BR112018014355A2 - processos para a preparação de f-benzoxazinorifamicina i e para a preparação de 2-amino-5-fluorobenzeno-1,3-diol iii - Google Patents

processos para a preparação de f-benzoxazinorifamicina i e para a preparação de 2-amino-5-fluorobenzeno-1,3-diol iii

Info

Publication number
BR112018014355A2
BR112018014355A2 BR112018014355-3A BR112018014355A BR112018014355A2 BR 112018014355 A2 BR112018014355 A2 BR 112018014355A2 BR 112018014355 A BR112018014355 A BR 112018014355A BR 112018014355 A2 BR112018014355 A2 BR 112018014355A2
Authority
BR
Brazil
Prior art keywords
preparation
benzoxazinorifamycin
processes
fluorobenzene
amino
Prior art date
Application number
BR112018014355-3A
Other languages
English (en)
Portuguese (pt)
Inventor
Bachmann Stephen
Maria Fantasia Serena
Jansen Michael
Koenig Stefan
LINGHU Xin
Rieth Sebastian
L. Segraves Nathaniel
Zogg Andreas
Original Assignee
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.)
Filing date
Publication date
Application filed by Genentech, Inc. filed Critical Genentech, Inc.
Publication of BR112018014355A2 publication Critical patent/BR112018014355A2/pt

Links

Classifications

    • 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
    • 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 [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/12—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from bacteria
    • C07K16/1267—Gram-positive bacteria
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/12—Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from bacteria
    • C07K16/1267—Gram-positive bacteria
    • C07K16/1271—Micrococcaceae (F); Staphylococcaceae (F), e.g. Staphylococcus (G)
    • 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)
  • 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)
BR112018014355-3A 2016-03-04 2017-03-03 processos para a preparação de f-benzoxazinorifamicina i e para a preparação de 2-amino-5-fluorobenzeno-1,3-diol iii BR112018014355A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662303556P 2016-03-04 2016-03-04
US62/303,556 2016-03-04
PCT/US2017/020711 WO2017152083A1 (en) 2016-03-04 2017-03-03 Process for the preparation of an antibody-rifamycin conjugate

Publications (1)

Publication Number Publication Date
BR112018014355A2 true BR112018014355A2 (pt) 2018-12-18

Family

ID=58361102

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018014355-3A BR112018014355A2 (pt) 2016-03-04 2017-03-03 processos para a preparação de f-benzoxazinorifamicina i e para a preparação de 2-amino-5-fluorobenzeno-1,3-diol iii

Country Status (13)

