EA202190059A1 - Конъюгаты связующее-активное средство, направленные против cxcr5, имеющие ферментативно расщепляемые линкеры и улучшенный профиль активности - Google Patents

Конъюгаты связующее-активное средство, направленные против cxcr5, имеющие ферментативно расщепляемые линкеры и улучшенный профиль активности

Info

Publication number
EA202190059A1
EA202190059A1 EA202190059A EA202190059A EA202190059A1 EA 202190059 A1 EA202190059 A1 EA 202190059A1 EA 202190059 A EA202190059 A EA 202190059A EA 202190059 A EA202190059 A EA 202190059A EA 202190059 A1 EA202190059 A1 EA 202190059A1
Authority
EA
Eurasian Patent Office
Prior art keywords
binder
crawler
linkers
enzymatically
improved activity
Prior art date
Application number
EA202190059A
Other languages
English (en)
Inventor
Сара Анна Лиеса Йоханнес
Ханс-Георг Лерхен
Беатрикс Стелте-Людвиг
Паскаль Лежен
Ханна Йориссен
Кристоф Махлерт
Зимоне Гревен
Стефан Марш
Стефани Хаммер
Original Assignee
Байер Акциенгезельшафт
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 Байер Акциенгезельшафт filed Critical Байер Акциенгезельшафт
Publication of EA202190059A1 publication Critical patent/EA202190059A1/ru

Links

Classifications

    • 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
    • A61K47/6889—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61K47/6849—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
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A61K47/6867—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from a cell of a blood cancer
    • 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
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2866—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for cytokines, lymphokines, interferons
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/40—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against enzymes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/70—Immunoglobulins specific features characterized by effect upon binding to a cell or to an antigen
    • C07K2317/77—Internalization into the cell
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2317/00—Immunoglobulins specific features
    • C07K2317/90—Immunoglobulins specific features characterized by (pharmaco)kinetic aspects or by stability of the immunoglobulin
    • C07K2317/92—Affinity (KD), association rate (Ka), dissociation rate (Kd) or EC50 value

Landscapes

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

Abstract

Настоящее изобретение относится к новым конъюгатам связующее-лекарственное средство с улучшенными свойствами, к активным метаболитам указанных ADC и к процессам их получения. Настоящее изобретение, в частности, относится к конъюгатам антитело-лекарственное средство (ADC) с антителом против CXCR5 и выбранными ингибиторами KSP. Настоящее изобретение, кроме того, относится к применению указанных конъюгатов для лечения и/или предупреждения заболеваний и к применению указанных конъюгатов для получения медицинских препаратов для лечения и/или предупреждения заболеваний, в частности гиперпролиферативных и/или ангиогенных заболеваний, таких как, например, раковые заболевания.
EA202190059A 2018-06-18 2019-06-13 Конъюгаты связующее-активное средство, направленные против cxcr5, имеющие ферментативно расщепляемые линкеры и улучшенный профиль активности EA202190059A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP18178299 2018-06-18
PCT/EP2019/065517 WO2019243159A1 (de) 2018-06-18 2019-06-13 Gegen cxcr5 gerichtete binder-wirkstoff-konjugate mit enzymatisch spaltbaren linkern und verbessertem wirkungsprofil

Publications (1)

Publication Number Publication Date
EA202190059A1 true EA202190059A1 (ru) 2021-04-21

Family

ID=62705502

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202190059A EA202190059A1 (ru) 2018-06-18 2019-06-13 Конъюгаты связующее-активное средство, направленные против cxcr5, имеющие ферментативно расщепляемые линкеры и улучшенный профиль активности

Country Status (13)

Country Link
US (1) US20210275686A1 (ru)
EP (1) EP3806908A1 (ru)
JP (1) JP2021527640A (ru)
KR (1) KR20210033470A (ru)
CN (1) CN112601553A (ru)
AU (1) AU2019289506A1 (ru)
BR (1) BR112020025718A2 (ru)
CA (1) CA3103327A1 (ru)
EA (1) EA202190059A1 (ru)
IL (1) IL279400A (ru)
MX (1) MX2020013832A (ru)
SG (1) SG11202012608VA (ru)
WO (1) WO2019243159A1 (ru)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10973923B2 (en) 2015-06-23 2021-04-13 Bayer Pharma Aktiengesellschaft Site specific homogeneous with KSP inhibitors
KR20180123047A (ko) 2016-03-24 2018-11-14 바이엘 파마 악티엔게젤샤프트 효소적으로 절단가능한 기를 갖는 세포독성 활성제의 전구약물
EP3919518A1 (en) 2016-06-15 2021-12-08 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies
PE20191235A1 (es) 2016-12-21 2019-09-11 Bayer Pharma AG Conjugados de ligando-farmaco (adcs) con grupos escindibles enzimaticamente
EP3558387B1 (de) 2016-12-21 2021-10-20 Bayer Pharma Aktiengesellschaft Spezifische antikörper-wirkstoff-konjugate (adcs) mit ksp-inhibitoren
TW202216771A (zh) 2020-06-26 2022-05-01 德商拜耳廠股份有限公司 用於治療應用之ccr8抗體
AU2022210371A1 (en) 2021-01-22 2023-07-20 Bayer Aktiengesellschaft Lrrc15 antibodies and conjugates thereof

