JP6560681B2 - 薬物結合体のためのスルホンアミド含有連結系 - Google Patents

薬物結合体のためのスルホンアミド含有連結系 Download PDF

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JP6560681B2
JP6560681B2 JP2016542987A JP2016542987A JP6560681B2 JP 6560681 B2 JP6560681 B2 JP 6560681B2 JP 2016542987 A JP2016542987 A JP 2016542987A JP 2016542987 A JP2016542987 A JP 2016542987A JP 6560681 B2 JP6560681 B2 JP 6560681B2
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amino
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JP2017502047A (ja
JP2017502047A5 (enExample
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シー．ウィンターズ ジェフリー
シー．ウィンターズ ジェフリー
エル．マンデル アレクサンダー
エル．マンデル アレクサンダー
マリー ジョゼー ブルケ エリス
マリー ジョゼー ブルケ エリス
アール．リッチ ジェイムズ
アール．リッチ ジェイムズ
ハン シャオ シー トム
ハン シャオ シー トム
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ザイムワークス インコーポレイティド
ザイムワークス インコーポレイティド
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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • 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
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • 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
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817—Toxins
    • 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
    • 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
    • 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
    • A61K47/6889—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide

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  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Toxicology (AREA)
  • Cell Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hematology (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
JP2016542987A 2013-12-27 2014-12-29 薬物結合体のためのスルホンアミド含有連結系 Active JP6560681B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2019132496A JP6908656B2 (ja) 2013-12-27 2019-07-18 薬物結合体のためのスルホンアミド含有連結系

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361921242P 2013-12-27 2013-12-27
US61/921,242 2013-12-27
US201462051899P 2014-09-17 2014-09-17
US62/051,899 2014-09-17
PCT/CA2014/000920 WO2015095953A1 (en) 2013-12-27 2014-12-29 Sulfonamide-containing linkage systems for drug conjugates

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JP2017502047A JP2017502047A (ja) 2017-01-19
JP2017502047A5 JP2017502047A5 (enExample) 2018-02-22
JP6560681B2 true JP6560681B2 (ja) 2019-08-14

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US (2) US11560422B2 (enExample)
EP (1) EP3086815B1 (enExample)
JP (2) JP6560681B2 (enExample)
KR (1) KR102384740B1 (enExample)
CN (1) CN106255513B (enExample)
AU (1) AU2014373574B2 (enExample)
CA (1) CA2935077C (enExample)
DK (1) DK3086815T3 (enExample)
ES (1) ES2916722T3 (enExample)
IL (1) IL246457B (enExample)
MX (1) MX384608B (enExample)
PL (1) PL3086815T3 (enExample)
RU (1) RU2729194C2 (enExample)
WO (1) WO2015095953A1 (enExample)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX368258B (es) 2013-03-15 2019-09-25 Zymeworks Inc Compuestos citotoxicos y antimitoticos y metodos de uso de los mismos.
BR112016015105A8 (pt) 2013-12-27 2018-04-24 Var2 Pharmaceuticals Aps conjugados var2csa-droga
KR102384740B1 (ko) 2013-12-27 2022-04-07 자임워크스 인코포레이티드 약물 접합체를 위한 설폰아마이드-함유 연결 시스템
AU2015318556C1 (en) * 2014-09-17 2021-01-07 Zymeworks Bc Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
