AU2011307608B8 - Crystalline naloxol-PEG conjugate - Google Patents
Crystalline naloxol-PEG conjugate Download PDFInfo
- Publication number
- AU2011307608B8 AU2011307608B8 AU2011307608A AU2011307608A AU2011307608B8 AU 2011307608 B8 AU2011307608 B8 AU 2011307608B8 AU 2011307608 A AU2011307608 A AU 2011307608A AU 2011307608 A AU2011307608 A AU 2011307608A AU 2011307608 B8 AU2011307608 B8 AU 2011307608B8
- Authority
- AU
- Australia
- Prior art keywords
- naloxol
- mpeg
- salt
- oxalate salt
- polyethylene glycol
- 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.)
- Active
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
- C07C55/02—Dicarboxylic acids
- C07C55/06—Oxalic acid
- C07C55/07—Salts 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
- A61K47/56—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
-
- 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
- A61P39/00—General protective or antinoxious agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/41—Preparation of salts of carboxylic acids
-
- 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:
- C07D489/02—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 oxygen atoms attached in positions 3 and 6, e.g. morphine, morphinone
- C07D489/04—Salts; Organic complexes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pain & Pain Management (AREA)
- Toxicology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Emergency Medicine (AREA)
- Compression Or Coding Systems Of Tv Signals (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38850110P | 2010-09-30 | 2010-09-30 | |
| US61/388,501 | 2010-09-30 | ||
| PCT/SE2011/051161 WO2012044243A1 (en) | 2010-09-30 | 2011-09-29 | Crystalline naloxol-peg conjugate |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| AU2011307608A1 AU2011307608A1 (en) | 2013-05-02 |
| AU2011307608B2 AU2011307608B2 (en) | 2015-04-09 |
| AU2011307608A8 AU2011307608A8 (en) | 2015-08-27 |
| AU2011307608B8 true AU2011307608B8 (en) | 2015-08-27 |
Family
ID=45893441
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2011307608A Active AU2011307608B8 (en) | 2010-09-30 | 2011-09-29 | Crystalline naloxol-PEG conjugate |
Country Status (39)
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2621496T2 (sl) | 2010-09-30 | 2019-04-30 | Astrazeneca Ab | Kristalinični konjugat naloksol-PEG |
| CA2886276A1 (en) * | 2012-10-30 | 2014-05-08 | Nektar Therapeutics | Solid salt form of alpha-6-mpeg6-o-hydroxycodone as opioid agonists and uses thereof |
| CN107660207B (zh) * | 2015-03-10 | 2020-09-29 | 罗德科技公司 | 丁丙诺啡乙酸盐及用于制备丁丙诺啡的方法 |
| 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 |
| CN107033155B (zh) * | 2016-02-04 | 2019-04-26 | 国药集团国瑞药业有限公司 | 一种吗啡酮类化合物的立体选择性还原方法 |
| EP3228307A1 (en) | 2016-04-05 | 2017-10-11 | Sandoz Ag | Solid dispersion comprising opioid antagonists |
| CN107303392A (zh) * | 2016-04-19 | 2017-10-31 | 石家庄蒎格医药科技有限公司 | 一种聚乙二醇-纳洛酮组合物及应用 |
| US11077103B2 (en) * | 2016-11-23 | 2021-08-03 | Aurobindo Pharma Ltd. | Naloxegol oxalate and solid dispersion thereof |
| US11373198B2 (en) * | 2016-12-02 | 2022-06-28 | Honda Motor Co., Ltd. | Evaluation device, evaluation method, and evaluation program |
| WO2019058387A1 (en) * | 2017-09-19 | 2019-03-28 | Msn Laboratories Private Limited, R&D Center | IMPROVED PROCESS FOR THE PREPARATION OF (5Α, 6Α) -17-ALLYL-6- (2,5,8,11,14,17,20-HEPTAOXADOCOSAN-22-YLOXY) -4,5-EPOXYMORPHINANE-3,14-DIOL AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS |
| JP7690493B2 (ja) * | 2020-05-04 | 2025-06-10 | 大鵬薬品工業株式会社 | Ｉａｐアンタゴニスト化合物及びその中間体、並びにそれを合成する方法 |
| CN114137133B (zh) * | 2021-12-03 | 2023-06-09 | 北京尚修堂医药科技有限公司 | 一种纳洛醇-peg衍生物有关物质的检测方法 |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2507136A (en) † | 1949-02-19 | 1950-05-09 | New York Quinine And Chemical | Alkaloid purification |
| EP0668764A1 (en) * | 1992-09-21 | 1995-08-30 | QIN, Bo-yi | Methods for identifying and using low/non-addictive opioid analgesics |
