EP2038251A4 - Positively charged water-soluble prodrugs of aspirin - Google Patents

Positively charged water-soluble prodrugs of aspirin

Info

Publication number
EP2038251A4
EP2038251A4 EP06780025A EP06780025A EP2038251A4 EP 2038251 A4 EP2038251 A4 EP 2038251A4 EP 06780025 A EP06780025 A EP 06780025A EP 06780025 A EP06780025 A EP 06780025A EP 2038251 A4 EP2038251 A4 EP 2038251A4
Authority
EP
European Patent Office
Prior art keywords
aspirin
positively charged
charged water
soluble prodrugs
prodrugs
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
EP06780025A
Other languages
German (de)
French (fr)
Other versions
EP2038251A1 (en
Inventor
Chongxi Yu
Lina Xu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
YU, CHONGXI
Techfields Biochem Co Ltd
Original Assignee
Techfields Biochem Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38922980&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EP2038251(A4) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Techfields Biochem Co Ltd filed Critical Techfields Biochem Co Ltd
Priority to EP13155198.8A priority Critical patent/EP2610242A1/en
Publication of EP2038251A1 publication Critical patent/EP2038251A1/en
Publication of EP2038251A4 publication Critical patent/EP2038251A4/en
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C219/00—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C219/02—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C219/04—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C219/14—Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having at least one of the hydroxy groups esterified by a carboxylic acid having the esterifying carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/44—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/58—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C235/60—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring with carbon atoms of carboxamide groups and singly-bound oxygen atoms, bound in ortho-position to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00—Thiocarboxylic acids
    • C07C327/20—Esters of monothiocarboxylic acids
    • C07C327/30—Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms, not being part of nitro or nitroso groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Emergency Medicine (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
EP06780025A 2006-07-09 2006-07-09 Positively charged water-soluble prodrugs of aspirin Pending EP2038251A4 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP13155198.8A EP2610242A1 (en) 2006-07-09 2006-07-09 Positively charged water-soluble prodrugs of aspirin

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/IB2006/052318 WO2008007171A1 (en) 2006-07-09 2006-07-09 Positively charged water-soluble prodrugs of aspirin

Publications (2)

Publication Number Publication Date
EP2038251A1 EP2038251A1 (en) 2009-03-25
EP2038251A4 true EP2038251A4 (en) 2010-04-21

Family

ID=38922980

Family Applications (2)

Application Number Title Priority Date Filing Date
EP13155198.8A Withdrawn EP2610242A1 (en) 2006-07-09 2006-07-09 Positively charged water-soluble prodrugs of aspirin
EP06780025A Pending EP2038251A4 (en) 2006-07-09 2006-07-09 Positively charged water-soluble prodrugs of aspirin

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EP13155198.8A Withdrawn EP2610242A1 (en) 2006-07-09 2006-07-09 Positively charged water-soluble prodrugs of aspirin

Country Status (6)

