CN101678120A - 前药及其制备和使用方法 - Google Patents

前药及其制备和使用方法 Download PDF

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Publication number
CN101678120A
CN101678120A CN200780050871A CN200780050871A CN101678120A CN 101678120 A CN101678120 A CN 101678120A CN 200780050871 A CN200780050871 A CN 200780050871A CN 200780050871 A CN200780050871 A CN 200780050871A CN 101678120 A CN101678120 A CN 101678120A
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CN
China
Prior art keywords
compound
hydrogen
prodrug
prodrug moiety
methyl
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Pending
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CN200780050871A
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English (en)
Chinese (zh)
Inventor
N·穆罕默德
K·R·布雷
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NeurogesX Inc
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NeurogesX Inc
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Publication of CN101678120A publication Critical patent/CN101678120A/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:
    • C07D489/09—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: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems
    • C07D489/10—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: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14
    • C07D489/12—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: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/548—Phosphates or phosphonates, e.g. bone-seeking
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
    • C07D211/28—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms to which a second hetero atom is attached
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D225/00—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom
    • C07D225/04—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D225/06—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with one six-membered ring

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Psychology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
CN200780050871A 2006-12-05 2007-12-05 前药及其制备和使用方法 Pending CN101678120A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US87351906P 2006-12-05 2006-12-05
US60/873,519 2006-12-05
PCT/US2007/024984 WO2008070149A2 (en) 2006-12-05 2007-12-05 Prodrugs and methods of making and using the same

Publications (1)

Publication Number Publication Date
CN101678120A true CN101678120A (zh) 2010-03-24

Family

ID=39361296

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200780050871A Pending CN101678120A (zh) 2006-12-05 2007-12-05 前药及其制备和使用方法

Country Status (12)

Country Link
US (1) US20080318905A1 (enExample)
EP (1) EP2121029A2 (enExample)
JP (1) JP2010511717A (enExample)
KR (1) KR20090086627A (enExample)
CN (1) CN101678120A (enExample)
AU (1) AU2007328007A1 (enExample)
BR (1) BRPI0719937A2 (enExample)
CA (1) CA2671737A1 (enExample)
MX (1) MX2009006007A (enExample)
NO (1) NO20092527L (enExample)
RU (1) RU2009125597A (enExample)
WO (1) WO2008070149A2 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019086017A1 (en) * 2017-11-03 2019-05-09 Nirsum Laboratories, Inc. Opioid receptor antagonist prodrugs
CN114380859A (zh) * 2020-10-22 2022-04-22 威智医药有限公司 磷酸二苄酯及焦磷酸四苄酯的制备方法
WO2024061250A1 (zh) * 2022-09-23 2024-03-28 合肥瀚微生物科技有限公司 一种抑郁症诊断的生物标记物及其应用

