AR088551A1 - Conjugados de hidromorfona con acido benzoico, derivados de acido benzoico y acido heteroarilcarboxilico; profarmacos, metodos de preparacion y uso de los mismos - Google Patents

Conjugados de hidromorfona con acido benzoico, derivados de acido benzoico y acido heteroarilcarboxilico; profarmacos, metodos de preparacion y uso de los mismos

Info

Publication number
AR088551A1
AR088551A1 ARP120104022A ARP120104022A AR088551A1 AR 088551 A1 AR088551 A1 AR 088551A1 AR P120104022 A ARP120104022 A AR P120104022A AR P120104022 A ARP120104022 A AR P120104022A AR 088551 A1 AR088551 A1 AR 088551A1
Authority
AR
Argentina
Prior art keywords
hydromorphone
benzoic acid
acid
compositions
profarmacos
Prior art date
Application number
ARP120104022A
Other languages
English (en)
Inventor
Guenther Sven
Kanski Jaroslaw
Chi Guochen
K Martin Andrea
Bera Bindu
Mickle Travis
Original Assignee
Kempharm Inc
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 Kempharm Inc filed Critical Kempharm Inc
Publication of AR088551A1 publication Critical patent/AR088551A1/es

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Classifications

    • 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
    • A61K47/55—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 the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds
    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • 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
    • A61K31/60—Salicylic acid; Derivatives thereof
    • A61K31/612—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
    • A61K31/616—Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0043—Nose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Emergency Medicine (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Molecular Biology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nutrition Science (AREA)
  • Otolaryngology (AREA)
  • Physiology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pulmonology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

Composiciones que comprenden ácidos arilcarboxílicos conjugados químicamente con una hidromorfona. La tecnología que se describe consiste en composiciones que comprenden ácidos arilcarboxílicos conjugados químicamente con hidromorfona (4,5-a-epoxi-3-hidroxi-17-metil morfinan-6-ona) para formar profármacos/composiciones de hidromorfona. El uso de los mismos en el tratamiento del dolor. Reivindicación 4: La composición de prodroga de la reivindicación 2, donde el benzoato tiene la fórmula general (1) donde R¹, R² y R³ se seleccionan en forma independiente entre el grupo que consiste en hidrógeno, hidroxilo, amino, amina, amida, tiol, ciano, nitro, halógeno, imina, alquilo, alcoxi, arilo, alquenilo, alquinilo, haloalquilo, alquilarilo, arilalquilo, heterociclo, arilalcoxi, cicloalquilo, cicloalquenilo, cicloalquinilo, carbonilo, tioéter, selenoéter, sililo, sililoxi, sulfonilo, fosfonato.
ARP120104022A 2011-10-26 2012-10-26 Conjugados de hidromorfona con acido benzoico, derivados de acido benzoico y acido heteroarilcarboxilico; profarmacos, metodos de preparacion y uso de los mismos AR088551A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161551600P 2011-10-26 2011-10-26
US201261657201P 2012-06-08 2012-06-08

Publications (1)

Publication Number Publication Date
AR088551A1 true AR088551A1 (es) 2014-06-18

Family

ID=48168468

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120104022A AR088551A1 (es) 2011-10-26 2012-10-26 Conjugados de hidromorfona con acido benzoico, derivados de acido benzoico y acido heteroarilcarboxilico; profarmacos, metodos de preparacion y uso de los mismos

Country Status (19)

Country Link
US (6) US8816083B2 (es)
EP (1) EP2771002A4 (es)
JP (1) JP5769889B2 (es)
KR (1) KR101589846B1 (es)
CN (2) CN104136031B (es)
AR (1) AR088551A1 (es)
AU (1) AU2012328837B2 (es)
BR (1) BR112014010099A8 (es)
CA (1) CA2856608C (es)
CL (1) CL2014000995A1 (es)
CO (1) CO7010825A2 (es)
HK (2) HK1197191A1 (es)
IL (1) IL231822A0 (es)
IN (1) IN2014DN03009A (es)
MX (1) MX362857B (es)
RU (1) RU2573388C2 (es)
SG (1) SG11201401856VA (es)
WO (1) WO2013063204A1 (es)
ZA (1) ZA201402339B (es)

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Also Published As

Publication number Publication date
CN105749294A (zh) 2016-07-13
KR20140089520A (ko) 2014-07-15
US20140330021A1 (en) 2014-11-06
US8816083B2 (en) 2014-08-26
CL2014000995A1 (es) 2014-07-25
CN104136031B (zh) 2016-05-04
NZ623106A (en) 2015-06-26
EP2771002A1 (en) 2014-09-03
EP2771002A4 (en) 2015-08-12
MX362857B (es) 2019-02-20
AU2012328837A1 (en) 2014-05-01
BR112014010099A2 (pt) 2017-06-27
CA2856608C (en) 2017-05-16
CO7010825A2 (es) 2014-07-31
IL231822A0 (en) 2014-05-28
US20180064820A1 (en) 2018-03-08
JP2014532651A (ja) 2014-12-08
RU2573388C2 (ru) 2016-01-20
US20180339056A1 (en) 2018-11-29
US20170143839A1 (en) 2017-05-25
US20190192670A1 (en) 2019-06-27
US20130150395A1 (en) 2013-06-13
ZA201402339B (en) 2015-07-29
HK1197191A1 (en) 2015-01-09
HK1223279A1 (zh) 2017-07-28
CN104136031A (zh) 2014-11-05
RU2014121065A (ru) 2015-12-10
JP5769889B2 (ja) 2015-08-26
KR101589846B1 (ko) 2016-01-28
US10441661B2 (en) 2019-10-15
US10258696B2 (en) 2019-04-16
MX2014004691A (es) 2014-07-09
SG11201401856VA (en) 2014-05-29
AU2012328837B2 (en) 2015-07-09
US9566343B2 (en) 2017-02-14
CA2856608A1 (en) 2013-05-02
US9849185B2 (en) 2017-12-26
IN2014DN03009A (es) 2015-05-08
BR112014010099A8 (pt) 2018-01-16
WO2013063204A1 (en) 2013-05-02
US10064956B2 (en) 2018-09-04

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