BR112018069483A2 - pró-fármacos de medicamentos citotóxicos contendo grupos enzimaticamente cliváveis. - Google Patents

pró-fármacos de medicamentos citotóxicos contendo grupos enzimaticamente cliváveis.

Info

Publication number
BR112018069483A2
BR112018069483A2 BR112018069483A BR112018069483A BR112018069483A2 BR 112018069483 A2 BR112018069483 A2 BR 112018069483A2 BR 112018069483 A BR112018069483 A BR 112018069483A BR 112018069483 A BR112018069483 A BR 112018069483A BR 112018069483 A2 BR112018069483 A2 BR 112018069483A2
Authority
BR
Brazil
Prior art keywords
cleavable groups
prodrugs
enzymatically cleavable
cytotoxic drug
conjugates
Prior art date
Application number
BR112018069483A
Other languages
English (en)
Inventor
Sommer Anette
Rebstock Anne-Sophie
Stelte-Ludwig Beatrix
Terjung Carsten
Mahlert Christoph
Lerchen Hans-Georg
Marx Leo
DIETZ Lisa
Berndt Sandra
Anna Liesa Johannes Sarah
Greven Simone
Original Assignee
Bayer Pharma AG
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=58361030&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112018069483(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of BR112018069483A2 publication Critical patent/BR112018069483A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/335—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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
    • A61K47/6845—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 cytokine, e.g. growth factors, VEGF, TNF, a lymphokine or an interferon
    • 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
    • A61K47/6849—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 receptor, a cell surface antigen or a cell surface determinant
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Cell Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

pró-fármacos de medicamentos citotóxicos contendo grupos enzimaticamente cliváveis. a presente invenção refere-se a novos pró-fármacos ou conjugados de fórmula geral (ia) (ia) em que os fármacos citotóxicos, por exemplo inibidores da proteína do fuso de cinesina, são mascarados com grupos cliváveis por legumain e, assim, liberam o fármaco e uso desses pró-fármacos ou conjugados para tratamento e/ou prevenção de doenças e uso desses pro fármacos ou conjugados para produção de medicamentos para tratamento e/ou prevenção de doenças, especialmente de distúrbios hiperproliferativos e/ou angiogênicos, por exemplo, cânceres.
BR112018069483A 2016-03-24 2017-03-21 pró-fármacos de medicamentos citotóxicos contendo grupos enzimaticamente cliváveis. BR112018069483A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP16162400 2016-03-24
EP16205988 2016-12-21
PCT/EP2017/056684 WO2017162663A1 (de) 2016-03-24 2017-03-21 Prodrugs von cytotoxischen wirkstoffen mit enzymatisch spaltbaren gruppen

Publications (1)

Publication Number Publication Date
BR112018069483A2 true BR112018069483A2 (pt) 2019-07-30

Family

ID=58361030

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018069483A BR112018069483A2 (pt) 2016-03-24 2017-03-21 pró-fármacos de medicamentos citotóxicos contendo grupos enzimaticamente cliváveis.

Country Status (18)

