Nothing Special   »   [go: up one dir, main page]

UY37168A - Profármacos de principios activos citotóxicos con grupos enzimáticamente escindibles - Google Patents

Profármacos de principios activos citotóxicos con grupos enzimáticamente escindibles

Info

Publication number
UY37168A
UY37168A UY0001037168A UY37168A UY37168A UY 37168 A UY37168 A UY 37168A UY 0001037168 A UY0001037168 A UY 0001037168A UY 37168 A UY37168 A UY 37168A UY 37168 A UY37168 A UY 37168A
Authority
UY
Uruguay
Prior art keywords
groups
active
scindible
propharms
cytotox
Prior art date
Application number
UY0001037168A
Other languages
English (en)
Inventor
Hans-Georg Lerchen Dr
Anne-Sophie Rebstock Dra
Leo Marx
Sarah Wagner Dra
Beatrix Stelte-Ludwig Dra
Lisa Dietz Dra
Carsten Terjung Dr
Christoph Mahlert Dr
Simone Greven
Anette Sommer Dr
Sandra Berndt Dra
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=UY37168(A) "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 UY37168A publication Critical patent/UY37168A/es

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
    • A61K47/6801—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
    • A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
    • 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
    • A61K47/68035—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a pyrrolobenzodiazepine
    • 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
    • A61K47/68037—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a camptothecin [CPT] or derivatives
    • 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
    • A61K47/6805—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a vinca alkaloid
    • 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)
  • Cell Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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

La invención se refiere a nuevos profármacos o bien conjugados de la fórmula general (Ia) en los que se enmascaran los principios activos citotóxicos tales como, por ejemplo, inhibidores de la proteína del huso de la quinesina con grupos escindibles por legumaína y así liberan el principio activo, así como al uso de estos profármacos o conjugados para el tratamiento y/o la prevención de enfermedades, así como al uso de estos profármacos o bien conjugados para la preparación de medicamentos para el tratamiento y/o la prevención de enfermedades, en especial de enfermedades hiperproliferativas y/o angiogénicas tales como, por ejemplo, enfermedades cancerosas.
UY0001037168A 2016-03-24 2017-03-24 Profármacos de principios activos citotóxicos con grupos enzimáticamente escindibles UY37168A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP16162400 2016-03-24
EP16205988 2016-12-21

Publications (1)

Publication Number Publication Date
UY37168A true UY37168A (es) 2017-10-31

Family

ID=58361030

Family Applications (1)

Application Number Title Priority Date Filing Date
UY0001037168A UY37168A (es) 2016-03-24 2017-03-24 Profármacos de principios activos citotóxicos con grupos enzimáticamente escindibles

Country Status (18)