EP3134128B1 (en) 2014-10-03 2019-06-05 Synaffix B.V. Sulfamide linker, conjugates thereof, and methods of preparation
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
WO2017096311A1 (en) 2015-12-04 2017-06-08 Seattle Genetics, Inc. Conjugates of quaternized tubulysin compounds
WO2017137456A1 (en) * 2016-02-08 2017-08-17 Synaffix B.V. Bioconjugates containing sulfamide linkers for use in treatment
WO2017137423A1 (en) 2016-02-08 2017-08-17 Synaffix B.V. Improved sulfamide linkers for use in bioconjugates
EP3413915A1 (en) * 2016-02-08 2018-12-19 Synaffix B.V. Antibody-conjugates with improved therapeutic index for targeting her2 tumours and method for improving therapeutic index of antibody-conjugates
JOP20170067B1 (ar) 2016-03-22 2021-08-17 Merck Sharp & Dohme معدِّلات مختلفة الشكل الفراغي لمستقبلات أسيتيل كولين النيكوتينية
US10517958B2 (en) 2016-10-04 2019-12-31 Zymeworks Inc. Compositions and methods for the treatment of platinum-drug resistant cancer
CA3072500A1 (en) 2017-08-10 2019-02-14 Sumitomo Dainippon Pharma Co., Ltd. Hemiasterlin derivatives and antibody-drug conjugates including same
PT3666787T (pt) 2017-08-10 2024-03-21 Sumitomo Pharma Co Ltd Conjugados anticorpo-fármaco que incluem um derivado da hemiasterlina
EP4253421A3 (en) * 2018-03-13 2024-01-03 Zymeworks BC Inc. Anti-her2 biparatopic antibody-drug conjugates and methods of use
US11084801B2 (en) 2018-05-29 2021-08-10 Intocell, Inc. Benzodiazepine derivatives and uses thereof
EA202191180A1 (ru) 2018-10-31 2021-09-21 Интоселл, Инк. Производные конденсированного гетероциклического бензодиазепина и их применение
WO2020094561A1 (en) 2018-11-09 2020-05-14 Synthon Biopharmaceuticals B.V. Filterable duocarmycin-containing antibody-drug conjugate compositions and related methods
MX2021006972A (es) 2018-12-11 2021-08-16 Sanofi Sa Conjugados de insulina.
JP7432531B2 (ja) * 2019-02-13 2024-02-16 住友ファーマ株式会社 システイン残基を有するヘミアスタリン誘導体
JP7479302B2 (ja) 2019-02-13 2024-05-08 住友ファーマ株式会社 ヘミアスタリン誘導体とその抗体薬物複合体
CN113024405A (zh) * 2019-12-25 2021-06-25 上海奥博生物医药技术有限公司 一种新的拉考沙胺杂质及其制备方法和用途
BR112022018002A2 (pt) * 2020-03-09 2022-11-08 Sigma Aldrich Co Llc Preparação eficiente de análogos de dolastatina e auristatina por meio de um intermediário comum
EP4577578A1 (en) 2022-08-22 2025-07-02 Abdera Therapeutics Inc. Dll3 binding molecules and uses thereof

Family Cites Families (155)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2036891B (en) 1978-12-05 1983-05-05 Windsor Smith C Change speed gear
CA1213229A (en) 1982-04-12 1986-10-28 Gary S. David Antibodies having dual specificities, their preparation and uses therefor
GB8308235D0 (en) 1983-03-25 1983-05-05 Celltech Ltd Polypeptides
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
JPS6147500A (ja) 1984-08-15 1986-03-07 Res Dev Corp Of Japan キメラモノクロ−ナル抗体及びその製造法
EP0173494A3 (en) 1984-08-27 1987-11-25 The Board Of Trustees Of The Leland Stanford Junior University Chimeric receptors by dna splicing and expression
GB8422238D0 (en) 1984-09-03 1984-10-10 Neuberger M S Chimeric proteins
JPS61134325A (ja) 1984-12-04 1986-06-21 Teijin Ltd ハイブリツド抗体遺伝子の発現方法
CA1282069C (en) 1985-09-12 1991-03-26 Damon L. Meyer Antibody complexes of hapten-modified diagnostic or therapeutic agents
JPS63501765A (ja) 1985-11-01 1988-07-21 インタ−ナショナル、ジェネティック、エンジニアリング　インコ−ポレ−テッド 抗体遺伝子のモジュ−ル組立体、それにより産生された抗体及び用途
US5225539A (en) 1986-03-27 1993-07-06 Medical Research Council Recombinant altered antibodies and methods of making altered antibodies
