KR102384740B1 - 약물 접합체를 위한 설폰아마이드-함유 연결 시스템 - Google Patents

약물 접합체를 위한 설폰아마이드-함유 연결 시스템 Download PDF

Info

Publication number
KR102384740B1
KR102384740B1 KR1020167019869A KR20167019869A KR102384740B1 KR 102384740 B1 KR102384740 B1 KR 102384740B1 KR 1020167019869 A KR1020167019869 A KR 1020167019869A KR 20167019869 A KR20167019869 A KR 20167019869A KR 102384740 B1 KR102384740 B1 KR 102384740B1
Authority
KR
South Korea
Prior art keywords
optionally substituted
amino
alkyl
group
compound
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
KR1020167019869A
Other languages
English (en)
Korean (ko)
Other versions
KR20160124751A (ko
Inventor
조프리 씨 윈터스
알렉산더 엘 맨델
엘리스 마리 조제 부르끄
제임스 알 리치
톰 한 샤오 시에
Original Assignee
자임워크스 인코포레이티드
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 자임워크스 인코포레이티드 filed Critical 자임워크스 인코포레이티드
Publication of KR20160124751A publication Critical patent/KR20160124751A/ko
Application granted granted Critical
Publication of KR102384740B1 publication Critical patent/KR102384740B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Toxicology (AREA)
  • Cell Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (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)
KR1020167019869A 2013-12-27 2014-12-29 약물 접합체를 위한 설폰아마이드-함유 연결 시스템 Active KR102384740B1 (ko)

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

Publications (2)

Publication Number Publication Date
KR20160124751A KR20160124751A (ko) 2016-10-28
KR102384740B1 true KR102384740B1 (ko) 2022-04-07

Family

ID=53477242

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020167019869A Active KR102384740B1 (ko) 2013-12-27 2014-12-29 약물 접합체를 위한 설폰아마이드-함유 연결 시스템

Country Status (14)

Country Link
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.
CA2935077C (en) 2013-12-27 2022-03-15 Geoffrey C. Winters Sulfonamide-containing linkage systems for drug conjugates
RU2714933C2 (ru) 2013-12-27 2020-02-21 Займворкс Инк. Конъюгаты var2csa-лекарственное средство
KR102494557B1 (ko) * 2014-09-17 2023-02-02 자임워크스 비씨 인코포레이티드 세포독성 및 항유사분열성 화합물, 그리고 이를 이용하는 방법
ES2740907T3 (es) 2014-10-03 2020-02-07 Synaffix Bv Enlazador de sulfamida, conjugados de los mismos y métodos de preparación
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
SG11201804268RA (en) 2015-12-04 2018-06-28 Seattle Genetics Inc Conjugates of quaternized tubulysin compounds
EP3413920A1 (en) * 2016-02-08 2018-12-19 Synaffix B.V. Bioconjugates containing sulfamide linkers for use in treatment
US11590239B2 (en) 2016-02-08 2023-02-28 Synaffix B.V. Antibody-conjugates with improved therapeutic index for targeting CD30 tumours and method for improving therapeutic index of antibody-conjugates
US10874746B2 (en) 2016-02-08 2020-12-29 Synaffix B.V. Sulfamide linkers for use in bioconjugates
LT3433234T (lt) 2016-03-22 2021-12-10 Merck Sharp & Dohme Corp. Nikotino acetilcholino receptorių alosteriniai moduliatoriai
US10517958B2 (en) 2016-10-04 2019-12-31 Zymeworks Inc. Compositions and methods for the treatment of platinum-drug resistant cancer
JP7202301B2 (ja) 2017-08-10 2023-01-11 住友ファーマ株式会社 ヘミアスタリン誘導体及びこれらの抗体薬物複合体
EP3666787B9 (en) 2017-08-10 2024-08-28 Sumitomo Pharma Co., Ltd. Antibody-drug conjugates including hemiasterlin derivative
IL277049B2 (en) 2018-03-13 2024-02-01 Zymeworks Bc Inc Conjugates of biparatopic anti-HER2 antibody and drug and methods of use
MX2020012718A (es) 2018-05-29 2021-02-16 Intocell Inc Derivados de benzodiazepinas novedosos y usos de los mismos.
BR112021008354A2 (pt) 2018-10-31 2021-08-03 Intocell, Inc. derivados de benzodiazepina heterocíclica fundida e usos dos mesmos
WO2020094561A1 (en) 2018-11-09 2020-05-14 Synthon Biopharmaceuticals B.V. Filterable duocarmycin-containing antibody-drug conjugate compositions and related methods
CA3122636A1 (en) 2018-12-11 2020-06-18 Sanofi Insulin analogs having reduced insulin receptor binding affinity
US12178879B2 (en) 2019-02-13 2024-12-31 Sumitomo Pharma Co., Ltd. Hemiasterlin derivative and antibody-drug conjugate thereof
CN113412271B (zh) 2019-02-13 2024-10-22 住友制药株式会社 具有半胱氨酸残基的哈米特林衍生物
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
CN115190882A (zh) * 2020-03-09 2022-10-14 西格马-奥尔德里奇有限责任公司 通过共同中间体有效制备多拉司他汀和奥里斯他汀类似物
EP4577578A1 (en) 2022-08-22 2025-07-02 Abdera Therapeutics Inc. Dll3 binding molecules and uses thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006027711A2 (en) 2004-08-26 2006-03-16 Nicholas Piramal India Limited Prodrugs and codrugs containing bio- cleavable disulfide linkers

