SG11201507619PA - Cytotoxic and anti-mitotic compounds, and methods of using the same - Google Patents

Cytotoxic and anti-mitotic compounds, and methods of using the same

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Publication number
SG11201507619PA
SG11201507619PA SG11201507619PA SG11201507619PA SG11201507619PA SG 11201507619P A SG11201507619P A SG 11201507619PA SG 11201507619P A SG11201507619P A SG 11201507619PA SG 11201507619P A SG11201507619P A SG 11201507619PA SG 11201507619P A SG11201507619P A SG 11201507619PA
Authority
SG
Singapore
Prior art keywords
cytotoxic
methods
same
mitotic compounds
mitotic
Prior art date
Application number
SG11201507619PA
Other languages
English (en)
Inventor
Geoffrey C Winters
Alexander Laurence Mandel
James R Rich
Bradley John Hedberg
Tom Han Hsiao Hsieh
Elyse Marie Josée Bourque
John Babcook
Original Assignee
Ct For Drug Res And Dev
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ct For Drug Res And Dev filed Critical Ct For Drug Res And Dev
Publication of SG11201507619PA publication Critical patent/SG11201507619PA/en

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    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05—Dipeptides
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
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    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
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Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2968440T (pt) * 2013-03-15 2019-07-31 Zymeworks Inc Compostos citotóxicos e antimitóticos e métodos de utilização dos mesmos
CA2935064C (en) 2013-12-27 2023-06-27 Zymeworks Inc. Var2csa-drug conjugates
EP3086815B1 (en) * 2013-12-27 2022-02-09 Zymeworks Inc. Sulfonamide-containing linkage systems for drug conjugates
EP3194421B1 (en) 2014-09-17 2021-11-03 Zymeworks Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
GB201416960D0 (en) * 2014-09-25 2014-11-12 Antikor Biopharma Ltd Biological materials and uses thereof
JP6733993B2 (ja) * 2014-10-03 2020-08-05 シンアフィックス ビー．ブイ． スルファミドリンカー、スルファミドリンカーのコンジュゲート、及び調製の方法
PL3240785T3 (pl) 2014-12-29 2021-12-06 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Inhibitory drobnocząsteczkowe dehydrogenazy mleczanowej i sposoby ich wykorzystania
EP3250237B1 (en) 2015-01-30 2021-05-26 Sutro Biopharma, Inc. Hemiasterlin derivatives for conjugation and therapy
SG11201802777XA (en) 2015-10-14 2018-05-30 X Therma Inc Compositions and methods for reducing ice crystal formation
JP2017200902A (ja) * 2016-02-08 2017-11-09 シンアフィックス ビー．ブイ． Ｈｅｒ２腫瘍を標的化するための改善された治療指数を有する新規な抗体−コンジュゲート及び抗体−コンジュゲートの治療指数を改善するための方法
JP2017197512A (ja) * 2016-02-08 2017-11-02 シンアフィックス ビー．ブイ． Ｃｄ３０腫瘍を標的化するための改善された治療指数を有する新規な抗体−コンジュゲート及び抗体−コンジュゲートの治療指数を改善するための方法
SG10202007520WA (en) 2016-03-02 2020-09-29 Eisai R&D Man Co Ltd Eribulin-based antibody-drug conjugates and methods of use
ES2901197T3 (es) 2016-03-22 2022-03-21 Merck Sharp & Dohme Moduladores alostéricos de los receptores nicotínicos de la acetilcolina
US10517958B2 (en) 2016-10-04 2019-12-31 Zymeworks Inc. Compositions and methods for the treatment of platinum-drug resistant cancer
WO2018187563A1 (en) 2017-04-06 2018-10-11 Nissan Chemical America Corporation Hydrocarbon formation treatment micellar solutions
ES2974288T3 (es) 2017-08-10 2024-06-26 Sumitomo Pharma Co Ltd Conjugados de anticuerpo-fármaco que incluyen un derivado de hemiasterlina
