AR107800A1 - Proceso para la preparación de un conjugado de anticuerpo-rifamicina - Google Patents

Proceso para la preparación de un conjugado de anticuerpo-rifamicina

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Publication number
AR107800A1
AR107800A1 ARP170100538A ARP170100538A AR107800A1 AR 107800 A1 AR107800 A1 AR 107800A1 AR P170100538 A ARP170100538 A AR P170100538A AR P170100538 A ARP170100538 A AR P170100538A AR 107800 A1 AR107800 A1 AR 107800A1
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AR
Argentina
Prior art keywords
formula
preparation
otf
compound
reacting
Prior art date
Application number
ARP170100538A
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English (en)
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Genentech Inc
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.)
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Publication date
Application filed by Genentech Inc filed Critical Genentech Inc
Publication of AR107800A1 publication Critical patent/AR107800A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • 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
    • C07D498/02—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 two hetero rings
    • C07D498/04—Ortho-condensed systems
    • 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
    • A61K47/68—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
    • 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
    • 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
    • A61K47/68—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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C201/00—Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
    • C07C201/06—Preparation of nitro compounds
    • C07C201/12—Preparation of nitro compounds by reactions not involving the formation of nitro groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C205/00—Compounds containing nitro groups bound to a carbon skeleton
    • C07C205/27—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups
    • C07C205/35—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups having nitro groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C205/36—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups having nitro groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton to carbon atoms of the same non-condensed six-membered aromatic ring or to carbon atoms of six-membered aromatic rings being part of the same condensed ring system
    • C07C205/37—Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups having nitro groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton to carbon atoms of the same non-condensed six-membered aromatic ring or to carbon atoms of six-membered aromatic rings being part of the same condensed ring system the oxygen atom of at least one of the etherified hydroxy groups being further bound to an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/02—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/74—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C215/76—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton of the same non-condensed six-membered aromatic ring
    • C07C215/78—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton of the same non-condensed six-membered aromatic ring containing at least two hydroxy groups bound to the carbon skeleton
    • 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
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/12—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from bacteria
    • C07K16/1267—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from bacteria from Gram-positive bacteria
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/12—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from bacteria
    • C07K16/1267—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from bacteria from Gram-positive bacteria
    • C07K16/1271—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from bacteria from Gram-positive bacteria from Micrococcaceae (F), e.g. Staphylococcus
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/77—Internalization into the cell

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Catalysts (AREA)

Abstract

Se describen procesos para la preparación de F-benzoxazinorifamicina y compuestos intermedios para la conjugación con un anticuerpo. Reivindicación 1: Un proceso para la preparación de F-benzoxazinorifamicina de fórmula (1), que comprende hacer reaccionar rifamicina S de fórmula (2), 2-amino-5-fluorobenceno-1,3-diol de fórmula (3), y uno o más oxidantes seleccionados entre TEMPO y los análogos de TEMPO, aire ambiente, oxígeno gaseoso, benzoquinona, óxido de manganeso (MnO₂), (PhI(OTs)OH, peryodato de sodio (NalO₄), cloranilo, peróxido de hidrógeno, Fe₂O₃, Na₂S₂O₈, Co(acac)₃, Mn(acac)₂, Cu(OAc)₂, CuO, CuBr₂, ZnCl₂, InCl₃, Ag(OTf)₂, Sc(OTf)₃, e Yb(OTf)₃, para formar el compuesto de fórmula (1). Reivindicación 18: Un proceso para la preparación de 2-amino-5-fluorobenceno-1,3-diol de fórmula (3), que comprende: (a) hacer reaccionar 1,3,5-trifluoro-2-nitrobenceno de fórmula (4), fenilmetanol, y un reactivo básico seleccionado entre bis(trimetilsililamida)diisopropilamida de litio, y un reactivo alcóxido, para formar (((5-fluoro-2-nitro-1,3- fenilen)bis(oxi))bis(metilen))dibenceno de fórmula (5); y (b) hacer reaccionar el compuesto de fórmula (5) con hidrógeno gaseoso y un catalizador metal heterogéneo para formar el compuesto de fórmula (3).
ARP170100538A 2016-03-04 2017-03-03 Proceso para la preparación de un conjugado de anticuerpo-rifamicina AR107800A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662303556P 2016-03-04 2016-03-04

Publications (1)

Publication Number Publication Date
AR107800A1 true AR107800A1 (es) 2018-06-06

Family

ID=58361102

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP170100538A AR107800A1 (es) 2016-03-04 2017-03-03 Proceso para la preparación de un conjugado de anticuerpo-rifamicina

Country Status (13)

Country Link
US (2) US10336683B2 (es)
EP (1) EP3423457B1 (es)
JP (2) JP6705904B2 (es)
KR (1) KR102204805B1 (es)
CN (1) CN108713020A (es)
AR (1) AR107800A1 (es)
AU (1) AU2017228468B2 (es)
BR (1) BR112018014355A2 (es)
CA (1) CA3012046C (es)
IL (1) IL260465B (es)
MX (1) MX2018010491A (es)
SG (1) SG11201807537RA (es)
WO (1) WO2017152083A1 (es)

Families Citing this family (7)

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CA3012046C (en) 2016-03-04 2020-11-10 Genentech, Inc. Process for the preparation of an antibody-rifamycin conjugate
CN108047250B (zh) * 2018-02-12 2020-08-14 丹诺医药(苏州）有限公司 一种利福霉素-硝基咪唑偶联分子的应用
CN110687217B (zh) * 2018-08-07 2021-04-23 中国科学院大连化学物理研究所 液相色谱测定利福霉素s的方法
CN110687218B (zh) * 2018-08-07 2021-04-23 中国科学院大连化学物理研究所 液相色谱测定苯并噁嗪利福霉素的方法
EP3897841A1 (en) 2018-12-21 2021-10-27 Regeneron Pharmaceuticals, Inc. Rifamycin analogs and antibody-drug conjugates thereof
WO2023023378A1 (en) * 2021-08-20 2023-02-23 Rutgers, The State University Of New Jersey DUAL-TARGETED RNA POLYMERASE INHIBITORS: CONJUGATES OF BENZOXAZINO- AND SPIRO-RIFAMYCINS WITH Nα-AROYL- N-ARYL-PHENYLALANINAMIDES
CN114436864A (zh) * 2022-02-17 2022-05-06 浙江鼎龙科技股份有限公司 一种2-甲基-5氨基苯酚的制备方法

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CA3012046C (en) 2016-03-04 2020-11-10 Genentech, Inc. Process for the preparation of an antibody-rifamycin conjugate

Also Published As

Publication number Publication date
CA3012046C (en) 2020-11-10
EP3423457B1 (en) 2021-02-17
IL260465B (en) 2020-11-30
WO2017152083A1 (en) 2017-09-08
JP6705904B2 (ja) 2020-06-03
US20170252457A1 (en) 2017-09-07
KR20180118173A (ko) 2018-10-30
CA3012046A1 (en) 2017-09-08
US10689325B2 (en) 2020-06-23
AU2017228468A1 (en) 2018-07-26
MX2018010491A (es) 2018-11-09
KR102204805B1 (ko) 2021-01-20
BR112018014355A2 (pt) 2018-12-18
AU2017228468B2 (en) 2019-12-05
EP3423457A1 (en) 2019-01-09
JP2020090506A (ja) 2020-06-11
JP2019510740A (ja) 2019-04-18
US20190270695A1 (en) 2019-09-05
US10336683B2 (en) 2019-07-02
SG11201807537RA (en) 2018-09-27
CN108713020A (zh) 2018-10-26

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