ES2525351T3 - Compuestos antiproliferativos, conjugados de los mismos, procedimientos para éstos y usos de los mismos - Google Patents

Compuestos antiproliferativos, conjugados de los mismos, procedimientos para éstos y usos de los mismos Download PDF

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Publication number
ES2525351T3
ES2525351T3 ES10739817.4T ES10739817T ES2525351T3 ES 2525351 T3 ES2525351 T3 ES 2525351T3 ES 10739817 T ES10739817 T ES 10739817T ES 2525351 T3 ES2525351 T3 ES 2525351T3
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compound
substituted
alkyl
unsubstituted
alkenyl
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Spanish (es)
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Heng Cheng
Qiang Cong
Sanjeev Gangwar
Qian Zhang
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ER Squibb and Sons LLC
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ER Squibb and Sons LLC
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/06Tripeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817Toxins
    • A61K47/6829Bacterial toxins, e.g. diphteria toxins or Pseudomonas exotoxin A
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/10Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
    • C07C229/14Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of carbon skeletons containing rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/06Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
    • C07C229/10Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
    • C07C229/16Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/021Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06139Dipeptides with the first amino acid being heterocyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10Tetrapeptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Epidemiology (AREA)
  • Toxicology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
ES10739817.4T 2009-08-03 2010-08-02 Compuestos antiproliferativos, conjugados de los mismos, procedimientos para éstos y usos de los mismos Active ES2525351T3 (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US23093209P 2009-08-03 2009-08-03
US230932P 2009-08-03
US23288309P 2009-08-11 2009-08-11
US232883P 2009-08-11
PCT/US2010/044078 WO2011017249A1 (en) 2009-08-03 2010-08-02 Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof

Publications (1)

Publication Number Publication Date
ES2525351T3 true ES2525351T3 (es) 2014-12-22

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ES10739817.4T Active ES2525351T3 (es) 2009-08-03 2010-08-02 Compuestos antiproliferativos, conjugados de los mismos, procedimientos para éstos y usos de los mismos

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Country Link
US (6) US8394922B2 (enExample)
EP (1) EP2461830B1 (enExample)
JP (1) JP5859964B2 (enExample)
KR (1) KR101759359B1 (enExample)
CN (2) CN104592351A (enExample)
AR (1) AR077701A1 (enExample)
AU (1) AU2010279674B2 (enExample)
BR (1) BR112012002615A2 (enExample)
CA (1) CA2770042C (enExample)
CL (1) CL2012000302A1 (enExample)
CO (1) CO6501196A2 (enExample)
DK (1) DK2461830T3 (enExample)
EA (1) EA022288B1 (enExample)
ES (1) ES2525351T3 (enExample)
HR (1) HRP20140976T1 (enExample)
HU (1) HUE026997T2 (enExample)
IL (1) IL217717A (enExample)
IN (1) IN2012DN00860A (enExample)
MX (1) MX2012001665A (enExample)
NZ (1) NZ597985A (enExample)
PE (1) PE20121087A1 (enExample)
PL (1) PL2461830T3 (enExample)
PT (1) PT2461830E (enExample)
SG (2) SG10201503332XA (enExample)
SI (1) SI2461830T1 (enExample)
SM (1) SMT201400183B (enExample)
TW (1) TWI469794B (enExample)
WO (1) WO2011017249A1 (enExample)

Families Citing this family (90)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8288557B2 (en) 2004-07-23 2012-10-16 Endocyte, Inc. Bivalent linkers and conjugates thereof
CN101678124A (zh) 2007-03-14 2010-03-24 恩多塞特公司 结合配体连接的微管溶素递药缀合物
CN101784565B (zh) 2007-06-25 2014-12-10 恩多塞特公司 含有亲水性间隔区接头的共轭物
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
PL2187965T3 (pl) 2007-08-17 2020-05-18 Purdue Research Foundation Koniugaty wiążący psma ligand-łącznik i sposoby ich zastosowania
IT1394860B1 (it) * 2009-07-22 2012-07-20 Kemotech S R L Composti farmaceutici
US8394922B2 (en) 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
US9951324B2 (en) 2010-02-25 2018-04-24 Purdue Research Foundation PSMA binding ligand-linker conjugates and methods for using
MX336540B (es) 2010-06-08 2016-01-22 Genentech Inc Conjugados y anticuerpos manipulados geneticamente con cisteina.
