HRP20221120T1 - Materijali i postupci koji se odnose na linkere za uporabu u konjugatima proteina i lijeka - Google Patents
Materijali i postupci koji se odnose na linkere za uporabu u konjugatima proteina i lijeka Download PDFInfo
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- HRP20221120T1 HRP20221120T1 HRP20221120TT HRP20221120T HRP20221120T1 HR P20221120 T1 HRP20221120 T1 HR P20221120T1 HR P20221120T T HRP20221120T T HR P20221120TT HR P20221120 T HRP20221120 T HR P20221120T HR P20221120 T1 HRP20221120 T1 HR P20221120T1
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- Prior art keywords
- protein
- group
- linker
- drug
- conjugate according
- Prior art date
Links
- 239000001990 protein-drug conjugate Substances 0.000 title claims 11
- 238000000034 method Methods 0.000 title claims 3
- 239000000463 material Substances 0.000 title claims 2
- 125000005647 linker group Chemical group 0.000 claims 13
- 239000003814 drug Substances 0.000 claims 6
- 229940079593 drug Drugs 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 108090000765 processed proteins & peptides Proteins 0.000 claims 4
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 4
- 101710112752 Cytotoxin Proteins 0.000 claims 3
- 231100000599 cytotoxic agent Toxicity 0.000 claims 3
- 239000002619 cytotoxin Substances 0.000 claims 3
- 102000034238 globular proteins Human genes 0.000 claims 3
- 108091005896 globular proteins Proteins 0.000 claims 3
- 229920001223 polyethylene glycol Polymers 0.000 claims 3
- 229920001184 polypeptide Polymers 0.000 claims 3
- 102000004196 processed proteins & peptides Human genes 0.000 claims 3
- 108090000623 proteins and genes Proteins 0.000 claims 3
- 102000004169 proteins and genes Human genes 0.000 claims 3
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 3
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N ethylene glycol Natural products OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 2
- 125000003827 glycol group Chemical group 0.000 claims 2
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- 150000001350 alkyl halides Chemical class 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 229940041181 antineoplastic drug Drugs 0.000 claims 1
- 150000001540 azides Chemical class 0.000 claims 1
- 125000002843 carboxylic acid group Chemical group 0.000 claims 1
- 239000000562 conjugate Substances 0.000 claims 1
- 230000021615 conjugation Effects 0.000 claims 1
- 231100000433 cytotoxic Toxicity 0.000 claims 1
- 230000001472 cytotoxic effect Effects 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical group [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000002243 precursor Substances 0.000 claims 1
- -1 succinimidyl Chemical group 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
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- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/42—Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
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- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/06—Tripeptides
- A61K38/063—Glutathione
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- 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
- A61K47/54—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 compound
- A61K47/545—Heterocyclic compounds
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- 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
- A61K47/643—Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]
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- A—HUMAN NECESSITIES
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- 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
- A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
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- 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
- A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
- A61K47/6813—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin the drug being a peptidic cytokine, e.g. an interleukin or interferon
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- 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
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- 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
- A61K47/6855—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 the tumour determinant being from breast cancer cell
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
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- Proteomics, Peptides & Aminoacids (AREA)
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- Oncology (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (13)
1. Konjugat proteina i lijeka formiran reakcijom globularnog proteina, linkera i lijeka, naznačen time, što je globularni protein antitijelo ili njegov fragment koji sadrži najmanje jednu reaktivnu tiol grupu i gdje linker sadrži heterociklični aromatični prsten koji sadrži dušik, koji uključuje vinilni supstituent predstavljen sljedećom formulom,
[image]
u kojoj je:
R1 odabrano od;
▪ (CH2)n - C(O)- R, ili
▪ (CH2)m - S - (CH2)n - C(O) - R, ili
▪ (CH2)n - CH(CO2R)2, ili,
▪ (CH2)m - S - (CH2)2CH(CO2R)2, ili,
gdje,
- R2 je odabrano iz iste grupe molekula kao R1, vodika, ili alkil grupe,
- n je bilo koji cijeli broj od 0 do 10,
- m je bilo koji cijeli broj između 0 i 10,
- R je hidroksid (OH), amin ili grupa poli-(alkilen glikola),
ili gdje R1 predstavlja -CH2-CH(C(O)-NH-PEG)2 i R2 je metil grupa;
pri čemu je globularni protein konjugiran sa linkerom putem konjugacije tiol grupe sa vinilnim supstituentom; i
pri čemu je lijek konjugiran sa linkerom preko R1 grupe, ili kada je R2 izabrano iz iste grupe molekula kao R1, lijek je konjugiran sa linkerom preko R2 grupe, ili preko R1 grupe i R2 grupe.
2. Konjugat proteina i lijeka prema patentnom zahtjevu 1, naznačen time, što je antitijelo monoklonsko antitijelo.
3. Konjugat proteina i lijeka prema bilo kojem prethodnom patentnom zahtjevu, naznačen time, što je lijek citotoksin ili terapeutski peptid ili polipeptid.
