BR112012021269A2 - composição modular. - Google Patents

composição modular.

Info

Publication number
BR112012021269A2
BR112012021269A2 BR112012021269A BR112012021269A BR112012021269A2 BR 112012021269 A2 BR112012021269 A2 BR 112012021269A2 BR 112012021269 A BR112012021269 A BR 112012021269A BR 112012021269 A BR112012021269 A BR 112012021269A BR 112012021269 A2 BR112012021269 A2 BR 112012021269A2
Authority
BR
Brazil
Prior art keywords
modular composition
oligonucleotide
linkers
attached
peptides
Prior art date
Application number
BR112012021269A
Other languages
English (en)
Inventor
Aaron A Momose
Anthony W Shaw
David M Tellers
Jeffrey G Aaronson
Rene Bartz
Stanley F Barnett
Steven L Colletti
Thomas J Tucker
Vasant R Jadhav
Weimin Wang
Yu Yuan
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of BR112012021269A2 publication Critical patent/BR112012021269A2/pt

Links

Classifications

    • 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
    • A61K31/7105—Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/645—Polycationic or polyanionic oligopeptides, polypeptides or polyamino acids, e.g. polylysine, polyarginine, polyglutamic acid or peptide TAT
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K48/00—Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K19/00—Hybrid peptides, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Organic Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Botany (AREA)
  • Biotechnology (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Apparatus Associated With Microorganisms And Enzymes (AREA)

Abstract

composição modular. em uma modalidade, a presente invenção revela uma composição modular que comprrende 1) um oligonucleotídeo; 2) um ou mais ligadores, que podem ser os mesmos ou diferentes, selecionados da tabela 1, em que os ligadores são anexados ao oligonucleotídeo em qualquer extremidade 3^,^ e/ou 5^,^; 3) um ou mais peptídeos, que podem ser os mesmos ou diferentes, selecionados de seq id nos: 1-59, em que os peptídeos são anexados aos ligadroes; e opcionalmente um ou mais lipídeos, grupos de solubilização e/ou ligantes de marcação anexados ao oligonucleotídeo.
BR112012021269A 2010-04-09 2011-04-04 composição modular. BR112012021269A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US32242210P 2010-04-09 2010-04-09
PCT/US2011/031080 WO2011126974A1 (en) 2010-04-09 2011-04-04 Novel single chemical entities and methods for delivery of oligonucleotides

Publications (1)

Publication Number Publication Date
BR112012021269A2 true BR112012021269A2 (pt) 2016-10-25

Family

ID=44763234

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012021269A BR112012021269A2 (pt) 2010-04-09 2011-04-04 composição modular.

Country Status (11)

Country Link
US (1) US8691580B2 (pt)
EP (1) EP2555777B1 (pt)
JP (1) JP2013523149A (pt)
KR (1) KR20130040811A (pt)
CN (1) CN102892420A (pt)
AU (1) AU2011238501A1 (pt)
BR (1) BR112012021269A2 (pt)
CA (1) CA2792942A1 (pt)
MX (1) MX2012011515A (pt)
RU (1) RU2012147589A (pt)
WO (1) WO2011126974A1 (pt)

