CN114828961B - 通过阿片类己二烯酸酯和任选取代的己二烯酸酯增强阿片受体结合的组合物及方法 - Google Patents

通过阿片类己二烯酸酯和任选取代的己二烯酸酯增强阿片受体结合的组合物及方法 Download PDF

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Publication number
CN114828961B
CN114828961B CN202080071185.9A CN202080071185A CN114828961B CN 114828961 B CN114828961 B CN 114828961B CN 202080071185 A CN202080071185 A CN 202080071185A CN 114828961 B CN114828961 B CN 114828961B
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opioid
nalbuphine
naloxone
compound
composition
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Chinese (zh)
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CN114828961A (zh
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G·尼科诺夫
L·伊萨库兰
M·V·沃隆科夫
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Kapa Pharmaceutical Co ltd
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Kapa Pharmaceutical Co ltd
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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)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Addiction (AREA)
  • Psychology (AREA)
  • Dermatology (AREA)
  • Psychiatry (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)
CN202080071185.9A 2019-08-11 2020-03-07 通过阿片类己二烯酸酯和任选取代的己二烯酸酯增强阿片受体结合的组合物及方法 Active CN114828961B (zh)

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 (en) 2019-08-11 2020-03-07 Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates

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CN114828961A CN114828961A (zh) 2022-07-29
CN114828961B true CN114828961B (zh) 2024-03-29

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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
WO2017091827A1 (en) * 2015-11-29 2017-06-01 Thottathil John K Novel alpha-hydroxy carboxylic acid and derivatives and other gras based prodrugs of oxycodone and uses thereof

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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 (en) * 1993-03-15 2001-06-27 National Science Council Nalbuphine esters and long-acting pharmaceutical compositions containing them
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
CA2771263A1 (en) 2000-07-27 2002-02-07 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
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 (en) 2005-08-19 2008-06-11 Pharmacofore, Inc. Prodrugs of active agents
US20090186832A1 (en) 2008-01-18 2009-07-23 Shire Llc Amino acid peptide pro-drugs of phenolic analgesics and uses thereof
EP2413937A1 (en) 2009-04-02 2012-02-08 Shire LLC Novel dicarboxylic acid linked amino acid and peptide prodrugs of opioids and uses thereof
AU2010272233A1 (en) 2009-07-17 2012-02-09 Shire Llc Novel carbamate amino acid and peptide prodrugs of opioids and uses thereof
EP2628489B1 (en) * 2009-07-21 2017-03-01 Nektar Therapeutics PEG oligomer-fentanyl conjugates
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
EP2552924B1 (en) * 2010-04-02 2015-09-16 Zynerba Pharmaceuticals, Inc. Transdermally deliverable opioid prodrugs, abuse-resistant compositions and methods of using opioid prodrugs
AR084620A1 (es) * 2010-12-28 2013-05-29 Euro Celtique Sa Una combinacion de un agonista opiaceo y un antagonista opiaceo en el tratamiento de la enfermedad de parkinson
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
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
US9974858B2 (en) * 2015-08-29 2018-05-22 Medrx Co., Ltd Percutaneous absorption composition
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

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017091827A1 (en) * 2015-11-29 2017-06-01 Thottathil John K Novel alpha-hydroxy carboxylic acid and derivatives and other gras based prodrugs of oxycodone and uses thereof

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Publication number Publication date
MX2022001520A (es) 2022-07-21
JP7535569B2 (ja) 2024-08-16
CA3149152A1 (en) 2021-02-18
JP2022544564A (ja) 2022-10-19
EP4010078A4 (en) 2023-08-09
WO2021029914A1 (en) 2021-02-18
EP4010078A1 (en) 2022-06-15
CN114828961A (zh) 2022-07-29

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