Country Link
US (2) US11685714B2 (pt)
EP (1) EP3432934B1 (pt)
JP (1) JP7251981B2 (pt)
KR (1) KR20180123047A (pt)
CN (2) CN116059390A (pt)
AU (1) AU2017236431A1 (pt)
BR (1) BR112018069483A2 (pt)
CA (1) CA3018630A1 (pt)
CL (1) CL2018002699A1 (pt)
CO (1) CO2018010026A2 (pt)
IL (1) IL261758A (pt)
MX (1) MX2018011627A (pt)
PE (1) PE20181852A1 (pt)
RU (1) RU2018136778A (pt)
SG (2) SG10202008909VA (pt)
TW (1) TW201735954A (pt)
UY (1) UY37168A (pt)
WO (1) WO2017162663A1 (pt)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2017017172A (es) 2015-06-22 2018-02-23 Bayer Pharma AG Conjugados de ligador-principio activo (adcs) y conjugados de ligador-profarmaco (apdcs) con grupos enzimaticamente escindibles.
CA2990398A1 (en) 2015-06-23 2016-12-29 Bayer Pharma Aktiengesellschaft Antibody drug conjugates of kinesin spindel protein (ksp) inhibitors with anti-cd123-antibodies
AU2016282724A1 (en) 2015-06-23 2018-01-18 Bayer Pharma Aktiengesellschaft Targeted conjugates of KSP inhibitors
AU2017236431A1 (en) 2016-03-24 2018-09-27 Bayer Pharma Aktiengesellschaft Prodrugs of cytotoxic active agents having enzymatically cleavable groups
CA3027445A1 (en) 2016-06-15 2017-12-21 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies
JP7174704B2 (ja) * 2016-12-21 2022-11-17 バイエル・アクチエンゲゼルシヤフト 酵素開裂基を有する細胞毒性活性剤のプロドラッグ
EP3558387B1 (de) 2016-12-21 2021-10-20 Bayer Pharma Aktiengesellschaft Spezifische antikörper-wirkstoff-konjugate (adcs) mit ksp-inhibitoren
KR102556826B1 (ko) * 2016-12-21 2023-07-18 바이엘 파마 악티엔게젤샤프트 효소적으로 절단가능한 기를 갖는 항체 약물 접합체 (adc)
SG11202012608VA (en) * 2018-06-18 2021-02-25 Bayer Ag Binder/active agent conjugates directed against cxcr5, having enzymatically cleavable linkers and improved activity profile
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
CN110428870B (zh) * 2019-08-08 2023-03-21 苏州泓迅生物科技股份有限公司 一种预测抗体重链轻链配对概率的方法及其应用
CN113754541A (zh) * 2020-06-02 2021-12-07 深圳湾实验室 靶向eb病毒核抗原蛋白的小分子抑制剂、制备方法及其应用
WO2022167052A1 (en) * 2021-02-08 2022-08-11 Y-Mabs Therapeutics, Inc. Use of ascorbic acid as stabilizing agent for anti b7-h3 antibodies
EP4294453A1 (en) * 2021-02-16 2023-12-27 Glykos Finland Oy Linker-payloads and conjugates thereof
CN112979491B (zh) * 2021-02-24 2022-04-15 中国药科大学 一种包含过氧化氢/组织蛋白酶l响应性保护基的化合物及其应用
WO2024105205A1 (en) 2022-11-17 2024-05-23 Bayer Aktiengesellschaft Antibody-drug conjugates (a2dcs) with enzymatically cleavable groups

