SG11201704309YA - Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods and making and use thereof - Google Patents

Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods and making and use thereof

Info

Publication number
SG11201704309YA
SG11201704309YA SG11201704309YA SG11201704309YA SG11201704309YA SG 11201704309Y A SG11201704309Y A SG 11201704309YA SG 11201704309Y A SG11201704309Y A SG 11201704309YA SG 11201704309Y A SG11201704309Y A SG 11201704309YA SG 11201704309Y A SG11201704309Y A SG 11201704309YA
Authority
SG
Singapore
Prior art keywords
benzoic acid
oxymorphone
prodrugs
making
methods
Prior art date
Application number
SG11201704309YA
Inventor
Travis Mickle
Sven Guenther
Sanjib Bera
Jaroslaw Kanski
Andrea Martin
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 SG11201704309YA publication Critical patent/SG11201704309YA/en

Links

Classifications

    • 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
    • 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
    • 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
    • A61K47/545Heterocyclic 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
    • 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
    • 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
    • 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]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/22Bridged ring systems
    • C07D221/28Morphinans
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D489/00Heterocyclic 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:
    • C07D489/06Heterocyclic 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
    • C07D489/08Oxygen atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
SG11201704309YA 2014-12-02 2015-12-02 Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods and making and use thereof SG11201704309YA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462086326P 2014-12-02 2014-12-02
PCT/US2015/063351 WO2016089951A1 (en) 2014-12-02 2015-12-02 Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods and making and use thereof

Publications (1)

Publication Number Publication Date
SG11201704309YA true SG11201704309YA (en) 2017-06-29

Family

ID=55022688

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201704309YA SG11201704309YA (en) 2014-12-02 2015-12-02 Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods and making and use thereof

Country Status (19)

Country Link
US (4) US9682076B2 (en)
EP (1) EP3226907A1 (en)
JP (2) JP6462877B2 (en)
KR (1) KR20170094251A (en)
CN (1) CN106999487A (en)
AU (1) AU2015358606B9 (en)
BR (1) BR112017011764A2 (en)
CA (1) CA2969221C (en)
CL (1) CL2017001417A1 (en)
CO (1) CO2017005203A2 (en)
HK (1) HK1244209A1 (en)
IL (1) IL252472A0 (en)
MA (1) MA40937A (en)
MX (1) MX2017006935A (en)
NZ (1) NZ731586A (en)
PH (1) PH12017500859A1 (en)
RU (1) RU2683274C2 (en)
SG (1) SG11201704309YA (en)
WO (1) WO2016089951A1 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9682076B2 (en) 2014-12-02 2017-06-20 Kempharm, Inc. Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods of making and use thereof
RU2657803C1 (en) * 2017-03-21 2018-06-15 федеральное государственное бюджетное образовательное учреждение высшего образования "Алтайский государственный университет" Agent possessing anti-inflammatory and analgesic action
JP7369687B2 (en) 2017-07-20 2023-10-26 スーチョウ ランシンダタイ ファーマシューティクス エルティーディー シーオー. Abuse Deterrent Long Acting Extended Release Opioid Prodrug
CN111836813A (en) * 2018-02-23 2020-10-27 罗德科技公司 Novel opioid compounds and uses thereof

