CA2694497C - Quaternary opioid carboxamides - Google Patents

Quaternary opioid carboxamides Download PDF

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Publication number
CA2694497C
CA2694497C CA2694497A CA2694497A CA2694497C CA 2694497 C CA2694497 C CA 2694497C CA 2694497 A CA2694497 A CA 2694497A CA 2694497 A CA2694497 A CA 2694497A CA 2694497 C CA2694497 C CA 2694497C
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compound
compounds
morphine
hydrogen
alkyl
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CA2694497A
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English (en)
French (fr)
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CA2694497A1 (en
Inventor
Mark P. Wentland
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Rensselaer Polytechnic Institute
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Rensselaer Polytechnic Institute
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic 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
    • C07D221/22Bridged ring systems
    • C07D221/28Morphinans
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/485Morphinan derivatives, e.g. morphine, codeine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/20Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D489/00Heterocyclic 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:
    • C07D489/06Heterocyclic 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
    • C07D489/08Oxygen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/12Heterocyclic 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
    • C07D491/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/22Heterocyclic 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Anesthesiology (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)
CA2694497A 2007-08-09 2008-08-08 Quaternary opioid carboxamides Active CA2694497C (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
CA2694497A1 CA2694497A1 (en) 2009-02-19
CA2694497C true CA2694497C (en) 2016-07-12

Family

ID=39941437

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2694497A Active CA2694497C (en) 2007-08-09 2008-08-08 Quaternary opioid carboxamides

Country Status (14)

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

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JP5555890B2 (ja) * 2009-03-19 2014-07-23 アルカーメス ファーマ アイルランド リミテッド 高い経口バイオアベイラビリティを有するモルフィナン誘導体
US9119848B2 (en) 2009-12-04 2015-09-01 Alkermes Pharma Ireland Limited Morphinan derivatives for the treatment of drug overdose
EP2550253B9 (en) 2010-03-22 2016-09-21 Rensselaer Polytechnic Institute Morphinane derivatives containing a carboxamide group as opioid receptor ligands
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
NZ606730A (en) 2010-08-23 2015-05-29 Alkermes Pharma Ireland Ltd Methods for treating antipsychotic-induced weight gain
JP2014505113A (ja) * 2011-02-14 2014-02-27 アルカーメス,インコーポレイテッド 末梢作用性μオピオイドアンタゴニスト
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CA2840643C (en) * 2011-06-29 2017-11-21 Alkermes, Inc. Peripherally acting opioid compounds
US9096606B2 (en) 2011-12-08 2015-08-04 Purdue Pharma, L.P. Quarternized buprenorphine analogs
TR201815154T4 (tr) 2011-12-15 2018-11-21 Alkermes Pharma Ireland Ltd Depresi̇f bozukluklarin tedavi̇si̇ne yöneli̇k buprenorfi̇n i̇le kombi̇nasyon hali̇nde sami̇dorfan (alks 33).
US9211293B2 (en) 2011-12-15 2015-12-15 Alkermes Pharma Ireland Limited Opioid agonist antagonist combinations
US20140066475A1 (en) 2012-09-04 2014-03-06 Euro-Celtique S.A. Method For Treating Pruritus
JP2016519161A (ja) 2013-05-24 2016-06-30 アルカームス ファーマ アイルランド リミテッド モルファン及びモルフィナン類似物及び使用の方法
WO2014190271A2 (en) 2013-05-24 2014-11-27 Alkermes Pharma Ireland Limted Methods for treating depressive symptoms
US20160243112A1 (en) * 2015-02-25 2016-08-25 Alkermes, Inc. Treatments for alzheimer's related diseases and disorders
TW202140009A (zh) * 2020-02-13 2021-11-01 大陸商上海翰森生物醫藥科技有限公司 3-甲醯胺基-4-羥基納曲酮氘代衍生物、其製備方法及其在醫藥上的應用
WO2022101444A1 (en) 2020-11-12 2022-05-19 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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Also Published As

Publication number Publication date
US20090197905A1 (en) 2009-08-06
EP2190819A1 (en) 2010-06-02
JP2010535814A (ja) 2010-11-25
US20120302594A1 (en) 2012-11-29
KR20100053627A (ko) 2010-05-20
US20170095469A1 (en) 2017-04-06
CN101827819B (zh) 2013-06-12
BRPI0815020A2 (pt) 2015-03-10
EA201070237A1 (ru) 2010-10-29
IL203459A (en) 2016-02-29
US8263807B2 (en) 2012-09-11
JP5581211B2 (ja) 2014-08-27
EA020658B1 (ru) 2014-12-30
MX2010001371A (es) 2010-03-10
KR101519682B1 (ko) 2015-05-19
CA2694497A1 (en) 2009-02-19
WO2009023567A1 (en) 2009-02-19
US8563572B2 (en) 2013-10-22
ES2586245T3 (es) 2016-10-13
AU2008286979B2 (en) 2013-03-28
US20140107143A1 (en) 2014-04-17
CN101827819A (zh) 2010-09-08
NO341089B1 (no) 2017-08-21
AU2008286979A1 (en) 2009-02-19
EP2190819B1 (en) 2016-05-25
NO20100289L (no) 2010-03-02
HK1141295A1 (zh) 2010-11-05

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