CA2768392C - Oligomer-opioid agonist conjugates - Google Patents

Oligomer-opioid agonist conjugates Download PDF

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Publication number
CA2768392C
CA2768392C CA2768392A CA2768392A CA2768392C CA 2768392 C CA2768392 C CA 2768392C CA 2768392 A CA2768392 A CA 2768392A CA 2768392 A CA2768392 A CA 2768392A CA 2768392 C CA2768392 C CA 2768392C
Authority
CA
Canada
Prior art keywords
compound
oligomer
conjugates
nalbuphine
conjugate
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CA2768392A
Other languages
English (en)
French (fr)
Other versions
CA2768392A1 (en
Inventor
Jennifer Riggs-Sauthier
Bo-Liang Deng
Timothy A. Riley
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Nektar Therapeutics
Original Assignee
Nektar Therapeutics
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
Priority claimed from US12/558,395 external-priority patent/US8173666B2/en
Application filed by Nektar Therapeutics filed Critical Nektar Therapeutics
Publication of CA2768392A1 publication Critical patent/CA2768392A1/en
Application granted granted Critical
Publication of CA2768392C publication Critical patent/CA2768392C/en
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • 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
    • 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
    • A61K47/56—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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]
    • 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:
    • C07D489/09—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: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems
    • C07D489/10—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: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14
    • C07D489/12—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: containing 4aH-8, 9 c-Iminoethano- phenanthro [4, 5-b, c, d] furan ring systems condensed with carbocyclic rings or ring systems with a bridge between positions 6 and 14 the bridge containing only two carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Addiction (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Rheumatology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA2768392A 2009-07-21 2010-07-21 Oligomer-opioid agonist conjugates Expired - Fee Related CA2768392C (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US22739909P 2009-07-21 2009-07-21
US61/227,399 2009-07-21
US12/558,395 2009-09-11
US12/558,395 US8173666B2 (en) 2007-03-12 2009-09-11 Oligomer-opioid agonist conjugates
US35085310P 2010-06-02 2010-06-02
US61/350,853 2010-06-02
PCT/US2010/042792 WO2011011543A1 (en) 2009-07-21 2010-07-21 Oligomer-opioid agonist conjugates

Publications (2)

Publication Number Publication Date
CA2768392A1 CA2768392A1 (en) 2011-01-27
CA2768392C true CA2768392C (en) 2018-04-17

Family

ID=43499405

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2768392A Expired - Fee Related CA2768392C (en) 2009-07-21 2010-07-21 Oligomer-opioid agonist conjugates

Country Status (9)

