JP2020536960A - シロシビン、異なる多形形態、中間体、調合物の調製及びそれらの使用 - Google Patents

シロシビン、異なる多形形態、中間体、調合物の調製及びそれらの使用 Download PDF

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Publication number
JP2020536960A
JP2020536960A JP2020540865A JP2020540865A JP2020536960A JP 2020536960 A JP2020536960 A JP 2020536960A JP 2020540865 A JP2020540865 A JP 2020540865A JP 2020540865 A JP2020540865 A JP 2020540865A JP 2020536960 A JP2020536960 A JP 2020536960A
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polymorph
psilocybin
crystalline
crystalline psilocybin
xrpd
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JPWO2019073379A5 (enExample
JP2020536960A5 (enExample
Inventor
デレク ジョン ロンデスブラ，
デレク ジョン ロンデスブラ，
クリストファー ブラウン，
クリストファー ブラウン，
ジュリアン スコット ノーゼン，
ジュリアン スコット ノーゼン，
ジリアン ムーア，
ジリアン ムーア，
ヘマント パティル，
ヘマント パティル，
デイビッド ニコルス，
デイビッド ニコルス，
Original Assignee
コンパス パスファインダー リミテッド
コンパス パスファインダー リミテッド
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Application filed by コンパス パスファインダー リミテッド, コンパス パスファインダー リミテッド filed Critical コンパス パスファインダー リミテッド
Publication of JP2020536960A publication Critical patent/JP2020536960A/ja
Publication of JP2020536960A5 publication Critical patent/JP2020536960A5/ja
Priority to JP2022208641A priority Critical patent/JP2023024755A/ja
Publication of JPWO2019073379A5 publication Critical patent/JPWO2019073379A5/ja
Priority to JP2024040039A priority patent/JP2024069473A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572—Five-membered rings
    • C07F9/5728—Five-membered rings condensed with carbocyclic rings or carbocyclic ring systems
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B63/00—Purification; Separation; Stabilisation; Use of additives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C07D209/16—Tryptamines
    • 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
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Inorganic Chemistry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
JP2020540865A 2017-10-09 2018-10-09 シロシビン、異なる多形形態、中間体、調合物の調製及びそれらの使用 Pending JP2020536960A (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2022208641A JP2023024755A (ja) 2017-10-09 2022-12-26 シロシビン、異なる多形形態、中間体、調合物の調製及びそれらの使用
JP2024040039A JP2024069473A (ja) 2017-10-09 2024-03-14 シロシビン、異なる多形形態、中間体、調合物の調製及びそれらの使用

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GB1716505.1A GB2571696B (en) 2017-10-09 2017-10-09 Large scale method for the preparation of Psilocybin and formulations of Psilocybin so produced
GB1716505.1 2017-10-09
GB1810588.2A GB2572023C2 (en) 2017-10-09 2018-06-28 Crystaline psilocybin polymorph A, a formulation and uses thereof together with a method of preparation
GB1810588.2 2018-06-28
PCT/IB2018/057811 WO2019073379A1 (en) 2017-10-09 2018-10-09 PREPARATION OF PSILOCYBIN, DIFFERENT POLYMORPHIC FORMS, INTERMEDIAIRES, FORMULATIONS AND THEIR USE
GB1816438.4A GB2576059B (en) 2017-10-09 2018-10-09 A pharmaceutical formulation comprising psilocybin
GB1816438.4 2018-10-10

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JP2022208641A Division JP2023024755A (ja) 2017-10-09 2022-12-26 シロシビン、異なる多形形態、中間体、調合物の調製及びそれらの使用

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JP2020536960A true JP2020536960A (ja) 2020-12-17
JP2020536960A5 JP2020536960A5 (enExample) 2021-11-25
JPWO2019073379A5 JPWO2019073379A5 (enExample) 2023-01-11

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JP2020540865A Pending JP2020536960A (ja) 2017-10-09 2018-10-09 シロシビン、異なる多形形態、中間体、調合物の調製及びそれらの使用
JP2022208641A Pending JP2023024755A (ja) 2017-10-09 2022-12-26 シロシビン、異なる多形形態、中間体、調合物の調製及びそれらの使用
JP2024040039A Pending JP2024069473A (ja) 2017-10-09 2024-03-14 シロシビン、異なる多形形態、中間体、調合物の調製及びそれらの使用

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JP2022208641A Pending JP2023024755A (ja) 2017-10-09 2022-12-26 シロシビン、異なる多形形態、中間体、調合物の調製及びそれらの使用
JP2024040039A Pending JP2024069473A (ja) 2017-10-09 2024-03-14 シロシビン、異なる多形形態、中間体、調合物の調製及びそれらの使用

Country Status (19)

Country Link
US (15) US10519175B2 (enExample)
EP (1) EP3694835A1 (enExample)
JP (3) JP2020536960A (enExample)
KR (2) KR20250041070A (enExample)
CN (1) CN111491919A (enExample)
AU (2) AU2018349279B2 (enExample)
BR (1) BR112020006947A2 (enExample)
CA (1) CA3078765A1 (enExample)
CO (1) CO2020005643A2 (enExample)
DE (1) DE202018006384U1 (enExample)
EA (1) EA202090917A1 (enExample)
GB (4) GB2571696B (enExample)
IL (3) IL322447A (enExample)
MX (3) MX2020003910A (enExample)
MY (1) MY205385A (enExample)
PH (1) PH12020550246A1 (enExample)
SG (1) SG11202003198RA (enExample)
WO (1) WO2019073379A1 (enExample)
ZA (1) ZA202407520B (enExample)

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JP2022523700A (ja) * 2019-01-30 2022-04-26 ダイヤモンド セラピューティクス インク． 心理性、認知性、行動性、および／または気分性の障害を処置するための方法、ならびに５ｈｔ受容体アゴニストを含む組成物
JP2024506383A (ja) * 2021-02-10 2024-02-13 エレウシス セラピューティクス ユーエス，インコーポレーテッド シロシンの薬学的に許容可能な塩及びその使用
WO2025178027A1 (ja) * 2024-02-22 2025-08-28 株式会社島津製作所 液体クロマトグラフィーの方法および液体クロマトグラフィーシステム

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