CL2020001762A1 - Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán. (divisional solicitud 201902464) - Google Patents

Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán. (divisional solicitud 201902464)

Info

Publication number
CL2020001762A1
CL2020001762A1 CL2020001762A CL2020001762A CL2020001762A1 CL 2020001762 A1 CL2020001762 A1 CL 2020001762A1 CL 2020001762 A CL2020001762 A CL 2020001762A CL 2020001762 A CL2020001762 A CL 2020001762A CL 2020001762 A1 CL2020001762 A1 CL 2020001762A1
Authority
CL
Chile
Prior art keywords
crystalline forms
procytentan
pyrimidin
bromo
pyrimidinesulfamide
Prior art date
Application number
CL2020001762A
Other languages
English (en)
Inventor
Raumer Markus Von
Martin Bolli
Philipp Kohler
Ivan Schindelholz
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 CL2020001762A1 publication Critical patent/CL2020001762A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/40—Heterocyclic 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
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
    • 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
    • A61K31/40—Heterocyclic 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
    • A61K31/403—Heterocyclic 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
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • 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
    • A61K31/41—Heterocyclic 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
    • 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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • A61K31/4422—1,4-Dihydropyridines, e.g. nifedipine, nicardipine
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K31/54—Heterocyclic 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
    • A61K31/549—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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)
  • 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)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)

Abstract

La presente invención se refiere a formas cristalinas de {5-(4-bromo-fenil)-6-[2-(5-bromo-pirimidin-2-iloxi)-etoxi]-pirimidin-4-il}-sulfamida, procedimientos de preparación de las mismas, composiciones farmacéuticas que las comprenden, y su uso como antagonistas del receptor de endotelina. También se refiere a usos nuevos de la {5-(4-bromo-fenil)-6-[2-(5-bromo-pirimidin-2-iloxi)-etoxi]-pirimidin-4-il}-sulfamida, ya sea sola o en combinación con otros ingredientes activos o agentes terapéuticos.
CL2020001762A 2017-02-27 2020-06-30 Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán. (divisional solicitud 201902464) CL2020001762A1 (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
CL2020001762A1 true CL2020001762A1 (es) 2020-11-20

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)

Family Applications Before (2)

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.

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) TW202330502A (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
US11174247B2 (en) 2017-02-27 2021-11-16 Idorsia Pharmaceuticals Ltd Combinations of a 4-pyrimidinesulfamide derivative with active ingredients for the treatment of endothelin related diseases
MA51203A (fr) * 2017-11-30 2020-10-07 Idorsia Pharmaceuticals Ltd Combinaison d'un dérivé de 4-pyrimidinesulfamide avec un inhibiteur de sglt-2 pour le traitement de maladies liées à l'endothéline
SG11202105098VA (en) * 2018-12-21 2021-06-29 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
CN114630668B (zh) * 2019-11-07 2024-02-27 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
US20230167090A1 (en) 2020-05-21 2023-06-01 Teva Pharmaceuticals International Gmbh Solid state forms of aprocitentan and process for preparation thereof
CN115803028A (zh) 2020-07-10 2023-03-14 阿斯利康(瑞典)有限公司 用于治疗慢性肾病的齐泊腾坦和达格列净的组合
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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DK0634175T3 (da) * 1993-07-15 2001-04-30 Hoffmann La Roche Farmaceutisk kombination, der indeholder en hæmmer af renin-angiotensin-systemet og en endothelin-antagonist
IL155805A0 (en) 2000-12-18 2003-12-23 Actelion Pharmaceuticals Ltd Novel sulfamides and their use as endothelin receptor antagonists
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PE20080991A1 (es) 2006-06-27 2008-09-05 Novartis Ag Formas de dosificacion solidas de valsartan, amlodipina e hidroclorotiazida y metodo para elaborarlas
MX2010001837A (es) 2007-08-17 2010-03-10 Actelion Pharmaceuticals Ltd Derivados de 4-pirimidinasulfamida.
JP2010536880A (ja) 2007-08-22 2010-12-02 ギリード・コロラド・インコーポレーテッド 糖尿病の合併症のための療法
CN102614189B (zh) * 2012-04-17 2014-10-22 北京哈三联科技股份有限公司 含缬沙坦、氨氯地平和氢氯噻嗪的微丸药物组合
EP2907811A1 (en) 2014-02-14 2015-08-19 Actelion Pharmaceuticals Ltd. Process for manufacturing pyrimidine sulfamide derivatives
CA2966756A1 (en) 2014-11-07 2016-05-12 Donald K. Kohan Methods of treating ckd using predictors of fluid retention
WO2017185142A1 (en) 2016-04-29 2017-11-02 Adelaide Research & Innovation Pty Ltd Method for preventing and/or treating atrial fibrillation
US11174247B2 (en) 2017-02-27 2021-11-16 Idorsia Pharmaceuticals Ltd Combinations of a 4-pyrimidinesulfamide derivative with active ingredients for the treatment of endothelin related diseases
MA51203A (fr) 2017-11-30 2020-10-07 Idorsia Pharmaceuticals Ltd Combinaison d'un dérivé de 4-pyrimidinesulfamide avec un inhibiteur de sglt-2 pour le traitement de maladies liées à l'endothéline
SG11202105098VA (en) * 2018-12-21 2021-06-29 Actelion Pharmaceuticals Ltd Pharmaceutical composition for the treatment of pulmonary arterial hypertension