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

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108713020A (zh) 2016-03-04 2018-10-26 豪夫迈·罗氏有限公司 制备抗体-利福霉素缀合物的方法
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
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
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
CA3123607A1 (en) * 2018-12-21 2020-06-25 Regeneron Pharmaceuticals, Inc. Rifamycin analogs and antibody-drug conjugates thereof
CN118076353A (zh) * 2021-08-20 2024-05-24 罗格斯新泽西州立大学 双重靶向RNA聚合酶抑制剂：苯并噁嗪并-和螺-利福霉素与Nα-芳酰基-N-芳基-苯基丙氨酰胺的缀合物
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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GB877732A (en) 1958-08-12 1961-09-20 Lepetit Spa The antibiotic rifomycin, its components and methods of preparing same
US4690919A (en) 1984-01-04 1987-09-01 Kanegafuchi Kagaku Kogyo Kabushiki Kaisha Benzoxazinorifamycin derivative, process for preparing the same and antibacterial agent containing the same
JPS63183587A (ja) 1985-02-05 1988-07-28 Kanegafuchi Chem Ind Co Ltd ベンゾキサジノリフアマイシン誘導体
CA1304363C (en) 1988-11-01 1992-06-30 Takehiko Yamane 3'-hydroxybenzoxazinorifamycin derivative, process for preparing the same and antibacterial agent containing the same
US6322788B1 (en) 1998-08-20 2001-11-27 Stanley Arthur Kim Anti-bacterial antibodies and methods of use
ES2544527T3 (es) 2002-07-31 2015-09-01 Seattle Genetics, Inc. Conjugados de fármacos y su uso para tratar el cáncer, una enfermedad autoinmune o una enfermedad infecciosa
EP1663107A4 (en) 2003-08-22 2010-06-23 Activbiotics Pharma Llc RIFAMYCIN ANALOGS AND USES THEREOF
EP3434275A1 (en) 2003-11-06 2019-01-30 Seattle Genetics, Inc. Assay for cancer cells based on the use of auristatin conjugates with antibodies
WO2005062882A2 (en) 2003-12-23 2005-07-14 Activbiotics, Inc Rifamycin analogs and uses thereof
US7265107B2 (en) 2004-03-10 2007-09-04 Cumbre Pharmaceuticals Inc. Rifamycin C-11 oxime cyclo derivatives effective against drug-resistant microbes
ES2579805T3 (es) 2004-09-23 2016-08-16 Genentech, Inc. Anticuerpos y conjugados modificados por ingeniería genética con cisteína
CN101395259A (zh) 2005-12-14 2009-03-25 活跃生物药物学有限公司 利福霉素类似物及其应用
WO2008008480A2 (en) 2006-07-12 2008-01-17 Cumbre Pharmaceuticals Inc. Nitroheteroaryl-containing rifamycin derivatives
JP5669397B2 (ja) 2007-03-01 2015-02-12 シムフォゲン・アクティーゼルスカブＳｙｍｐｈｏｇｅｎ Ａ／Ｓ 同族抗体をクローニングするための方法
TW200902554A (en) 2007-05-08 2009-01-16 Genentech Inc Cysteine engineered anti-MUC16 antibodies and antibody drug conjugates
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WO2014142117A1 (ja) 2013-03-12 2014-09-18 全薬工業株式会社 抗ブドウ球菌抗体、その製造方法並びにその使用
MA38686A1 (fr) * 2013-05-31 2017-10-31 Genentech Inc Anticorps anti-acide téichoïque de la paroi cellulaire et conjugués associés
TWI692483B (zh) * 2013-05-31 2020-05-01 美商建南德克公司 抗壁磷壁酸抗體（ａｎｔｉ-ｗａｌｌ ｔｅｉｃｈｏｉｃ ａｃｉｄ ａｎｔｉｂｏｄｉｅｓ）及結合物
BR112015029754A2 (pt) 2013-05-31 2017-09-26 Genentech Inc anticorpos anti-teicoico da parede e conjugados
KR20170086536A (ko) * 2014-12-03 2017-07-26 제넨테크, 인크. 항-스타필로코커스 아우레우스 항체 리파마이신 접합체 및 이의 용도
JP6751393B2 (ja) * 2014-12-03 2020-09-02 ジェネンテック， インコーポレイテッド 抗ｓｔａｐｈｙｌｏｃｏｃｃｕｓ ａｕｒｅｕｓ抗体リファマイシン抱合体及びその使用
CN108713020A (zh) 2016-03-04 2018-10-26 豪夫迈·罗氏有限公司 制备抗体-利福霉素缀合物的方法

Also Published As

Publication number Publication date
US20170252457A1 (en) 2017-09-07
MX2018010491A (es) 2018-11-09
KR102204805B1 (ko) 2021-01-20
CA3012046C (en) 2020-11-10
AU2017228468B2 (en) 2019-12-05
CN108713020A (zh) 2018-10-26
US10336683B2 (en) 2019-07-02
US20190270695A1 (en) 2019-09-05
WO2017152083A1 (en) 2017-09-08
SG11201807537RA (en) 2018-09-27
CA3012046A1 (en) 2017-09-08
AR107800A1 (es) 2018-06-06
AU2017228468A1 (en) 2018-07-26
JP2020090506A (ja) 2020-06-11
KR20180118173A (ko) 2018-10-30
US10689325B2 (en) 2020-06-23
JP6705904B2 (ja) 2020-06-03
JP2019510740A (ja) 2019-04-18
EP3423457B1 (en) 2021-02-17
IL260465B (en) 2020-11-30
EP3423457A1 (en) 2019-01-09

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI N? 10196/2001, QUE MODIFICOU A LEI N? 9279/96, A CONCESS?O DA PATENTE EST? CONDICIONADA ? ANU?NCIA PR?VIA DA ANVISA. CONSIDERANDO A APROVA??O DOS TERMOS DO PARECER N? 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL N? 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVID?NCIAS CAB?VEIS.

B15K Others concerning applications: alteration of classification

Free format text: AS CLASSIFICACOES ANTERIORES ERAM: C07D 498/04 , C07C 215/78

Ipc: C07D 498/04 (2006.01), C07C 215/78 (2006.01), A61P

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Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B350 Update of information on the portal [chapter 15.35 patent gazette]
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements