WO1997021416A3 - Glicoconjugados de substancias opiaceas - Google Patents

Glicoconjugados de substancias opiaceas Download PDF

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Publication number
WO1997021416A3
WO1997021416A3 PCT/ES1996/000214 ES9600214W WO9721416A3 WO 1997021416 A3 WO1997021416 A3 WO 1997021416A3 ES 9600214 W ES9600214 W ES 9600214W WO 9721416 A3 WO9721416 A3 WO 9721416A3
Authority
WO
WIPO (PCT)
Prior art keywords
opiated
opiate
glycoconjugates
residue
molecule
Prior art date
Application number
PCT/ES1996/000214
Other languages
English (en)
French (fr)
Other versions
WO1997021416A2 (es
Inventor
Diana Cowie
Parera Gregori Valencia
Original Assignee
Farmhispania
Diana Cowie
Parera Gregori Valencia
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Farmhispania, Diana Cowie, Parera Gregori Valencia filed Critical Farmhispania
Priority to JP9521758A priority Critical patent/JPH10513485A/ja
Priority to EP96938222A priority patent/EP0816375A1/en
Publication of WO1997021416A2 publication Critical patent/WO1997021416A2/es
Publication of WO1997021416A3 publication Critical patent/WO1997021416A3/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00—Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/06—Heterocyclic radicals

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

Están constituidos por una serie de derivados de carbohidratos de una familia de agentes opiáceos biológicamente activos, que presentan en su estructura por lo menos un residuo de carbohidrato por molécula de opiáceo, unido directamente a un grupo hidroxilo del opiáceo o a través de un enlace C-glicosídico formado entre dos funciones situadas en cada una de las dos partes constituyentes del glicoconjugado. Dichos derivados contienen más de un residuo de carbohidrato y/o más de una molécula opiácea por residuo de carbohidrato. Las sales de ácido y los compuestos de estos glicoconjugados opiáceos están también incluidos entre los compuestos de esta invención.
PCT/ES1996/000214 1995-11-29 1996-11-15 Glicoconjugados de substancias opiaceas WO1997021416A2 (es)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP9521758A JPH10513485A (ja) 1995-11-29 1996-11-15 オピエート性物質の糖結合体
EP96938222A EP0816375A1 (en) 1995-11-29 1996-11-15 Glycoconjugates of opiated substances

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ES9502346 1995-11-29
ESP9502346 1995-11-29

Publications (2)

Publication Number Publication Date
WO1997021416A2 WO1997021416A2 (es) 1997-06-19
WO1997021416A3 true WO1997021416A3 (es) 1997-09-12

Family

ID=8292324

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/ES1996/000214 WO1997021416A2 (es) 1995-11-29 1996-11-15 Glicoconjugados de substancias opiaceas

Country Status (4)

Country Link
EP (1) EP0816375A1 (es)
JP (1) JPH10513485A (es)
CA (1) CA2211596A1 (es)
WO (1) WO1997021416A2 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU723859B2 (en) * 1997-04-14 2000-09-07 Ufc Limited Morphine derivatives
GB9711118D0 (en) * 1997-05-29 1997-07-23 Rolabo Sl Compound
US6740641B2 (en) * 2001-07-27 2004-05-25 Euro-Celtique, S.A. Sugar derivatives of hydromorphone, dihydromorphine and dihydromorphine, compositions thereof and uses for treating or preventing pain
GB0218811D0 (en) * 2002-08-14 2002-09-18 Cenes Ltd Salts of morphine-6-glucuronide
FR2864082B1 (fr) 2003-12-22 2006-03-10 Synt Em Nouveau derive de la morphine-6-glucuronide, composition pharmaceutique le contenant et son utilisation pour le traitement de la douleur
FR2907121B1 (fr) * 2006-10-12 2012-05-04 Neorphys Nouveaux derives morphiniques
US10512644B2 (en) 2007-03-12 2019-12-24 Inheris Pharmaceuticals, Inc. Oligomer-opioid agonist conjugates
US8173666B2 (en) 2007-03-12 2012-05-08 Nektar Therapeutics Oligomer-opioid agonist conjugates
CN103360271B (zh) * 2013-06-19 2015-09-16 广州万孚生物技术股份有限公司 美沙酮半抗原及其制备方法、美沙酮抗原和美沙酮单克隆抗体及其应用
CN106008621B (zh) * 2014-03-26 2019-02-19 宜昌人福药业有限责任公司 一种吗啡-6-β-D-葡萄糖醛酸苷的合成方法及其中间体化合物

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE839799C (de) * 1952-04-17 Muri Bern Dr. Paul Casparis (Schweiz) Verfahren zur Herstellung von Morphin-6-glycosiden
US3647806A (en) * 1966-04-18 1972-03-07 Syntex Corp Tetrahydropyranyl and tetrahydro-furanyl benzomorphan ethers
US4012525A (en) * 1975-10-10 1977-03-15 Eli Lilly And Company Novel propoxyphene dosage regimen
US4159333A (en) * 1970-06-11 1979-06-26 United States Of America N-Methyl levo benzomorphan analgesics having non-addictive and morphine antagonistic properties
JPS54105237A (en) * 1978-02-02 1979-08-18 Sankyo Co Ltd Analgesic agent containing nalorphine-6-glucuronide
JPS59152328A (ja) * 1983-02-18 1984-08-31 Eisai Co Ltd サリチル酸誘導体含有鎮痛剤
US4973596A (en) * 1988-05-20 1990-11-27 Barr Laboratories, Inc. Method of administering a narcotic analgesic and dosage forms therefor
WO1993003051A1 (en) * 1991-08-06 1993-02-18 Salford Ultrafine Chemicals And Research Limited A process for making morphine-6-glucuronide or substituted morphine-6-glucuronide
WO1993005057A1 (fr) * 1991-09-04 1993-03-18 Irepa (Institut Regional De Promotion De La Recherche Appliquee) Procede de synthese de glucuronides d'epoxy-4,5 morphinanes
WO1995005831A1 (en) * 1993-08-23 1995-03-02 Euro-Celtique S.A. Pharmaceutical compositions containing morphine-6-glucuronide for the treatment of pain

