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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Psychology (AREA)
  • Anesthesiology (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (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 (https=)
EP (1) EP2121029A2 (https=)
JP (1) JP2010511717A (https=)
KR (1) KR20090086627A (https=)
CN (1) CN101678120A (https=)
AU (1) AU2007328007A1 (https=)
BR (1) BRPI0719937A2 (https=)
CA (1) CA2671737A1 (https=)
MX (1) MX2009006007A (https=)
NO (1) NO20092527L (https=)
RU (1) RU2009125597A (https=)
WO (1) WO2008070149A2 (https=)

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
WO2009143299A1 (en) 2008-05-20 2009-11-26 Neurogesx, Inc. Hepatoprotectant acetaminophen mutual prodrugs
EP2291084A4 (en) 2008-05-20 2012-04-25 Neurogesx Inc CARBONATE PRODRUGS AND METHOD FOR THEIR USE
JP5757864B2 (ja) 2008-05-20 2015-08-05 ニューロジェシックス， インコーポレイテッド 水溶性アセトアミノフェン類似体
ES2527137T3 (es) 2008-07-28 2015-01-21 Pfizer Inc. Compuestos de fenantrenona, composiciones y procedimientos
WO2010033540A1 (en) * 2008-09-19 2010-03-25 Mallinckrodt Inc. Crystalline forms of fentanyl alkaloid
CA2937222C (en) * 2009-06-25 2019-06-04 Alkermes Pharma Ireland Limited Prodrugs of nh-acidic compounds
US8431576B2 (en) 2009-06-25 2013-04-30 Alkermes Pharma Ireland Limited Heterocyclic compounds for the treatment of neurological and psychological disorders
ES2691671T3 (es) 2010-06-24 2018-11-28 Alkermes Pharma Ireland Limited Profármacos de compuestos NH-acídicos: derivados de éster, carbonato, carbamato y fosfonato
HUE065359T2 (hu) 2011-03-18 2024-05-28 Alkermes Pharma Ireland Ltd Szorbitán-észtereket tartalmazó gyógyászati készítmények
CA3123900A1 (en) * 2011-07-28 2013-01-31 Kempharm Inc. Methylphenidate-prodrugs, processes of making and using the same
US9024055B2 (en) 2011-09-22 2015-05-05 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
ES2765036T3 (es) 2012-03-19 2020-06-05 Alkermes Pharma Ireland Ltd Composiciones farmacéuticas que comprenden esteres de ácidos grasos
ES2950418T3 (es) 2012-03-19 2023-10-09 Alkermes Pharma Ireland Ltd Composiciones farmacéuticas que comprenden alcohol bencílico
JP6219918B2 (ja) 2012-03-19 2017-10-25 アルカームス ファーマ アイルランド リミテッド グリセロールエステルを含む医薬組成物
EP2897592B1 (en) 2012-09-19 2020-02-19 Alkermes Pharma Ireland Limited Pharmaceutical compositions having improved storage stability
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
CN105246897B (zh) 2013-05-24 2017-12-26 罗德科技公司 阿片样缩酮化合物和其用途
ES2784690T3 (es) 2013-12-05 2020-09-29 Univ Bath Nuevos compuestos opioides y sus usos
BR112016021535A8 (pt) 2014-03-20 2021-07-20 Alkermes Pharma Ireland Ltd kit compreendendo formulações de aripiprazol tendo velocidades de injeção aumentadas útil para o tratamento de uma desordem do sistema nervoso central e uso
AU2016259861B2 (en) * 2015-05-13 2020-08-13 4P-Pharma Stimulant abuse-deterrent compositions
EP3434267B1 (en) * 2016-03-24 2023-07-26 MEDRx Co., Ltd. Patch preparation having misuse prevention characteristics
AU2019224127B2 (en) 2018-02-23 2021-12-09 Rhodes Technologies Novel opioid compounds and uses thereof
EP3761983A1 (en) 2018-03-05 2021-01-13 Alkermes Pharma Ireland Limited Aripiprazole dosing strategy
WO2020012245A1 (en) 2018-07-13 2020-01-16 Alkermes Pharma Ireland Limited Thienothiophene-naltrexone prodrugs for long-acting injectable compositions
US10799496B2 (en) 2018-07-13 2020-10-13 Alkermes Pharma Ireland Limited Naphthylenyl compounds for long-acting injectable compositions and related methods
SG11202102648UA (en) * 2018-10-13 2021-04-29 Biohaven Pharm Holding Co Ltd Prodrugs of cgrp antagonists
US10975099B2 (en) 2018-11-05 2021-04-13 Alkermes Pharma Ireland Limited Thiophene compounds for long-acting injectable compositions and related methods
WO2020227337A1 (en) * 2019-05-07 2020-11-12 Bristol-Myers Squibb Company Prodrug compounds
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
EP4039331A4 (en) * 2019-09-30 2024-01-17 Nippon Chemiphar Co., Ltd. Azepan derivative

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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
JP2001526228A (ja) * 1997-12-22 2001-12-18 ユーロ−セルティーク，エス．エイ． オピオイド作動薬／拮抗薬の併用
AU754965B2 (en) * 1997-12-31 2002-11-28 University Of Kansas, The Water soluble prodrugs of tertiary amine containing drugs and methods of making thereof
US6703398B2 (en) * 2001-11-26 2004-03-09 Oliver Yoa-Pu Hu Orally administered analgesic compositions containing nalbuphine
JP2006520392A (ja) * 2003-03-13 2006-09-07 コントロールド・ケミカルズ・インコーポレーテッド 薬物の乱用可能性を低下させ且つ作用持続時間を延長する化合物および方法
CA2916869A1 (en) * 2004-06-12 2005-12-29 Jane C. Hirsh Abuse-deterrent drug formulations

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

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