CN102149412A - 肝脏保护剂对乙酰氨基酚协同前药 - Google Patents

肝脏保护剂对乙酰氨基酚协同前药 Download PDF

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Publication number
CN102149412A
CN102149412A CN2009801282430A CN200980128243A CN102149412A CN 102149412 A CN102149412 A CN 102149412A CN 2009801282430 A CN2009801282430 A CN 2009801282430A CN 200980128243 A CN200980128243 A CN 200980128243A CN 102149412 A CN102149412 A CN 102149412A
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China
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compound
acetaminophen
substituted
unsubstituted
amino acid
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CN2009801282430A
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English (en)
Chinese (zh)
Inventor
N·穆罕默德
K·R·布雷
J·托比阿斯
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NeurogesX Inc
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NeurogesX Inc
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Publication of CN102149412A publication Critical patent/CN102149412A/zh
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/52Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/02Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C07C233/04Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C233/07Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/485Morphinan derivatives, e.g. morphine, codeine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Toxicology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
CN2009801282430A 2008-05-20 2009-05-20 肝脏保护剂对乙酰氨基酚协同前药 Pending CN102149412A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US5477708P 2008-05-20 2008-05-20
US61/054,777 2008-05-20
PCT/US2009/044749 WO2009143299A1 (en) 2008-05-20 2009-05-20 Hepatoprotectant acetaminophen mutual prodrugs

Publications (1)

Publication Number Publication Date
CN102149412A true CN102149412A (zh) 2011-08-10

Family

ID=41340540

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2009801282430A Pending CN102149412A (zh) 2008-05-20 2009-05-20 肝脏保护剂对乙酰氨基酚协同前药

Country Status (12)

Country Link
US (3) US20110263545A1 (https=)
EP (1) EP2285419A4 (https=)
JP (6) JP5701750B2 (https=)
KR (1) KR101717145B1 (https=)
CN (1) CN102149412A (https=)
AU (1) AU2009249071A1 (https=)
BR (1) BRPI0912820A2 (https=)
CA (2) CA2724788C (https=)
IL (1) IL209384A0 (https=)
MX (1) MX2010012647A (https=)
RU (1) RU2010151951A (https=)
WO (1) WO2009143299A1 (https=)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101717145B1 (ko) 2008-05-20 2017-03-16 노이로제스엑스, 인코포레이티드 간보호제 아세트아미노펜 공통 프로드러그
RU2010151953A (ru) 2008-05-20 2012-06-27 Ньюроджесэкс, Инк. (Us) Карбонатные продукты и способы их применения
KR101698028B1 (ko) 2008-05-20 2017-01-26 노이로제스엑스, 인코포레이티드 수용성 아세트아미노펜 유사체
AU2012312136B2 (en) 2011-09-22 2017-06-29 Acorda Therapeutics, Inc. Acetaminophen conjugates, compositions and methods of use thereof
US20140179615A1 (en) * 2012-07-12 2014-06-26 Hainan Weikang Pharmaceutical (Qianshan) Co., Ltd. Glutathione and Acetaminophen Composition and Preparation Method Thereof
CA3042642A1 (en) 2013-08-12 2015-02-19 Pharmaceutical Manufacturing Research Services, Inc. Extruded immediate release abuse deterrent pill
US10172797B2 (en) 2013-12-17 2019-01-08 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
CA2955229C (en) 2014-07-17 2020-03-10 Pharmaceutical Manufacturing Research Services, Inc. Immediate release abuse deterrent liquid fill dosage form
US20170246194A1 (en) * 2014-08-15 2017-08-31 Purdue Pharma L.P. Acetaminophen-Containing Analgesic Formulations With Reduced Hepatotoxicity
WO2016064873A1 (en) 2014-10-20 2016-04-28 Pharmaceutical Manufacturing Research Services, Inc. Extended release abuse deterrent liquid fill dosage form
US11389409B2 (en) * 2019-08-30 2022-07-19 Remedy Diagnostics LLC Transdermal device comprising acetaminophen prodrug