Family Cites Families (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
US4474893A (en) 1981-07-01 1984-10-02 The University of Texas System Cancer Center Recombinant monoclonal antibodies
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
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
GB8905592D0 (en) 1989-03-10 1989-04-19 Gkn Technology Ltd Automatic length adjuster
WO1991000360A1 (en) 1989-06-29 1991-01-10 Medarex, Inc. Bispecific reagents for aids therapy
US5270163A (en) 1990-06-11 1993-12-14 University Research Corporation Methods for identifying nucleic acid ligands
WO1992005793A1 (en) 1990-10-05 1992-04-16 Medarex, Inc. Targeted immunostimulation with bispecific reagents
ATE160379T1 (de) 1990-10-29 1997-12-15 Chiron Corp Bispezifische antikörper, verfahren zu ihrer herstellung und deren verwendungen
AP257A (en) 1991-04-26 1993-06-03 Surface Active Ltd A method of releasing an antigen from an antibody and methods for their use in diagnosis and therapy.
ATE239506T1 (de) 1992-03-05 2003-05-15 Univ Texas Verwendung von immunokonjugate zur diagnose und/oder therapie der vaskularisierten tumoren
WO1997008320A1 (en) 1995-08-18 1997-03-06 Morphosys Gesellschaft Für Proteinoptimierung Mbh Protein/(poly)peptide libraries
AU2002365195A1 (en) 2001-07-12 2003-07-30 Incyte Genomics, Inc. Intracellular signaling molecules
SG114505A1 (en) 2001-10-17 2005-09-28 First Cube Pte Ltd System and method for facilitating delivery and return service
EP1458726B1 (en) 2001-12-06 2009-07-15 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2004100873A2 (en) 2003-05-07 2004-11-25 Cytokinetics, Inc. Compounds, compositions, and methods
BR122018071968B8 (pt) 2003-11-06 2021-07-27 Seattle Genetics Inc conjugado de anticorpo-droga, composição farmacêutica, artigo de manufatura e uso de um conjugado de anticorpo-droga
KR20060127413A (ko) 2003-11-25 2006-12-12 카이론 코포레이션 항암제로서의 퀴나졸리논 화합물
US7662581B1 (en) 2003-12-18 2010-02-16 Novartis Vaccines And Diagnostics, Inc. Eg5 co-crystals
KR101170925B1 (ko) 2004-06-18 2012-08-07 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 암 치료용 키네신 방추 단백질 (ｋｓｐ) 억제제로서의ｎ-(1-(1-벤질-4-페닐-1ｈ-이미다졸-2-일)-2,2-디메틸프로필)벤자미드 유도체 및 관련 화합물
US7449486B2 (en) 2004-10-19 2008-11-11 Array Biopharma Inc. Mitotic kinesin inhibitors and methods of use thereof
US20100093767A1 (en) 2004-12-03 2010-04-15 Takeda San Diego, Inc. Mitotic Kinase Inhibitors
TW200800951A (en) 2005-08-09 2008-01-01 Novartis Ag Substituted imidazole compounds as KSP inhibitors
DOP2006000277A (es) 2005-12-12 2007-08-31 Bayer Pharmaceuticals Corp Anticuerpos anti mn y métodos para su utilización
JP2010515687A (ja) 2007-01-05 2010-05-13 ノバルティス アーゲー キネシンスピンドルタンパク質阻害剤（ｅｇ−５）としてのイミダゾール誘導体
SI2195023T1 (en) * 2007-08-29 2018-07-31 Sanofi Humanized anti-CXCR5 antibodies, their derivatives and their uses
WO2012171020A1 (en) 2011-06-10 2012-12-13 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
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
AU2014261398B2 (en) 2013-05-02 2019-08-29 Ares Trading S.A Monoclonal antibody directed against CXCR5
ES2815098T3 (es) 2013-12-23 2021-03-29 Bayer Pharma AG Conjugados de ligadores (ADCs) con inhibidores de KSP
CN107635586B (zh) 2014-12-15 2021-09-24 拜耳医药股份有限公司 Ksp抑制剂与无糖基化抗-tweakr抗体的抗体-药物缀合物(adc)
CN114917361A (zh) * 2015-06-22 2022-08-19 拜耳医药股份有限公司 具有酶可裂解基团的抗体药物缀合物（adc）和抗体前药缀合物（apdc）
KR20180123047A (ko) * 2016-03-24 2018-11-14 바이엘 파마 악티엔게젤샤프트 효소적으로 절단가능한 기를 갖는 세포독성 활성제의 전구약물
PE20191235A1 (es) * 2016-12-21 2019-09-11 Bayer Pharma AG Conjugados de ligando-farmaco (adcs) con grupos escindibles enzimaticamente

