KR101791724B1 - 결정질 날록솔-ｐｅｇ 접합체 - Google Patents

결정질 날록솔-ｐｅｇ 접합체 Download PDF

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Publication number
KR101791724B1
KR101791724B1 KR1020137008014A KR20137008014A KR101791724B1 KR 101791724 B1 KR101791724 B1 KR 101791724B1 KR 1020137008014 A KR1020137008014 A KR 1020137008014A KR 20137008014 A KR20137008014 A KR 20137008014A KR 101791724 B1 KR101791724 B1 KR 101791724B1
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mpeg
naloxol
salt
solid
crystalline
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Korean (ko)
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KR101791724B9 (ko
KR20130135844A (ko
Inventor
벤트 레오나르드 오스룬드
카를-요한 아우렐
마틴 한스 볼린
테스파이 세파투
보 잉바 위멘
에릭 토마스 힐리
데이비드 리차드 젠슨
데이비드 토마스 조나이티스
스테판 패런트
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아스트라제네카 아베
넥타르 테라퓨틱스
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Application filed by 아스트라제네카 아베, 넥타르 테라퓨틱스 filed Critical 아스트라제네카 아베
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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

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  • 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)
KR1020137008014A 2010-09-30 2011-09-29 결정질 날록솔-ｐｅｇ 접합체 Active KR101791724B1 (ko)

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
KR20130135844A KR20130135844A (ko) 2013-12-11
KR101791724B1 true KR101791724B1 (ko) 2017-10-30
KR101791724B9 KR101791724B9 (ko) 2022-06-16

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US (2) US9012469B2 (enExample)
EP (2) EP2621496B2 (enExample)
JP (1) JP6034789B2 (enExample)
KR (1) KR101791724B1 (enExample)
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MX (1) MX2013003587A (enExample)
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TW (1) TWI518088B (enExample)
UA (1) UA112847C2 (enExample)
UY (1) UY33643A (enExample)
WO (1) WO2012044243A1 (enExample)

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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

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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
WO2012044243A1 (en) 2010-09-30 2012-04-05 Astrazeneca Ab Crystalline naloxol-peg conjugate

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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
WO2012044243A1 (en) 2010-09-30 2012-04-05 Astrazeneca Ab Crystalline naloxol-peg conjugate

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ES2562643T3 (es) 2016-03-07
MX2013003587A (es) 2013-05-31
AU2011307608B2 (en) 2015-04-09
CU20130047A7 (es) 2013-08-29
GT201300084A (es) 2015-01-16
SMT201600004B (it) 2016-02-25
AU2011307608A1 (en) 2013-05-02
AU2011307608A8 (en) 2015-08-27
PH12013500561A1 (en) 2013-06-10
ES2819305T3 (es) 2021-04-15
MY173890A (en) 2020-02-26
TW201307356A (zh) 2013-02-16
IL225308A0 (en) 2013-06-27
AU2011307608B8 (en) 2015-08-27
JP6034789B2 (ja) 2016-11-30
CL2013000866A1 (es) 2013-08-30
KR101791724B9 (ko) 2022-06-16
EP2992903B1 (en) 2020-07-15
BR112013007113B1 (pt) 2020-09-24
CA2812649A1 (en) 2012-04-05
UY33643A (es) 2012-04-30
RS54488B2 (sr) 2019-03-29
US9149539B1 (en) 2015-10-06
ES2562643T5 (es) 2019-05-24
EP2992903A1 (en) 2016-03-09
EA023929B1 (ru) 2016-07-29
ME02313B (me) 2016-06-20
US20150283257A1 (en) 2015-10-08
HK1187248A1 (zh) 2014-04-04
EP2621496B2 (en) 2018-12-12
JP2013538849A (ja) 2013-10-17
EA201300423A1 (ru) 2013-09-30
NI201300034A (es) 2014-01-23
EP2621496A4 (en) 2014-09-24
AR083268A1 (es) 2013-02-13
KR20130135844A (ko) 2013-12-11
CN103237547B (zh) 2015-10-07
EP2992903B8 (en) 2022-06-08
HRP20151420T1 (hr) 2016-01-29
US9012469B2 (en) 2015-04-21
ES2562643T8 (es) 2022-07-12
US20150038524A1 (en) 2015-02-05
CU24317B1 (es) 2018-02-08
PE20140636A1 (es) 2014-06-18
CR20130146A (es) 2013-05-15
DK2621496T3 (en) 2016-01-18
EP2621496B1 (en) 2015-12-16
CN103237547A (zh) 2013-08-07
SG188474A1 (en) 2013-05-31
NZ609874A (en) 2014-10-31
TWI518088B (zh) 2016-01-21
SI2621496T1 (sl) 2016-02-29
WO2012044243A1 (en) 2012-04-05
SA111320808B1 (ar) 2014-12-15
CO6700851A2 (es) 2013-06-28
PL2621496T5 (pl) 2019-05-31
EP2621496A1 (en) 2013-08-07
BR112013007113A2 (pt) 2017-07-25
SI2621496T2 (sl) 2019-04-30
PL2621496T3 (pl) 2016-05-31
PT2621496E (pt) 2016-02-01
DK2621496T4 (en) 2019-03-18
RS54488B1 (sr) 2016-06-30
RS54488B8 (sr) 2022-11-30
ES2819305T8 (es) 2022-05-26
ECSP13012531A (es) 2013-06-28
HUE026726T2 (en) 2016-07-28
CA2812649C (en) 2016-03-01
HRP20151420T4 (hr) 2019-04-05
UA112847C2 (uk) 2016-11-10

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