MX362857B - Acido benzoico, derivados de acido benzoico y conjugados de acido heteroarilcarboxilico de hidromorfona, profarmacos, metodos de elaboracion y uso de los mismos. - Google Patents

Acido benzoico, derivados de acido benzoico y conjugados de acido heteroarilcarboxilico de hidromorfona, profarmacos, metodos de elaboracion y uso de los mismos.

Info

Publication number
MX362857B
MX362857B MX2014004691A MX2014004691A MX362857B MX 362857 B MX362857 B MX 362857B MX 2014004691 A MX2014004691 A MX 2014004691A MX 2014004691 A MX2014004691 A MX 2014004691A MX 362857 B MX362857 B MX 362857B
Authority
MX
Mexico
Prior art keywords
hydromorphone
benzoic acid
prodrugs
methods
making
Prior art date
Application number
MX2014004691A
Other languages
English (en)
Other versions
MX2014004691A (es
Inventor
Chi Guochen
Guenther Sven
Bera Bindu
Mickle Travis
Kanski Jaroslaw
K Martin Andrea
Original Assignee
Kempharm Inc Star
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 Star filed Critical Kempharm Inc Star
Publication of MX2014004691A publication Critical patent/MX2014004691A/es
Publication of MX362857B publication Critical patent/MX362857B/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/55Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/485Morphinan derivatives, e.g. morphine, codeine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/60Salicylic acid; Derivatives thereof
    • A61K31/612Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid
    • A61K31/616Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0043Nose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/14Antitussive agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36Opioid-abuse
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

La presente invención se refiere a composiciones que comprenden ácidos aril carboxílicos químicamente conjugados a hidromorfona (4,5-a-epoxi-3-hidroxi-17-metilmorfinan-6-ona) para formar nuevos profármacos/composiciones de hidromorfona. Los profármacos de hidromorfona de la presente invención tienen efectos secundaros disminuidos y potencial disminuido para abuso comparado a hidromorfona no conjugada. La presente invención también proporciona métodos para tratar pacientes, kits farmacéuticos y métodos para sintetizar conjugados de la presente invención.
MX2014004691A 2011-10-26 2012-10-25 Acido benzoico, derivados de acido benzoico y conjugados de acido heteroarilcarboxilico de hidromorfona, profarmacos, metodos de elaboracion y uso de los mismos. MX362857B (es)

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 (2)

Publication Number Publication Date
MX2014004691A MX2014004691A (es) 2014-07-09
MX362857B true MX362857B (es) 2019-02-20

Family

ID=48168468

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2014004691A MX362857B (es) 2011-10-26 2012-10-25 Acido benzoico, derivados de acido benzoico y conjugados de acido heteroarilcarboxilico de hidromorfona, profarmacos, metodos de elaboracion 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) CN105749294A (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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UA102916C2 (uk) 2009-07-02 2013-08-27 Кемфарм, Інк. Композиція на основі кон'югату гідрокодону з бензойною кислотою, похідними бензойної кислоти або гетероарилкарбоновою кислотою, проліки, спосіб лікування від зловживань
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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
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US10226456B2 (en) 2015-04-27 2019-03-12 3St Research Llc Methods and compositions for preventing opioid abuse
EP3210630A1 (en) 2016-02-29 2017-08-30 G.L. Pharma GmbH Abuse-deterrent pharmaceutical compositions
EP3231420A1 (en) * 2016-02-29 2017-10-18 G.L. Pharma GmbH Abuse-deterrent pharmaceutical compositions
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WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
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WO2021097532A1 (en) * 2019-11-22 2021-05-27 Deakin University Organic corrosion inhibitors

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Also Published As

Publication number Publication date
US9849185B2 (en) 2017-12-26
HK1223279A1 (zh) 2017-07-28
CA2856608A1 (en) 2013-05-02
CN105749294A (zh) 2016-07-13
US10441661B2 (en) 2019-10-15
KR101589846B1 (ko) 2016-01-28
JP2014532651A (ja) 2014-12-08
US20130150395A1 (en) 2013-06-13
RU2573388C2 (ru) 2016-01-20
US20170143839A1 (en) 2017-05-25
US10064956B2 (en) 2018-09-04
WO2013063204A1 (en) 2013-05-02
NZ623106A (en) 2015-06-26
US10258696B2 (en) 2019-04-16
HK1197191A1 (en) 2015-01-09
KR20140089520A (ko) 2014-07-15
CN104136031A (zh) 2014-11-05
ZA201402339B (en) 2015-07-29
EP2771002A1 (en) 2014-09-03
RU2014121065A (ru) 2015-12-10
CA2856608C (en) 2017-05-16
BR112014010099A8 (pt) 2018-01-16
US9566343B2 (en) 2017-02-14
BR112014010099A2 (pt) 2017-06-27
AR088551A1 (es) 2014-06-18
CO7010825A2 (es) 2014-07-31
US20190192670A1 (en) 2019-06-27
US20180339056A1 (en) 2018-11-29
AU2012328837B2 (en) 2015-07-09
MX2014004691A (es) 2014-07-09
SG11201401856VA (en) 2014-05-29
US20140330021A1 (en) 2014-11-06
US20180064820A1 (en) 2018-03-08
JP5769889B2 (ja) 2015-08-26
IL231822A0 (en) 2014-05-28
IN2014DN03009A (es) 2015-05-08
CL2014000995A1 (es) 2014-07-25
EP2771002A4 (en) 2015-08-12
AU2012328837A1 (en) 2014-05-01
US8816083B2 (en) 2014-08-26
CN104136031B (zh) 2016-05-04

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