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
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ARP170100538A
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English (en)
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Genentech Inc
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Publication of AR107800A1 publication Critical patent/AR107800A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C201/00Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
    • C07C201/06Preparation of nitro compounds
    • C07C201/12Preparation of nitro compounds by reactions not involving the formation of nitro groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C205/00Compounds containing nitro groups bound to a carbon skeleton
    • C07C205/27Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by etherified hydroxy groups
    • C07C205/35Compounds 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
    • C07C205/36Compounds 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
    • C07C205/37Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/02Preparation 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/74Compounds 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
    • C07C215/76Compounds 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
    • C07C215/78Compounds 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/12Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from bacteria
    • C07K16/1267Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from bacteria from Gram-positive bacteria
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/12Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from bacteria
    • C07K16/1267Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from bacteria from Gram-positive bacteria
    • C07K16/1271Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from bacteria from Gram-positive bacteria from Micrococcaceae (F), e.g. Staphylococcus
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K2039/505Medicinal preparations containing antigens or antibodies comprising antibodies
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K2317/00Immunoglobulins specific features
    • C07K2317/70Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/77Internalization into the cell

Landscapes

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

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
EP4387618A1 (en) * 2021-08-20 2024-06-26 Rutgers, the State University of New Jersey Dual-targeted rna polymerase inhibitors: conjugates of benzoxazino- and spiro-rifamycins with n?-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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Also Published As

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

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