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE839799C (de) * 1952-04-17 Muri Bern Dr. Paul Casparis (Schweiz) Verfahren zur Herstellung von Morphin-6-glycosiden
US3647806A (en) * 1966-04-18 1972-03-07 Syntex Corp Tetrahydropyranyl and tetrahydro-furanyl benzomorphan ethers
US4159333A (en) * 1970-06-11 1979-06-26 United States Of America N-Methyl levo benzomorphan analgesics having non-addictive and morphine antagonistic properties
US4012525A (en) * 1975-10-10 1977-03-15 Eli Lilly And Company Novel propoxyphene dosage regimen
JPS54105237A (en) * 1978-02-02 1979-08-18 Sankyo Co Ltd Analgesic agent containing nalorphine-6-glucuronide
JPS59152328A (ja) * 1983-02-18 1984-08-31 Eisai Co Ltd サリチル酸誘導体含有鎮痛剤
US4973596A (en) * 1988-05-20 1990-11-27 Barr Laboratories, Inc. Method of administering a narcotic analgesic and dosage forms therefor
WO1993003051A1 (en) * 1991-08-06 1993-02-18 Salford Ultrafine Chemicals And Research Limited A process for making morphine-6-glucuronide or substituted morphine-6-glucuronide
WO1993005057A1 (fr) * 1991-09-04 1993-03-18 Irepa (Institut Regional De Promotion De La Recherche Appliquee) Procede de synthese de glucuronides d'epoxy-4,5 morphinanes
WO1995005831A1 (en) * 1993-08-23 1995-03-02 Euro-Celtique S.A. Pharmaceutical compositions containing morphine-6-glucuronide for the treatment of pain

Non-Patent Citations (12)

* Cited by examiner, † Cited by third party
Title
"PHARMACOLOGICAL EFFECTS OF DRUG CONJUGATES: IS MORPHINE 6-GLUCURONIDE AN EXCEPTION?", TRENDS IN PHARMACOLOGICAL SCIENCES, vol. 13, August 1992 (1992-08-01), pages 302 - 304, XP002025771 *
H. BRZEZINKA ET AL: "Hochdruckflüssigkeits-chromatographische trennung von glucuroniden und deren massenspektrometrische identifizierung", FRESENIUS' Z. ANAL. CHEM., vol. 323, no. 3, 1986, pages 220 - 224, XP000675080 *
H. MIYAZAKI ET AL: "Disposition and metabolism of [14C]loperamide in rats.", EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS, vol. 4, no. 1-2, 1979, pages 199 - 206, XP000675089 *
J. CALDWELL ET AL: "Non-human primate species as metabolic models for the human situation: comparative studies on meperidine metabolism", TOXICOLOGY AND APPLIED PHARMACOLOGY, vol. 48, no. 2, 1979, pages 273 - 278, XP000675098 *
KOVAC P ET AL: "SYNTHESIS AND CHARACTERIZATION OF 6-0-ALPHA- AND 6-0-BETA-D-GLUCOPYRANOSYLMORPHINE AND 6-0-BETA-D-GLUCOPYRANOSYL-CODEINE", HETEROCYCLES, vol. 41, no. 4, 1 April 1995 (1995-04-01), pages 697 - 707, XP000645042 *
N. D. EDDINGTON & D. YOUNG: "Biliary excretion of reduced haloperidol glucuronide", PSYCHOPHARMACOLOGY, vol. 100, no. 1, 1990, pages 46 - 48, XP000675101 *
OSBORNE R: "ANALGESIC ACTIVITY OF MORPHINE-6-FLUCURONIDE", LANCET THE, vol. 9, 9 April 1988 (1988-04-09), pages 828/829, XP002025770 *
PATENT ABSTRACTS OF JAPAN vol. 003, no. 123 (C - 061) 16 October 1979 (1979-10-16) *
PATENT ABSTRACTS OF JAPAN vol. 008, no. 283 (C - 258) 25 December 1984 (1984-12-25) *
R. K. LYNN ET AL: "Identification of glucoronide metabolites of benzomorphan narcotic analgesic drugs in bile from the isolated perfused rat liver by gas chromatography and mass spectrometry.", DRUG METABOLISM AND DISPOSITION, vol. 5, no. 1, 1977, pages 47 - 55, XP000675095 *
SILEK ET AL: "Synthesis of piperidine derivatives as potential analgesic agents", COLLECT. CZECH. CHEM. COMMUN., vol. 55, 1990, pages 1828 - 1853, XP002032852 *
YOSHIMURA H ET AL: "METABOLISM OF DRUGS. LX. THE SYNTHESIS OF CODEINE AND MORPHINE GLUCURONIDES", CHEMICAL AND PHARMACEUTICAL BULLETIN, vol. 16, no. 11, 1968, pages 2114 - 2119, XP002025772 *

Also Published As

Publication number Publication date
JPH10513485A (ja) 1998-12-22
WO1997021416A2 (es) 1997-06-19
CA2211596A1 (en) 1997-06-19
EP0816375A1 (en) 1998-01-07

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