Family Cites Families (154)

* 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
WO1987002671A1 (en) 1985-11-01 1987-05-07 International Genetic Engineering, Inc. Modular assembly of antibody genes, antibodies prepared thereby and use
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
IL106992A (en) 1988-02-11 1994-06-24 Bristol Myers Squibb Co Acylhydrazone derivatives of anthracycline and methods for their preparation
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
US5028697A (en) 1988-08-08 1991-07-02 Eli Lilly And Company Cytotoxic antibody conjugates of hydrazide derivatized methotrexate analogs via simple organic linkers
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
US5633425A (en) 1990-08-29 1997-05-27 Genpharm International, Inc. Transgenic non-human animals capable of producing heterologous antibodies
KR100272077B1 (ko) 1990-08-29 2000-11-15 젠팜인터내셔날,인코포레이티드 이종 항체를 생산할 수 있는 전이유전자를 가진 인간이외의 동물
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
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
ATE149570T1 (de) 1992-08-17 1997-03-15 Genentech Inc Bispezifische immunoadhesine
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
ATE196296T1 (de) 1992-12-16 2000-09-15 Basf Ag Dolastatin analog
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
DE69434136T2 (de) 1993-10-01 2005-12-01 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
US6103236A (en) 1995-05-10 2000-08-15 Kyowa Hakko Kogyo Co., Ltd. Toxin conjugates
WO1997034631A1 (en) 1996-03-18 1997-09-25 Board Of Regents, The University Of Texas System Immunoglobin-like domains with increased half lives
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
US7553969B1 (en) 1999-01-28 2009-06-30 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
US7214663B2 (en) 2000-06-14 2007-05-08 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
EP1531846A4 (en) 2002-02-27 2006-04-19 Us Gov Health & Human Serv Conjugates of ligand, linker and cytotoxic agent and related compositions and methods of use
AU2003228354B8 (en) 2002-03-22 2010-03-04 Eisai R&D Management Co., Ltd. Hemiasterlin derivatives and uses thereof in the treatment of cancer
US7064211B2 (en) 2002-03-22 2006-06-20 Eisai Co., Ltd. Hemiasterlin derivatives and uses thereof
EP1560574A4 (en) 2002-04-23 2010-01-13 Univ Ohio State ANTI-LEISHMANIA-DINITROANILINSULFONAMIDE WITH EFFECT AGAINST PARASITIC TUBULIN
ITMI20021391A1 (it) 2002-06-25 2003-12-29 Nicox Sa Nitroderivati di inibitori della cicloossigenasi-2
CA2494104A1 (en) * 2002-07-31 2004-04-22 Seattle Genetics, Inc. Anti-cd20 antibody-drug conjugates for the treatment of cancer and immune disorders
CA2802205C (en) 2002-07-31 2016-01-19 Seattle Genetics, Inc. Drug conjugates and their use for treating cancer, an autoimmune disease or an infectious disease
US7087229B2 (en) 2003-05-30 2006-08-08 Enzon Pharmaceuticals, Inc. Releasable polymeric conjugates based on aliphatic biodegradable linkers
US7122189B2 (en) 2002-08-13 2006-10-17 Enzon, Inc. Releasable polymeric conjugates based on aliphatic biodegradable linkers
JP2006500364A (ja) 2002-08-16 2006-01-05 イムノージェン インコーポレーテッド 高い反応性と溶解度を有する架橋剤および小分子薬物の標的化送達用コンジュゲートの調製におけるそれらの使用
WO2004026293A2 (en) 2002-09-20 2004-04-01 Wyeth Holdings Corporation Hemiasterlin derivatives for treating resistant tumors
MXPA05002874A (es) 2002-09-20 2005-05-27 Wyeth Corp Procedimiento para la sintesis de intermediarios utiles para la sintesis de inhibidores de tubulina.
CA2506080A1 (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
NZ583292A (en) 2003-11-06 2012-03-30 Seattle Genetics Inc Monomethylvaline compounds capable of conjugation to ligands
