JP7034079B2 - ５－アミノ－２，３－ジヒドロフタラジン－１，４－ジオンの結晶形の製造方法 - Google Patents

５－アミノ－２，３－ジヒドロフタラジン－１，４－ジオンの結晶形の製造方法 Download PDF

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JP7034079B2
JP7034079B2 JP2018542755A JP2018542755A JP7034079B2 JP 7034079 B2 JP7034079 B2 JP 7034079B2 JP 2018542755 A JP2018542755 A JP 2018542755A JP 2018542755 A JP2018542755 A JP 2018542755A JP 7034079 B2 JP7034079 B2 JP 7034079B2
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acid
precipitate
luminol
sodium
amino
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JP2019509268A (ja
JP2019509268A5 (enExample
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トーマス マーティン
ヨセフ ブロイ
ジュリアン フリンスナー
ヴォルフガング ブリシュ
ヨーグ フォン・ウェーゲーナー
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メトリオファーム アーゲー
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30—Phthalazines
    • C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • 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
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/04—Drugs for disorders of the respiratory system for throat disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
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    • C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
    • C09K—MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FOR ELSEWHERE
    • C09K11/00—Luminescent materials, e.g. electroluminescent or chemiluminescent
    • C09K11/06—Luminescent materials, e.g. electroluminescent or chemiluminescent containing organic luminescent materials
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N21/00—Investigating or analysing materials by the use of optical means, i.e. using sub-millimetre waves, infrared, visible or ultraviolet light
    • G01N21/62—Systems in which the material investigated is excited whereby it emits light or causes a change in wavelength of the incident light
    • G01N21/63—Systems in which the material investigated is excited whereby it emits light or causes a change in wavelength of the incident light optically excited
    • G01N21/64—Fluorescence; Phosphorescence
    • G01N21/6428—Measuring fluorescence of fluorescent products of reactions or of fluorochrome labelled reactive substances, e.g. measuring quenching effects, using measuring "optrodes"
    • 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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    • C09K2211/00—Chemical nature of organic luminescent or tenebrescent compounds
    • C09K2211/10—Non-macromolecular compounds
    • C09K2211/1018—Heterocyclic compounds
    • C09K2211/1025—Heterocyclic compounds characterised by ligands
    • C09K2211/1044—Heterocyclic compounds characterised by ligands containing two nitrogen atoms as heteroatoms

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  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Otolaryngology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Physics & Mathematics (AREA)
  • Pain & Pain Management (AREA)
  • Analytical Chemistry (AREA)
  • Materials Engineering (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Optics & Photonics (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2018542755A 2016-02-16 2017-02-15 ５－アミノ－２，３－ジヒドロフタラジン－１，４－ジオンの結晶形の製造方法 Active JP7034079B2 (ja)

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JP2021192808A JP7331067B2 (ja) 2016-02-16 2021-11-29 ５－アミノ－２，３－ジヒドロフタラジン－１，４－ジオンの結晶形

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Application Number Priority Date Filing Date Title
EP16000379.4 2016-02-16
EP16000379 2016-02-16
PCT/EP2017/000227 WO2017140430A1 (en) 2016-02-16 2017-02-15 Crystalline form of 5-amino-2,3-dihydrophthalazine-1,4-dione

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JP2019509268A JP2019509268A (ja) 2019-04-04
JP2019509268A5 JP2019509268A5 (enExample) 2020-03-26
JP7034079B2 true JP7034079B2 (ja) 2022-03-11

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JP2021192808A Active JP7331067B2 (ja) 2016-02-16 2021-11-29 ５－アミノ－２，３－ジヒドロフタラジン－１，４－ジオンの結晶形

