CN100387600C - N-取代的氢吗啡酮及其用途 - Google Patents

N-取代的氢吗啡酮及其用途 Download PDF

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Publication number
CN100387600C
CN100387600C CNB038229587A CN03822958A CN100387600C CN 100387600 C CN100387600 C CN 100387600C CN B038229587 A CNB038229587 A CN B038229587A CN 03822958 A CN03822958 A CN 03822958A CN 100387600 C CN100387600 C CN 100387600C
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CN
China
Prior art keywords
pharmaceutically acceptable
acceptable salt
pain
compound
salt
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Expired - Fee Related
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CNB038229587A
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English (en)
Chinese (zh)
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CN1684967A (zh
Inventor
D·J·凯尔
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Euro Celtique SA
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Euro Celtique SA
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Publication of CN100387600C publication Critical patent/CN100387600C/zh
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    • 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
    • C07D489/04—Salts; Organic complexes
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CNB038229587A 2002-09-25 2003-09-24 N-取代的氢吗啡酮及其用途 Expired - Fee Related CN100387600C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US41325402P 2002-09-25 2002-09-25
US60/413,254 2002-09-25

Publications (2)

Publication Number Publication Date
CN1684967A CN1684967A (zh) 2005-10-19
CN100387600C true CN100387600C (zh) 2008-05-14

Family

ID=32043224

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB038229587A Expired - Fee Related CN100387600C (zh) 2002-09-25 2003-09-24 N-取代的氢吗啡酮及其用途

Country Status (18)

Country Link
US (1) US6825205B2 (enExample)
EP (2) EP1803724A1 (enExample)
JP (2) JP4806190B2 (enExample)
KR (1) KR20050074462A (enExample)
CN (1) CN100387600C (enExample)
AT (1) ATE360633T1 (enExample)
AU (1) AU2003272642B2 (enExample)
BR (1) BR0314488A (enExample)
CA (1) CA2500118C (enExample)
CY (1) CY1106697T1 (enExample)
DE (1) DE60313478T2 (enExample)
DK (1) DK1543010T3 (enExample)
ES (1) ES2286461T3 (enExample)
MX (1) MXPA05003104A (enExample)
NZ (1) NZ538726A (enExample)
PT (1) PT1543010E (enExample)
WO (1) WO2004029059A1 (enExample)
ZA (1) ZA200502174B (enExample)

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US20040202717A1 (en) 2003-04-08 2004-10-14 Mehta Atul M. Abuse-resistant oral dosage forms and method of use thereof
US20070185145A1 (en) * 2006-02-03 2007-08-09 Royds Robert B Pharmaceutical composition containing a central opioid agonist, a central opioid antagonist, and a peripheral opioid antagonist, and method for making the same
EP2099764B1 (en) 2006-09-20 2011-07-27 Mallinckrodt Inc. Preparation of substituted morphinan-6-ones and salts and intermediates thereof
US20080234306A1 (en) * 2006-11-22 2008-09-25 Progenics Pharmaceuticals, Inc. N-Oxides of 4,5-Epoxy-Morphinanium Analogs
JP2010510329A (ja) * 2006-11-22 2010-04-02 プロジェニックス ファーマスーティカルス インコーポレーテッド ７，８−飽和−４，５−エポキシ−モルフィナニウム類似体
JP5875748B2 (ja) * 2007-03-06 2016-03-02 マリンクロッド エルエルシー 第４級ｎ−アルキルモルフィナンアルカロイド塩の調製のための方法
US9040726B2 (en) 2007-03-06 2015-05-26 Mallinckrodt Llc Process for the preparation of quaternary N-alkyl morphinan alkaloid salts
WO2009023567A1 (en) * 2007-08-09 2009-02-19 Rensselaer Polytechnic Institute Quaternary opioid carboxamides
CA2702680A1 (en) * 2007-10-18 2009-04-23 Aiko Biotechnology Combination analgesic employing opioid and neutral antagonist
US8748448B2 (en) 2007-10-18 2014-06-10 Aiko Biotechnology Combination analgesic employing opioid agonist and neutral antagonist
WO2009070733A1 (en) * 2007-11-26 2009-06-04 Pharmacofore, Inc. Peripheral phenolic opioid antagonist
EP2896614B1 (en) 2008-05-27 2017-07-12 Mallinckrodt LLC Processes and compounds for the preparation of normorphinans
WO2010028004A2 (en) 2008-09-03 2010-03-11 Mallinckrodt Inc. Substituted berbines and processes for their synthesis
ME02367B (me) 2010-09-21 2016-06-20 Purdue Pharma Lp Analozi buprenorfina kao agonisti i/ili antagonisti opioidnog receptora
US10138207B2 (en) 2012-11-09 2018-11-27 Purdue Pharma, L.P. Benzomorphan analogs and the use thereof
EP2951160B1 (en) 2013-01-31 2019-04-24 Purdue Pharma LP Benzomorphan analogs and the use thereof
US8969358B2 (en) 2013-03-15 2015-03-03 Purdue Pharma L.P. Buprenorphine analogs
WO2015097547A1 (en) 2013-12-26 2015-07-02 Purdue Pharma L.P. 10-substituted morphinan hydantoins
EP3087057A4 (en) 2013-12-26 2017-06-28 Purdue Pharma LP Ring-contracted morphinans and the use thereof
EP3087078B1 (en) 2013-12-26 2019-05-15 Purdue Pharma LP 7-beta-alkyl analogs of orvinols
US9862726B2 (en) 2013-12-26 2018-01-09 Purdue Pharma L.P. Opioid receptor modulating oxabicyclo[2.2.2]octane morphinans
EP3086790A4 (en) 2013-12-27 2017-07-19 Purdue Pharma LP 6-substituted and 7-substituted morphinan analogs and the use thereof
CA2950567A1 (en) 2014-05-27 2015-12-03 Purdue Pharma L.P. Spirocyclic morphinans and use thereof
CA2951697A1 (en) 2014-06-13 2015-12-17 Purdue Pharma L.P. Azamophinan derivatives and use thereof
MA41125A (fr) 2014-12-05 2017-10-10 Purdue Pharma Lp Dérivés de 6.7-cyclomorphinane et leur utilisation
US10745402B2 (en) 2017-01-02 2020-08-18 Purdue Pharma L.P. Morphinan derivatives and use thereof
CN117567477B (zh) * 2023-11-15 2026-05-26 宜昌人福药业有限责任公司 一种氢吗啡酮和二氢吗啡类药物低分子聚乙二醇化物及其制备方法和应用

