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CU24749B1 - Método para preparar una forma cristalina de 2-[(4s)-8-fluoro-2-[4-(3-metoxifenil)piperazin-1-il]-3-[2-metoxi-5-(trifluorometil) fenil]-4h-quinazolin-4-il]acetato de sodio trihidrato - Google Patents

Método para preparar una forma cristalina de 2-[(4s)-8-fluoro-2-[4-(3-metoxifenil)piperazin-1-il]-3-[2-metoxi-5-(trifluorometil) fenil]-4h-quinazolin-4-il]acetato de sodio trihidrato

Info

Publication number
CU24749B1
CU24749B1 CU2022000049A CU20220049A CU24749B1 CU 24749 B1 CU24749 B1 CU 24749B1 CU 2022000049 A CU2022000049 A CU 2022000049A CU 20220049 A CU20220049 A CU 20220049A CU 24749 B1 CU24749 B1 CU 24749B1
Authority
CU
Cuba
Prior art keywords
quinazolin
piperazin
methoxyphenyl
trifluoromethyl
fluoro
Prior art date
Application number
CU2022000049A
Other languages
English (en)
Other versions
CU20220049A7 (es
Inventor
Helmut Buschmann
Bertran Jordi Carles Ceron
Thomas Goldner
Original Assignee
Aic246 Ag & Co Kg
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 Aic246 Ag & Co Kg filed Critical Aic246 Ag & Co Kg
Publication of CU20220049A7 publication Critical patent/CU20220049A7/es
Publication of CU24749B1 publication Critical patent/CU24749B1/es

Links

Classifications

    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • A61P31/22Antivirals for DNA viruses for herpes viruses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84Nitrogen atoms
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Virology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

<p>La presente invención se refiere a un método para preparar una forma cristalina de trihidrato de sodio del ácido 2-[(4S)-8-fluoro-2-[4-(3-metoxifenil) piperazin-1-il]-3-[2-metoxi-5-(trifluorometil)fenil]-4H-quinazolin-4-il]acético de fórmula (I):</p> <p>ESPACIO PARA FÓRMULA</p> <p>que comprende las etapas de: proporcionar una solución de concentración entre de 0,3 M y 0,7 M de ácido 2-[(4S)-8-fluoro-2-[4-(3-metoxifenil)piperazin-1-il]-3-[2-metoxi-5-(trifluorometil)fenil]-4H- quinazolin-4-il]acético en una mezcla de un acetato de alquilo (C1-C6): dialquil (C1-C6) ( 1:1 a 1:3) y en la que la temperatura de la solución está en el intervalo de 30 °C a 60 °C; añadir de 1,0 a 2,0 equivalentes molares de una solución acuosa de hidróxido de sodio basada en el contenido de ácido 2-[(4S)-8-fluoro-2-[4-(3-metoxifenil)piperazin-1-il]-3-[2-metoxi-5-(trifluorometil)fenil]-4H-quinazolin-4-il]acético con respecto a la solución resultante de la etapa 1 para proporcionar una mezcla; agitar dicha mezcla resultante a una temperatura en el intervalo de 30 °C a 60 °C para obtener una suspensión que contiene un compuesto sólido; separar el compuesto sólido de la suspensión resultante; secar el compuesto sólido obtenido a una temperatura entre 30 °C y 60 °C para obtener 2-[(4S)-8-fluoro-2-[4-(3-metoxifenil)piperazin-1-il]-3-[2-metoxi-5-(trifluorometil)fenil]-4H-quinazolin-4il]acetato de sodio trihidrato cristalino.</p>
CU2022000049A 2020-02-27 2021-03-01 Método para preparar una forma cristalina de 2-[(4s)-8-fluoro-2-[4-(3-metoxifenil)piperazin-1-il]-3-[2-metoxi-5-(trifluorometil) fenil]-4h-quinazolin-4-il]acetato de sodio trihidrato CU24749B1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP20159727 2020-02-27
PCT/EP2021/055045 WO2021170874A1 (en) 2020-02-27 2021-03-01 A method of producing a crystalline form of sodium 2-[(4s)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-4h-quinazolin-4-yl]acetate trihydrate

Publications (2)

Publication Number Publication Date
CU20220049A7 CU20220049A7 (es) 2023-04-10
CU24749B1 true CU24749B1 (es) 2025-05-05

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CU2022000049A CU24749B1 (es) 2020-02-27 2021-03-01 Método para preparar una forma cristalina de 2-[(4s)-8-fluoro-2-[4-(3-metoxifenil)piperazin-1-il]-3-[2-metoxi-5-(trifluorometil) fenil]-4h-quinazolin-4-il]acetato de sodio trihidrato

Country Status (21)

Country Link
US (1) US20230219899A1 (es)
EP (1) EP4110470A1 (es)
JP (2) JP7645276B2 (es)
KR (1) KR102889550B1 (es)
CN (1) CN115581118B (es)
AR (1) AR121439A1 (es)
AU (1) AU2021225363B2 (es)
BR (1) BR112022016929A2 (es)
CA (1) CA3169484A1 (es)
CL (1) CL2022002291A1 (es)
CO (1) CO2022012039A2 (es)
CU (1) CU24749B1 (es)
EC (1) ECSP22066680A (es)
IL (1) IL295795A (es)
MX (1) MX2022010441A (es)
PE (1) PE20230515A1 (es)
PH (1) PH12022552260A1 (es)
TW (1) TWI870559B (es)
UA (1) UA128999C2 (es)
UY (1) UY39096A (es)
WO (1) WO2021170874A1 (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025133248A1 (en) 2023-12-21 2025-06-26 Aic246 Ag & Co. Kg Diastereomeric aminoalcohol and aminoether salts of 2-[(4r,s)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-4-yl]acetic acid and their use for enantiomeric separation

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10319612A1 (de) 2003-05-02 2004-11-18 Bayer Healthcare Ag Substituierte Dihydrochinazoline
DE102012101659A1 (de) * 2012-02-29 2013-08-29 Aicuris Gmbh & Co. Kg Salze eines Dihydrochinazolinderivats

Also Published As

Publication number Publication date
MX2022010441A (es) 2022-10-18
KR20220148863A (ko) 2022-11-07
CA3169484A1 (en) 2021-09-02
JP7645276B2 (ja) 2025-03-13
US20230219899A1 (en) 2023-07-13
CN115581118A (zh) 2023-01-06
AR121439A1 (es) 2022-06-08
CN115581118B (zh) 2025-01-28
JP2023519813A (ja) 2023-05-15
IL295795A (en) 2022-10-01
WO2021170874A1 (en) 2021-09-02
ECSP22066680A (es) 2022-12-30
BR112022016929A2 (pt) 2022-12-06
CO2022012039A2 (es) 2022-11-18
TWI870559B (zh) 2025-01-21
TW202140453A (zh) 2021-11-01
AU2021225363A1 (en) 2022-10-13
AU2021225363B2 (en) 2024-09-19
CU20220049A7 (es) 2023-04-10
NZ792583A (en) 2025-07-25
CL2022002291A1 (es) 2023-02-03
JP2025016547A (ja) 2025-02-04
KR102889550B1 (ko) 2025-11-24
EP4110470A1 (en) 2023-01-04
PH12022552260A1 (en) 2023-11-13
UA128999C2 (uk) 2024-12-18
UY39096A (es) 2021-09-30
PE20230515A1 (es) 2023-03-24

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