IL268850B2 - Combinations of 4-pyrimidinsulfamide derivatives with active ingredients for the treatment of endothelin-related diseases - Google Patents

Combinations of 4-pyrimidinsulfamide derivatives with active ingredients for the treatment of endothelin-related diseases

Info

Publication number
IL268850B2
IL268850B2 IL268850A IL26885019A IL268850B2 IL 268850 B2 IL268850 B2 IL 268850B2 IL 268850 A IL268850 A IL 268850A IL 26885019 A IL26885019 A IL 26885019A IL 268850 B2 IL268850 B2 IL 268850B2
Authority
IL
Israel
Prior art keywords
aprocitentan
pharmaceutically acceptable
acceptable salt
pharmaceutical composition
hypertension
Prior art date
Application number
IL268850A
Other languages
English (en)
Hebrew (he)
Other versions
IL268850B1 (en
IL268850A (en
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=60268369&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=IL268850(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Idorsia Pharmaceuticals Ltd filed Critical Idorsia Pharmaceuticals Ltd
Publication of IL268850A publication Critical patent/IL268850A/en
Publication of IL268850B1 publication Critical patent/IL268850B1/en
Publication of IL268850B2 publication Critical patent/IL268850B2/en

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Classifications

    • 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
    • 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
    • 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
    • A61K31/40—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
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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
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    • A—HUMAN NECESSITIES
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    • 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
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
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    • 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

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  • Health & Medical Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • 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)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (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)
IL268850A 2017-02-27 2017-11-06 Combinations of 4-pyrimidinsulfamide derivatives with active ingredients for the treatment of endothelin-related diseases IL268850B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP2017054489 2017-02-27
EP2017061487 2017-05-12
PCT/EP2017/078371 WO2018153513A1 (en) 2017-02-27 2017-11-06 Combinations of a 4-pyrimidinesulfamide derivative with active ingredients for the treatment of endothelin related diseases

Publications (3)

Publication Number Publication Date
IL268850A IL268850A (en) 2019-10-31
IL268850B1 IL268850B1 (en) 2024-10-01
IL268850B2 true IL268850B2 (en) 2025-02-01

Family

ID=60268369

Family Applications (4)

Application Number Title Priority Date Filing Date
IL268850A IL268850B2 (en) 2017-02-27 2017-11-06 Combinations of 4-pyrimidinsulfamide derivatives with active ingredients for the treatment of endothelin-related diseases
IL315563A IL315563A (en) 2017-02-27 2017-11-06 Combinations of a 4-pyrimidinesulfamide derivative with active ingredients for the treatment of endothelin related diseases
IL297993A IL297993B2 (en) 2017-02-27 2018-02-26 Combination of aprocitantan and valsartan for use in the treatment of chronic/end-stage kidney disease
IL26885219A IL268852A (en) 2017-02-27 2019-08-22 Crystalline forms of the 4-pyrimidinesulfamide derivative aprocitentan

Family Applications After (3)

Application Number Title Priority Date Filing Date
IL315563A IL315563A (en) 2017-02-27 2017-11-06 Combinations of a 4-pyrimidinesulfamide derivative with active ingredients for the treatment of endothelin related diseases
IL297993A IL297993B2 (en) 2017-02-27 2018-02-26 Combination of aprocitantan and valsartan for use in the treatment of chronic/end-stage kidney disease
IL26885219A IL268852A (en) 2017-02-27 2019-08-22 Crystalline forms of the 4-pyrimidinesulfamide derivative aprocitentan

Country Status (29)

Country Link
US (5) US11174247B2 (enExample)
EP (3) EP3658140B1 (enExample)
JP (3) JP7223701B2 (enExample)
KR (3) KR102700778B1 (enExample)
CN (3) CN110325186A (enExample)
AU (2) AU2017400276B2 (enExample)
BR (2) BR112019017658A2 (enExample)
CA (2) CA3053991A1 (enExample)
CL (3) CL2019002464A1 (enExample)
DK (2) DK3658140T3 (enExample)
ES (2) ES3038007T3 (enExample)
FI (2) FI3658140T3 (enExample)
HR (2) HRP20250921T1 (enExample)
HU (2) HUE072288T2 (enExample)
IL (4) IL268850B2 (enExample)
LT (2) LT3658140T (enExample)
MA (2) MA49664A (enExample)
MX (3) MX392313B (enExample)
MY (2) MY199557A (enExample)
NZ (1) NZ757344A (enExample)
PH (2) PH12019501938A1 (enExample)
PL (2) PL3658140T3 (enExample)
PT (2) PT3658140T (enExample)
RS (2) RS67082B1 (enExample)
SG (3) SG11201907435PA (enExample)
SI (2) SI3658140T1 (enExample)
TW (2) TWI786089B (enExample)
UA (1) UA126122C2 (enExample)
WO (2) WO2018153513A1 (enExample)

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WO2016025671A2 (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
SI3658140T1 (sl) 2017-02-27 2025-08-29 Idorsia Pharmaceuticals Ltd Kombinacije aprocitentana z nadaljnjimi učinkovinami za zdravljenje rezistentne hipertenzije
EP3716979B1 (en) * 2017-11-30 2025-04-09 Idorsia Pharmaceuticals Ltd Combination of a 4-pyrimidinesulfamide derivative with an sglt-2 inhibitor for the treatment of endothelin related diseases
JP7312262B2 (ja) 2018-09-28 2023-07-20 フロー メディカル コーポレイション カテーテル装置
BR112021011999A2 (pt) 2018-12-21 2021-09-08 Actelion Pharmaceuticals Ltd Composição farmacêutica para o tratamento de hipertensão arterial pulmonar
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
EP4056182A1 (en) * 2019-11-07 2022-09-14 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystal form of aprocitentan, preparation method therefor and use thereof
US12421214B2 (en) 2020-05-21 2025-09-23 Assia Chemical Industries Ltd. Solid state forms of aprocitentan and process for preparation thereof
PH12023550025A1 (en) 2020-07-10 2024-03-11 Astrazeneca Ab Combination of zibotentan and dapagliflozin for the treatment of chronic kidney disease
CN114644595A (zh) * 2020-12-19 2022-06-21 普济生物科技（台州）有限公司 阿普昔腾坦的无定型态、其药物组合物和用途
WO2023111797A1 (en) * 2021-12-17 2023-06-22 Janssen Biotech, Inc. Pyrimidine sulfamide derivatives and process for manufacturing them
CN119255805A (zh) 2022-05-22 2025-01-03 爱杜西亚药品有限公司 用于治疗高血压的阿普昔腾坦
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
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
KR20250152723A (ko) 2024-04-16 2025-10-24 경북대학교 산학협력단 신규한 피리미딘 유도체 화합물 및 이의 용도

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