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4035507A (en) * 1975-04-17 1977-07-12 Interx Research Corporation Novel, transient pro-drug forms of L-DOPA to treat Parkinson's disease
GB1583602A (en) 1977-05-26 1981-01-28 Sterwin Ag N-acetyl-para-aminophenyl-n'-acetyl-amino-thioalkanoic acid ester derivatives
US4562024A (en) 1982-07-06 1985-12-31 Sterling Drug Inc. Process for preparing granulate containing poorly compressible medicinally active matter
CH654302A5 (de) * 1983-05-04 1986-02-14 Sandoz Ag Acylaminophenolderivate, ihre herstellung und arzneimittel, welche sie enthalten.
US5001115A (en) * 1989-05-17 1991-03-19 University Of Florida Prodrugs of biologically active hydroxyaromatic compounds
US5474757A (en) * 1992-10-16 1995-12-12 Rutgers University Prevention of acetaminophen overdose toxicity with organosulfur compounds
DE4327462A1 (de) * 1993-08-16 1995-02-23 Carl Heinrich Dr Weischer Neue N-Acetyl-p-Aminophenol-Derivate zur Bekämpfung von Schmerzzuständen
US5916910A (en) 1997-06-04 1999-06-29 Medinox, Inc. Conjugates of dithiocarbamates with pharmacologically active agents and uses therefore
US6710086B1 (en) 2000-02-25 2004-03-23 Medinox, Inc. Protected forms of pharmacologically active agents and uses therefor
DE60108236T2 (de) 2000-03-14 2005-12-22 Actelion Pharmaceuticals Ltd. 1,2,3,4-tetrahydroisochinolin-derivate
AU4085201A (en) 2000-03-15 2001-09-24 Imperial College Innovations Limited Pharmaceutical composition
IT1319202B1 (it) 2000-10-12 2003-09-26 Nicox Sa Farmaci per le malattie a base infiammatoria.
US20030073618A1 (en) * 2001-02-08 2003-04-17 Kozhemyakin Leonid A. Compounds comprising disulfide-containing peptides and nitrogenous bases, and medical uses thereof
US7129261B2 (en) 2001-05-31 2006-10-31 Medarex, Inc. Cytotoxic agents
KR20040014544A (ko) 2001-06-05 2004-02-14 컨트롤 딜리버리 시스템즈 인코포레이티드 서방 진통제 화합물
EP1448231A1 (en) 2001-11-19 2004-08-25 Control Delivery Systems, Inc. Topical delivery of codrugs
US20050164994A1 (en) 2001-12-10 2005-07-28 Control Deliver Systems, Inc. Treatment of genitourinary tract disorders
EP1461122A4 (en) 2001-12-10 2006-08-23 Control Delivery Sys Inc TREATMENT OF DISEASES OF THE UROGENITAL SYSTEM
CA2472188C (en) 2002-01-18 2011-06-21 Control Delivery Systems, Inc. Polymeric gel system for the controlled delivery of codrugs
US20040058946A1 (en) 2002-07-05 2004-03-25 Buchwald Stephen L. Abuse-resistant prodrugs of oxycodone and other pharmaceuticals
US7381721B2 (en) 2003-03-17 2008-06-03 Adolor Corporation Substituted piperidine compounds
CN101921279A (zh) 2003-10-01 2010-12-22 阿得罗公司 螺环杂环衍生物及其应用方法
CA2544814C (en) 2003-11-12 2013-05-14 Applied Nanosystems B.V. Non-symmetrical gelling agent
US20050113294A1 (en) 2003-11-21 2005-05-26 Adolor Corporation. Carboxamide and amino derivatives and methods of their use
TW200616604A (en) 2004-08-26 2006-06-01 Nicholas Piramal India Ltd Nitric oxide releasing prodrugs containing bio-cleavable linker
US7598261B2 (en) 2005-03-31 2009-10-06 Adolor Corporation Spirocyclic heterocyclic derivatives and methods of their use
WO2007016108A1 (en) 2005-07-27 2007-02-08 Orexigen Therapeutics, Inc. Compositions for affecting weight loss
KR20080110759A (ko) 2006-03-24 2008-12-19 와이어쓰 통증 치료
CN101678120A (zh) 2006-12-05 2010-03-24 纽罗吉斯克斯公司 前药及其制备和使用方法
KR101698028B1 (ko) 2008-05-20 2017-01-26 노이로제스엑스, 인코포레이티드 수용성 아세트아미노펜 유사체
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

Also Published As

Publication number Publication date
KR20110011694A (ko) 2011-02-08
JP2021036001A (ja) 2021-03-04
BRPI0912820A2 (pt) 2015-10-13
MX2010012647A (es) 2010-12-14
JP2019081793A (ja) 2019-05-30
CA2724788C (en) 2016-12-06
KR101717145B1 (ko) 2017-03-16
US20110263545A1 (en) 2011-10-27
JP5701750B2 (ja) 2015-04-15
IL209384A0 (en) 2011-01-31
US20160326107A1 (en) 2016-11-10
US20190062273A1 (en) 2019-02-28
RU2010151951A (ru) 2012-06-27
US9951001B2 (en) 2018-04-24
JP2014111632A (ja) 2014-06-19
EP2285419A1 (en) 2011-02-23
JP2011523645A (ja) 2011-08-18
EP2285419A4 (en) 2012-05-02
CA2946445A1 (en) 2009-11-26
JP2017186380A (ja) 2017-10-12
JP2015227384A (ja) 2015-12-17
CA2724788A1 (en) 2009-11-26
CA2946445C (en) 2019-01-08
WO2009143299A1 (en) 2009-11-26
AU2009249071A1 (en) 2009-11-26

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