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

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11123439B2 (en) 2015-06-22 2021-09-21 Bayer Pharma Aktiengesellschaft Antibody drug conjugates (ADCS) and antibody prodrug conjugates (APDCS) with enzymatically cleavable groups
CN107921146A (zh) 2015-06-23 2018-04-17 拜耳医药股份有限公司 纺锤体驱动蛋白(ksp)抑制剂与抗‑cd123的抗体的抗体药物缀合物(adc)
CN107921288A (zh) 2015-06-23 2018-04-17 拜耳医药股份有限公司 Ksp抑制剂的靶向缀合物
CN116059390A (zh) 2016-03-24 2023-05-05 拜耳制药股份公司 具有酶促可裂解基团的细胞毒性活性物质的前药
EP3471776B1 (en) 2016-06-15 2022-05-04 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates with ksp inhibitors and anti-cd123-antibodies
EP3558388A1 (de) 2016-12-21 2019-10-30 Bayer Pharma Aktiengesellschaft Binder-wirkstoff-konjugate (adcs) mit enzymatisch spaltbaren gruppen
CN110072556B (zh) * 2016-12-21 2023-05-02 拜耳制药股份公司 具有ksp抑制剂的特异性抗体药物缀合物(adc)
WO2018114798A1 (de) * 2016-12-21 2018-06-28 Bayer Aktiengesellschaft Prodrugs von cytotoxischen wirkstoffen mit enzymatisch spaltbaren gruppen
US20210275686A1 (en) * 2018-06-18 2021-09-09 Bayer Aktiengesellschaft Binder/active agent conjugates directed against cxcr5, having enzymatically cleavable linkers and improved activity profile
EP3886854A4 (en) 2018-11-30 2022-07-06 Nuvation Bio Inc. PYRROLE AND PYRAZOLE COMPOUNDS AND METHODS OF USE THERE
UY38526A (es) 2018-12-20 2020-06-30 Amgen Inc Inhibidores de kif18a
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
AU2022222386A1 (en) * 2021-02-16 2023-07-20 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
US12084420B2 (en) 2021-08-26 2024-09-10 Volastra Therapeutics, Inc. Indoline compounds for inhibiting KIF18A
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 (de) 1988-07-06 1988-08-25 Hofer, Daniel, 7730 Villingen-Schwenningen Anzeigeeinrichtung für Feuerlöscher
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
DE69029036T2 (de) 1989-06-29 1997-05-22 Medarex Inc Bispezifische reagenzien für die aids-therapie
JP3360108B2 (ja) 1989-10-20 2002-12-24 メダレックス インク． 二つのエフェクター機能を有する二元特異性異種抗体
US5270163A (en) 1990-06-11 1993-12-14 University Research Corporation Methods for identifying nucleic acid ligands
ES2129029T5 (es) 1990-10-05 2005-10-16 Celldex Therapeutics, Inc. Inmunoestimulacion dirigida con reactivos biespecificos.
AU8727291A (en) 1990-10-29 1992-06-11 Cetus Oncology Corporation Bispecific antibodies, method of production, and uses thereof
EP1362868A3 (en) 1991-03-06 2004-02-11 MERCK PATENT GmbH Humanized and chimeric monoclonal antibodies that bind epidermal growth factor receptor (EGF-R)
WO1992019973A1 (en) 1991-04-26 1992-11-12 Surface Active Limited Novel antibodies, and methods for their use
PT627940E (pt) 1992-03-05 2003-07-31 Univ Texas Utilizacao de imunoconjugados para o diagnostico e/ou terapia de tumores vascularizados
PT719859E (pt) 1994-12-20 2003-11-28 Merck Patent Gmbh Anticorpo monoclonal anti-alfa v-integrina
DK0859841T3 (da) 1995-08-18 2002-09-09 Morphosys Ag Protein/(poly)peptidbiblioteker
WO1997024373A1 (en) 1995-12-29 1997-07-10 Medvet Science Pty. Limited Monoclonal antibody antagonists to haemopoietic growth factors
US6150508A (en) 1996-03-25 2000-11-21 Northwest Biotherapeutics, Inc. Monoclonal antibodies specific for the extracellular domain of prostate-specific membrane antigen
JP4295826B2 (ja) 1996-03-25 2009-07-15 メダレックス，インコーポレーテッド 前立腺特異的膜抗原の細胞外ドメインに対して特異的なモノクローナル抗体
ATE342282T1 (de) 1999-07-29 2006-11-15 Medarex Inc Humane monoklonale antikörper gegen prostata spezifisches membranantigen
ATE419354T1 (de) 2000-02-25 2009-01-15 Us Gov Health & Human Serv Scfv-moleküle gegen egfrviii mit verbesserter zytotoxizität und ausbeute, darauf basierte immuntoxine, und verfahren zur deren verwendung
CA2409361A1 (en) 2000-05-19 2001-11-22 Scancell Limited Humanised antibodies to the epidermal growth factor receptor
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
CA2443840C (en) 2001-04-26 2010-10-26 Biogen, Inc. Cripto blocking antibodies and uses thereof