Country Link
EP (2) EP2610242A1 (en)
JP (1) JP5759672B2 (en)
CN (1) CN101484415B (en)
AU (1) AU2006346195B2 (en)
CA (1) CA2656858C (en)
WO (1) WO2008007171A1 (en)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090221703A1 (en) 2006-07-09 2009-09-03 Chongxi Yu High penetration composition and uses thereof
US20090238763A1 (en) 2006-07-09 2009-09-24 Chongxi Yu High penetration compositions and uses thereof
DK2041068T3 (en) * 2006-07-18 2017-02-27 Techfields Biochem Co Ltd POSITIVELY CHARGED, WATER SOLUBLE PRODRUGS OF IBUPROFEN WITH VERY FAST SKIN PENETRATION SPEED
ES2466346T3 (en) 2006-10-02 2014-06-10 Techfields Biochem Co. Ltd Prodrugs of water soluble prostaglandins with positive charge and compounds related to very high skin penetration rates
AU2006350707A1 (en) 2006-11-08 2008-05-15 Chongxi Yu Transdermal delivery systems of peptides and related compounds
PL2121593T3 (en) 2006-12-10 2015-11-30 Chongxi Yu Transdermal delivery systems of beta-lactam antibiotics
EP3181132A1 (en) 2007-01-15 2017-06-21 Chongxi Yu Positively charged water-soluble prodrugs of retinoids and retinoid-like compounds with very high skin penetration rates
PL2115140T3 (en) 2007-01-31 2017-03-31 Yu Positively charged water-soluble prodrugs of 1H-imidazo[4,5-c]quinolin-4-amines and related compounds with very high skin penetration rates
US9371284B2 (en) 2007-06-04 2016-06-21 Techfields Pharma Co., Ltd. Pro-drugs of NSAIAS with very high skin and membranes penetration rates and their new medicinal uses
CN102124086A (en) * 2008-07-31 2011-07-13 国际壳牌研究有限公司 Poly(hydroxycarboxylic acid) amide salt derivative and lubricating composition containing it
KR20230085223A (en) * 2008-12-04 2023-06-13 충시 위 High Penetration Compositions and Their Applications
US8575217B2 (en) * 2009-03-16 2013-11-05 Genmedica Therapeutics Sl Anti-inflammatory and antioxidant conjugates useful for treating metabolic disorders
CN102459313A (en) 2009-05-08 2012-05-16 上海泰飞尔生化技术有限公司 High penetration prodrug compositions of peptides and peptide-related compounds
US9969751B2 (en) 2009-06-10 2018-05-15 Techfields Pharma Co., Ltd. High penetration prodrug compositions of antimicrobials and antimicrobial-related compounds
EP2693876B1 (en) * 2011-04-08 2020-01-15 Sphaera Pharma Pte. Ltd Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds
KR102309973B1 (en) 2012-05-16 2021-10-06 테크필즈 파마 코., 엘티디. High penetration prodrug compositions and pharmaceutical composition thereof for treatment of pulmonary conditions
JP2016516018A (en) 2013-03-15 2016-06-02 テックフィールズ ファーマ カンパニー リミテッド Novel high-permeability drug and its composition for treating Parkinson's disease
JP5905411B2 (en) * 2013-06-12 2016-04-20 テックフィールズ バイオケム カンパニー リミテッド Positively charged water-soluble prodrug of aspirin
CN104276962B (en) * 2013-07-08 2019-04-12 浙江越甲药业有限公司 A kind of aspirin derivatives and combinations thereof and application
US20150072005A1 (en) * 2013-09-10 2015-03-12 Vitalis Llc Aspirin formulation for increased efficacy
US20160168108A1 (en) 2014-12-16 2016-06-16 Adt Pharmaceuticals, Inc. Method of treating or preventing ras-mediated diseases
US9862698B2 (en) 2014-12-16 2018-01-09 Adt Pharmaceuticals, Inc. Indenyl compounds, pharmaceutical compositions, and medical uses thereof
JP6153264B2 (en) * 2015-01-05 2017-06-28 テックフィールズ インコーポレイテッド NSAIA prodrug with very fast skin and membrane permeation rate and novel pharmaceutical use thereof
CN115521216A (en) 2015-04-01 2022-12-27 浙江越甲药业有限公司 Acetylsalicylic acid derivative crystal, and preparation method and application thereof
JP6289438B2 (en) * 2015-12-03 2018-03-07 テックフィールズ バイオケム カンパニー リミテッド Positively charged water-soluble prodrug of aspirin
JP6588485B2 (en) * 2017-02-21 2019-10-09 テックフィールズ バイオケム カンパニー リミテッド Positively charged water-soluble prodrug of aspirin
JP6961817B2 (en) 2017-10-26 2021-11-05 浙江越甲▲薬▼▲業▼有限公司 Stable pharmaceutical composition comprising a non-steroidal anti-inflammatory drug derivative
JP2021503474A (en) * 2017-11-17 2021-02-12 浙江越甲▲薬▼▲業▼有限公司 Local anesthetic
JP7169008B2 (en) 2018-04-26 2022-11-10 エーディーティー ファーマシューティカルズ，エルエルシー Anti-Cancer Indene, Indane, Azaindene, Azaindane, Pharmaceutical Compositions and Uses
CN113677660A (en) * 2018-12-29 2021-11-19 张婧 Acetylsalicylic acid derivative and application thereof
CN111925362B (en) * 2020-08-20 2023-06-23 陕西中医药大学 Anticancer compound and synthesis method and application thereof
CN113599375B (en) * 2021-06-21 2023-08-18 李萍 Oral administration medicine for treating oral diseases and application thereof
WO2023134733A1 (en) * 2022-01-17 2023-07-20 Techfields Pharma Co., Ltd. Treatment of signs, symptoms and/or complications of viral, bacterial, protozoal, and/or fungal infections by high penetration prodrugs
WO2023134732A1 (en) * 2022-01-17 2023-07-20 Techfields Pharma Co., Ltd. Prevention or treatment of cardiovascular diseases with high penetration prodrugs of aspirin and other nsaids

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GB958186A (en) * 1962-10-02 1964-05-21 Biosedra Lab Salicylamide derivatives
EP0152379A2 (en) * 1984-02-15 1985-08-21 Ciba-Geigy Ag Process for preparing pharmaceutical compositions containing unilamellar liposomes

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Title
CHANAL, J. L. ET AL: "Study on the distribution and elimination of dimethylaminoethyl acetylsalicylate in the rat. Effect of the carbon-14 labeling position", BOLLETTINO CHIMICO FARMACEUTICO , 119(6), 331-8 CODEN: BCFAAI; ISSN: 0006-6648, 1980, XP008119887 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 1966, MACHON, ZDZISLAW ET AL: "Synthesis of benzoylcholine derivatives", XP002571761, retrieved from STN Database accession no. 1966:412012 *
DATABASE CA [online] CHEMICAL ABSTRACTS SERVICE, COLUMBUS, OHIO, US; 1981, WOLINSKI, JERZY ET AL: "Search for anticholinergic compounds. XX. Synthesis of aminoalkyl o-, m-, and p-hydroxybenzoates and o-, m-, and p-acetoxybenzoates", XP002571760, retrieved from STN Database accession no. 1981:424459 *
MACHON, ZDZISLAW ET AL: "Synthesis of benzoylcholine derivatives", DISSERTATIONES PHARMACEUTICAE , 17(4), 491-6 CODEN: DIPHAH; ISSN: 0301-1615, 1965 *
See also references of WO2008007171A1 *
WOLINSKI, JERZY ET AL: "Search for anticholinergic compounds. XX. Synthesis of aminoalkyl o-, m-, and p-hydroxybenzoates and o-, m-, and p-acetoxybenzoates", ACTA POLONIAE PHARMACEUTICA , 37(3), 275-80 CODEN: APPHAX; ISSN: 0001-6837, 1980, XP008119888 *

Also Published As

Publication number Publication date
CA2656858C (en) 2016-01-19
CA2656858A1 (en) 2008-01-17
AU2006346195B2 (en) 2013-03-07
CN101484415B (en) 2013-08-14
EP2610242A1 (en) 2013-07-03
AU2006346195A1 (en) 2008-01-17
CN101484415A (en) 2009-07-15
WO2008007171A1 (en) 2008-01-17
EP2038251A1 (en) 2009-03-25
JP5759672B2 (en) 2015-08-05
JP2009542797A (en) 2009-12-03

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