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
AU2005216251B2 (en) 2004-02-23 2011-03-10 Genentech, Inc. Heterocyclic self-immolative linkers and conjugates
MXPA06013413A (es) 2004-05-19 2007-01-23 Medarex Inc Enlazadores quimicos y conjugados de los mismos.
MXPA06014065A (es) * 2004-06-01 2007-01-31 Genentech Inc Conjugados de droga-anticuerpo y metodos.
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
WO2006039652A2 (en) 2004-09-30 2006-04-13 The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Chondroitin sulfate a binding domains
AU2005332660A1 (en) 2004-11-12 2006-12-14 Seattle Genetics, Inc. Auristatins having an aminobenzoic acid unit at the N terminus
AU2005316844A1 (en) 2004-11-29 2006-06-22 Seattle Genetics, Inc. Engineered antibodies and immunoconjugates
CA2590431A1 (en) 2004-12-13 2006-06-22 F. Hoffmann-La Roche Ag Novel pharmaceutical composition containing at least one dolastatin 10 derivative
CA2589773A1 (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
AU2006269422B2 (en) 2005-07-07 2012-12-06 Seagen Inc. Monomethylvaline compounds having phenylalanine side-chain modifications at the C-terminus
US8871720B2 (en) 2005-07-07 2014-10-28 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine carboxy modifications at the C-terminus
PT3248613T (pt) 2005-07-18 2022-03-16 Seagen Inc Conjugados de ligante de fármaco e beta-glucuronida
AU2006277117B2 (en) 2005-08-05 2013-01-10 Syntarga B.V. Triazole-containing releasable linkers and conjugates comprising the same
JP5290756B2 (ja) 2005-09-26 2013-09-18 メダレックス インコーポレイテッド 抗体−薬剤コンジュゲート及びその使用
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
JP2010519310A (ja) 2007-02-21 2010-06-03 メダレックス インコーポレイテッド 単一のアミノ酸を有する化学リンカーおよびその複合体
WO2009134279A1 (en) 2007-07-20 2009-11-05 The Regents Of The University Of California Tubulysin d analogues
JP5095824B2 (ja) 2007-10-10 2012-12-12 ノバルティス アーゲー スピロピロリジン類およびｈｃｖおよびｈｉｖ感染に対するその使用
WO2009059309A2 (en) 2007-11-01 2009-05-07 Panacea Pharmaceuticals, Inc. Furin-cleavable peptide linkers for drug-ligand conjugates
CA2713557C (en) 2008-01-30 2016-06-07 Pieris Ag Muteins of tear lipocalin having affinity to human c-met receptor tyrosine kinase and methods for obtaining the same
DK2842575T3 (da) 2008-03-18 2017-11-27 Seattle Genetics Inc Auristatin-lægemiddel-linker-konjugater
BRPI0911442A2 (pt) 2008-04-30 2019-03-12 Immunogen, Inc. conjugados potentes e ligantes hidrofílicos
CN102076717B (zh) 2008-04-30 2016-02-03 伊缪诺金公司 交联剂和它们的用途
RU2559524C2 (ru) 2008-06-27 2015-08-10 Мерюс Б.В. Продуцирующие антитела млекопитающие, не являющиеся человеком
GB2461546B (en) 2008-07-02 2010-07-07 Argen X Bv Antigen binding polypeptides
JP5622117B2 (ja) 2008-07-21 2014-11-12 ポリテリクスリミテッド 生体分子を接合するための新規な試薬及び方法
MX2011003117A (es) 2008-09-19 2011-04-21 Nektar Therapeutics Conjugados polimericos de peptidos terapeuticos.
BRPI0921927B8 (pt) 2008-11-21 2021-08-31 Koebenhavns Univ University Of Copenhagen Sensibilização de uma resposta imune
US20110182850A1 (en) 2009-04-10 2011-07-28 Trixi Brandl Organic compounds and their uses
US8524214B2 (en) 2009-05-28 2013-09-03 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
CN102596913B (zh) 2009-08-28 2016-11-09 艾尼纳制药公司 大麻素受体调节剂
MX2012003560A (es) 2009-09-25 2012-10-05 Astellas Pharma Inc Compuesto de amida sustituida.
RU2012145183A (ru) 2010-03-29 2014-05-10 Займворкс, Инк. Антитела с повышенной или пониженной эффекторной функцией
CN110066339A (zh) 2010-04-20 2019-07-30 根马布股份公司 含异二聚体抗体fc的蛋白及其制备方法
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
