TWI838372B - 丁基原啡因衍生物之長效注射劑型及結晶型 - Google Patents

丁基原啡因衍生物之長效注射劑型及結晶型 Download PDF

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Publication number
TWI838372B
TWI838372B TW108116576A TW108116576A TWI838372B TW I838372 B TWI838372 B TW I838372B TW 108116576 A TW108116576 A TW 108116576A TW 108116576 A TW108116576 A TW 108116576A TW I838372 B TWI838372 B TW I838372B
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Taiwan
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crystalline form
butyl
acyl
orthomorphine
butylorphine
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TW108116576A
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English (en)
Chinese (zh)
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TW202016117A (zh
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林東和
文永順
梁芮瑋
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昱展新藥生技股份有限公司
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
    • C07D489/04—Salts; Organic complexes
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/24—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/08—Solutions
    • 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
    • A61K9/10—Dispersions; Emulsions
    • 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
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
    • 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
    • A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5031—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poly(lactide-co-glycolide)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/09—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems
    • C07D489/10—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14
    • C07D489/12—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
    • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Addiction (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biochemistry (AREA)
  • Rheumatology (AREA)
  • Dispersion Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Inorganic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
TW108116576A 2018-05-11 2019-05-10 丁基原啡因衍生物之長效注射劑型及結晶型 TWI838372B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862670714P 2018-05-11 2018-05-11
US62/670,714 2018-05-11

Publications (2)

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TW202016117A TW202016117A (zh) 2020-05-01
TWI838372B true TWI838372B (zh) 2024-04-11

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TW108116576A TWI838372B (zh) 2018-05-11 2019-05-10 丁基原啡因衍生物之長效注射劑型及結晶型

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US (2) US11524965B2 (https=)
EP (1) EP3790881B1 (https=)
JP (3) JP7421804B2 (https=)
KR (2) KR102839314B1 (https=)
CN (1) CN111954672B (https=)
AR (1) AR117426A1 (https=)
AU (1) AU2019266795B2 (https=)
BR (1) BR112020016576A2 (https=)
CA (1) CA3089256C (https=)
MX (1) MX2020008471A (https=)
NZ (1) NZ766474A (https=)
TW (1) TWI838372B (https=)
WO (1) WO2019214726A1 (https=)
ZA (1) ZA202004582B (https=)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112020016576A2 (pt) 2018-05-11 2020-12-15 Alar Pharmaceuticals Inc. Formulações injetáveis de ação prolongada e formas cristalinas de derivados de buprenorfina
GB202019594D0 (en) * 2020-12-11 2021-01-27 Univ London Queen Mary Sustained release formulations of crystalline drugs
CN117999079A (zh) * 2021-08-20 2024-05-07 苏州恩华生物医药科技有限公司 一种包含塞纳布啡的药物组合物
IL317873A (en) * 2022-06-24 2025-02-01 Alar Pharmaceuticals Inc Stable pharmaceutical composition of buprenorphine and method of preparation and use thereof
CN115317453A (zh) * 2022-09-01 2022-11-11 广东嘉博制药有限公司 一种缓释微球制剂及其制备方法与用途
EP4719414A2 (en) * 2023-06-02 2026-04-08 Board of Regents of the University of Nebraska Compounds, nanoparticles, and pharmaceutical compositions for the treatment of drug addiction

Citations (3)

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CN1263760C (zh) * 2002-11-12 2006-07-12 财团法人奇美医院 新颖的丁丙诺啡酯衍生物及其制备方法，以及长效作用镇痛药学组合物
CN101410402A (zh) * 2006-03-28 2009-04-15 雷克特本克斯尔保健(英国)有限公司 丁丙诺啡衍生物及其应用
WO2018050043A1 (en) * 2016-09-13 2018-03-22 Alar Pharmaceuticals Inc. Sustained-release buprenorphine formulations background of invention

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RO121631B1 (ro) 1999-08-27 2008-01-30 Southern Research Institute Compoziţie cu buprenorfină şi utilizarea acesteia pentru reducerea consumului de heroină şi/sau alcool
DE60329515D1 (de) 2002-10-25 2009-11-12 Euro Celtique Sa Analoga und prodrugs von buprenorphin
DE60224288T2 (de) 2002-11-25 2009-04-16 Chi Mei Foundation Medical Center Buprenorphinesterderivate, Verfahren zu ihrer Herstellung, und langwirksame analgetische Arzneimittel
JP2004175706A (ja) * 2002-11-26 2004-06-24 Chi Mei Foundation Medical Center 新規なブプレノルフィンのエステル誘導体及びそれらの調製方法、及び長時間効力持続性鎮痛薬剤組成物
WO2005117830A1 (en) 2004-06-04 2005-12-15 Camurus Ab Liquid depot formulations
US9272044B2 (en) * 2010-06-08 2016-03-01 Indivior Uk Limited Injectable flowable composition buprenorphine
GB2481017B (en) 2010-06-08 2015-01-07 Rb Pharmaceuticals Ltd Microparticle buprenorphine suspension
GB2481018B (en) 2010-06-08 2015-03-18 Rb Pharmaceuticals Ltd Injectable flowable composition comprising buprenorphine
FR2975912B1 (fr) * 2011-05-30 2013-06-14 Flamel Tech Sa Composition a liberation controlee de buprenorphine
CA2867121C (en) * 2012-03-19 2021-05-25 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising fatty acid esters
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BR112020016576A2 (pt) 2018-05-11 2020-12-15 Alar Pharmaceuticals Inc. Formulações injetáveis de ação prolongada e formas cristalinas de derivados de buprenorfina

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Publication number Priority date Publication date Assignee Title
CN1263760C (zh) * 2002-11-12 2006-07-12 财团法人奇美医院 新颖的丁丙诺啡酯衍生物及其制备方法，以及长效作用镇痛药学组合物
CN101410402A (zh) * 2006-03-28 2009-04-15 雷克特本克斯尔保健(英国)有限公司 丁丙诺啡衍生物及其应用
WO2018050043A1 (en) * 2016-09-13 2018-03-22 Alar Pharmaceuticals Inc. Sustained-release buprenorphine formulations background of invention

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Publication number Publication date
WO2019214726A1 (en) 2019-11-14
US20210122756A1 (en) 2021-04-29
TW202016117A (zh) 2020-05-01
JP2023106478A (ja) 2023-08-01
JP2025121948A (ja) 2025-08-20
JP7421804B2 (ja) 2024-01-25
JP2021522306A (ja) 2021-08-30
US20230002399A1 (en) 2023-01-05
EP3790881A4 (en) 2022-03-09
US11524965B2 (en) 2022-12-13
EP3790881A1 (en) 2021-03-17
CA3089256A1 (en) 2019-11-14
AU2019266795B2 (en) 2023-02-09
ZA202004582B (en) 2023-01-25
CN111954672A (zh) 2020-11-17
AR117426A1 (es) 2021-08-04
US12522610B2 (en) 2026-01-13
AU2019266795A1 (en) 2020-08-13
BR112020016576A2 (pt) 2020-12-15
NZ766474A (en) 2023-03-31
KR20210021459A (ko) 2021-02-26
KR102839314B1 (ko) 2025-07-29
EP3790881B1 (en) 2026-04-15
KR20230093535A (ko) 2023-06-27
CN111954672B (zh) 2023-09-01
MX2020008471A (es) 2020-09-25
CA3089256C (en) 2023-10-10

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