CN103237547B - 结晶纳络醇-peg缀合物 - Google Patents
结晶纳络醇-peg缀合物 Download PDFInfo
- Publication number
- CN103237547B CN103237547B CN201180057584.0A CN201180057584A CN103237547B CN 103237547 B CN103237547 B CN 103237547B CN 201180057584 A CN201180057584 A CN 201180057584A CN 103237547 B CN103237547 B CN 103237547B
- Authority
- CN
- China
- Prior art keywords
- naloxol
- mpeg7
- salt
- mpeg
- acid
- 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.)
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Classifications
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- 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)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (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 (2)
| Publication Number | Publication Date |
|---|---|
| CN103237547A CN103237547A (zh) | 2013-08-07 |
| CN103237547B true CN103237547B (zh) | 2015-10-07 |
Family
ID=45893441
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201180057584.0A Active CN103237547B (zh) | 2010-09-30 | 2011-09-29 | 结晶纳络醇-peg缀合物 |
Country Status (39)
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2819305T3 (es) | 2010-09-30 | 2021-04-15 | Astrazeneca Ab | Combinación de un conjugado de naloxol-peg y un agonista opioide |
| 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 |
| CA3104099A1 (en) * | 2015-03-10 | 2016-09-15 | 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 |
| 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050136031A1 (en) * | 2003-12-16 | 2005-06-23 | Bentley Michael D. | Chemically modified small molecules |
| WO2008057579A2 (en) * | 2006-11-07 | 2008-05-15 | Nektar Therapeutics Al, Corporation | Dosage forms and co-administration of an opioid agonist and an opioid antagonist |
| WO2009137086A1 (en) * | 2008-05-07 | 2009-11-12 | Nektar Therapeutics | Oral administration of peripherally-acting opioid antagonists |
Family Cites Families (28)
| 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 |
| EP1037649B1 (en) | 1997-12-17 | 2009-09-30 | 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 |
| KR100653153B1 (ko) | 1999-12-22 | 2006-12-01 | 넥타르 테라퓨틱스 에이엘, 코포레이션 | 수용성 중합체의 입체장애 유도체 |
| 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 |
| AU2002217981A1 (en) | 2000-11-30 | 2002-06-11 | Cornerstone Pharmaceuticals, Inc. | Water-soluble polymer conjugates of triazine derivatives |
| US20040082620A1 (en) | 2000-12-22 | 2004-04-29 | Craig Andrew Simon | 5'-4-'2-(n-methyl-n-(2-pyridyl)amino)ethoxy!benzyl!thiazolidine-2, 4-dione mesylate salt |
| MXPA03007392A (es) | 2001-02-20 | 2003-12-04 | Enzon Inc | Enlazantes polimericos ramificados terminalmente y conjugados polimericos que contienen los mismos. |
| 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 |
| US7056500B2 (en) | 2001-10-18 | 2006-06-06 | Nektar Therapeutics Al, Corporation | Polymer conjugates of opioid antagonists |
| AU2002342193B2 (en) | 2001-10-29 | 2006-10-26 | Nektar Therapeutics Al, Corporation | Polymer conjugates of protein kinase C inhibitors |
| 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 |
| PT2425824T (pt) * | 2002-04-05 | 2017-08-23 | Mundipharma Farmacêutica Lda | Preparação farmacêutica contendo oxicodona e naloxona |
| 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 |
| 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 |
| US8173666B2 (en) | 2007-03-12 | 2012-05-08 | Nektar Therapeutics | Oligomer-opioid agonist conjugates |
| JP5837491B2 (ja) † | 2009-07-21 | 2015-12-24 | ウェルズ ファーゴ バンク ナショナル アソシエイション | オリゴマー−オピオイドアゴニスト抱合体 |
| ES2819305T3 (es) | 2010-09-30 | 2021-04-15 | Astrazeneca Ab | Combinación de un conjugado de naloxol-peg y un agonista opioide |
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2011
- 2011-09-29 ES ES15188944T patent/ES2819305T3/es active Active
- 2011-09-29 PE PE2013000652A patent/PE20140636A1/es active IP Right Grant
- 2011-09-29 WO PCT/SE2011/051161 patent/WO2012044243A1/en not_active Ceased
- 2011-09-29 DK DK11829686.2T patent/DK2621496T4/en active
- 2011-09-29 HU HUE11829686A patent/HUE026726T2/en unknown
- 2011-09-29 JP JP2013531533A patent/JP6034789B2/ja active Active
- 2011-09-29 CU CUP2013000047A patent/CU24317B1/xx unknown
- 2011-09-29 AU AU2011307608A patent/AU2011307608B8/en active Active
- 2011-09-29 ES ES11829686T patent/ES2562643T5/es active Active
- 2011-09-29 BR BR112013007113-3A patent/BR112013007113B1/pt active IP Right Grant
- 2011-09-29 SI SI201130699T patent/SI2621496T2/sl unknown
- 2011-09-29 PH PH1/2013/500561A patent/PH12013500561A1/en unknown
- 2011-09-29 US US13/823,953 patent/US9012469B2/en active Active
- 2011-09-29 HR HRP20151420TT patent/HRP20151420T4/hr unknown
- 2011-09-29 MY MYPI2013700499A patent/MY173890A/en unknown
- 2011-09-29 ME MEP-2015-217A patent/ME02313B/me unknown
- 2011-09-29 PT PT118296862T patent/PT2621496E/pt unknown
- 2011-09-29 EA EA201300423A patent/EA023929B1/ru unknown
- 2011-09-29 CA CA2812649A patent/CA2812649C/en active Active
- 2011-09-29 SG SG2013017447A patent/SG188474A1/en unknown
- 2011-09-29 EP EP11829686.2A patent/EP2621496B2/en active Active
- 2011-09-29 RS RS20150876A patent/RS54488B8/sr unknown
- 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 MX MX2013003587A patent/MX2013003587A/es active IP Right Grant
- 2011-09-29 UA UAA201303320A patent/UA112847C2/uk unknown
- 2011-09-29 KR KR1020137008014A patent/KR101791724B1/ko active Active
- 2011-09-29 EP EP15188944.1A patent/EP2992903B8/en 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 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
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050136031A1 (en) * | 2003-12-16 | 2005-06-23 | Bentley Michael D. | Chemically modified small molecules |
| WO2008057579A2 (en) * | 2006-11-07 | 2008-05-15 | Nektar Therapeutics Al, Corporation | Dosage forms and co-administration of an opioid agonist and an opioid antagonist |
| WO2009137086A1 (en) * | 2008-05-07 | 2009-11-12 | Nektar Therapeutics | Oral administration of peripherally-acting opioid antagonists |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| CB03 | Change of inventor or designer information |
Inventor after: B.L. Aslund Inventor after: D. Lechuga Ballesteros Inventor after: C-J. Orell Inventor after: M.H. Polin Inventor after: T. Sebhatu Inventor after: Ymen Bo Ingvar Inventor after: Healy Eric Thomas Inventor after: D.R. Jansen Inventor after: Jonaitis David Thomas Inventor after: S. Palente Inventor before: B.L. Aslund Inventor before: C-J. Orell Inventor before: M.H. Polin Inventor before: T. Sebhatu Inventor before: Ymen Bo Ingvar Inventor before: Healy Eric Thomas Inventor before: D.R. Jansen Inventor before: Jonaitis David Thomas Inventor before: S. Palente |
|
| CB03 | Change of inventor or designer information |