KR20120080611A - 효능 있는 접합체 및 친수성 링커 - Google Patents

효능 있는 접합체 및 친수성 링커 Download PDF

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KR20120080611A
KR20120080611A KR1020127010084A KR20127010084A KR20120080611A KR 20120080611 A KR20120080611 A KR 20120080611A KR 1020127010084 A KR1020127010084 A KR 1020127010084A KR 20127010084 A KR20127010084 A KR 20127010084A KR 20120080611 A KR20120080611 A KR 20120080611A
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cell
antibody
bond
maytansinoid
formula
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KR1020127010084A
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Korean (ko)
Inventor
라제바 싱
샤론 디. 윌헬름
라비 브이.제이. 체리
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이뮤노젠 아이엔씨
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • 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
    • A61K47/56—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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
    • A61K47/68033—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection

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  • 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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Virology (AREA)
  • Cell Biology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
KR1020127010084A 2009-10-06 2009-10-06 효능 있는 접합체 및 친수성 링커 Withdrawn KR20120080611A (ko)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US2009/059620 WO2010126551A1 (en) 2009-04-30 2009-10-06 Potent conjugates and hydrophilic linkers

Publications (1)

Publication Number Publication Date
KR20120080611A true KR20120080611A (ko) 2012-07-17

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KR1020127010084A Withdrawn KR20120080611A (ko) 2009-10-06 2009-10-06 효능 있는 접합체 및 친수성 링커

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EP (1) EP2486023A4 (enrdf_load_html_response)
JP (1) JP2013506709A (enrdf_load_html_response)
KR (1) KR20120080611A (enrdf_load_html_response)
CN (1) CN102596922A (enrdf_load_html_response)
IL (1) IL219020A0 (enrdf_load_html_response)
IN (1) IN2012DN02780A (enrdf_load_html_response)
WO (1) WO2010126551A1 (enrdf_load_html_response)