ES2656167T5 (es) * 2011-03-16 2021-03-26 Hoffmann La Roche Cromatografía de intercambio iónico con selectividad mejorada para la separación de monómeros, agregados y fragmentos polipeptídicos mediante la modulación de la fase móvil
EP3228325A1 (en) 2011-06-10 2017-10-11 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
WO2013126797A1 (en) 2012-02-24 2013-08-29 Purdue Research Foundation Cholecystokinin b receptor targeting for imaging and therapy
US20140080175A1 (en) 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
HK1208216A1 (en) * 2012-05-15 2016-02-26 Concortis Biosystems, Corp Drug-conjugates, conjugation methods, and uses thereof
HUE048574T2 (hu) * 2012-07-12 2020-08-28 Hangzhou Dac Biotech Co Ltd Sejthez kötõdõ molekulák citotoxikus szerekkel képzett konjugátumai
US11873281B2 (en) 2012-07-12 2024-01-16 Hangzhou Dac Biotech Co., Ltd. Conjugates of cell binding molecules with cytotoxic agents
EP2708243A1 (en) 2012-09-17 2014-03-19 OntoChem GmbH Receptor ligand linked cytotoxic molecules
AU2013331440A1 (en) 2012-10-16 2015-04-30 Endocyte, Inc. Drug delivery conjugates containing unnatural amino acids and methods for using
MY171561A (en) 2012-11-15 2019-10-18 Endocyte Inc Conjugates for treating diseases caused by psma expressing cells
CA2891280C (en) 2012-11-24 2018-03-20 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and their uses for conjugation of drugs to cell binding molecules
AU2013359506B2 (en) 2012-12-10 2018-05-24 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
EP2931316B1 (en) 2012-12-12 2019-02-20 Mersana Therapeutics, Inc. Hydroxyl-polymer-drug-protein conjugates
SI2956173T1 (sl) 2013-02-14 2017-06-30 Bristol-Myers Squibb Company Spojine tubulizina, postopki pridobivanja in uporaba
US20140249315A1 (en) 2013-03-01 2014-09-04 Endocyte, Inc. Processes for preparing tubulysins
AU2014228489B2 (en) 2013-03-15 2018-11-15 Zymeworks Bc Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
JP6171435B2 (ja) * 2013-03-18 2017-08-02 富士通株式会社 半導体装置及びその製造方法、電源装置、高周波増幅器
WO2014197866A1 (en) 2013-06-06 2014-12-11 Igenica Biotherapeutics, Inc. Modified antibodies and related compounds, compositions, and methods of use
WO2015057585A1 (en) * 2013-10-14 2015-04-23 Regents Of The University Of Minnesota Therapeutic compounds
GEP20237479B (en) 2013-10-18 2023-03-27 Deutsches Krebsforsch Labeled inhibitors of prostate specific membrane antigen (psma), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer
EP3069147A4 (en) 2013-11-14 2017-10-11 Endocyte, Inc. Compounds for positron emission tomography
EP3074773A1 (en) 2013-11-25 2016-10-05 OntoChem GmbH Method for diagnosing g-protein coupled receptor-related diseases
DK3086815T3 (da) 2013-12-27 2022-05-23 Zymeworks Inc Sulfonamidholdige forbindelsessystemer til lægemiddelkonjugater
KR20160125361A (ko) 2013-12-27 2016-10-31 자임워크스 인코포레이티드 Var2csa-약물 접합체
CN106132959B (zh) * 2014-01-28 2020-04-17 管道制药有限责任公司 用于缀合的细胞毒性微管溶素化合物
CN106414465B (zh) 2014-02-28 2021-11-16 杭州多禧生物科技有限公司 带电荷链接体及其在共轭反应上的应用
WO2015135659A1 (en) 2014-03-14 2015-09-17 Ontochem Gmbh Receptor ligand linked cytotoxic molecules
CN115322253A (zh) 2014-03-20 2022-11-11 百时美施贵宝公司 稳定化的基于纤连蛋白的支架分子
KR20160142392A (ko) * 2014-04-11 2016-12-12 메디뮨 엘엘씨 튜부리신 유도체
US9579317B2 (en) * 2014-06-03 2017-02-28 Jiarui Biopharmaceuticals, Ltd. Peptide-drug conjugates
CN104262455B (zh) * 2014-08-22 2017-05-03 亚飞(上海)生物医药科技有限公司 肿瘤微环境靶向激活的紫杉醇衍生物及其制备和用途
CA2958495C (en) 2014-08-22 2023-04-18 Yafei Shanghai Biolog Medicine Science & Technology Co., Ltd. Small molecule conjugates specifically activated in tumor microenvironment for targeting and use thereof
DK3191502T3 (da) * 2014-09-11 2021-07-19 Seagen Inc Målrettet indgivelse af tertiært aminholdige lægemiddelstoffer