Family Cites Families (109)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5179017A (en) 1980-02-25 1993-01-12 The Trustees Of Columbia University In The City Of New York Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US4634665A (en) 1980-02-25 1987-01-06 The Trustees Of Columbia University In The City Of New York Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US4399216A (en) 1980-02-25 1983-08-16 The Trustees Of Columbia University Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US4474893A (en) 1981-07-01 1984-10-02 The University of Texas System Cancer Center Recombinant monoclonal antibodies
US4714681A (en) 1981-07-01 1987-12-22 The Board Of Reagents, The University Of Texas System Cancer Center Quadroma cells and trioma cells and methods for the production of same
US4510245A (en) 1982-11-18 1985-04-09 Chiron Corporation Adenovirus promoter system
GB8308235D0 (en) 1983-03-25 1983-05-05 Celltech Ltd Polypeptides
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
US5168062A (en) 1985-01-30 1992-12-01 University Of Iowa Research Foundation Transfer vectors and microorganisms containing human cytomegalovirus immediate-early promoter-regulatory DNA sequence
US4968615A (en) 1985-12-18 1990-11-06 Ciba-Geigy Corporation Deoxyribonucleic acid segment from a virus
DE8808645U1 (pt) 1988-07-06 1988-08-25 Hofer, Daniel, 7730 Villingen-Schwenningen, De
US4925648A (en) 1988-07-29 1990-05-15 Immunomedics, Inc. Detection and treatment of infectious and inflammatory lesions
US5601819A (en) 1988-08-11 1997-02-11 The General Hospital Corporation Bispecific antibodies for selective immune regulation and for selective immune cell binding
DK0479909T3 (da) 1989-06-29 1997-04-07 Medarex Inc Bispecifikke reagenser til AIDS-behandling
ES2133139T3 (es) 1989-10-20 1999-09-01 Medarex Inc Hetero anticuerpos biespecificos con funciones efectoras dobles.
US5270163A (en) 1990-06-11 1993-12-14 University Research Corporation Methods for identifying nucleic acid ligands
ATE175118T1 (de) 1990-10-05 1999-01-15 Medarex Inc Gezielte immunostimulierung mit bispezifischen stoffen
DE69128253T2 (de) 1990-10-29 1998-06-18 Chiron Corp Bispezifische antikörper, verfahren zu ihrer herstellung und deren verwendungen
HU219537B (hu) 1991-03-06 2001-05-28 Merck Patent Gmbh. Humanizált és kiméra monoklonális antitestek, azokat tartalmazó gyógyászati készítmények, az antitesteket kódoló szekvenciát tartalmazó expressziós vektorok, valamint eljárás az antitestek előállítására
DE69214709T2 (de) 1991-04-26 1997-02-20 Surface Active Ltd Neue Antikörper und Verfahren zu ihrer Verwendung
CA2131528C (en) 1992-03-05 2004-07-13 Philip E. Thorpe Methods and compositions for targeting the vasculature of solid tumors
DK0719859T3 (da) 1994-12-20 2003-10-20 Merck Patent Gmbh Anti-alfa V-integrin monoklonalt antistof
AU725609C (en) 1995-08-18 2002-01-03 Morphosys Ag Protein/(poly)peptide libraries
US6177078B1 (en) 1995-12-29 2001-01-23 Medvet Science Pty Limited Monoclonal antibody antagonists to IL-3
US6150508A (en) 1996-03-25 2000-11-21 Northwest Biotherapeutics, Inc. Monoclonal antibodies specific for the extracellular domain of prostate-specific membrane antigen
ES2260788T3 (es) 1996-03-25 2006-11-01 Medarex, Inc. Anticuerpos monoclonales especificos para el dominio estracelular de antigeno de membrana especifico de la prostata.
