CN115536594A - 5-氨基-2,3-二氢噻嗪-1,4-二酮的结晶体 - Google Patents

5-氨基-2,3-二氢噻嗪-1,4-二酮的结晶体 Download PDF

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Publication number
CN115536594A
CN115536594A CN202211145086.8A CN202211145086A CN115536594A CN 115536594 A CN115536594 A CN 115536594A CN 202211145086 A CN202211145086 A CN 202211145086A CN 115536594 A CN115536594 A CN 115536594A
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Prior art keywords
crystalline form
amino
acid
luminol
pharmaceutical composition
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CN202211145086.8A
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Chinese (zh)
Inventor
T·马丁
J·布罗伊
J·弗莱斯纳
W·布里施
J·冯韦格尔
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Metriopharm AG
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Metriopharm AG
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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
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    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
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    • 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
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    • A61P37/00—Drugs for immunological or allergic disorders
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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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  • Health & Medical Sciences (AREA)
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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Otolaryngology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Pathology (AREA)
  • General Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Optics & Photonics (AREA)
  • Materials Engineering (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN202211145086.8A 2016-02-16 2017-02-15 5-氨基-2,3-二氢噻嗪-1,4-二酮的结晶体 Pending CN115536594A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP16000379 2016-02-16
EP16000379.4 2016-02-16
CN201780023199.1A CN109563052A (zh) 2016-02-16 2017-02-15 5-氨基-2,3-二氢噻嗪-1,4-二酮的结晶体
PCT/EP2017/000227 WO2017140430A1 (en) 2016-02-16 2017-02-15 Crystalline form of 5-amino-2,3-dihydrophthalazine-1,4-dione

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201780023199.1A Division CN109563052A (zh) 2016-02-16 2017-02-15 5-氨基-2,3-二氢噻嗪-1,4-二酮的结晶体

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CN115536594A true CN115536594A (zh) 2022-12-30

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CN202211145086.8A Pending CN115536594A (zh) 2016-02-16 2017-02-15 5-氨基-2,3-二氢噻嗪-1,4-二酮的结晶体
CN201780023199.1A Pending CN109563052A (zh) 2016-02-16 2017-02-15 5-氨基-2,3-二氢噻嗪-1,4-二酮的结晶体

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CN201780023199.1A Pending CN109563052A (zh) 2016-02-16 2017-02-15 5-氨基-2,3-二氢噻嗪-1,4-二酮的结晶体

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Country Link
US (1) US11111218B2 (https=)
EP (1) EP3416951B1 (https=)
JP (2) JP7034079B2 (https=)
KR (1) KR102535960B1 (https=)
CN (2) CN115536594A (https=)
CA (1) CA3011767C (https=)
ES (1) ES2797299T3 (https=)
WO (1) WO2017140430A1 (https=)

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
KR20220158030A (ko) * 2020-03-25 2022-11-29 메트리오팜 아게 급성 폐손상 치료용 5-아미노-2,3-디히드로-1,4-프탈라진디온
EP3981405A1 (en) 2020-10-08 2022-04-13 MetrioPharm AG Compound for the treatment of coronaviral infections
MX2022015601A (es) * 2020-06-10 2023-01-30 Metriopharm Ag Compuesto para el tratamiento de infecciones coronavirales.
CN116963738A (zh) 2020-12-02 2023-10-27 麦翠奥制药公司 用于SARS-CoV-2感染的后遗症的预防和治疗的鲁米诺
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
AU2023204891A1 (en) * 2022-01-07 2024-08-08 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
WO2025067689A1 (en) 2023-09-26 2025-04-03 Metriopharm Ag 5-amino-2,3-dihydro-1,4-phthalazinedione for the treatment of infections with an rna virus

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1646918A (zh) * 2002-04-25 2005-07-27 Roc进口公司 探测和定位血迹的方法以及为探测血迹设计的组合物
CN102971300A (zh) * 2010-03-01 2013-03-13 梅特里奥药品股份公司 5-氨基-2,3-二氢-(2,3-二氮杂萘)-1,4-二酮钠盐的晶型、含有它们的药物制剂以及所述晶型的生产方法

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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.
WO2011123776A2 (en) 2010-04-01 2011-10-06 Guthery B Eugene Method for detecting occult blood
CA2966671C (en) 2014-12-18 2020-10-27 Metriopharm Ag Crystalline form of 5-amino-2,3-dihydrophthalazine-1,4-dione sodium salt, pharmaceutical preparations containing the same and method for the production of said form

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1646918A (zh) * 2002-04-25 2005-07-27 Roc进口公司 探测和定位血迹的方法以及为探测血迹设计的组合物
CN102971300A (zh) * 2010-03-01 2013-03-13 梅特里奥药品股份公司 5-氨基-2,3-二氢-(2,3-二氮杂萘)-1,4-二酮钠盐的晶型、含有它们的药物制剂以及所述晶型的生产方法

Non-Patent Citations (1)

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Title
HENRICH H. PARADIES等: "The Crystal and Molecular Structure of 3-Aminophthalhydrazide (Luminol)", 《BERICHTE DER BUNSEN-GESELLSCHAFT-PHYSICAL CHEMISTRY CHEMICAL PHYSICS》, vol. 96, no. 8, pages 1028 *

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Publication number Publication date
EP3416951B1 (en) 2020-04-08
ES2797299T3 (es) 2020-12-01
WO2017140430A1 (en) 2017-08-24
JP2022037005A (ja) 2022-03-08
KR20180107277A (ko) 2018-10-01
JP7034079B2 (ja) 2022-03-11
JP2019509268A (ja) 2019-04-04
JP7331067B2 (ja) 2023-08-22
EP3416951A1 (en) 2018-12-26
US11111218B2 (en) 2021-09-07
CA3011767C (en) 2024-02-06
KR102535960B1 (ko) 2023-05-23
CN109563052A (zh) 2019-04-02
CA3011767A1 (en) 2017-08-24
US20200369624A1 (en) 2020-11-26

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