KR102753593B1 - 5,10-메틸렌-(6r)-테트라하이드로폴산 및 디카르복시산을 포함하는 안정한 동결건조물 - Google Patents
5,10-메틸렌-(6r)-테트라하이드로폴산 및 디카르복시산을 포함하는 안정한 동결건조물 Download PDFInfo
- Publication number
- KR102753593B1 KR102753593B1 KR1020207007389A KR20207007389A KR102753593B1 KR 102753593 B1 KR102753593 B1 KR 102753593B1 KR 1020207007389 A KR1020207007389 A KR 1020207007389A KR 20207007389 A KR20207007389 A KR 20207007389A KR 102753593 B1 KR102753593 B1 KR 102753593B1
- Authority
- KR
- South Korea
- Prior art keywords
- acid
- methylene
- lyophilisate
- pharmaceutically acceptable
- tetrahydrofolic acid
- Prior art date
- Legal status (The legal status 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 status listed.)
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
- C07D475/02—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
- C07D475/04—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
-
- 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
- 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
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- 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
- A61K9/10—Dispersions; Emulsions
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
- C07C55/02—Dicarboxylic acids
- C07C55/06—Oxalic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
- C07C55/02—Dicarboxylic acids
- C07C55/10—Succinic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
- C07C57/13—Dicarboxylic acids
- C07C57/145—Maleic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
- C07C57/13—Dicarboxylic acids
- C07C57/15—Fumaric acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/235—Saturated compounds containing more than one carboxyl group
- C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
- C07C59/235—Saturated compounds containing more than one carboxyl group
- C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
- C07C59/255—Tartaric acid
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Dispersion Chemistry (AREA)
- Dermatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17186518.1 | 2017-08-16 | ||
| EP17186518 | 2017-08-16 | ||
| PCT/EP2018/072077 WO2019034673A1 (en) | 2017-08-16 | 2018-08-15 | STABLE LYOPHILISATES COMPRISING 5,10-METHYLENE- (6R) -TETRAHYDROFOLIC ACID AND DICARBOXYLIC ACID |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20200041354A KR20200041354A (ko) | 2020-04-21 |
| KR102753593B1 true KR102753593B1 (ko) | 2025-01-10 |
Family
ID=59699495
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020207007389A Active KR102753593B1 (ko) | 2017-08-16 | 2018-08-15 | 5,10-메틸렌-(6r)-테트라하이드로폴산 및 디카르복시산을 포함하는 안정한 동결건조물 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US11337978B2 (enExample) |
| EP (1) | EP3668516B1 (enExample) |
| JP (1) | JP7232815B2 (enExample) |
| KR (1) | KR102753593B1 (enExample) |
| CN (1) | CN110996958B (enExample) |
| AU (1) | AU2018317789B2 (enExample) |
| DK (1) | DK3668516T3 (enExample) |
| ES (1) | ES2902051T3 (enExample) |
| PT (1) | PT3668516T (enExample) |
| WO (1) | WO2019034673A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20250319022A1 (en) | 2022-06-08 | 2025-10-16 | Merck Patent Gmbh | Concentrated solutions comprising sodium 5,10-methylene-(6r)-tetrahydrofolate |
| EP4536186A1 (en) | 2022-06-08 | 2025-04-16 | Merck Patent GmbH | Concentrated solutions comprising 5,10-methylene-(6r)-tetrahydrofolic acid |
| EP4536188A1 (en) | 2022-06-08 | 2025-04-16 | Merck Patent GmbH | Stable lyophilisates comprising 5,10-methylene-(6r)-tetrahydrofolic acid |
| AU2023282347A1 (en) * | 2022-06-08 | 2025-01-16 | Merck Patent Gmbh | Compositions comprising disodium 5,10-methylene-(6r)-tetrahydrofolate |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA1215945A (en) | 1983-03-20 | 1986-12-30 | Bengt Gustavsson | Fluid transfer system |
| US5747469A (en) | 1991-03-06 | 1998-05-05 | Board Of Regents, The University Of Texas System | Methods and compositions comprising DNA damaging agents and p53 |
| CH682664A5 (en) | 1991-10-15 | 1993-10-29 | Eprova Ag | Stable salts of 5,10-methylene tetrahydrofolate. |