4. Konjugat proteina i lijeka prema patentnom zahtjevu 3, naznačen time, što je citotoksin biološki aktivan citotoksični materijal.
5. Konjugat proteina i lijeka prema patentnom zahtjevu 3 ili patentnom zahtjevu 4, naznačen time, što je citotoksin lijek protiv raka.
6. Konjugat proteina i lijeka prema bilo kojem prethodnom patentnom zahtjevu, naznačen time, što linker sadrži grupu poli-(alkilen glikola), gdje je poželjno grupa poli-(alkilen glikola) polietilen glikol (PEG).
7. Konjugat proteina i lijeka prema patentnom zahtjevu 6, naznačen time, što je u strukturi poli-(alkilen glikola) osigurana jedna ili više reaktivnih funkcionalnih grupa, uključujući hidroksi grupu, grupu amina, grupu karboksilne kiseline, alkil halogenid, azid, sukcinimidil ili tiol grupe.
8. Konjugat proteina i lijeka prema bilo kojem prethodnom patentnom zahtjevu koji dalje sadrži produžni linker, gdje se poželjno navedeni produžni linker može cijepati enzimom.
9. Postupak za proizvodnju konjugata proteina i lijeka prema bilo kojem prethodnom patentnom zahtjevu, koji obuhvaća dovođenje u kontakt proteina sa linkerom koji je vezan za lijek.
10. Postupak za proizvodnju konjugata proteina i lijeka prema bilo kojem od patentnih zahtjeva 1 do 8, koji obuhvaća dovođenje u kontakt proteina sa linkerom, i zatim, dovođenje u kontakt linkera sa lijekom.
11. Postupak prema patentnom zahtjevu 9 ili 10, koji uključuje početni korak reakcije prekursorskog linkera, koji sadrži heterociklični aromatični prsten koji sadrži dušik, koji ima vinilni supstituent, sa molekulom poli-(alkilen glikola), kako bi se proizveo linker.
12. Postupak prema bilo kojem od patentnih zahtjeva 9 do 11, koji dalje obuhvaća početni korak modificiranja proteina kako bi se proizveo varijantni polipeptid koji ima tiol grupu na jednoj ili više željenih pozicija u polipeptidu.
13. Konjugat lijeka i proteina prema bilo kojem od patentnih zahtjeva 1 do 8 za uporabu u terapiji.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB1419108.4A GB201419108D0 (en) | 2014-10-27 | 2014-10-27 | Materials and methods relating to linkers for use in antibody drug conjugates |
GB201503012A GB201503012D0 (en) | 2014-10-27 | 2015-02-23 | Materials and methods relating to linkers for use in antibody or albumin drug conjugates |
PCT/GB2015/053227 WO2016067021A1 (en) | 2014-10-27 | 2015-10-27 | Materials and methods relating to linkers for use in protein drug conjugates |
EP15794625.2A EP3223853B1 (en) | 2014-10-27 | 2015-10-27 | Materials and methods relating to linkers for use in protein drug conjugates |
Publications (1)
Publication Number | Publication Date |
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HRP20221120T1 true HRP20221120T1 (hr) | 2022-11-25 |
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HRP20221120TT HRP20221120T1 (hr) | 2014-10-27 | 2015-10-27 | Materijali i postupci koji se odnose na linkere za uporabu u konjugatima proteina i lijeka |
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EP (1) | EP3223853B1 (hr) |
JP (2) | JP2018502045A (hr) |
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SI (1) | SI3223853T1 (hr) |
WO (1) | WO2016067021A1 (hr) |
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WO2020123275A1 (en) * | 2018-12-10 | 2020-06-18 | Genentech, Inc. | Photocrosslinking peptides for site specific conjugation to fc-containing proteins |
CN111650267B (zh) * | 2020-06-11 | 2023-02-28 | 南京师范大学 | 一种系列共轭芳香分子掺杂蛋白质的制备及调节蛋白质电子传输带隙的方法 |
Family Cites Families (27)
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GB8308235D0 (en) | 1983-03-25 | 1983-05-05 | Celltech Ltd | Polypeptides |
US4816567A (en) | 1983-04-08 | 1989-03-28 | Genentech, Inc. | Recombinant immunoglobin preparations |
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 |
GB8603537D0 (en) * | 1986-02-13 | 1986-03-19 | Parker D | Conjugate compound |
GB8607679D0 (en) | 1986-03-27 | 1986-04-30 | Winter G P | Recombinant dna product |