| WO1999030727A1 (en) | 1997-12-17 | 1999-06-24 | Enzon, Inc. | Polymeric prodrugs of amino- and hydroxyl-containing bioactive agents |
| US6624142B2 (en) | 1997-12-30 | 2003-09-23 | Enzon, Inc. | Trimethyl lock based tetrapartate prodrugs |
| EP0995757A3 (en) | 1998-08-26 | 2002-05-22 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | Bivalent inhibitors of the proteasome |
| US6380405B1 (en) | 1999-09-13 | 2002-04-30 | Nobex Corporation | Taxane prodrugs |
| CA2394980C (en) | 1999-12-22 | 2008-05-13 | Shearwater Corporation | Sterically hindered derivatives of water soluble polymers |
| US6413507B1 (en) | 1999-12-23 | 2002-07-02 | Shearwater Corporation | Hydrolytically degradable carbamate derivatives of poly (ethylene glycol) |
| WO2001062299A2 (en) | 2000-02-28 | 2001-08-30 | Shearwater Corporation | Water-soluble polymer conjugates of artelinic acid |
| US7829074B2 (en) | 2001-10-18 | 2010-11-09 | Nektar Therapeutics | Hydroxypatite-targeting poly(ethylene glycol) and related polymers |
| US20020182172A1 (en) | 2000-11-30 | 2002-12-05 | Shearwater Corporation | Water-soluble polymer conjugates of triazine derivatives |
| DE60122580T2 (de) | 2000-12-22 | 2007-08-30 | Smithkline Beecham P.L.C., Brentford | 5-4'-2'-(n-methyl-n-(2-pyridyl)amino) ethoxy!benzyl!thiazolidin-2,4-dion mesylatsalz |
| EP1362053B1 (en) | 2001-02-20 | 2007-11-14 | Enzon, Inc. | Terminally-branched polymeric linkers and polymeric conjugates containing the same |
| US6828305B2 (en) | 2001-06-04 | 2004-12-07 | Nobex Corporation | Mixtures of growth hormone drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same |
| US6713452B2 (en) | 2001-06-04 | 2004-03-30 | Nobex Corporation | Mixtures of calcitonin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same |
| US6756354B2 (en) | 2001-09-05 | 2004-06-29 | Deanna Jean Nelson | Therapeutic compositions containing oligo (ethylene glycol)-terminated 1,2-dithiolanes and their conjugates |
| US7056500B2 (en) | 2001-10-18 | 2006-06-06 | Nektar Therapeutics Al, Corporation | Polymer conjugates of opioid antagonists |
| KR20050040832A (ko) | 2001-10-29 | 2005-05-03 | 넥타르 테라퓨틱스 에이엘, 코포레이션 | 단백질 키나아제 ｃ 억제제의 중합체 공액 |
| DE60219677T2 (de) | 2001-10-30 | 2008-05-15 | Nektar Therapeutics Al, Corp., Huntsville | Wasserlösliche polymerkonjugate von retinoesäure |
| LT2425821T (lt) * | 2002-04-05 | 2017-07-25 | Euro-Celtique S.A. | Farmacinis preparatas, turintis oksikodono ir naloksono |
| GB0317815D0 (en) | 2003-07-30 | 2003-09-03 | Amersham Health As | Imaging agents |
| NZ547168A (en) | 2003-11-24 | 2010-05-28 | Biogenerix Ag | Glycopegylated erythropoietin |
| US20060182692A1 (en) | 2003-12-16 | 2006-08-17 | Fishburn C S | Chemically modified small molecules |
| CN1925875A (zh) | 2003-12-16 | 2007-03-07 | 尼克塔治疗亚拉巴马公司 | 化学改性的小分子 |
| US8320574B2 (en) * | 2006-04-20 | 2012-11-27 | Hewlett-Packard Development Company, L.P. | Methods and systems for reducing acoustic echoes in communication systems |
| ES2629766T3 (es) | 2006-04-21 | 2017-08-14 | Nektar Therapeutics | Reducción estereoselectiva de una morfinona |
| JP2010509227A (ja) * | 2006-11-07 | 2010-03-25 | ネクター セラピューティックス エイエル，コーポレイション | オピオイド作動薬およびオピオイド拮抗薬の用量形態および同時投与 |
| US8173666B2 (en) | 2007-03-12 | 2012-05-08 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| CN102014907A (zh) * | 2008-05-07 | 2011-04-13 | 尼克塔治疗公司 | 外周作用阿片拮抗剂的口服给药 |
| MX2012000980A (es) † | 2009-07-21 | 2012-06-12 | Nektar Therapeutics | Conjugados de agonistas de oligómeros-opioides. |
| SI2621496T2 (sl) | 2010-09-30 | 2019-04-30 | Astrazeneca Ab | Kristalinični konjugat naloksol-PEG |
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2011
- 2011-09-29 SI SI201130699T patent/SI2621496T2/sl unknown
- 2011-09-29 CN CN201180057584.0A patent/CN103237547B/zh active Active
- 2011-09-29 ES ES15188944T patent/ES2819305T3/es active Active
- 2011-09-29 MX MX2013003587A patent/MX2013003587A/es active IP Right Grant
- 2011-09-29 EP EP15188944.1A patent/EP2992903B8/en active Active
