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)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Rheumatology (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
RU2010151953A (ru) 2008-05-20 2012-06-27 Ньюроджесэкс, Инк. (Us) Карбонатные продукты и способы их применения
KR101717145B1 (ko) 2008-05-20 2017-03-16 노이로제스엑스, 인코포레이티드 간보호제 아세트아미노펜 공통 프로드러그
KR101698028B1 (ko) 2008-05-20 2017-01-26 노이로제스엑스, 인코포레이티드 수용성 아세트아미노펜 유사체
EP2307375B1 (en) 2008-07-28 2014-11-19 Pfizer Inc. Phenanthrenone compounds, compositions and methods
WO2010033540A1 (en) * 2008-09-19 2010-03-25 Mallinckrodt Inc. Crystalline forms of fentanyl alkaloid
LT2445502T (lt) 2009-06-25 2017-09-25 Alkermes Pharma Ireland Limited Heterocikliniai junginiai, skirti neurologinių ir fiziologinių susirgimų gydymui
CA2937222C (en) 2009-06-25 2019-06-04 Alkermes Pharma Ireland Limited Prodrugs of nh-acidic compounds
AU2011270701B2 (en) 2010-06-24 2015-05-14 Alkermes Pharma Ireland Limited Prodrugs of NH-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives
BR112013023847B1 (pt) 2011-03-18 2021-02-23 Alkermes Pharma Ireland Limited composições farmacêuticas compreendendo ésteres de sorbitano e uso das mesmas
ES2883259T3 (es) * 2011-07-28 2021-12-07 Kempharm Inc Profármacos de metilfenidato, procesos para la obtención y uso de los mismos
AU2012312136B2 (en) 2011-09-22 2017-06-29 Acorda Therapeutics, Inc. Acetaminophen conjugates, compositions and methods of use thereof
NZ722096A (en) 2011-12-15 2016-11-25 Alkermes Pharma Ireland Ltd Prodrugs of secondary amine compounds
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
CA2867121C (en) 2012-03-19 2021-05-25 Alkermes Pharma Ireland Limited Pharmaceutical compositions comprising fatty acid esters
JP6654042B2 (ja) 2012-09-19 2020-02-26 アルカームス ファーマ アイルランド リミテッド 貯蔵安定性が改善された医薬組成物
WO2014172482A1 (en) 2013-04-17 2014-10-23 Robert Alfred Volkmann Compounds for treatment of pain
WO2014172478A1 (en) 2013-04-17 2014-10-23 VOLKMANN Robert Compounds for treatment of pain
EP3004115B1 (en) 2013-05-24 2019-03-06 Rhodes Technologies Opioid ketal compounds and uses thereof
WO2015082932A1 (en) 2013-12-05 2015-06-11 The University Of Bath Novel opioid compounds and their uses
CN106132415A (zh) 2014-03-20 2016-11-16 奥克梅斯制药爱尔兰有限公司 具有增加的注射速度的阿立哌唑制剂
EP3294278B1 (en) 2015-05-13 2022-05-11 4P-Pharma Apomorphine for the treatment of methylphenidate induced hyperactivity
US20170273974A1 (en) * 2016-03-24 2017-09-28 Medrx Co., Ltd Patch preparations with misuse prevention features
EP3755704A1 (en) 2018-02-23 2020-12-30 Rhodes Technologies Inc. Novel opioid compounds and uses thereof
EP3761983A1 (en) 2018-03-05 2021-01-13 Alkermes Pharma Ireland Limited Aripiprazole dosing strategy
US10799496B2 (en) 2018-07-13 2020-10-13 Alkermes Pharma Ireland Limited 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
US12030868B2 (en) 2018-10-13 2024-07-09 Pfizer Ireland Pharmaceuticals 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
CN114072403A (zh) * 2019-05-07 2022-02-18 百时美施贵宝公司 前药化合物
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
KR20220071223A (ko) * 2019-09-30 2022-05-31 닛뽕 케미파 가부시키가이샤 아제판 유도체

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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
EP1041987B1 (en) * 1997-12-22 2006-04-19 Euro-Celtique S.A. Pharmaceutical oral dosage form comprising a combination of an opioid agonist and naltrexone
KR20010033811A (ko) * 1997-12-31 2001-04-25 토마스 안 빅토리아 2차 및 3차 아민을 함유하는 약제의 물에 용해가능한프로드럭 및 그것의 제조방법
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
PT1765292T (pt) * 2004-06-12 2017-12-29 Collegium Pharmaceutical Inc Formulações de fármacos dissuasoras de abuso

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

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