US10077318B2 (en) 2014-09-12 2018-09-18 Genentech, Inc. Cysteine engineered antibodies and conjugates
RU2723651C2 (ru) 2014-09-17 2020-06-17 Займворкс Инк. Цитотоксические и антимитотические соединения и способы их применения
US10077287B2 (en) 2014-11-10 2018-09-18 Bristol-Myers Squibb Company Tubulysin analogs and methods of making and use
HUE050596T2 (hu) 2014-11-21 2020-12-28 Bristol Myers Squibb Co Antitestek CD73 ellen és azok felhasználásai
LT3221346T (lt) 2014-11-21 2020-11-10 Bristol-Myers Squibb Company Antikūnai, apimantys modifikuotas sunkiosios grandinės pastoviąsias sritis
ES2822990T3 (es) 2014-11-25 2021-05-05 Bristol Myers Squibb Co Novedosos polipéptidos de unión a PD-L1 para obtención de imágenes
US10188759B2 (en) 2015-01-07 2019-01-29 Endocyte, Inc. Conjugates for imaging
KR20170137725A (ko) * 2015-02-25 2017-12-13 윌리엄 마쉬 라이스 유니버시티 데스아세톡시투불리신 h 및 이의 유사체
CN107406496A (zh) 2015-03-10 2017-11-28 百时美施贵宝公司 可通过转谷氨酰胺酶缀合的抗体和由其制备的缀合物
UY36687A (es) 2015-05-29 2016-11-30 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Anticuerpos contra ox40 y sus usos
NZ739830A (en) 2015-07-12 2021-12-24 Hangzhou Dac Biotech Co Ltd Bridge linkers for conjugation of cell-binding molecules
US9839687B2 (en) 2015-07-15 2017-12-12 Suzhou M-Conj Biotech Co., Ltd. Acetylenedicarboxyl linkers and their uses in specific conjugation of a cell-binding molecule
ES2809125T3 (es) 2015-09-23 2021-03-03 Bristol Myers Squibb Co Moléculas de armazón a base de fibronectina de unión a glipicano-3
JP6707804B2 (ja) * 2015-09-24 2020-06-10 エルジー・ケム・リミテッド 化合物およびこれを含む有機発光素子
EP3165532B1 (en) 2015-11-03 2018-12-19 Industrial Technology Research Institute Auristatin derivatives, linker-drugs and ligand-drug conjugates
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
US11229708B2 (en) 2015-12-04 2022-01-25 Seagen Inc. Conjugates of quaternized tubulysin compounds
JP2019505575A (ja) 2015-12-21 2019-02-28 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 部位特異的な結合のための変異型抗体
US10723727B2 (en) 2016-02-01 2020-07-28 Pfizer Inc. Tubulysin analogs and methods for their preparation
IL295230A (en) 2016-03-04 2022-10-01 Bristol Myers Squibb Co Combination therapy with anti-cd73 antibodies
CN105664134B (zh) * 2016-03-13 2019-04-26 浙江药苑生物科技有限公司 一种用于治疗骨癌的药物组合物
EP3454909A1 (en) 2016-05-10 2019-03-20 Bristol-Myers Squibb Company Antibody-drug conjugates of tubulysin analogs with enhanced stability
US20170326249A1 (en) * 2016-05-10 2017-11-16 Bristol-Myers Squibb Company Antibody-drug conjugate of an anti-glypican-3 antibody and a tubulysin analog, preparation and uses
WO2017218724A1 (en) 2016-06-16 2017-12-21 Bristol-Myers Squibb Company Process and intermediates for making tubulysin analogs
ES2902179T3 (es) 2016-08-19 2022-03-25 Bristol Myers Squibb Co Compuestos de seco-ciclopropapirroloindol, conjugados de anticuerpo-fármaco de los mismos y métodos de elaboración y uso
US20190218294A1 (en) 2016-09-09 2019-07-18 Bristol-Myers Squibb Company Use of an anti-pd-1 antibody in combination with an anti-mesothelin antibody in cancer treatment
US10517958B2 (en) 2016-10-04 2019-12-31 Zymeworks Inc. Compositions and methods for the treatment of platinum-drug resistant cancer
WO2018075842A1 (en) 2016-10-20 2018-04-26 Bristol-Myers Squibb Company Condensed benzodiazepine derivatives and conjugates made therefrom
CN116143678A (zh) 2016-11-14 2023-05-23 杭州多禧生物科技有限公司 偶联连接体,含有此连接体的细胞结合分子-药物偶联物及其制备和应用
JP6585650B2 (ja) * 2017-03-23 2019-10-02 ハンヂョウ ディーエイシー バイオテック カンパニー リミテッド 細胞毒性剤と細胞結合受容体との共役体
MX2019013132A (es) 2017-05-25 2020-01-27 Bristol Myers Squibb Co Anticuerpos que comprenden regiones constantes pesadas modificadas.