Also Published As

Publication number Publication date
AU2019289506A1 (en) 2021-02-04
WO2019243159A1 (de) 2019-12-26
BR112020025718A2 (pt) 2021-04-06
KR20210033470A (ko) 2021-03-26
US20210275686A1 (en) 2021-09-09
MX2020013832A (es) 2021-03-25
JP2021527640A (ja) 2021-10-14
SG11202012608VA (en) 2021-02-25
EP3806908A1 (de) 2021-04-21
IL279400A (en) 2021-01-31
CN112601553A (zh) 2021-04-02
CA3103327A1 (en) 2019-12-26

Similar Documents

Publication Publication Date Title
EA202190059A1 (ru) Конъюгаты связующее-активное средство, направленные против cxcr5, имеющие ферментативно расщепляемые линкеры и улучшенный профиль активности
MX2023009205A (es) Conjugados de ligando-farmaco (adcs) con grupos escindibles enzimaticamente.
PH12019502545A1 (en) Anti-cdh6 antibody and anti-cdh6 antibody-drug conjugate
SG11201906554RA (en) Anti-gpr20 antibody and anti-gpr20 antibody-drug conjugate
MX2016008013A (es) Conjugados de farmacos anticuerpo (adcs) con inhibidores de ksp.
WO2020056198A3 (en) Substituted benzazepine compounds, conjugates, and uses thereof
MX2019012464A (es) Terapia combinada con un conjugado de anticuerpo y farmaco anti-axl.
MX2021010453A (es) Conjugados anticuerpo-farmaco que comprenden anticuerpos contra dlk1 humana y uso de estos.
MX2016001640A (es) Composicion farmaceutica para el tratamiento y/o prevencion del cancer.
MX2018011627A (es) Profarmacos de farmacos citotoxicos que tienen grupos enzimaticamente escindibles.
MX2017017138A (es) Conjugados homogeneos especificos de sitio con inhibidores de ksp.
EA202191175A1 (ru) Сконструированные с цистеином конъюгаты антитело-лекарственное средство, содержащие пептидсодержащие линкеры
EA201892541A1 (ru) Гуманизированные анти-il-1r3 антитела
CO2022002622A2 (es) Anticuerpos anti-cd73 y composiciones
EA202193309A1 (ru) Конъюгаты антитело к тканевому фактору-лекарственное средство и связанные способы
EA201991196A1 (ru) Претерпевшие самосборку диблок-сополимеры, состоящие из pegmema и несущих лекарственное средство полимерных сегментов
EA202091533A1 (ru) Способы лечения диабета, гепатита и/или воспалительного заболевания печени
WO2017136731A8 (en) Rapaglutins, novel inhibitors of glut and use thereof
PH12020551556A1 (en) Drug conjugates of cmet monoclonal binding agents, and uses thereof
PH12020500417A1 (en) Anti-efgr antibody drug conjugates (adc) and uses thereof
EA202090741A1 (ru) Конъюгаты антитела к тканевому фактору и лекарственного средства и их применение в лечении рака
MX2022003243A (es) Conjugados anticuerpo-farmaco anti-ptcra y usos de los mismos.
MX2019008773A (es) Derivados de caliqueamicina y conjugados anticuerpo-farmaco de los mismos.
MX2022014231A (es) Conjugados de anticuerpo-farmaco que se enfocan a la uparap.
MX2022016232A (es) Marcadores para uso en metodos para tratar canceres con conjugados de anticuerpo y farmaco (adc).