WO2002092771A2 (en) 2001-05-11 2002-11-21 Ludwig Institute For Cancer Research Specific binding proteins and uses thereof
US7247301B2 (en) 2001-06-13 2007-07-24 Genmab A/S Human monoclonal antibodies to epidermal growth factor receptor (EGFR)
US7595378B2 (en) 2001-06-13 2009-09-29 Genmab A/S Human monoclonal antibodies to epidermal growth factor receptor (EGFR)
WO2003034903A2 (en) 2001-10-23 2003-05-01 Psma Development Company, L.L.C. Psma antibodies and protein multimers
EP2287198A3 (en) 2002-03-13 2011-05-25 Biogen Idec MA Inc. Anti-alpha V beta 6 antibodies
JP2005520566A (ja) 2002-03-22 2005-07-14 バイオジェン・アイデック・エムエイ・インコーポレイテッド Ｃｒｉｐｔｏ特異的抗体
CN101824090B (zh) 2002-06-14 2013-01-02 免疫医疗公司 人源化单克隆抗体hPAM4
EP1617864A4 (en) 2003-04-11 2006-06-21 Medimmune Inc EPHA2 AND NON-NEOPLASTIC HYPERPROLIFERATIVE CELL TROUBLESHOOTING
CA2530285C (en) 2003-06-27 2019-12-24 Abgenix, Inc. Antibodies directed to the deletion mutants of epidermal growth factor receptor and uses thereof
BRPI0412879A8 (pt) 2003-07-21 2015-12-15 Immunogen Inc Conjugado citotóxico específico do antígeno ca6 e métodos de seu uso
EP3434275A1 (en) 2003-11-06 2019-01-30 Seattle Genetics, Inc. Assay for cancer cells based on the use of auristatin conjugates with antibodies
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
RU2402569C2 (ru) 2004-03-19 2010-10-27 Имклоун Элэлси Человеческие антитела к рецептору эпидермального фактора роста
DK2412728T3 (en) 2004-08-03 2015-04-07 Innate Pharma Therapeutic compositions for cancer, that target 4Ig-B7-H3
HUE025449T2 (en) 2004-12-09 2016-04-28 Janssen Biotech Inc Immunoconjugates against Integrin, a method for their preparation and use
ES2343746T3 (es) 2005-01-07 2010-08-09 Diadexus, Inc. Composiciones de anticuerpo ovr110 y metodos de uso.
US7811572B2 (en) 2005-08-24 2010-10-12 Immunogen, Inc. Process for preparing purified drug conjugates
CN101128486A (zh) 2005-02-18 2008-02-20 米德列斯公司 缺乏岩藻糖残基的抗cd30单克隆抗体
BRPI0612529A2 (pt) 2005-06-20 2010-11-23 Psma Dev Company Llc conjugados de anticorpo-medicamento de psma
NZ566395A (en) 2005-09-26 2012-03-30 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
CN103694349A (zh) 2006-09-08 2014-04-02 米迪缪尼有限公司 人源化抗cd19抗体及其在治疗癌症、移植病和自身免疫病中的应用
EP2428224B1 (en) 2006-09-10 2016-12-21 Glycotope GmbH Use of human cells of myeloid leukaemia origin for expression of antibodies
EP1911766A1 (en) 2006-10-13 2008-04-16 Glycotope Gmbh Use of human cells of myeloid leukaemia origin for expression of antibodies
EP1900750A1 (en) 2006-09-18 2008-03-19 Glycotope Gmbh Fully human high yield production system for improved antibodies
US8394374B2 (en) 2006-09-18 2013-03-12 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
DK2099823T4 (da) 2006-12-01 2022-05-09 Seagen Inc Målbindingsmiddelvarianter og anvendelser deraf
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
CA2680111C (en) 2007-03-22 2018-05-08 Sloan-Kettering Institute For Cancer Research Use of the anti-b7h3 (cd276) antibody, 8h9, for the treatment of neuroblastoma tumors
NZ556142A (en) 2007-06-25 2009-11-27 Novartis Ag Animal remedy dispensing means
EP2182982B1 (en) 2007-08-03 2013-03-27 AbbVie Biotherapeutics Inc. Therapeutic use of anti-tweak receptor antibodies
JP5532486B2 (ja) 2007-08-14 2014-06-25 ルードヴィッヒ インスティテュート フォー キャンサー リサーチ Ｅｇｆ受容体を標的とするモノクローナル抗体１７５ならびにその誘導体および用途
EP2185188B1 (en) 2007-08-22 2014-08-06 Medarex, L.L.C. Site-specific attachment of drugs or other agents to engineered antibodies with c-terminal extensions
MY159201A (en) 2007-08-29 2016-12-30 Sanofi-Aventis Humanized anti-cxcr5 antibodies, derivatives thereof and their uses
WO2009033094A2 (en) 2007-09-07 2009-03-12 Agensys, Inc. Antibodies and related molecules that bind to 24p4c12 proteins
US8039597B2 (en) 2007-09-07 2011-10-18 Agensys, Inc. Antibodies and related molecules that bind to 24P4C12 proteins
CN104151429B (zh) 2007-11-26 2018-07-10 拜耳知识产权有限责任公司 抗-间皮素抗体及其用途
MX2010006213A (es) 2007-12-06 2010-09-07 Csl Ltd Metodo de inhibicion de celulas madre leucemicas.