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10201706294VA (en) 2009-02-05 2017-09-28 Immunogen Inc Novel benzodiazepine derivatives
CN106046159B (zh) 2010-03-12 2020-06-16 德彪发姆国际有限公司 Cd37结合分子及其免疫缀合物
CA2816426A1 (en) * 2010-11-17 2012-06-07 Genentech, Inc. Alaninyl maytansinol antibody conjugates
WO2012086857A1 (ko) 2010-12-21 2012-06-28 (주)파낙스이엠 광역학 진단 또는 치료를 위한 결합체 및 이의 제조방법
ES2717657T3 (es) 2011-02-15 2019-06-24 Immunogen Inc Métodos para la preparación de conjugados
US9447189B2 (en) 2011-04-01 2016-09-20 Immunogen, Inc. CD37-binding molecules and immunoconjugates thereof
RU2014121820A (ru) * 2011-11-21 2015-12-27 Иммьюноджен, Инк. Способ лечения опухолей, устойчивых к анти-egfr терапиям, с помощью конъюгата антитела egfr с цитотоксическим средством
US9353150B2 (en) 2012-12-04 2016-05-31 Massachusetts Institute Of Technology Substituted pyrazino[1′,2′:1 ,5]pyrrolo[2,3-b]-indole-1,4-diones for cancer treatment
CN103044677A (zh) * 2012-12-28 2013-04-17 上海景宇生物科技有限公司 一种异端基遥爪聚乙二醇及其制备方法
CN103083652B (zh) * 2013-02-06 2016-08-10 中国科学院过程工程研究所 一种以异型双功能试剂为连接桥的脑膜炎多糖结合疫苗及其制备方法
US9415118B2 (en) 2013-03-13 2016-08-16 Novartis Ag Antibody drug conjugates
US9498532B2 (en) * 2013-03-13 2016-11-22 Novartis Ag Antibody drug conjugates
MY183572A (en) 2013-03-15 2021-02-26 Regeneron Pharma Biologically active molecules, conjugates thereof, and therapeutic uses
CN103254311B (zh) * 2013-05-09 2015-05-13 齐鲁制药有限公司 一种制备抗体-美登素类生物碱药物偶联物的方法
US10208125B2 (en) 2013-07-15 2019-02-19 University of Pittsburgh—of the Commonwealth System of Higher Education Anti-mucin 1 binding agents and uses thereof
EP3027218A1 (en) * 2013-08-02 2016-06-08 Sanofi Use of anti-muc1 maytansinoid immunoconjugate antibody for the treatment of solid tumors
JP6608823B2 (ja) 2013-08-26 2019-11-20 レゲネロン ファーマシューティカルス，インコーポレーテッド マクロライドジアステレオマーを含む医薬組成物、その合成方法、及び治療上の使用
CN103483357B (zh) * 2013-10-12 2015-11-18 齐鲁制药有限公司 一种抗体-美登素偶联物的中间体新晶型及其制备方法
ES2826398T3 (es) 2013-10-15 2021-05-18 Seagen Inc Enlazadores-fármacos pegilados para una mejor farmacocinética de los conjugados ligando-fármaco
AU2015210578B2 (en) * 2014-01-29 2020-04-16 Jiangsu Hengrui Medicine Co., Ltd. Ligand-cytotoxic drug conjugate, preparation method therefor, and uses thereof
GB201402009D0 (en) * 2014-02-06 2014-03-26 Oncomatryx Biopharma S L Antibody-drug conjugates and immunotoxins
WO2015153401A1 (en) * 2014-04-04 2015-10-08 Merck Sharp & Dohme Corp Phosphate based linkers for intracellular delivery of drug conjugates
WO2016167798A1 (en) * 2015-04-17 2016-10-20 Northwestern University Phosphatidylethanolamine-specific probes
CA2954599A1 (en) * 2014-08-12 2016-02-18 Novartis Ag Anti-cdh6 antibody drug conjugates
KR20240011258A (ko) * 2014-09-02 2024-01-25 이뮤노젠 아이엔씨 항체 약물 컨쥬게이트 조성물의 제형화 방법
EP3271329B1 (en) * 2015-03-19 2021-08-18 Hangzhou Dac Biotech Co., Ltd Novel hydrophilic linkers and ligand-drug conjugates thereof
