CN103561770B - 硫辛酰基化合物及其用于治疗缺血性伤害的用途 - Google Patents

硫辛酰基化合物及其用于治疗缺血性伤害的用途 Download PDF

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Publication number
CN103561770B
CN103561770B CN201180065214.1A CN201180065214A CN103561770B CN 103561770 B CN103561770 B CN 103561770B CN 201180065214 A CN201180065214 A CN 201180065214A CN 103561770 B CN103561770 B CN 103561770B
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ischemia
injury
reperfusion
pharmaceutically acceptable
compound
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Chinese (zh)
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CN103561770A (zh
Inventor
亚历山大·B·巴奎西
莱尼尔·必优克斯
罗夫·卡萨尔
史蒂芬·A·凯特斯
艾伦·S·雷得
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Ischemix LLC
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D339/00—Heterocyclic compounds containing rings having two sulfur atoms as the only ring hetero atoms
    • C07D339/02—Five-membered rings
    • C07D339/04—Five-membered rings having the hetero atoms in positions 1 and 2, e.g. lipoic acid
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/385—Heterocyclic compounds having sulfur as a ring hetero atom having two or more sulfur atoms in the same ring
    • 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
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • 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
    • 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
    • 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
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
    • C07F9/655345—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms the sulfur atom being part of a five-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06104—Dipeptides with the first amino acid being acidic
    • C07K5/06113—Asp- or Asn-amino acid

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201180065214.1A 2010-11-18 2011-11-10 硫辛酰基化合物及其用于治疗缺血性伤害的用途 Expired - Fee Related CN103561770B (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US41524110P 2010-11-18 2010-11-18
US41524010P 2010-11-18 2010-11-18
US61/415,240 2010-11-18
US61/415,241 2010-11-18
US201161478310P 2011-04-22 2011-04-22
US61/478,310 2011-04-22
US201161500974P 2011-06-24 2011-06-24
US61/500,974 2011-06-24
PCT/US2011/060259 WO2012067947A1 (en) 2010-11-18 2011-11-10 Lipoyl compounds and their use for treating ischemic injury

Publications (2)

Publication Number Publication Date
CN103561770A CN103561770A (zh) 2014-02-05
CN103561770B true CN103561770B (zh) 2016-11-09

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CN201180065214.1A Expired - Fee Related CN103561770B (zh) 2010-11-18 2011-11-10 硫辛酰基化合物及其用于治疗缺血性伤害的用途

Country Status (15)

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US (2) US8815937B2 (enExample)
EP (1) EP2640423B1 (enExample)
JP (3) JP2014502264A (enExample)
KR (1) KR20140020840A (enExample)
CN (1) CN103561770B (enExample)
AU (1) AU2011329215C1 (enExample)
BR (1) BR112013012057B1 (enExample)
CA (1) CA2817362C (enExample)
DK (1) DK2640423T3 (enExample)
ES (1) ES2640474T3 (enExample)
IL (1) IL226258A (enExample)
MX (1) MX344933B (enExample)
NZ (1) NZ610378A (enExample)
SG (1) SG190794A1 (enExample)
WO (1) WO2012067947A1 (enExample)

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US7928067B2 (en) 2009-05-14 2011-04-19 Ischemix Llc Compositions and methods for treating ischemia and ischemia-reperfusion injury
JP2014502264A (ja) 2010-11-18 2014-01-30 イスケミックス エルエルシー リポイル化合物および虚血性傷害を治療するためのその使用
ITFI20120170A1 (it) * 2012-08-28 2014-03-01 Consorzio Interuniversitario Nazion Ale Per La Sci Nuovi composti ad azione anti-allodinica ed anti-iperalgesica.
CA2940361A1 (en) 2014-02-27 2015-09-03 Consorzio Interuniversitario Nazionale Per La Scienza E Tecnologia Dei Materiali Instm Novel compounds having anti-allodynic and antihyperalgesic activity
WO2015174948A1 (en) 2014-05-14 2015-11-19 Ischemix, LLC Formulations comprising lipoyl compounds
US11155531B2 (en) * 2016-03-14 2021-10-26 Neostrata Company, Inc. N-lipoic-amino acid or peptide, derivatives and their uses
RU2657820C1 (ru) * 2017-03-13 2018-06-15 Федеральное государственное бюджетное образовательное учреждение высшего образования "Волгоградский государственный медицинский университет" Министерства здравоохранения Российской Федерации ФГБОУ ВО ВолгГМУ МЗ РФ 4-(4-Ацетоксибензоиламино)бутаноилглицин, обладающий церебропротекторным действием при ишемии головного мозга
JP7203756B2 (ja) 2017-04-25 2023-01-13 イスケミックス エルエルシー 外傷性脳傷害を治療するための組成物および方法
US20240124520A1 (en) * 2019-10-16 2024-04-18 The Board Of Trustees Of The Leland Stanford Junior University N-acylated histidine dipeptides as anticancer agents
US11306076B2 (en) * 2020-05-11 2022-04-19 Xi'an Taikomed Pharmaceutical Technology Co., Ltd. Silibinin lipoic acid ester with hepatoprotective activity and a method of preparing the same
CN116199666B (zh) * 2023-03-07 2025-02-28 中国药科大学 两亲性化合物及其药物组合物

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SG190794A1 (en) 2013-07-31
CA2817362A1 (en) 2012-05-24
AU2011329215C1 (en) 2016-08-11
EP2640423A1 (en) 2013-09-25
IL226258A (en) 2017-02-28
AU2011329215B2 (en) 2016-04-28
US9359325B2 (en) 2016-06-07
MX344933B (es) 2017-01-11
US20130237483A1 (en) 2013-09-12
BR112013012057B1 (pt) 2021-11-09
MX2013005508A (es) 2013-07-17
NZ610378A (en) 2015-05-29
JP2014502264A (ja) 2014-01-30
ES2640474T3 (es) 2017-11-03
KR20140020840A (ko) 2014-02-19
CA2817362C (en) 2018-10-23
US20150065564A1 (en) 2015-03-05
US8815937B2 (en) 2014-08-26
DK2640423T3 (en) 2017-10-02
EP2640423B1 (en) 2017-07-26
JP6280094B2 (ja) 2018-02-14
JP2018016652A (ja) 2018-02-01
BR112013012057A2 (pt) 2020-08-04
AU2011329215A1 (en) 2013-05-30
CN103561770A (zh) 2014-02-05
WO2012067947A1 (en) 2012-05-24
IL226258A0 (en) 2013-07-31
JP2016033157A (ja) 2016-03-10

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