- 2011-09-29 PT PT118296862T patent/PT2621496E/pt unknown
- 2011-09-29 KR KR1020137008014A patent/KR101791724B1/ko active Active
- 2011-09-29 JP JP2013531533A patent/JP6034789B2/ja active Active
- 2011-09-29 US US13/823,953 patent/US9012469B2/en active Active
- 2011-09-29 PL PL11829686T patent/PL2621496T5/pl unknown
- 2011-09-29 PE PE2013000652A patent/PE20140636A1/es active IP Right Grant
- 2011-09-29 SG SG2013017447A patent/SG188474A1/en unknown
- 2011-09-29 NZ NZ609874A patent/NZ609874A/en unknown
- 2011-09-29 HR HRP20151420TT patent/HRP20151420T4/hr unknown
- 2011-09-29 AU AU2011307608A patent/AU2011307608B8/en active Active
- 2011-09-29 ES ES11829686T patent/ES2562643T5/es active Active
- 2011-09-29 PH PH1/2013/500561A patent/PH12013500561A1/en unknown
- 2011-09-29 CA CA2812649A patent/CA2812649C/en active Active
- 2011-09-29 CU CUP2013000047A patent/CU24317B1/xx unknown
- 2011-09-29 HU HUE11829686A patent/HUE026726T2/en unknown
- 2011-09-29 ME MEP-2015-217A patent/ME02313B/me unknown
- 2011-09-29 WO PCT/SE2011/051161 patent/WO2012044243A1/en not_active Ceased
- 2011-09-29 BR BR112013007113-3A patent/BR112013007113B1/pt active IP Right Grant
- 2011-09-29 EA EA201300423A patent/EA023929B1/ru unknown
- 2011-09-29 EP EP11829686.2A patent/EP2621496B2/en active Active
- 2011-09-29 MY MYPI2013700499A patent/MY173890A/en unknown
- 2011-09-29 DK DK11829686.2T patent/DK2621496T4/en active
- 2011-09-29 UA UAA201303320A patent/UA112847C2/uk unknown
- 2011-09-29 RS RS20150876A patent/RS54488B8/sr unknown
- 2011-09-30 TW TW100135672A patent/TWI518088B/zh active
- 2011-09-30 AR ARP110103631A patent/AR083268A1/es not_active Application Discontinuation
- 2011-09-30 UY UY0001033643A patent/UY33643A/es active IP Right Grant
- 2011-10-01 SA SA111320808A patent/SA111320808B1/ar unknown
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2013
- 2013-03-18 IL IL225308A patent/IL225308A0/en active IP Right Grant
- 2013-03-27 EC ECSP13012531 patent/ECSP13012531A/es unknown
- 2013-03-28 CL CL2013000866A patent/CL2013000866A1/es unknown
- 2013-04-01 GT GT201300084A patent/GT201300084A/es unknown
- 2013-04-01 CR CR20130146A patent/CR20130146A/es unknown
- 2013-04-01 NI NI201300034A patent/NI201300034A/es unknown
- 2013-04-08 CO CO13090985A patent/CO6700851A2/es unknown
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2015
- 2015-03-11 US US14/645,347 patent/US9149539B1/en active Active
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2016
- 2016-01-05 SM SM201600004T patent/SMT201600004B/it unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) | ||
| TH | Corrigenda |
Free format text: IN VOL 27 , NO 16 , PAGE(S) 2355 UNDER THE HEADING PCT APPLICATIONS THAT HAVE ENTERED THE NATIONAL PHASE - NAME INDEX UNDER THE NAME ASTRAZENECA AB, APPLICATION NO. 2011307608, UNDER INID (71) ADD COAPPLICANT NEKTAR THERAPEUTICS Free format text: IN VOL 29 , NO 13 , PAGE(S) 2034 UNDER THE HEADING APPLICATIONS ACCEPTED - NAME INDEX UNDER THE NAME ASTRAZENECA AB, APPLICATION NO. 2011307608, UNDER INID (71) ADD CO-APPLICANT NEKTAR THERAPEUTICS |
|
| DA2 | Applications for amendment section 104 |
Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ ASLUND, BENGT LEONARD; AURELL, CARL-JOHAN; BOHLIN, MARTIN HANS; SEBHATU, TESFAI; YMEN, BO INGVAR; HEALY, ERIC THOMAS; JENSEN, DAVID RICHARD; JONAITIS, DAVID THOMAS; PARENT, STEPHAN AND LECHUGA-BALLESTEROS, DAVID |
|
| DA3 | Amendments made section 104 |
Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ ASLUND, BENGT LEONARD; AURELL, CARL-JOHAN; BOHLIN, MARTIN HANS; SEBHATU, TESFAI; YMEN, BO INGVAR; HEALY, ERIC THOMAS; JENSEN, DAVID RICHARD; JONAITIS, DAVID THOMAS; PARENT, STEPHAN AND LECHUGA-BALLESTEROS, DAVID |
|
| PC | Assignment registered |
Owner name: NEKTAR THERAPEUTICS Free format text: FORMER OWNER(S): NEKTAR THERAPEUTICS; ASTRAZENECA AB Owner name: GRUENENTHAL GMBH Free format text: FORMER OWNER(S): NEKTAR THERAPEUTICS; ASTRAZENECA AB |