DK2238168T3 (da) 2007-12-26 2014-08-25 Biotest Ag Midler, der er målrettet mod cd138 og anvendelser deraf
PL2242772T3 (pl) 2007-12-26 2015-05-29 Biotest Ag Immunokonjugaty nakierowane na CD138 i ich zastosowanie
US8802093B2 (en) 2008-04-02 2014-08-12 Macrogenics, Inc. HER2/neu-specific antibodies and methods of using same
CA2723973A1 (en) 2008-05-15 2009-11-19 Biogen Idec Ma Inc. Anti-fn14 antibodies and uses thereof
CN102137874B (zh) 2008-08-29 2015-02-18 西福根有限公司 抗表皮生长因子受体的重组抗体组合物
AR075982A1 (es) 2009-03-31 2011-05-11 Roche Glycart Ag Terapia de combinacion de un anticuerpo afucosilado y una o mas de las citoquinas seleccionadas de gm- csf humano, m -csf humano y/o il-3 humano y composicion
SG174963A1 (en) 2009-03-31 2011-11-28 Roche Glycart Ag Treatment of cancer with a humanized anti-egfr igg1 antibody and irinotecan
CN104558179A (zh) 2009-04-27 2015-04-29 协和发酵麒麟株式会社 用于治疗血液肿瘤的抗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
ES2672121T3 (es) 2009-10-07 2018-06-12 Macrogenics, Inc. Polipéptidos que contienen región Fc que presentan una función efectora mejorada debido a alteraciones del grado de fucosilación, y métodos para su uso
EP2550257B1 (en) 2010-03-22 2016-12-21 Lead Discovery Center GmbH Pharmaceutically active disubstituted triazine derivatives
NZ604510A (en) 2010-08-17 2013-10-25 Csl Ltd Dilutable biocidal compositions and methods of use
WO2012112363A1 (en) 2011-02-14 2012-08-23 Merck Sharp & Dohme Corp. Cathepsin cysteine protease inhibitors
WO2012143497A2 (de) 2011-04-21 2012-10-26 Bayer Intellectual Property Gmbh Neue binder-wirkstoff konjugate (adcs) und ihre verwendung
AR088941A1 (es) 2011-11-23 2014-07-16 Bayer Ip Gmbh Anticuerpos anti-fgfr2 y sus usos
WO2013092983A2 (en) 2011-12-23 2013-06-27 Innate Pharma Enzymatic conjugation of polypeptides
ES2924722T3 (es) 2012-05-18 2022-10-10 Aptevo Res & Development Llc Unión de inmunofusión de scFv biespecífico (BIf) a CD123 y CD3
AU2013331440A1 (en) * 2012-10-16 2015-04-30 Endocyte, Inc. Drug delivery conjugates containing unnatural amino acids and methods for using
US9872924B2 (en) 2012-10-19 2018-01-23 Daiichi Sankyo Company, Limited Antibody-drug conjugate produced by binding through linker having hydrophilic structure
WO2014151030A1 (en) 2013-03-15 2014-09-25 Novartis Ag Cell proliferation inhibitors and conjugates thereof
CN105308070A (zh) 2013-06-14 2016-02-03 拜耳制药股份公司 抗tweakr抗体及其用途
JP6721507B2 (ja) 2013-12-23 2020-07-15 バイエル・ファルマ・アクティエンゲゼルシャフト Ｋｓｐ阻害剤との抗体薬物複合体（ａｄｃ）
MA40030A (fr) * 2014-06-03 2015-12-10 Jiarui Biopharmaceuticals Ltd Conjugués peptide-médicament
WO2015189143A1 (en) 2014-06-12 2015-12-17 Bayer Pharma Aktiengesellschaft Aglycosyl anti-tweakr antibodies and uses thereof
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)
US11123439B2 (en) * 2015-06-22 2021-09-21 Bayer Pharma Aktiengesellschaft Antibody drug conjugates (ADCS) and antibody prodrug conjugates (APDCS) with enzymatically cleavable groups
EP3313522A1 (de) 2015-06-23 2018-05-02 Bayer Pharma Aktiengesellschaft Antikörper-wirkstoff-konjugate (adcs) von ksp-inhibitoren mit anti-b7h3-antikörpern
CN107921146A (zh) 2015-06-23 2018-04-17 拜耳医药股份有限公司 纺锤体驱动蛋白(ksp)抑制剂与抗‑cd123的抗体的抗体药物缀合物(adc)
CN107921288A (zh) 2015-06-23 2018-04-17 拜耳医药股份有限公司 Ksp抑制剂的靶向缀合物
CN116059390A (zh) 2016-03-24 2023-05-05 拜耳制药股份公司 具有酶促可裂解基团的细胞毒性活性物质的前药
EP3471776B1 (en) 2016-06-15 2022-05-04 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates with ksp inhibitors and anti-cd123-antibodies
EP3558388A1 (de) 2016-12-21 2019-10-30 Bayer Pharma Aktiengesellschaft Binder-wirkstoff-konjugate (adcs) mit enzymatisch spaltbaren gruppen
CN110072556B (zh) 2016-12-21 2023-05-02 拜耳制药股份公司 具有ksp抑制剂的特异性抗体药物缀合物(adc)
WO2018114798A1 (de) 2016-12-21 2018-06-28 Bayer Aktiengesellschaft Prodrugs von cytotoxischen wirkstoffen mit enzymatisch spaltbaren gruppen
US20210275686A1 (en) 2018-06-18 2021-09-09 Bayer Aktiengesellschaft Binder/active agent conjugates directed against cxcr5, having enzymatically cleavable linkers and improved activity profile

