AU2008286979B2 - Quaternary opioid carboxamides - Google Patents

Quaternary opioid carboxamides Download PDF

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Publication number
AU2008286979B2
AU2008286979B2 AU2008286979A AU2008286979A AU2008286979B2 AU 2008286979 B2 AU2008286979 B2 AU 2008286979B2 AU 2008286979 A AU2008286979 A AU 2008286979A AU 2008286979 A AU2008286979 A AU 2008286979A AU 2008286979 B2 AU2008286979 B2 AU 2008286979B2
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hydrogen
alkyl
chosen
hydroxy
substituted
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AU2008286979A1 (en
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Mark P. Wentland
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Rensselaer Polytechnic Institute
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Rensselaer Polytechnic Institute
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    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Anesthesiology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
  • Saccharide Compounds (AREA)
AU2008286979A 2007-08-09 2008-08-08 Quaternary opioid carboxamides Active AU2008286979B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US95496007P 2007-08-09 2007-08-09
US60/954,960 2007-08-09
PCT/US2008/072632 WO2009023567A1 (en) 2007-08-09 2008-08-08 Quaternary opioid carboxamides

Publications (2)

Publication Number Publication Date
AU2008286979A1 AU2008286979A1 (en) 2009-02-19
AU2008286979B2 true AU2008286979B2 (en) 2013-03-28

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AU2008286979A Active AU2008286979B2 (en) 2007-08-09 2008-08-08 Quaternary opioid carboxamides

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Country Link
US (4) US8263807B2 (enExample)
EP (1) EP2190819B1 (enExample)
JP (1) JP5581211B2 (enExample)
KR (1) KR101519682B1 (enExample)
CN (1) CN101827819B (enExample)
AU (1) AU2008286979B2 (enExample)
BR (1) BRPI0815020A2 (enExample)
CA (1) CA2694497C (enExample)
EA (1) EA020658B1 (enExample)
ES (1) ES2586245T3 (enExample)
IL (1) IL203459A (enExample)
MX (1) MX2010001371A (enExample)
NO (1) NO341089B1 (enExample)
WO (1) WO2009023567A1 (enExample)

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US8436175B2 (en) * 2010-03-22 2013-05-07 Rensselaer Polytechnic Institute Carboxamide bioisosteres of opiates
NZ605234A (en) * 2010-07-08 2015-02-27 Alkermes Pharma Ireland Ltd Process for the synthesis of substituted morphinans
EP2407469A1 (en) * 2010-07-13 2012-01-18 Chemo Ibérica, S.A. Salt of sitagliptin
SMT202400030T1 (it) 2010-08-23 2024-03-13 Alkermes Pharma Ireland Ltd Metodi per trattare l'aumento di peso indotto da antipsicotici
US20120245193A1 (en) * 2011-02-14 2012-09-27 Alkermes, Inc. PERIPHERIALLY ACTING μ OPIOID ANTAGONISTS
BR112013022504A8 (pt) * 2011-03-03 2018-01-23 Cadila Healthcare Ltd sal de gentisato, de adipato, de ácido trifluoroacético, forma cristalina de hidrocloreto, forma cristalina de besilato, besilato amórfico e processos para a preparação dos mesmos
US9029543B2 (en) * 2011-04-05 2015-05-12 Alkermes, Inc. Process for the synthesis of quaternary amine compounds
US8962646B2 (en) 2011-06-29 2015-02-24 Alkermes, Inc. Peripherally acting opioid compounds
EP2788358B1 (en) * 2011-12-08 2018-08-29 Purdue Pharma LP Quaternized buprenorphine analogs
US9211293B2 (en) 2011-12-15 2015-12-15 Alkermes Pharma Ireland Limited Opioid agonist antagonist combinations
ES2692771T3 (es) 2011-12-15 2018-12-05 Alkermes Pharma Ireland Limited Samidorfano (ALKS 33) en combinación con buprenorfina para el tratamiento de trastornos depresivos
US20140066475A1 (en) 2012-09-04 2014-03-06 Euro-Celtique S.A. Method For Treating Pruritus
EP3003311A2 (en) 2013-05-24 2016-04-13 Alkermes Pharma Ireland Limited Methods for treating depressive symptoms
AU2014268361B2 (en) * 2013-05-24 2018-09-06 Alkermes Pharma Ireland Limited Morphan and morphinan analogues, and methods of use
WO2016138103A1 (en) * 2015-02-25 2016-09-01 Alkermes, Inc. Treatments for alzheimer's related diseases and disorders
CN113248435B (zh) * 2020-02-13 2024-06-04 上海翰森生物医药科技有限公司 3-甲酰胺基-4-羟基纳曲酮氘代衍生物、其制备方法及其在医药上的应用
EP4243768A1 (en) 2020-11-12 2023-09-20 Alkermes Pharma Ireland Limited Immediate release multilayer tablet
CN115521317B (zh) * 2021-02-02 2025-07-25 山东新时代药业有限公司 一种制备纳呋拉啡中间体的方法
WO2025104754A1 (en) * 2023-11-17 2025-05-22 Msn Laboratories Private Limited, R&D Center A process for the preparation of samidorphan and its intermediates
CN118598813B (zh) * 2024-08-08 2024-10-29 山东齐都药业有限公司 L-苹果酸萨米多芬及其制备方法