US11274124B2 (en) 2017-11-29 2022-03-15 William Marsh Rice University Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith
SG11202010217YA (en) 2018-04-17 2020-11-27 Endocyte Inc Methods of treating cancer
WO2019209811A1 (en) 2018-04-24 2019-10-31 Bristol-Myers Squibb Company Macrocyclic toll-like receptor 7 (tlr7) agonists
AU2019277094B2 (en) 2018-05-29 2025-12-18 Bristol-Myers Squibb Company Modified self-immolating moieties for use in prodrugs and conjugates and methods of using and making
US11020490B2 (en) 2018-06-22 2021-06-01 Bristol-Myers Squibb Company Antibody-drug conjugate with a tubulysin analog warhead having a stabilized acetate group in the TUV subunit
US20220106400A1 (en) 2018-11-28 2022-04-07 Bristol-Myers Squibb Company Antibodies comprising modified heavy constant regions
BR112021010060B1 (pt) 2018-11-30 2024-03-12 Bristol-Myers Squibb Company Anticorpo que compreende uma extensão c-terminal de cadeia leve que contém glutamina, conjugados do mesmo, e método de preparação de conjugados
WO2020123425A2 (en) 2018-12-12 2020-06-18 Bristol-Myers Squibb Company Antibodies modified for transglutaminase conjugation, conjugates thereof, and methods and uses
MY208067A (en) 2018-12-21 2025-04-11 Regeneron Pharma Tubulysins and protein-tubulysin conjugates
US12473265B2 (en) 2019-05-20 2025-11-18 Endocyte, Inc. Methods for preparing PSMA conjugates
JP6842127B2 (ja) * 2019-05-22 2021-03-17 ハンヂョウ ディーエイシー バイオテック カンパニー リミテッド 細胞毒性剤と細胞結合受容体との共役体
CN114040778A (zh) 2019-06-29 2022-02-11 杭州多禧生物科技有限公司 一种细胞结合分子-Tubulysin衍生物偶联物及其制备方法
US20240377413A1 (en) 2019-09-16 2024-11-14 Bristol-Myers Squibb Company Dual capture method for analysis of antibody-drug conjugates
CN113387829B (zh) * 2020-03-13 2023-04-07 凯特立斯(深圳)科技有限公司 一种沙库必曲的制备方法
CN115867563B (zh) * 2020-06-24 2025-06-27 里珍纳龙药品有限公司 微管溶素及蛋白质-微管溶素偶联物
JP7044419B2 (ja) * 2021-02-04 2022-03-30 ハンヂョウ ディーエイシー バイオテック カンパニー リミテッド 細胞毒性剤と細胞結合受容体との共役体
WO2022078524A2 (en) 2021-11-03 2022-04-21 Hangzhou Dac Biotech Co., Ltd. Specific conjugation of an antibody

Family Cites Families (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1981001145A1 (en) 1979-10-18 1981-04-30 Univ Illinois Hydrolytic enzyme-activatible pro-drugs
US4475196A (en) 1981-03-06 1984-10-02 Zor Clair G Instrument for locating faults in aircraft passenger reading light and attendant call control system
US4447233A (en) 1981-04-10 1984-05-08 Parker-Hannifin Corporation Medication infusion pump
US4631190A (en) 1981-06-26 1986-12-23 Shen Wei C Acidity-sensitive spacer molecule to control the release of pharmaceuticals from molecular carriers
US5144011A (en) 1981-06-26 1992-09-01 Boston University Acidity-sensitive spacer molecule to control the release of pharmaceuticals from molecular carriers
US4439196A (en) 1982-03-18 1984-03-27 Merck & Co., Inc. Osmotic drug delivery system
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US4447224A (en) 1982-09-20 1984-05-08 Infusaid Corporation Variable flow implantable infusion apparatus
US4487603A (en) 1982-11-26 1984-12-11 Cordis Corporation Implantable microinfusion pump system
US4486194A (en) 1983-06-08 1984-12-04 James Ferrara Therapeutic device for administering medicaments through the skin
US4698420A (en) 1985-02-25 1987-10-06 Xoma Corporation Antibody hybrid molecules and process for their preparation
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
US5374548A (en) 1986-05-02 1994-12-20 Genentech, Inc. Methods and compositions for the attachment of proteins to liposomes using a glycophospholipid anchor
MX9203291A (es) 1985-06-26 1992-08-01 Liposome Co Inc Metodo para acoplamiento de liposomas.
