CN102573918A - 低聚物-阿片样激动剂轭合物 - Google Patents

低聚物-阿片样激动剂轭合物 Download PDF

Info

Publication number
CN102573918A
CN102573918A CN2010800376109A CN201080037610A CN102573918A CN 102573918 A CN102573918 A CN 102573918A CN 2010800376109 A CN2010800376109 A CN 2010800376109A CN 201080037610 A CN201080037610 A CN 201080037610A CN 102573918 A CN102573918 A CN 102573918A
Authority
CN
China
Prior art keywords
mpeg
conjugates
nalbuphine
peg
oligomer
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.)
Pending
Application number
CN2010800376109A
Other languages
English (en)
Chinese (zh)
Inventor
J·里吉斯-索希尔
邓波良
T·A·赖利
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
Priority to CN201610080597.4A priority Critical patent/CN105503889B/zh
Publication of CN102573918A publication Critical patent/CN102573918A/zh
Pending legal-status Critical Current

Links

Images

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
    • 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
    • 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
    • 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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN2010800376109A 2009-07-21 2010-07-21 低聚物-阿片样激动剂轭合物 Pending CN102573918A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201610080597.4A CN105503889B (zh) 2009-07-21 2010-07-21 低聚物-阿片样激动剂轭合物

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201610080597.4A Division CN105503889B (zh) 2009-07-21 2010-07-21 低聚物-阿片样激动剂轭合物

Publications (1)

Publication Number Publication Date
CN102573918A true CN102573918A (zh) 2012-07-11

Family

ID=43499405

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2010800376109A Pending CN102573918A (zh) 2009-07-21 2010-07-21 低聚物-阿片样激动剂轭合物

Country Status (9)

Country Link
EP (2) EP2628489B1 (enExample)
JP (2) JP5837491B2 (enExample)
KR (1) KR101788886B1 (enExample)
CN (1) CN102573918A (enExample)
AU (1) AU2010276244B2 (enExample)
CA (1) CA2768392C (enExample)
IL (3) IL217634B (enExample)
MX (1) MX2012000980A (enExample)
WO (1) WO2011011543A1 (enExample)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104755481A (zh) * 2012-10-30 2015-07-01 尼克塔治疗公司 作为阿片激动剂的α-6-mPEG6-O-羟基可酮的固体盐形式以及其用途
CN107033154A (zh) * 2016-02-02 2017-08-11 苏州派格生物科技有限公司 阿片受体拮抗剂缀合物及其应用
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
WO2023197934A1 (zh) * 2022-04-11 2023-10-19 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

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8173666B2 (en) 2007-03-12 2012-05-08 Nektar Therapeutics Oligomer-opioid agonist conjugates
US10512644B2 (en) 2007-03-12 2019-12-24 Inheris Pharmaceuticals, Inc. Oligomer-opioid agonist conjugates
ES2562643T5 (es) 2010-09-30 2019-05-24 Astrazeneca Ab Conjugado de naloxol-peg cristalino
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
AU2012336030B2 (en) * 2011-11-07 2017-09-14 Nektar Therapeutics Compositions, dosage forms, and coadministration of an opioid agonist compound and an analgesic compound
ITRM20130223A1 (it) * 2013-04-15 2014-10-16 Rosario Nicoletti Derivati della codeina come inibitori della glucuronazione della morfina
CA3042642A1 (en) 2013-08-12 2015-02-19 Pharmaceutical Manufacturing Research Services, Inc. Extruded immediate release abuse deterrent pill
WO2015095391A1 (en) 2013-12-17 2015-06-25 Pharmaceutical Manufacturing Research Services, Inc. Extruded extended release abuse deterrent pill
US9492444B2 (en) 2013-12-17 2016-11-15 Pharmaceutical Manufacturing Research Services, Inc. Extruded extended release abuse deterrent pill
EP3169315B1 (en) 2014-07-17 2020-06-24 Pharmaceutical Manufacturing Research Services, Inc. Immediate release abuse deterrent liquid fill dosage form
WO2016064873A1 (en) 2014-10-20 2016-04-28 Pharmaceutical Manufacturing Research Services, Inc. Extended release abuse deterrent liquid fill dosage form
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
WO2019189188A1 (ja) * 2018-03-29 2019-10-03 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
CA3149152A1 (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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008112288A2 (en) * 2007-03-12 2008-09-18 Nektar Therapeutics Oligomer-opioid agonist conjugates