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Publication number Priority date Publication date Assignee Title
EP3406730B1 (en) * 2010-08-31 2022-02-23 Sirna Therapeutics, Inc. Novel single chemical entities and methods for delivery of oligonucleotides
AR090905A1 (es) 2012-05-02 2014-12-17 Merck Sharp & Dohme Conjugados que contienen tetragalnac y peptidos y procedimientos para la administracion de oligonucleotidos, composicion farmaceutica
TW201808342A (zh) * 2012-05-02 2018-03-16 喜納製藥公司 包含四ｇａｌｎａｃ之新穎結合物及傳送寡核苷酸之方法
JP6373762B2 (ja) * 2012-12-28 2018-08-15 国立大学法人東北大学 ターゲット分子細胞内導入用ペプチド
US20160184449A1 (en) * 2013-02-28 2016-06-30 University Of Massachusetts Peptide-and amine-modified glucan particles for delivery of therapeutic cargoes
WO2015031059A1 (en) * 2013-08-26 2015-03-05 The Trustees Of The University Of Pennsylvania Ph-sensitive peptides and their nanoparticles for drug delivery
WO2015056713A1 (ja) 2013-10-15 2015-04-23 国立大学法人東京大学 ｃ－Ｍｅｔタンパク質アゴニスト
US10239957B2 (en) 2013-11-06 2019-03-26 Merck Sharp & Dohme Corp. Peptide containing conjugates for dual molecular delivery of oligonucleotides
AR107823A1 (es) 2016-03-07 2018-06-06 Hanmi Pharm Ind Co Ltd Derivados de polietilenglicol y uso de los mismos
EP3654941A1 (en) 2017-07-17 2020-05-27 Keith Roizman Topical delivery of therapeutic agents comprising cell-penetrating peptides for use for the treatment of age-related macular degeneration and other eye diseases
CN110997917B (zh) 2017-12-01 2024-04-09 苏州瑞博生物技术股份有限公司 一种核酸、含有该核酸的组合物与缀合物及制备方法和用途
CN110997919B (zh) 2017-12-01 2024-04-02 苏州瑞博生物技术股份有限公司 双链寡核苷酸、含双链寡核苷酸的组合物与缀合物及制备方法和用途
CA3087106A1 (en) * 2017-12-29 2019-07-04 Suzhou Ribo Life Science Co., Ltd. Conjugates and preparation and use thereof
WO2020038377A1 (zh) * 2018-08-21 2020-02-27 苏州瑞博生物技术有限公司 一种核酸、含有该核酸的药物组合物和缀合物及其用途
JP7376952B2 (ja) * 2018-09-30 2023-11-09 スーチョウ リボ ライフ サイエンス カンパニー、リミテッド ｓｉＲＮＡ複合体及びその調製方法と使用
NZ784956A (en) * 2019-07-18 2023-01-27 Hanmi Pharm Ind Co Ltd Novel method for preparing long-acting drug conjugate through preparation of intermediate
CN113214353B (zh) * 2021-04-12 2022-09-23 武汉泽智生物医药有限公司 两亲性寡肽结构物质
CN113717254B (zh) * 2021-09-23 2022-03-22 中山大学附属口腔医院 一种抗菌肽及其应用

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KR100468316B1 (ko) 2002-01-29 2005-01-27 주식회사 웰진 Ｄｎａ의 세포 또는 조직 내 전달 효율을 높이는 펩타이드
EP1487995A4 (en) * 2002-02-13 2006-08-02 Medbridge Inc PROTEIN CARRIER SYSTEM FOR THERAPEUTIC OLIGONUCLEOTIDES
ATE465255T1 (de) * 2002-11-26 2010-05-15 Univ Massachusetts Verabreichung von sirnas
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EP2323695B1 (en) * 2008-08-19 2018-12-05 Nektar Therapeutics Complexes of small-interfering nucleic acids

Also Published As

Publication number Publication date
AU2011238501A1 (en) 2012-08-30
EP2555777B1 (en) 2019-02-20
CN102892420A (zh) 2013-01-23
WO2011126974A1 (en) 2011-10-13
EP2555777A1 (en) 2013-02-13
KR20130040811A (ko) 2013-04-24
EP2555777A4 (en) 2015-01-21
CA2792942A1 (en) 2011-10-13
MX2012011515A (es) 2012-11-06
JP2013523149A (ja) 2013-06-17
US20130041133A1 (en) 2013-02-14
US8691580B2 (en) 2014-04-08
RU2012147589A (ru) 2014-05-20

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Legal Events

Date Code Title Description
B08F Application fees: application dismissed [chapter 8.6 patent gazette]
B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]