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
Authority
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
Other languages
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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Classifications

    • 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

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 US11186585B2 (en) 2018-08-17 2019-08-14 Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates
US16/540,058 2019-08-14
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
DE69427551T2 (de) * 1993-03-15 2002-05-16 Nat Science Council Taipeh T A Nalbuphinester und diese enthaltende Arzneimittel mit verzögerter Wirkstoffabgabe
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
ES2188481T3 (es) 2000-04-27 2003-07-01 Oliver Yoa-Pu Hu Derivados de polinalbufina.
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
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
EP1928881A2 (fr) 2005-08-19 2008-06-11 Pharmacofore, Inc. Promedicaments d'agents actifs
WO2009092071A2 (fr) 2008-01-18 2009-07-23 Shire Llc Promédicaments à base d'acides aminés et de peptides d'analgésiques phénoliques et leurs utilisations
MX2011010448A (es) 2009-04-02 2011-10-28 Shire Llc Profarmacos de opioides novedosos de amino acidos y peptidos enlazados a acido dicarboxilico y usos de los mismos.
JP2013527124A (ja) 2009-07-17 2013-06-27 シャイア エルエルシー オピオイドの新規カルバマートアミノ酸およびペプチドプロドラッグならびにその使用
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
EP4010078A1 (fr) 2022-06-15
EP4010078A4 (fr) 2023-08-09
MX2022001520A (es) 2022-07-21
CN114828961A (zh) 2022-07-29
JP2022544564A (ja) 2022-10-19
CN114828961B (zh) 2024-03-29
WO2021029914A1 (fr) 2021-02-18

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Effective date: 20240305