US12018093B2 (en) 2017-08-10 2024-06-25 Sumitomo Pharma Co., Ltd. Hemiasterlin derivatives and antibody-drug conjugates including same
JP2021006595A (ja) 2017-09-13 2021-01-21 日産化学株式会社 原油回収用薬液
CA3080924C (en) 2017-11-03 2022-03-29 Nissan Chemical America Corporation Using brine resistant silicon dioxide nanoparticle dispersions to improve oil recovery
JP2021526792A (ja) 2018-06-06 2021-10-11 マサチューセッツ インスティテュート オブ テクノロジー 真核細胞における翻訳のための環状ｒｎａ
RU2695787C1 (ru) * 2018-11-07 2019-07-26 Федеральное государственное бюджетное учреждение "Национальный медицинский исследовательский центр онкологии имени Н.Н. Петрова" Министерства здравоохранения Российской Федерации Применение соединения 2-[3-(2-хлорэтил)-3-нитрозоуреидо]-1,3-пропандиол для лечения her2-положительных опухолей в эксперименте
CA3127312A1 (en) 2019-02-13 2020-08-20 Sumitomo Dainippon Pharma Co., Ltd. Hemiasterlin derivative having cysteine residue
JP7479302B2 (ja) * 2019-02-13 2024-05-08 住友ファーマ株式会社 ヘミアスタリン誘導体とその抗体薬物複合体
JP2020132638A (ja) * 2019-02-13 2020-08-31 大日本住友製薬株式会社 ヘミアスタリン誘導体を含む抗体薬物複合体を含有する医薬
SG11202112922WA (en) 2019-05-22 2021-12-30 Massachusetts Inst Technology Circular rna compositions and methods
EP3920976B1 (en) 2019-12-04 2023-07-19 Orna Therapeutics, Inc. Circular rna compositions and methods

Family Cites Families (137)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2036891B (en) 1978-12-05 1983-05-05 Windsor Smith C Change speed gear
CA1213229A (en) 1982-04-12 1986-10-28 Gary S. David Antibodies having dual specificities, their preparation and uses therefor
GB8308235D0 (en) 1983-03-25 1983-05-05 Celltech Ltd Polypeptides
US4816567A (en) 1983-04-08 1989-03-28 Genentech, Inc. Recombinant immunoglobin preparations
JPS6147500A (ja) 1984-08-15 1986-03-07 Res Dev Corp Of Japan キメラモノクロ−ナル抗体及びその製造法
EP0173494A3 (en) 1984-08-27 1987-11-25 The Board Of Trustees Of The Leland Stanford Junior University Chimeric receptors by dna splicing and expression
GB8422238D0 (en) 1984-09-03 1984-10-10 Neuberger M S Chimeric proteins
JPS61134325A (ja) 1984-12-04 1986-06-21 Teijin Ltd ハイブリツド抗体遺伝子の発現方法
CA1282069C (en) 1985-09-12 1991-03-26 Damon L. Meyer Antibody complexes of hapten-modified diagnostic or therapeutic agents
WO1987002671A1 (en) 1985-11-01 1987-05-07 International Genetic Engineering, Inc. Modular assembly of antibody genes, antibodies prepared thereby and use
US5225539A (en) 1986-03-27 1993-07-06 Medical Research Council Recombinant altered antibodies and methods of making altered antibodies
US4946778A (en) 1987-09-21 1990-08-07 Genex Corporation Single polypeptide chain binding molecules
US5053394A (en) 1988-09-21 1991-10-01 American Cyanamid Company Targeted forms of methyltrithio antitumor agents
FI102355B (fi) 1988-02-11 1998-11-30 Squibb Bristol Myers Co Menetelmä yhdistävän välikappaleen omaavien antrasykliini-immunokonjug aattien valmistamiseksi
US5006652A (en) 1988-08-08 1991-04-09 Eli Lilly And Company Intermediates for antibody-vinca drug conjugates
US5028697A (en) 1988-08-08 1991-07-02 Eli Lilly And Company Cytotoxic antibody conjugates of hydrazide derivatized methotrexate analogs via simple organic linkers
US5094849A (en) 1988-08-08 1992-03-10 Eli Lilly And Company Cytotoxic antibody conjugates of hydrazide derivatized vinca analogs via simple organic linkers
