CA2754984C - Morphinan derivatives with high oral bioavailability - Google Patents

Morphinan derivatives with high oral bioavailability Download PDF

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Publication number
CA2754984C
CA2754984C CA2754984A CA2754984A CA2754984C CA 2754984 C CA2754984 C CA 2754984C CA 2754984 A CA2754984 A CA 2754984A CA 2754984 A CA2754984 A CA 2754984A CA 2754984 C CA2754984 C CA 2754984C
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Canada
Prior art keywords
compound
disease
pharmaceutically acceptable
formula
day
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.)
Active
Application number
CA2754984A
Other languages
English (en)
French (fr)
Other versions
CA2754984A1 (en
Inventor
Ryan Turncliff
Daniel Deaver
Derrick Arnelle
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.)
Alkermes Pharma Ireland Ltd
Original Assignee
Alkermes Pharma Ireland Ltd
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
Application filed by Alkermes Pharma Ireland Ltd filed Critical Alkermes Pharma Ireland Ltd
Publication of CA2754984A1 publication Critical patent/CA2754984A1/en
Application granted granted Critical
Publication of CA2754984C publication Critical patent/CA2754984C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/24—Antidepressants
    • 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
    • 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
    • A61P25/32—Alcohol-abuse
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA2754984A 2009-03-19 2009-12-04 Morphinan derivatives with high oral bioavailability Active CA2754984C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US16170209P 2009-03-19 2009-03-19
US61/161,702 2009-03-19
PCT/US2009/066801 WO2010107457A1 (en) 2009-03-19 2009-12-04 Morphinan derivatives with high oral bioavailability

Publications (2)

Publication Number Publication Date
CA2754984A1 CA2754984A1 (en) 2010-09-23
CA2754984C true CA2754984C (en) 2018-06-26

Family

ID=42738186

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2754984A Active CA2754984C (en) 2009-03-19 2009-12-04 Morphinan derivatives with high oral bioavailability

Country Status (6)

Country Link
US (4) US20100240691A1 (https=)
EP (2) EP2408303A4 (https=)
JP (4) JP5555890B2 (https=)
AU (1) AU2009342654B2 (https=)
CA (1) CA2754984C (https=)
WO (1) WO2010107457A1 (https=)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2408303A4 (en) * 2009-03-19 2012-07-25 Alkermes Inc MORPHINANE DERIVATIVES HAVING HIGH ORAL BIOLOGICAL AVAILABILITY
US9119848B2 (en) * 2009-12-04 2015-09-01 Alkermes Pharma Ireland Limited Morphinan derivatives for the treatment of drug overdose
HUE065427T2 (hu) 2010-08-23 2024-05-28 Alkermes Pharma Ireland Ltd Eljárások antipszichotikum által indukált súlygyarapodás kezelésére
MX375348B (es) * 2011-12-15 2025-03-06 Alkermes Pharma Ireland Ltd Composiciones de la buprenorfina y antagonistas de los receptores opioide-mu.
US9211293B2 (en) 2011-12-15 2015-12-15 Alkermes Pharma Ireland Limited Opioid agonist antagonist combinations
US10195191B2 (en) 2011-12-15 2019-02-05 Alkermes Pharma Ireland Limited Opioid agonist antagonist combinations
EP2790703B1 (en) * 2011-12-15 2019-06-12 Alkermes Pharma Ireland Limited Samidorphan (alks 33) in combination with opioid agonists
US8637538B1 (en) 2012-12-14 2014-01-28 Trevi Therapeutics, Inc. Methods for treatment of pruritis
US8987289B2 (en) 2012-12-14 2015-03-24 Trevi Therapeutics, Inc. Methods for treating pruritus
US20140179727A1 (en) 2012-12-14 2014-06-26 Trevi Therapeutics, Inc. Methods for treating pruritus
CA2911231C (en) 2013-05-24 2021-12-07 Alkermes Pharma Ireland Limited Morphan and morphinan analogues, and methods of use
EP3003311A2 (en) 2013-05-24 2016-04-13 Alkermes Pharma Ireland Limited Methods for treating depressive symptoms
IL318587A (en) 2018-07-23 2025-03-01 Trevi Therapeutics Inc Treatment of chronic cough, shortness of breath and wheezing
IL294601A (en) 2020-01-10 2022-09-01 Trevi Therapeutics Inc Methods of administration of nalbuphine
WO2021178405A1 (en) * 2020-03-02 2021-09-10 University Of Southern California Opioid receptor antagonists
WO2022101444A1 (en) 2020-11-12 2022-05-19 Alkermes Pharma Ireland Limited Immediate release multilayer tablet
WO2025038406A1 (en) * 2023-08-11 2025-02-20 Virginia Commonwealth University Design, synthesis, and biological evaluation of nitrogen-walk derivatives of nan as mu opioid receptor selective modulators