Also Published As

Publication number Publication date
MX2018011627A (es) 2019-01-10
SG10202008909VA (en) 2020-10-29
EP3432934A1 (de) 2019-01-30
RU2018136778A (ru) 2020-04-24
US20240043379A1 (en) 2024-02-08
US11685714B2 (en) 2023-06-27
SG11201808167VA (en) 2018-10-30
WO2017162663A1 (de) 2017-09-28
IL261758A (en) 2018-10-31
US20190077752A1 (en) 2019-03-14
EP3432934B1 (de) 2022-02-23
PE20181852A1 (es) 2018-12-03
CL2018002699A1 (es) 2019-01-18
CN108883195A (zh) 2018-11-23
JP2019512517A (ja) 2019-05-16
AU2017236431A2 (en) 2018-11-08
TW201735954A (zh) 2017-10-16
CA3018630A1 (en) 2017-09-28
JP7251981B2 (ja) 2023-04-04
AU2017236431A1 (en) 2018-09-27
KR20180123047A (ko) 2018-11-14
CO2018010026A2 (es) 2018-09-28
CN116059390A (zh) 2023-05-05
BR112018069483A2 (pt) 2019-07-30

Similar Documents

Publication Publication Date Title
UY37168A (es) Profármacos de principios activos citotóxicos con grupos enzimáticamente escindibles
CL2020000501A1 (es) Inhibidores de la ectonucleótido pirofosfatasa-fosfodiesterasa 1 (enpp1) y usos de los mismos.
CO2019000386A2 (es) Compuestos heterocíclicos como inmunomoduladores
CO2019007863A2 (es) Derivados de benzooxazol como inmunomoduladores
SV2018005687A (es) Derivados de dihidroimidazopirazinona usados en el tratamiento del cancer
CO2017013708A2 (es) Macrociclos peptídicos contra acinetobacter baumannii.
AR110419A1 (es) Profármacos de principios activos citotóxicos con grupos enzimáticamente escindibles
NI201600144A (es) Derivados de quinoxalina utiles como moduladores del fgfr cinasa
DOP2015000189A (es) Inhibidores quinazolínicos de formas mutadas activantes del receptor del factor de crecimiento epidérmico
SV2015005115A (es) Derivados de la pirazolopirrolidina y su uso en el tratamiento de enfermedades
CL2015001864A1 (es) Compuestos derivados de espiropirido[1,2-a]pirazina sustituidos, como inhibidores de la integrasa del vih; composicion farmaceutica que los comprende; y su uso para la profilaxis o el tratamiento de una infeccion por vih.
DOP2015000082A (es) Inhibidores no nucleósidos de la transcriptasa inversa
BR112017003054A2 (pt) compostos de aminopirimidinila como inibidores de jak
ECSP18073293A (es) Derivados de indolina sustituidos como inhibidores de la replicación viral del dengue
AR108021A1 (es) Conjugados de anticuerpo-principio activo (adcs) de inhibidores de ksp con anticuerpos anti-b7h3
BR112016028845A2 (pt) composto, composição farmacêutica e uso de um composto
CL2021001388A1 (es) Compuestos útiles en la terapia para el vih
CR20140144A (es) Derivados de estra-1,3,5 (10), 16-tetraen-3-carboxamida, procedimientos para su preparación, preparados farmacéuticos que los contienen, así como su uso para la preparación de medicamentos
BR112017009012A2 (pt) derivados de anel benzo de seis membros como inibidor de dpp-4 e seu uso
UY38228A (es) Compuestos de triazolopirimidina y su uso en el tratamiento del cáncer
BR112017022158A2 (pt) compostos, composições farmacêuticas e uso de um composto
CY1120602T1 (el) [1,2,4]τριαζολο[4,3-β]πυριδαζινες για χρηση στη θεραπευτικη αντιμετωπιση πολλαπλασιαστικων ασθενειων
CL2020001062A1 (es) Sulfonas y sulfóxidos bicíclicos y métodos de uso de los mismos.
PE20151607A1 (es) Formulaciones de compuestos organicos
BR112017014189A2 (pt) terapia de câncer com um parvovirus combinado com bevacizumabe

Legal Events

Date Code Title Description
109 Application deemed to be withdrawn

Effective date: 20230605