US4946778A (en) 1987-09-21 1990-08-07 Genex Corporation Single polypeptide chain binding molecules
US5053394A (en) 1988-09-21 1991-10-01 American Cyanamid Company Targeted forms of methyltrithio antitumor agents
FI102355B1 (fi) 1988-02-11 1998-11-30 Bristol Myers Squibb Co Menetelmä yhdistävän välikappaleen omaavien antrasykliini-immunokonjugaattien valmistamiseksi
US5028697A (en) 1988-08-08 1991-07-02 Eli Lilly And Company Cytotoxic antibody conjugates of hydrazide derivatized methotrexate analogs via simple organic linkers
US5094849A (en) 1988-08-08 1992-03-10 Eli Lilly And Company Cytotoxic antibody conjugates of hydrazide derivatized vinca analogs via simple organic linkers
US5006652A (en) 1988-08-08 1991-04-09 Eli Lilly And Company Intermediates for antibody-vinca drug conjugates
US5530101A (en) 1988-12-28 1996-06-25 Protein Design Labs, Inc. Humanized immunoglobulins
US5137877B1 (en) 1990-05-14 1996-01-30 Bristol Myers Squibb Co Bifunctional linking compounds conjugates and methods for their production
GB9017024D0 (en) 1990-08-03 1990-09-19 Erba Carlo Spa New linker for bioactive agents
DK0546073T3 (da) 1990-08-29 1998-02-02 Genpharm Int Frembringelse og anvendelse af transgene, ikke-humane dyr, der er i stand til at danne heterologe antistoffer
US5545806A (en) 1990-08-29 1996-08-13 Genpharm International, Inc. Ransgenic non-human animals for producing heterologous antibodies
US5625126A (en) 1990-08-29 1997-04-29 Genpharm International, Inc. Transgenic non-human animals for producing heterologous antibodies
US5661016A (en) 1990-08-29 1997-08-26 Genpharm International Inc. Transgenic non-human animals capable of producing heterologous antibodies of various isotypes
US5633425A (en) 1990-08-29 1997-05-27 Genpharm International, Inc. Transgenic non-human animals capable of producing heterologous antibodies
WO1993008829A1 (en) 1991-11-04 1993-05-13 The Regents Of The University Of California Compositions that mediate killing of hiv-infected cells
US5622929A (en) 1992-01-23 1997-04-22 Bristol-Myers Squibb Company Thioether conjugates
CA2140280A1 (en) 1992-08-17 1994-03-03 Avi J. Ashkenazi Bispecific immunoadhesins
US5635483A (en) 1992-12-03 1997-06-03 Arizona Board Of Regents Acting On Behalf Of Arizona State University Tumor inhibiting tetrapeptide bearing modified phenethyl amides
US6569834B1 (en) 1992-12-03 2003-05-27 George R. Pettit Elucidation and synthesis of antineoplastic tetrapeptide w-aminoalkyl-amides
NZ258882A (en) 1992-12-16 1997-06-24 Basf Ag Antineoplastic peptides and compositions thereof
US5780588A (en) 1993-01-26 1998-07-14 Arizona Board Of Regents Elucidation and synthesis of selected pentapeptides
US5556623A (en) 1993-03-30 1996-09-17 Eli Lilly And Company Antibody-drug conjugates
US6214345B1 (en) * 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
ATE282630T1 (de) 1993-10-01 2004-12-15 Teikoku Hormone Mfg Co Ltd Dolastatin-derivate
US5599902A (en) 1994-11-10 1997-02-04 Arizona Board Of Regents Acting On Behalf Of Arizona State University Cancer inhibitory peptides
US5663149A (en) 1994-12-13 1997-09-02 Arizona Board Of Regents Acting On Behalf Of Arizona State University Human cancer inhibitory pentapeptide heterocyclic and halophenyl amides
GB9508195D0 (en) 1995-04-20 1995-06-07 Univ British Columbia Novel biologically active compounds and compositions,their use and derivation