Family Cites Families (24)

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US3856795A (en) * 1972-04-25 1974-12-24 American Home Prod Process for preparation of secondary amines from tertiary amines
US4032529A (en) * 1974-09-20 1977-06-28 Sterling Drug Inc. Aminomethanobenzazocine intermediates
US3957793A (en) * 1974-09-20 1976-05-18 Sterling Drug Inc. Hydroxyiminobenzazocines
US4127577A (en) * 1975-11-24 1978-11-28 Sterling Drug Inc. Aminomethanobenzazocine process
US4205171A (en) * 1976-01-12 1980-05-27 Sterling Drug Inc. Aminomethanobenzazocines and nitromethanobenzazocines
US4464378A (en) * 1981-04-28 1984-08-07 University Of Kentucky Research Foundation Method of administering narcotic antagonists and analgesics and novel dosage forms containing same
US4649200A (en) * 1986-05-08 1987-03-10 Regents Of The University Of Minnesota Substituted pyrroles with opioid receptor activity
US5028612A (en) * 1990-03-22 1991-07-02 Hillel Glover Method for treating emotional numbness
US5258386A (en) * 1991-06-05 1993-11-02 The United States Of America As Represented By The Secretary Of The Army (+)-3-substituted-N alkylmorphinans, synthesis and use as anticonvulsant and neuroprotective agents
US5607941A (en) * 1992-06-26 1997-03-04 Boehringer Ingelheim Kg Useful for treating neurodegenerative diseases
US5512593A (en) * 1993-03-02 1996-04-30 John S. Nagle Composition and method of treating depression using natoxone or naltrexone in combination with a serotonin reuptake inhibitor
BR9707136A (pt) * 1996-01-10 1999-08-31 Smithkline Beecham Spa Derivados morfinóides condesados em heterociclo (ii)
GB9912411D0 (en) * 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
JP4340437B2 (ja) * 2000-10-31 2009-10-07 レンセラール ポリテクニック インスティチュート ８−カルボキサミド−２，６−メタノ−３−ベンズアゾシン
MXPA06013270A (es) * 2004-05-14 2007-04-23 Johnson & Johnson Compuestos de opioide carboxamido.
US20060063792A1 (en) * 2004-09-17 2006-03-23 Adolor Corporation Substituted morphinans and methods of their use
PT2251330E (pt) * 2004-11-05 2012-07-20 Rensselaer Polytech Inst 4-hidroxibenzomorfanos
US20070099947A1 (en) * 2005-11-03 2007-05-03 Alkermes, Inc. Methods and compositions for the treatment of brain reward system disorders by combination therapy
US20090214650A1 (en) * 2006-02-01 2009-08-27 Alkermes, Inc. Methods of Treating alcoholism and alcohol related disorders using combination drug therapy and swellable polymers
AU2008286979B2 (en) * 2007-08-09 2013-03-28 Rensselaer Polytechnic Institute Quaternary opioid carboxamides
EP2408303A4 (en) * 2009-03-19 2012-07-25 Alkermes Inc MORPHINANE DERIVATIVES HAVING HIGH ORAL BIOLOGICAL AVAILABILITY
WO2010141666A2 (en) * 2009-06-04 2010-12-09 The General Hospital Corporation Modulating endogenous beta-endorphin levels
US9211293B2 (en) * 2011-12-15 2015-12-15 Alkermes Pharma Ireland Limited Opioid agonist antagonist combinations
JP5929635B2 (ja) * 2012-08-30 2016-06-08 株式会社デンソー 多段式横型鍛造装置

Also Published As

Publication number Publication date
EP2408303A4 (en) 2012-07-25
JP6362644B2 (ja) 2018-07-25
AU2009342654A1 (en) 2011-10-06
JP2012520877A (ja) 2012-09-10
US20200383970A1 (en) 2020-12-10
US20150094325A1 (en) 2015-04-02
WO2010107457A1 (en) 2010-09-23
JP2016185995A (ja) 2016-10-27
JP2014101388A (ja) 2014-06-05
US20170112827A1 (en) 2017-04-27
AU2009342654B2 (en) 2013-09-05
JP2014139257A (ja) 2014-07-31
JP5555890B2 (ja) 2014-07-23
EP3170395A1 (en) 2017-05-24
CA2754984A1 (en) 2010-09-23
US20100240691A1 (en) 2010-09-23
EP2408303A1 (en) 2012-01-25

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