CA3149152A1 - Compositions et procedes pour ameliorer la mobilisation de recepteur opioide par des hexadienoates d'opioides et des hexadienoates eventuellement substitues - Google Patents

Compositions et procedes pour ameliorer la mobilisation de recepteur opioide par des hexadienoates d'opioides et des hexadienoates eventuellement substitues Download PDF

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Publication number
CA3149152A1
CA3149152A1 CA3149152A CA3149152A CA3149152A1 CA 3149152 A1 CA3149152 A1 CA 3149152A1 CA 3149152 A CA3149152 A CA 3149152A CA 3149152 A CA3149152 A CA 3149152A CA 3149152 A1 CA3149152 A1 CA 3149152A1
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CA
Canada
Prior art keywords
hexadienoate
compound
opioid
naloxone
methylhexadienoate
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CA3149152A
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English (en)
Inventor
Georgiy Nikonov
Levon Isakulyan
Michael V. Voronkov
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Kappa Pharma LLC
Original Assignee
Kappa Pharma LLC
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
Priority claimed from US16/540,058 external-priority patent/US11186585B2/en
Application filed by Kappa Pharma LLC filed Critical Kappa Pharma LLC
Publication of CA3149152A1 publication Critical patent/CA3149152A1/fr
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C219/00Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C219/02Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C219/20Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
    • C07C219/22Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/22Bridged ring systems
    • C07D221/26Benzomorphans
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/22Bridged ring systems
    • C07D221/28Morphinans
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D489/00Heterocyclic 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:
    • C07D489/02Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D489/00Heterocyclic 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:
    • C07D489/06Heterocyclic 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 a hetero atom directly attached in position 14
    • C07D489/08Oxygen atom

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Addiction (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La présente invention concerne des compositions dérivées d'opiacés et leurs antagonistes utiles dans des domaines thérapeutiques associées à la modulation des récepteurs opioïdes. Une modification de 3-hexanediénoate des opioïdes est formulée pour améliorer la mobilisation d'opiacés des récepteurs opioïdes lorsqu'ils sont administrés par voie orale. L'invention concerne une modification de 3-hexanediénoate de Nalbuphine ou d'un sel pharmaceutiquement acceptable de celle-ci pour améliorer la qualité de la gestion de la douleur lorsqu'elle est administrée par voie intraveineuse, intranasale, transdermique, sublinguale, rectale, topique, intramusculaire, sous-cutanée ou par inhalation. Une modification de 3-hexanediénoate des antagonistes d'opioïdes est formulée pour améliorer l'inhibition des récepteurs opioïdes lorsqu'ils sont administrés par voie orale. L'invention concerne une modification de 3-hexanediénoate de Naloxone ou d'un sel pharmaceutiquement acceptable de celle-ci pour améliorer la qualité du sevrage lorsqu'elle est administrée par voie intraveineuse, intranasale, transdermique, sublinguale, rectale, topique, intramusculaire, sous-cutanée ou par inhalation.
CA3149152A 2019-08-11 2020-03-07 Compositions et procedes pour ameliorer la mobilisation de recepteur opioide par des hexadienoates d'opioides et des hexadienoates eventuellement substitues Pending CA3149152A1 (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962885311P 2019-08-11 2019-08-11
US62/885,311 2019-08-11
US16/540,058 2019-08-14
US16/540,058 US11186585B2 (en) 2018-08-17 2019-08-14 Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates
PCT/US2020/021599 WO2021029914A1 (fr) 2019-08-11 2020-03-07 Compositions et procédés pour améliorer la mobilisation de récepteur opioïde par des héxadiénoates d'opioïdes et des héxadiénoates éventuellement substitués

Publications (1)

Publication Number Publication Date
CA3149152A1 true CA3149152A1 (fr) 2021-02-18

Family

ID=74571142

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3149152A Pending CA3149152A1 (fr) 2019-08-11 2020-03-07 Compositions et procedes pour ameliorer la mobilisation de recepteur opioide par des hexadienoates d'opioides et des hexadienoates eventuellement substitues

