EP0941120A4 - Branched peptide linkers - Google Patents

Branched peptide linkers

Info

Publication number
EP0941120A4
EP0941120A4 EP97946428A EP97946428A EP0941120A4 EP 0941120 A4 EP0941120 A4 EP 0941120A4 EP 97946428 A EP97946428 A EP 97946428A EP 97946428 A EP97946428 A EP 97946428A EP 0941120 A4 EP0941120 A4 EP 0941120A4
Authority
EP
European Patent Office
Prior art keywords
peptide linkers
branched peptide
branched
linkers
peptide
Prior art date
Legal status (The legal status 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 status listed.)
Withdrawn
Application number
EP97946428A
Other languages
German (de)
French (fr)
Other versions
EP0941120A1 (en
Inventor
Dalton King
Raymond A Firestone
Gene M Dubowchik
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of EP0941120A1 publication Critical patent/EP0941120A1/en
Publication of EP0941120A4 publication Critical patent/EP0941120A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/641—Branched, dendritic or hypercomb peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides 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-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • C07K5/06052—Val-amino acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EP97946428A 1996-11-05 1997-10-31 Branched peptide linkers Withdrawn EP0941120A4 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US3036796P 1996-11-05 1996-11-05
US30367P 1996-11-05
PCT/US1997/019851 WO1998019705A1 (en) 1996-11-05 1997-10-31 Branched peptide linkers

Publications (2)

Publication Number Publication Date
EP0941120A1 EP0941120A1 (en) 1999-09-15
EP0941120A4 true EP0941120A4 (en) 2004-08-18

Family

ID=21853889

Family Applications (1)

Application Number Title Priority Date Filing Date
EP97946428A Withdrawn EP0941120A4 (en) 1996-11-05 1997-10-31 Branched peptide linkers

Country Status (5)

Country Link
EP (1) EP0941120A4 (en)
JP (1) JP2001505194A (en)
AU (1) AU5159798A (en)
CA (1) CA2264610A1 (en)
WO (1) WO1998019705A1 (en)

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AU739028B2 (en) * 1996-09-27 2001-10-04 Bristol-Myers Squibb Company Hydrolyzable prodrugs for delivery of anticancer drugs to metastatic cells
US6261537B1 (en) 1996-10-28 2001-07-17 Nycomed Imaging As Diagnostic/therapeutic agents having microbubbles coupled to one or more vectors
BR9712683A (en) 1996-10-28 1999-10-19 Nyomed Imaging A S Diagnostic and / or therapeutically active targetable agent, combined formulation, process for preparing and using it, combined formulation, and processes for generating enhanced images of a human or non-human animal body and for in vitro targeting investigation by an agent.
US6331289B1 (en) 1996-10-28 2001-12-18 Nycomed Imaging As Targeted diagnostic/therapeutic agents having more than one different vectors
AU1172599A (en) * 1997-11-18 1999-06-07 Chugai Seiyaku Kabushiki Kaisha Compounds with antitumor activity
JP4560210B2 (en) * 1998-05-22 2010-10-13 第一三共株式会社 Drug complex
CN1661044A (en) * 1998-10-30 2005-08-31 第一制药株式会社 DDS compound and method for measurement thereof
EP1154782A4 (en) * 1999-02-24 2002-09-25 Uab Research Foundation Taxane derivatives for targeted therapy of cancer
AU772074B2 (en) * 1999-04-28 2004-04-08 Vectramed, Inc. Enzymatically activated polymeric drug conjugates
JP2003514903A (en) * 1999-11-24 2003-04-22 イムノージェン インコーポレーテッド Taxane-containing cytotoxic drugs and their therapeutic use
DE10048417A1 (en) * 2000-09-29 2002-04-11 Roche Diagnostics Gmbh Branched linker connections
CA2441484A1 (en) 2001-03-23 2002-10-03 Napro Biotherapeutics, Inc. Molecular conjugates for use in treatment of cancer
AU2002366303B2 (en) * 2001-12-17 2007-09-20 University College Cardiff Consultants Limited Enzymatic cleavable reagents for specific delivery to disease sites
JP2005539009A (en) 2002-08-02 2005-12-22 イミュノジェン・インコーポレーテッド Cytotoxic substances including new potent taxanes and their therapeutic use
US7390898B2 (en) 2002-08-02 2008-06-24 Immunogen Inc. Cytotoxic agents containing novel potent taxanes and their therapeutic use
US20050271615A1 (en) * 2002-08-30 2005-12-08 Doron Shabat Self-immolative dendrimers releasing many active moieties upon a single activating event
WO2004043493A1 (en) * 2002-11-14 2004-05-27 Syntarga B.V. Prodrugs built as multiple self-elimination-release spacers
WO2004081538A2 (en) 2003-03-13 2004-09-23 Irm, Llc Compositions and methods of vinyl oxazolone polymerization
US20040228831A1 (en) * 2003-05-15 2004-11-18 Belinka Benjamin A. Polymeric conjugates for tissue activated drug delivery
CA2534708A1 (en) * 2003-08-05 2005-02-17 Wisconsin Alumni Research Foundation Targeted carrier fusions for delivery of chemotherapeutic agents
ES2408704T3 (en) 2005-01-05 2013-06-21 Biogen Idec Ma Inc. Crypto binding molecules
EP2695608B1 (en) * 2006-10-03 2016-11-23 Arbutus Biopharma Corporation Lipid containing formulations
US9738707B2 (en) 2011-07-15 2017-08-22 Biogen Ma Inc. Heterodimeric Fc regions, binding molecules comprising same, and methods relating thereto
CN104159922B (en) 2012-01-10 2018-03-02 比奥根Ma公司 Transhipment therapeutic molecules are passed through with the enhancing of blood-brain barrier
WO2014194030A2 (en) * 2013-05-31 2014-12-04 Immunogen, Inc. Conjugates comprising cell-binding agents and cytotoxic agents
JP6671292B2 (en) * 2013-12-16 2020-03-25 ジェネンテック， インコーポレイテッド Peptidomimetic compounds and antibody-drug conjugates thereof
PE20161394A1 (en) * 2013-12-16 2017-01-06 Genentech Inc PEPTIDOMIMETIC COMPOUNDS AND THEIR ANTIBODY-DRUG CONJUGATES
CA2937753A1 (en) 2014-02-17 2015-08-20 Seattle Genetics, Inc. Hydrophilic antibody-drug conjugates
WO2015148126A1 (en) * 2014-03-12 2015-10-01 Invictus Oncology Pvt. Ltd. Targeted drug delivery through affinity based linkers
KR101628872B1 (en) 2014-05-28 2016-06-09 주식회사 레고켐 바이오사이언스 Compounds comprising self-immolative group
US10017577B2 (en) 2015-06-15 2018-07-10 Genentech, Inc. Antibodies and immunoconjugates
AU2016359235B2 (en) * 2015-11-25 2022-09-15 Legochem Biosciences, Inc. Antibody-drug conjugates comprising branched linkers and methods related thereto
CN117244076A (en) 2015-11-25 2023-12-19 乐高化学生物科学股份有限公司 Conjugates comprising self-degrading groups and methods related thereto
AU2016359234B2 (en) 2015-11-25 2022-09-08 Legochem Biosciences, Inc. Conjugates comprising peptide groups and methods related thereto
BR112019020136A2 (en) 2017-03-29 2020-04-22 Legochem Biosciences Inc prodrug of pyrrolobenzodiazepine dimer and compound of ligand-ligand conjugate of the same
JP2021513990A (en) 2018-02-20 2021-06-03 シージェン インコーポレイテッド Hydrophobic auristatin F compound and its conjugate
TW202000239A (en) 2018-05-09 2020-01-01 韓商樂高化學生物科學股份有限公司 Compositions and methods related to anti-CD19 antibody drug conjugates
KR20210028544A (en) 2019-09-04 2021-03-12 주식회사 레고켐 바이오사이언스 Antibody-drug conjugate comprising antibody binding to antibody against human ROR1 and its use
US20220031858A1 (en) 2020-08-03 2022-02-03 Bicycle TX Limited Novel linkers
EP4222257A1 (en) 2020-09-30 2023-08-09 F. Hoffmann-La Roche AG Bacterial pilus protein complex fimgt-dsf stabilized protein complexes for producing filamentous phages
AU2022286137A1 (en) * 2021-06-01 2023-12-14 Ajinomoto Co., Inc. Conjugate of antibody and functional substance or salt of said conjugate, and compound for use in production of said conjugate or salt of said compound