BR112017020149A8 (pt) 2015-03-27 2023-05-02 Regeneron Pharma Derivados de maitansinoide, conjugados dos mesmos e métodos de uso
UA125496C2 (uk) 2015-06-08 2022-04-13 Дебіофарм Інтернаціонал, С.А. Спосіб лікування пацієнта з в-клітинним раком імунокон’югатом, який зв’язується з cd37 разом з антитілом, що зв'язується з cd20
SG10202106529XA (en) 2015-07-21 2021-07-29 Immunogen Inc Methods of preparing cytotoxic benzodiazepine derivatives
JP6890581B2 (ja) 2015-08-28 2021-06-18 デビオファーム インターナショナル， エス． アー． Ｃｄ３７の検出のための抗体およびアッセイ
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
CN108367043A (zh) 2015-12-04 2018-08-03 西雅图基因公司 季铵化的微管溶素化合物的缀合物
CN105435241A (zh) * 2015-12-10 2016-03-30 浙江大学 一种iRGD-抗癌药物偶联物及其制备方法和应用
MY198605A (en) 2016-01-25 2023-09-08 Regeneron Pharma Maytansinoid derivatives conjugates thereof, and methods of use
UA125510C2 (uk) 2016-03-25 2022-04-13 Сіджен Інк. Спосіб отримання пегильованої сполуки лікарський препарат-лінкер, де лікарським препаратом є ауристатин, та її проміжних сполук
US10918627B2 (en) 2016-05-11 2021-02-16 Massachusetts Institute Of Technology Convergent and enantioselective total synthesis of Communesin analogs
GB201615725D0 (en) 2016-09-15 2016-11-02 Polytherics Ltd Novel cytotoxic agents and conjugates thereof
CN110088138B (zh) * 2016-09-23 2023-08-25 瑞泽恩制药公司 抗steap2抗体、抗体药物偶联物和结合steap2和cd3的双特异性抗原结合分子以及其用途
US11278629B2 (en) 2016-11-02 2022-03-22 Debiopharm International, S.A. Methods for improving anti-CD37 immunoconjugate therapy
CN118562004A (zh) 2016-12-16 2024-08-30 蓝鳍生物医药公司 抗-含cub结构域蛋白1(cdcp1)抗体、抗体药物缀合物及其使用方法
US11730822B2 (en) 2017-03-24 2023-08-22 Seagen Inc. Process for the preparation of glucuronide drug-linkers and intermediates thereof
WO2018209239A1 (en) 2017-05-11 2018-11-15 Massachusetts Institute Of Technology Potent agelastatin derivatives as modulators for cancer invasion and metastasis
US10646585B2 (en) 2017-09-15 2020-05-12 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and ligand-drug conjugates thereof
US10640508B2 (en) 2017-10-13 2020-05-05 Massachusetts Institute Of Technology Diazene directed modular synthesis of compounds with quaternary carbon centers
CA3079402A1 (en) * 2017-11-01 2019-05-09 Arrowhead Pharmaceuticals, Inc. Integrin ligands and uses thereof
AU2019277836A1 (en) 2018-05-30 2021-01-21 Debiopharm International, S.A. Anti-CD37 immunoconjugate dosing regimens
CN112543770A (zh) * 2018-06-26 2021-03-23 伊缪诺金公司 靶向adam9的免疫缀合物及其使用方法
WO2020247054A1 (en) 2019-06-05 2020-12-10 Massachusetts Institute Of Technology Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
EP4021511A4 (en) * 2019-08-28 2023-10-04 Starpharma Pty Ltd TARGETED DENDRIMER CONJUGATES
WO2022182415A1 (en) 2021-02-24 2022-09-01 Massachusetts Institute Of Technology Himastatin derivatives, and processes of preparation thereof, and uses thereof