IL147638A0 (en) 1999-07-29 2002-08-14 Medarex Inc Human monoclonal antibodies to prostate specific membrane antigen
US7129332B2 (en) 2000-02-25 2006-10-31 The United States Of America As Represented By The Department Of Health And Human Services Anti-EGFRvIII scFvs with improved cytotoxicity and yield, immunotoxins based thereon, and methods of use thereof
JP2003533987A (ja) 2000-05-19 2003-11-18 イス ケミカル カンパニー リミテッド 表皮成長因子収容体に対するヒト化抗体
US7288390B2 (en) 2000-08-07 2007-10-30 Centocor, Inc. Anti-dual integrin antibodies, compositions, methods and uses
AUPR395801A0 (en) 2001-03-26 2001-04-26 Austin Research Institute, The Antibodies against cancer
WO2003083041A2 (en) 2002-03-22 2003-10-09 Biogen, Inc. Cripto-specific antibodies
DK1390389T3 (da) 2001-04-26 2009-04-20 Biogen Idec Inc Cripto-blokerende antistoffer og anvendelser deraf
DK2163256T3 (en) 2001-05-11 2015-12-07 Ludwig Inst For Cancer Res Ltd Specific binding proteins and use thereof
CZ200438A3 (cs) 2001-06-13 2004-06-16 Genmab A/S Název neuveden
US7595378B2 (en) 2001-06-13 2009-09-29 Genmab A/S Human monoclonal antibodies to epidermal growth factor receptor (EGFR)
EP3184539A3 (en) 2001-10-23 2017-09-13 PSMA Development Company L.L.C. Psma antibodies
NZ535425A (en) 2002-03-13 2008-05-30 Biogen Idec Inc Anti-alphavbeta6 antibodies
BR0311799A (pt) 2002-06-14 2005-05-10 Immunomedics Inc Anticorpo monoclonal hpam4
US20050059592A1 (en) 2003-04-11 2005-03-17 Kiener Peter A. EphA2 and hyperproliferative cell disorders
CN102675462A (zh) 2003-06-27 2012-09-19 艾默根佛蒙特有限公司 针对表皮生长因子受体的缺失突变体的抗体及其使用
BRPI0412879A8 (pt) 2003-07-21 2015-12-15 Immunogen Inc Conjugado citotóxico específico do antígeno ca6 e métodos de seu uso
DK1725249T3 (en) 2003-11-06 2014-03-17 Seattle Genetics Inc Monomethylvaline compounds capable of conjugating to ligands.
US20050142133A1 (en) 2003-12-03 2005-06-30 Xencor, Inc. Optimized proteins that target the epidermal growth factor receptor
US7767792B2 (en) 2004-02-20 2010-08-03 Ludwig Institute For Cancer Research Ltd. Antibodies to EGF receptor epitope peptides
ES2387809T3 (es) 2004-03-19 2012-10-02 Imclone Llc Anticuerpo frente al receptor del factor de crecimiento epidérmico humano
US7732131B2 (en) 2004-08-03 2010-06-08 Innate Pharma S.A. Therapeutic and diagnostic methods and compositions targeting 4Ig-B7-H3 and its counterpart NK cell receptor
ES2539126T3 (es) 2004-12-09 2015-06-26 Janssen Biotech, Inc. Inmunoconjugados anti integrina, métodos para su producción y su uso
DE602006013275D1 (de) 2005-01-07 2010-05-12 Diadexus Inc Ovr110-antikörperzusammensetzungen und verwendungsverfahren dafür
RU2492186C2 (ru) 2005-02-18 2013-09-10 Медарекс Ллс Выделенное анти-cd30 антитело (варианты), хозяйская клетка, способ получения химерного или гуманизированного варианта анти-cd30 антител (варианты), способ ингибирования роста клеток cd30+ и способ ингибирования роста опухолевых клеток, экспрессирующих cd30
PL1912677T3 (pl) 2005-06-20 2014-03-31 Psma Dev Company L L C Koniugaty przeciwciało PSMA-lek
RS52470B (en) 2005-08-24 2013-02-28 Immunogen Inc. PROCEDURE FOR PREPARATION OF PURE CONJUGATED MEDICINES
AU2006294663B2 (en) 2005-09-26 2012-03-22 Medarex, Inc. Human monoclonal antibodies to CD70
DOP2006000277A (es) 2005-12-12 2007-08-31 Bayer Pharmaceuticals Corp Anticuerpos anti mn y métodos para su utilización
