CN102149672A - 水溶性对乙酰氨基酚类似物 - Google Patents

水溶性对乙酰氨基酚类似物 Download PDF

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Publication number
CN102149672A
CN102149672A CN2009801282182A CN200980128218A CN102149672A CN 102149672 A CN102149672 A CN 102149672A CN 2009801282182 A CN2009801282182 A CN 2009801282182A CN 200980128218 A CN200980128218 A CN 200980128218A CN 102149672 A CN102149672 A CN 102149672A
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CN
China
Prior art keywords
acetaminophen
compound
prodrug
pain
administered
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN2009801282182A
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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 date
Application filed by NeurogesX Inc filed Critical NeurogesX Inc
Priority to CN201510381430.7A priority Critical patent/CN105254662A/zh
Publication of CN102149672A publication Critical patent/CN102149672A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C07F9/094—Esters of phosphoric acids with arylalkanols
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C07F9/091—Esters of phosphoric acids with hydroxyalkyl compounds with further substituents on alkyl

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CN2009801282182A 2008-05-20 2009-05-20 水溶性对乙酰氨基酚类似物 Pending CN102149672A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201510381430.7A CN105254662A (zh) 2008-05-20 2009-05-20 水溶性对乙酰氨基酚类似物

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US5477408P 2008-05-20 2008-05-20
US61/054,774 2008-05-20
PCT/US2009/044743 WO2009143295A1 (en) 2008-05-20 2009-05-20 Water-soluble acetaminophen analogs

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201510381430.7A Division CN105254662A (zh) 2008-05-20 2009-05-20 水溶性对乙酰氨基酚类似物

Publications (1)

Publication Number Publication Date
CN102149672A true CN102149672A (zh) 2011-08-10

Family

ID=41340538

Family Applications (2)

Application Number Title Priority Date Filing Date
CN2009801282182A Pending CN102149672A (zh) 2008-05-20 2009-05-20 水溶性对乙酰氨基酚类似物
CN201510381430.7A Pending CN105254662A (zh) 2008-05-20 2009-05-20 水溶性对乙酰氨基酚类似物

Family Applications After (1)

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CN201510381430.7A Pending CN105254662A (zh) 2008-05-20 2009-05-20 水溶性对乙酰氨基酚类似物

Country Status (12)

Country Link
US (4) US20110212926A1 (enExample)
EP (1) EP2291348A4 (enExample)
JP (6) JP5757864B2 (enExample)
KR (1) KR101698028B1 (enExample)
CN (2) CN102149672A (enExample)
AU (1) AU2009249067A1 (enExample)
BR (1) BRPI0912326A2 (enExample)
CA (1) CA2724877C (enExample)
IL (1) IL209382A0 (enExample)
MX (1) MX2010012648A (enExample)
RU (1) RU2010151952A (enExample)
WO (1) WO2009143295A1 (enExample)

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AU2009249071A1 (en) 2008-05-20 2009-11-26 Neurogesx, Inc. Hepatoprotectant acetaminophen mutual prodrugs
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
EP2177215A1 (en) 2008-10-17 2010-04-21 Laboratorios Del. Dr. Esteve, S.A. Co-crystals of tramadol and NSAIDs
US9359376B2 (en) * 2011-04-08 2016-06-07 Sphaera Pharma Pte. Ltd Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds
EP2758133A4 (en) 2011-09-22 2015-05-27 Acorda Therapeutics Inc ACETAMINOPHONE CONJUGATES, COMPOSITIONS AND METHOD OF USE THEREOF
CA3042642A1 (en) 2013-08-12 2015-02-19 Pharmaceutical Manufacturing Research Services, Inc. Extruded immediate release abuse deterrent pill
WO2015095391A1 (en) 2013-12-17 2015-06-25 Pharmaceutical Manufacturing Research Services, Inc. Extruded extended release abuse deterrent pill
US9492444B2 (en) 2013-12-17 2016-11-15 Pharmaceutical Manufacturing Research Services, Inc. Extruded extended release abuse deterrent pill
DK3169315T3 (da) 2014-07-17 2020-08-10 Pharmaceutical Manufacturing Res Services In Væskefyldt doseringsform til forhindring af misbrug med øjeblikkelig frigivelse
CN117164657A (zh) 2014-08-12 2023-12-05 莫纳什大学 定向淋巴的前药
AU2015336065A1 (en) 2014-10-20 2017-05-04 Pharmaceutical Manufacturing Research Services, Inc. Extended release abuse deterrent liquid fill dosage form
ES2739536T3 (es) 2014-10-21 2020-01-31 Abbvie Inc Profármacos de carbidopa y L-dopa y su uso para tratar la enfermedad de Parkinson
EP3265097A4 (en) 2015-03-03 2018-11-07 Kindred Biosciences Inc. Compositions and methods for treatment and prevention of pyrexia in horses
CN118063537A (zh) 2015-09-08 2024-05-24 莫纳什大学 定向淋巴的前药
US20190224220A1 (en) * 2016-04-20 2019-07-25 Abbvie Inc. Carbidopa and L-Dopa Prodrugs and Methods of Use
EP4306524A3 (en) 2017-08-29 2024-09-11 PureTech LYT, Inc. Lymphatic system-directing lipid prodrugs
US11883497B2 (en) 2017-08-29 2024-01-30 Puretech Lyt, Inc. Lymphatic system-directing lipid prodrugs
EP3727362A4 (en) 2017-12-19 2021-10-06 PureTech LYT, Inc. MYCOPHENOLIC ACID LIPID PRODRUGS AND THEIR USES
US11608345B1 (en) 2017-12-19 2023-03-21 Puretech Lyt, Inc. Lipid prodrugs of rapamycin and its analogs and uses thereof
US11304954B2 (en) 2017-12-19 2022-04-19 Puretech Lyt, Inc. Lipid prodrugs of mycophenolic acid and uses thereof
KR102928295B1 (ko) 2018-09-07 2026-02-13 알.피.쉐러 테크놀러지즈 엘엘씨 경화 및 낮은 hlb 계면 활성제(들)의 첨가를 통한 고체 또는 반고체 지질 기반 제형 안정화
TW202031265A (zh) 2018-11-15 2020-09-01 美商艾伯維有限公司 用於皮下投藥之醫藥調配物
US11389409B2 (en) * 2019-08-30 2022-07-19 Remedy Diagnostics LLC Transdermal device comprising acetaminophen prodrug
JP7810970B2 (ja) 2020-02-05 2026-02-04 シーポート・セラピューティクス・インコーポレイテッド 神経ステロイドの脂質プロドラッグ

