ES2654474T3 - Nueva sal estable del ácido 5,10-metilen-(6R)-tetrahidrofólico - Google Patents
Nueva sal estable del ácido 5,10-metilen-(6R)-tetrahidrofólico Download PDFInfo
- Publication number
- ES2654474T3 ES2654474T3 ES14758102.9T ES14758102T ES2654474T3 ES 2654474 T3 ES2654474 T3 ES 2654474T3 ES 14758102 T ES14758102 T ES 14758102T ES 2654474 T3 ES2654474 T3 ES 2654474T3
- Authority
- ES
- Spain
- Prior art keywords
- methylene
- tetrahydrofolic acid
- stable salt
- new stable
- peaks
- 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.)
- Active
Links
- 150000003839 salts Chemical class 0.000 title abstract description 5
- QYNUQALWYRSVHF-OLZOCXBDSA-N (6R)-5,10-methylenetetrahydrofolic acid Chemical compound C([C@H]1CNC=2N=C(NC(=O)C=2N1C1)N)N1C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 QYNUQALWYRSVHF-OLZOCXBDSA-N 0.000 title abstract 2
- 238000001069 Raman spectroscopy Methods 0.000 description 3
- 238000002441 X-ray diffraction Methods 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 230000005855 radiation Effects 0.000 description 3
- 238000005079 FT-Raman Methods 0.000 description 2
- 238000001228 spectrum Methods 0.000 description 2
- 238000004566 IR spectroscopy Methods 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 238000002329 infrared spectrum Methods 0.000 description 1
- 238000003836 solid-state method Methods 0.000 description 1
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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
-
- 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
- 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
- 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
- A61K9/14—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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
- C07D475/12—Heterocyclic compounds containing pteridine ring systems containing pteridine ring systems condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
- C07D475/12—Heterocyclic compounds containing pteridine ring systems containing pteridine ring systems condensed with carbocyclic rings or ring systems
- C07D475/14—Benz [g] pteridines, e.g. riboflavin
-
- 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
-
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13004050.4A EP2837631A1 (en) | 2013-08-14 | 2013-08-14 | New stable salt of 5,10-methylene-(6R)-tetrahydrofolic acid |
| EP13004050 | 2013-08-14 | ||
| PCT/EP2014/067447 WO2015022407A1 (en) | 2013-08-14 | 2014-08-14 | Hemisulfate salt of 5,10-methylene-(6r)-tetrahydrofolic acid |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2654474T3 true ES2654474T3 (es) | 2018-02-13 |
Family
ID=48998397
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES14758102.9T Active ES2654474T3 (es) | 2013-08-14 | 2014-08-14 | Nueva sal estable del ácido 5,10-metilen-(6R)-tetrahidrofólico |
| ES17190279T Active ES2871483T3 (es) | 2013-08-14 | 2014-08-14 | Sal hemisulfato del ácido 5,10-metilen-(6r)-tetrahidrofólico |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES17190279T Active ES2871483T3 (es) | 2013-08-14 | 2014-08-14 | Sal hemisulfato del ácido 5,10-metilen-(6r)-tetrahidrofólico |
Country Status (27)
| Country | Link |
|---|---|
| US (4) | US20160185787A1 (enExample) |
| EP (3) | EP2837631A1 (enExample) |
| JP (5) | JP6617104B2 (enExample) |
| KR (2) | KR102410373B1 (enExample) |
| CN (2) | CN105452250B (enExample) |
| AU (2) | AU2014307872B2 (enExample) |
| BR (2) | BR122020002802B1 (enExample) |
| CA (1) | CA2921178C (enExample) |
| CY (2) | CY1119694T1 (enExample) |
| DK (2) | DK3033344T3 (enExample) |
| EA (3) | EA202091271A3 (enExample) |
| ES (2) | ES2654474T3 (enExample) |
