KR20200085753A - 실로시빈의 제조, 상이한 다형 형태, 중간체, 제제 및 이의 용도 - Google Patents

실로시빈의 제조, 상이한 다형 형태, 중간체, 제제 및 이의 용도 Download PDF

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KR20200085753A
KR20200085753A KR1020207012821A KR20207012821A KR20200085753A KR 20200085753 A KR20200085753 A KR 20200085753A KR 1020207012821 A KR1020207012821 A KR 1020207012821A KR 20207012821 A KR20207012821 A KR 20207012821A KR 20200085753 A KR20200085753 A KR 20200085753A
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polymorph
psilocybin
crystalline psilocybin
reaction
crystalline
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Ceased
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KR1020207012821A
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Korean (ko)
Inventor
데릭 존 론데스브로
크리스토퍼 브라운
줄리안 스캇 노턴
질리언 무어
헤만트 파틸
헤만트 파틸
데이비드 니콜스
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컴퍼스 패스웨이즈 리미티드
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Application filed by 컴퍼스 패스웨이즈 리미티드 filed Critical 컴퍼스 패스웨이즈 리미티드
Priority to KR1020257007706A priority Critical patent/KR20250041070A/ko
Publication of KR20200085753A publication Critical patent/KR20200085753A/ko
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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)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
KR1020207012821A 2017-10-09 2018-10-09 실로시빈의 제조, 상이한 다형 형태, 중간체, 제제 및 이의 용도 Ceased KR20200085753A (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1020257007706A KR20250041070A (ko) 2017-10-09 2018-10-09 실로시빈의 제조, 상이한 다형 형태, 중간체, 제제 및 이의 용도

Applications Claiming Priority (7)

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020257007706A Division KR20250041070A (ko) 2017-10-09 2018-10-09 실로시빈의 제조, 상이한 다형 형태, 중간체, 제제 및 이의 용도

Publications (1)

Publication Number Publication Date
KR20200085753A true KR20200085753A (ko) 2020-07-15

Family

ID=60326674

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020207012821A Ceased KR20200085753A (ko) 2017-10-09 2018-10-09 실로시빈의 제조, 상이한 다형 형태, 중간체, 제제 및 이의 용도
KR1020257007706A Pending KR20250041070A (ko) 2017-10-09 2018-10-09 실로시빈의 제조, 상이한 다형 형태, 중간체, 제제 및 이의 용도

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020257007706A Pending KR20250041070A (ko) 2017-10-09 2018-10-09 실로시빈의 제조, 상이한 다형 형태, 중간체, 제제 및 이의 용도

Country Status (19)

Country Link
US (15) US10519175B2 (https=)
EP (1) EP3694835A1 (https=)
JP (3) JP2020536960A (https=)
KR (2) KR20200085753A (https=)
CN (1) CN111491919A (https=)
AU (3) AU2018349279B2 (https=)
BR (1) BR112020006947A2 (https=)
CA (1) CA3078765A1 (https=)
CO (1) CO2020005643A2 (https=)
DE (1) DE202018006384U1 (https=)
EA (1) EA202090917A1 (https=)
GB (4) GB2571696B (https=)
IL (3) IL311953B2 (https=)
MX (3) MX2020003910A (https=)
MY (1) MY205385A (https=)
PH (1) PH12020550246A1 (https=)
SG (1) SG11202003198RA (https=)
WO (1) WO2019073379A1 (https=)
ZA (1) ZA202407520B (https=)

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St.27 status event code: A-0-1-A10-A18-div-PA0104

St.27 status event code: A-0-1-A10-A16-div-PA0104

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PJ1301 Trial decision

St.27 status event code: A-3-3-V10-V15-crt-PJ1301

Decision date: 20251118

Appeal event data comment text: Appeal Kind Category : Appeal against decision to decline refusal, Appeal Ground Text : 2020 7012821

Appeal request date: 20250307

Appellate body name: Patent Examination Board

Decision authority category: Office appeal board

Decision identifier: 2025101000441

V15 Decision substituted

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