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
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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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C219/00—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C219/02—Compounds 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
    • C07C219/20—Compounds 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
    • C07C219/22—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic 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
    • C07D221/22—Bridged ring systems
    • C07D221/26—Benzomorphans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic 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
    • C07D221/22—Bridged ring systems
    • C07D221/28—Morphinans
    • 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
    • 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:
    • C07D489/06—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 a hetero atom directly attached in position 14
    • C07D489/08—Oxygen 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)
  • Dermatology (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (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) JP7535569B2 (fr)
CN (1) CN114828961B (fr)
CA (1) CA3149152A1 (fr)
MX (1) MX2022001520A (fr)
WO (1) WO2021029914A1 (fr)

Family Cites Families (25)

* 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
EP1309354A2 (fr) 2000-07-27 2003-05-14 Rutgers, The State University Polyesters et polyamides therapeutiques
US6569449B1 (en) * 2000-11-13 2003-05-27 University Of Kentucky Research Foundation Transdermal delivery of opioid antagonist prodrugs
US20040033253A1 (en) 2002-02-19 2004-02-19 Ihor Shevchuk Acyl opioid antagonists
WO2005009377A2 (fr) 2003-07-23 2005-02-03 University Of Kentucky Research Foundation Nouveaux promedicaments assimilables par voie orale
US20050137141A1 (en) 2003-10-24 2005-06-23 John Hilfinger Prodrug composition
US8163701B2 (en) 2005-08-19 2012-04-24 Signature Therapeutics, Inc. Prodrugs of active agents
US20090192095A1 (en) 2008-01-18 2009-07-30 Shire Llc Amino acid and peptide prodrugs of opioid analgesics with reduced gi side-effects
BRPI1015108A2 (pt) 2009-04-02 2016-04-26 Shire Llc pró-fármacos de aminoácidos e peptídios ligados a ácido dicarboxílico de opiáceos e seus usos
WO2011007247A1 (fr) 2009-07-17 2011-01-20 Llc Shire Nouvel acide amine de carbamate et promedicaments peptidiques d'opioïdes, et utilisations associees
MX2012000980A (es) 2009-07-21 2012-06-12 Nektar Therapeutics Conjugados de agonistas de oligómeros-opioides.
US20110190267A1 (en) * 2010-01-05 2011-08-04 Shire Pharmaceuticals, Inc. Prodrugs of opioids and uses thereof
US8461171B2 (en) 2010-02-09 2013-06-11 QRxPharma Ltd. Hybrid opioid compounds and compositions
CA2795156C (fr) * 2010-04-02 2019-05-14 Alltranz Inc. Prodrogues opioides administrables par voie transdermique, compositions anti-abus et methodes d'utilisation de prodrogues opioides
EP2658523A1 (fr) 2010-12-28 2013-11-06 Euro-Celtique S.A. Combinaison d'un agoniste des opioïdes et d'un antagoniste des opioïdes dans le traitement de la maladie de parkinson
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
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
US9987269B2 (en) 2015-04-27 2018-06-05 3St Research Llc Alpha-hydroxy carboxylic acid and derivatives and other GRAS-based prodrugs of oxymorphone and uses thereof
CN107427509B (zh) * 2015-08-29 2021-06-15 美德阿利克斯株式会社 含有碱性药物和山梨酸的经皮吸收组成物
US12590065B2 (en) 2017-04-14 2026-03-31 Zevra Therapeutics, Inc. Levorphanol prodrugs and processes for making and using them
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
JP2022544564A (ja) 2022-10-19
WO2021029914A1 (fr) 2021-02-18
CN114828961A (zh) 2022-07-29
MX2022001520A (es) 2022-07-21
CN114828961B (zh) 2024-03-29
EP4010078A1 (fr) 2022-06-15
EP4010078A4 (fr) 2023-08-09
JP7535569B2 (ja) 2024-08-16

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