SG11201807537RA - Process for the preparation of an antibody-rifamycin conjugate - Google Patents

Process for the preparation of an antibody-rifamycin conjugate

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Publication number
SG11201807537RA
SG11201807537RA SG11201807537RA SG11201807537RA SG11201807537RA SG 11201807537R A SG11201807537R A SG 11201807537RA SG 11201807537R A SG11201807537R A SG 11201807537RA SG 11201807537R A SG11201807537R A SG 11201807537RA SG 11201807537R A SG11201807537R A SG 11201807537RA
Authority
SG
Singapore
Prior art keywords
hoffmann
basel
roche
international
dna
Prior art date
Application number
SG11201807537RA
Inventor
Stephan Bachmann
Serena Maria Fantasia
Michael Jansen
Stefan Koenig
Xin Linghu
Sebastian Rieth
Nathaniel L Segraves
Andreas Zogg
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 SG11201807537RA publication Critical patent/SG11201807537RA/en

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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
    • 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Peptides Or Proteins (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

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property -, Organization IIIM141101110101011111 HO 11111011101111101010 111111111100111110 1111 III N International Bureau ... .jd .... ..or::,„, (10) International Publication Number (43) International Publication Date WO 2017/152083 Al 8 September 2017 (08.09.2017) WIP0 I PCT (51) International Patent Classification: (72) Inventors: BACHMANN, Stephan; c/o F. Hoffmann-La C07D 498/04 (2006.01) CO7C 215/78 (2006.01) Roche AG, Grenzacherstrasse 124, 4070 Basel (CH). FANTASIA, Serena Maria; c/o F. Hoffmann-La Roche (21) International Application Number: AG, Grenzacherstrasse 124, 4070 Basel (CH). JANSEN, PCT/US2017/020711 Michael; c/o F. Hoffmann-La Roche AG, Grenzacher- (22) International Filing Date: strasse 124, 4070 Basel (CH). KOENIG, Stefan; c/o Gen- 3 March 2017 (03.03.2017) entech, Inc., 1 DNA Way, South San Francisco, California 94080 (US). LINGHU, Xin; c/o Genentech, Inc., 1 DNA (25) Filing Language: English Way, South San Francisco, California 94080 (US). RI- (26) Publication Language: English ETH, Sebastian; c/o F. Hoffmann-La Roche AG, Gren- zacherstrasse 124, 4070 Basel (CH). SEGRAVES, Nath- (30) Priority Data: aniel L.; c/o Genentech, Inc., 1 DNA Way, South San 62/303,556 4 March 2016 (04.03.2016) US Francisco, California 94080 (US). ZOGG, Andreas; c/o F. (71) Applicant (for all designated States except AL, AT, BE, Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 BG, CH, CN, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, Basel (CH). HR, HU, IE, IN, IS, IT, LT, LU, LV, MC, MK, MT, NL, (74) Agents: ANDRUS, Alex et al.; Genentech, Inc., 1 DNA NO, PL, PT, RO, RS, SE, SI, SK, SM, TR): GENENTECH, Way, MS 49, South San Francisco, California 94080 (US). INC. [US/US]; 1 DNA Way, South San Francisco, Califor- nia 94080 (US). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, (71) Applicant (for AL, AT, BE, BG, CH, CN, CY, CZ, DE, DK, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, EE, ES, FI, FR, GB, GR, HR, HU, IE, IN, IS, IT, LT, LU, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, = LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, SM, TR only): F. HOFFMANN-LA ROCHE AG HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KH, KN, — [CH/CH]; Grenzacherstrasse 124, 4070 Basel (CH). KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, [Continued on next page] (54) Title: PROCESS FOR THE PREPARATION OF AN ANTIBODY-RIFAMYCIN CONJUGATE (57) : Processes are described for the preparation of = F-benzoxazinorifamycin I: and intermediates for conjugation with an antibody. — ' = = = Ulf. (.1 .o) — s Batch-reactor . \"I = nah Oxidant 02, I Rmn sv etc benroquinone, RIKA , . n g .1 1-1 0 0— o en GC HO ° Op (;,0,p N 0 0 0 Ho,, HN 0 kr) Il IN Il 0 N O WO 2017/152083 Al MIDEDIMOMOIDEIR0101311101011MMODEVOIMIE MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC , VN, ZA, ZM, ZW. GN, GQ, GW, KM, ML, MR, NE, SN, TD, Published: TG). (84) Designated States (unless otherwise indicated, for every with international search report (Art. 21(3)) kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, — before the expiration of the time limit for claims and to be republished in the event amendments (Rule 48.2(h)) amending of receipt the of
SG11201807537RA 2016-03-04 2017-03-03 Process for the preparation of an antibody-rifamycin conjugate SG11201807537RA (en)

Applications Claiming Priority (2)

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

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SG11201807537RA true SG11201807537RA (en) 2018-09-27

Family

ID=58361102

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SG11201807537RA SG11201807537RA (en) 2016-03-04 2017-03-03 Process for the preparation of an antibody-rifamycin conjugate

Country Status (13)

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

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US10336683B2 (en) 2016-03-04 2019-07-02 Genentech, Inc. Process for the preparation of an antibody-rifamycin conjugate
CN108047250B (en) * 2018-02-12 2020-08-14 丹诺医药(苏州）有限公司 Application of rifamycin-nitroimidazole coupled molecule
CN110687217B (en) * 2018-08-07 2021-04-23 中国科学院大连化学物理研究所 Method for measuring rifamycin S by liquid chromatography
CN110687218B (en) * 2018-08-07 2021-04-23 中国科学院大连化学物理研究所 Method for determining benzoxazine rifamycin by liquid chromatography
US11666658B2 (en) * 2018-12-21 2023-06-06 Regeneran Pharmaceuticals, Inc. Rifamycin analogs and antibody-drug conjugates thereof
CN118076353A (en) * 2021-08-20 2024-05-24 罗格斯新泽西州立大学 Dual targeted RNA polymerase inhibitors: conjugates of benzoxazino-and spiro-rifamycins with nα -aroyl-N-aryl-phenylalaninamides
CN114436864A (en) * 2022-02-17 2022-05-06 浙江鼎龙科技股份有限公司 Preparation method of 2-methyl-5-aminophenol

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Also Published As

Publication number Publication date
US20170252457A1 (en) 2017-09-07
KR20180118173A (en) 2018-10-30
JP2019510740A (en) 2019-04-18
WO2017152083A1 (en) 2017-09-08
AR107800A1 (en) 2018-06-06
JP6705904B2 (en) 2020-06-03
US20190270695A1 (en) 2019-09-05
AU2017228468B2 (en) 2019-12-05
EP3423457B1 (en) 2021-02-17
US10689325B2 (en) 2020-06-23
KR102204805B1 (en) 2021-01-20
AU2017228468A1 (en) 2018-07-26
CN108713020A (en) 2018-10-26
MX2018010491A (en) 2018-11-09
US10336683B2 (en) 2019-07-02
EP3423457A1 (en) 2019-01-09
CA3012046C (en) 2020-11-10
IL260465B (en) 2020-11-30
JP2020090506A (en) 2020-06-11
CA3012046A1 (en) 2017-09-08
BR112018014355A2 (en) 2018-12-18

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