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US5563250A (en) * 1987-12-02 1996-10-08 Neorx Corporation Cleavable conjugates for the delivery and release of agents in native form
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US5252713A (en) * 1988-09-23 1993-10-12 Neorx Corporation Polymeric carriers for non-covalent drug conjugation
US5116944A (en) * 1989-12-29 1992-05-26 Neorx Corporation Conjugates having improved characteristics for in vivo administration
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Title
DUBOWCHIK GENE M ET AL: "Doxorubicin immunoconjugates containing bivalent, lysosomally-cleavable dipeptide linkages", BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, vol. 12, no. 11, 3 June 2002 (2002-06-03), pages 1529 - 1532, XP002284221, ISSN: 0960-894X *
KING H D ET AL: "Monoclonal antibody conjugates of doxorubicin prepared with branched linkers: A novel method for increasing the potency of doxorubicin immunoconjugates.", BIOCONJUGATE CHEMISTRY. UNITED STATES 1999 MAR-APR, vol. 10, no. 2, March 1999 (1999-03-01), pages 279 - 288, XP002284220, ISSN: 1043-1802 *
See also references of WO9819705A1 *
SHIH L B ET AL: "ANTHRACYCLINE IMMUNOCONJUGATES PREPARED BY A SITE-SPECIFIC LINKAGE VIA AN AMINODEXTRAN INTERMEDIATE CARRIER", CANCER RESEARCH, vol. 51, no. 16, 1991, pages 4192 - 4198, XP001181850, ISSN: 0008-5472 *
WILLNER DAVID ET AL: "(6-Maleimidocaproyl)hydrazone of doxorubicin-A new derivative for the preparation of immunoconjugates of doxorubicin", BIOCONJUGATE CHEMISTRY, vol. 4, no. 6, 1993, pages 521 - 527, XP002284219, ISSN: 1043-1802 *

Also Published As

Publication number Publication date
EP0941120A1 (en) 1999-09-15
JP2001505194A (en) 2001-04-17
AU5159798A (en) 1998-05-29
WO1998019705A1 (en) 1998-05-14
CA2264610A1 (en) 1998-05-14

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