WO2005081711A3 - Monomethylvaline compounds capable of conjugation to ligands - Google Patents

Monomethylvaline compounds capable of conjugation to ligands Download PDF

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Publication number
WO2005081711A3
WO2005081711A3 PCT/US2004/038392 US2004038392W WO2005081711A3 WO 2005081711 A3 WO2005081711 A3 WO 2005081711A3 US 2004038392 W US2004038392 W US 2004038392W WO 2005081711 A3 WO2005081711 A3 WO 2005081711A3
Authority
WO
WIPO (PCT)
Prior art keywords
ligands
conjugation
val
compounds capable
monomethylvaline compounds
Prior art date
Application number
PCT/US2004/038392
Other languages
French (fr)
Other versions
WO2005081711A2 (en
Inventor
Svetlana O Doronina
Peter D Senter
Brian E Toki
Allen J Ebens
Toni Beth Kline
Paul Polakis
Mark X Sliwkowski
Susan D Spencer
Original Assignee
Seattle Genetics Inc
Svetlana O Doronina
Peter D Senter
Brian E Toki
Allen J Ebens
Toni Beth Kline
Paul Polakis
Mark X Sliwkowski
Susan D Spencer
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34916511&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=WO2005081711(A3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority to ZA200603619A priority Critical patent/ZA200603619B/en
Priority to JP2006538564A priority patent/JP5020636B2/en
Priority to IN520DEN2012 priority patent/IN2012DN00520A/en
Priority to KR1020127014676A priority patent/KR101438983B1/en
Priority to EP16184693.6A priority patent/EP3120861B1/en
Priority to CA2543888A priority patent/CA2543888C/en
Priority to KR1020067008478A priority patent/KR101192496B1/en
Priority to AU2004316290A priority patent/AU2004316290C1/en
Priority to DK04821486.0T priority patent/DK1725249T3/en
Priority to BR122018071808A priority patent/BR122018071808B8/en
Priority to ES04821486.0T priority patent/ES2456325T3/en
Priority to EP18180055.8A priority patent/EP3434275A1/en
Priority to KR1020137025895A priority patent/KR101520209B1/en
Application filed by Seattle Genetics Inc, Svetlana O Doronina, Peter D Senter, Brian E Toki, Allen J Ebens, Toni Beth Kline, Paul Polakis, Mark X Sliwkowski, Susan D Spencer filed Critical Seattle Genetics Inc
Priority to CN200480039706.3A priority patent/CN1938046B/en
Priority to SI200432141T priority patent/SI1725249T1/en
Priority to BRPI0416028A priority patent/BRPI0416028B8/en
Priority to EP04821486.0A priority patent/EP1725249B1/en
Priority to PL04821486T priority patent/PL1725249T3/en
Priority to BR122018071968A priority patent/BR122018071968B8/en
Priority to EP20192962.7A priority patent/EP3858387A1/en
Priority to NZ547633A priority patent/NZ547633A/en
Publication of WO2005081711A2 publication Critical patent/WO2005081711A2/en
Priority to IL175247A priority patent/IL175247A/en
Publication of WO2005081711A3 publication Critical patent/WO2005081711A3/en
Priority to HK07105547.0A priority patent/HK1098071A1/en
Priority to IL215981A priority patent/IL215981A/en
Priority to IL244159A priority patent/IL244159A/en
Priority to IL250690A priority patent/IL250690A/en
Priority to IL255015A priority patent/IL255015B/en

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    • A61K38/08—Peptides having 5 to 11 amino acids
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    • A61K47/6851—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 the antibody targeting a determinant of a tumour cell
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    • 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
    • A61K47/6851—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 the antibody targeting a determinant of a tumour cell
    • A61K47/6855—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 the antibody targeting a determinant of a tumour cell the tumour determinant being from breast cancer cell
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    • 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
    • A61K47/6889—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
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/32—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
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    • A61K2039/505—Medicinal preparations containing antigens or antibodies comprising antibodies
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    • C—CHEMISTRY; METALLURGY
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    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/20—Immunoglobulins specific features characterized by taxonomic origin
    • C07K2317/24—Immunoglobulins specific features characterized by taxonomic origin containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y10—TECHNICAL SUBJECTS COVERED BY FORMER USPC
    • Y10T—TECHNICAL SUBJECTS COVERED BY FORMER US CLASSIFICATION
    • Y10T428/00—Stock material or miscellaneous articles
    • Y10T428/13—Hollow or container type article [e.g., tube, vase, etc.]

