CL2019002464A1 - Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán. - Google Patents

Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán.

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Publication number
CL2019002464A1
CL2019002464A1 CL2019002464A CL2019002464A CL2019002464A1 CL 2019002464 A1 CL2019002464 A1 CL 2019002464A1 CL 2019002464 A CL2019002464 A CL 2019002464A CL 2019002464 A CL2019002464 A CL 2019002464A CL 2019002464 A1 CL2019002464 A1 CL 2019002464A1
Authority
CL
Chile
Prior art keywords
crystalline forms
pyrimidin
bromo
procytentan
iloxi
Prior art date
Application number
CL2019002464A
Other languages
English (en)
Inventor
Martin Bolli
Philipp Kohler
Ivan Schindelholz
Raumer Markus Von
Original Assignee
Idorsia 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 Idorsia Pharmaceuticals Ltd filed Critical Idorsia Pharmaceuticals Ltd
Publication of CL2019002464A1 publication Critical patent/CL2019002464A1/es

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    • 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
    • C07D403/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401Proline; Derivatives thereof, e.g. captopril
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035Isoindoles, e.g. phthalimide
    • 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
    • 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
    • A61K31/4418Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • A61K31/44221,4-Dihydropyridines, e.g. nifedipine, nicardipine
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/549Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • 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
    • 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)
  • 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)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)

Abstract

LA PRESENTE INVENCIÓN SE REFIERE A FORMAS CRISTALINAS NOVEDOSAS DE {5-(4-BROMO-FENIL)-6-[2-(5- BROMO-PIRIMIDIN-2-ILOXI)-ETOXI]-PIRIMIDIN-4-IL}-SULFAMIDA, PROCEDIMIENTOS PARA LA PREPARACIÓN DE LAS MISMAS, COMPOSICIONES FARMACÉUTICAS QUE COMPRENDEN DICHAS FORMAS CRISTALINAS, COMPOSICIONES FARMACÉUTICAS PREPARADAS A PARTIR DE TALES FORMAS CRISTALINAS Y SU USO COMO ANTAGONISTAS DEL RECEPTOR DE ENDOTELINA. TAMBIÉN SE REFIERE A USOS NUEVOS DE LA {5-(4-BROMO-FENIL)-6-[2-(5-BROMOPIRIMIDIN-2-ILOXI)-ETOXI]-PIRIMIDIN-4-IL}-SULFAMIDA, YA SEA SOLA O EN COMBINACIÓN CON OTROS INGREDIENTES ACTIVOS O AGENTES TERAPÉUTICOS.
CL2019002464A 2017-02-27 2019-08-27 Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán. CL2019002464A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP2017054489 2017-02-27
EP2017061487 2017-05-12

Publications (1)

Publication Number Publication Date
CL2019002464A1 true CL2019002464A1 (es) 2020-01-31

Family

ID=60268369

Family Applications (3)

Application Number Title Priority Date Filing Date
CL2019002470A CL2019002470A1 (es) 2017-02-27 2019-08-27 Combinaciones de un derivado de 4-pirimidinsulfamida con ingredientes activos para el tratamiento de enfermedades relacionadas con endotelina.
CL2019002464A CL2019002464A1 (es) 2017-02-27 2019-08-27 Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán.
CL2020001762A CL2020001762A1 (es) 2017-02-27 2020-06-30 Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán. (divisional solicitud 201902464)

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Application Number Title Priority Date Filing Date
CL2019002470A CL2019002470A1 (es) 2017-02-27 2019-08-27 Combinaciones de un derivado de 4-pirimidinsulfamida con ingredientes activos para el tratamiento de enfermedades relacionadas con endotelina.

Family Applications After (1)

Application Number Title Priority Date Filing Date
CL2020001762A CL2020001762A1 (es) 2017-02-27 2020-06-30 Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán. (divisional solicitud 201902464)

Country Status (17)

