimidin-4-il]-2-fluorobenzonitrilo como inhibidor de demetilasa 1 específica de lisina
PE20121050A1 (es) Compuestos de n-(1-(4-(1h-pirazol-5-il)ftalazin-1-il)piperidin-4-il)-benzamida sustituidos como antagonistas de la trayectoria hedgehog
AR073348A1 (es) Inhibidores ciclicos de 11 beta-hidroxiesteroide deshidrogenasa 1
AR117814A1 (es) Compuestos moduladores de fxr (nr1h4)
ES2655091T3 (es) Derivados del ácido pirrolidíncarboxílico como agonistas del receptor 43 acoplado a proteína G (GPR43), composición farmacéutica y métodos para su uso en el tratamiento de trastornos metabólicos
JP2014062126A5 (es)
BRPI0409454A (pt) compostos, processo para a sua manufatura, composições farmacêuticas que compreendem os mesmos, método para o tratamento e/ou profilaxia de enfermidades que estão associadas com o receptor de glucagon e sua utilização
CL2024000755A1 (es) Sal de calcio de ácido 2-[4-[(5,6-difenilpirazin-2-il)-propan-2-ilamino]butoxi]acético
RU2019105794A (ru) Кристаллогидрат соединения (2s, 3r) -изопропил 2 - (((2- (1,5-диметил-6-оксо-1,6-дигидропиридин-3-ил) -1 - ((тетрагидро-2h-пиран) -4-ил) метил) -1h-бензо [d] имидазол-5-ил) метил) амино) -3-гидроксибутаноат эдисилат
EA200971086A1 (ru) Фармацевтические композиции и способ лечения шизофрении
UY29393A1 (es) Nuevos derivados de amidas, sales farmacéuticas aceptables, composiciones que los contienen, procedimientos de preparación y aplicaciones.
AR056575A1 (es) Compuesto de (alfa)-aminocarboxiamida que es 5-(4-[[(2-fluorofenil) metil] oxi] fenil)prolinamida, composicion farmaceutica que lo comprende, su uso para la fabricacion de un medicamento y proceso para prepararlo
ATE485292T1 (de) Neue kristalline form von lamivudin
AR119318A1 (es) Un derivado de tetrahidroisoquinolina sustituido como modulador alostérico positivo de d1
MX2023012521A (es) Formas en estado solido de (s)-n-(3-(2-((r)-1-hidroxipropano-2-il) amino)-6-morfolinopiridin-4-il)-4-metilfenil)-3-(2,2,2-trifluoroe til)pirrolidin-1-carboxamida y sales de las mismas.
AR110251A1 (es) Una sal maleato de la base libre de n-[5-(aminosulfonil)-4-metil-1,3-tiazol-2-il]-n-metil-2-[4-(2-piridinil)-fenil]-acetamida, formulaciones farmacéuticas, métodos de fabricación y usos de la misma