US5530101A (en) 1988-12-28 1996-06-25 Protein Design Labs, Inc. Humanized immunoglobulins
US5137877B1 (en) 1990-05-14 1996-01-30 Bristol Myers Squibb Co Bifunctional linking compounds conjugates and methods for their production
GB9017024D0 (en) 1990-08-03 1990-09-19 Erba Carlo Spa New linker for bioactive agents
US5633425A (en) 1990-08-29 1997-05-27 Genpharm International, Inc. Transgenic non-human animals capable of producing heterologous antibodies
US5661016A (en) 1990-08-29 1997-08-26 Genpharm International Inc. Transgenic non-human animals capable of producing heterologous antibodies of various isotypes
EP0814159B1 (en) 1990-08-29 2005-07-27 GenPharm International, Inc. Transgenic mice capable of producing heterologous antibodies
US5625126A (en) 1990-08-29 1997-04-29 Genpharm International, Inc. Transgenic non-human animals for producing heterologous antibodies
US5545806A (en) 1990-08-29 1996-08-13 Genpharm International, Inc. Ransgenic non-human animals for producing heterologous antibodies
WO1993008829A1 (en) 1991-11-04 1993-05-13 The Regents Of The University Of California Compositions that mediate killing of hiv-infected cells
US5622929A (en) 1992-01-23 1997-04-22 Bristol-Myers Squibb Company Thioether conjugates
ATE149570T1 (de) 1992-08-17 1997-03-15 Genentech Inc Bispezifische immunoadhesine
US6569834B1 (en) 1992-12-03 2003-05-27 George R. Pettit Elucidation and synthesis of antineoplastic tetrapeptide w-aminoalkyl-amides
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
NZ258882A (en) 1992-12-16 1997-06-24 Basf Ag Antineoplastic peptides and compositions thereof
US5780588A (en) 1993-01-26 1998-07-14 Arizona Board Of Regents Elucidation and synthesis of selected pentapeptides
US5556623A (en) 1993-03-30 1996-09-17 Eli Lilly And Company Antibody-drug conjugates
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
AU689131B2 (en) 1993-10-01 1998-03-26 Teikoku Hormone Mfg. Co., Ltd. Novel peptide derivative
US5599902A (en) 1994-11-10 1997-02-04 Arizona Board Of Regents Acting On Behalf Of Arizona State University Cancer inhibitory peptides
US5663149A (en) 1994-12-13 1997-09-02 Arizona Board Of Regents Acting On Behalf Of Arizona State University Human cancer inhibitory pentapeptide heterocyclic and halophenyl amides
GB9508195D0 (en) 1995-04-20 1995-06-07 Univ British Columbia Novel biologically active compounds and compositions,their use and derivation
DE69637383T2 (de) 1995-05-10 2008-12-11 Kyowa Hakko Kogyo Co., Ltd. Cytotoxinkonjugate umfassend dipeptide
CA2249195A1 (en) 1996-03-18 1997-09-25 Board Of Regents, The University Of Texas System Immunoglobin-like domains with increased half lives
US6759509B1 (en) 1996-11-05 2004-07-06 Bristol-Myers Squibb Company Branched peptide linkers
CA2225325A1 (en) 1997-12-19 1999-06-19 The University Of British Columbia Hemiasterlin analogs
US8097648B2 (en) 1998-06-17 2012-01-17 Eisai R&D Management Co., Ltd. Methods and compositions for use in treating cancer
EP1149843A4 (en) * 1999-01-28 2012-06-06 Chugai Pharmaceutical Co Ltd SUBSTITUTED PHENETHYLAMINE DERIVATIVES
US6468522B1 (en) 1999-07-22 2002-10-22 University Of Medicine And Dentistry Of New Jersey Controlled release of thioamide moiety-containing therapeutic agents
US6323315B1 (en) 1999-09-10 2001-11-27 Basf Aktiengesellschaft Dolastatin peptides