Country Status (6)

Country Link
EP (1) EP4010078A4 (fr)
JP (1) JP2022544564A (fr)
CN (1) CN114828961B (fr)
CA (1) CA3149152A1 (fr)
MX (1) MX2022001520A (fr)
WO (1) WO2021029914A1 (fr)

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4668685A (en) 1984-07-05 1987-05-26 E.I. Du Pont De Nemours And Company Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, which are analgesics or narcotic antagonists
EP0615756B1 (fr) * 1993-03-15 2001-06-27 National Science Council Esters de nalbuphine, et compositions pharmaceutiques à action prolongée les contenant
CN1050130C (zh) 1997-07-04 2000-03-08 卢正堂 纳洛酮酸脂和纳屈酮酸脂及系列物和制备方法
DE60001487T2 (de) 2000-04-27 2003-12-24 Oliver Yoa-Pu Hu Polynalbuphinderivat
TWI226239B (en) 2000-05-15 2005-01-11 You-Pu Hu Novel oral pharmaceutical composition containing nalbuphine ester prodrug
CA2417389C (fr) 2000-07-27 2012-05-29 Rutgers, The State University Polyesters et polyamides therapeutiques
US20040033253A1 (en) 2002-02-19 2004-02-19 Ihor Shevchuk Acyl opioid antagonists
US7759358B2 (en) 2003-07-23 2010-07-20 Crooks Peter A Oral bioavailable prodrugs
US20050137141A1 (en) 2003-10-24 2005-06-23 John Hilfinger Prodrug composition
WO2007022535A2 (fr) 2005-08-19 2007-02-22 Pharmacofore, Inc. Promedicaments d'agents actifs
WO2009092073A2 (fr) 2008-01-18 2009-07-23 Shire Llc Promédicaments à base d'acides aminés et de peptides d'analgésiques opioïdes avec effets secondaires gi réduits
JP2013523599A (ja) 2009-04-02 2013-06-17 シャイア エルエルシー 新規なオピオイドのジカルボン酸結合アミノ酸及びペプチドプロドラッグ並びにその用途
WO2011007247A1 (fr) 2009-07-17 2011-01-20 Llc Shire Nouvel acide amine de carbamate et promedicaments peptidiques d'opioïdes, et utilisations associees
WO2011083304A1 (fr) 2010-01-05 2011-07-14 Shire Llc Promédicaments d'opioïdes et leurs utilisations
JP5941038B2 (ja) * 2010-04-02 2016-06-29 ジネルバ ファーマシューティカルズ, インコーポレイティド 経皮送達可能なオピオイドプロドラッグ、乱用抵抗性組成物及びオピオイドプロドラッグを使用する方法
US10449190B2 (en) * 2015-04-27 2019-10-22 John K. Thottathil Alpha-hydroxy carboxylic acid and derivatives and other GRAS-based prodrugs of opioids and uses thereof
US10017519B2 (en) * 2015-04-27 2018-07-10 3St Research Llc Alpha-hydroxy carboxylic acid and derivatives and other GRAS based prodrugs of oxycodone and uses thereof
US9974858B2 (en) * 2015-08-29 2018-05-22 Medrx Co., Ltd Percutaneous absorption composition
US11186585B2 (en) * 2018-08-17 2021-11-30 Kappa-Pharma LLC Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates

Also Published As

Publication number Publication date
WO2021029914A1 (fr) 2021-02-18
CN114828961B (zh) 2024-03-29
JP2022544564A (ja) 2022-10-19
EP4010078A1 (fr) 2022-06-15
EP4010078A4 (fr) 2023-08-09
MX2022001520A (es) 2022-07-21
CN114828961A (zh) 2022-07-29

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Effective date: 20240305