Abstract

Auristatin peptides, including MeVal-Val-Dil-Dap-Norephedrine (MMAE) and MeVal-Val-Dil-Dap-Phe (MMAF), were prepared and attached to Ligands through various linkers, including maleimidocaproyl-val-cit-PAB. The resulting ligand drug conjugates were active in vitro and in vivo.
PCT/US2004/038392 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands WO2005081711A2 (en)

Priority Applications (27)

Application Number Priority Date Filing Date Title
CN200480039706.3A CN1938046B (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands
SI200432141T SI1725249T1 (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands
JP2006538564A JP5020636B2 (en) 2003-11-06 2004-11-05 Monomethylvaline compounds that can be conjugated to a ligand
KR1020127014676A KR101438983B1 (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands
EP16184693.6A EP3120861B1 (en) 2003-11-06 2004-11-05 Intermediate for conjugate preparation comprising auristatin derivatives and a linker
CA2543888A CA2543888C (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands
KR1020067008478A KR101192496B1 (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands
AU2004316290A AU2004316290C1 (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands
DK04821486.0T DK1725249T3 (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugating to ligands.
BR122018071808A BR122018071808B8 (en) 2003-11-06 2004-11-05 conjugate
ES04821486.0T ES2456325T3 (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation with ligands
EP18180055.8A EP3434275A1 (en) 2003-11-06 2004-11-05 Assay for cancer cells based on the use of auristatin conjugates with antibodies
KR1020137025895A KR101520209B1 (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands
ZA200603619A ZA200603619B (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands
NZ547633A NZ547633A (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands
IN520DEN2012 IN2012DN00520A (en) 2003-11-06 2004-11-05
BRPI0416028A BRPI0416028B8 (en) 2003-11-06 2004-11-05 compound, compound conjugates, pharmaceutical composition and conjugate uses
EP04821486.0A EP1725249B1 (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands
PL04821486T PL1725249T3 (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands
BR122018071968A BR122018071968B8 (en) 2003-11-06 2004-11-05 antibody-drug conjugate, pharmaceutical composition, article of manufacture and use of an antibody-drug conjugate
EP20192962.7A EP3858387A1 (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands
IL175247A IL175247A (en) 2003-11-06 2006-04-27 Monomethylvaline compounds , uses thereof and conjugates, pharmaceutical compositions, assays and articles comprising the same
HK07105547.0A HK1098071A1 (en) 2003-11-06 2007-05-28 Monomethylvaline compounds capable of conjugation to ligands
IL215981A IL215981A (en) 2003-11-06 2011-10-27 Antibody-drug conjugate and an article of manufacture and pharmaceutical compositions comprising it
IL244159A IL244159A (en) 2003-11-06 2016-02-16 Monomethylvaline compounds capable of conjugation to ligands
IL250690A IL250690A (en) 2003-11-06 2017-02-20 Monomethylvaline compounds capable of conjugation to ligands
IL255015A IL255015B (en) 2003-11-06 2017-10-15 Monomethylvaline compounds capable of conjugation to ligands

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US51853403P 2003-11-06 2003-11-06
US60/518,534 2003-11-06
US55711604P 2004-03-26 2004-03-26
US60/557,116 2004-03-26
US59889904P 2004-08-04 2004-08-04
US60/598,899 2004-08-04
US62245504P 2004-10-27 2004-10-27
US60/622,455 2004-10-27

Publications (2)

Publication Number Publication Date
WO2005081711A2 WO2005081711A2 (en) 2005-09-09
WO2005081711A3 true WO2005081711A3 (en) 2006-11-23

Family

ID=34916511

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/038392 WO2005081711A2 (en) 2003-11-06 2004-11-05 Monomethylvaline compounds capable of conjugation to ligands

Country Status (20)

Country Link
US (21) US7498298B2 (en)
EP (8) EP2260858B1 (en)
JP (4) JP5020636B2 (en)
KR (3) KR101520209B1 (en)
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AU (1) AU2004316290C1 (en)
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