EP0867190B1 (en) 1995-05-10 2007-12-26 Kyowa Hakko Kogyo Co., Ltd. Cytotoxin complexes comprising dipeptides
JP4046354B2 (ja) 1996-03-18 2008-02-13 ボード オブ リージェンツ，ザ ユニバーシティ オブ テキサス システム 増大した半減期を有する免疫グロブリン様ドメイン
US6759509B1 (en) 1996-11-05 2004-07-06 Bristol-Myers Squibb Company Branched peptide linkers
CA2225325A1 (en) 1997-12-19 1999-06-19 The University Of British Columbia Hemiasterlin analogs
US8097648B2 (en) 1998-06-17 2012-01-17 Eisai R&D Management Co., Ltd. Methods and compositions for use in treating cancer
CA2359030A1 (en) 1999-01-28 2000-08-03 Chugai Seiyaku Kabushiki Kaisha Substituted phenethylamine derivatives
US6468522B1 (en) 1999-07-22 2002-10-22 University Of Medicine And Dentistry Of New Jersey Controlled release of thioamide moiety-containing therapeutic agents
US6323315B1 (en) 1999-09-10 2001-11-27 Basf Aktiengesellschaft Dolastatin peptides
US6756037B2 (en) 2000-03-31 2004-06-29 Enzon, Inc. Polymer conjugates of biologically active agents and extension moieties for facilitating conjugation of biologically active agents to polymeric terminal groups
AU2001275525B2 (en) 2000-06-14 2007-04-26 Medarex, Inc. Tripeptide prodrug compounds
TWI245034B (en) 2000-07-24 2005-12-11 Matsushita Electric Industrial Co Ltd Capacitor
US6884869B2 (en) 2001-04-30 2005-04-26 Seattle Genetics, Inc. Pentapeptide compounds and uses related thereto
US6737409B2 (en) 2001-07-19 2004-05-18 Hoffmann-La Roche Inc. Dolastatin 10 derivatives
WO2003026577A2 (en) 2001-09-24 2003-04-03 Seattle Genetics, Inc. P-amidobenzylethers in drug delivery agents
US6716821B2 (en) 2001-12-21 2004-04-06 Immunogen Inc. Cytotoxic agents bearing a reactive polyethylene glycol moiety, cytotoxic conjugates comprising polyethylene glycol linking groups, and methods of making and using the same
AU2003224644A1 (en) 2002-02-27 2003-09-09 The Government Of The United States Of America, Represented By The Secretary, Department Of Healtan Conjugates of ligand, linker and cytotoxic agent and related compositions and methods of use
US7064211B2 (en) 2002-03-22 2006-06-20 Eisai Co., Ltd. Hemiasterlin derivatives and uses thereof
RU2342399C2 (ru) * 2002-03-22 2008-12-27 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Производные гемиастерлина и их применение при лечении рака
AU2003263094A1 (en) 2002-04-23 2003-11-10 National Institutes Of Health Antileishmanial dinitroaniline sulfonamides with activity against parasite tubulin
ITMI20021391A1 (it) * 2002-06-25 2003-12-29 Nicox Sa Nitroderivati di inibitori della cicloossigenasi-2
DK1545613T3 (da) 2002-07-31 2011-11-14 Seattle Genetics Inc Auristatinkonjugater og deres anvendelse til behandling af cancer, en autoimmun sygdom eller en infektiøs sygdom
AU2003294210A1 (en) * 2002-07-31 2004-05-04 Seattle Genetics, Inc Anti-cd20 antibody-drug conjugates for the treatment of cancer and immune disorders
US7122189B2 (en) 2002-08-13 2006-10-17 Enzon, Inc. Releasable polymeric conjugates based on aliphatic biodegradable linkers
US7087229B2 (en) 2003-05-30 2006-08-08 Enzon Pharmaceuticals, Inc. Releasable polymeric conjugates based on aliphatic biodegradable linkers
ES2361739T3 (es) 2002-08-16 2011-06-21 Immunogen, Inc. Reticulantes con elevada reactividad y solubilidad y su uso en la preparación de conjugados para el suministro dirigido de fármacos de molécula pequeña.
