AR090905A1 - Conjugados que contienen tetragalnac y peptidos y procedimientos para la administracion de oligonucleotidos, composicion farmaceutica - Google Patents

Conjugados que contienen tetragalnac y peptidos y procedimientos para la administracion de oligonucleotidos, composicion farmaceutica

Info

Publication number
AR090905A1
AR090905A1 ARP130101480A ARP130101480A AR090905A1 AR 090905 A1 AR090905 A1 AR 090905A1 AR P130101480 A ARP130101480 A AR P130101480A AR P130101480 A ARP130101480 A AR P130101480A AR 090905 A1 AR090905 A1 AR 090905A1
Authority
AR
Argentina
Prior art keywords
different
same
optionally
ligands
agents
Prior art date
Application number
ARP130101480A
Other languages
English (en)
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 AR090905A1 publication Critical patent/AR090905A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings
    • 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
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-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
    • 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
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • 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
    • C12N2310/17—Immunomodulatory nucleic acids
    • 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
    • C12N2310/3513—Protein; Peptide

Abstract

Reivindicación 1: Una composición modular que comprende: I) un oligonucleótido monocatenario o bicatenario; II) uno o más ligandos de tetraGaINAc de fórmula (1), (2) ó (3), que pueden ser iguales o diferentes, en las que X es -O-, -S-, -CR¹R²- o -NR¹-, en las que R¹ y R² están seleccionados cada uno independientemente del grupo que consiste en hidrógeno y alquilo C₁₋₆; n es 1, 2, 3 ó 4; y el enlace con línea ondulada indica el punto de unión; opcionalmente, III) uno o más ligadores, que pueden ser iguales o diferentes; opcionalmente IV) uno o más péptidos independientemente seleccionados de SEC ID Nº 1 - 474, o las variantes puntuales de conjugación de D-aminoácidos, retro-inversas y de cisteína de los mismos, que pueden ser iguales o diferentes; y opcionalmente, V) uno o más ligandos que eligen diana, agentes solubilizantes, agentes potenciadores de la farmacocinética, lípidos y/o agentes de enmascaramiento. Reivindicación 3: Una composición modular que comprende: I) un ARNip monocatenario o bicatenario; II) 1 - 8 ligandos de tetraGalNAc de fórmula (1), (2) ó (3), que pueden ser iguales o diferentes, en las que X es -O-, -S-, -CH₂- o -NH-; y n es 1, 2, 3 ó 4; III) 1 - 24 ligadores, que pueden ser iguales o diferentes; IV) 1 - 12 péptidos independientemente seleccionados de SEC ID Nº 1 - 474, o las variantes puntuales de conjugación de D-aminoácidos, retro-inversas y de cisteína de los mismos, que pueden ser iguales o diferentes; y opcionalmente, V) 1 - 8 ligandos que eligen diana, agentes solubilizantes, agentes potenciadores de la farmacocinética, lípidos y/o agentes de enmascaramiento.
ARP130101480A 2012-05-02 2013-04-30 Conjugados que contienen tetragalnac y peptidos y procedimientos para la administracion de oligonucleotidos, composicion farmaceutica AR090905A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261641741P 2012-05-02 2012-05-02

Publications (1)

Publication Number Publication Date
AR090905A1 true AR090905A1 (es) 2014-12-17

Family

ID=49514853

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130101480A AR090905A1 (es) 2012-05-02 2013-04-30 Conjugados que contienen tetragalnac y peptidos y procedimientos para la administracion de oligonucleotidos, composicion farmaceutica

Country Status (8)

Country Link
US (5) US9655976B2 (es)
EP (1) EP2844662B1 (es)
JP (2) JP6259448B2 (es)
AR (1) AR090905A1 (es)
AU (1) AU2013256341B2 (es)
CA (1) CA2871150A1 (es)
TW (1) TWI629996B (es)
WO (1) WO2013166155A1 (es)

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Also Published As

Publication number Publication date
US20180079769A1 (en) 2018-03-22
AU2013256341A1 (en) 2014-12-11
US20170306324A1 (en) 2017-10-26
JP2015520743A (ja) 2015-07-23
US20150246133A1 (en) 2015-09-03
WO2013166155A1 (en) 2013-11-07
EP2844662A4 (en) 2015-12-09
US9655976B2 (en) 2017-05-23
JP6259448B2 (ja) 2018-01-10
EP2844662B1 (en) 2020-09-16
TWI629996B (zh) 2018-07-21
CA2871150A1 (en) 2013-11-07
US11117917B2 (en) 2021-09-14
EP2844662A1 (en) 2015-03-11
TW201408325A (zh) 2014-03-01
AU2013256341B2 (en) 2017-10-19
US20220289785A1 (en) 2022-09-15
US9840531B2 (en) 2017-12-12
US10221205B2 (en) 2019-03-05
JP2018083816A (ja) 2018-05-31
US20190153016A1 (en) 2019-05-23

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