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TWI385169B (zh) 2005-10-31 2013-02-11 Eisai R&D Man Co Ltd 經雜環取代之吡啶衍生物及含有彼之抗真菌劑
JP5221514B2 (ja) * 2007-03-06 2013-06-26 エーザイ・アール・アンド・ディー・マネジメント株式会社 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物及びその製造方法
TW200841879A (en) 2007-04-27 2008-11-01 Eisai R&D Man Co Ltd Pyridine derivatives substituted by heterocyclic ring and phosphonoamino group, and anti-fungal agent containing same
US8513287B2 (en) 2007-12-27 2013-08-20 Eisai R&D Management Co., Ltd. Heterocyclic ring and phosphonoxymethyl group substituted pyridine derivatives and antifungal agent containing same
BRPI0912326A2 (pt) 2008-05-20 2015-10-06 Neurogesx Inc análogos de acetaminofeno hidrossolúveis
EP2285419A4 (en) 2008-05-20 2012-05-02 Neurogesx Inc LUBRICANT MUTUAL PARACETAMOL PRODRUGS
CA2724881C (en) 2008-05-20 2016-09-27 Neurogesx, Inc. Carbonate prodrugs and methods of using the same
MX2011001053A (es) 2008-07-28 2011-04-21 Pfizer Compuestos de fenantrenona, composiciones y metodos.
US20100076198A1 (en) * 2008-09-19 2010-03-25 Mallinckrodt Inc. Crystalline forms of Fentanyl Alkaloid
HUE033442T2 (en) 2009-06-25 2017-11-28 Alkermes Pharma Ireland Ltd Heterocyclic compounds for the treatment of neurological and psychological disorders
EP2445343B1 (en) 2009-06-25 2021-08-04 Alkermes Pharma Ireland Limited Prodrugs of nh-acidic compounds
JP5848761B2 (ja) 2010-06-24 2016-01-27 アルカーメス ファーマ アイルランド リミテッド Ｎｈ酸性化合物のプロドラッグ：エステル、カルボネート、カルバメートおよびホスホネートの誘導体
EP3156056B1 (en) 2011-03-18 2023-12-06 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising sorbitan esters
PH12014500049A1 (en) * 2011-07-28 2016-07-29 Kempharm Inc Methylphenidate-prodrugs, processes of making and using the same
CA2849731C (en) 2011-09-22 2020-01-14 Acorda Therapeutics, Inc. Acetaminophen conjugates, compositions and methods of use thereof
JP5952912B2 (ja) 2011-12-15 2016-07-13 アルカーメス ファーマ アイルランド リミテッド 二級アミン化合物のプロドラッグ
CA2867121C (en) 2012-03-19 2021-05-25 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising fatty acid esters
AU2013235523B9 (en) 2012-03-19 2018-01-04 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising glycerol esters
AU2013235526B2 (en) 2012-03-19 2017-11-30 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising benzyl alcohol
ES2792149T3 (es) 2012-09-19 2020-11-10 Alkermes Pharma Ireland Ltd Composiciones farmacéuticas que tienen estabilidad de almacenamiento mejorada
EP2986295A4 (en) 2013-04-17 2016-11-09 Biopharma Works PROCESS FOR PAIN TREATMENT
EP2986294A4 (en) 2013-04-17 2016-11-16 Biopharma Works PROCESS FOR PAIN TREATMENT
ES2718211T3 (es) 2013-05-24 2019-06-28 Rhodes Tech Compuestos cetales opioides y usos de los mismos
US9969746B2 (en) 2013-12-05 2018-05-15 The University Of Bath Opioid compounds and their uses
AU2015231278B2 (en) 2014-03-20 2020-01-23 Alkermes Pharma Ireland Limited Aripiprazole formulations having increased injection speeds
ES2922976T3 (es) * 2015-05-13 2022-09-22 4P Pharma Apomorfina para el tratamiento de la hiperactividad inducida por metilfenidato
US20170273974A1 (en) * 2016-03-24 2017-09-28 Medrx Co., Ltd Patch preparations with misuse prevention features
AU2019224127B2 (en) 2018-02-23 2021-12-09 Rhodes Technologies Novel opioid compounds and uses thereof
CA3092335A1 (en) 2018-03-05 2019-09-12 Alkermes Pharma Ireland Limited Aripiprazole dosing strategy
WO2020012248A1 (en) 2018-07-13 2020-01-16 Alkermes Pharma Ireland Limited Novel naphthylenyl compounds for long-acting injectable compositions and related methods
US10807995B2 (en) 2018-07-13 2020-10-20 Alkermes Pharma Ireland Limited Thienothiophene compounds for long-acting injectable compositions and related methods
EP3863629A4 (en) * 2018-10-13 2022-06-22 Biohaven Pharmaceutical Holding Company Ltd. Prodrugs of cgrp antagonists
WO2020094634A1 (en) 2018-11-05 2020-05-14 Alkermes Pharma Ireland Limited Thiophene prodrugs of naltroxene for long-acting injectable compositions and related methods
KR20220005554A (ko) * 2019-05-07 2022-01-13 브리스톨-마이어스 스큅 컴퍼니 전구약물 화합물
FI130262B (en) * 2019-08-30 2023-05-17 Medicortex Finland Oy Formulations and compositions for use in the prevention or treatment of brain injury and neurodegenerative diseases
CN114761082A (zh) * 2019-09-30 2022-07-15 日本化学药品株式会社 氮杂环庚烷衍生物

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US6225321B1 (en) * 1997-06-05 2001-05-01 Oliver Yoa-Pu Hu Long analgesic acting nalbuphine polyester derivative and method of use
AU773642C (en) * 1997-12-22 2006-04-06 Mundipharma Pty Limited Opioid agonist/antagonist combinations
DE69822514T2 (de) * 1997-12-31 2005-03-24 The University Of Kansas, Lawrence Wasserlösliche pro-pharmaka von arzneistoffen, die ein tertiäres amin enthalten, und verfahren zu ihrer herstellung
US6703398B2 (en) * 2001-11-26 2004-03-09 Oliver Yoa-Pu Hu Orally administered analgesic compositions containing nalbuphine
EP1603597B1 (en) * 2003-03-13 2010-01-06 Controlled Chemicals, Inc. Oxycodone conjugates with lower abuse potential and extended duration of action
HUE037643T2 (hu) * 2004-06-12 2018-09-28 Collegium Pharmaceutical Inc Visszaélésre nem alkalmas gyógyszerkészítmények

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019086017A1 (en) * 2017-11-03 2019-05-09 Nirsum Laboratories, Inc. Opioid receptor antagonist prodrugs
CN114380859A (zh) * 2020-10-22 2022-04-22 威智医药有限公司 磷酸二苄酯及焦磷酸四苄酯的制备方法
CN114380859B (zh) * 2020-10-22 2024-11-01 威智医药股份有限公司 磷酸二苄酯及焦磷酸四苄酯的制备方法
WO2024061250A1 (zh) * 2022-09-23 2024-03-28 合肥瀚微生物科技有限公司 一种抑郁症诊断的生物标记物及其应用

Also Published As

Publication number Publication date
AU2007328007A1 (en) 2008-06-12
WO2008070149A3 (en) 2009-12-10
WO2008070149A2 (en) 2008-06-12
US20080318905A1 (en) 2008-12-25
MX2009006007A (es) 2009-07-17
BRPI0719937A2 (pt) 2014-03-11
RU2009125597A (ru) 2011-01-20
JP2010511717A (ja) 2010-04-15
KR20090086627A (ko) 2009-08-13
EP2121029A2 (en) 2009-11-25
CA2671737A1 (en) 2008-06-12
NO20092527L (no) 2009-09-04

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