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US2806033A (en) 1955-08-03 1957-09-10 Lewenstein Morphine derivative
EP0832106A2 (en) * 1995-06-05 1998-04-01 Cortech, Inc. Compounds having bradykinin antagonistic activity and mu-opioid agonistic activity
US5672662A (en) 1995-07-07 1997-09-30 Shearwater Polymers, Inc. Poly(ethylene glycol) and related polymers monosubstituted with propionic or butanoic acids and functional derivatives thereof for biotechnical applications
US6835802B2 (en) 2001-06-04 2004-12-28 Nobex Corporation Methods of synthesizing substantially monodispersed mixtures of polymers having polyethylene glycol moieties
EP1782834A3 (en) * 2003-03-13 2007-08-01 Controlled Chemicals, Inc. Oxycodone conjugates with lower abuse potential and extended duration of action
DK1694363T3 (en) 2003-12-16 2014-03-24 Nektar Therapeutics Monodisperse PEGylated Naloxole Compositions
AU2009292631A1 (en) * 2008-09-16 2010-03-25 Nektar Therapeutics Pegylated opioids with low potential for abuse

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008112288A2 (en) * 2007-03-12 2008-09-18 Nektar Therapeutics Oligomer-opioid agonist conjugates

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104755481A (zh) * 2012-10-30 2015-07-01 尼克塔治疗公司 作为阿片激动剂的α-6-mPEG6-O-羟基可酮的固体盐形式以及其用途
CN110615796A (zh) * 2012-10-30 2019-12-27 尼克塔治疗公司 作为阿片激动剂的α-6-mPEG6-O-羟基可酮的固体盐形式以及其用途
CN107033154A (zh) * 2016-02-02 2017-08-11 苏州派格生物科技有限公司 阿片受体拮抗剂缀合物及其应用
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
US11311533B2 (en) 2016-02-02 2022-04-26 Shanghai Hanmai Bio-Pharma Co., Ltd. Opioid receptor antagonist conjugate and use thereof
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
WO2023197934A1 (zh) * 2022-04-11 2023-10-19 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

Also Published As

Publication number Publication date
EP2456469A1 (en) 2012-05-30
KR20120056828A (ko) 2012-06-04
IL263713A (en) 2019-01-31
MX2012000980A (es) 2012-06-12
JP2015180698A (ja) 2015-10-15
IL256822A (en) 2018-05-31
WO2011011543A1 (en) 2011-01-27
EP2628489B1 (en) 2017-03-01
AU2010276244A1 (en) 2012-03-15
IL217634B (en) 2018-01-31
CA2768392C (en) 2018-04-17
JP2013500256A (ja) 2013-01-07
KR101788886B1 (ko) 2017-10-20
AU2010276244B2 (en) 2015-08-13
JP5837491B2 (ja) 2015-12-24
IL256822B (en) 2018-12-31
EP2628489A1 (en) 2013-08-21
CA2768392A1 (en) 2011-01-27

Similar Documents

Publication Publication Date Title
CN102573918A (zh) 低聚物-阿片样激动剂轭合物
US10143690B2 (en) Oligomer-opioid agonist conjugates
CN101646464A (zh) 低聚物-阿片样激动剂偶联物
CN105503889B (zh) 低聚物-阿片样激动剂轭合物
US10512644B2 (en) Oligomer-opioid agonist conjugates
HK1138501A (en) Oligomer-opioid agonist conjugates

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C12 Rejection of a patent application after its publication
RJ01 Rejection of invention patent application after publication

Application publication date: 20120711