IN2014DN03009A - - Google Patents

Info

Publication number
IN2014DN03009A
IN2014DN03009A IN3009DEN2014A IN2014DN03009A IN 2014DN03009 A IN2014DN03009 A IN 2014DN03009A IN 3009DEN2014 A IN3009DEN2014 A IN 3009DEN2014A IN 2014DN03009 A IN2014DN03009 A IN 2014DN03009A
Authority
IN
India
Prior art keywords
hydromorphone
present technology
prodrugs
compositions
methods
Prior art date
Application number
Inventor
Travis Mickle
Sven Guenther
Guochen Chi
Jaroslaw Kanski
Andrea K Martin
Bindu Bera
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 IN2014DN03009A publication Critical patent/IN2014DN03009A/en

Links

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
    • 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

The presently described technology provides compositions comprising aryl carboxylic acids chemically conjugated to hydromorphone (4 5 a epoxy 3 hydroxy 17 methyl morphinan 6 one) to form novel prodrugs/compositions of hydromorphone. The hydromorphone prodrugs of the present technology have decreased side effects and decreased potential for abuse compared to unconjugated hydromorphone. The present technology also provides methods of treating patients pharmaceutical kits and methods of synthesizing conjugates of the present technology.
IN3009DEN2014 2011-10-26 2012-10-25 IN2014DN03009A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161551600P 2011-10-26 2011-10-26
US201261657201P 2012-06-08 2012-06-08
PCT/US2012/061813 WO2013063204A1 (en) 2011-10-26 2012-10-25 Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof

Publications (1)

Publication Number Publication Date
IN2014DN03009A true IN2014DN03009A (en) 2015-05-08

Family

ID=48168468

Family Applications (1)

Application Number Title Priority Date Filing Date
IN3009DEN2014 IN2014DN03009A (en) 2011-10-26 2012-10-25

Country Status (20)

Country Link
US (6) US8816083B2 (en)
EP (1) EP2771002A4 (en)
JP (1) JP5769889B2 (en)
KR (1) KR101589846B1 (en)
CN (2) CN104136031B (en)
AR (1) AR088551A1 (en)
AU (1) AU2012328837B2 (en)
BR (1) BR112014010099A8 (en)
CA (1) CA2856608C (en)
CL (1) CL2014000995A1 (en)
CO (1) CO7010825A2 (en)
HK (2) HK1197191A1 (en)
IL (1) IL231822A0 (en)
IN (1) IN2014DN03009A (en)
MX (1) MX362857B (en)
PH (1) PH12014500791A1 (en)
RU (1) RU2573388C2 (en)
SG (1) SG11201401856VA (en)
WO (1) WO2013063204A1 (en)
ZA (1) ZA201402339B (en)

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SG11201401856VA (en) 2011-10-26 2014-05-29 Kempharm Inc Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof
US10626156B2 (en) 2013-12-06 2020-04-21 Jie Han Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs
GB201417529D0 (en) 2014-10-03 2014-11-19 Isis Innovation Beta lactamase inhibitors
RU2683317C2 (en) * 2014-11-25 2019-03-28 Кемфарм, Инк. Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxycodone
RU2683274C2 (en) 2014-12-02 2019-03-27 Кемфарм, Инк. Benzoic acid, benzoic acid derivatives and conjugates of heteroaryl carboxylic acid and oxymorphone, prodrugs, methods for obtaining and use thereof
US9987269B2 (en) 2015-04-27 2018-06-05 3St Research Llc Alpha-hydroxy carboxylic acid and derivatives and other GRAS-based prodrugs of oxymorphone and uses thereof
US10449190B2 (en) 2015-04-27 2019-10-22 John K. Thottathil Alpha-hydroxy carboxylic acid and derivatives and other GRAS-based prodrugs of opioids and uses thereof
US10017519B2 (en) 2015-04-27 2018-07-10 3St Research Llc Alpha-hydroxy carboxylic acid and derivatives and other GRAS based prodrugs of oxycodone and uses thereof
US10226456B2 (en) 2015-04-27 2019-03-12 3St Research Llc Methods and compositions for preventing opioid abuse
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US20200038383A1 (en) * 2016-10-14 2020-02-06 Kempharm, Inc. Immediate-release abuse deterrent compositions or medicaments for treating pain, add, adhd and other syndromes or disorders
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US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
WO2021097532A1 (en) * 2019-11-22 2021-05-27 Deakin University Organic corrosion inhibitors
WO2021097531A1 (en) * 2019-11-22 2021-05-27 Deakin University Polyionic corrosion inhibitors

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Also Published As

Publication number Publication date
ZA201402339B (en) 2015-07-29
US20190192670A1 (en) 2019-06-27
WO2013063204A1 (en) 2013-05-02
CN105749294A (en) 2016-07-13
CA2856608C (en) 2017-05-16
HK1223279A1 (en) 2017-07-28
RU2573388C2 (en) 2016-01-20
US8816083B2 (en) 2014-08-26
CL2014000995A1 (en) 2014-07-25
US9566343B2 (en) 2017-02-14
PH12014500791A1 (en) 2022-12-02
JP2014532651A (en) 2014-12-08
CN104136031A (en) 2014-11-05
US20180064820A1 (en) 2018-03-08
US20140330021A1 (en) 2014-11-06
RU2014121065A (en) 2015-12-10
NZ623106A (en) 2015-06-26
US9849185B2 (en) 2017-12-26
BR112014010099A2 (en) 2017-06-27
US20170143839A1 (en) 2017-05-25
US10441661B2 (en) 2019-10-15
US20130150395A1 (en) 2013-06-13
KR101589846B1 (en) 2016-01-28
EP2771002A4 (en) 2015-08-12
EP2771002A1 (en) 2014-09-03
BR112014010099A8 (en) 2018-01-16
JP5769889B2 (en) 2015-08-26
US10258696B2 (en) 2019-04-16
AU2012328837A1 (en) 2014-05-01
CA2856608A1 (en) 2013-05-02
MX2014004691A (en) 2014-07-09
SG11201401856VA (en) 2014-05-29
KR20140089520A (en) 2014-07-15
AR088551A1 (en) 2014-06-18
CO7010825A2 (en) 2014-07-31
MX362857B (en) 2019-02-20
CN104136031B (en) 2016-05-04
AU2012328837B2 (en) 2015-07-09
US10064956B2 (en) 2018-09-04
HK1197191A1 (en) 2015-01-09
IL231822A0 (en) 2014-05-28
US20180339056A1 (en) 2018-11-29

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