KR102410373B1 - 5,10-메틸렌-(6r)-테트라하이드로폴산의 헤미설페이트 염 - Google Patents

5,10-메틸렌-(6r)-테트라하이드로폴산의 헤미설페이트 염 Download PDF

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KR102410373B1
KR102410373B1 KR1020217009189A KR20217009189A KR102410373B1 KR 102410373 B1 KR102410373 B1 KR 102410373B1 KR 1020217009189 A KR1020217009189 A KR 1020217009189A KR 20217009189 A KR20217009189 A KR 20217009189A KR 102410373 B1 KR102410373 B1 KR 102410373B1
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thf
water
lyophilisate
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KR20210038995A (ko
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루돌프 모세르
비올라 그로엔
토마스 에거
토마스 암만
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메르크 앤드 씨에
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    • 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
    • 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
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    • 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
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    • C—CHEMISTRY; METALLURGY
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    • 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
    • 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
    • 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

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  • Engineering & Computer Science (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)
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KR1020217009189A 2013-08-14 2014-08-14 5,10-메틸렌-(6r)-테트라하이드로폴산의 헤미설페이트 염 Active KR102410373B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP13004050.4 2013-08-14
EP13004050.4A EP2837631A1 (en) 2013-08-14 2013-08-14 New stable salt of 5,10-methylene-(6R)-tetrahydrofolic acid
PCT/EP2014/067447 WO2015022407A1 (en) 2013-08-14 2014-08-14 Hemisulfate salt of 5,10-methylene-(6r)-tetrahydrofolic acid
KR1020167006595A KR102439605B1 (ko) 2013-08-14 2014-08-14 5,10-메틸렌-(6r)-테트라하이드로폴산의 헤미설페이트 염

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
KR1020167006595A Division KR102439605B1 (ko) 2013-08-14 2014-08-14 5,10-메틸렌-(6r)-테트라하이드로폴산의 헤미설페이트 염

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Publication Number Publication Date
KR20210038995A KR20210038995A (ko) 2021-04-08
KR102410373B1 true KR102410373B1 (ko) 2022-06-22

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KR1020217009189A Active KR102410373B1 (ko) 2013-08-14 2014-08-14 5,10-메틸렌-(6r)-테트라하이드로폴산의 헤미설페이트 염
KR1020167006595A Active KR102439605B1 (ko) 2013-08-14 2014-08-14 5,10-메틸렌-(6r)-테트라하이드로폴산의 헤미설페이트 염

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US (4) US20160185787A1 (enExample)
EP (3) EP2837631A1 (enExample)
JP (5) JP6617104B2 (enExample)
KR (2) KR102410373B1 (enExample)
CN (2) CN108096200A (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) ES2871483T3 (enExample)
HK (1) HK1256262A1 (enExample)
HR (2) HRP20171895T1 (enExample)
HU (2) HUE054504T2 (enExample)
IL (2) IL244069B (enExample)
LT (2) LT3033344T (enExample)
MX (2) MX360355B (enExample)
NO (1) NO3033344T3 (enExample)
NZ (2) NZ717825A (enExample)
PL (2) PL3033344T3 (enExample)
PT (2) PT3287460T (enExample)
RS (2) RS56910B1 (enExample)
SG (2) SG11201601016PA (enExample)
SI (2) SI3033344T1 (enExample)
WO (1) WO2015022407A1 (enExample)
ZA (1) ZA201509204B (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
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
PT3668516T (pt) * 2017-08-16 2021-12-23 Merck Patent Gmbh Liofilizados estáveis que compreendem ácido 5,10-metileno-(6r)-tetra-hidrofólico e um ácido dicarboxílico
MX2020007009A (es) * 2018-01-05 2020-11-11 Isofol Medical Ab Metodos para tratar canceres colorrectales metastasicos y colorrectales.
KR20220152385A (ko) * 2020-03-30 2022-11-15 수미토모 케미칼 컴퍼니 리미티드 적층체
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
WO2023237483A1 (en) 2022-06-08 2023-12-14 Merck Patent Gmbh Concentrated solutions comprising 5,10-methylene-(6r)-tetrahydrofolic acid
KR20250022144A (ko) 2022-06-08 2025-02-14 메르크 파텐트 게엠베하 5,10-메틸렌-(6R)-테트라히드로폴산 및 NACl을 포함하는 안정한 약학적 조성물
CN119343131A (zh) 2022-06-08 2025-01-21 默克专利股份有限公司 包含5,10-亚甲基-(6r)-四氢叶酸钠的浓缩溶液
WO2023237484A1 (en) 2022-06-08 2023-12-14 Merck Patent Gmbh Compositions comprising disodium 5,10-methylene-(6r)-tetrahydrofolate

