KR101975843B1 - 리포좀 나노입자에 사용하기 위한 변형된 약물 - Google Patents

리포좀 나노입자에 사용하기 위한 변형된 약물 Download PDF

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KR101975843B1
KR101975843B1 KR1020187032439A KR20187032439A KR101975843B1 KR 101975843 B1 KR101975843 B1 KR 101975843B1 KR 1020187032439 A KR1020187032439 A KR 1020187032439A KR 20187032439 A KR20187032439 A KR 20187032439A KR 101975843 B1 KR101975843 B1 KR 101975843B1
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drug
group
docetaxel
derivative
liposomal nanoparticles
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KR20180123595A (ko
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피에터 컬리스
마르셀 발리
마르코 시우폴리니
노르버트 마우러
이고르 지갈트세브
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더 유니버시티 오브 브리티쉬 콜롬비아
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4525—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • 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
    • A61K47/54—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 compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • 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
    • A61K47/54—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 compound
    • A61K47/545—Heterocyclic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/127—Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
    • A61K9/1277—Preparation processes; Proliposomes
    • A61K9/1278—Post-loading, e.g. by ion or pH gradient
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D305/00—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms
    • C07D305/14—Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/04—Heterocyclic radicals containing only oxygen as ring hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/64—Cyclic peptides containing only normal peptide links
    • C07K7/645—Cyclosporins; Related peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Dispersion Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Rheumatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
KR1020187032439A 2008-05-23 2009-05-26 리포좀 나노입자에 사용하기 위한 변형된 약물 Expired - Fee Related KR101975843B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US5592908P 2008-05-23 2008-05-23
US61/055,929 2008-05-23
PCT/IB2009/006532 WO2009141738A2 (en) 2008-05-23 2009-05-26 Modified drugs for use in liposomal nanoparticles

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KR1020187003893A Division KR101919093B1 (ko) 2008-05-23 2009-05-26 리포좀 나노입자에 사용하기 위한 변형된 약물

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KR1020197012513A Division KR20190049930A (ko) 2008-05-23 2009-05-26 리포좀 나노입자에 사용하기 위한 변형된 약물

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KR20180123595A KR20180123595A (ko) 2018-11-16
KR101975843B1 true KR101975843B1 (ko) 2019-05-09

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KR1020197012513A Ceased KR20190049930A (ko) 2008-05-23 2009-05-26 리포좀 나노입자에 사용하기 위한 변형된 약물
KR1020187032439A Expired - Fee Related KR101975843B1 (ko) 2008-05-23 2009-05-26 리포좀 나노입자에 사용하기 위한 변형된 약물
KR1020167025450A Expired - Fee Related KR101830018B1 (ko) 2008-05-23 2009-05-26 리포좀 나노입자에 사용하기 위한 변형된 약물
KR1020107028838A Expired - Fee Related KR101659457B1 (ko) 2008-05-23 2009-05-26 리포좀 나노입자에 사용하기 위한 변형된 약물
KR1020187003893A Expired - Fee Related KR101919093B1 (ko) 2008-05-23 2009-05-26 리포좀 나노입자에 사용하기 위한 변형된 약물

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KR1020197012513A Ceased KR20190049930A (ko) 2008-05-23 2009-05-26 리포좀 나노입자에 사용하기 위한 변형된 약물

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KR1020167025450A Expired - Fee Related KR101830018B1 (ko) 2008-05-23 2009-05-26 리포좀 나노입자에 사용하기 위한 변형된 약물
KR1020107028838A Expired - Fee Related KR101659457B1 (ko) 2008-05-23 2009-05-26 리포좀 나노입자에 사용하기 위한 변형된 약물
KR1020187003893A Expired - Fee Related KR101919093B1 (ko) 2008-05-23 2009-05-26 리포좀 나노입자에 사용하기 위한 변형된 약물

Country Status (9)

Country Link
US (7) US8790691B2 (enExample)
EP (2) EP2282724B1 (enExample)
JP (5) JP5542804B2 (enExample)
KR (5) KR20190049930A (enExample)
CN (2) CN102105135B (enExample)
CA (3) CA2989616A1 (enExample)
ES (1) ES2694481T3 (enExample)
IL (2) IL209419A (enExample)
WO (1) WO2009141738A2 (enExample)

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CN102617517B (zh) * 2011-01-27 2015-11-18 李勤耕 一类新的7,10-o,o-二甲多西紫杉醇衍生物及其应用
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WO2012166949A1 (en) * 2011-05-31 2012-12-06 Regents Of The University Of Minnesota Silicate prodrugs and nanoparticles
WO2014058744A2 (en) 2012-10-09 2014-04-17 California Institute Of Technology In vivo and in vitro olefin cyclopropanation catalyzed by heme enzymes
WO2014058729A1 (en) * 2012-10-09 2014-04-17 California Institute Of Technology In vivo and in vitro carbene insertion and nitrene transfer reactions catalyzed by heme enzymes
BR112015022819A8 (pt) * 2013-03-13 2019-11-26 Mallinckrodt Llc método para a preparação de um taxano lipossomal, composição compreendendo um lipossoma e taxano lipossomal
GB201315321D0 (en) * 2013-08-28 2013-10-09 Koninklijke Nederlandse Akademie Van Wetenschappen Transduction Buffer
WO2015043792A1 (en) 2013-09-30 2015-04-02 Danmarks Tekniske Universitet Silicone chain extender
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CN105085437B (zh) * 2014-05-23 2018-07-03 上海交通大学 3-(1-叔丁氧羰酰哌嗪-4-yl)丙酸的两亲性衍生物及其用途
CN104368011B (zh) * 2014-11-27 2017-05-10 东南大学 一种药物甜菜碱缀合物、其药物组合物及应用
US20160250177A1 (en) * 2015-02-17 2016-09-01 Mallinckrodt Llc Modified docetaxel liposome formulations and uses thereof
TWI678213B (zh) * 2015-07-22 2019-12-01 美商史倍壯製藥公司 用於長春新鹼硫酸鹽脂質體注射之即可使用的調配物
EP3352733A1 (en) 2015-09-21 2018-08-01 Mallinckrodt LLC Improved stability of liposome formulations and uses thereof
GB201521101D0 (en) 2015-11-30 2016-01-13 Koninklijke Nederlandse Akademie Van Wetenschappen Transduction buffer
EP3394080B1 (en) * 2015-12-23 2023-06-07 The University Of British Columbia Lipid-linked prodrugs
WO2018160794A1 (en) 2017-03-01 2018-09-07 Merrimack Pharmaceuticals, Inc. Epha2-targeted docetaxel -generating liposomes in combination with an agent that impedes regulatory t cell activity for treating cancer
CN109422759B (zh) * 2017-08-22 2021-05-04 复旦大学 小分子修饰的紫杉烷类水溶性前药及其药用用途
CN111004195B (zh) * 2019-12-03 2022-01-28 沈阳药科大学 卡巴他赛弱碱性衍生物及其制剂
CN120569223A (zh) * 2022-07-07 2025-08-29 薇芯制药有限公司 多层囊泡药物制剂
CN117024381B (zh) * 2023-08-14 2025-08-12 沈阳药科大学 卡巴他赛衍生物及其脂质体制剂
CN118324842B (zh) * 2024-04-10 2025-05-02 沈阳药科大学 地塞米松弱碱性衍生物及其制剂的制备及应用

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