BR112020016576A2 - Formulações injetáveis de ação prolongada e formas cristalinas de derivados de buprenorfina - Google Patents

Formulações injetáveis de ação prolongada e formas cristalinas de derivados de buprenorfina Download PDF

Info

Publication number
BR112020016576A2
BR112020016576A2 BR112020016576-0A BR112020016576A BR112020016576A2 BR 112020016576 A2 BR112020016576 A2 BR 112020016576A2 BR 112020016576 A BR112020016576 A BR 112020016576A BR 112020016576 A2 BR112020016576 A2 BR 112020016576A2
Authority
BR
Brazil
Prior art keywords
buprenorphine
acyl
release
injectable pharmaceutical
derivatives
Prior art date
Application number
BR112020016576-0A
Other languages
English (en)
Portuguese (pt)
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 BR112020016576A2 publication Critical patent/BR112020016576A2/pt

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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Biochemistry (AREA)
  • Dispersion Chemistry (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
BR112020016576-0A 2018-05-11 2019-05-10 Formulações injetáveis de ação prolongada e formas cristalinas de derivados de buprenorfina BR112020016576A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862670714P 2018-05-11 2018-05-11
US62/670,714 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
BR112020016576A2 true BR112020016576A2 (pt) 2020-12-15

Family

ID=68466685

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112020016576-0A BR112020016576A2 (pt) 2018-05-11 2019-05-10 Formulações injetáveis de ação prolongada e formas cristalinas de derivados de buprenorfina

Country Status (14)

Country Link
US (2) US11524965B2 (https=)
EP (1) EP3790881B1 (https=)
JP (3) JP7421804B2 (https=)
KR (2) KR20210021459A (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
AR117426A1 (es) 2018-05-11 2021-08-04 Alar Pharmaceuticals Inc Formulaciones inyectables de acción prolongada y formas cristalinas de derivados de buprenorfina
GB202019594D0 (en) * 2020-12-11 2021-01-27 Univ London Queen Mary Sustained release formulations of crystalline drugs
WO2023020608A1 (zh) * 2021-08-20 2023-02-23 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
KR20250036827A (ko) * 2022-06-24 2025-03-14 에일러 파마슈티컬스 아이엔씨. 부프레노르핀의 안정한 약제학적 조성물 및 이의 제조 방법 및 용도
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
IL325075A (en) * 2023-06-02 2026-02-01 Univ Nebraska Compounds, nanoparticles and pharmaceutical preparations 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
JP4913298B2 (ja) 1999-08-27 2012-04-11 ブルックウッド ファーマシューティカルズ，インコーポレイティド 注射可能なブプレノルフィン微粒子組成物及びその使用
EP1554290B1 (en) 2002-10-25 2009-09-30 Euro-Celtique S.A. Analogs and prodrugs of buprenorphine
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
US8236292B2 (en) 2004-06-04 2012-08-07 Camurus Ab Liquid depot formulations
GB0606124D0 (en) 2006-03-28 2006-05-03 Reckitt Benckiser Healthcare Buprenorphine derivatives and uses thereof
GB2513060B (en) 2010-06-08 2015-01-07 Rb Pharmaceuticals Ltd Microparticle buprenorphine suspension
GB2513267B (en) 2010-06-08 2015-03-18 Rb Pharmaceuticals Ltd Injectable flowable composition comprising buprenorphine
US9272044B2 (en) * 2010-06-08 2016-03-01 Indivior Uk Limited Injectable flowable composition buprenorphine
FR2975912B1 (fr) 2011-05-30 2013-06-14 Flamel Tech Sa Composition a liberation controlee de buprenorphine
ES2765036T3 (es) 2012-03-19 2020-06-05 Alkermes Pharma Ireland Ltd Composiciones farmacéuticas que comprenden esteres de ácidos grasos
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
CA3104099A1 (en) 2015-03-10 2016-09-15 Rhodes Technologies Acetate salt of buprenorphine and methods for preparing buprenorphine
SG11201901294QA (en) 2016-09-13 2019-03-28 Alar Pharmaceuticals Inc Sustained-release buprenorphine formulations background of invention
AR117426A1 (es) 2018-05-11 2021-08-04 Alar Pharmaceuticals Inc Formulaciones inyectables de acción prolongada y formas cristalinas de derivados de buprenorfina

Also Published As

Publication number Publication date
JP2023106478A (ja) 2023-08-01
AU2019266795B2 (en) 2023-02-09
NZ766474A (en) 2023-03-31
CA3089256A1 (en) 2019-11-14
ZA202004582B (en) 2023-01-25
AU2019266795A1 (en) 2020-08-13
EP3790881A4 (en) 2022-03-09
JP2021522306A (ja) 2021-08-30
TWI838372B (zh) 2024-04-11
WO2019214726A1 (en) 2019-11-14
KR20210021459A (ko) 2021-02-26
JP2025121948A (ja) 2025-08-20
US11524965B2 (en) 2022-12-13
CA3089256C (en) 2023-10-10
MX2020008471A (es) 2020-09-25
EP3790881B1 (en) 2026-04-15
KR102839314B1 (ko) 2025-07-29
AR117426A1 (es) 2021-08-04
JP7421804B2 (ja) 2024-01-25
US12522610B2 (en) 2026-01-13
CN111954672B (zh) 2023-09-01
EP3790881A1 (en) 2021-03-17
US20230002399A1 (en) 2023-01-05
TW202016117A (zh) 2020-05-01
CN111954672A (zh) 2020-11-17
KR20230093535A (ko) 2023-06-27
US20210122756A1 (en) 2021-04-29

Similar Documents

Publication Publication Date Title
US12522610B2 (en) Long-acting injectable formulations and crystalline forms of buprenorphine derivatives
EP2310363B1 (en) Anticancer oral formulation
ES2855976T3 (es) Behenato de rotigotina y procedimiento de fabricación y aplicación del mismo
US10744132B2 (en) Sustained-release buprenorphine formulations
WO2018177232A1 (zh) 难溶性复合物或其溶剂合物、药物组合物及其应用
CA3118921A1 (en) Naltrexone injectable sustained release formulation
HK40038905A (en) Long-acting injectable formulations and crystalline forms of buprenorphine derivatives
HK40038905B (zh) 丁丙诺啡衍生物的长效注射制剂及结晶形式
US20200352896A1 (en) Local anesthetic
EP3740190B1 (en) Apomorphine·palmitic acid cocrystal solid particle crystalline form
CN118598807A (zh) 多酚化衍生物前药化合物其在制备乙酸异丁酸蔗糖酯长效缓释原位凝胶中的应用
NZ750367B2 (en) Sustained-release buprenorphine formulations
CN113861048A (zh) 去甲曲马多的盐及其用途

Legal Events

Date Code Title Description
B350 Update of information on the portal [chapter 15.35 patent gazette]
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]