BR112016002770B1 - Sal de hemissulfato de ácido 5,10-metileno-(6r)-tetra-hidrofólico, sua composição farmacêutica e seu uso - Google Patents

Sal de hemissulfato de ácido 5,10-metileno-(6r)-tetra-hidrofólico, sua composição farmacêutica e seu uso Download PDF

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Publication number
BR112016002770B1
BR112016002770B1 BR112016002770-1A BR112016002770A BR112016002770B1 BR 112016002770 B1 BR112016002770 B1 BR 112016002770B1 BR 112016002770 A BR112016002770 A BR 112016002770A BR 112016002770 B1 BR112016002770 B1 BR 112016002770B1
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Prior art keywords
hemisulfate salt
thf
salt
pharmaceutical composition
hemisulfate
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BR112016002770-1A
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English (en)
Portuguese (pt)
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BR112016002770A2 (pt
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Rudolf Moser
Viola Groehn
Thomas Egger
Thomas Ammann
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Merck & Cie
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Publication of BR112016002770B1 publication Critical patent/BR112016002770B1/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic 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
    • C07D487/14Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/02Inorganic compounds
    • 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
    • A61K47/12Carboxylic acids; Salts or anhydrides 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
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/02Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
    • C07D475/04Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/12Heterocyclic compounds containing pteridine ring systems containing pteridine ring systems condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/12Heterocyclic compounds containing pteridine ring systems containing pteridine ring systems condensed with carbocyclic rings or ring systems
    • C07D475/14Benz [g] pteridines, e.g. riboflavin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • 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)
BR112016002770-1A 2013-08-14 2014-08-14 Sal de hemissulfato de ácido 5,10-metileno-(6r)-tetra-hidrofólico, sua composição farmacêutica e seu uso BR112016002770B1 (pt)

Applications Claiming Priority (3)

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

Publications (2)

Publication Number Publication Date
BR112016002770A2 BR112016002770A2 (pt) 2017-08-01
BR112016002770B1 true BR112016002770B1 (pt) 2022-12-06

Family

ID=48998397

Family Applications (2)

Application Number Title Priority Date Filing Date
BR122020002802-5A BR122020002802B1 (pt) 2013-08-14 2014-08-14 Liofilizado de um sal de hemissulfato do ácido 5,10-metileno-(6r)-tetra-hidrofólico e produto reconstituído
BR112016002770-1A BR112016002770B1 (pt) 2013-08-14 2014-08-14 Sal de hemissulfato de ácido 5,10-metileno-(6r)-tetra-hidrofólico, sua composição farmacêutica e seu uso

Family Applications Before (1)

Application Number Title Priority Date Filing Date
BR122020002802-5A BR122020002802B1 (pt) 2013-08-14 2014-08-14 Liofilizado de um sal de hemissulfato do ácido 5,10-metileno-(6r)-tetra-hidrofólico e produto reconstituído

Country Status (27)

Country Link
US (4) US20160185787A1 (enExample)
EP (3) EP2837631A1 (enExample)
JP (5) JP6617104B2 (enExample)
KR (2) KR102439605B1 (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) NZ745811A (enExample)
PL (2) PL3033344T3 (enExample)
PT (2) PT3033344T (enExample)
RS (2) RS56910B1 (enExample)
SG (2) SG11201601016PA (enExample)
SI (2) SI3287460T1 (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
DK3668516T3 (da) 2017-08-16 2021-12-13 Merck Patent Gmbh Stabile lyofilisater omfattende 5,10-methylen-(6r)-tetrahydrofolsyre og en dicarboxylsyre
EP3735267B8 (en) * 2018-01-05 2022-11-09 Isofol Medical AB Administration of multiple boluses of [6r] mthf in a 5-fluorouracil-based chemotherapy
KR20220152385A (ko) * 2020-03-30 2022-11-15 수미토모 케미칼 컴퍼니 리미티드 적층체
CA3258607A1 (en) 2022-06-08 2023-12-14 Merck Patent Gmbh STABLE PHARMACEUTICAL COMPOSITIONS COMPRISING 5,10-METHYLENE-(6R)-TETRAHYDROFOLIC ACID AND NACL
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