Country Link
EP (2) EP2628489B1 (cg-RX-API-DMAC7.html)
JP (2) JP5837491B2 (cg-RX-API-DMAC7.html)
KR (1) KR101788886B1 (cg-RX-API-DMAC7.html)
CN (1) CN102573918A (cg-RX-API-DMAC7.html)
AU (1) AU2010276244B2 (cg-RX-API-DMAC7.html)
CA (1) CA2768392C (cg-RX-API-DMAC7.html)
IL (3) IL217634B (cg-RX-API-DMAC7.html)
MX (1) MX2012000980A (cg-RX-API-DMAC7.html)
WO (1) WO2011011543A1 (cg-RX-API-DMAC7.html)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10512644B2 (en) 2007-03-12 2019-12-24 Inheris Pharmaceuticals, Inc. Oligomer-opioid agonist conjugates
US8173666B2 (en) 2007-03-12 2012-05-08 Nektar Therapeutics Oligomer-opioid agonist conjugates
SG188474A1 (en) 2010-09-30 2013-05-31 Astrazeneca Ab Crystalline naloxol-peg conjugate
KR102016305B1 (ko) * 2011-11-07 2019-08-30 넥타르 테라퓨틱스 오피오이드 작용제 화합물 및 진통제 화합물의 조성물, 투여형 및 공동 투여
US10525054B2 (en) 2011-11-07 2020-01-07 Inheris Biopharma, Inc. Compositions, dosage forms, and co-administration of an opioid agonist compound and an analgesic compound
EP3327022A1 (en) * 2012-10-30 2018-05-30 Nektar Therapeutics Solid salt form of alpha-6-mpeg6-o-hydroxycodone as opioid agonists and uses thereof
ITRM20130223A1 (it) * 2013-04-15 2014-10-16 Rosario Nicoletti Derivati della codeina come inibitori della glucuronazione della morfina
CA2919892C (en) 2013-08-12 2019-06-18 Pharmaceutical Manufacturing Research Services, Inc. Extruded immediate release abuse deterrent pill
US9492444B2 (en) 2013-12-17 2016-11-15 Pharmaceutical Manufacturing Research Services, Inc. Extruded extended release abuse deterrent pill
WO2015095391A1 (en) 2013-12-17 2015-06-25 Pharmaceutical Manufacturing Research Services, Inc. Extruded extended release abuse deterrent pill
DK3169315T3 (da) 2014-07-17 2020-08-10 Pharmaceutical Manufacturing Res Services In Væskefyldt doseringsform til forhindring af misbrug med øjeblikkelig frigivelse
JP2017531026A (ja) 2014-10-20 2017-10-19 ファーマシューティカル マニュファクチュアリング リサーチ サービシズ，インコーポレーテッド 徐放性乱用抑止性液体充填剤形
CN107019803B (zh) * 2016-01-29 2020-09-15 北京键凯科技股份有限公司 具有低成瘾作用的聚乙二醇化阿片样物质
CN107033154B (zh) 2016-02-02 2020-02-04 上海瀚迈生物医药科技有限公司 阿片受体拮抗剂缀合物及其应用
JP7177392B2 (ja) * 2018-03-29 2022-11-24 日油株式会社 トリチル基含有単分散ポリエチレングリコールの精製方法
CN111039764A (zh) * 2018-10-12 2020-04-21 山东大学 一种双亲乙烯衍生物及制备方法
WO2021029914A1 (en) * 2019-08-11 2021-02-18 Kappa-Pharma LLC Compositions and methods of enhancing opioid receptor engagement by opioid hexadienoates and optionally substituted hexadienoates
CN116925105B (zh) * 2022-04-11 2025-11-25 上海瀚迈生物医药科技有限公司 阿片受体拮抗剂缀合物的固体盐型、晶型及其制备方法、组合物和用途
CN117567477A (zh) * 2023-11-15 2024-02-20 宜昌人福药业有限责任公司 一种氢吗啡酮和二氢吗啡类药物低分子聚乙二醇化物及其制备方法和应用

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US2654756A (en) 1949-10-20 1953-10-06 Mallinckrodt Chemical Works Process of preparing codeinone, dihydrocodeinone, and dihydromorphinone
US2628962A (en) 1949-10-20 1953-02-17 Mallinckrodt Chemical Works Method for preparing dihydrocodeinone, dihydromorphinone, and codeinone
US2649454A (en) 1951-08-20 1953-08-18 Univ California Method for preparing dihydromorphinone, dihydrocodeinone, and dihydropseudocodeinone
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EP0832106A2 (en) * 1995-06-05 1998-04-01 Cortech, Inc. Compounds having bradykinin antagonistic activity and mu-opioid agonistic activity
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EP2134371B1 (en) * 2007-03-12 2015-01-14 Nektar Therapeutics Oligomer-opioid agonist conjugates
WO2010033195A1 (en) * 2008-09-16 2010-03-25 Nektar Therapeutics Pegylated opioids with low potential for abuse

Also Published As

Publication number Publication date
JP2013500256A (ja) 2013-01-07
EP2628489A1 (en) 2013-08-21
WO2011011543A1 (en) 2011-01-27
IL263713A (en) 2019-01-31
JP2015180698A (ja) 2015-10-15
MX2012000980A (es) 2012-06-12
IL256822B (en) 2018-12-31
CN102573918A (zh) 2012-07-11
KR20120056828A (ko) 2012-06-04
IL217634B (en) 2018-01-31
CA2768392A1 (en) 2011-01-27
EP2628489B1 (en) 2017-03-01
AU2010276244A1 (en) 2012-03-15
IL256822A (en) 2018-05-31
EP2456469A1 (en) 2012-05-30
KR101788886B1 (ko) 2017-10-20
AU2010276244B2 (en) 2015-08-13
JP5837491B2 (ja) 2015-12-24

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Effective date: 20150710

MKLA Lapsed

Effective date: 20210721