EP4010078A4 - COMPOSITIONS AND METHODS FOR ENHANCING OPIOID RECEPTOR MOBILIZATION BY OPIOID HEXADENOATES AND OPTIONALLY SUBSTITUTED HEXADIENATES - Google Patents

COMPOSITIONS AND METHODS FOR ENHANCING OPIOID RECEPTOR MOBILIZATION BY OPIOID HEXADENOATES AND OPTIONALLY SUBSTITUTED HEXADIENATES Download PDF

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Publication number
EP4010078A4
EP4010078A4 EP20852037.9A EP20852037A EP4010078A4 EP 4010078 A4 EP4010078 A4 EP 4010078A4 EP 20852037 A EP20852037 A EP 20852037A EP 4010078 A4 EP4010078 A4 EP 4010078A4
Authority
EP
European Patent Office
Prior art keywords
hexadienoates
opioid
compositions
methods
optionally substituted
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
EP20852037.9A
Other languages
German (de)
English (en)
French (fr)
Other versions
EP4010078A1 (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 EP4010078A1 publication Critical patent/EP4010078A1/en
Publication of EP4010078A4 publication Critical patent/EP4010078A4/en
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

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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)
EP20852037.9A 2019-08-11 2020-03-07 COMPOSITIONS AND METHODS FOR ENHANCING OPIOID RECEPTOR MOBILIZATION BY OPIOID HEXADENOATES AND OPTIONALLY SUBSTITUTED HEXADIENATES Pending EP4010078A4 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962885311P 2019-08-11 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
PCT/US2020/021599 WO2021029914A1 (en) 2019-08-11 2020-03-07 Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates

Publications (2)

Publication Number Publication Date
EP4010078A1 EP4010078A1 (en) 2022-06-15
EP4010078A4 true EP4010078A4 (en) 2023-08-09

Family

ID=74571142

Family Applications (1)

Application Number Title Priority Date Filing Date
EP20852037.9A Pending EP4010078A4 (en) 2019-08-11 2020-03-07 COMPOSITIONS AND METHODS FOR ENHANCING OPIOID RECEPTOR MOBILIZATION BY OPIOID HEXADENOATES AND OPTIONALLY SUBSTITUTED HEXADIENATES

Country Status (6)

Country Link
EP (1) EP4010078A4 (https=)
JP (1) JP7535569B2 (https=)
CN (1) CN114828961B (https=)
CA (1) CA3149152A1 (https=)
MX (1) MX2022001520A (https=)
WO (1) WO2021029914A1 (https=)

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0615756A1 (en) * 1993-03-15 1994-09-21 National Science Council Nalbuphine esters and long-acting pharmaceutical compositions containing them

Family Cites Families (24)

* 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
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 (en) 2000-07-27 2003-05-14 Rutgers, The State University Therapeutic polyesters and polyamides
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 (en) 2003-07-23 2005-02-03 University Of Kentucky Research Foundation Novel oral bioavailable prodrugs
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 (en) 2009-07-17 2011-01-20 Llc Shire Novel carbamate amino acid and peptide prodrugs of opioids and uses thereof
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 (en) * 2010-04-02 2019-05-14 Alltranz Inc. Transdermally deliverable opioid prodrugs, abuse-resistant compositions and methods of using opioid prodrugs
EP2658523A1 (en) 2010-12-28 2013-11-06 Euro-Celtique S.A. A combination of an opioid agonist and an opioid antagonist in the treatment of parkinson's disease
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0615756A1 (en) * 1993-03-15 1994-09-21 National Science Council Nalbuphine esters and long-acting pharmaceutical compositions containing them

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
PENG, X. ET AL.: "Synthesis and Preliminary In vitro Investigation of Bivalent Ligands Containing Homo- and Heterodimeric Pharmacophores at [mu], [delta], and [kappa] Opioid Receptors", JOURNAL OF MEDICINAL CHEMISTRY, vol. 49, no. 1, 2005, pages 256 - 262, XP055925192, ISSN: 0022-2623, DOI: 10.1021/jm050577x *

Also Published As

Publication number Publication date
JP2022544564A (ja) 2022-10-19
WO2021029914A1 (en) 2021-02-18
CN114828961A (zh) 2022-07-29
MX2022001520A (es) 2022-07-21
CN114828961B (zh) 2024-03-29
CA3149152A1 (en) 2021-02-18
EP4010078A1 (en) 2022-06-15
JP7535569B2 (ja) 2024-08-16

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