WO2008004834A1 (en) 2006-07-06 2008-01-10 Isu Abxis Co., Ltd Humanized monoclonal antibody highly binding to epidermal growth factor receptor, egf receptor
US8323653B2 (en) 2006-09-08 2012-12-04 Medimmune, Llc Humanized anti-CD19 antibodies and their use in treatment of oncology, transplantation and autoimmune disease
EP1911766A1 (en) 2006-10-13 2008-04-16 Glycotope Gmbh Use of human cells of myeloid leukaemia origin for expression of antibodies
DK2073842T4 (da) 2006-09-10 2024-01-15 Glycotope Gmbh Anvendelse af humane celler af myloid leukæmioprindelse til udtrykkelse af anti-stoffer
EP1900750A1 (en) 2006-09-18 2008-03-19 Glycotope Gmbh Fully human high yield production system for improved antibodies
EP2064240A2 (en) 2006-09-18 2009-06-03 Xencor, Inc. Optimized antibodies that target hm1.24
EP1914242A1 (en) 2006-10-19 2008-04-23 Sanofi-Aventis Novel anti-CD38 antibodies for the treatment of cancer
ES2523915T5 (es) 2006-12-01 2022-05-26 Seagen Inc Agentes de unión a la diana variantes y usos de los mismos
WO2008140603A2 (en) 2006-12-08 2008-11-20 Macrogenics, Inc. METHODS FOR THE TREATMENT OF DISEASE USING IMMUNOGLOBULINS HAVING FC REGIONS WITH ALTERED AFFINITIES FOR FCγR ACTIVATING AND FCγR INHIBITING
WO2008092117A2 (en) 2007-01-25 2008-07-31 Xencor, Inc. Immunoglobulins with modifications in the fcr binding region
JP2010523478A (ja) 2007-03-22 2010-07-15 スローン − ケタリング・インスティテュート・フォー・キャンサー・リサーチ モノクローナル抗体８ｈ９の使用
NZ556142A (en) 2007-06-25 2009-11-27 Novartis Ag Animal remedy dispensing means
EP2545938A1 (en) 2007-08-03 2013-01-16 Abbott Biotherapeutics Corp. Therapeutic use of anti-tweak receptor antibodies
US9283276B2 (en) 2007-08-14 2016-03-15 Ludwig Institute For Cancer Research Ltd. Monoclonal antibody 175 targeting the EGF receptor and derivatives and uses thereof
WO2009026274A1 (en) 2007-08-22 2009-02-26 Medarex, Inc. Site-specific attachment of drugs or other agents to engineered antibodies with c-terminal extensions
UA117446C2 (uk) 2007-08-29 2018-08-10 Санофі-Авентіс Гуманізоване антитіло до cxcr5
ES2424745T3 (es) 2007-09-07 2013-10-08 Agensys, Inc. Anticuerpos y moléculas relacionadas que se unen a las proteínas 24P4C12
US8039597B2 (en) 2007-09-07 2011-10-18 Agensys, Inc. Antibodies and related molecules that bind to 24P4C12 proteins
DK2215121T3 (en) 2007-11-26 2016-05-02 Bayer Ip Gmbh ANTI-mesothelin ANTIBODIES AND USES THEREOF
AU2008331436A1 (en) 2007-12-06 2009-06-11 Csl Limited Method of inhibition of leukemic stem cells
PT2242772E (pt) 2007-12-26 2015-02-09 Biotest Ag Imunoconjugados dirigidos contra cd138 e as suas utilizações
EP2238168B8 (en) 2007-12-26 2014-07-23 Biotest AG Agents targeting cd138 and uses thereof
JP5555223B2 (ja) 2008-04-02 2014-07-23 マクロジェニクス，インコーポレーテッド ＨＥＲ２／ｎｅｕ特異的抗体およびその使用方法
CA2723973A1 (en) 2008-05-15 2009-11-19 Biogen Idec Ma Inc. Anti-fn14 antibodies and uses thereof
JP5719298B2 (ja) 2008-08-29 2015-05-13 シムフォゲン・アクティーゼルスカブＳｙｍｐｈｏｇｅｎ Ａ／Ｓ 組換え抗上皮増殖因子受容体抗体組成物
CN102325549A (zh) 2009-03-31 2012-01-18 罗氏格黎卡特股份公司 用人源化抗-EGFR IgG1抗体和伊立替康治疗癌症
US20100247484A1 (en) 2009-03-31 2010-09-30 Heinrich Barchet Combination therapy of an afucosylated antibody and one or more of the cytokines gm csf, m csf and/or il3
WO2010126066A1 (ja) 2009-04-27 2010-11-04 協和発酵キリン株式会社 血液腫瘍治療を目的とした抗IL-3Rα抗体
CN101959216B (zh) 2009-07-20 2014-06-18 电信科学技术研究院 一种分载波配置增强cell_fach的方法、系统和设备