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DE2254298A1 (de) * 1972-11-06 1974-05-16 Boehringer Sohn Ingelheim Neue (heteroarylmethyl)-normorphine, deren saeureadditionssalze, verfahren zu deren herstellung sowie deren verwendung als arzneimittel
US4176186A (en) * 1978-07-28 1979-11-27 Boehringer Ingelheim Gmbh Quaternary derivatives of noroxymorphone which relieve intestinal immobility
ES2121553A1 (es) * 1996-12-23 1998-11-16 Univ Santiago Compostela Nuevos endoperoxidos morfinicos funcionalizados en posiciones c-6 y c-14 del anillo c y procedimiento para su obtencion.
US20050176645A1 (en) * 2002-02-22 2005-08-11 New River Pharmaceuticals Inc. Abuse-resistant hydrocodone compounds
WO2007022535A2 (en) * 2005-08-19 2007-02-22 Pharmacofore, Inc. Prodrugs of active agents

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DE10229842A1 (de) 2002-07-03 2004-02-05 Helmut Prof. Dr. Schmidhammer Morphinanderivate und deren quartäre Ammoniumsalze substituiert in Position 14, Herstellungsverfahren und Verwendung
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Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB874217A (en) * 1958-10-30 1961-08-02 Albert Boehringer Normorphine derivatives
DE2254298A1 (de) * 1972-11-06 1974-05-16 Boehringer Sohn Ingelheim Neue (heteroarylmethyl)-normorphine, deren saeureadditionssalze, verfahren zu deren herstellung sowie deren verwendung als arzneimittel
US4176186A (en) * 1978-07-28 1979-11-27 Boehringer Ingelheim Gmbh Quaternary derivatives of noroxymorphone which relieve intestinal immobility
ES2121553A1 (es) * 1996-12-23 1998-11-16 Univ Santiago Compostela Nuevos endoperoxidos morfinicos funcionalizados en posiciones c-6 y c-14 del anillo c y procedimiento para su obtencion.
US20050176645A1 (en) * 2002-02-22 2005-08-11 New River Pharmaceuticals Inc. Abuse-resistant hydrocodone compounds
WO2007022535A2 (en) * 2005-08-19 2007-02-22 Pharmacofore, Inc. Prodrugs of active agents

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Publication number Publication date
EA201070237A1 (ru) 2010-10-29
KR101519682B1 (ko) 2015-05-19
KR20100053627A (ko) 2010-05-20
WO2009023567A1 (en) 2009-02-19
US20140107143A1 (en) 2014-04-17
NO341089B1 (no) 2017-08-21
US20090197905A1 (en) 2009-08-06
CN101827819A (zh) 2010-09-08
US8563572B2 (en) 2013-10-22
CN101827819B (zh) 2013-06-12
MX2010001371A (es) 2010-03-10
CA2694497C (en) 2016-07-12
US20120302594A1 (en) 2012-11-29
AU2008286979A1 (en) 2009-02-19
NO20100289L (no) 2010-03-02
CA2694497A1 (en) 2009-02-19
JP2010535814A (ja) 2010-11-25
US20170095469A1 (en) 2017-04-06
EP2190819B1 (en) 2016-05-25
IL203459A (en) 2016-02-29
JP5581211B2 (ja) 2014-08-27
ES2586245T3 (es) 2016-10-13
EA020658B1 (ru) 2014-12-30
EP2190819A1 (en) 2010-06-02
BRPI0815020A2 (pt) 2015-03-10
HK1141295A1 (zh) 2010-11-05
US8263807B2 (en) 2012-09-11

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