CO2021011046A2 - Composición farmacéutica que comprende macitentán para el tratamiento de la hipertensión pulmonar tromboembólica crónica - Google Patents

Composición farmacéutica que comprende macitentán para el tratamiento de la hipertensión pulmonar tromboembólica crónica

Info

Publication number
CO2021011046A2
CO2021011046A2 CONC2021/0011046A CO2021011046A CO2021011046A2 CO 2021011046 A2 CO2021011046 A2 CO 2021011046A2 CO 2021011046 A CO2021011046 A CO 2021011046A CO 2021011046 A2 CO2021011046 A2 CO 2021011046A2
Authority
CO
Colombia
Prior art keywords
macitentan
treatment
aprocitentan
cteph
prevention
Prior art date
Application number
CONC2021/0011046A
Other languages
English (en)
Inventor
Dénes Csonka
Wassim Fares
Hans Hoogkamer
Koen Torfs
Original Assignee
Actelion Pharmaceuticals 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 Actelion Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Publication of CO2021011046A2 publication Critical patent/CO2021011046A2/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
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/2027Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)

Abstract

La presente invención se relaciona con dosis elevadas de macitentán (INN), es decir, ácido propilsulfámico [5-(4-bromo-fenil)-6-[2-(5-bromo-pirimidin-2-iloxi)-etoxi]-pirimidin-4-il]-amida o sales farmacéuticamente aceptables, solvatos, hidratos o formas morfológicas de este, o de aprocitentán, para uso en el tratamiento y/o la prevención de la hipertensión pulmonar tromboembólica crónica (HPTEC). Además, la presente invención se relaciona con el uso de dosis elevadas de macitentán o de aprocitentán para la elaboración de un medicamento para el tratamiento y/o la prevención de la HPTEC, así como con un método para el tratamiento y/o la prevención de la HPTEC que comprende administrar dosis elevadas de macitentán o de aprocitentán a un paciente. Adicionalmente, la presente invención se relaciona con un régimen de dosificación para el tratamiento y/o la prevención de la HAP así como con una combinación de macitentán, o de aprocitentán, con uno o más inhibidores de la fosfodiesterasa tipo 5 (PDE5), análogos de prostaciclina, agonistas del receptor de prostaciclina o estimuladores de la guanilato ciclasa solubles. Además, la presente invención se relaciona con una composición farmacéutica para el tratamiento de la HPTEC que comprende una dosis elevada de macitentán o de aprocitentán.
CONC2021/0011046A 2019-01-25 2021-08-23 Composición farmacéutica que comprende macitentán para el tratamiento de la hipertensión pulmonar tromboembólica crónica CO2021011046A2 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP2019051874 2019-01-25
EP2019060152 2019-04-18
EP2019066495 2019-06-21
EP2019067187 2019-06-27
PCT/EP2020/051707 WO2020152308A1 (en) 2019-01-25 2020-01-24 Pharmaceutical composition comprising macitentan for the treatment of chronic thromboembolic pulmonary hypertension

Publications (1)

Publication Number Publication Date
CO2021011046A2 true CO2021011046A2 (es) 2022-01-17

Family

ID=69177170

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2021/0011046A CO2021011046A2 (es) 2019-01-25 2021-08-23 Composición farmacéutica que comprende macitentán para el tratamiento de la hipertensión pulmonar tromboembólica crónica

Country Status (17)

Country Link
US (2) US20220096474A1 (es)
EP (1) EP3914253A1 (es)
JP (1) JP2022522612A (es)
KR (1) KR20210120024A (es)
CN (1) CN113329751A (es)
AU (1) AU2020211014A1 (es)
BR (1) BR112021014499A2 (es)
CA (1) CA3127271A1 (es)
CL (1) CL2021001933A1 (es)
CO (1) CO2021011046A2 (es)
IL (1) IL284988A (es)
JO (1) JOP20210198A1 (es)
MA (1) MA54809A (es)
MX (1) MX2021008574A (es)
SG (1) SG11202106312SA (es)
TW (1) TW202042818A (es)
WO (1) WO2020152308A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2019410727A1 (en) 2018-12-21 2021-08-12 Actelion Pharmaceuticals Ltd Pharmaceutical composition for the treatment of pulmonary arterial hypertension
TW202042818A (zh) * 2019-01-25 2020-12-01 瑞士商艾克泰聯製藥有限公司 用於治療慢性血栓性肺高血壓之醫藥組成物

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4245130B2 (ja) 2000-12-18 2009-03-25 アクテリオン ファーマシューティカルズ リミテッド 新規なスルファミド類
AU2006290309B2 (en) 2005-09-12 2012-04-05 Actelion Pharmaceuticals Ltd. Stable pharmaceutical composition comprising a pyrimidine-sulfamide
AR062501A1 (es) 2006-08-29 2008-11-12 Actelion Pharmaceuticals Ltd Composiciones terapeuticas
MX2010001837A (es) 2007-08-17 2010-03-10 Actelion Pharmaceuticals Ltd Derivados de 4-pirimidinasulfamida.
PL2315587T3 (pl) 2008-08-13 2018-03-30 Actelion Pharmaceuticals Ltd. Kompozycje terapeutyczne zawierające macitentan
EP3538154A1 (en) 2016-11-10 2019-09-18 Arena Pharmaceuticals, Inc. Methods of treating pah with combinations of ralinepag and other agents
WO2018153925A1 (en) * 2017-02-22 2018-08-30 Amneal Pharmaceuticals Company Gmbh Stable pharmaceutical compositions comprising macitentan
MA49664A (fr) 2017-02-27 2020-06-03 Idorsia Pharmaceuticals Ltd Combinaisons d'un dérivé de 4-pyrimidinesulfamide avec des principes actifs pour le traitement de maladies liées à l'endothéline
AU2019410727A1 (en) * 2018-12-21 2021-08-12 Actelion Pharmaceuticals Ltd Pharmaceutical composition for the treatment of pulmonary arterial hypertension
TW202042818A (zh) * 2019-01-25 2020-12-01 瑞士商艾克泰聯製藥有限公司 用於治療慢性血栓性肺高血壓之醫藥組成物
TW202103703A (zh) 2019-04-05 2021-02-01 瑞士商艾克泰聯製藥有限公司 用於治療門脈肺高血壓之方法
CN114727951A (zh) 2019-11-26 2022-07-08 埃科特莱茵药品有限公司 用于治疗房坦姑息术后患者中的肺血管疾病和/或心功能障碍的药物组合物

Also Published As

Publication number Publication date
CA3127271A1 (en) 2020-07-30
SG11202106312SA (en) 2021-07-29
MA54809A (fr) 2022-04-20
JOP20210198A1 (ar) 2023-01-30
AU2020211014A1 (en) 2021-09-16
MX2021008574A (es) 2021-08-11
BR112021014499A2 (pt) 2021-09-28
CL2021001933A1 (es) 2022-04-08
CN113329751A (zh) 2021-08-31
WO2020152308A1 (en) 2020-07-30
TW202042818A (zh) 2020-12-01
JP2022522612A (ja) 2022-04-20
IL284988A (en) 2021-09-30
KR20210120024A (ko) 2021-10-06
EP3914253A1 (en) 2021-12-01
US20220096474A1 (en) 2022-03-31
US11612600B2 (en) 2023-03-28
US20220331319A1 (en) 2022-10-20

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