AU2010293028B2 - Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof - Google Patents

Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof Download PDF

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Publication number
AU2010293028B2
AU2010293028B2 AU2010293028A AU2010293028A AU2010293028B2 AU 2010293028 B2 AU2010293028 B2 AU 2010293028B2 AU 2010293028 A AU2010293028 A AU 2010293028A AU 2010293028 A AU2010293028 A AU 2010293028A AU 2010293028 B2 AU2010293028 B2 AU 2010293028B2
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AU
Australia
Prior art keywords
compound
substituted
ketone
prodrug
alkyl
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AU2010293028A
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AU2010293028A1 (en
Inventor
Craig O. Husfeld
Thomas E. Jenkins
Julie D. Seroogy
Jonathan W. Wray
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Signature Therapeutics Inc
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Signature Therapeutics Inc
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Priority to AU2015201341A priority Critical patent/AU2015201341A1/en
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/02—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/485—Morphinan derivatives, e.g. morphine, codeine
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • 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
    • A61K38/05—Dipeptides
    • 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
    • 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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
    • C07D489/08—Oxygen atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (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)
  • Hydrogenated Pyridines (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Peptides Or Proteins (AREA)
AU2010293028A 2009-09-08 2010-04-21 Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof Active AU2010293028B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2015201341A AU2015201341A1 (en) 2009-09-08 2015-03-13 Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US24061109P 2009-09-08 2009-09-08
US61/240,611 2009-09-08
US28814809P 2009-12-18 2009-12-18
US61/288,148 2009-12-18
PCT/US2010/031956 WO2011031350A1 (en) 2009-09-08 2010-04-21 Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2015201341A Division AU2015201341A1 (en) 2009-09-08 2015-03-13 Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof

Publications (2)

Publication Number Publication Date
AU2010293028A1 AU2010293028A1 (en) 2012-04-05
AU2010293028B2 true AU2010293028B2 (en) 2014-12-18

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AU2010293028A Active AU2010293028B2 (en) 2009-09-08 2010-04-21 Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof

Country Status (13)

Country Link
US (2) US9493477B2 (https=)
EP (1) EP2475429B1 (https=)
JP (3) JP2013503862A (https=)
CN (1) CN102695545B (https=)
AU (1) AU2010293028B2 (https=)
BR (1) BR112012005124B1 (https=)
CA (1) CA2773340C (https=)
IL (1) IL218498A (https=)
MX (1) MX348262B (https=)
PH (1) PH12012500485A1 (https=)
RU (1) RU2600736C2 (https=)
SG (1) SG179026A1 (https=)
WO (1) WO2011031350A1 (https=)

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US20110262355A1 (en) 2010-04-21 2011-10-27 Jenkins Thomas E Compositions comprising enzyme-cleavable opioid prodrugs and inhibitors thereof
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CA2798884C (en) 2010-05-10 2016-09-13 Euro-Celtique S.A. Manufacturing of active-free granules and tablets comprising the same
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AU2011252039B2 (en) 2010-05-10 2014-06-12 Euro-Celtique S.A. Pharmaceutical compositions comprising hydromorphone and naloxone
ES2584634T3 (es) * 2011-01-11 2016-09-28 Signature Therapeutics, Inc. Composiciones que comprenden un profármaco de oxicodona escindible enzimáticamente
AU2012225337B2 (en) 2011-03-09 2016-04-28 Signature Therapeutics, Inc. Active agent prodrugs with heterocyclic linkers
WO2012122420A2 (en) 2011-03-09 2012-09-13 Pharmacofore, Inc. Opioid prodrugs with heterocyclic linkers
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WO2015071380A1 (en) 2013-11-13 2015-05-21 Euro-Celtique S.A. Hydromorphone and naloxone for treatment of pain and opioid bowel dysfunction syndrome
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US10717712B2 (en) * 2018-07-27 2020-07-21 Concentric Analgesics, Inc. Pegylated prodrugs of phenolic TRPV1 agonists
US10975099B2 (en) 2018-11-05 2021-04-13 Alkermes Pharma Ireland Limited Thiophene compounds for long-acting injectable compositions and related methods
US12599578B2 (en) 2021-03-09 2026-04-14 Ensysce Biosciences Inc. Compositions comprising enzyme-cleavable prodrugs and controlled release nafamostat and methods of use thereof
CN113624665A (zh) * 2021-07-30 2021-11-09 中国药科大学 一种抗肿瘤候选化合物在治疗结直肠癌药物中的应用及测定方法
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Also Published As

Publication number Publication date
AU2010293028A1 (en) 2012-04-05
MX348262B (es) 2017-06-05
EP2475429A4 (en) 2013-04-03
WO2011031350A1 (en) 2011-03-17
EP2475429B1 (en) 2015-07-29
MX2012002847A (es) 2012-08-23
IL218498A0 (en) 2012-07-31
JP2018172387A (ja) 2018-11-08
RU2012108874A (ru) 2013-09-20
HK1172283A1 (zh) 2013-04-19
US9493477B2 (en) 2016-11-15
BR112012005124A2 (pt) 2020-08-25
JP2016041698A (ja) 2016-03-31
SG179026A1 (en) 2012-04-27
CA2773340C (en) 2019-07-23
US20170119754A1 (en) 2017-05-04
US10028945B2 (en) 2018-07-24
IL218498A (en) 2017-03-30
JP2013503862A (ja) 2013-02-04
CA2773340A1 (en) 2011-03-17
CN102695545A (zh) 2012-09-26
JP6778234B2 (ja) 2020-10-28
RU2600736C2 (ru) 2016-10-27
CN102695545B (zh) 2016-08-17
PH12012500485A1 (en) 2012-10-22
EP2475429A1 (en) 2012-07-18
US20120230916A1 (en) 2012-09-13
BR112012005124B1 (pt) 2021-11-09

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