AU2003299042A1 (en) 2002-09-20 2004-04-08 Wyeth Holdings Corporation Process for the synthesis of intermediates useful for the synthesis of tubulin inhibitors
WO2004026293A2 (en) * 2002-09-20 2004-04-01 Wyeth Holdings Corporation Hemiasterlin derivatives for treating resistant tumors
WO2004043493A1 (en) 2002-11-14 2004-05-27 Syntarga B.V. Prodrugs built as multiple self-elimination-release spacers
US20070026478A1 (en) 2002-11-21 2007-02-01 Wyeth Hemiasterlin affinity probes and their uses
US7332164B2 (en) 2003-03-21 2008-02-19 Enzon Pharmaceuticals, Inc. Heterobifunctional polymeric bioconjugates
US7390910B2 (en) 2003-08-08 2008-06-24 Wyeth Compounds for treating tumors
US7576206B2 (en) * 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
CA2538829A1 (en) 2003-09-15 2005-03-24 The University Of British Columbia Ceratamines a and b, and analogues, syntheses and pharmaceutical compositions thereof
ATE459364T1 (de) 2003-10-22 2010-03-15 Univ Johns Hopkins Verbesserte bakteriolyse-kombinationstherapie für die behandlung von tumoren
PL2489364T3 (pl) 2003-11-06 2015-06-30 Seattle Genetics Inc Związki monometylowaliny zdolne do sprzęgania do przeciwciał
US7078562B2 (en) 2004-01-19 2006-07-18 Mitsubishi Gas Chemical Company, Inc. Adamantane derivatives and resin compositions using the same as raw material
US20050175619A1 (en) 2004-02-05 2005-08-11 Robert Duffy Methods of producing antibody conjugates
EP1718667B1 (en) 2004-02-23 2013-01-09 Genentech, Inc. Heterocyclic self-immolative linkers and conjugates
JP4806680B2 (ja) 2004-05-19 2011-11-02 メダレックス インコーポレイテッド 自己犠牲リンカー及び薬剤複合体
CN114053429A (zh) * 2004-06-01 2022-02-18 健泰科生物技术公司 抗体-药物偶联物和方法
CN101039701A (zh) 2004-08-26 2007-09-19 尼古拉斯皮拉马尔印度有限公司 含有生物可裂解二硫化物连接物的前药和共药
EP1789091B1 (en) 2004-08-26 2010-08-25 Piramal Life Sciences Limited Prodrugs containing novel bio-cleavable linkers
US20090130136A1 (en) 2004-09-30 2009-05-21 Miller Louis H Chondroitin Sulphate a Binding Domains
ES2715776T3 (es) 2004-11-12 2019-06-06 Seattle Genetics Inc Auristatinas que tienen una unidad de ácido aminobenzoico en el extremo N
EP1817341A2 (en) 2004-11-29 2007-08-15 Seattle Genetics, Inc. Engineered antibodies and immunoconjugates
MX2007006430A (es) 2004-12-13 2007-07-19 Hoffmann La Roche Nueva composicion farmaceutica que contiene por lo menos un derivado de dolastatina-10.
WO2006067446A1 (en) 2004-12-22 2006-06-29 Astrazeneca Ab Pyridine carboxamide derivatives for use as anticancer agents
US7714016B2 (en) 2005-04-08 2010-05-11 Medarex, Inc. Cytotoxic compounds and conjugates with cleavable substrates
WO2007008603A1 (en) 2005-07-07 2007-01-18 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine side-chain modifications at the c-terminus
WO2007008848A2 (en) 2005-07-07 2007-01-18 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine carboxy modifications at the c-terminus
ES2649550T3 (es) 2005-07-18 2018-01-12 Seattle Genetics, Inc. Conjugados del enlazador fármaco de beta-glucurónido
WO2007018431A2 (en) 2005-08-05 2007-02-15 Syntarga B.V. Triazole-containing releasable linkers and conjugates comprising the same
NZ566982A (en) 2005-09-26 2011-06-30 Medarex Inc Duocarmycin drug conjugates
WO2007059404A2 (en) 2005-11-10 2007-05-24 Medarex, Inc. Duocarmycin derivatives as novel cytotoxic compounds and conjugates
WO2007103288A2 (en) 2006-03-02 2007-09-13 Seattle Genetics, Inc. Engineered antibody drug conjugates
TWI412367B (zh) 2006-12-28 2013-10-21 Medarex Llc 化學鏈接劑與可裂解基質以及其之綴合物