| CH684644A5 (de) | 1992-07-13 | 1994-11-15 | Eprova Ag | 5,10-Methylentetrahydrofolsäure-Cyclodextrin-Einschlussverbindungen. |
| US20020103126A1 (en) | 1997-04-18 | 2002-08-01 | Roche Diagnostics Gmbh | Stable pharmaceutical form of administration for peptides, proteins and nucleic acids |
| GB9904387D0 (en) | 1999-02-25 | 1999-04-21 | Pharmacia & Upjohn Spa | Antitumour synergistic composition |
| CH696628A5 (de) * | 2002-02-26 | 2007-08-31 | Eprova Ag | Verwendung von Folaten zur Herstellung einer Zubereitung geeignet zur Vorbeugung und Behandlung von Entzündungen und entzündungsassoziierter Krankheiten, im Speziellen zur Beeinflussung der |
| CH697021A5 (de) | 2003-06-26 | 2008-03-31 | Merck Eprova Ag | Stabile pharmazeutische Zusammensetzungen von 5, 10-Methylentetrahydrofolat. |
| CN101321518A (zh) * | 2005-12-02 | 2008-12-10 | 阿德文特克斯药物有限公司 | 5,10-亚甲基四氢叶酸盐的稳定药物组合物 |
| US20120252852A1 (en) | 2011-03-29 | 2012-10-04 | Sanofi | Otamixaban formulations with improved stability |
| JP6235779B2 (ja) * | 2012-03-28 | 2017-11-22 | 株式会社コーセー | 葉酸含有組成物及び葉酸の安定化方法 |
| EP2799061A1 (en) * | 2013-04-30 | 2014-11-05 | Aprofol AG | Stable high dose pharmaceutical composition containing folates |
| EP2837631A1 (en) | 2013-08-14 | 2015-02-18 | Merck & Cie | New stable salt of 5,10-methylene-(6R)-tetrahydrofolic acid |
| CN107812195B (zh) | 2014-09-04 | 2021-04-20 | 连云港金康和信药业有限公司 | (6s)‐5‐甲基‐四氢叶酸钙盐的稳定药物组合物 |
| US10059710B2 (en) * | 2016-02-17 | 2018-08-28 | Merck & Cie | Stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid |
-
2018
- 2018-08-15 DK DK18752161.2T patent/DK3668516T3/da active
- 2018-08-15 AU AU2018317789A patent/AU2018317789B2/en active Active
- 2018-08-15 US US16/638,528 patent/US11337978B2/en active Active
- 2018-08-15 WO PCT/EP2018/072077 patent/WO2019034673A1/en not_active Ceased
- 2018-08-15 PT PT187521612T patent/PT3668516T/pt unknown
- 2018-08-15 ES ES18752161T patent/ES2902051T3/es active Active
- 2018-08-15 EP EP18752161.2A patent/EP3668516B1/en active Active
- 2018-08-15 CN CN201880052764.1A patent/CN110996958B/zh active Active
- 2018-08-15 KR KR1020207007389A patent/KR102753593B1/ko active Active
- 2018-08-15 JP JP2020508004A patent/JP7232815B2/ja active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP7232815B2 (ja) | 2023-03-03 |
| EP3668516B1 (en) | 2021-09-22 |
| WO2019034673A1 (en) | 2019-02-21 |
| RU2020110073A3 (enExample) | 2022-01-24 |
| US11337978B2 (en) | 2022-05-24 |
| CN110996958A (zh) | 2020-04-10 |
| ES2902051T3 (es) | 2022-03-24 |
| PT3668516T (pt) | 2021-12-23 |
| CN110996958B (zh) | 2023-05-12 |
| US20200368236A1 (en) | 2020-11-26 |
| CA3073127A1 (en) | 2019-02-21 |
| EP3668516A1 (en) | 2020-06-24 |
| KR20200041354A (ko) | 2020-04-21 |
| JP2020531415A (ja) | 2020-11-05 |
| DK3668516T3 (da) | 2021-12-13 |
| RU2020110073A (ru) | 2021-09-16 |
| AU2018317789B2 (en) | 2023-06-29 |
| AU2018317789A1 (en) | 2020-04-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20200312 Patent event code: PA01051R01D Comment text: International Patent Application |
|
| PG1501 | Laying open of application | ||
| A201 | Request for examination | ||
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 20210811 Comment text: Request for Examination of Application |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
Comment text: Notification of reason for refusal Patent event date: 20240220 Patent event code: PE09021S01D |
|
| E701 | Decision to grant or registration of patent right | ||
| PE0701 | Decision of registration |
Patent event code: PE07011S01D Comment text: Decision to Grant Registration Patent event date: 20241126 |
|
| GRNT | Written decision to grant | ||
| PR0701 | Registration of establishment |
Comment text: Registration of Establishment Patent event date: 20250108 Patent event code: PR07011E01D |
|
| PR1002 | Payment of registration fee |
Payment date: 20250108 End annual number: 3 Start annual number: 1 |
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| PG1601 | Publication of registration |