KR20120080611A - 효능 있는 접합체 및 친수성 링커 - Google Patents

효능 있는 접합체 및 친수성 링커 Download PDF

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Publication number
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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South Korea
Prior art keywords
cell
antibody
bond
maytansinoid
formula
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KR1020127010084A
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English (en)
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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Transplantation (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Cell Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (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

Country Status (7)

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

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2011008328A (es) 2009-02-05 2011-11-04 Immunogen Inc Derivados novedosos de benzodiacepina.
MX338932B (es) 2010-03-12 2016-05-06 Immunogen Inc Moleculas de union cd37 y sus inmunoconjugados.
ES2544608T3 (es) * 2010-11-17 2015-09-02 Genentech, Inc. Conjugados de anticuerpo y de alaninil-maitansinol
WO2012086857A1 (ko) * 2010-12-21 2012-06-28 (주)파낙스이엠 광역학 진단 또는 치료를 위한 결합체 및 이의 제조방법
PL2675479T3 (pl) * 2011-02-15 2016-09-30 Cytotoksyczne pochodne benzodiazepiny
US9447189B2 (en) * 2011-04-01 2016-09-20 Immunogen, Inc. CD37-binding molecules and immunoconjugates thereof
EP2794010A4 (en) * 2011-11-21 2015-10-21 Immunogen Inc METHOD OF TREATING TUMORS RESISTANT TO EGFR THERAPIES BY A CYTOTOXIC EGFR-AGENT ANTIBODY CONJUGATE
WO2014089177A2 (en) 2012-12-04 2014-06-12 Massachusetts Institute Of Technology Compounds, conjugates and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines
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
US9498532B2 (en) * 2013-03-13 2016-11-22 Novartis Ag Antibody drug conjugates
US9415118B2 (en) 2013-03-13 2016-08-16 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
KR20160035600A (ko) * 2013-08-02 2016-03-31 사노피 고형 종양의 치료를 위한 항-muc1 메이탄시노이드 면역접합체 항체의 용도
EP3038624B1 (en) * 2013-08-26 2024-09-25 Regeneron Pharmaceuticals, Inc. Pharmaceutical compositions comprising macrolide diastereomers, methods of their synthesis and therapeutic uses
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
JP6747971B2 (ja) 2013-10-15 2020-08-26 シアトル ジェネティックス， インコーポレイテッド 改善されたリガンド−薬物コンジュゲート薬物動態のためのｐｅｇ化薬物−リンカー
WO2015113476A1 (zh) * 2014-01-29 2015-08-06 上海恒瑞医药有限公司 配体-细胞毒性药物偶联物、其制备方法及其应用
GB201402009D0 (en) 2014-02-06 2014-03-26 Oncomatryx Biopharma S L Antibody-drug conjugates and immunotoxins
US10550190B2 (en) * 2014-04-04 2020-02-04 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
PE20170903A1 (es) * 2014-08-12 2017-07-12 Novartis Ag Conjugados de farmacos con anticuerpos anti-cdh6
MA40539A (fr) * 2014-09-02 2016-03-10 Immunogen Inc Procédés de formulation de compositions de conjugués anticorps-médicaments
EP3912982A1 (en) * 2015-03-19 2021-11-24 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
US20170000900A1 (en) 2015-06-08 2017-01-05 Immunogen, Inc. Anti-cd37 immunoconjugate and anti-cd20 antibody combinations
IL305279A (en) 2015-07-21 2023-10-01 Immunogen Inc Methods for the preparation of cytotoxic benzodiazepine compounds
CN108699144B (zh) 2015-08-28 2022-07-19 德彪发姆国际有限公司 用于检测cd37的抗体和测定
SG11201804268RA (en) 2015-12-04 2018-06-28 Seattle Genetics Inc Conjugates of quaternized tubulysin compounds
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
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
NZ744373A (en) 2016-01-25 2025-03-28 Regeneron Pharma Maytansinoid derivatives, conjugates thereof, and methods of use
EA201892040A1 (ru) 2016-03-25 2019-04-30 Сиэтл Дженетикс, Инк. Способ получения пегилированных соединений лекарственный препарат - линкер и их промежуточных соединений
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
CA3037732A1 (en) * 2016-09-23 2018-03-29 Regeneron Pharmaceuticals, Inc. Anti-steap2 antibodies, antibody-drug conjugates, and bispecific antigen-binding molecules that bind steap2 and cd3, and uses thereof
US11278629B2 (en) 2016-11-02 2022-03-22 Debiopharm International, S.A. Methods for improving anti-CD37 immunoconjugate therapy
