CN115023223A - 用于治疗口服利尿剂难治性水肿的方法和组合物 - Google Patents

用于治疗口服利尿剂难治性水肿的方法和组合物 Download PDF

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Publication number
CN115023223A
CN115023223A CN202080090912.6A CN202080090912A CN115023223A CN 115023223 A CN115023223 A CN 115023223A CN 202080090912 A CN202080090912 A CN 202080090912A CN 115023223 A CN115023223 A CN 115023223A
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China
Prior art keywords
bumetanide
pharmaceutical composition
subject
administration
salt
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Pending
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CN202080090912.6A
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English (en)
Chinese (zh)
Inventor
B·拉哈克里什南
B·埃斯克
W·林
A·X·陈
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Resjoy Pharmaceuticals LLC
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Resjoy Pharmaceuticals LLC
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Publication of CN115023223A publication Critical patent/CN115023223A/zh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • 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
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K47/24Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • 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
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0021Intradermal administration, e.g. through microneedle arrays or needleless injectors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0043Nose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Inorganic Chemistry (AREA)
  • Otolaryngology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Dispersion Chemistry (AREA)
  • Molecular Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN202080090912.6A 2019-12-04 2020-12-04 用于治疗口服利尿剂难治性水肿的方法和组合物 Pending CN115023223A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962943638P 2019-12-04 2019-12-04
US62/943638 2019-12-04
PCT/US2020/063491 WO2021113775A1 (en) 2019-12-04 2020-12-04 Methods and compositions for treating edema refractory to oral diuretics

Publications (1)

Publication Number Publication Date
CN115023223A true CN115023223A (zh) 2022-09-06

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CN202080090912.6A Pending CN115023223A (zh) 2019-12-04 2020-12-04 用于治疗口服利尿剂难治性水肿的方法和组合物

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Country Link
US (5) US11123319B2 (https=)
EP (1) EP4069222A4 (https=)
JP (1) JP2023505189A (https=)
KR (1) KR20220113436A (https=)
CN (1) CN115023223A (https=)
AU (1) AU2020397176A1 (https=)
BR (1) BR112022010879A2 (https=)
CA (1) CA3160278A1 (https=)
IL (1) IL293429A (https=)
WO (1) WO2021113775A1 (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL293429A (en) 2019-12-04 2022-07-01 RESQ Pharmaceuticals LLC Methods and preparations for the treatment of edema resistant to oral diuretics
JP2024520788A (ja) * 2021-06-09 2024-05-24 レスク ファーマシューティカルズ エルエルシー 経口利尿薬に不応性の浮腫を処置するための皮下製剤及び方法
CA3225946A1 (en) 2021-07-16 2023-01-19 Hubert Clemens Pellikaan Aqueous bumetanide-containing liquid
AU2022425382A1 (en) * 2021-12-30 2024-07-11 Neuropro Therapeutics, Inc. Pharmaceutical composition
CN115645363B (zh) * 2022-10-31 2025-06-10 浙江普利药业有限公司 一种布美他尼注射液及其制备方法
WO2026017600A1 (en) 2024-07-15 2026-01-22 Dripel B.V. Aqueous bumetanide-containing liquid

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120277249A1 (en) * 2011-04-28 2012-11-01 Andersson Borje S Parenteral formulations of lipophilic pharmaceutical agents and methods for preparing and using the same
CN106572984A (zh) * 2014-06-08 2017-04-19 奥托泰里克有限责任公司 用于疼痛缓解而不引起水肿的固定的剂量组合
US20190151263A1 (en) * 2009-01-22 2019-05-23 Neuropro Therapeutics, Inc. Bumetanide analgos, compositions, and methods of use
WO2019193161A1 (en) * 2018-04-06 2019-10-10 Universität Wien Bumetanide derivatives for the therapy of stroke and other neurological diseases/disorders involving nkccs

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040105818A1 (en) 2002-11-26 2004-06-03 Alexza Molecular Delivery Corporation Diuretic aerosols and methods of making and using them
LT2523661T (lt) * 2010-01-15 2017-08-10 INSERM (Institut National de la Santé et de la Recherche Médicale) Nkcc inhibitoriai autizmo gydymui
US20140128469A1 (en) * 2011-05-10 2014-05-08 Concert Pharmaceuticals Inc. Deuterated n-butyl bumetanide
US20150239832A1 (en) * 2012-09-04 2015-08-27 Neuro Pro Therapeutics, Inc. Analogs and prodrugs of loop diuretics, including bumetanide, furosemide and piretanide; compositions and methods of use
IL293429A (en) 2019-12-04 2022-07-01 RESQ Pharmaceuticals LLC Methods and preparations for the treatment of edema resistant to oral diuretics
JP2024520788A (ja) 2021-06-09 2024-05-24 レスク ファーマシューティカルズ エルエルシー 経口利尿薬に不応性の浮腫を処置するための皮下製剤及び方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20190151263A1 (en) * 2009-01-22 2019-05-23 Neuropro Therapeutics, Inc. Bumetanide analgos, compositions, and methods of use
US20120277249A1 (en) * 2011-04-28 2012-11-01 Andersson Borje S Parenteral formulations of lipophilic pharmaceutical agents and methods for preparing and using the same
CN106572984A (zh) * 2014-06-08 2017-04-19 奥托泰里克有限责任公司 用于疼痛缓解而不引起水肿的固定的剂量组合
WO2019193161A1 (en) * 2018-04-06 2019-10-10 Universität Wien Bumetanide derivatives for the therapy of stroke and other neurological diseases/disorders involving nkccs

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
"Bumetanide 0.2mg/ml Oral Solution (PL17736/0132)", Retrieved from the Internet <URL:drugfuture.com/ukmed/search.aspx> *
H.W.NIELSEN 等: "Intranasal administration of different liquid formulations of bumetanide to rabbits", INTERNATIONAL JOURNAL OF PHARMACEUTICS, vol. 204, 31 December 2000 (2000-12-31), pages 35 - 41, XP027379985 *
WINSTON ONG 等: "Sodium and potassium salts of bumetanide trihydrate: Impact of counterion on structure, aqueous solubility and dehydration kinetics", CRYSTENGCOMM, vol. 14, 31 December 2012 (2012-12-31), pages 2428 - 2434 *

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Publication number Publication date
JP2023505189A (ja) 2023-02-08
US20250268853A1 (en) 2025-08-28
WO2021113775A8 (en) 2021-07-22
EP4069222A4 (en) 2023-12-27
US20210169833A1 (en) 2021-06-10
WO2021113775A1 (en) 2021-06-10
US11123319B2 (en) 2021-09-21
US20220287996A1 (en) 2022-09-15
US12150923B2 (en) 2024-11-26
US12558330B2 (en) 2026-02-24
KR20220113436A (ko) 2022-08-12
IL293429A (en) 2022-07-01
CA3160278A1 (en) 2021-06-10
US12329731B2 (en) 2025-06-17
EP4069222A1 (en) 2022-10-12
AU2020397176A1 (en) 2022-06-30
US20250032436A1 (en) 2025-01-30
BR112022010879A2 (pt) 2022-10-18
US11260038B1 (en) 2022-03-01

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