Family Cites Families (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4307016A (en) 1978-03-24 1981-12-22 Takeda Chemical Industries, Ltd. Demethyl maytansinoids
US4563304A (en) 1981-02-27 1986-01-07 Pharmacia Fine Chemicals Ab Pyridine compounds modifying proteins, polypeptides or polysaccharides
US5208020A (en) 1989-10-25 1993-05-04 Immunogen Inc. Cytotoxic agents comprising maytansinoids and their therapeutic use
GB9015198D0 (en) 1990-07-10 1990-08-29 Brien Caroline J O Binding substance
PT1696031E (pt) 1991-12-02 2010-06-25 Medical Res Council Produção de auto-anticorpos a partir de reportórios de segmentos de anticorpo e exibidos em fagos
CA2076465C (en) 1992-03-25 2002-11-26 Ravi V. J. Chari Cell binding agent conjugates of analogues and derivatives of cc-1065
US5639641A (en) 1992-09-09 1997-06-17 Immunogen Inc. Resurfacing of rodent antibodies
US5635483A (en) 1992-12-03 1997-06-03 Arizona Board Of Regents Acting On Behalf Of Arizona State University Tumor inhibiting tetrapeptide bearing modified phenethyl amides
GB9320575D0 (en) 1993-10-06 1993-11-24 Amp Gmbh Coaxial connector having improved locking mechanism
IL111748A0 (en) 1993-12-03 1995-01-24 Zeneca Ltd Proteins
US5773001A (en) 1994-06-03 1998-06-30 American Cyanamid Company Conjugates of methyltrithio antitumor agents and intermediates for their synthesis
US6355780B1 (en) 1995-02-22 2002-03-12 Yeda Research And Development Co. Ltd. Antibodies to the death domain motifs of regulatory proteins
US5714586A (en) 1995-06-07 1998-02-03 American Cyanamid Company Methods for the preparation of monomeric calicheamicin derivative/carrier conjugates
US6680311B1 (en) 1996-08-30 2004-01-20 Eli Lilly And Company Cryptophycin compounds
FR2763066B1 (fr) 1997-05-08 2001-01-05 Agency Ind Science Techn Nouveau compose d'ester aromatique et materiau optique non lineaire de second ordre qui en est produit
CA2297070A1 (en) 1997-08-01 1999-02-11 Morphosys Ag Novel method and phage for the identification of nucleic acid sequences encoding members of a multimeric (poly)peptide complex
US7115396B2 (en) 1998-12-10 2006-10-03 Compound Therapeutics, Inc. Protein scaffolds for antibody mimics and other binding proteins
US7303749B1 (en) 1999-10-01 2007-12-04 Immunogen Inc. Compositions and methods for treating cancer using immunoconjugates and chemotherapeutic agents
ATE349438T1 (de) 1999-11-24 2007-01-15 Immunogen Inc Cytotoxische wirkstoffe enthaltend taxane und deren therapeutische anwendung
PT1242438E (pt) 1999-12-29 2007-02-28 Immunogen Inc Agentes citotóxicos compreendendo dixorrubicinas e daunorrubicinas modificadas e seu uso terapêutico
US6956036B1 (en) 2000-03-17 2005-10-18 Alcon, Inc. 6-hydroxy-indazole derivatives for treating glaucoma
US6333410B1 (en) 2000-08-18 2001-12-25 Immunogen, Inc. Process for the preparation and purification of thiol-containing maytansinoids
US6596503B1 (en) 2000-08-18 2003-07-22 East Carolina University Monoclonal antibody DS6, tumor-associated antigen CA6, and methods of use thereof
US6747021B2 (en) 2000-10-02 2004-06-08 Eli Lilly And Company Cryptophycin compound
US6989450B2 (en) 2000-10-13 2006-01-24 The University Of Mississippi Synthesis of epothilones and related analogs
US7767802B2 (en) 2001-01-09 2010-08-03 Alnylam Pharmaceuticals, Inc. Compositions and methods for inhibiting expression of anti-apoptotic genes
US6441163B1 (en) 2001-05-31 2002-08-27 Immunogen, Inc. Methods for preparation of cytotoxic conjugates of maytansinoids and cell binding agents
US6560782B2 (en) 2001-06-11 2003-05-13 Playtex Products, Inc. Antimicrobial glove and method of making same
US6716821B2 (en) * 2001-12-21 2004-04-06 Immunogen Inc. Cytotoxic agents bearing a reactive polyethylene glycol moiety, cytotoxic conjugates comprising polyethylene glycol linking groups, and methods of making and using the same
DE10202419A1 (de) 2002-01-22 2003-08-07 Ribopharma Ag Verfahren zur Hemmung der Expression eines durch eine Chromosomen-Aberration entstandenen Zielgens