| HK (1) | HK1256262A1 (enExample) |
| HR (2) | HRP20171895T1 (enExample) |
| HU (2) | HUE054504T2 (enExample) |
| IL (2) | IL244069B (enExample) |
| LT (2) | LT3033344T (enExample) |
| MX (2) | MX382578B (enExample) |
| NO (1) | NO3033344T3 (enExample) |
| NZ (2) | NZ745811A (enExample) |
| PL (2) | PL3033344T3 (enExample) |
| PT (2) | PT3287460T (enExample) |
| RS (2) | RS56910B1 (enExample) |
| SG (2) | SG10201801179VA (enExample) |
| SI (2) | SI3033344T1 (enExample) |
| WO (1) | WO2015022407A1 (enExample) |
| ZA (1) | ZA201509204B (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2837631A1 (en) * | 2013-08-14 | 2015-02-18 | Merck & Cie | New stable salt of 5,10-methylene-(6R)-tetrahydrofolic acid |
| US10059710B2 (en) * | 2016-02-17 | 2018-08-28 | Merck & Cie | Stable formulations of 5,10-methylene-(6R)-tetrahydrofolic acid |
| EP3446703A1 (en) * | 2017-08-24 | 2019-02-27 | Isofol Medical AB | 6r]-mthf multiple bolus administration in 5-fluorouracil based chemotherapy |
| EP3446704A1 (en) * | 2017-08-24 | 2019-02-27 | Isofol Medical AB | [6r]-mthf - an efficient folate alternative in 5-fluorouracil based chemotherapy |
| KR102753593B1 (ko) * | 2017-08-16 | 2025-01-10 | 메르크 파텐트 게엠베하 | 5,10-메틸렌-(6r)-테트라하이드로폴산 및 디카르복시산을 포함하는 안정한 동결건조물 |
| MX2020007009A (es) * | 2018-01-05 | 2020-11-11 | Isofol Medical Ab | Metodos para tratar canceres colorrectales metastasicos y colorrectales. |
| CN115335740A (zh) * | 2020-03-30 | 2022-11-11 | 住友化学株式会社 | 层叠体 |
| CN119365186A (zh) | 2022-06-08 | 2025-01-24 | 默克专利股份有限公司 | 包含5,10-亚甲基-(6r)-四氢叶酸二钠的组合物 |
| CA3258607A1 (en) | 2022-06-08 | 2023-12-14 | Merck Patent Gmbh | STABLE PHARMACEUTICAL COMPOSITIONS COMPRISING 5,10-METHYLENE-(6R)-TETRAHYDROFOLIC ACID AND NACL |
| CN119325374A (zh) | 2022-06-08 | 2025-01-17 | 默克专利股份有限公司 | 包含5,10-亚甲基-(6r)-四氢叶酸的稳定的冻干物 |
| US20250319022A1 (en) | 2022-06-08 | 2025-10-16 | Merck Patent Gmbh | Concentrated solutions comprising sodium 5,10-methylene-(6r)-tetrahydrofolate |
| CN119325373A (zh) | 2022-06-08 | 2025-01-17 | 默克专利股份有限公司 | 包含5,10-亚甲基-(6r)-四氢叶酸的浓缩溶液 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2300505A (en) * | 1940-10-31 | 1942-11-03 | Bell Telephone Labor Inc | Selective system |
| AU575814B2 (en) | 1983-03-03 | 1988-08-11 | Bengt Gustavsson | A device for transferring a substance |
| DE3821875C1 (enExample) * | 1988-06-29 | 1990-02-15 | Eprova Ag, Forschungsinstitut, Schaffhausen, Ch | |
| 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. |
| HU226998B1 (en) * | 2000-11-23 | 2010-04-28 | Richter Gedeon Nyrt | Desloratadine hemisulphate, process for the preparation thereof and pharmaceutical compositions containing the same |
| 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. |
| KR20080074201A (ko) | 2005-12-02 | 2008-08-12 | 어드벤트륵스 파마슈티칼스, 인크. | 5,10 메틸렌테트라히드로폴레이트의 안정한 약학 조성물 |
| HRP20160950T1 (hr) | 2006-12-21 | 2016-10-07 | F. Hoffmann-La Roche Ag | Polimorfi antagonista mglur5 receptora |
| JP5294968B2 (ja) | 2009-05-01 | 2013-09-18 | 三星ダイヤモンド工業株式会社 | スクライブヘッド及び該スクライブヘッドを用いたスクライブ装置 |
| JP6069336B2 (ja) * | 2011-10-19 | 2017-02-01 | マーケイター メドシステムズ， インコーポレイテッド | 腎の脱神経を包含する治療効果を増強するための組織および細胞の局所的調節 |
| EP2837766A1 (de) * | 2013-08-14 | 2015-02-18 | Sika Technology AG | Verfahren zum Ausfüllen einer Fuge mit einem Kleb- und/oder Dichtstoff sowie System zum Ausfüllen einer Fuge mit einem Kleb- und/oder Dichtstoff |
| EP2837631A1 (en) * | 2013-08-14 | 2015-02-18 | Merck & Cie | New stable salt of 5,10-methylene-(6R)-tetrahydrofolic acid |
| JP6971761B2 (ja) * | 2017-10-11 | 2021-11-24 | 株式会社Ｉｈｉプラント | タンクの構築方法 |
-
2013
- 2013-08-14 EP EP13004050.4A patent/EP2837631A1/en not_active Withdrawn
-
2014
