CA2773340C - 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
CA2773340C
CA2773340C CA2773340A CA2773340A CA2773340C CA 2773340 C CA2773340 C CA 2773340C CA 2773340 A CA2773340 A CA 2773340A CA 2773340 A CA2773340 A CA 2773340A CA 2773340 C CA2773340 C CA 2773340C
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Prior art keywords
substituted
compound
alkyl
aryl
hydrogen
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CA2773340A
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English (en)
French (fr)
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CA2773340A1 (en
Inventor
Thomas E. Jenkins
Craig O. Husfeld
Julie D. Seroogy
Jonathan W. Wray
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Signature Therapeutics Inc
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Signature Therapeutics Inc
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Publication of CA2773340A1 publication Critical patent/CA2773340A1/en
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Classifications

    • 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:
    • C07D489/02—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
    • 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)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (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)
CA2773340A 2009-09-08 2010-04-21 Compositions comprising enzyme-cleavable ketone-modified opioid prodrugs and optional inhibitors thereof Active CA2773340C (en)

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

Publications (2)

Publication Number Publication Date
CA2773340A1 CA2773340A1 (en) 2011-03-17
CA2773340C true CA2773340C (en) 2019-07-23

Family

ID=43732738

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2773340A Active CA2773340C (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 (cg-RX-API-DMAC7.html)
EP (1) EP2475429B1 (cg-RX-API-DMAC7.html)
JP (3) JP2013503862A (cg-RX-API-DMAC7.html)
CN (1) CN102695545B (cg-RX-API-DMAC7.html)
AU (1) AU2010293028B2 (cg-RX-API-DMAC7.html)
BR (1) BR112012005124B1 (cg-RX-API-DMAC7.html)
CA (1) CA2773340C (cg-RX-API-DMAC7.html)
IL (1) IL218498A (cg-RX-API-DMAC7.html)
MX (1) MX348262B (cg-RX-API-DMAC7.html)
PH (1) PH12012500485A1 (cg-RX-API-DMAC7.html)
RU (1) RU2600736C2 (cg-RX-API-DMAC7.html)
SG (1) SG179026A1 (cg-RX-API-DMAC7.html)
WO (1) WO2011031350A1 (cg-RX-API-DMAC7.html)

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Also Published As

Publication number Publication date
US20120230916A1 (en) 2012-09-13
RU2012108874A (ru) 2013-09-20
AU2010293028A1 (en) 2012-04-05
IL218498A0 (en) 2012-07-31
HK1172283A1 (zh) 2013-04-19
JP2018172387A (ja) 2018-11-08
CN102695545A (zh) 2012-09-26
JP2016041698A (ja) 2016-03-31
EP2475429B1 (en) 2015-07-29
RU2600736C2 (ru) 2016-10-27
WO2011031350A1 (en) 2011-03-17
US20170119754A1 (en) 2017-05-04
CN102695545B (zh) 2016-08-17
BR112012005124A2 (pt) 2020-08-25
CA2773340A1 (en) 2011-03-17
EP2475429A1 (en) 2012-07-18
SG179026A1 (en) 2012-04-27
MX348262B (es) 2017-06-05
IL218498A (en) 2017-03-30
US9493477B2 (en) 2016-11-15
PH12012500485A1 (en) 2012-10-22
JP6778234B2 (ja) 2020-10-28
AU2010293028B2 (en) 2014-12-18
EP2475429A4 (en) 2013-04-03
JP2013503862A (ja) 2013-02-04
MX2012002847A (es) 2012-08-23
US10028945B2 (en) 2018-07-24
BR112012005124B1 (pt) 2021-11-09

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