EA201690051A1 - Поликонъюгаты для доставки триггеров рнк интерференции в клетки опухоли in vivo - Google Patents

Поликонъюгаты для доставки триггеров рнк интерференции в клетки опухоли in vivo

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Publication number
EA201690051A1
EA201690051A1 EA201690051A EA201690051A EA201690051A1 EA 201690051 A1 EA201690051 A1 EA 201690051A1 EA 201690051 A EA201690051 A EA 201690051A EA 201690051 A EA201690051 A EA 201690051A EA 201690051 A1 EA201690051 A1 EA 201690051A1
Authority
EA
Eurasian Patent Office
Prior art keywords
polyconjugates
tumor
delivery
rnai
trigger
Prior art date
Application number
EA201690051A
Other languages
English (en)
Russian (ru)
Inventor
Вэйцзюнь Чэн
Со Вон
Аарон М. Альмейда
Дэвид Б. Розема
Андрей В. Блохин
Джеффри С. Карлсон
Original Assignee
Эрроухэд Рисерч Корпорейшн
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Эрроухэд Рисерч Корпорейшн filed Critical Эрроухэд Рисерч Корпорейшн
Publication of EA201690051A1 publication Critical patent/EA201690051A1/ru

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    • CCHEMISTRY; METALLURGY
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    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09Recombinant DNA-technology
    • C12N15/11DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113Non-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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7088Compounds having three or more nucleosides or nucleotides
    • A61K31/713Double-stranded nucleic acids or oligonucleotides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06043Leu-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06017Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052Val-amino acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • C07K5/06156Dipeptides with the first amino acid being heterocyclic and Trp-amino acid; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0815Tripeptides with the first amino acid being basic
    • C07K5/0817Tripeptides with the first amino acid being basic the first amino acid being Arg
    • CCHEMISTRY; METALLURGY
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    • C12N2310/00Structure or type of the nucleic acid
    • C12N2310/10Type of nucleic acid
    • C12N2310/14Type of nucleic acid interfering nucleic acids [NA]
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    • C12N2310/00Structure or type of the nucleic acid
    • C12N2310/30Chemical structure
    • C12N2310/32Chemical structure of the sugar
    • C12N2310/3222'-R Modification
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    • C12N2310/00Structure or type of the nucleic acid
    • C12N2310/30Chemical structure
    • C12N2310/35Nature of the modification
    • C12N2310/351Conjugate
    • C12N2310/3513Protein; Peptide
    • CCHEMISTRY; METALLURGY
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    • C12N2310/00Structure or type of the nucleic acid
    • C12N2310/30Chemical structure
    • C12N2310/35Nature of the modification
    • C12N2310/353Nature of the modification linked to the nucleic acid via an atom other than carbon
    • C12N2310/3535Nitrogen
    • CCHEMISTRY; METALLURGY
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    • C12N2320/00Applications; Uses
    • C12N2320/30Special therapeutic applications
    • C12N2320/32Special delivery means, e.g. tissue-specific

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Zoology (AREA)
  • Biotechnology (AREA)
  • Wood Science & Technology (AREA)
  • Epidemiology (AREA)
  • General Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Physics & Mathematics (AREA)
  • Plant Pathology (AREA)
  • Microbiology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
EA201690051A 2013-08-07 2014-08-06 Поликонъюгаты для доставки триггеров рнк интерференции в клетки опухоли in vivo EA201690051A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361863056P 2013-08-07 2013-08-07
PCT/US2014/049851 WO2015021092A1 (en) 2013-08-07 2014-08-06 Polyconjugates for delivery of rnai triggers to tumor cells in vivo
US14/452,626 US9487556B2 (en) 2013-08-07 2014-08-06 Polyconjugates for delivery of RNAi triggers to tumor cells in vivo

Publications (1)

Publication Number Publication Date
EA201690051A1 true EA201690051A1 (ru) 2016-06-30

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201690051A EA201690051A1 (ru) 2013-08-07 2014-08-06 Поликонъюгаты для доставки триггеров рнк интерференции в клетки опухоли in vivo

Country Status (13)