- 2014-08-14 SG SG10201801179VA patent/SG10201801179VA/en unknown
- 2014-08-14 LT LTEP14758102.9T patent/LT3033344T/lt unknown
- 2014-08-14 CA CA2921178A patent/CA2921178C/en active Active
- 2014-08-14 AU AU2014307872A patent/AU2014307872B2/en active Active
- 2014-08-14 EA EA202091271A patent/EA202091271A3/ru unknown
- 2014-08-14 PT PT171902794T patent/PT3287460T/pt unknown
- 2014-08-14 HU HUE17190279A patent/HUE054504T2/hu unknown
- 2014-08-14 PL PL14758102T patent/PL3033344T3/pl unknown
- 2014-08-14 BR BR122020002802-5A patent/BR122020002802B1/pt active IP Right Grant
- 2014-08-14 LT LTEP17190279.4T patent/LT3287460T/lt unknown
- 2014-08-14 SG SG11201601016PA patent/SG11201601016PA/en unknown
- 2014-08-14 RS RS20171337A patent/RS56910B1/sr unknown
- 2014-08-14 MX MX2018013134A patent/MX382578B/es unknown
- 2014-08-14 RS RS20210630A patent/RS61986B1/sr unknown
- 2014-08-14 PT PT147581029T patent/PT3033344T/pt unknown
- 2014-08-14 BR BR112016002770-1A patent/BR112016002770B1/pt active IP Right Grant
- 2014-08-14 EA EA201892729A patent/EA201892729A1/ru unknown
- 2014-08-14 KR KR1020217009189A patent/KR102410373B1/ko active Active
- 2014-08-14 ES ES14758102.9T patent/ES2654474T3/es active Active
- 2014-08-14 NZ NZ745811A patent/NZ745811A/en unknown
- 2014-08-14 PL PL17190279T patent/PL3287460T3/pl unknown
- 2014-08-14 HU HUE14758102A patent/HUE037615T2/hu unknown
- 2014-08-14 ES ES17190279T patent/ES2871483T3/es active Active
- 2014-08-14 DK DK14758102.9T patent/DK3033344T3/en active
- 2014-08-14 SI SI201430529T patent/SI3033344T1/en unknown
- 2014-08-14 HR HRP20171895TT patent/HRP20171895T1/hr unknown
- 2014-08-14 JP JP2016533926A patent/JP6617104B2/ja active Active
- 2014-08-14 WO PCT/EP2014/067447 patent/WO2015022407A1/en not_active Ceased
- 2014-08-14 SI SI201431825T patent/SI3287460T1/sl unknown
- 2014-08-14 US US14/912,328 patent/US20160185787A1/en not_active Abandoned
- 2014-08-14 NO NO14758102A patent/NO3033344T3/no unknown
- 2014-08-14 CN CN201480044477.8A patent/CN105452250B/zh active Active
- 2014-08-14 NZ NZ71782514A patent/NZ717825A/en unknown
- 2014-08-14 MX MX2016001834A patent/MX360355B/es active IP Right Grant
- 2014-08-14 KR KR1020167006595A patent/KR102439605B1/ko active Active
- 2014-08-14 DK DK17190279.4T patent/DK3287460T3/da active
- 2014-08-14 CN CN201810160334.3A patent/CN108096200A/zh active Pending
- 2014-08-14 EP EP14758102.9A patent/EP3033344B1/en active Active
- 2014-08-14 EP EP17190279.4A patent/EP3287460B1/en active Active
- 2014-08-14 EA EA201600172A patent/EA032179B1/ru not_active IP Right Cessation
-
2015
- 2015-12-17 ZA ZA2015/09204A patent/ZA201509204B/en unknown
-
2016
- 2016-02-11 IL IL244069A patent/IL244069B/en active IP Right Grant
-
2017
- 2017-12-12 CY CY20171101298T patent/CY1119694T1/el unknown
-
2018
- 2018-09-03 JP JP2018164332A patent/JP6735321B2/ja active Active
- 2018-11-29 HK HK18115320.9A patent/HK1256262A1/zh unknown
- 2018-12-06 US US16/212,056 patent/US20190106431A1/en not_active Abandoned
- 2018-12-13 AU AU2018278943A patent/AU2018278943B2/en active Active
-
2019
- 2019-04-02 JP JP2019070293A patent/JP6764501B2/ja active Active
- 2019-09-08 IL IL269170A patent/IL269170B/en active IP Right Grant
-
2020
- 2020-05-11 JP JP2020083208A patent/JP7396960B2/ja active Active
-
2021
- 2021-04-27 CY CY20211100364T patent/CY1124076T1/el unknown
- 2021-05-12 HR HRP20210743TT patent/HRP20210743T1/hr unknown
- 2021-10-08 US US17/496,939 patent/US12122783B2/en active Active
- 2021-11-11 JP JP2021183793A patent/JP7710356B2/ja active Active
-
2024
- 2024-08-09 US US18/799,606 patent/US20240400574A1/en active Pending
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