US6756037B2 (en) 2000-03-31 2004-06-29 Enzon, Inc. Polymer conjugates of biologically active agents and extension moieties for facilitating conjugation of biologically active agents to polymeric terminal groups
TWI245034B (en) 2000-07-24 2005-12-11 Matsushita Electric Ind Co Ltd Capacitor
US6884869B2 (en) 2001-04-30 2005-04-26 Seattle Genetics, Inc. Pentapeptide compounds and uses related thereto
WO2003026577A2 (en) 2001-09-24 2003-04-03 Seattle Genetics, Inc. P-amidobenzylethers in drug delivery agents
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
AU2003224644A1 (en) 2002-02-27 2003-09-09 The Government Of The United States Of America, Represented By The Secretary, Department Of Healtan Conjugates of ligand, linker and cytotoxic agent and related compositions and methods of use
US7064211B2 (en) 2002-03-22 2006-06-20 Eisai Co., Ltd. Hemiasterlin derivatives and uses thereof
KR101208266B1 (ko) 2002-03-22 2012-12-05 에자이 알앤드디 매니지먼트 가부시키가이샤 헤미아스텔린 유도체 및 이의 용도
WO2003090678A2 (en) 2002-04-23 2003-11-06 Ohio State University Antileishmanial dinitroaniline sulfonamides with activity against parasite tubulin
ITMI20021391A1 (it) 2002-06-25 2003-12-29 Nicox Sa Nitroderivati di inibitori della cicloossigenasi-2
HUE027549T2 (hu) 2002-07-31 2016-10-28 Seattle Genetics Inc Hatóanyagot tartalmazó konjugátumok és alkalmazásuk rák, autoimmun betegség vagy fertõzéses betegség kezelésére
US20050180972A1 (en) 2002-07-31 2005-08-18 Wahl Alan F. Anti-CD20 antibody-drug conjugates for the treatment of cancer and immune disorders
US7087229B2 (en) 2003-05-30 2006-08-08 Enzon Pharmaceuticals, Inc. Releasable polymeric conjugates based on aliphatic biodegradable linkers
US7122189B2 (en) 2002-08-13 2006-10-17 Enzon, Inc. Releasable polymeric conjugates based on aliphatic biodegradable linkers
AU2003259163B2 (en) 2002-08-16 2008-07-03 Immunogen, Inc. Cross-linkers with high reactivity and solubility and their use in the preparation of conjugates for targeted delivery of small molecule drugs
MXPA05002874A (es) 2002-09-20 2005-05-27 Wyeth Corp Procedimiento para la sintesis de intermediarios utiles para la sintesis de inhibidores de tubulina.
US20040121965A1 (en) 2002-09-20 2004-06-24 Wyeth Holdings Corporation Method of treating resistant tumors
AU2003282624A1 (en) 2002-11-14 2004-06-03 Syntarga B.V. Prodrugs built as multiple self-elimination-release spacers
US20070026478A1 (en) 2002-11-21 2007-02-01 Wyeth Hemiasterlin affinity probes and their uses
US7332164B2 (en) 2003-03-21 2008-02-19 Enzon Pharmaceuticals, Inc. Heterobifunctional polymeric bioconjugates
US7390910B2 (en) 2003-08-08 2008-06-24 Wyeth Compounds for treating tumors
US7576206B2 (en) 2003-08-14 2009-08-18 Cephalon, Inc. Proteasome inhibitors and methods of using the same
NZ546417A (en) 2003-09-15 2009-09-25 Univ British Columbia Ceratamines A and B, and analogues, syntheses and pharmaceutical compositions thereof
DE602004025834D1 (de) 2003-10-22 2010-04-15 Univ Johns Hopkins Die behandlung von tumoren
US7078562B2 (en) 2004-01-19 2006-07-18 Mitsubishi Gas Chemical Company, Inc. Adamantane derivatives and resin compositions using the same as raw material
US20050175619A1 (en) 2004-02-05 2005-08-11 Robert Duffy Methods of producing antibody conjugates
US7375078B2 (en) 2004-02-23 2008-05-20 Genentech, Inc. Heterocyclic self-immolative linkers and conjugates
