BR112021025394A2 - Derivados de antraciclina, conjugados de fármaco e molécula de ligação ao alvo, uso de conjugado de fármaco e molécula de ligação ao alvo, método de tratamento de uma doença em um paciente em necessidade de tratamento, e composição farmacêutica - Google Patents

Derivados de antraciclina, conjugados de fármaco e molécula de ligação ao alvo, uso de conjugado de fármaco e molécula de ligação ao alvo, método de tratamento de uma doença em um paciente em necessidade de tratamento, e composição farmacêutica

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Publication number
BR112021025394A2
BR112021025394A2 BR112021025394A BR112021025394A BR112021025394A2 BR 112021025394 A2 BR112021025394 A2 BR 112021025394A2 BR 112021025394 A BR112021025394 A BR 112021025394A BR 112021025394 A BR112021025394 A BR 112021025394A BR 112021025394 A2 BR112021025394 A2 BR 112021025394A2
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BR
Brazil
Prior art keywords
target binding
drug
binding molecule
conjugates
anthracycline derivatives
Prior art date
Application number
BR112021025394A
Other languages
English (en)
Inventor
Graham Cotton
Jennifer Thom
Paul Trumper
Original Assignee
Almac Discovery Ltd
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 Almac Discovery Ltd filed Critical Almac Discovery Ltd
Publication of BR112021025394A2 publication Critical patent/BR112021025394A2/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • 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
    • 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
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    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6807—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug or compound being a sugar, nucleoside, nucleotide, nucleic acid, e.g. RNA antisense
    • A61K47/6809—Antibiotics, e.g. antitumor antibiotics anthracyclins, adriamycin, doxorubicin or daunomycin
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    • A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
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    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
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    • C07K5/06104—Dipeptides with the first amino acid being acidic
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Abstract

derivados de antraciclina, conjugados de fármaco e molécula de ligação ao alvo, uso de conjugado de fármaco e molécula de ligação ao alvo, método de tratamento de uma doença em um paciente em necessidade de tratamento, e composição farmacêutica. o presente pedido refere-se a derivados de antraciclina e seu uso na formação de conjugados com moléculas de ligação ao alvo, incluindo, mas sem limitação, anticorpos. conjugados de moléculas de ligação ao alvo e derivados de antraciclina também são fornecidos. também são fornecidos usos médicos e composições farmacêuticas que compreendem os conjugados.
BR112021025394A 2019-06-20 2020-06-19 Derivados de antraciclina, conjugados de fármaco e molécula de ligação ao alvo, uso de conjugado de fármaco e molécula de ligação ao alvo, método de tratamento de uma doença em um paciente em necessidade de tratamento, e composição farmacêutica BR112021025394A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1908886.3A GB201908886D0 (en) 2019-06-20 2019-06-20 Anthracycline derivatives
PCT/EP2020/067210 WO2020254640A1 (en) 2019-06-20 2020-06-19 Anthracycline derivatives

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