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US5108921A (en) 1989-04-03 1992-04-28 Purdue Research Foundation Method for enhanced transmembrane transport of exogenous molecules
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
TW420681B (en) 1995-12-08 2001-02-01 Lederle Japan Ltd Carbapenem-3-carboxylic acid ester derivatives
DE19638870B4 (de) 1996-09-23 2009-05-14 Helmholtz-Zentrum für Infektionsforschung GmbH Tubulysine, Verfahren zu ihrer Gewinnung und sie enthaltende Mittel
US7214487B2 (en) 1998-06-26 2007-05-08 Sunesis Pharmaceuticals, Inc. Methods for identifying compounds that modulate enzymatic activities by employing covalently bonded target-extender complexes with ligand candidates
NZ517202A (en) * 1999-08-24 2004-05-28 Medarex Inc Human CTLA-4 antibodies and their uses
DE10008089A1 (de) 2000-02-22 2001-10-31 Biotechnolog Forschung Gmbh Syntheseverfahren zur Herstellung von Tubulysinen
US20020169125A1 (en) * 2001-03-21 2002-11-14 Cell Therapeutics, Inc. Recombinant production of polyanionic polymers and uses thereof
US7129261B2 (en) * 2001-05-31 2006-10-31 Medarex, Inc. Cytotoxic agents
US7091186B2 (en) 2001-09-24 2006-08-15 Seattle Genetics, Inc. p-Amidobenzylethers in drug delivery agents
CN1638800A (zh) * 2002-01-09 2005-07-13 米德列斯公司 抗cd30的人类单克隆抗体
EP1523493B1 (de) * 2002-07-09 2013-09-04 Dömling, Alexander Neue tubulysinanaloga
WO2004005326A2 (de) * 2002-07-09 2004-01-15 Morphochem Aktiengellschaft Fu Tubulysinkonjugate
DE10241152A1 (de) * 2002-09-05 2004-03-18 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Tubulysin-Biosynthese-Gene
FR2845630B1 (fr) * 2002-10-09 2005-09-30 Helitest Ags Dispositif de demasticage, notamment pour la refection de joints dans des structures de reservoirs d'aeronefs et container d'intervention
DE10254439A1 (de) * 2002-11-21 2004-06-03 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Tubulysine, Herstellungsverfahren und Tubulysin-Mittel
EP2261244A3 (en) 2003-04-15 2011-02-23 Glaxosmithkline LLC Human il-18 substitution mutants and their conjugates
MXPA06000798A (es) * 2003-07-22 2006-04-07 Schering Ag Anticuerpos de rg1 y usos de los mismos.
