AU2005304950B2 - 4-Hydroxybenzomorphans - Google Patents

4-Hydroxybenzomorphans Download PDF

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Publication number
AU2005304950B2
AU2005304950B2 AU2005304950A AU2005304950A AU2005304950B2 AU 2005304950 B2 AU2005304950 B2 AU 2005304950B2 AU 2005304950 A AU2005304950 A AU 2005304950A AU 2005304950 A AU2005304950 A AU 2005304950A AU 2005304950 B2 AU2005304950 B2 AU 2005304950B2
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AU
Australia
Prior art keywords
hydrogen
chosen
hydroxy
carbonyl
mmol
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Expired
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AU2005304950A
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AU2005304950A1 (en
Inventor
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
    • C07D221/26—Benzomorphans
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P1/12—Antidiarrhoeals
    • 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D215/12—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D215/14—Radicals substituted by oxygen atoms
    • 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
    • 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:
    • 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)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
AU2005304950A 2004-11-05 2005-11-03 4-Hydroxybenzomorphans Expired AU2005304950B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US62534804P 2004-11-05 2004-11-05
US60/625,348 2004-11-05
PCT/US2005/039911 WO2006052710A1 (en) 2004-11-05 2005-11-03 4-hydroxybenzomorphans

Publications (2)

Publication Number Publication Date
AU2005304950A1 AU2005304950A1 (en) 2006-05-18
AU2005304950B2 true AU2005304950B2 (en) 2010-12-09

Family

ID=36128632

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2005304950A Expired AU2005304950B2 (en) 2004-11-05 2005-11-03 4-Hydroxybenzomorphans

Country Status (20)

Country Link
US (7) US7262298B2 (OSRAM)
EP (2) EP2251330B1 (OSRAM)
JP (3) JP5198067B2 (OSRAM)
KR (1) KR101115841B1 (OSRAM)
CN (1) CN101090891B (OSRAM)
AT (1) ATE557006T1 (OSRAM)
AU (1) AU2005304950B2 (OSRAM)
BR (1) BRPI0517091B8 (OSRAM)
CA (1) CA2587074C (OSRAM)
CY (1) CY1112946T1 (OSRAM)
DK (1) DK2251330T3 (OSRAM)
ES (1) ES2387737T3 (OSRAM)
IL (1) IL182983A (OSRAM)
MX (1) MX2007005389A (OSRAM)
NO (1) NO340204B1 (OSRAM)
PL (1) PL2251330T3 (OSRAM)
PT (1) PT2251330E (OSRAM)
RU (2) RU2415131C2 (OSRAM)
SI (1) SI2251330T1 (OSRAM)
WO (1) WO2006052710A1 (OSRAM)

