CN110402152B - 用于分子的跨膜递送的化合物和方法 - Google Patents

用于分子的跨膜递送的化合物和方法 Download PDF

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Publication number
CN110402152B
CN110402152B CN201880017053.0A CN201880017053A CN110402152B CN 110402152 B CN110402152 B CN 110402152B CN 201880017053 A CN201880017053 A CN 201880017053A CN 110402152 B CN110402152 B CN 110402152B
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formula
group
conjugate
moiety
pharmaceutically acceptable
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CN110402152A (zh
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伊兰·齐夫
约瑟夫·杜布罗夫斯基
哈吉特·格林贝格
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Aposense Ltd
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    • 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
    • A61K47/554—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 the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • 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
    • A61K31/7088—Compounds having three or more nucleosides or nucleotides
    • A61K31/713—Double-stranded nucleic acids or oligonucleotides
    • 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
    • C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/10—Type of nucleic acid
    • C12N2310/14—Type of nucleic acid interfering nucleic acids [NA]
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/32—Chemical structure of the sugar
    • C12N2310/321—2'-O-R Modification
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/35—Nature of the modification
    • C12N2310/351—Conjugate
    • C12N2310/3515—Lipophilic moiety, e.g. cholesterol

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Wood Science & Technology (AREA)
  • Biotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biophysics (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Physics & Mathematics (AREA)
  • Botany (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201880017053.0A 2017-01-09 2018-01-09 用于分子的跨膜递送的化合物和方法 Active CN110402152B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762443822P 2017-01-09 2017-01-09
US62/443,822 2017-01-09
PCT/IL2018/050031 WO2018127927A1 (en) 2017-01-09 2018-01-09 Compounds and methods for trans-membrane delivery of molecules

Publications (2)

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CN110402152A CN110402152A (zh) 2019-11-01
CN110402152B true CN110402152B (zh) 2024-03-19

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US (1) US11230710B2 (enExample)
EP (1) EP3565603B1 (enExample)
JP (1) JP7348064B2 (enExample)
KR (1) KR20190104392A (enExample)
CN (1) CN110402152B (enExample)
AU (1) AU2018205898B2 (enExample)
CA (1) CA3049640A1 (enExample)
EA (1) EA201991661A1 (enExample)
IL (1) IL267919B2 (enExample)
WO (1) WO2018127927A1 (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11318206B2 (en) 2014-03-28 2022-05-03 Aposense Ltd Compounds and methods for trans-membrane delivery of molecules
CN110402152B (zh) 2017-01-09 2024-03-19 艾博森斯有限公司 用于分子的跨膜递送的化合物和方法
US10195286B2 (en) * 2017-07-04 2019-02-05 Aposense Ltd. Compounds and methods for trans-membrane delivery of molecules
EP3735276A4 (en) * 2018-01-01 2021-10-13 Aposense Ltd. COMPOUNDS AND METHODS FOR THE TRANSMEMBRANARY ADMINISTRATION OF MOLECULES
WO2020044349A1 (en) * 2018-08-30 2020-03-05 Aposense Ltd. Compounds, cojugates and compositions for use in the methods for trans-membrane delivery of molecules
JPWO2023022055A1 (enExample) * 2021-08-17 2023-02-23
KR20260110145A (ko) 2023-10-30 2026-07-14 올페라 코퍼레이션 후각 전달 스캐폴드 및 이를 제조하고 사용하는 방법

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160106855A1 (en) * 2014-03-28 2016-04-21 Aposense Ltd. Compounds and methods for trans-membrane delivery of molecules

