JP2013538849A5 - - Google Patents
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- Publication number
- JP2013538849A5 JP2013538849A5 JP2013531533A JP2013531533A JP2013538849A5 JP 2013538849 A5 JP2013538849 A5 JP 2013538849A5 JP 2013531533 A JP2013531533 A JP 2013531533A JP 2013531533 A JP2013531533 A JP 2013531533A JP 2013538849 A5 JP2013538849 A5 JP 2013538849A5
- Authority
- JP
- Japan
- Prior art keywords
- naloxol
- polyethylene glycol
- mpeg
- glycol conjugate
- oxalate
- 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.)
- Granted
Links
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical class OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims 23
- 239000002202 Polyethylene glycol Substances 0.000 claims 12
- 229920001223 polyethylene glycol Polymers 0.000 claims 12
- 229920001427 mPEG Polymers 0.000 claims 6
- 239000013078 crystal Substances 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 238000000034 method Methods 0.000 claims 4
- 235000006408 oxalic acid Nutrition 0.000 claims 4
- 238000000634 powder X-ray diffraction Methods 0.000 claims 4
- 230000005855 radiation Effects 0.000 claims 4
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- 239000012458 free base Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000002002 slurry Substances 0.000 claims 2
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 1
- 102000016397 Methyltransferase Human genes 0.000 claims 1
- 108060004795 Methyltransferase Proteins 0.000 claims 1
- 229910019142 PO4 Inorganic materials 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- AQEFLFZSWDEAIP-UHFFFAOYSA-N di-tert-butyl ether Chemical compound CC(C)(C)OC(C)(C)C AQEFLFZSWDEAIP-UHFFFAOYSA-N 0.000 claims 1
- 238000000113 differential scanning calorimetry Methods 0.000 claims 1
- 230000001747 exhibiting effect Effects 0.000 claims 1
- 150000003891 oxalate salts Chemical class 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 1
- 239000010452 phosphate Substances 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2013538849A JP2013538849A (ja) | 2013-10-17 |
| JP2013538849A5 true JP2013538849A5 (enExample) | 2016-02-18 |
| JP6034789B2 JP6034789B2 (ja) | 2016-11-30 |
Family
ID=45893441
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013531533A Active JP6034789B2 (ja) | 2010-09-30 | 2011-09-29 | 結晶性ナロキソール−ｐｅｇ接合体 |
Country Status (39)
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA023929B1 (ru) | 2010-09-30 | 2016-07-29 | Астразенека Аб | Кристаллический конъюгат налоксол-peg |
| WO2014070745A1 (en) * | 2012-10-30 | 2014-05-08 | Nektar Therapeutics | Solid salt form of alpha-6-mpeg6-o-hydroxycodone as opioid agonists and uses thereof |
| CA2977732C (en) * | 2015-03-10 | 2021-02-23 | Rhodes Technologies | Acetate salt of buprenorphine and methods for preparing buprenorphine |
| 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 |
| WO2018096464A1 (en) * | 2016-11-23 | 2018-05-31 | Aurobindo Pharma Limited | 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 |
| KR20230005928A (ko) * | 2020-05-04 | 2023-01-10 | 오츠카 세이야쿠 가부시키가이샤 | Iap 길항제 화합물 및 중간체 및 이를 합성하는 방법 |
| 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 |
| JPH08504189A (ja) * | 1992-09-21 | 1996-05-07 | キン、ボーイ | 低／非たんでき性オピオイド鎮痛剤の確認及び使用方法 |
| 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 |
| DE60026073T2 (de) | 1999-12-22 | 2006-09-28 | Nektar Therapeutics Al, Corp., Huntsville | Sterisch gehinderte derivate von wasserlöslichen polymeren |
| US6413507B1 (en) | 1999-12-23 | 2002-07-02 | Shearwater Corporation | Hydrolytically degradable carbamate derivatives of poly (ethylene glycol) |
| AU2001257577A1 (en) | 2000-02-28 | 2001-09-03 | 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 |
| AU2002217981A1 (en) | 2000-11-30 | 2002-06-11 | Cornerstone Pharmaceuticals, Inc. | Water-soluble polymer conjugates of triazine derivatives |
| ATE337313T1 (de) | 2000-12-22 | 2006-09-15 | Smithkline Beecham Plc | 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 |
| EP1436012B1 (en) | 2001-10-18 | 2017-12-20 | Nektar Therapeutics | Polymer conjugates of opioid antagonists |