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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
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CH697021A5 (de) 2003-06-26 2008-03-31 Merck Eprova Ag Stabile pharmazeutische Zusammensetzungen von 5, 10-Methylentetrahydrofolat.
WO2007064968A2 (en) 2005-12-02 2007-06-07 Adventrx Pharmaceuticals, Inc. Stable pharmaceutical compositions of 5,10 methylenetetrahydrofolate
AU2007336369B2 (en) * 2006-12-21 2013-01-17 F. Hoffmann-La Roche Ag Polymorphs of a mGluR5 receptor antagonist
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
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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

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JP6617104B2 (ja) 2019-12-04
JP6735321B2 (ja) 2020-08-05
IL269170B (en) 2020-09-30
EP2837631A1 (en) 2015-02-18
JP2019131579A (ja) 2019-08-08
CN105452250B (zh) 2018-02-27
HK1217018A1 (zh) 2016-12-16
PT3033344T (pt) 2018-01-03
CN105452250A (zh) 2016-03-30
NZ717825A (en) 2019-11-29
KR20160043054A (ko) 2016-04-20
HUE037615T2 (hu) 2018-09-28
HRP20210743T1 (hr) 2021-06-25
US12122783B2 (en) 2024-10-22
MX2016001834A (es) 2016-04-15
KR102439605B1 (ko) 2022-09-05
EA201892729A1 (ru) 2019-04-30
MX360355B (es) 2018-10-30
JP7396960B2 (ja) 2023-12-12
BR112016002770B1 (pt) 2022-12-06
RS56910B1 (sr) 2018-05-31
CN108096200A (zh) 2018-06-01
SG10201801179VA (en) 2018-03-28
ES2654474T3 (es) 2018-02-13
SG11201601016PA (en) 2016-03-30
EP3033344B1 (en) 2017-09-27
HUE054504T2 (hu) 2021-09-28
CY1119694T1 (el) 2018-04-04
DK3287460T3 (da) 2021-05-03
HK1256262A1 (zh) 2019-09-20
EP3287460A1 (en) 2018-02-28
EA201600172A1 (ru) 2016-07-29
IL269170A (en) 2019-11-28
AU2018278943B2 (en) 2019-12-05
NZ745811A (en) 2020-05-29
EP3033344A1 (en) 2016-06-22
NO3033344T3 (enExample) 2018-02-24
PL3033344T3 (pl) 2018-02-28
US20220024940A1 (en) 2022-01-27
JP6764501B2 (ja) 2020-09-30
EP3287460B1 (en) 2021-02-24
CA2921178C (en) 2020-12-08
DK3033344T3 (en) 2017-12-18
JP2020128410A (ja) 2020-08-27
LT3287460T (lt) 2021-07-26
ES2871483T3 (es) 2021-10-29
ZA201509204B (en) 2017-04-26
EA032179B1 (ru) 2019-04-30
SI3033344T1 (en) 2018-01-31
JP7710356B2 (ja) 2025-07-18
KR20210038995A (ko) 2021-04-08
HRP20171895T1 (hr) 2018-01-26
CA2921178A1 (en) 2015-02-19
US20190106431A1 (en) 2019-04-11
MX382578B (es) 2025-03-13
IL244069B (en) 2019-09-26
PT3287460T (pt) 2021-05-27
IL244069A0 (en) 2016-04-21
US20240400574A1 (en) 2024-12-05
SI3287460T1 (sl) 2021-08-31
AU2014307872A1 (en) 2016-03-24
US20160185787A1 (en) 2016-06-30
EA202091271A2 (ru) 2020-09-30
JP2022024035A (ja) 2022-02-08
JP2018203763A (ja) 2018-12-27
WO2015022407A1 (en) 2015-02-19
PL3287460T3 (pl) 2021-07-19
JP2016528242A (ja) 2016-09-15
LT3033344T (lt) 2017-12-27
AU2018278943A1 (en) 2019-01-17
AU2014307872B2 (en) 2018-09-27
BR112016002770A2 (pt) 2017-08-01
RS61986B1 (sr) 2021-07-30
EA202091271A3 (ru) 2020-11-30
BR122020002802B1 (pt) 2022-11-29
CY1124076T1 (el) 2022-05-27

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