AU2010303415B2 (en) 2009-10-07 2015-02-19 Macrogenics, Inc. Fc region-containing polypeptides that exhibit improved effector function due to alterations of the extent of fucosylation, and methods for their use
ES2619585T3 (es) 2010-03-22 2017-06-26 Lead Discovery Center Gmbh Derivados de triazina disustituidos farmacéuticamente activos
NZ604510A (en) 2010-08-17 2013-10-25 Csl Ltd Dilutable biocidal compositions and methods of use
EP2675440B1 (en) 2011-02-14 2020-03-25 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
JP6088488B2 (ja) 2011-04-21 2017-03-01 シアトル ジェネティックス， インコーポレイテッド 新規な結合剤−薬物複合体（ａｄｃ）およびそれらの使用
AR088941A1 (es) 2011-11-23 2014-07-16 Bayer Ip Gmbh Anticuerpos anti-fgfr2 y sus usos
WO2013092998A1 (en) 2011-12-23 2013-06-27 Innate Pharma Enzymatic conjugation of antibodies
ES2924722T3 (es) 2012-05-18 2022-10-10 Aptevo Res & Development Llc Unión de inmunofusión de scFv biespecífico (BIf) a CD123 y CD3
MX2015004757A (es) * 2012-10-16 2015-07-17 Endocyte Inc Conjugados de suministro de farmacos que contienen aminoacidos no naturales y metodo para usarlos.
JP6272230B2 (ja) 2012-10-19 2018-01-31 第一三共株式会社 親水性構造を含むリンカーで結合させた抗体−薬物コンジュゲート
CN105451773A (zh) 2013-03-15 2016-03-30 诺华股份有限公司 细胞增殖抑制剂及其缀合物
RU2016100892A (ru) 2013-06-14 2017-07-19 Байер Фарма Акциенгезельшафт Антитела против tweakr и их применение
RU2698697C2 (ru) 2013-12-23 2019-08-29 Байер Фарма Акциенгезельшафт Конъюгаты связующего (ADC) с ингибиторами KSP
CA2951049C (en) 2014-06-03 2023-01-03 Jiarui Biopharmaceuticals, Ltd. Peptide-drug conjugates
WO2015189143A1 (en) 2014-06-12 2015-12-17 Bayer Pharma Aktiengesellschaft Aglycosyl anti-tweakr antibodies and uses thereof
EP3233127A1 (de) 2014-12-15 2017-10-25 Bayer Pharma Aktiengesellschaft Antikörper-wirkstoff-konjugate (adcs) von ksp-inhibitoren mit aglycosylierten anti-tweakrantikörpern
MX2017017172A (es) * 2015-06-22 2018-02-23 Bayer Pharma AG Conjugados de ligador-principio activo (adcs) y conjugados de ligador-profarmaco (apdcs) con grupos enzimaticamente escindibles.
WO2016207104A1 (de) 2015-06-23 2016-12-29 Bayer Pharma Aktiengesellschaft Antikörper-wirkstoff-konjugate (adcs) von ksp-inhibitoren mit anti-b7h3-antikörpern
AU2016282724A1 (en) 2015-06-23 2018-01-18 Bayer Pharma Aktiengesellschaft Targeted conjugates of KSP inhibitors
CA2990398A1 (en) 2015-06-23 2016-12-29 Bayer Pharma Aktiengesellschaft Antibody drug conjugates of kinesin spindel protein (ksp) inhibitors with anti-cd123-antibodies
AU2017236431A1 (en) 2016-03-24 2018-09-27 Bayer Pharma Aktiengesellschaft Prodrugs of cytotoxic active agents having enzymatically cleavable groups
CA3027445A1 (en) 2016-06-15 2017-12-21 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies
EP3558387B1 (de) 2016-12-21 2021-10-20 Bayer Pharma Aktiengesellschaft Spezifische antikörper-wirkstoff-konjugate (adcs) mit ksp-inhibitoren
KR102556826B1 (ko) 2016-12-21 2023-07-18 바이엘 파마 악티엔게젤샤프트 효소적으로 절단가능한 기를 갖는 항체 약물 접합체 (adc)
JP7174704B2 (ja) 2016-12-21 2022-11-17 バイエル・アクチエンゲゼルシヤフト 酵素開裂基を有する細胞毒性活性剤のプロドラッグ
SG11202012608VA (en) 2018-06-18 2021-02-25 Bayer Ag Binder/active agent conjugates directed against cxcr5, having enzymatically cleavable linkers and improved activity profile

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CN116059390A (zh) 2023-05-05
US11685714B2 (en) 2023-06-27
TW201735954A (zh) 2017-10-16
JP7251981B2 (ja) 2023-04-04
RU2018136778A (ru) 2020-04-24
EP3432934A1 (de) 2019-01-30
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