AR065404A1 (es) 2007-02-21 2009-06-03 Medarex Inc Conjugados farmaco-ligando, los que se unen a citotoxinas potentes, composicion farmaceutica que los contienen y su uso para retardar o detener el crecimiento de un tumor en un mamifero
US8476451B2 (en) 2007-07-20 2013-07-02 The Regents Of The University Of California Tubulysin D analogues
BRPI0817881A2 (pt) 2007-10-10 2015-03-31 Novartis Ag Compostos orgânicos e seus usos
WO2009059309A2 (en) 2007-11-01 2009-05-07 Panacea Pharmaceuticals, Inc. Furin-cleavable peptide linkers for drug-ligand conjugates
SG172737A1 (en) 2008-01-30 2011-07-28 Pieris Ag Muteins of tear lipocalin having affinity to human c-met receptor tyrosine kinaseand methods for obtaining the same
ES2647927T3 (es) 2008-03-18 2017-12-27 Seattle Genetics, Inc. Conjugados enlazadores del fármaco auriestatina
UA108598C2 (xx) 2008-04-30 2015-05-25 Високоефективні кон'югати та гідрофільні зшиваючі агенти (лінкери)
KR101892411B1 (ko) 2008-04-30 2018-08-27 이뮤노젠 아이엔씨 가교제 및 그 용도
EP4650441A2 (en) 2008-06-27 2025-11-19 Merus N.V. Antibody producing non-human mammals
GB2461546B (en) 2008-07-02 2010-07-07 Argen X Bv Antigen binding polypeptides
AU2009275358C1 (en) 2008-07-21 2015-09-24 Polytherics Limited Novel reagents and method for conjugating biological molecules
US20110166063A1 (en) 2008-09-19 2011-07-07 Nektar Therapeutics Polymer conjugates of therapeutic peptides
SI2865387T1 (sl) 2008-11-21 2019-10-30 Kobenhavns Univ University Of Copenhagen Primiranje imunskega odziva
US20110182850A1 (en) 2009-04-10 2011-07-28 Trixi Brandl Organic compounds and their uses
WO2010138719A1 (en) 2009-05-28 2010-12-02 Mersana Therapeutics, Inc. Polyal drug conjugates comprising variable rate-releasing linkers
US8394922B2 (en) 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
EP4036082A1 (en) 2009-08-28 2022-08-03 Arena Pharmaceuticals, Inc. Cannabinoid receptor modulators
RU2609021C2 (ru) * 2009-09-25 2017-01-30 Астеллас Фарма Инк. Замещенные соединения амида
AU2011235569B2 (en) 2010-03-29 2016-06-30 Zymeworks Bc Inc. Antibodies with enhanced or suppressed effector function
JP6040148B2 (ja) 2010-04-20 2016-12-07 ゲンマブ エー／エス ヘテロ二量体抗体Ｆｃ含有タンパク質およびその産生方法
JP5791707B2 (ja) 2010-06-10 2015-10-07 シアトル ジェネティックス， インコーポレイテッド 新規アウリスタチン誘導体およびその使用
WO2012032080A1 (en) 2010-09-07 2012-03-15 F-Star Biotechnologische Forschungs- Und Entwicklungsges.M.B.H Stabilised human fc
PH12012500542A1 (en) * 2010-09-24 2012-11-12 Astellas Pharma Inc Substituted amide compound
CA2930801C (en) 2010-11-05 2019-05-28 Rinat Neuroscience Corporation Engineered polypeptide conjugates and methods for making thereof using transglutaminase
WO2012113847A1 (en) 2011-02-25 2012-08-30 Lonza Ltd Branched linker for protein drug conjugates
AU2012222833B2 (en) 2011-03-03 2017-03-16 Zymeworks Inc. Multivalent heteromultimer scaffold design and constructs
WO2012123423A1 (de) 2011-03-16 2012-09-20 Bayer Pharma Aktiengesellschaft N-carboxyalkyl-auristatine und ihre verwendung
US9200034B2 (en) 2011-03-16 2015-12-01 Council Of Scientific & Industrial Research Oligopeptides and process for preparation thereof
CA2831307A1 (en) 2011-03-30 2012-10-04 Arizona Board Of Regents, For And On Behalf Of, Arizona State Universi Auristatin tyramine phosphate salts and auristatin aminoquinoline derivatives and prodrugs thereof
US20130066055A1 (en) 2011-04-21 2013-03-14 Bayer Intellectual Property Gmbh New binder-drug conjugates (adcs) and use thereof
SG195183A1 (en) 2011-05-27 2013-12-30 Ambrx Inc Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