Country Link
US (3) US9487556B2 (https=)
EP (1) EP3030244B1 (https=)
JP (1) JP6433001B2 (https=)
KR (1) KR20160035081A (https=)
CN (1) CN105451743B (https=)
AU (1) AU2014306021B2 (https=)
CA (1) CA2919088A1 (https=)
EA (1) EA201690051A1 (https=)
IL (1) IL243941B (https=)
MX (1) MX2016001006A (https=)
SG (1) SG11201600379TA (https=)
TW (1) TWI685347B (https=)
WO (1) WO2015021092A1 (https=)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015021092A1 (en) * 2013-08-07 2015-02-12 Arrowhead Research Corporation Polyconjugates for delivery of rnai triggers to tumor cells in vivo
EP3270903B1 (en) 2015-03-17 2020-05-06 Arrowhead Pharmaceuticals, Inc. Disulfide-containing alkyne linking agents
CA2979703A1 (en) * 2015-03-17 2016-09-22 Arrowhead Pharmaceuticals, Inc. Compositions and methods for inhibiting gene expression of factor xii
CN107614002B (zh) 2015-05-29 2022-01-04 箭头药业股份有限公司 生物学可切割四肽连接剂
AR104754A1 (es) 2015-05-29 2017-08-09 Arrowhead Pharmaceuticals Inc Agentes de unión de tetrapéptido escindibles biológicamente
JOP20160211B1 (ar) 2015-10-01 2021-08-17 Arrowhead Pharmaceuticals Inc تراكيب وأساليب لتثبيط تعبير جيني للـ lpa
EP3397651B1 (en) 2015-12-29 2020-05-06 Galderma S.A. Carbohydrate crosslinker
EP3252082A1 (en) * 2016-05-31 2017-12-06 Galderma S.A. Method for deacetylation of biopolymers
PT3623390T (pt) * 2016-05-31 2023-10-27 Galderma Sa Reticulador de hidrato de carbono
WO2018218004A1 (en) 2017-05-24 2018-11-29 The Board Of Regents Of The University Of Texas System Linkers for antibody drug conjugates
SG11202009734VA (en) * 2018-04-27 2020-11-27 Arrowhead Pharmaceuticals Inc Integrin targeting ligands and uses thereof
SG11202105577TA (en) 2019-01-09 2021-06-29 Arrowhead Pharmaceuticals Inc Rnai agents for inhibiting expression of hif-2 alpha (epas1), compositions thereof, and methods of use
CN110240551B (zh) * 2019-06-25 2022-02-11 成都郑源生化科技有限公司 Fmoc-β-Ala-Gly-OH的制备方法
CA3160575A1 (en) 2019-12-02 2021-06-10 Johan Olsson High molecular weight esthetic compositions
CN113004515B (zh) * 2021-03-02 2023-02-24 厦门大学附属中山医院 一种仿透明质酸聚氨基酸衍生物、其制备方法及其应用