Country Link
US (5) US11174247B2 (es)
EP (3) EP3658140A1 (es)
JP (3) JP7223701B2 (es)
KR (3) KR102568472B1 (es)
CN (3) CN110325186A (es)
AU (2) AU2017400276B2 (es)
BR (2) BR112019017658A2 (es)
CA (2) CA3053991A1 (es)
CL (3) CL2019002470A1 (es)
IL (3) IL297993A (es)
MA (2) MA49664A (es)
MX (3) MX2019010222A (es)
PH (2) PH12019501937A1 (es)
SG (3) SG11201907435PA (es)
TW (2) TWI786089B (es)
UA (1) UA126122C2 (es)
WO (2) WO2018153513A1 (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
BR112020010831A2 (pt) * 2017-11-30 2020-11-10 Idorsia Pharmaceuticals Ltd composição farmacêutica, aprocitentan, e, método
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
CN112569357B (zh) * 2019-09-30 2023-03-28 深圳奥萨制药有限公司 双重内皮素受体拮抗剂与利尿剂的组合物
CN112679441A (zh) * 2019-10-18 2021-04-20 普济生物科技(台州)有限公司 阿普昔腾坦的晶型、制备方法及其用途
WO2021088645A1 (zh) * 2019-11-07 2021-05-14 苏州科睿思制药有限公司 一种Aprocitentan晶型及其制备方法和用途
WO2021237004A1 (en) 2020-05-21 2021-11-25 Teva Pharmaceuticals International Gmbh Solid state forms of aprocitentan and process for preparation thereof
KR20230038234A (ko) 2020-07-10 2023-03-17 아스트라제네카 아베 만성 신장 질환 치료를 위한 지보텐탄 및 다파글리플로진의 조합
WO2023111797A1 (en) * 2021-12-17 2023-06-22 Janssen Biotech, Inc. Pyrimidine sulfamide derivatives and process for manufacturing them
WO2023227490A1 (en) 2022-05-22 2023-11-30 Idorsia Pharmaceuticals Ltd Aprocitentan for the treatment of hypertension
WO2023227721A1 (en) 2022-05-25 2023-11-30 Idorsia Pharmaceuticals Ltd Crystalline forms of sodium (5-(4-bromophenyl)-6-(2-((5-bromopyrimidin-2-yl)oxy)ethoxy)pyrimidin-4-yl)(sulfamoyl)amide

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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
BR112020010831A2 (pt) 2017-11-30 2020-11-10 Idorsia Pharmaceuticals Ltd composição farmacêutica, aprocitentan, e, método
AU2019410727A1 (en) * 2018-12-21 2021-08-12 Actelion Pharmaceuticals Ltd Pharmaceutical composition for the treatment of pulmonary arterial hypertension

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Publication number Publication date
PH12019501938A1 (en) 2020-07-06
CA3053991A1 (en) 2018-08-30
TWI786089B (zh) 2022-12-11
TW201835071A (zh) 2018-10-01
MA47596A (fr) 2021-05-05
MX2019010222A (es) 2019-10-24
JP2023027305A (ja) 2023-03-01
JP2020508338A (ja) 2020-03-19
CN110325186A (zh) 2019-10-11
IL268850A (en) 2019-10-31
AU2017400276B2 (en) 2024-01-11
US20200002317A1 (en) 2020-01-02
CN110381948A (zh) 2019-10-25
US20200061061A1 (en) 2020-02-27
JP2020508339A (ja) 2020-03-19
KR20190121827A (ko) 2019-10-28
US20210206750A1 (en) 2021-07-08
AU2017400276A1 (en) 2019-10-17
SG11201907435PA (en) 2019-09-27
EP3585391A1 (en) 2020-01-01
KR20190119635A (ko) 2019-10-22
KR102568472B1 (ko) 2023-08-18
SG10202111695RA (en) 2021-12-30
WO2018154101A1 (en) 2018-08-30
CA3053994A1 (en) 2018-08-30
BR112019017658A2 (pt) 2020-03-31
BR112019017644A2 (pt) 2020-03-31
EP4014976A1 (en) 2022-06-22
EP3658140A1 (en) 2020-06-03
MX2021007184A (es) 2021-07-21
CL2019002470A1 (es) 2020-02-21
KR102577375B1 (ko) 2023-09-11
US10919881B2 (en) 2021-02-16
IL297993A (en) 2023-01-01
KR20230074610A (ko) 2023-05-30
UA126122C2 (uk) 2022-08-17
US20220064149A1 (en) 2022-03-03
IL268852A (en) 2019-10-31
US11787782B2 (en) 2023-10-17
PH12019501937A1 (en) 2020-07-06
US11174247B2 (en) 2021-11-16
WO2018153513A1 (en) 2018-08-30
MA49664A (fr) 2020-06-03
AU2018225309B2 (en) 2024-01-18
MX2019010221A (es) 2019-10-21
SG11201907604UA (en) 2019-09-27
AU2018225309A1 (en) 2019-10-17
JP7223701B2 (ja) 2023-02-16
CN117946011A (zh) 2024-04-30
US11680058B2 (en) 2023-06-20
US20230391757A1 (en) 2023-12-07
TW202330502A (zh) 2023-08-01
CL2020001762A1 (es) 2020-11-20

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