KR102356286B1 (ko) 2011-05-27 2022-02-08 암브룩스, 인코포레이티드 비-천연 아미노산 연결된 돌라스타틴 유도체를 함유하는 조성물, 이를 수반하는 방법, 및 용도
CA2837840C (en) 2011-06-10 2020-08-04 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
UA117901C2 (uk) 2011-07-06 2018-10-25 Ґенмаб Б.В. Спосіб посилення ефекторної функції вихідного поліпептиду, його варіанти та їх застосування
US20130190248A1 (en) 2011-07-26 2013-07-25 Agensys, Inc. Substituted peptide analogs
JP2015504425A (ja) 2011-11-09 2015-02-12 アンサンブル・セラピューティクス アポトーシスのインヒビターを阻害するための大環状化合物
WO2013068874A1 (en) 2011-11-11 2013-05-16 Pfizer Inc. Antibody-drug conjugates
SI2780039T1 (en) 2011-11-17 2018-06-29 Pfizer Inc. Cytotoxic peptides and their conjugates between the antibody and the drug
US20130224228A1 (en) 2011-12-05 2013-08-29 Igenica, Inc. Antibody-Drug Conjugates and Related Compounds, Compositions, and Methods
US9061000B2 (en) 2012-01-19 2015-06-23 Chao-Han LAI Pharmacological treatment of aortic aneurysm development
EP2812024B1 (en) 2012-02-09 2018-04-11 Var2 Pharmaceuticals ApS Targeting of chondroitin sulfate glycans
JP6280103B2 (ja) 2012-05-15 2018-02-14 ソレント・セラピューティクス・インコーポレイテッドＳｏｒｒｅｎｔｏ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． 薬物コンジュゲート、コンジュゲーション方法およびその使用
CN104619349B (zh) 2012-06-07 2018-07-10 Ambrx公司 前列腺特异性膜抗原抗体药物结合物
JP6343609B2 (ja) 2012-06-19 2018-06-13 アンブルックス, インコーポレイテッドAmbrx, Inc. 抗ｃｄ７０抗体薬物複合体
KR102427777B1 (ko) * 2012-06-26 2022-08-01 델 마 파마슈티컬스 디안하이드로갈락티톨, 디아세틸디안하이드로갈락티톨, 디브로모둘시톨, 또는 그의 유사체 또는 유도체를 이용하여 유전학적 다형성이 있는 환자에 있어서 티로신-키나아제-억제제 내성 악성종양, ahi1 조절곤란 또는 돌연변이를 치료하는 방법
PL3210627T3 (pl) 2012-07-12 2023-04-17 Hangzhou Dac Biotech Co., Ltd Koniugaty zawierające cząsteczki wiążące się z komórką i środek cytotoksyczny
EP2917218B1 (en) 2012-11-09 2017-01-04 Ensemble Therapeutics Corporation Macrocyclic compounds for inhibition of inhibitors of apoptosis
US10131682B2 (en) 2012-11-24 2018-11-20 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and their uses for conjugation of drugs to a cell binding molecules
EP2740491A1 (en) 2012-12-05 2014-06-11 Institut Curie Conjugates of the B-subunit of shiga toxin for use as contrasting agents for imaging and therapy
EP2740493A1 (en) 2012-12-05 2014-06-11 Institut Curie Conjugates of the B-subunit of Shiga toxin for anticancer therapies
AU2013364065B2 (en) 2012-12-21 2018-10-04 Altrubio Inc. Hydrophilic self-immolative linkers and conjugates thereof
AU2014216539B2 (en) 2013-02-14 2017-03-23 Bristol-Myers Squibb Company Tubulysin compounds, methods of making and use
US9644028B2 (en) 2013-02-15 2017-05-09 Perseus Proteomics Inc. Anti-CDH3 humanized antibody, drug conjugate thereof, and use thereof
MX368258B (es) * 2013-03-15 2019-09-25 Zymeworks Inc Compuestos citotoxicos y antimitoticos y metodos de uso de los mismos.
US10836821B2 (en) 2013-10-15 2020-11-17 Sorrento Therapeutics, Inc. Drug-conjugates with a targeting molecule and two different drugs
KR20160098257A (ko) 2013-12-17 2016-08-18 노파르티스 아게 세포독성 펩티드 및 그의 접합체
BR112016015105A8 (pt) 2013-12-27 2018-04-24 Var2 Pharmaceuticals Aps conjugados var2csa-droga
KR102384740B1 (ko) 2013-12-27 2022-04-07 자임워크스 인코포레이티드 약물 접합체를 위한 설폰아마이드-함유 연결 시스템
AU2015318556C1 (en) 2014-09-17 2021-01-07 Zymeworks Bc Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
US10590165B2 (en) 2015-01-28 2020-03-17 Sorrento Therapeutics, Inc. Antibody drug conjugates
US10975112B2 (en) 2015-06-16 2021-04-13 Hangzhou Dac Biotech Co., Ltd. Linkers for conjugation of cell-binding molecules

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