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IN2015DN02913A - - Google Patents

Info

Publication number
IN2015DN02913A
IN2015DN02913A IN2913DEN2015A IN2015DN02913A IN 2015DN02913 A IN2015DN02913 A IN 2015DN02913A IN 2913DEN2015 A IN2913DEN2015 A IN 2913DEN2015A IN 2015DN02913 A IN2015DN02913 A IN 2015DN02913A
Authority
IN
India
Prior art keywords
protein
sulfur atoms
cysteines
payload
dihaloacetone
Prior art date
Application number
Inventor
Qi-Ying Hu
Hidetomo Imase
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of IN2015DN02913A publication Critical patent/IN2015DN02913A/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61FFILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS
    • A61F5/00Orthopaedic methods or devices for non-surgical treatment of bones or joints; Nursing devices; Anti-rape devices
    • A61F5/0003Apparatus for the treatment of obesity; Anti-eating devices
    • A61F5/0006Diet or mouth appliances
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61CDENTISTRY; APPARATUS OR METHODS FOR ORAL OR DENTAL HYGIENE
    • A61C5/00Filling or capping teeth
    • A61C5/90Oral protectors for use during treatment, e.g. lip or mouth protectors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61FFILTERS IMPLANTABLE INTO BLOOD VESSELS; PROSTHESES; DEVICES PROVIDING PATENCY TO, OR PREVENTING COLLAPSING OF, TUBULAR STRUCTURES OF THE BODY, e.g. STENTS; ORTHOPAEDIC, NURSING OR CONTRACEPTIVE DEVICES; FOMENTATION; TREATMENT OR PROTECTION OF EYES OR EARS; BANDAGES, DRESSINGS OR ABSORBENT PADS; FIRST-AID KITS
    • A61F5/00Orthopaedic methods or devices for non-surgical treatment of bones or joints; Nursing devices; Anti-rape devices
    • A61F5/56Devices for preventing snoring
    • A61F5/566Intra-oral devices
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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 compound
    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/62Medicinal 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
    • A61K47/64Drug-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
    • A61K47/6415Toxins or lectins, e.g. clostridial toxins or Pseudomonas exotoxins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/62Medicinal 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
    • A61K47/64Drug-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
    • A61K47/646Drug-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 the entire peptide or protein drug conjugate elicits an immune response, e.g. conjugate vaccines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/68033Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a maytansine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6845Medicinal 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 cytokine, e.g. growth factors, VEGF, TNF, a lymphokine or an interferon
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6849Medicinal 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 receptor, a cell surface antigen or a cell surface determinant

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Nursing (AREA)
  • Oral & Maxillofacial Surgery (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Obesity (AREA)
  • Otolaryngology (AREA)
  • Dentistry (AREA)
  • Pulmonology (AREA)
  • Toxicology (AREA)
  • Cell Biology (AREA)
  • Virology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Dental Tools And Instruments Or Auxiliary Dental Instruments (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

The invention provides methods to prepare protein conjugates from proteins having at least two cysteines. In one embodiment , a protein with a disulfide linkage is reduced to provide two free cysteines for reaction with a 1 ,3- dihaloacetone or similar reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form a Schiff base to an aminated payload molecule, thus conjugating the protein to a payload. In another embodiment, two cysteine residues are tied together by reaction with a 1, 3 -dihaloacetone or similar reactant. The linkage between the sulfur atoms in each case holds the protein or peptide in a constrained conformation, while also providing a convenient place for attaching a payload with good specificity and efficiency.
IN2913DEN2015 2012-11-30 2013-11-26 IN2015DN02913A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261731852P 2012-11-30 2012-11-30
PCT/IB2013/060427 WO2014083505A1 (en) 2012-11-30 2013-11-26 Methods for making conjugates from disulfide-containing proteins

Publications (1)

Publication Number Publication Date
IN2015DN02913A true IN2015DN02913A (en) 2015-09-18

Family

ID=49726841

Family Applications (1)

Application Number Title Priority Date Filing Date
IN2913DEN2015 IN2015DN02913A (en) 2012-11-30 2013-11-26

Country Status (13)

