ZA202004582B - Long-acting injectable formulations and crystalline forms of buprenorphine derivatives - Google Patents

Long-acting injectable formulations and crystalline forms of buprenorphine derivatives

Info

Publication number
ZA202004582B
ZA202004582B ZA2020/04582A ZA202004582A ZA202004582B ZA 202004582 B ZA202004582 B ZA 202004582B ZA 2020/04582 A ZA2020/04582 A ZA 2020/04582A ZA 202004582 A ZA202004582 A ZA 202004582A ZA 202004582 B ZA202004582 B ZA 202004582B
Authority
ZA
South Africa
Prior art keywords
long
crystalline forms
injectable formulations
acting injectable
buprenorphine derivatives
Prior art date
Application number
ZA2020/04582A
Other languages
English (en)
Inventor
Tong-Ho Lin
Yung-Shun Wen
Jui-Wei Liang
Original Assignee
Alar Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Alar Pharmaceuticals Inc filed Critical Alar Pharmaceuticals Inc
Publication of ZA202004582B publication Critical patent/ZA202004582B/en

Links

Classifications

    • 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
    • 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
    • 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
    • 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

Landscapes

  • 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)
ZA2020/04582A 2018-05-11 2020-07-23 Long-acting injectable formulations and crystalline forms of buprenorphine derivatives ZA202004582B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862670714P 2018-05-11 2018-05-11
PCT/CN2019/086449 WO2019214726A1 (en) 2018-05-11 2019-05-10 Long-acting injectable formulations and crystalline forms of buprenorphine derivatives

Publications (1)

Publication Number Publication Date
ZA202004582B true ZA202004582B (en) 2023-01-25

Family

ID=68466685

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA2020/04582A ZA202004582B (en) 2018-05-11 2020-07-23 Long-acting injectable formulations and crystalline forms of buprenorphine derivatives

Country Status (14)

Country Link
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

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
GB0606124D0 (en) 2006-03-28 2006-05-03 Reckitt Benckiser Healthcare Buprenorphine derivatives and uses thereof
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
EP2970188A4 (en) 2013-03-15 2016-10-19 Vm Therapeutics Llc NOVEL CRYSTALLINE FORMS
US9393211B2 (en) 2013-03-15 2016-07-19 Oakwood Laboratories LLC High drug load buprenorphine microspheres and method of producing same
GB201404139D0 (en) * 2014-03-10 2014-04-23 Rb Pharmaceuticals Ltd Sustained release buprenorphine solution formulations
CN107660207B (zh) * 2015-03-10 2020-09-29 罗德科技公司 丁丙诺啡乙酸盐及用于制备丁丙诺啡的方法
TWI743193B (zh) * 2016-09-13 2021-10-21 昱展新藥生技股份有限公司 丁基原啡因緩釋製劑
BR112020016576A2 (pt) 2018-05-11 2020-12-15 Alar Pharmaceuticals Inc. Formulações injetáveis de ação prolongada e formas cristalinas de derivados de buprenorfina

Also Published As

Publication number Publication date
WO2019214726A1 (en) 2019-11-14
US20210122756A1 (en) 2021-04-29
TW202016117A (zh) 2020-05-01
TWI838372B (zh) 2024-04-11
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
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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