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 (https=) | 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 |
|---|---|---|---|---|
| AU2011307608B8 (en) | 2010-09-30 | 2015-08-27 | Grünenthal GmbH | Crystalline naloxol-PEG conjugate |
| LT2914599T (lt) * | 2012-10-30 | 2018-02-12 | Nektar Therapeutics | Alfa-6-mpeg6-hidroksikodono, kaip opioidų agonistų, kieta druskos forma ir jos panaudojimas |
| 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 |
| US20230183234A1 (en) * | 2020-05-04 | 2023-06-15 | Otsuka Pharmaceutical Co., Ltd. | Iap antagonist compounds and intermediates and methods for synthesizing the same |
| 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 |
| WO1994006426A1 (en) * | 1992-09-21 | 1994-03-31 | 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 |
| AU781839B2 (en) | 1999-12-22 | 2005-06-16 | Nektar Therapeutics | 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) |
| 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 |
| EP1355671A2 (en) | 2000-11-30 | 2003-10-29 | Nektar Therapeutics Al, Corporation | Water-soluble polymer conjugates of triazine derivatives |
| EP1349855B1 (en) | 2000-12-22 | 2006-08-23 | Smithkline Beecham Plc | 5-'4-'2-(n-methyl-n- (2-pyridyl)amino)ethoxy]benzyl]thiazolidine-2, 4-dione mesylate salt |
| AU2002251988A1 (en) | 2001-02-20 | 2002-09-04 | Enzon, Inc. | Terminally-branched polymeric linkers and polymeric conjugates containing the 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 |
| 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 |
| US6756354B2 (en) | 2001-09-05 | 2004-06-29 | Deanna Jean Nelson | Therapeutic compositions containing oligo (ethylene glycol)-terminated 1,2-dithiolanes and their conjugates |
| ES2654819T3 (es) | 2001-10-18 | 2018-02-15 | Nektar Therapeutics | Conjugados poliméricos de antagonistas de opioides |
| WO2003037384A2 (en) | 2001-10-29 | 2003-05-08 | Nektar Therapeutics Al, Corporation | Polymer conjugates of protein kinase c inhibitors |
| KR20050042013A (ko) | 2001-10-30 | 2005-05-04 | 넥타르 테라퓨틱스 에이엘, 코포레이션 | 레티노산의 수용성 중합체 콘쥬게이트 |
| HUE032656T2 (en) * | 2002-04-05 | 2017-10-30 | Euro Celtique Sa | Pharmaceutical composition containing oxicodone and naloxone |
| GB0317815D0 (en) | 2003-07-30 | 2003-09-03 | Amersham Health As | Imaging agents |
| ES2445948T3 (es) | 2003-11-24 | 2014-03-06 | Ratiopharm Gmbh | Eritropoyetina glicopegilada |
| 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 |
| KR101421747B1 (ko) | 2006-04-21 | 2014-07-30 | 넥타르 테라퓨틱스 | 모르피논의 입체선택적 환원 |
| 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 |
| MX2010011727A (es) * | 2008-05-07 | 2010-11-30 | Nektar Therapeutics | Administracion oral de antagonistas opioides que actuan perifericamente. |
| EP2628489B1 (en) † | 2009-07-21 | 2017-03-01 | Nektar Therapeutics | PEG oligomer-fentanyl conjugates |
| AU2011307608B8 (en) | 2010-09-30 | 2015-08-27 | Grünenthal GmbH | Crystalline naloxol-PEG conjugate |
-
2011
- 2011-09-29 AU AU2011307608A patent/AU2011307608B8/en active Active
- 2011-09-29 WO PCT/SE2011/051161 patent/WO2012044243A1/en not_active Ceased
- 2011-09-29 SI SI201130699T patent/SI2621496T2/sl unknown
- 2011-09-29 EP EP15188944.1A patent/EP2992903B8/en active Active
- 2011-09-29 UA UAA201303320A patent/UA112847C2/uk unknown
- 2011-09-29 RS RS20150876A patent/RS54488B8/sr unknown
- 2011-09-29 MY MYPI2013700499A patent/MY173890A/en unknown
- 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 US US13/823,953 patent/US9012469B2/en active Active
- 2011-09-29 SG SG2013017447A patent/SG188474A1/en unknown
- 2011-09-29 ES ES11829686T patent/ES2562643T5/es active Active
- 2011-09-29 PH PH1/2013/500561A patent/PH12013500561A1/en unknown
- 2011-09-29 JP JP2013531533A patent/JP6034789B2/ja active Active
- 2011-09-29 DK DK11829686.2T patent/DK2621496T4/en active
- 2011-09-29 EP EP11829686.2A patent/EP2621496B2/en active Active
- 2011-09-29 BR BR112013007113-3A patent/BR112013007113B1/pt active IP Right Grant
- 2011-09-29 CU CUP2013000047A patent/CU24317B1/xx unknown
- 2011-09-29 CN CN201180057584.0A patent/CN103237547B/zh active Active
- 2011-09-29 HR HRP20151420TT patent/HRP20151420T4/hr unknown
- 2011-09-29 PL PL11829686T patent/PL2621496T5/pl unknown
- 2011-09-29 PT PT118296862T patent/PT2621496E/pt unknown
- 2011-09-29 PE PE2013000652A patent/PE20140636A1/es active IP Right Grant
- 2011-09-29 CA CA2812649A patent/CA2812649C/en active Active
- 2011-09-29 EA EA201300423A patent/EA023929B1/ru unknown
- 2011-09-29 NZ NZ609874A patent/NZ609874A/en unknown
- 2011-09-29 ME MEP-2015-217A patent/ME02313B/me unknown
- 2011-09-29 HU HUE11829686A patent/HUE026726T2/en unknown
- 2011-09-29 KR KR1020137008014A patent/KR101791724B1/ko active Active
- 2011-09-30 AR ARP110103631A patent/AR083268A1/es not_active Application Discontinuation
- 2011-09-30 UY UY0001033643A patent/UY33643A/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
-
2016
- 2016-01-05 SM SM201600004T patent/SMT201600004B/it unknown
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