Also Published As

Publication number Publication date
WO2018154101A1 (en) 2018-08-30
AU2017400276A1 (en) 2019-10-17
CN110325186A (zh) 2019-10-11
CL2019002464A1 (es) 2020-01-31
US11680058B2 (en) 2023-06-20
JP2020508338A (ja) 2020-03-19
EP4014976A1 (en) 2022-06-22
KR102568472B1 (ko) 2023-08-18
CN110381948A (zh) 2019-10-25
CN117946011A (zh) 2024-04-30
JP7223701B2 (ja) 2023-02-16
US20230391757A1 (en) 2023-12-07
MX2019010222A (es) 2019-10-24
KR102577375B1 (ko) 2023-09-11
US10919881B2 (en) 2021-02-16
MA49664A (fr) 2020-06-03
SG11201907435PA (en) 2019-09-27
KR20190121827A (ko) 2019-10-28
SG11201907604UA (en) 2019-09-27
KR20230074610A (ko) 2023-05-30
BR112019017658A2 (pt) 2020-03-31
SG10202111695RA (en) 2021-12-30
JP2023027305A (ja) 2023-03-01
CA3053991A1 (en) 2018-08-30
WO2018153513A1 (en) 2018-08-30
MA47596A (fr) 2021-05-05
IL268850A (en) 2019-10-31
MX2021007184A (es) 2021-07-21
US20210206750A1 (en) 2021-07-08
PH12019501938A1 (en) 2020-07-06
US11787782B2 (en) 2023-10-17
PH12019501937A1 (en) 2020-07-06
KR20190119635A (ko) 2019-10-22
US20220064149A1 (en) 2022-03-03
BR112019017644A2 (pt) 2020-03-31
TW201835071A (zh) 2018-10-01
AU2018225309B2 (en) 2024-01-18
CA3053994A1 (en) 2018-08-30
MX2019010221A (es) 2019-10-21
US20200002317A1 (en) 2020-01-02
UA126122C2 (uk) 2022-08-17
EP3658140A1 (en) 2020-06-03
CL2019002470A1 (es) 2020-02-21
US20200061061A1 (en) 2020-02-27
EP3585391A1 (en) 2020-01-01
AU2018225309A1 (en) 2019-10-17
US11174247B2 (en) 2021-11-16
AU2017400276B2 (en) 2024-01-11
TWI786089B (zh) 2022-12-11
TW202330502A (zh) 2023-08-01
IL297993A (en) 2023-01-01
JP2020508339A (ja) 2020-03-19
IL268852A (en) 2019-10-31

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