NZ550934A (en) 2004-05-19 2010-05-28 Medarex Inc Chemical linkers and conjugates thereof
CN101039701A (zh) 2004-08-26 2007-09-19 尼古拉斯皮拉马尔印度有限公司 含有生物可裂解二硫化物连接物的前药和共药
KR20070053214A (ko) 2004-08-26 2007-05-23 니콜라스 피라말 인디아 리미티드 신규 생분해성 링커를 함유하는 프로드럭
US8288352B2 (en) 2004-11-12 2012-10-16 Seattle Genetics, Inc. Auristatins having an aminobenzoic acid unit at the N terminus
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
US7714016B2 (en) 2005-04-08 2010-05-11 Medarex, Inc. Cytotoxic compounds and conjugates with cleavable substrates
US8871720B2 (en) 2005-07-07 2014-10-28 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine carboxy modifications at the C-terminus
AU2006269422B2 (en) 2005-07-07 2012-12-06 Seagen Inc. Monomethylvaline compounds having phenylalanine side-chain modifications at the C-terminus
HUE035853T2 (en) 2005-07-18 2018-05-28 Seattle Genetics Inc Beta-glucuronide-linker-drug conjugates
CA2617907A1 (en) 2005-08-05 2007-02-15 Syntarga B.V. Triazole-containing releasable linkers and conjugates comprising the same
US20080279868A1 (en) 2005-09-26 2008-11-13 Medarex, Inc. Antibody-Drug Conjugates and Methods of Use
WO2007059404A2 (en) 2005-11-10 2007-05-24 Medarex, Inc. Duocarmycin derivatives as novel cytotoxic compounds and conjugates
WO2007103288A2 (en) 2006-03-02 2007-09-13 Seattle Genetics, Inc. Engineered antibody drug conjugates
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
US8664407B2 (en) 2007-02-21 2014-03-04 Medarex, LLC Chemical linkers with single amino acids and conjugates thereof
KR101396696B1 (ko) 2007-10-10 2014-05-16 노파르티스 아게 스피로피롤리딘, 및 ｈｃｖ 및 ｈｉｖ 감염에 대한 그의 용도
US20090155289A1 (en) 2007-11-01 2009-06-18 Steve Roberts Furin-cleavable peptide linkers for drug-ligand conjugates
WO2009095447A1 (en) 2008-01-30 2009-08-06 Pieris Ag Muteins of tear lipocalin having affinity to human c-met receptor tyrosine kinase and methods for obtaining the same
BRPI0908268A2 (pt) * 2008-02-29 2018-10-30 Array Biopharma Inc compostos do inibidor de raf e seus métodos de uso
DK2265283T3 (da) 2008-03-18 2014-10-20 Seattle Genetics Inc Auristatin-lægemiddel-linker-konjugater
SG189817A1 (en) 2008-04-30 2013-05-31 Immunogen Inc Potent conjugates and hydrophilic linkers
KR101764081B1 (ko) 2008-04-30 2017-08-01 이뮤노젠 아이엔씨 가교제 및 그 용도
KR20110029156A (ko) 2008-06-27 2011-03-22 메뤼스 베.페. 항체 생산 비-인간 포유동물
GB2461546B (en) 2008-07-02 2010-07-07 Argen X Bv Antigen binding polypeptides
EP2326349B1 (en) 2008-07-21 2015-02-25 Polytherics Limited Novel reagents and method for conjugating biological molecules
EP2341942A1 (en) * 2008-09-19 2011-07-13 Nektar Therapeutics Polymer conjugates of therapeutic peptides
CN104404068A (zh) 2008-11-21 2015-03-11 哥本哈根大学 免疫应答的引发
US20110182850A1 (en) 2009-04-10 2011-07-28 Trixi Brandl Organic compounds and their uses
CN102448469A (zh) 2009-05-28 2012-05-09 摩萨纳医疗有限公司 包括具有可变的释放速率的连接物的聚缩醛(酮)-药物共轭物
US8394922B2 (en) 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
TW201117809A (en) 2009-09-25 2011-06-01 Astellas Pharma Inc Substituted amide compounds
CN102971340A (zh) 2010-03-29 2013-03-13 酵活有限公司 具有增强的或抑制的效应子功能的抗体
CN103097417B (zh) 2010-04-20 2019-04-09 根马布股份公司 含异二聚体抗体fc的蛋白及其制备方法
ES2528956T3 (es) 2010-06-10 2015-02-13 Seattle Genetics, Inc. Nuevos derivados de auristatina y su uso
WO2012032080A1 (en) 2010-09-07 2012-03-15 F-Star Biotechnologische Forschungs- Und Entwicklungsges.M.B.H Stabilised human fc
