CL2023001025A1 - Método de preparación de partículas cristalinas de ácido 1-(3-ciano-1-isopropil-indol-5-il)pirazol-4-carboxílico y composición farmacéutica - Google Patents

Método de preparación de partículas cristalinas de ácido 1-(3-ciano-1-isopropil-indol-5-il)pirazol-4-carboxílico y composición farmacéutica

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Publication number
CL2023001025A1
CL2023001025A1 CL2023001025A CL2023001025A CL2023001025A1 CL 2023001025 A1 CL2023001025 A1 CL 2023001025A1 CL 2023001025 A CL2023001025 A CL 2023001025A CL 2023001025 A CL2023001025 A CL 2023001025A CL 2023001025 A1 CL2023001025 A1 CL 2023001025A1
Authority
CL
Chile
Prior art keywords
crystalline particles
pharmaceutical composition
indol
pyrazole
cyano
Prior art date
Application number
CL2023001025A
Other languages
English (en)
Inventor
Seok Ju Lee
Ah Byeol Park
Hui Rak Jeong
Jinok Ham
Doosup Shin
Original Assignee
Lg Chemical Ltd
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 Lg Chemical Ltd filed Critical Lg Chemical Ltd
Publication of CL2023001025A1 publication Critical patent/CL2023001025A1/es

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    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular 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
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invención se refiere a una composición farmacéutica que comprende partículas cristalinas que comprenden el compuesto de Fórmula 1 o una sal farmacéuticamente aceptable de este que incluye el compuesto de Fórmula 2 a continuación en una cantidad de 0,2% en peso o menos. Las partículas cristalinas según la presente invención tienen un tamaño, forma y distribución que mejoran la uniformidad y fluidez, además de estar optimizado para la entrada en el proceso de preparación del medicamento terminado, lo cual aumenta la uniformidad del contenido en el proceso de preparación del producto terminado y minimiza la rotura durante la compresión en comprimidos y, por lo tanto, puede usarse como un medicamento de materia prima adecuado para el proceso de preparación del medicamento terminado.
CL2023001025A 2020-11-04 2023-04-10 Método de preparación de partículas cristalinas de ácido 1-(3-ciano-1-isopropil-indol-5-il)pirazol-4-carboxílico y composición farmacéutica CL2023001025A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
KR20200145750 2020-11-04

Publications (1)

Publication Number Publication Date
CL2023001025A1 true CL2023001025A1 (es) 2023-12-11

Family

ID=81458100

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2023001025A CL2023001025A1 (es) 2020-11-04 2023-04-10 Método de preparación de partículas cristalinas de ácido 1-(3-ciano-1-isopropil-indol-5-il)pirazol-4-carboxílico y composición farmacéutica

Country Status (15)

Country Link
US (1) US20240000750A1 (es)
EP (1) EP4218755A4 (es)
JP (1) JP2023548160A (es)
KR (1) KR20220060488A (es)
CN (1) CN116456979A (es)
AR (1) AR123999A1 (es)
AU (1) AU2021374260A1 (es)
CA (1) CA3194595A1 (es)
CL (1) CL2023001025A1 (es)
CO (1) CO2023007110A2 (es)
MX (1) MX2023004835A (es)
PE (1) PE20240139A1 (es)
TW (2) TWI848241B (es)
WO (1) WO2022098057A1 (es)
ZA (1) ZA202305840B (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112023009427A2 (pt) * 2020-12-01 2024-02-06 Lg Chemical Ltd Formulação oral que compreende ácido 1-(3-ciano-1-isopropil-indol-5-il)pirazol-4-carboxílico e método de preparação da mesma
TWI840721B (zh) * 2020-12-01 2024-05-01 南韓商Lg化學股份有限公司 用於口服投予的包含1-(3-氰基-1-異丙基-吲哚-5-基)吡唑-4-羧酸之複合調製劑和製備彼之方法
US20240216331A1 (en) * 2021-04-16 2024-07-04 Lg Chem, Ltd. Oral formulation containing 1-(3-cyano-1-isopropyl-indol-5-yl)pyrazole-4-carboxylic acid
TWI822151B (zh) * 2021-07-02 2023-11-11 南韓商Lg化學股份有限公司 製備黃嘌呤氧化酶抑制劑的方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19602505A1 (de) * 1996-01-25 1997-07-31 Merck Patent Gmbh 1-(Pyrazol-4-Indol-3-yl)-Piperidine
CA2682391C (en) * 2007-04-11 2014-07-08 Kissei Pharmaceutical Co., Ltd. (aza)indole derivative and use thereof for medical purposes
TWI423962B (zh) 2009-10-07 2014-01-21 Lg Life Sciences Ltd 有效作為黃嘌呤氧化酶抑制劑之新穎化合物、其製備方法及含該化合物之醫藥組成物
TWI548630B (zh) 2011-04-06 2016-09-11 Lg生命科學有限公司 1-(3-氰基-1-異丙基-吲哚-5-基)吡唑-4-羧酸結晶型及其製造方法
KR20200145750A (ko) 2019-06-19 2020-12-30 한국전자통신연구원 시공간 예측을 이용한 비디오 부/복호화 방법 및 장치

Also Published As

Publication number Publication date
EP4218755A1 (en) 2023-08-02
CO2023007110A2 (es) 2023-07-10
WO2022098057A1 (ko) 2022-05-12
MX2023004835A (es) 2023-05-10
TW202336015A (zh) 2023-09-16
CN116456979A (zh) 2023-07-18
PE20240139A1 (es) 2024-01-30
KR20220060488A (ko) 2022-05-11
AR123999A1 (es) 2023-02-01
AU2021374260A1 (en) 2023-06-01
JP2023548160A (ja) 2023-11-15
ZA202305840B (en) 2024-09-25
TW202225158A (zh) 2022-07-01
TWI848241B (zh) 2024-07-11
US20240000750A1 (en) 2024-01-04
EP4218755A4 (en) 2024-03-27
CA3194595A1 (en) 2022-05-12

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