Country Link
US (3) US10022256B2 (en)
EP (1) EP2925368B1 (en)
JP (1) JP6408480B2 (en)
KR (1) KR20150090081A (en)
CN (1) CN104853781B (en)
AU (1) AU2013350802B2 (en)
BR (1) BR112015011317A2 (en)
CA (1) CA2888445A1 (en)
EA (1) EA201591049A1 (en)
ES (1) ES2732574T3 (en)
IN (1) IN2015DN02913A (en)
MX (1) MX2015006868A (en)
WO (1) WO2014083505A1 (en)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2015006868A (en) 2012-11-30 2015-10-05 Novartis Ag Methods for making conjugates from disulfide-containing proteins.
TW201518323A (en) * 2013-07-25 2015-05-16 Novartis Ag Bioconjugates of synthetic APELIN polypeptides
CA2918074A1 (en) * 2013-07-25 2015-01-29 Novartis Ag Cyclic polypeptides for the treatment of heart failure
EP3024847A1 (en) 2013-07-25 2016-06-01 Novartis AG Disulfide cyclic polypeptides for the treatment of heart failure
US9908919B2 (en) 2013-07-25 2018-03-06 Novartis Ag Cyclic apelin derivatives for the treatment of heart failure
CN105764530B (en) * 2013-11-26 2019-09-13 诺华股份有限公司 The method that polypeptide for modifying ketone carries out oxime conjugation
US20150182373A1 (en) * 2014-01-02 2015-07-02 DMD Todd D. Morgan Oral Exercise Appliance
US10406198B2 (en) 2014-05-23 2019-09-10 Novartis Ag Methods for making conjugates from disulfide-containing proteins
US10588980B2 (en) * 2014-06-23 2020-03-17 Novartis Ag Fatty acids and their use in conjugation to biomolecules
WO2016203432A1 (en) 2015-06-17 2016-12-22 Novartis Ag Antibody drug conjugates
US11155577B2 (en) 2015-06-22 2021-10-26 University Of Utah Research Foundation Thiol-ene based peptide stapling and uses thereof
MA44334A (en) * 2015-10-29 2018-09-05 Novartis Ag ANTIBODY CONJUGATES INCLUDING A TOLL-TYPE RECEPTOR AGONIST
AU2017204139B2 (en) * 2016-06-17 2018-08-09 Vor Biopharma, Inc. Compositions and methods for the depletion of cells
US11034720B2 (en) 2016-07-17 2021-06-15 University Of Utah Research Foundation Thiol-yne based peptide stapling and uses thereof
AR113224A1 (en) 2017-04-28 2020-02-19 Novartis Ag ANTIBODY CONJUGATES INCLUDING A STING AGONIST
WO2020089815A1 (en) 2018-10-31 2020-05-07 Novartis Ag Antibody conjugates comprising sting agonist
EA202191961A1 (en) * 2019-01-16 2021-12-13 Ридженерон Фармасьютикалз, Инк. METHOD AND SYSTEM FOR IDENTIFICATION AND QUANTITATION OF ANTIBODY FRAGMENTATION
WO2020236841A2 (en) 2019-05-20 2020-11-26 Novartis Ag Antibody drug conjugates having linkers comprising hydrophilic groups
WO2020236817A2 (en) 2019-05-20 2020-11-26 Novartis Ag Mcl-1 inhibitor antibody-drug conjugates and methods of use
CA3197961A1 (en) * 2020-11-09 2022-05-12 Kagoshima University Peptide crosslinking agent and crosslinked peptide which is crosslinked using said crosslinking agent
WO2023201181A2 (en) * 2022-04-15 2023-10-19 Jeffrey Goldberg Hunger satiating dental appliance
WO2024189481A1 (en) 2023-03-10 2024-09-19 Novartis Ag Panras inhibitor antibody-drug conjugates and methods of use thereof

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US6239110B1 (en) 1990-02-22 2001-05-29 W.R. Grace & Co. -Conn. Synthetic analogs of thrombospondin and therapeutic use thereof
WO1999013063A1 (en) 1997-09-09 1999-03-18 Nycomed Imaging As Factor vii fragments and analogs thereof and their use in the treatment of blood clottng disorders
WO1999013062A1 (en) 1997-09-09 1999-03-18 Nycomed Imaging As Factors vii fragments and analogs thereof and their use in the treatment of blood clotting disorders
GB0316294D0 (en) 2003-07-11 2003-08-13 Polytherics Ltd Conjugated biological molecules and their preparation
US8673848B2 (en) 2012-01-27 2014-03-18 Novartis Ag Synthetic apelin mimetics for the treatment of heart failure
RS51998B (en) 2005-11-08 2012-04-30 Ambrx Inc. Accelerants for the modification of non-natural amino acids and non-natural amino acid polypeptides
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ES2383191T3 (en) * 2008-02-05 2012-06-19 Medical Research Council Methods and compositions
WO2010025510A1 (en) 2008-09-03 2010-03-11 Xenome Ltd Libraries of peptide conjugates and methods for making them
AU2010283632B2 (en) 2009-08-10 2016-08-25 Ucl Business Plc Reversible covalent linkage of functional molecules
JP2015533832A (en) 2012-10-09 2015-11-26 アイジェニカ バイオセラピューティクス インコーポレイテッド Anti-C16orf54 antibody and method of use thereof
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MX2015006868A (en) 2012-11-30 2015-10-05 Novartis Ag Methods for making conjugates from disulfide-containing proteins.
CN105764530B (en) 2013-11-26 2019-09-13 诺华股份有限公司 The method that polypeptide for modifying ketone carries out oxime conjugation

Also Published As

Publication number Publication date
KR20150090081A (en) 2015-08-05
WO2014083505A1 (en) 2014-06-05
ES2732574T3 (en) 2019-11-25
US20190038444A1 (en) 2019-02-07
JP2015537045A (en) 2015-12-24
CA2888445A1 (en) 2014-06-05
MX2015006868A (en) 2015-10-05
CN104853781A (en) 2015-08-19
US20150290009A1 (en) 2015-10-15
JP6408480B2 (en) 2018-10-17
US11311400B2 (en) 2022-04-26
CN104853781B (en) 2017-10-24
EA201591049A1 (en) 2015-09-30
AU2013350802B2 (en) 2016-07-14
US10667935B2 (en) 2020-06-02
EP2925368A1 (en) 2015-10-07
EP2925368B1 (en) 2019-03-27
BR112015011317A2 (en) 2017-07-11
AU2013350802A1 (en) 2015-04-09
US10022256B2 (en) 2018-07-17
US20200253768A1 (en) 2020-08-13

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