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US4322410A (en) * 1978-12-15 1982-03-30 Jacques Dugniolle P-Acetaminophenyl phosphate salts as analgesics and antipyretics
US5985856A (en) * 1997-12-31 1999-11-16 University Of Kansas Water soluble prodrugs of secondary and tertiary amine containing drugs and methods of making thereof
CN1357000A (zh) * 1998-08-07 2002-07-03 堪萨斯州立大学 位阻醇或酚的水溶性前药
WO2005077394A1 (en) * 2004-02-11 2005-08-25 Ramot At Tel-Aviv University Ltd Compositions for treatment of cancer and inflammation with curcumin and at least one nsaid

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AU2009249071A1 (en) 2008-05-20 2009-11-26 Neurogesx, Inc. Hepatoprotectant acetaminophen mutual prodrugs
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
AU2009249069A1 (en) 2008-05-20 2009-11-26 Neurogesx, Inc. Carbonate prodrugs and methods of using the same
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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4322410A (en) * 1978-12-15 1982-03-30 Jacques Dugniolle P-Acetaminophenyl phosphate salts as analgesics and antipyretics
US5985856A (en) * 1997-12-31 1999-11-16 University Of Kansas Water soluble prodrugs of secondary and tertiary amine containing drugs and methods of making thereof
CN1357000A (zh) * 1998-08-07 2002-07-03 堪萨斯州立大学 位阻醇或酚的水溶性前药
WO2005077394A1 (en) * 2004-02-11 2005-08-25 Ramot At Tel-Aviv University Ltd Compositions for treatment of cancer and inflammation with curcumin and at least one nsaid

Also Published As

Publication number Publication date
KR101698028B1 (ko) 2017-01-26
BRPI0912326A2 (pt) 2015-10-06
IL209382A0 (en) 2011-01-31
JP2016084359A (ja) 2016-05-19
JP5757864B2 (ja) 2015-08-05
MX2010012648A (es) 2010-12-14
JP2020114876A (ja) 2020-07-30
CA2724877C (en) 2016-09-13
JP2011520977A (ja) 2011-07-21
US10442826B2 (en) 2019-10-15
AU2009249067A1 (en) 2009-11-26
EP2291348A1 (en) 2011-03-09
US20200002364A1 (en) 2020-01-02
EP2291348A4 (en) 2013-05-15
RU2010151952A (ru) 2012-06-27
WO2009143295A1 (en) 2009-11-26
KR20110018897A (ko) 2011-02-24
US20190092795A1 (en) 2019-03-28
US20110212926A1 (en) 2011-09-01
JP2018135392A (ja) 2018-08-30
US20160264605A1 (en) 2016-09-15
JP2017057217A (ja) 2017-03-23
US11021498B2 (en) 2021-06-01
JP6063072B2 (ja) 2017-01-18
CN105254662A (zh) 2016-01-20
US9981998B2 (en) 2018-05-29
JP2014111658A (ja) 2014-06-19
CA2724877A1 (en) 2009-11-26

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