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US (1) US11111218B2 (enExample)
EP (1) EP3416951B1 (enExample)
JP (2) JP7034079B2 (enExample)
KR (1) KR102535960B1 (enExample)
CN (2) CN109563052A (enExample)
CA (1) CA3011767C (enExample)
ES (1) ES2797299T3 (enExample)
WO (1) WO2017140430A1 (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3511325A1 (en) * 2018-01-11 2019-07-17 MetrioPharm AG Method for solubilizing 5-amino-2,3-dihydro-1,4-phthalazinedione
GB201804132D0 (en) * 2018-03-15 2018-05-02 Secr Defence Forensic analysis of an object for chemical and biological agents
EP3858328A1 (en) * 2020-01-31 2021-08-04 MetrioPharm AG Use of 5-amino-2,3-dihydro-1,4-phthalazinedione in the inhalatory treatment of inflammatory pulmonary diseases
EP3858358A1 (en) 2020-01-31 2021-08-04 MetrioPharm AG Use of 5-amino-2,3-dihydro-1,4-phthalazinedione in the treatment of rare chronic inflammatory pulmonary diseases
PL4125802T3 (pl) * 2020-03-25 2026-03-23 Metriopharm Ag 5-amino-2,3-dihydro-1,4-ftalazinedion do leczenia ostrego uszkodzenia płuc
EP3981405A1 (en) 2020-10-08 2022-04-13 MetrioPharm AG Compound for the treatment of coronaviral infections
AU2021288757B2 (en) * 2020-06-10 2026-01-08 Metriopharm Ag Compound for the treatment of coronaviral infections
US20240075029A1 (en) 2020-12-02 2024-03-07 Metriopharm Ag Luminol for the prophylaxis and the treatment of sequelae of a sars-cov-2 infection
US20230087473A1 (en) * 2021-09-22 2023-03-23 Hemant N. Joshi Composition of suspoemulsion formulation of anthelmintic drugs with essential oils for naso-pulmonary administration
EP4193994A1 (en) 2021-12-08 2023-06-14 MetrioPharm AG Combination of 5-amino-2,3-dihydro-1,4-phtalazinedione and a 6'-methoxycinchonan-9-ol for use in the treatment of coronaviral infections
EP4460309B1 (en) * 2022-01-07 2026-08-19 MetrioPharm AG Use of 5-amino-2,3-dihydro-1,4-phthalazinedione in the treatment of congenital muscular dystrophies
EP4209219A1 (en) * 2022-01-07 2023-07-12 MetrioPharm AG Combination of budesonide and 5-amino-2,3-dihydro-1,4-phtalazinedione
EP4248963A1 (en) 2022-03-25 2023-09-27 MetrioPharm AG Combination of 5-amino-2,3-dihydro-1,4-phtalazinedione and a fumaric acid ester
EP4483879A1 (en) 2023-06-29 2025-01-01 MetrioPharm AG 5-amino-2,3-dihydro-1,4-phthalazinedione for the prophylaxis and treatment of thrombotic disorders
EP4784132A1 (en) 2023-09-26 2026-08-05 MetrioPharm AG 5-amino-2,3-dihydro-1,4-phthalazinedione for the treatment of infections with an rna virus

Citations (2)

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WO2011123776A2 (en) 2010-04-01 2011-10-06 Guthery B Eugene Method for detecting occult blood
JP2013521239A (ja) 2010-03-01 2013-06-10 メトリオファーム アーゲー ５−アミノ−２，３−ジヒドロフタラジン−１，４−ジオンナトリウム塩の結晶形、それを含有する医薬品調製物、および前記形態の製造の方法

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CH683966A5 (it) * 1993-02-19 1994-06-30 Limad Marketing Exp & Imp Composti della classe dei ftalidrazidici come sostanze attive in agenti anti-ipossici e di difesa.
FR2839155B1 (fr) * 2002-04-25 2005-02-04 Roc Imp Procede pour detecter et localiser des traces de sang et compose pour detecter des traces de sang
JP2017537958A (ja) 2014-12-18 2017-12-21 メトリオファーム アーゲー ５−アミノ−２，３−ジヒドロフタラジン１，４−ジオンナトリウム塩の結晶形態、同一物を含む医薬製剤、及びこの形態の製造ための方法

Patent Citations (2)

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JP2013521239A (ja) 2010-03-01 2013-06-10 メトリオファーム アーゲー ５−アミノ−２，３−ジヒドロフタラジン−１，４−ジオンナトリウム塩の結晶形、それを含有する医薬品調製物、および前記形態の製造の方法
WO2011123776A2 (en) 2010-04-01 2011-10-06 Guthery B Eugene Method for detecting occult blood

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NEUMANN, H. et al.，A New Efficient Synthesis of Substituted Luminols Using Multicomponent Reactions，Zeitschrift fur Naturforschung B，2004年，Vol. 59，pp. 431-438
STOTT, R. A. W. et al.，Purification of luminol for use in enhanced chemluminescence immunoassay，Bioluminescence and Chemiluminescence，1987年，pp. 237-240
平山令明編，有機化合物結晶作製ハンドブック －原理とノウハウ－，丸善株式会社，2008年07月25日，p.57-84
緒方章，化学実験操作法 上巻，株式会社南江堂，1963年11月20日
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CN115536594A (zh) 2022-12-30
JP2022037005A (ja) 2022-03-08
ES2797299T3 (es) 2020-12-01
JP2019509268A (ja) 2019-04-04
US11111218B2 (en) 2021-09-07
EP3416951A1 (en) 2018-12-26
EP3416951B1 (en) 2020-04-08
CA3011767A1 (en) 2017-08-24
CN109563052A (zh) 2019-04-02
US20200369624A1 (en) 2020-11-26
JP7331067B2 (ja) 2023-08-22
KR102535960B1 (ko) 2023-05-23
CA3011767C (en) 2024-02-06
KR20180107277A (ko) 2018-10-01
WO2017140430A1 (en) 2017-08-24

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