CL2019002464A1 - Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán. - Google Patents
Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán.Info
- 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
Links
- -1 4-BROMO-PHENYL Chemical class 0.000 abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 abstract 2
- 102000010180 Endothelin receptor Human genes 0.000 abstract 1
- 108050001739 Endothelin receptor Proteins 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
-
- A—HUMAN NECESSITIES
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- 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)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Ophthalmology & Optometry (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Gynecology & Obstetrics (AREA)
- Reproductive Health (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Physiology (AREA)
- Nutrition Science (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.
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 |
---|---|---|---|
CL2019002464A CL2019002464A1 (es) | 2017-02-27 | 2019-08-27 | Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán. |
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. |
CL2020001762A CL2020001762A1 (es) | 2017-02-27 | 2020-06-30 | Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán. (divisional solicitud 201902464) |
Family Applications After (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. |
CL2020001762A CL2020001762A1 (es) | 2017-02-27 | 2020-06-30 | Formas cristalinas del derivado de 4-pirimidinsulfamida de aprocitentán. (divisional solicitud 201902464) |
Country Status (28)
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) | CL2019002464A1 (es) |
DK (1) | DK4014976T3 (es) |
ES (1) | ES3006308T3 (es) |
FI (1) | FI4014976T3 (es) |
HR (1) | HRP20241461T1 (es) |
HU (1) | HUE069231T2 (es) |
IL (4) | IL268850B2 (es) |
LT (1) | LT4014976T (es) |
MA (2) | MA49664A (es) |
MX (3) | MX2019010222A (es) |
MY (1) | MY199557A (es) |
PH (2) | PH12019501938A1 (es) |
PL (1) | PL4014976T3 (es) |
PT (1) | PT4014976T (es) |
RS (1) | RS66200B1 (es) |
SG (3) | SG11201907435PA (es) |
SI (1) | SI4014976T1 (es) |
TW (2) | TWI786089B (es) |
UA (1) | UA126122C2 (es) |
WO (2) | WO2018153513A1 (es) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
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US20160045527A1 (en) * | 2014-08-14 | 2016-02-18 | Vivus, Inc. | Treatment of sleep apnea with a combination of a carbonic anhydrase inhibitor and an aldosterone antagonist |
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 |
US12144811B2 (en) | 2017-11-30 | 2024-11-19 | Idorsia Pharmaceuticals Ltd | Combination of a 4-pyrimidinesulfamide derivative with an SGLT-2 inhibitor for the treatment of endothelin related diseases |
EP3856318A4 (en) | 2018-09-28 | 2022-06-15 | Flow Medical Corporation | CATHETER DEVICE |
DK3897646T3 (da) | 2018-12-21 | 2024-07-01 | Actelion Pharmaceuticals Ltd | Macitentan til behandling af pulmonal arteriel 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 |
EP4153574A1 (en) | 2020-05-21 | 2023-03-29 | Teva Pharmaceuticals International GmbH | Solid state forms of aprocitentan and process for preparation thereof |
BR112023000406A2 (pt) | 2020-07-10 | 2023-01-31 | Astrazeneca Ab | Combinação de zibotentan e dapagliflozina |
WO2023111797A1 (en) * | 2021-12-17 | 2023-06-22 | Janssen Biotech, Inc. | Pyrimidine sulfamide derivatives and process for manufacturing them |
IL317076A (en) | 2022-05-22 | 2025-01-01 | Idorsia Pharmaceuticals Ltd | Aprociten for the treatment of hypertension |
CN119255985A (zh) | 2022-05-25 | 2025-01-03 | 爱杜西亚药品有限公司 | (5-(4-溴苯基)-6-(2-((5-溴嘧啶-2-基)氧基)乙氧基)嘧啶-4-基)(氨磺酰基)酰胺钠的结晶形式 |
WO2024140425A1 (zh) * | 2022-12-30 | 2024-07-04 | 苏州科睿思制药有限公司 | 一种阿普昔腾坦晶型及其制备方法和用途 |
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ATE198551T1 (de) * | 1993-07-15 | 2001-01-15 | Hoffmann La Roche | Pharmazeutische kombination, die einen hemmer des renin-angiotensin-systems und einen endothelin- antagonisten enthält |
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 |
EG24716A (en) | 2002-05-17 | 2010-06-07 | Novartis Ag | Combination of organic compounds |
US20070196510A1 (en) | 2006-02-17 | 2007-08-23 | Gerber Michael J | Method for treating resistant hypertension |
US20070293552A1 (en) | 2006-06-15 | 2007-12-20 | Gorczynski Richard J | Antihypertensive therapy method |
PE20120542A1 (es) | 2006-06-27 | 2012-05-14 | 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. |
EP2545920A1 (en) * | 2007-08-22 | 2013-01-16 | Abbott GmbH & Co. KG | Therapy for complications of diabetes |
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 |
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