EP1718667B1 (en) 2004-02-23 2013-01-09 Genentech, Inc. Heterocyclic self-immolative linkers and conjugates
RU2402548C2 (ru) * 2004-05-19 2010-10-27 Медарекс, Инк. Химические линкеры и их конъюгаты
WO2005112919A2 (en) * 2004-05-19 2005-12-01 Medarex, Inc. Self-immolative linkers and drug conjugates
US7541330B2 (en) 2004-06-15 2009-06-02 Kosan Biosciences Incorporated Conjugates with reduced adverse systemic effects
DE102004030227A1 (de) 2004-06-23 2006-01-26 Dömling, Alexander, Dr. Wirkstoffe mit antiangiogenetischen Eigenschaften
KR101270829B1 (ko) 2004-09-23 2013-06-07 제넨테크, 인크. 시스테인 유전자조작 항체 및 접합체
WO2006089230A2 (en) * 2005-02-18 2006-08-24 Medarex, Inc. Human monoclonal antibodies to prostate specific membrane antigen (psma)
US7714016B2 (en) * 2005-04-08 2010-05-11 Medarex, Inc. Cytotoxic compounds and conjugates with cleavable substrates
ES2720160T3 (es) 2005-05-09 2019-07-18 Ono Pharmaceutical Co Anticuerpos monoclonales humanos contra muerte programada 1(PD-1) y métodos para tratar el cáncer usando anticuerpos dirigidos contra PD-1 solos o junto con otras sustancias inmunoterapéuticas
AU2006262232A1 (en) * 2005-06-20 2007-01-04 Medarex, Inc. CD19 antibodies and their uses
US8465724B2 (en) * 2005-08-19 2013-06-18 Endocyte, Inc. Multi-drug ligand conjugates
KR20080056167A (ko) * 2005-09-26 2008-06-20 메다렉스, 인코포레이티드 씨디70에 대한 인간 모노크로날 항체
EP1940470B1 (en) * 2005-09-26 2013-04-17 Medarex, Inc. Antibody-drug conjugates and their use
EA015324B1 (ru) * 2005-10-26 2011-06-30 Медарекс, Инк. Способы и соединения для получения аналогов сс-1065
CA2627190A1 (en) * 2005-11-10 2007-05-24 Medarex, Inc. Duocarmycin derivatives as novel cytotoxic compounds and conjugates
DK1957539T3 (da) * 2005-12-08 2013-05-06 Medarex Inc Humane monoklonale antistoffer til proteintyrosinkinase 7 (ptk7) og deres anvendelse
NZ568015A (en) * 2005-12-08 2012-03-30 Medarex Inc Human monoclonal antibodies to O8E
BRPI0717902A2 (pt) 2006-12-01 2013-10-29 Medarex Inc "anticorpo monoclonal humano isolado, composição, conjugado anticorpo-molécula parceria, imunoconjugado, molécula de ácido nucléico isolada, vetor de expressão, célula hospedeira, método para prepar um anticorpo anti-cd22, método para inibir o desenvolvimento de uma célula tumoral que expressa cd22 e método para tratar uma doença inflamatória ou autoimuneem um indivíduo"
JP2010513306A (ja) 2006-12-14 2010-04-30 メダレックス インコーポレーティッド Cd70に結合するヒト抗体およびその使用
UY30776A1 (es) * 2006-12-21 2008-07-03 Medarex Inc Anticuerpos cd44
TWI412367B (zh) 2006-12-28 2013-10-21 Medarex Llc 化學鏈接劑與可裂解基質以及其之綴合物
US20080176958A1 (en) * 2007-01-24 2008-07-24 Insert Therapeutics, Inc. Cyclodextrin-based polymers for therapeutics delivery
CA2678514A1 (en) * 2007-02-21 2008-08-28 Medarex, Inc. Chemical linkers with single amino acids and conjugates thereof
US20100047841A1 (en) * 2007-02-27 2010-02-25 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Synthesis of desacetoxytubulysin h and analogs thereof
CN101678124A (zh) * 2007-03-14 2010-03-24 恩多塞特公司 结合配体连接的微管溶素递药缀合物
US8980833B2 (en) 2007-05-10 2015-03-17 R&D-Biopharmaceuticals Gmbh Tubulysine derivatives
CN101784565B (zh) 2007-06-25 2014-12-10 恩多塞特公司 含有亲水性间隔区接头的共轭物
US7387981B1 (en) 2007-06-28 2008-06-17 Lyondell Chemical Technology, L.P. Direct epoxidation catalyst and process
WO2009012958A2 (en) 2007-07-20 2009-01-29 Helmholtz-Zentrum für Infektionsforschung GmbH Tubulysin d analogues
PL2187965T3 (pl) 2007-08-17 2020-05-18 Purdue Research Foundation Koniugaty wiążący psma ligand-łącznik i sposoby ich zastosowania
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
CA2700860C (en) 2007-10-01 2016-07-19 Jonathan A. Terrett Human antibodies that bind mesothelin, and uses thereof
CA2703491C (en) 2007-10-25 2017-06-13 Endocyte, Inc. Tubulysins and processes for preparing
EP2174947A1 (en) 2008-09-25 2010-04-14 Universität des Saarlandes Bioactive pre-tubulysins and use thereof
US8394922B2 (en) 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
WO2011057805A1 (en) * 2009-11-12 2011-05-19 R&D Biopharmaceuticals Gmbh Tubulin inhibitors

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