US6756397B2 (en) 2002-04-05 2004-06-29 Immunogen, Inc. Prodrugs of CC-1065 analogs
US6534660B1 (en) 2002-04-05 2003-03-18 Immunogen, Inc. CC-1065 analog synthesis
US6596757B1 (en) 2002-05-14 2003-07-22 Immunogen Inc. Cytotoxic agents comprising polyethylene glycol-containing taxanes and their therapeutic use
WO2004005326A2 (de) 2002-07-09 2004-01-15 Morphochem Aktiengellschaft Fu Tubulysinkonjugate
DK1545613T3 (da) 2002-07-31 2011-11-14 Seattle Genetics Inc Auristatinkonjugater og deres anvendelse til behandling af cancer, en autoimmun sygdom eller en infektiøs sygdom
ES2361739T3 (es) 2002-08-16 2011-06-21 Immunogen, Inc. Reticulantes con elevada reactividad y solubilidad y su uso en la preparación de conjugados para el suministro dirigido de fármacos de molécula pequeña.
KR20050059332A (ko) 2002-11-07 2005-06-17 이뮤노젠 아이엔씨 항-씨디33 항체와 이를 이용한 급성 골수성 백혈병의치료방법
CA2522637C (en) 2003-04-17 2014-01-21 Alnylam Pharmaceuticals, Inc. Modified irna agents
US8088387B2 (en) 2003-10-10 2012-01-03 Immunogen Inc. Method of targeting specific cell populations using cell-binding agent maytansinoid conjugates linked via a non-cleavable linker, said conjugates, and methods of making said conjugates
BRPI0419348B8 (pt) * 2003-05-20 2021-05-25 Immunogen Inc métodos para produzir o conjugado de maitansinóide-agente de ligação celular
US7276497B2 (en) 2003-05-20 2007-10-02 Immunogen Inc. Cytotoxic agents comprising new maytansinoids
US7595306B2 (en) 2003-06-09 2009-09-29 Alnylam Pharmaceuticals Inc Method of treating neurodegenerative disease
EP3604537B1 (en) 2003-06-13 2021-12-08 Alnylam Europe AG Double-stranded ribonucleic acid with increased effectiveness in an organism
JP4584987B2 (ja) 2004-04-30 2010-11-24 アルニラム ファーマスーティカルズ インコーポレイテッド Ｃ５修飾ピリミジンを含むオリゴヌクレオチド
MXPA06014065A (es) * 2004-06-01 2007-01-31 Genentech Inc Conjugados de droga-anticuerpo y metodos.
CA2572151A1 (en) 2004-06-30 2006-08-24 Alnylam Pharmaceuticals, Inc. Oligonucleotides comprising a non-phosphate backbone linkage
WO2006093526A2 (en) 2004-07-21 2006-09-08 Alnylam Pharmaceuticals, Inc. Oligonucleotides comprising a modified or non-natural nucleobase
JP4193771B2 (ja) 2004-07-27 2008-12-10 セイコーエプソン株式会社 階調電圧発生回路及び駆動回路
US7632932B2 (en) 2004-08-04 2009-12-15 Alnylam Pharmaceuticals, Inc. Oligonucleotides comprising a ligand tethered to a modified or non-natural nucleobase
AU2004224925C1 (en) 2004-08-30 2011-07-21 Biotest Ag Immunoconjugates targeting syndecan-1 expressing cells and use thereof
EP1791565B1 (en) * 2004-09-23 2016-04-20 Genentech, Inc. Cysteine engineered antibodies and conjugates
JP2008521828A (ja) 2004-11-29 2008-06-26 シアトル ジェネティックス， インコーポレイテッド 操作された抗体およびイムノコンジュゲート
PL1819359T3 (pl) 2004-12-09 2015-08-31 Janssen Biotech Inc Immunokoniugaty skierowane przeciw integrynie, metody ich wytwarzania oraz ich zastosowanie
WO2006076610A2 (en) 2005-01-14 2006-07-20 Cabot Corporation Controlling ink migration during the formation of printable electronic features
US7301019B2 (en) 2005-01-21 2007-11-27 Immunogen, Inc. Method for the preparation of maytansinoid esters
US20070213292A1 (en) 2005-08-10 2007-09-13 The Rockefeller University Chemically modified oligonucleotides for use in modulating micro RNA and uses thereof
WO2007062466A1 (en) 2005-11-29 2007-06-07 The University Of Sydney Demibodies: dimerisation-activated therapeutic agents
US7897568B2 (en) 2006-03-03 2011-03-01 Vinay K. Singh Compositions for treatment of cancer
EP2446904B1 (en) * 2006-05-30 2015-04-29 Genentech, Inc. Anti-CD22 antibodies, their immunoconjugates and uses thereof
WO2007147213A1 (en) 2006-06-22 2007-12-27 Walter And Eliza Hall Institute Of Medical Research Structure of the insulin receptor ectodomain
CN101802013B (zh) * 2007-07-16 2014-07-02 健泰科生物技术公司 人源化抗cd79b抗体和免疫偶联物及使用方法
SG189817A1 (en) * 2008-04-30 2013-05-31 Immunogen Inc Potent conjugates and hydrophilic linkers

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