JP7894470B2 - ５，１０－メチレン－（６ｒ）－テトラヒドロ葉酸二ナトリウムを含む組成物 - Google Patents

５，１０－メチレン－（６ｒ）－テトラヒドロ葉酸二ナトリウムを含む組成物

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Publication number
JP7894470B2
JP7894470B2 JP2024570947A JP2024570947A JP7894470B2 JP 7894470 B2 JP7894470 B2 JP 7894470B2 JP 2024570947 A JP2024570947 A JP 2024570947A JP 2024570947 A JP2024570947 A JP 2024570947A JP 7894470 B2 JP7894470 B2 JP 7894470B2
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Prior art keywords
tetrahydrofolate
methylene
freeze
citrate
disodium salt
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JP2024570947A
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English (en)
Japanese (ja)
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JP2025518274A5 (cg-RX-API-DMAC10.html
JP2025518274A (ja
Inventor
ルドルフ モーザー、
ヴィオーラ グレーン、
トーマス アムマン、
ジーン－ピエール クナップ、
マリアン スヴァエルド、
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Patent GmbH
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Merck Patent GmbH
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Publication date
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Publication of JP2025518274A publication Critical patent/JP2025518274A/ja
Publication of JP2025518274A5 publication Critical patent/JP2025518274A5/ja
Application granted granted Critical
Publication of JP7894470B2 publication Critical patent/JP7894470B2/ja
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Classifications

    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1611—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Dermatology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2024570947A 2022-06-08 2023-06-05 ５，１０－メチレン－（６ｒ）－テトラヒドロ葉酸二ナトリウムを含む組成物 Active JP7894470B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP22177932.5 2022-06-08
EP22177932 2022-06-08
PCT/EP2023/064972 WO2023237484A1 (en) 2022-06-08 2023-06-05 Compositions comprising disodium 5,10-methylene-(6r)-tetrahydrofolate

Publications (3)

Publication Number Publication Date
JP2025518274A JP2025518274A (ja) 2025-06-12
JP2025518274A5 JP2025518274A5 (cg-RX-API-DMAC10.html) 2025-12-18
JP7894470B2 true JP7894470B2 (ja) 2026-07-23

Family

ID=81984853

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2024570947A Active JP7894470B2 (ja) 2022-06-08 2023-06-05 ５，１０－メチレン－（６ｒ）－テトラヒドロ葉酸二ナトリウムを含む組成物

Country Status (11)

Country Link
US (1) US20250360135A1 (cg-RX-API-DMAC10.html)
EP (2) EP4706775A3 (cg-RX-API-DMAC10.html)
JP (1) JP7894470B2 (cg-RX-API-DMAC10.html)
KR (1) KR20250022145A (cg-RX-API-DMAC10.html)
CN (1) CN119365186A (cg-RX-API-DMAC10.html)
AU (1) AU2023282347A1 (cg-RX-API-DMAC10.html)
CA (1) CA3258734A1 (cg-RX-API-DMAC10.html)
ES (1) ES3069418T3 (cg-RX-API-DMAC10.html)
IL (1) IL317395A (cg-RX-API-DMAC10.html)
PL (1) PL4536187T3 (cg-RX-API-DMAC10.html)
WO (1) WO2023237484A1 (cg-RX-API-DMAC10.html)

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005524655A (ja) 2002-02-26 2005-08-18 メルック・エプロバ・アクチエンゲゼルシヤフト 炎症及び炎症に関連する疾患の予防及び治療に適する、特に炎症マーカーｃｒｐ及びｓａａに影響を与えるのに適する調合物の製造にホラートを使用する方法
JP2009514776A (ja) 2003-06-26 2009-04-09 メルック・エプロバ・アクチエンゲゼルシヤフト ５，１０−メチレンテトラヒドロホラートの安定な医薬調合物
JP2009518305A (ja) 2005-12-02 2009-05-07 アドベントアールエックス ファーマシューティカルズ， インコーポレイテッド ５，１０メチレンテトラヒドロ葉酸の安定な薬学的組成物
JP2013227274A (ja) 2012-03-28 2013-11-07 Kose Corp 葉酸含有組成物及び葉酸の安定化方法
US20160074402A1 (en) 2013-04-30 2016-03-17 Aprofol Ag Stable pharmaceutical composition containing folates
JP2016528242A (ja) 2013-08-14 2016-09-15 メルク・アンド・コンパニー ５，１０−メチレン−（６ｒ）−テトラヒドロ葉酸のヘミ硫酸塩
JP2020531415A (ja) 2017-08-16 2020-11-05 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ５，１０−メチレン−（６ｒ）−テトラヒドロ葉酸を含む安定な凍結乾燥物

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1215945A (en) 1983-03-20 1986-12-30 Bengt Gustavsson Fluid transfer system
CH682664A5 (en) 1991-10-15 1993-10-29 Eprova Ag Stable salts of 5,10-methylene tetrahydrofolate.
ATE262799T1 (de) * 1996-01-31 2004-04-15 Univ South Alabama Lebensmittel und vitamin herstellungen mit natürlichem isomeren von reduzierten folaten
US10059710B2 (en) * 2016-02-17 2018-08-28 Merck & Cie Stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid
CN107892692A (zh) * 2017-12-28 2018-04-10 华东理工大学 (6s)‑5‑甲基四氢叶酸锌盐的制备方法及其应用

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005524655A (ja) 2002-02-26 2005-08-18 メルック・エプロバ・アクチエンゲゼルシヤフト 炎症及び炎症に関連する疾患の予防及び治療に適する、特に炎症マーカーｃｒｐ及びｓａａに影響を与えるのに適する調合物の製造にホラートを使用する方法
JP2009514776A (ja) 2003-06-26 2009-04-09 メルック・エプロバ・アクチエンゲゼルシヤフト ５，１０−メチレンテトラヒドロホラートの安定な医薬調合物
JP2009518305A (ja) 2005-12-02 2009-05-07 アドベントアールエックス ファーマシューティカルズ， インコーポレイテッド ５，１０メチレンテトラヒドロ葉酸の安定な薬学的組成物
JP2013227274A (ja) 2012-03-28 2013-11-07 Kose Corp 葉酸含有組成物及び葉酸の安定化方法
US20160074402A1 (en) 2013-04-30 2016-03-17 Aprofol Ag Stable pharmaceutical composition containing folates
JP2016528242A (ja) 2013-08-14 2016-09-15 メルク・アンド・コンパニー ５，１０−メチレン−（６ｒ）−テトラヒドロ葉酸のヘミ硫酸塩
JP2020531415A (ja) 2017-08-16 2020-11-05 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ ５，１０−メチレン−（６ｒ）−テトラヒドロ葉酸を含む安定な凍結乾燥物

Also Published As

Publication number Publication date
EP4536187C0 (en) 2026-01-28
EP4536187B1 (en) 2026-01-28
EP4706775A2 (en) 2026-03-11
EP4536187A1 (en) 2025-04-16
IL317395A (en) 2025-02-01
PL4536187T3 (pl) 2026-05-04
CA3258734A1 (en) 2023-12-14
WO2023237484A1 (en) 2023-12-14
AU2023282347A1 (en) 2025-01-16
EP4706775A3 (en) 2026-06-10
KR20250022145A (ko) 2025-02-14
CN119365186A (zh) 2025-01-24
ES3069418T3 (en) 2026-06-08
US20250360135A1 (en) 2025-11-27
JP2025518274A (ja) 2025-06-12

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