US5079361A (en) | 1987-01-15 | 1992-01-07 | Celltech Limited | Thiol-reactive cross-linking reagents |
JPH0778082B2 (ja) | 1989-12-25 | 1995-08-23 | 日本ゼオン株式会社 | 大粒径ラテックスの製造方法 |
WO1992016221A1 (en) | 1991-03-15 | 1992-10-01 | Synergen, Inc. | Pegylation of polypeptides |
DK1136556T3 (da) | 1991-11-25 | 2005-10-03 | Enzon Inc | Fremgangsmåde til fremstilling af multivalente antigen-bindende proteiner |
US5837242A (en) | 1992-12-04 | 1998-11-17 | Medical Research Council | Multivalent and multispecific binding proteins, their manufacture and use |
US5446090A (en) | 1993-11-12 | 1995-08-29 | Shearwater Polymers, Inc. | Isolatable, water soluble, and hydrolytically stable active sulfones of poly(ethylene glycol) and related polymers for modification of surfaces and molecules |
US6309646B1 (en) | 1996-05-09 | 2001-10-30 | The Henry M. Jackson Foundation For The Advancement Of Military Medicine | Protein-polysaccharide conjugate vaccines and other immunological reagents prepared using homobifunctional and heterobifunctional vinylsulfones, and processes for preparing the conjugates |
US6602498B2 (en) | 2000-02-22 | 2003-08-05 | Shearwater Corporation | N-maleimidyl polymer derivatives |
WO2003061577A2 (en) | 2002-01-18 | 2003-07-31 | Biogen Idec Ma Inc. | Polyalkylene glycol with moiety for conjugating biologically active compound |
WO2004010957A2 (en) | 2002-07-31 | 2004-02-05 | Seattle Genetics, Inc. | Drug conjugates and their use for treating cancer, an autoimmune disease or an infectious disease |
JP4764630B2 (ja) | 2002-09-09 | 2011-09-07 | ネクター セラピューティックス | 水溶性ポリマーアルカナール |
BR122018071808B8 (pt) * | 2003-11-06 | 2020-06-30 | Seattle Genetics Inc | conjugado |
CA2580141C (en) | 2004-09-23 | 2013-12-10 | Genentech, Inc. | Cysteine engineered antibodies and conjugates |
RU2404193C2 (ru) * | 2005-03-25 | 2010-11-20 | Дженентек, Инк. | Способ лечения опухоли у субъекта |
ES2381788T3 (es) * | 2007-07-16 | 2012-05-31 | Genentech, Inc. | Anticuerpos anti-CD79b e inmunoconjugados y métodos de uso |
PL2842575T3 (pl) | 2008-03-18 | 2018-02-28 | Seattle Genetics, Inc. | Koniugaty aurystatyny lek łącznik |
CN102159248B (zh) | 2008-07-15 | 2013-09-11 | 健泰科生物技术公司 | 蒽环类衍生物缀合物、它们的制备方法以及它们作为抗肿瘤化合物的用途 |
GB0823309D0 (en) * | 2008-12-19 | 2009-01-28 | Univ Bath | Functionalising reagents and their uses |
FR2968663A1 (fr) | 2010-12-09 | 2012-06-15 | Univ Strasbourg | Peptides et medicament antiviral |
MY183977A (en) | 2011-02-15 | 2021-03-17 | Immunogen Inc | Cytotoxic benzodiazepine derivatives |
CN102206267A (zh) | 2011-04-18 | 2011-10-05 | 中国药科大学 | 一种肿瘤坏死因子受体1前配体装配域缀合物的结构及用途 |
IN2015DN02349A (hr) | 2012-10-24 | 2015-08-28 | Polytherics Ltd |
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DK3223853T3 (da) | 2022-08-22 |
EP3223853A1 (en) | 2017-10-04 |
US20180092981A9 (en) | 2018-04-05 |
GB201419108D0 (en) | 2014-12-10 |
CN107073133A (zh) | 2017-08-18 |
EP3223853B1 (en) | 2022-06-22 |
SI3223853T1 (sl) | 2022-10-28 |
LT3223853T (lt) | 2022-10-10 |
US11285220B2 (en) | 2022-03-29 |
RU2737553C2 (ru) | 2020-12-01 |
AU2015340370A9 (en) | 2019-08-01 |
RS63552B1 (sr) | 2022-09-30 |
JP7057391B2 (ja) | 2022-04-19 |
WO2016067021A1 (en) | 2016-05-06 |
PL3223853T3 (pl) | 2022-10-10 |
PT3223853T (pt) | 2022-08-01 |
NZ728857A (en) | 2023-08-25 |
HUE059641T2 (hu) | 2022-12-28 |
CN116115771A (zh) | 2023-05-16 |
JP2020147581A (ja) | 2020-09-17 |
KR20170076651A (ko) | 2017-07-04 |
JP2018502045A (ja) | 2018-01-25 |
ES2923853T3 (es) | 2022-10-03 |
IL250664B (en) | 2022-08-01 |
WO2016067021A9 (en) | 2018-03-15 |
KR102530542B1 (ko) | 2023-05-08 |
US20170232108A1 (en) | 2017-08-17 |
AU2015340370B2 (en) | 2020-07-02 |
GB201503012D0 (en) | 2015-04-08 |
RU2017103462A3 (hr) | 2019-04-04 |
IL250664A0 (en) | 2017-06-29 |
AU2015340370A1 (en) | 2017-03-09 |
RU2017103462A (ru) | 2018-11-29 |
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