NZ545570A - Amino acid prodrugs - Google Patents

Amino acid prodrugs

Info

Publication number
NZ545570A
NZ545570A NZ545570A NZ54557004A NZ545570A NZ 545570 A NZ545570 A NZ 545570A NZ 545570 A NZ545570 A NZ 545570A NZ 54557004 A NZ54557004 A NZ 54557004A NZ 545570 A NZ545570 A NZ 545570A
Authority
NZ
New Zealand
Prior art keywords
drug
amino acid
improved
enhanced
alpha
Prior art date
Application number
NZ545570A
Inventor
V Ravi Chandran
Original Assignee
Signature R & D Holdings Llc
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
Application filed by Signature R & D Holdings Llc filed Critical Signature R & D Holdings Llc
Publication of NZ545570A publication Critical patent/NZ545570A/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/02—Peptides of undefined number of amino acids; Derivatives thereof
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A61K38/13—Cyclosporins
    • 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
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • C07K7/645—Cyclosporins; Related peptides
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Biophysics (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Provided is a drug-conjugate product obtained by reacting the drug with an alpha-L- amino acid selected from L-Proline and L-Hydroxyproline under conditions effective to form a compound having a covalent bond between the drug and the alpha-L-amino acid, wherein the drug is selected from a list of specified drugs (including ibuprofen and aspirin), and characterized in that said drug-conjugate product provides for an enhanced therapeutic quality of the drug, the enhanced therapeutic quality being selected from the group consisting of: (a) improved taste or smell, (b) desired octanol/water partition coefficient, (c) improved stability, (d) enhanced penetration of blood-brain barrier, (e) elimination of first pass effect in the liver, (f) reduction of intero-hepatic recirculation, (g) painless injection with parental formulation, (h) improved bioavailability, (i) improved changes in the rate of absorption, (j) reduced side effects, (k) dose proportionality, (l) selective hydrolysis at site of action, (m) controlled release properties, (n) targeted drug delivery, (o) reduction in toxicity, (p) reduced dose, (q) alteration of metabolic pathway to deliver more drug at site of action, (r) increased solubility in aqueous solution and (s) enhanced efficacy.
NZ545570A 2003-07-29 2004-07-29 Amino acid prodrugs NZ545570A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US49133103P 2003-07-29 2003-07-29
PCT/US2004/024901 WO2005046575A2 (en) 2003-07-29 2004-07-29 Amino acid prodrugs

Publications (1)

Publication Number Publication Date
NZ545570A true NZ545570A (en) 2012-07-27

Family

ID=34590076

Family Applications (3)

Application Number Title Priority Date Filing Date
NZ601780A NZ601780A (en) 2003-07-29 2004-07-29 Amino Acid Prodrugs
NZ601772A NZ601772A (en) 2003-07-29 2004-07-29 Amino Acid Prodrugs
NZ545570A NZ545570A (en) 2003-07-29 2004-07-29 Amino acid prodrugs

Family Applications Before (2)

Application Number Title Priority Date Filing Date
NZ601780A NZ601780A (en) 2003-07-29 2004-07-29 Amino Acid Prodrugs
NZ601772A NZ601772A (en) 2003-07-29 2004-07-29 Amino Acid Prodrugs

Country Status (11)

Country Link
EP (1) EP1660017A4 (en)
JP (2) JP2007510621A (en)
KR (3) KR20120116991A (en)
CN (1) CN101123878A (en)
AU (1) AU2004289174B2 (en)
CA (1) CA2534342C (en)
IL (1) IL173382A0 (en)
NZ (3) NZ601780A (en)
SG (2) SG145693A1 (en)
WO (1) WO2005046575A2 (en)
ZA (1) ZA200600660B (en)

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AU2004289174A2 (en) 2005-05-26
WO2005046575A2 (en) 2005-05-26
AU2004289174B2 (en) 2011-05-19
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KR20130081319A (en) 2013-07-16
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SG178721A1 (en) 2012-03-29
EP1660017A2 (en) 2006-05-31
ZA200600660B (en) 2007-04-25
EP1660017A4 (en) 2011-03-09
AU2004289174A1 (en) 2005-05-26
CN101123878A (en) 2008-02-13
IL173382A0 (en) 2006-06-11
CA2534342C (en) 2016-05-10
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NZ601780A (en) 2012-10-26
CA2534342A1 (en) 2005-05-26

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