CA2813411C (en) 2010-11-05 2016-08-02 Rinat Neuroscience Corporation Engineered polypeptide conjugates and methods for making thereof using transglutaminase
EP2678037B1 (en) 2011-02-25 2014-12-03 Lonza Ltd Branched linker for protein drug conjugates
AU2012222833B2 (en) 2011-03-03 2017-03-16 Zymeworks Inc. Multivalent heteromultimer scaffold design and constructs
ES2543888T3 (es) 2011-03-16 2015-08-25 Seattle Genetics, Inc. N-carboxialquil-auristatinas y su utilización
US9200034B2 (en) 2011-03-16 2015-12-01 Council Of Scientific & Industrial Research Oligopeptides and process for preparation thereof
US9044518B2 (en) 2011-03-30 2015-06-02 Arizona Board Of Regents, A Body Corporate Of The State Of Arizona Acting For And On Behalf Of Arizona State University Auristatin tyramine phosphate salts and auristatin aminoquinoline derivatives and prodrugs thereof
TWI582112B (zh) 2011-04-21 2017-05-11 西雅圖遺傳學公司 新穎結合劑－藥物接合物（ＡＤＣｓ）及其用途（二）
US9796754B2 (en) 2011-05-27 2017-10-24 Ambrx, Inc. Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
ES2898854T3 (es) 2011-05-27 2022-03-09 Ambrx Inc Composiciones que contienen, métodos que implican, y usos de derivados de dolastatina enlazados con aminoácidos no naturales
KR101972303B1 (ko) 2011-06-10 2019-04-25 메르사나 테라퓨틱스, 인코포레이티드 단백질-중합체-약물 접합체
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
PT3327027T (pt) 2011-11-17 2021-02-15 Pfizer Péptidos citotóxicos e seus conjugados de anticorpos e fármacos
BR112014013526A8 (pt) 2011-12-05 2017-06-13 Igenica Biotherapeutics Inc conjugados de anticorpo-fármaco e compostos, composições e métodos relacionados
US9061000B2 (en) 2012-01-19 2015-06-23 Chao-Han LAI Pharmacological treatment of aortic aneurysm development
WO2013117705A1 (en) 2012-02-09 2013-08-15 Var2 Pharmaceuticals Aps Targeting of chondroitin sulfate glycans
EP2849797B1 (en) 2012-05-15 2019-12-18 Concortis Biosystems, Corp Drug-conjugates, conjugation methods, and uses thereof
EP2858676B1 (en) 2012-06-07 2019-03-13 Ambrx, Inc. Prostate-specific membrane antigen antibody drug conjugates
KR102190832B1 (ko) 2012-06-19 2020-12-15 암브룩스, 인코포레이티드 항cd70 항체 약물 컨쥬게이트
AU2013280644B2 (en) 2012-06-26 2018-08-02 Jeffrey A. BACHA Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or AHI1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
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
EP2922818B1 (en) 2012-11-24 2018-09-05 Hangzhou Dac Biotech Co., Ltd Hydrophilic linkers and their uses for conjugation of drugs to 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
US9089614B2 (en) 2012-12-21 2015-07-28 Bioalliance C.V. Hydrophilic self-immolative linkers and conjugates thereof
SI2956173T1 (sl) 2013-02-14 2017-06-30 Bristol-Myers Squibb Company Spojine tubulizina, postopki pridobivanja in uporaba
AU2014216959A1 (en) 2013-02-15 2015-10-01 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.
WO2015057876A1 (en) 2013-10-15 2015-04-23 Sorrento Therapeutics Inc. Drug-conjugates with a targeting molecule and two different drugs
EP3753578A1 (en) 2013-12-17 2020-12-23 Novartis AG Cytotoxic peptides and conjugates thereof
CA2935077C (en) 2013-12-27 2022-03-15 Geoffrey C. Winters Sulfonamide-containing linkage systems for drug conjugates
RU2714933C2 (ru) 2013-12-27 2020-02-21 Займворкс Инк. Конъюгаты var2csa-лекарственное средство
KR102494557B1 (ko) 2014-09-17 2023-02-02 자임워크스 비씨 인코포레이티드 세포독성 및 항유사분열성 화합물, 그리고 이를 이용하는 방법
EP3250238B1 (en) 2015-01-28 2022-06-01 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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006027711A2 (en) 2004-08-26 2006-03-16 Nicholas Piramal India Limited Prodrugs and codrugs containing bio- cleavable disulfide linkers