AU2011307040A1 (en) 2010-09-24 2013-04-11 Astellas Pharma Inc. Substituted amide compound
CA2813411C (en) 2010-11-05 2016-08-02 Rinat Neuroscience Corporation Engineered polypeptide conjugates and methods for making thereof using transglutaminase
US10294270B2 (en) 2011-02-25 2019-05-21 Lonza Ltd Branched linker for protein drug conjugates
AU2012222833B2 (en) 2011-03-03 2017-03-16 Zymeworks Inc. Multivalent heteromultimer scaffold design and constructs
US9200034B2 (en) 2011-03-16 2015-12-01 Council Of Scientific & Industrial Research Oligopeptides and process for preparation thereof
AU2012236511B2 (en) 2011-03-30 2016-04-28 Arizona Board Of Regents, For And On Behalf Of, Arizona State University Auristatin tyramine phosphate salts and auristatin aminoquinoline derivatives and prodrugs thereof
KR102023496B1 (ko) 2011-04-21 2019-09-20 시애틀 지네틱스, 인크. 신규 결합제-약물 콘주게이트 (adc) 및 그의 용도
CN110078787A (zh) 2011-05-27 2019-08-02 Ambrx 公司 含有非天然氨基酸连接的海兔毒素衍生物的组合物、涉及该海兔毒素衍生物的方法及其用途
CN106110332B (zh) 2011-06-10 2018-11-30 梅尔莎纳医疗公司 蛋白质-聚合物-药物共轭物
UA117901C2 (uk) 2011-07-06 2018-10-25 Ґенмаб Б.В. Спосіб посилення ефекторної функції вихідного поліпептиду, його варіанти та їх застосування
US20130190248A1 (en) 2011-07-26 2013-07-25 Agensys, Inc. Substituted peptide analogs
EP2776409B1 (en) * 2011-11-09 2016-02-03 Ensemble Therapeutics Corporation Macrocyclic compounds for inhibition of inhibitors of apoptosis
WO2013068874A1 (en) 2011-11-11 2013-05-16 Pfizer Inc. Antibody-drug conjugates
SI3327027T1 (sl) 2011-11-17 2021-03-31 Pfizer Inc. Citotoksični peptidi in njihovi konjugati zdravil s protitelesi
JP6517018B2 (ja) 2012-02-09 2019-05-22 ヴァー２・ファーマシューティカルズ・アンパルトセルスカブＶＡＲ２ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ ＡｐＳ コンドロイチン硫酸グリカンのターゲティング
US9801951B2 (en) 2012-05-15 2017-10-31 Concortis Biosystems, Corp. Drug-conjugates, conjugation methods, and uses thereof
EP3536700A1 (en) 2012-06-07 2019-09-11 Ambrx, Inc. Prostate-specific membrane antigen antibody drug conjugates
AU2013277169B2 (en) 2012-06-19 2017-02-02 Ambrx, Inc. Anti-CD70 antibody drug conjugates
SG10201610869TA (en) 2012-06-26 2017-02-27 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalacti
CA2930030A1 (en) * 2012-11-09 2014-05-15 Ensemble Therapeutics Corporation Macrocyclic compounds for inhibition of inhibitors of apoptosis
CN105849086B (zh) 2012-11-24 2018-07-31 杭州多禧生物科技有限公司 亲水性链接体及其在药物分子和细胞结合分子共轭反应上的应用
KR20150119848A (ko) 2012-12-21 2015-10-26 바이오얼라이언스 씨.브이. 친수성 자기-희생 링커 및 그것의 포합체
PT2968440T (pt) 2013-03-15 2019-07-31 Zymeworks Inc Compostos citotóxicos e antimitóticos e métodos de utilização dos mesmos
RU2016134258A (ru) 2013-10-15 2018-02-28 Сорренто Терапьютикс Инк. Конъюгат лекарственного средства с направляющей молекулой и двумя различными лекарственными средствами
MX2016007865A (es) 2013-12-17 2017-01-11 Novartis Ag Peptidos citotoxicos y conjugados de los mismos.
EP3086815B1 (en) * 2013-12-27 2022-02-09 Zymeworks Inc. Sulfonamide-containing linkage systems for drug conjugates
CA2935064C (en) 2013-12-27 2023-06-27 Zymeworks Inc. Var2csa-drug conjugates
EP3194421B1 (en) 2014-09-17 2021-11-03 Zymeworks Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
US10975112B2 (en) 2015-06-16 2021-04-13 Hangzhou Dac Biotech Co., Ltd. Linkers for conjugation of cell-binding molecules

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