| KR20050040832A (ko) | 2001-10-29 | 2005-05-03 | 넥타르 테라퓨틱스 에이엘, 코포레이션 | 단백질 키나아제 ｃ 억제제의 중합체 공액 |
| JP2005507934A (ja) | 2001-10-30 | 2005-03-24 | 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 | レチノイン酸の水溶性ポリマー結合体 |
| DE60325567D1 (de) * | 2002-04-05 | 2009-02-12 | Euro Celtique Sa | Matrix für die modifizierte freigabe von aktiven substanzen |
| GB0317815D0 (en) | 2003-07-30 | 2003-09-03 | Amersham Health As | Imaging agents |
| CA2547140A1 (en) | 2003-11-24 | 2005-06-09 | Neose Technologies, Inc. | Glycopegylated erythropoietin |
| US20060182692A1 (en) | 2003-12-16 | 2006-08-17 | Fishburn C S | Chemically modified small molecules |
| EP2905033B1 (en) | 2003-12-16 | 2020-09-02 | Nektar Therapeutics | Monodisperse PEGylated naloxol compositions |
| US8320574B2 (en) * | 2006-04-20 | 2012-11-27 | Hewlett-Packard Development Company, L.P. | Methods and systems for reducing acoustic echoes in communication systems |
| WO2007124114A2 (en) | 2006-04-21 | 2007-11-01 | Nektar Therapeutics Al, Corporation | Stereoselective reduction of a morphinone |
| US20100284960A1 (en) * | 2006-11-07 | 2010-11-11 | Nektar Therapeutics Al, Corporation | Dosage Forms and Co-Administration of Opioid Agonist and Opioid Antagonist |
| US8173666B2 (en) | 2007-03-12 | 2012-05-08 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| WO2009137086A1 (en) | 2008-05-07 | 2009-11-12 | Nektar Therapeutics | Oral administration of peripherally-acting opioid antagonists |
| AU2010276244B2 (en) | 2009-07-21 | 2015-08-13 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| EA023929B1 (ru) | 2010-09-30 | 2016-07-29 | Астразенека Аб | Кристаллический конъюгат налоксол-peg |
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2011
- 2011-09-29 EA EA201300423A patent/EA023929B1/ru unknown
- 2011-09-29 ES ES11829686T patent/ES2562643T5/es active Active
- 2011-09-29 MX MX2013003587A patent/MX2013003587A/es active IP Right Grant
- 2011-09-29 ES ES15188944T patent/ES2819305T3/es active Active
- 2011-09-29 SG SG2013017447A patent/SG188474A1/en unknown
- 2011-09-29 PT PT118296862T patent/PT2621496E/pt unknown
- 2011-09-29 ME MEP-2015-217A patent/ME02313B/me unknown
- 2011-09-29 BR BR112013007113-3A patent/BR112013007113B1/pt active IP Right Grant
- 2011-09-29 KR KR1020137008014A patent/KR101791724B1/ko active Active
- 2011-09-29 DK DK11829686.2T patent/DK2621496T4/en active
- 2011-09-29 UA UAA201303320A patent/UA112847C2/uk unknown
- 2011-09-29 MY MYPI2013700499A patent/MY173890A/en unknown
- 2011-09-29 CA CA2812649A patent/CA2812649C/en active Active
- 2011-09-29 US US13/823,953 patent/US9012469B2/en active Active
- 2011-09-29 EP EP15188944.1A patent/EP2992903B8/en active Active
- 2011-09-29 RS RS20150876A patent/RS54488B8/sr unknown
- 2011-09-29 HR HRP20151420TT patent/HRP20151420T4/hr unknown
- 2011-09-29 PE PE2013000652A patent/PE20140636A1/es active IP Right Grant
- 2011-09-29 CU CUP2013000047A patent/CU24317B1/xx unknown
- 2011-09-29 HU HUE11829686A patent/HUE026726T2/en unknown
- 2011-09-29 PH PH1/2013/500561A patent/PH12013500561A1/en unknown
- 2011-09-29 JP JP2013531533A patent/JP6034789B2/ja active Active
- 2011-09-29 AU AU2011307608A patent/AU2011307608B8/en active Active
- 2011-09-29 SI SI201130699T patent/SI2621496T2/sl unknown
- 2011-09-29 WO PCT/SE2011/051161 patent/WO2012044243A1/en not_active Ceased
- 2011-09-29 CN CN201180057584.0A patent/CN103237547B/zh active Active
- 2011-09-29 NZ NZ609874A patent/NZ609874A/en unknown
- 2011-09-29 PL PL11829686T patent/PL2621496T5/pl unknown
- 2011-09-29 EP EP11829686.2A patent/EP2621496B2/en active Active
- 2011-09-30 UY UY0001033643A patent/UY33643A/es not_active Application Discontinuation
- 2011-09-30 AR ARP110103631A patent/AR083268A1/es not_active Application Discontinuation
- 2011-09-30 TW TW100135672A patent/TWI518088B/zh active
- 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 NI NI201300034A patent/NI201300034A/es unknown
- 2013-04-01 CR CR20130146A patent/CR20130146A/es unknown
- 2013-04-01 GT GT201300084A patent/GT201300084A/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