KR101519682B1 - 4급 오피오이드 카르복스아미드 - Google Patents

4급 오피오이드 카르복스아미드 Download PDF

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KR101519682B1
KR101519682B1 KR1020107005151A KR20107005151A KR101519682B1 KR 101519682 B1 KR101519682 B1 KR 101519682B1 KR 1020107005151 A KR1020107005151 A KR 1020107005151A KR 20107005151 A KR20107005151 A KR 20107005151A KR 101519682 B1 KR101519682 B1 KR 101519682B1
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alkyl
hydrogen
hydroxy
compound
formula
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KR20100053627A (ko
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마크 피. 웬트랜드
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렌슬러 폴리테크닉 인스티튜트
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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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Anesthesiology (AREA)
  • Pain & Pain Management (AREA)
  • Diabetes (AREA)
  • Hospice & Palliative Care (AREA)
  • Otolaryngology (AREA)
  • Pulmonology (AREA)
  • Dermatology (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)
KR1020107005151A 2007-08-09 2008-08-08 4급 오피오이드 카르복스아미드 Active KR101519682B1 (ko)

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
KR20100053627A KR20100053627A (ko) 2010-05-20
KR101519682B1 true KR101519682B1 (ko) 2015-05-19

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KR1020107005151A Active KR101519682B1 (ko) 2007-08-09 2008-08-08 4급 오피오이드 카르복스아미드

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

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CN101878214A (zh) * 2007-11-30 2010-11-03 普渡制药公司 苯并吗啡烷化合物
EP3170395A1 (en) * 2009-03-19 2017-05-24 Alkermes Pharma Ireland Limited Morphinan derivatives with high oral bioavailability
SI2506712T1 (sl) * 2009-12-04 2019-06-28 Alkermes Pharma Ireland Limited, Derivati morfinana za zdravljenje prevelikega odmerka mamil
WO2011119605A2 (en) * 2010-03-22 2011-09-29 Rensselaer Polytechnic Institute Carboxamide biosiosteres of opiates
WO2012005795A1 (en) * 2010-07-08 2012-01-12 Alkermes, Inc. Process for the synthesis of substituted morphinans
EP2407469A1 (en) * 2010-07-13 2012-01-18 Chemo Ibérica, S.A. Salt of sitagliptin
AU2011293502B2 (en) 2010-08-23 2015-03-19 Alkermes Pharma Ireland Limited Methods for treating antipsychotic-induced weight gain
WO2012112525A1 (en) * 2011-02-14 2012-08-23 Alkermes, Inc. PERIPHERIALLY ACTING μ OPIOID ANTAGONISTS
EP2789616A1 (en) * 2011-03-03 2014-10-15 Cadila Healthcare Limited A novel gentisate salt of a DPP-IV inhibitor
US9029543B2 (en) * 2011-04-05 2015-05-12 Alkermes, Inc. Process for the synthesis of quaternary amine compounds
PT2725908T (pt) * 2011-06-29 2017-08-31 Alkermes Inc Compostos opioides de ação periférica
US9096606B2 (en) 2011-12-08 2015-08-04 Purdue Pharma, L.P. Quarternized buprenorphine analogs
EP3153171B1 (en) 2011-12-15 2018-09-19 Alkermes Pharma Ireland Limited Samidorphan (alks 33) in combination with buprenorphine for the treatment of depressive disorders
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
EP3003311A2 (en) 2013-05-24 2016-04-13 Alkermes Pharma Ireland Limited Methods for treating depressive symptoms
CA2911231C (en) 2013-05-24 2021-12-07 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
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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Publication number Publication date
US8563572B2 (en) 2013-10-22
NO20100289L (no) 2010-03-02
MX2010001371A (es) 2010-03-10
EP2190819B1 (en) 2016-05-25
JP5581211B2 (ja) 2014-08-27
HK1141295A1 (zh) 2010-11-05
CA2694497A1 (en) 2009-02-19
EA020658B1 (ru) 2014-12-30
US20090197905A1 (en) 2009-08-06
CA2694497C (en) 2016-07-12
IL203459A (en) 2016-02-29
BRPI0815020A2 (pt) 2015-03-10
AU2008286979A1 (en) 2009-02-19
US20170095469A1 (en) 2017-04-06
WO2009023567A1 (en) 2009-02-19
US20120302594A1 (en) 2012-11-29
NO341089B1 (no) 2017-08-21
US20140107143A1 (en) 2014-04-17
CN101827819B (zh) 2013-06-12
CN101827819A (zh) 2010-09-08
ES2586245T3 (es) 2016-10-13
US8263807B2 (en) 2012-09-11
AU2008286979B2 (en) 2013-03-28
JP2010535814A (ja) 2010-11-25
EP2190819A1 (en) 2010-06-02
KR20100053627A (ko) 2010-05-20
EA201070237A1 (ru) 2010-10-29

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