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL123164A (en) * 1995-08-30 2001-03-19 Searle & Co Meta-guanidine urea thiourea or azacyclic amino benzoic acid derivatives and pharmaceutical compositions containing them
DE69706407T2 (de) 1996-03-29 2002-05-29 G.D. Searle & Co., Chicago META-SUBSTITUIERTE PHENYLENDERIVATE UND IHRE VERWENDUNG ALS ALPHAvBETA3 INTERGRIN-ANTAGONISTEN ODER INHIBITOREN
CA2265484C (en) * 1996-09-10 2008-12-02 The Burnham Institute Tumor homing molecules, conjugates derived therefrom, and methods of using same
ATE208368T1 (de) 1997-04-07 2001-11-15 Cfpi Nufarm Verfahren zur herstellung von 3,4 disubstituirten dinitroanilinen
AU2002337954C1 (en) * 2001-10-22 2008-10-23 The Scripps Research Institute Integrin targeting compounds
JP2004261024A (ja) * 2003-02-28 2004-09-24 Japan Science & Technology Agency ペプチド修飾多糖類を用いる遺伝子治療剤
WO2004090108A2 (en) * 2003-04-03 2004-10-21 Alnylam Pharmaceuticals Irna conjugates
CA2559955C (en) 2004-03-15 2016-02-16 City Of Hope Methods and compositions for the specific inhibition of gene expression by double-stranded rna
WO2006052854A2 (en) * 2004-11-04 2006-05-18 Raul Andino Syntheses of polyamine conjugates of small interfering rnas (si-rnas) and conjugates formed thereby
CN101277704A (zh) * 2005-04-12 2008-10-01 因特拉迪格姆公司 用于治疗癌症及其它新血管生成疾病的RNAi治疗剂的组合物和方法
CN101500548A (zh) 2006-08-18 2009-08-05 弗·哈夫曼-拉罗切有限公司 用于体内递送多核苷酸的多缀合物
US8017109B2 (en) 2006-08-18 2011-09-13 Roche Madison Inc. Endosomolytic poly(acrylate) polymers
WO2008034123A2 (en) * 2006-09-15 2008-03-20 Enzon Pharmaceuticals, Inc. Polymeric conjugates containing positively-charged moieties
WO2008045252A2 (en) 2006-10-04 2008-04-17 The Board Of Trustees Of The Leland Stanford Junior University Engineered integrin binding peptides
KR101728655B1 (ko) 2008-12-18 2017-04-19 다이서나 파마수이티컬, 인크. 유전자 발현의 특이적 억제를 위한 연장된 다이서 기질 제제 및 방법
US20100249214A1 (en) 2009-02-11 2010-09-30 Dicerna Pharmaceuticals Multiplex dicer substrate rna interference molecules having joining sequences
SI2539451T1 (sl) 2010-02-24 2016-04-29 Arrowhead Research Corporation Sestavki za ciljano dostavo sirna
US8501930B2 (en) 2010-12-17 2013-08-06 Arrowhead Madison Inc. Peptide-based in vivo siRNA delivery system
CA3131967A1 (en) * 2010-12-29 2012-07-05 F. Hoffman-La Roche Ag Small molecule conjugates for intracellular delivery of nucleic acids
CA2816041C (en) * 2010-12-29 2019-01-08 Arrowhead Research Corporation In vivo polynucleotide delivery conjugates having enzyme sensitive linkages
WO2013032829A1 (en) 2011-08-26 2013-03-07 Arrowhead Research Corporation Poly(vinyl ester) polymers for in vivo nucleic acid delivery
WO2013110578A1 (en) * 2012-01-27 2013-08-01 F. Hoffmann-La Roche Ag Integrin antagonist conjugates for targeted delivery to cells expressing alpha-v-beta-3
KR20140120316A (ko) 2012-01-27 2014-10-13 에프. 호프만-라 로슈 아게 표적화된 전달을 위한 소분자 인테그린 안타고니스트와 공유 결합된 키토산
CA2842041A1 (en) 2012-04-18 2013-10-24 Arrowhead Research Corporation Poly(acrylate) polymers for in vivo nucleic acid delivery
WO2015021092A1 (en) * 2013-08-07 2015-02-12 Arrowhead Research Corporation Polyconjugates for delivery of rnai triggers to tumor cells in vivo

Also Published As

Publication number Publication date
SG11201600379TA (en) 2016-02-26
EP3030244B1 (en) 2021-04-21
EP3030244A1 (en) 2016-06-15
KR20160035081A (ko) 2016-03-30
AU2014306021A1 (en) 2016-01-28
US20190062748A1 (en) 2019-02-28
AU2014306021B2 (en) 2018-12-13
JP6433001B2 (ja) 2018-12-05
WO2015021092A1 (en) 2015-02-12
US20170022497A1 (en) 2017-01-26
US20150045573A1 (en) 2015-02-12
IL243941A0 (en) 2016-04-21
AU2014306021A2 (en) 2016-11-24
US9487556B2 (en) 2016-11-08
HK1220397A1 (zh) 2017-05-05
EP3030244A4 (en) 2017-06-28
TWI685347B (zh) 2020-02-21
CN105451743B (zh) 2019-11-19
TW201601742A (zh) 2016-01-16
IL243941B (en) 2019-06-30
CN105451743A (zh) 2016-03-30
JP2016535058A (ja) 2016-11-10
CA2919088A1 (en) 2015-02-12
MX2016001006A (es) 2016-04-19

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