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU736301B2 (en) 1996-05-01 2001-07-26 Imarx Therapeutics, Inc. Methods for delivering compounds into a cell
US6090800A (en) 1997-05-06 2000-07-18 Imarx Pharmaceutical Corp. Lipid soluble steroid prodrugs
WO1998050041A1 (en) 1997-05-06 1998-11-12 Imarx Pharmaceutical Corp. Novel prodrugs comprising fluorinated amphiphiles
FR2846969A1 (fr) 2002-11-08 2004-05-14 Salles Jean Pierre Nouveaux vecteurs moleculaires amphiphiles fluorocarbones a usage biomedical et medical
SE527131C2 (sv) 2004-02-13 2005-12-27 Innoventus Project Ab Steroider för cancerbehandling
JP2008505884A (ja) 2004-07-08 2008-02-28 エヌエスティー・ニューロサバイバル・テクノロジーズ・リミテッド 疾患を検出する方法および化合物
AU2005281359A1 (en) 2004-08-26 2006-03-16 Apparao Satyam Prodrugs and codrugs containing novel bio-cleavable disulfide linkers
EA200700741A1 (ru) 2004-10-01 2007-08-31 Прометик Байосайенсиз Инк. Жирные спирты со средней длиной цепи как стимуляторы гематопоэза
MX2007010113A (es) 2005-02-18 2007-12-07 Angiochem Inc Polipeptidos de aprotinina para transportar un compuesto a traves de la barrera hematoencefalica.
EP2081949B1 (en) 2006-09-22 2014-12-10 GE Healthcare Dharmacon, Inc. Tripartite oligonucleotide complexes and methods for gene silencing by rna interference
EP2229186A2 (en) 2007-12-04 2010-09-22 Alnylam Pharmaceuticals Inc. Carbohydrate conjugates as delivery agents for oligonucleotides
MX2010012238A (es) 2008-05-13 2011-04-11 Univ Washington Copolimeros dibloque y sus complejos con polinucleotidos destinados a introducirlos en celulas.
WO2009155335A2 (en) 2008-06-19 2009-12-23 University Of Maryland, Baltimore Conjugates of 19f mr imaging tracers and chemotherapeutic agents for drug quantification and drug dose individualization
EP2342340A1 (en) 2008-09-22 2011-07-13 Rxi Pharmaceuticals Corporation Rna interference in skin indications
WO2012018729A1 (en) 2010-08-03 2012-02-09 Berry And Associates, Inc. Phosphoramidite derivatives of folic acid
GB201122458D0 (en) 2011-12-30 2012-02-08 Univ Wageningen Modified cascade ribonucleoproteins and uses thereof
ES2728782T3 (es) 2012-05-25 2019-10-28 Univ California Métodos y composiciones para la modificación de ADN objetivo dirigida por ARN y para la modulación de la transcripción dirigida por ARN
WO2013181440A1 (en) 2012-05-30 2013-12-05 Baylor College Of Medicine Supercoiled minivectors as a tool for dna repair, alteration and replacement
EA201590622A1 (ru) * 2012-10-16 2015-10-30 Эндосайт, Инк. Конъюгаты для доставки лекарственного средства, содержащие не встречающиеся в природе аминокислоты, и способы применения
US20160002159A1 (en) 2013-02-13 2016-01-07 Neal ZONDLO Perfluoro-tert-butyl hydroxyproline
CN110003066B (zh) 2013-11-18 2021-09-03 阿克丘勒斯治疗公司 用于rna递送的可电离的阳离子脂质
US9889202B2 (en) 2014-03-28 2018-02-13 Aposense Ltd. Compounds and methods for trans-membrane delivery of molecules
US9993563B2 (en) 2014-03-28 2018-06-12 Aposense Ltd. Compounds and methods for trans-membrane delivery of molecules
US20160016855A1 (en) * 2014-07-21 2016-01-21 Benxin Wu Fabrication of carbon nanotube-nonoxide structural ceramic nanocomposites through laser sintering
CN110402152B (zh) 2017-01-09 2024-03-19 艾博森斯有限公司 用于分子的跨膜递送的化合物和方法
US10195286B2 (en) 2017-07-04 2019-02-05 Aposense Ltd. Compounds and methods for trans-membrane delivery of molecules

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160106855A1 (en) * 2014-03-28 2016-04-21 Aposense Ltd. Compounds and methods for trans-membrane delivery of molecules

Also Published As

Publication number Publication date
IL267919A (en) 2019-09-26
JP2020514299A (ja) 2020-05-21
EA201991661A1 (ru) 2019-12-30
WO2018127927A1 (en) 2018-07-12
JP7348064B2 (ja) 2023-09-20
AU2018205898A1 (en) 2019-08-22
EP3565603B1 (en) 2022-12-07
IL267919B1 (en) 2023-11-01
EP3565603A1 (en) 2019-11-13
KR20190104392A (ko) 2019-09-09
US20200392490A1 (en) 2020-12-17
EP3565603A4 (en) 2020-09-09
US11230710B2 (en) 2022-01-25
CN110402152A (zh) 2019-11-01
IL267919B2 (en) 2024-03-01
AU2018205898B2 (en) 2020-12-10
CA3049640A1 (en) 2018-07-12

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