EP3554544A4 (en) 2016-12-16 2020-07-29 Bluefin Biomedicine, Inc. ANTI-PROTEIN 1 ANTIBODY CONTAINING AN ANTI-CUB DOMAIN (CDCP1), ANTIBODY-DRUG CONJUGATES AND THEIR METHODS OF USE
KR102648564B1 (ko) 2017-03-24 2024-03-19 씨젠 인크. 글루쿠로니드 약물-링커의 제조 공정 및 그 중간물
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
MY208467A (en) * 2017-11-01 2025-05-11 Arrowhead Pharmaceuticals Inc Integrin ligands and uses thereof
CA3101790A1 (en) 2018-05-30 2019-12-05 Debiopharm International, S.A. Anti-cd37 immunoconjugate dosing regimens
WO2020005945A1 (en) * 2018-06-26 2020-01-02 Immunogen, Inc. Immunoconjugates targeting adam9 and methods of use thereof
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
DE69233782D1 (de) 1991-12-02 2010-05-20 Medical Res Council Herstellung von Autoantikörpern auf Phagenoberflächen ausgehend von Antikörpersegmentbibliotheken
EP0563475B1 (en) 1992-03-25 2000-05-31 Immunogen Inc Cell binding agent conjugates of 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
NZ517772A (en) 1999-11-24 2004-03-26 Immunogen Inc Cytotoxic agents comprising taxanes and their therapeutic use
CA2395660A1 (en) 1999-12-29 2001-07-12 Immunogen, Inc. Cytotoxic agents comprising modified doxorubicins and daunorubicins and their therapeutic use
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
JP2005500974A (ja) 2000-10-13 2005-01-13 ザ ユニバーシテイ オブ ミシシッピー エポシロン類及び関連類似体の合成
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
US20060159838A1 (en) 2005-01-14 2006-07-20 Cabot Corporation Controlling ink migration during the formation of printable electronic features
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
US6534660B1 (en) 2002-04-05 2003-03-18 Immunogen, Inc. CC-1065 analog synthesis
US6756397B2 (en) 2002-04-05 2004-06-29 Immunogen, Inc. Prodrugs of CC-1065 analogs
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
EP2353611B1 (en) 2002-07-31 2015-05-13 Seattle Genetics, Inc. Drug conjugates and their use for treating cancer, an autoimmune disease or an infectious disease
ATE499116T1 (de) 2002-08-16 2011-03-15 Immunogen Inc Vernetzer mit hoher reaktivität und löslichkeit und ihre verwendung bei der herstellung von konjugaten für die gezielte abgabe von kleinmolekularen arzneimitteln
AU2003285878B2 (en) 2002-11-07 2011-04-28 Immunogen, Inc. Anti-CD33 antibodies and method for treatment of acute myeloid leukemia using the same
JP4597976B2 (ja) 2003-04-17 2010-12-15 アルナイラム ファーマシューティカルズ インコーポレイテッド 修飾ｉＲＮＡ剤
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
NZ542695A (en) * 2003-05-20 2009-04-30 Immunogen Inc Improved cytotoxic agents comprising new maytansinoids
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
AU2004263830B2 (en) 2003-06-13 2008-12-18 Alnylam Pharmaceuticals, Inc. Double-stranded ribonucleic acid with increased effectiveness in an organism
EP3034510A1 (en) 2004-04-30 2016-06-22 Alnylam Pharmaceuticals Inc. Oligonucleotides comprising a c5-modified pyrimidine
EP1753463A2 (en) * 2004-06-01 2007-02-21 Genentech, Inc. Antibody drug conjugates and methods
US7615618B2 (en) 2004-06-30 2009-11-10 Alnylam Pharmaceuticals, Inc. Oligonucleotides comprising a non-phosphate backbone linkage
AU2005328382C1 (en) 2004-07-21 2013-01-24 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
WO2006112872A2 (en) 2004-08-04 2006-10-26 Alnylam Pharmaceuticals, Inc. Oligonucleotides comprising a ligand tethered to a modified or non-natural nucleobase
US20060045877A1 (en) 2004-08-30 2006-03-02 Goldmakher Viktor S Immunoconjugates targeting syndecan-1 expressing cells and use thereof
RU2412947C2 (ru) * 2004-09-23 2011-02-27 Дженентек, Инк. Антитела, сконструированные на основе цистеинов, и их конъюгаты
CA2587589A1 (en) 2004-11-29 2006-06-22 Seattle Genetics, Inc. Engineered antibodies and immunoconjugates
UA94388C2 (ru) 2004-12-09 2011-05-10 Центокор, Инк. Антиинтегриновый иммуноконьюгат и способы лечения с его помощью
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
EP2447282B1 (en) * 2006-05-30 2016-01-27 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
PE20140625A1 (es) * 2007-07-16 2014-05-29 Genentech Inc ANTICUERPOS ANTI-CD79b E INMUNOCONJUGADOS HUMANIZADOS
UA108598C2 (xx) * 2008-04-30 2015-05-25 Високоефективні кон'югати та гідрофільні зшиваючі агенти (лінкери)

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