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Withdrawn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Withdrawn legal-status Critical Current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)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)

Families Citing this family (41)

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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
CA2270120A1 (en) 1996-10-28 1998-05-07 Pal Rongved Improvements in or relating to diagnostic/therapeutic agents
US6331289B1 (en) 1996-10-28 2001-12-18 Nycomed Imaging As Targeted diagnostic/therapeutic agents having more than one different vectors
EP1033372A4 (en) * 1997-11-18 2000-10-04 Chugai Pharmaceutical Co Ltd Compounds with antitumor activity
US6835807B1 (en) * 1998-05-22 2004-12-28 Daiichi Pharmaceuticals Co., Ltd. Drug complex and drug delivery system
EA003790B1 (en) * 1998-10-30 2003-10-30 Дайити Фармасьютикал Ко., Лтд. Ddc compounds and methods for assaying the same
AU768027B2 (en) * 1999-02-24 2003-11-27 Uab Research Foundation, The Taxane derivatives for targeted therapy of cancer
AU772074B2 (en) * 1999-04-28 2004-04-08 Vectramed, Inc. Enzymatically activated polymeric drug conjugates
AU765588C (en) 1999-11-24 2004-12-16 Immunogen, Inc. Cytotoxic agents comprising taxanes and their therapeutic use
DE10048417A1 (en) * 2000-09-29 2002-04-11 Roche Diagnostics Gmbh Branched linker connections
US6825166B2 (en) 2001-03-23 2004-11-30 Tapestry Pharmaceuticals, 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
US7390898B2 (en) 2002-08-02 2008-06-24 Immunogen Inc. Cytotoxic agents containing novel potent taxanes and their therapeutic use
BR0313197A (en) 2002-08-02 2005-08-09 Immunogen Inc Cytotoxic agents containing potent taxanes and their therapeutic use
WO2004019993A1 (en) * 2002-08-30 2004-03-11 Ramot At Tel Aviv University Ltd. Self-immolative dendrimers releasing many active moieties upon a single activating event
EP1560599A1 (en) * 2002-11-14 2005-08-10 Syntarga B.V. Prodrugs built as multiple self-elimination-release spacers
US6906158B2 (en) 2003-03-13 2005-06-14 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
JP2007501014A (en) * 2003-08-05 2007-01-25 ウイスコンシン アラムニ リサーチ ファンデーション Targeted carrier fusion for delivery of chemotherapeutic agents
SG173313A1 (en) 2005-01-05 2011-08-29 Biogen Idec Inc Cripto binding molecules
DK2068886T3 (en) * 2006-10-03 2013-11-18 Tekmira Pharmaceuticals Corp Lipid-containing preparations
US9738707B2 (en) 2011-07-15 2017-08-22 Biogen Ma Inc. Heterodimeric Fc regions, binding molecules comprising same, and methods relating thereto
KR102104686B1 (en) 2012-01-10 2020-04-24 바이오젠 엠에이 인코포레이티드 Enhancement of transport of therapeutic molecules across the blood brain barrier
WO2014194030A2 (en) * 2013-05-31 2014-12-04 Immunogen, Inc. Conjugates comprising cell-binding agents and cytotoxic agents
RU2689388C1 (en) * 2013-12-16 2019-05-28 Дженентек, Инк. Peptidomimetic compounds and their conjugates of antibodies with drugs
EP3082875B1 (en) 2013-12-16 2020-11-25 Genentech, Inc. Peptidomimetic compounds and antibody-drug conjugates thereof
MX2016009862A (en) 2014-02-17 2016-10-31 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
JP2018524295A (en) 2015-06-15 2018-08-30 ジェネンテック， インコーポレイテッド Antibodies and immune complexes
AU2016359234B2 (en) 2015-11-25 2022-09-08 Legochem Biosciences, Inc. Conjugates comprising peptide groups and methods related thereto
CN113599533A (en) 2015-11-25 2021-11-05 乐高化学生物科学股份有限公司 Antibody-drug conjugates comprising branched linkers and methods related thereto
KR20180079452A (en) 2015-11-25 2018-07-10 주식회사 레고켐 바이오사이언스 Conjugates comprising self-sacrificial groups and methods for their preparation
AU2018246806B2 (en) 2017-03-29 2022-05-12 Legochem Biosciences, Inc. Pyrrolobenzodiazepine dimer precursor and ligand-linker conjugate compound thereof
EP3755707A1 (en) 2018-02-20 2020-12-30 Seagen Inc. Hydrophobic auristatin f compounds and conjugates thereof
JP7459063B2 (en) 2018-05-09 2024-04-01 レゴケム バイオサイエンシズ， インク． 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
WO2022029420A1 (en) 2020-08-03 2022-02-10 Bicycletx Limited Peptide-based linkers
CN116348479A (en) 2020-09-30 2023-06-27 豪夫迈·罗氏有限公司 Bacterial pilus protein complex FimGt-DsF stable protein complex for the production of filamentous phage
KR20240016287A (en) * 2021-06-01 2024-02-06 아지노모토 가부시키가이샤 Conjugates of antibodies and functional substances or salts thereof, and compounds or salts thereof used in their production

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US4975278A (en) * 1988-02-26 1990-12-04 Bristol-Myers Company Antibody-enzyme conjugates in combination with prodrugs for the delivery of cytotoxic agents to tumor cells
US5563250A (en) * 1987-12-02 1996-10-08 Neorx Corporation Cleavable conjugates for the delivery and release of agents in native form
US5017693A (en) * 1987-12-02 1991-05-21 Neorx Corporation Methods for introducing a sulfhydryl amino or hydroxyl groups to a compound
IL106992A (en) * 1988-02-11 1994-06-24 Bristol Myers Squibb Co Acylhydrazone derivatives of anthracycline and methods for their preparation
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
IT1240643B (en) * 1990-05-11 1993-12-17 Mediolanum Farmaceutici Spa BIOLOGICALLY ACTIVE PEPTIDES CONTAINING IN 2-ALCHYL TRIPTOFANE CHAIN
US5137877B1 (en) * 1990-05-14 1996-01-30 Bristol Myers Squibb Co Bifunctional linking compounds conjugates and methods for their production
CA2107553C (en) * 1991-04-05 2001-07-31 Nancy Lin Monoclonal antibodies to stem cell factor receptors
US5622929A (en) * 1992-01-23 1997-04-22 Bristol-Myers Squibb Company Thioether conjugates
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
US5443953A (en) * 1993-12-08 1995-08-22 Immunomedics, Inc. Preparation and use of immunoconjugates

Non-Patent Citations (5)

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

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