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US4668685A (en) 1984-07-05 1987-05-26 E.I. Du Pont De Nemours And Company Substituted benzoate ester prodrug derivatives of 3-hydroxymorphinans, which are analgesics or narcotic antagonists
US5965161A (en) 1994-11-04 1999-10-12 Euro-Celtique, S.A. Extruded multi-particulates
NZ298712A (en) 1995-01-16 1998-12-23 Commw Scient Ind Res Org Fatty acid acyl group conjugates as therapeutic compounds
DE19602963A1 (en) 1995-12-20 1997-07-31 Nycomed Arzneimittel Gmbh New morphine derivatives
ATE526950T1 (en) 1999-10-29 2011-10-15 Euro Celtique Sa CONTROLLED RELEASE HYDROCODONE FORMULATIONS
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CN1514729B (en) 2001-06-05 2012-09-05 控制释放***公司 Sustained-release analgesic compounds
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US20040033253A1 (en) * 2002-02-19 2004-02-19 Ihor Shevchuk Acyl opioid antagonists
US7135575B2 (en) * 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
WO2004082620A2 (en) 2003-03-13 2004-09-30 Controlled Chemicals, Inc. Oxycodone conjugates with lower the abuse potential and extended duration of action
AU2007238625A1 (en) 2006-04-14 2007-10-25 Shire Llc Compositions and methods for enhancing analgesic potency of covalently bound compounds, attenuating its adverse side effects, and preventing their abuse
EP2046393B1 (en) * 2006-05-26 2014-02-12 Signature Therapeutics, Inc. Controlled release of phenolic opioids
WO2008055237A2 (en) 2006-10-31 2008-05-08 Rebit, Inc. System for automatically recovering a computer memory using shadowed data and file directory structures
US20120142718A1 (en) 2007-02-16 2012-06-07 Jenkins Thomas E N-17-Alkylated Prodrugs of Opioids
WO2009092073A2 (en) 2008-01-18 2009-07-23 Shire Llc Amino acid and peptide prodrugs of opioid analgesics with reduced gi side-effects
JP2013523599A (en) 2009-04-02 2013-06-17 シャイア エルエルシー Novel opioid dicarboxylic acid linked amino acid and peptide prodrugs and uses thereof
US8871780B2 (en) 2009-07-02 2014-10-28 Kempharm, Inc. Phenylethanoic acid, phenylpropanoic acid and phenylpropenoic acid conjugates and prodrugs of hydrocodone, method of making and use thereof
UA102916C2 (en) 2009-07-02 2013-08-27 Кемфарм, Інк. Composition based on conjugates of hydrocodone with benzoic acid, benzoic acid or heteroaryl carboxylic acid derivatives, prodrugs and method for treatment of abuses
WO2011009012A1 (en) 2009-07-15 2011-01-20 Columbia University METHODS OF SUPPRESSING APPETITE BY THE ADMINISTRATION OF ANTAGONISTS OF THE SEROTONIN HTR1a or HTR2b RECEPTORS OR INHIBITORS OF TPH2
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JP2013503862A (en) 2009-09-08 2013-02-04 シグネーチャー セラピューティクス,インク. Composition comprising an enzyme-cleavable ketone-modified opioid prodrug and an optional inhibitor thereof
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KR101589846B1 (en) * 2011-10-26 2016-01-28 켐팜 인코포레이티드 Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of hydromorphone, prodrugs, methods of making and use thereof
US9682076B2 (en) 2014-12-02 2017-06-20 Kempharm, Inc. Benzoic acid, benzoic acid derivatives and heteroaryl carboxylic acid conjugates of oxymorphone, prodrugs, methods of making and use thereof

Also Published As

Publication number Publication date
RU2017123161A3 (en) 2019-01-09
IL252472A0 (en) 2017-07-31
CO2017005203A2 (en) 2017-08-31
PH12017500859A1 (en) 2017-11-06
AU2015358606B9 (en) 2019-05-02
NZ731586A (en) 2018-06-29
US10071091B2 (en) 2018-09-11
US9682076B2 (en) 2017-06-20
US10463660B2 (en) 2019-11-05
US20180338968A1 (en) 2018-11-29
MA40937A (en) 2017-10-11
MX2017006935A (en) 2017-08-10
US10758528B2 (en) 2020-09-01
RU2683274C2 (en) 2019-03-27
US20170312270A1 (en) 2017-11-02
WO2016089951A1 (en) 2016-06-09
JP2017538696A (en) 2017-12-28
CA2969221C (en) 2021-01-12
KR20170094251A (en) 2017-08-17
CA2969221A1 (en) 2016-06-09
RU2017123161A (en) 2019-01-09
US20200030316A1 (en) 2020-01-30
AU2015358606A1 (en) 2017-05-25
CN106999487A (en) 2017-08-01
HK1244209A1 (en) 2018-08-03
EP3226907A1 (en) 2017-10-11
BR112017011764A2 (en) 2018-07-10
CL2017001417A1 (en) 2018-02-09
JP2019077695A (en) 2019-05-23
JP6462877B2 (en) 2019-01-30
US20160151352A1 (en) 2016-06-02
AU2015358606B2 (en) 2019-04-18

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