Citations (2)

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US4176186A (en) * 1978-07-28 1979-11-27 Boehringer Ingelheim Gmbh Quaternary derivatives of noroxymorphone which relieve intestinal immobility
EP0306575A1 (en) * 1987-09-10 1989-03-15 The University Of Chicago Quaternary derivatives of noroxymorphone which relieve nausea and emesis

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US3536809A (en) 1969-02-17 1970-10-27 Alza Corp Medication method
US3598123A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
US4008719A (en) 1976-02-02 1977-02-22 Alza Corporation Osmotic system having laminar arrangement for programming delivery of active agent
IE58110B1 (en) 1984-10-30 1993-07-14 Elan Corp Plc Controlled release powder and process for its preparation
US5073543A (en) 1988-07-21 1991-12-17 G. D. Searle & Co. Controlled release formulations of trophic factors in ganglioside-lipsome vehicle
IT1229203B (it) 1989-03-22 1991-07-25 Bioresearch Spa Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative.
US5120548A (en) 1989-11-07 1992-06-09 Merck & Co., Inc. Swelling modulated polymeric drug delivery device
US5733566A (en) 1990-05-15 1998-03-31 Alkermes Controlled Therapeutics Inc. Ii Controlled release of antiparasitic agents in animals
US5698155A (en) 1991-05-31 1997-12-16 Gs Technologies, Inc. Method for the manufacture of pharmaceutical cellulose capsules
US5580578A (en) 1992-01-27 1996-12-03 Euro-Celtique, S.A. Controlled release formulations coated with aqueous dispersions of acrylic polymers
US5968551A (en) 1991-12-24 1999-10-19 Purdue Pharma L.P. Orally administrable opioid formulations having extended duration of effect
US5591767A (en) 1993-01-25 1997-01-07 Pharmetrix Corporation Liquid reservoir transdermal patch for the administration of ketorolac
IT1270594B (it) 1994-07-07 1997-05-07 Recordati Chem Pharm Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida
CN1535687A (zh) * 1996-11-25 2004-10-13 ������������ʽ���� 止痒药物
WO2001014382A1 (en) * 1999-08-23 2001-03-01 Toray Industries, Inc. Analgesics containing as the active ingredient quaternary ammonium salt derivatives of morphinan

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
US4176186A (en) * 1978-07-28 1979-11-27 Boehringer Ingelheim Gmbh Quaternary derivatives of noroxymorphone which relieve intestinal immobility
EP0306575A1 (en) * 1987-09-10 1989-03-15 The University Of Chicago Quaternary derivatives of noroxymorphone which relieve nausea and emesis

Non-Patent Citations (2)

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Addition of organomagnesium halides to pseudocodeinetypes.Ⅱ.preparation of nuclear alkylated mophine derivatives. Lyndon Small.Journal of the american chemical society,Vol.58 . 1938 *

Also Published As

Publication number Publication date
EP1543010A1 (en) 2005-06-22
WO2004029059A1 (en) 2004-04-08
PT1543010E (pt) 2007-07-26
DK1543010T3 (da) 2007-09-17
JP2006503850A (ja) 2006-02-02
JP4806190B2 (ja) 2011-11-02
DE60313478D1 (de) 2007-06-06
JP2011042681A (ja) 2011-03-03
CY1106697T1 (el) 2012-05-23
BR0314488A (pt) 2005-08-02
CA2500118C (en) 2011-04-12
CA2500118A1 (en) 2004-04-08
HK1080456A1 (en) 2006-04-28
US20040067973A1 (en) 2004-04-08
KR20050074462A (ko) 2005-07-18
EP1543010B1 (en) 2007-04-25
NZ538726A (en) 2006-11-30
EP1803724A1 (en) 2007-07-04
US6825205B2 (en) 2004-11-30
DE60313478T2 (de) 2008-01-03
CN1684967A (zh) 2005-10-19
MXPA05003104A (es) 2005-05-27
ATE360633T1 (de) 2007-05-15
ZA200502174B (en) 2006-05-31
ES2286461T3 (es) 2007-12-01
AU2003272642B2 (en) 2009-07-09
AU2003272642A1 (en) 2004-04-19

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Granted publication date: 20080514

Termination date: 20110924