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US2300505A (en) * 1940-10-31 1942-11-03 Bell Telephone Labor Inc Selective system
CA1215945A (en) 1983-03-20 1986-12-30 Bengt Gustavsson Fluid transfer system
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.
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
MX2009006694A (es) 2006-12-21 2009-06-30 Hoffmann La Roche Polimorfos de un antagonista del receptor mglur5.
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

Also Published As

Publication number Publication date
HRP20171895T1 (hr) 2018-01-26
KR20160043054A (ko) 2016-04-20
NZ745811A (en) 2020-05-29
WO2015022407A1 (en) 2015-02-19
HK1217018A1 (zh) 2016-12-16
HUE037615T2 (hu) 2018-09-28
US12122783B2 (en) 2024-10-22
HUE054504T2 (hu) 2021-09-28
CA2921178C (en) 2020-12-08
PT3033344T (pt) 2018-01-03
MX2016001834A (es) 2016-04-15
PL3033344T3 (pl) 2018-02-28
CN105452250A (zh) 2016-03-30
EP3287460B1 (en) 2021-02-24
JP6764501B2 (ja) 2020-09-30
US20220024940A1 (en) 2022-01-27
US20160185787A1 (en) 2016-06-30
EP3033344A1 (en) 2016-06-22
JP2020128410A (ja) 2020-08-27
EP2837631A1 (en) 2015-02-18
BR112016002770A2 (pt) 2017-08-01
HK1256262A1 (zh) 2019-09-20
PL3287460T3 (pl) 2021-07-19
JP2018203763A (ja) 2018-12-27
EA032179B1 (ru) 2019-04-30
AU2014307872A1 (en) 2016-03-24
LT3287460T (lt) 2021-07-26
PT3287460T (pt) 2021-05-27
MX360355B (es) 2018-10-30
IL269170B (en) 2020-09-30
EA201600172A1 (ru) 2016-07-29
IL244069A0 (en) 2016-04-21
AU2018278943A1 (en) 2019-01-17
CY1119694T1 (el) 2018-04-04
US20240400574A1 (en) 2024-12-05
EA202091271A3 (ru) 2020-11-30
ES2871483T3 (es) 2021-10-29
RS61986B1 (sr) 2021-07-30
SI3033344T1 (en) 2018-01-31
CN105452250B (zh) 2018-02-27
MX382578B (es) 2025-03-13
JP6735321B2 (ja) 2020-08-05
RS56910B1 (sr) 2018-05-31
CA2921178A1 (en) 2015-02-19
US20190106431A1 (en) 2019-04-11
ZA201509204B (en) 2017-04-26
KR20210038995A (ko) 2021-04-08
CY1124076T1 (el) 2022-05-27
BR122020002802B1 (pt) 2022-11-29
JP2022024035A (ja) 2022-02-08
CN108096200A (zh) 2018-06-01
DK3033344T3 (en) 2017-12-18
HRP20210743T1 (hr) 2021-06-25
KR102439605B1 (ko) 2022-09-05
JP7710356B2 (ja) 2025-07-18
IL244069B (en) 2019-09-26
AU2018278943B2 (en) 2019-12-05
EP3033344B1 (en) 2017-09-27
JP2019131579A (ja) 2019-08-08
SG11201601016PA (en) 2016-03-30
JP7396960B2 (ja) 2023-12-12
LT3033344T (lt) 2017-12-27
EP3287460A1 (en) 2018-02-28
NZ717825A (en) 2019-11-29
IL269170A (en) 2019-11-28
JP6617104B2 (ja) 2019-12-04
JP2016528242A (ja) 2016-09-15
NO3033344T3 (enExample) 2018-02-24
EA201892729A1 (ru) 2019-04-30
EA202091271A2 (ru) 2020-09-30
KR102410373B1 (ko) 2022-06-22
SG10201801179VA (en) 2018-03-28
DK3287460T3 (da) 2021-05-03
ES2654474T3 (es) 2018-02-13
SI3287460T1 (sl) 2021-08-31
AU2014307872B2 (en) 2018-09-27

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 14/08/2014, OBSERVADAS AS CONDICOES LEGAIS