Also Published As

Publication number Publication date
CA2935077A1 (en) 2015-07-02
RU2729194C2 (ru) 2020-08-05
US20230265173A1 (en) 2023-08-24
JP6560681B2 (ja) 2019-08-14
ES2916722T3 (es) 2022-07-05
IL246457B (en) 2019-12-31
EP3086815A1 (en) 2016-11-02
RU2016130933A3 (enExample) 2018-09-13
KR20160124751A (ko) 2016-10-28
IL246457A0 (en) 2016-08-31
MX384608B (es) 2025-03-14
US20170029490A1 (en) 2017-02-02
JP2017502047A (ja) 2017-01-19
AU2014373574B2 (en) 2020-07-16
CN106255513B (zh) 2022-01-14
US11560422B2 (en) 2023-01-24
JP2019172710A (ja) 2019-10-10
EP3086815B1 (en) 2022-02-09
CA2935077C (en) 2022-03-15
WO2015095953A1 (en) 2015-07-02
PL3086815T3 (pl) 2022-06-13
AU2014373574A1 (en) 2016-07-14
RU2016130933A (ru) 2018-02-01
JP6908656B2 (ja) 2021-07-28
MX2016008444A (es) 2017-01-11
DK3086815T3 (da) 2022-05-23
EP3086815A4 (en) 2017-08-02
CN106255513A (zh) 2016-12-21

Similar Documents

Publication Publication Date Title
KR102384740B1 (ko) 약물 접합체를 위한 설폰아마이드-함유 연결 시스템
JP7204083B2 (ja) 細胞傷害性及び抗有糸分裂性化合物、ならびにその使用方法
HK1230510B (en) Sulfonamide-containing linkage systems for drug conjugates
HK1230510A1 (en) Sulfonamide-containing linkage systems for drug conjugates
HK1230981A1 (en) Sulfonamide-containing linkage systems for drug conjugates
HK40077461A (en) Cytotoxic and anti-mitotic compounds, and methods of using the same
HK1240251A1 (en) Cytotoxic and anti-mitotic compounds, and methods of using the same
HK1240597B (en) Cytotoxic and anti-mitotic compounds, and methods of using the same

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20160720

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20191227

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20210601

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20220112

GRNT Written decision to grant
PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20220405

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20220405

End annual number: 3

Start annual number: 1

PG1601 Publication of registration