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WO2006052710A1 (en) * 2004-11-05 2006-05-18 Rensselaer Polytechnic Institute 4-hydroxybenzomorphans
EP1924559B1 (en) 2005-07-21 2014-04-16 Rensselaer Polytechnic Institute 8-carboxamido-substituted-2 , 6-methano-3-benzazocines and 3 - carboxamido- substituted morphanes as opioid receptor binding agents
US7985858B2 (en) 2007-05-04 2011-07-26 Mallinckrodt Inc. Process for the preparation of 6-alpha-hydroxy-N-alkylated opiates
NZ582668A (en) 2007-07-17 2012-02-24 Mallinckrodt Llc Preparation of n-alkylated opiates by reductive amination
MX2010001371A (es) 2007-08-09 2010-03-10 Rensselaer Polytech Inst Carboxamidas opioides cuaternarias.
PL2340253T3 (pl) 2008-09-30 2014-04-30 SpecGx LLC Sposoby selektywnego aminowania ketomorfinanów
US8946419B2 (en) 2009-02-23 2015-02-03 Mallinckrodt Llc (+)-6-hydroxy-morphinan or (+)-6-amino-morphinan derivatives
WO2010107457A1 (en) * 2009-03-19 2010-09-23 Alkermes, Inc. Morphinan derivatives with high oral bioavailability
US20100261906A1 (en) * 2009-04-09 2010-10-14 Mallinckrodt Inc. Preparation of 6-Keto, 3-Alkoxy Morphinans
PL2440561T3 (pl) 2009-06-11 2014-09-30 SpecGx LLC Redukcyjne aminowanie 6-keto-normorfinanow przez katalityczne przeniesienie wodoru
EP2440562B1 (en) 2009-06-11 2016-08-10 Mallinckrodt LLC Preparation of 6-alpha-amino n-substituted morphinans by catalytic hydrogen transfer
CA2782529C (en) * 2009-12-04 2015-05-26 Alkermes, Inc. Morphinan derivatives for the treatment of drug overdose
ES2582306T3 (es) 2010-03-22 2016-09-12 Rensselaer Polytechnic Institute Derivados de morfinano que contienen un grupo carboxamida como ligandos de receptores opioides
EP2563793B1 (en) * 2010-04-29 2014-10-22 Mallinckrodt LLC Preparation of saturated ketone morphinan compounds having low metal content
NZ605234A (en) 2010-07-08 2015-02-27 Alkermes Pharma Ireland Ltd Process for the synthesis of substituted morphinans
HUE041981T2 (hu) 2010-08-23 2019-06-28 Alkermes Pharma Ireland Ltd Eljárások antipszichotikum által kiváltott súlygyarapodás kezelésére
US9029543B2 (en) 2011-04-05 2015-05-12 Alkermes, Inc. Process for the synthesis of quaternary amine compounds
EP2718294B1 (en) 2011-06-09 2018-09-05 SpecGx LLC Reductive amination of 6-keto morphinans by catalytic hydrogen transfer
PL2725908T3 (pl) 2011-06-29 2017-10-31 Alkermes Inc Działające obwodowo związki opioidowe
PL2753622T3 (pl) 2011-09-08 2016-07-29 SpecGx LLC Wytwarzanie alkaloidów bez oddzielania związków pośrednich
US9211293B2 (en) 2011-12-15 2015-12-15 Alkermes Pharma Ireland Limited Opioid agonist antagonist combinations
CA2858812C (en) 2011-12-15 2019-02-26 Alkermes Pharma Ireland Limited Compositions of buprenorphine and mu-opioid receptor antagonists
US9656961B2 (en) 2013-05-24 2017-05-23 Alkermes Pharma Ireland Limited Methods for treating depressive symptoms
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
AU2018229062A1 (en) * 2017-03-02 2019-09-26 Ube Industries, Ltd. Therapeutic agent for alcohol use disorders
CN107089948B (zh) * 2017-04-28 2020-07-17 云南大学 吗吩衍生物及其制备方法和应用
CN111978252A (zh) * 2019-05-21 2020-11-24 复旦大学 手性苯并吗吩烷类衍生物及其制备方法和在药学上的应用
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
CN111205151B (zh) * 2020-02-29 2021-03-05 深圳市祥根生物科技有限公司 一种布洛芬杂质i的环保制备方法
EP4243768A1 (en) 2020-11-12 2023-09-20 Alkermes Pharma Ireland Limited Immediate release multilayer tablet
CN114621238A (zh) * 2020-12-10 2022-06-14 鲁南制药集团股份有限公司 一种制备纳呋拉啡的方法
KR102663533B1 (ko) * 2021-11-09 2024-05-08 백미선 레이저 치료기기용 온냉각장치

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BRPI0517091B1 (pt) 2019-10-08
EP2251330B1 (en) 2012-05-09
US20160075658A1 (en) 2016-03-17
CA2587074A1 (en) 2006-05-18
JP2013067636A (ja) 2013-04-18
RU2007120759A (ru) 2008-12-10
US20070238748A1 (en) 2007-10-11
IL182983A (en) 2012-06-28
EP2251330A1 (en) 2010-11-17
CN101090891A (zh) 2007-12-19
CY1112946T1 (el) 2016-04-13
RU2415131C2 (ru) 2011-03-27
CA2587074C (en) 2012-09-04
US7262298B2 (en) 2007-08-28
US20240092740A1 (en) 2024-03-21
RU2010147915A (ru) 2012-05-27
KR20070085723A (ko) 2007-08-27
AU2005304950A1 (en) 2006-05-18
ES2387737T3 (es) 2012-10-01
US20130231361A1 (en) 2013-09-05
PT2251330E (pt) 2012-07-20
CN101090891B (zh) 2012-08-01
US8680112B2 (en) 2014-03-25
DK2251330T3 (da) 2012-08-06
US20060111384A1 (en) 2006-05-25
PL2251330T3 (pl) 2012-12-31
EP1817291A1 (en) 2007-08-15
US8802655B2 (en) 2014-08-12
SI2251330T1 (sl) 2012-09-28
BRPI0517091A (pt) 2008-09-30
US20150011768A1 (en) 2015-01-08
JP6058981B2 (ja) 2017-01-11
JP2008519035A (ja) 2008-06-05
IL182983A0 (en) 2007-08-19
JP2016020364A (ja) 2016-02-04
JP5198067B2 (ja) 2013-05-15
ATE557006T1 (de) 2012-05-15
WO2006052710A1 (en) 2006-05-18
RU2480455C2 (ru) 2013-04-27
BRPI0517091B8 (pt) 2021-05-25
US20140148475A1 (en) 2014-05-29
KR101115841B1 (ko) 2012-03-09
NO20072839L (no) 2007-08-03
MX2007005389A (es) 2007-12-07
NO340204B1 (no) 2017-03-20

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