HRP20210126T1 - Pirolobenzodiazepini i njihovi konjugati - Google Patents
Pirolobenzodiazepini i njihovi konjugati Download PDFInfo
- Publication number
- HRP20210126T1 HRP20210126T1 HRP20210126TT HRP20210126T HRP20210126T1 HR P20210126 T1 HRP20210126 T1 HR P20210126T1 HR P20210126T T HRP20210126T T HR P20210126TT HR P20210126 T HRP20210126 T HR P20210126T HR P20210126 T1 HRP20210126 T1 HR P20210126T1
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- Prior art keywords
- antibody
- conjugate
- conjugate according
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- drug
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- YUOCYTRGANSSRY-UHFFFAOYSA-N pyrrolo[2,3-i][1,2]benzodiazepine Chemical class C1=CN=NC2=C3C=CN=C3C=CC2=C1 YUOCYTRGANSSRY-UHFFFAOYSA-N 0.000 title 1
- 239000000562 conjugate Substances 0.000 claims 12
- 238000002360 preparation method Methods 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 4
- 229940079593 drug Drugs 0.000 claims 4
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 3
- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 239000000427 antigen Substances 0.000 claims 3
- 102000036639 antigens Human genes 0.000 claims 3
- 108091007433 antigens Proteins 0.000 claims 3
- 239000011230 binding agent Substances 0.000 claims 3
- 210000004027 cell Anatomy 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 102100040842 3-galactosyl-N-acetylglucosaminide 4-alpha-L-fucosyltransferase FUT3 Human genes 0.000 claims 2
- 102100040006 Annexin A1 Human genes 0.000 claims 2
- 102100022005 B-lymphocyte antigen CD20 Human genes 0.000 claims 2
- 102100037241 Endoglin Human genes 0.000 claims 2
- 108700041152 Endoplasmic Reticulum Chaperone BiP Proteins 0.000 claims 2
- 102100021451 Endoplasmic reticulum chaperone BiP Human genes 0.000 claims 2
- 101150112743 HSPA5 gene Proteins 0.000 claims 2
- 108010007712 Hepatitis A Virus Cellular Receptor 1 Proteins 0.000 claims 2
- 102100034459 Hepatitis A virus cellular receptor 1 Human genes 0.000 claims 2
- 101000893701 Homo sapiens 3-galactosyl-N-acetylglucosaminide 4-alpha-L-fucosyltransferase FUT3 Proteins 0.000 claims 2
- 101000897405 Homo sapiens B-lymphocyte antigen CD20 Proteins 0.000 claims 2
- 101001106413 Homo sapiens Macrophage-stimulating protein receptor Proteins 0.000 claims 2
- 101001136592 Homo sapiens Prostate stem cell antigen Proteins 0.000 claims 2
- 101000633784 Homo sapiens SLAM family member 7 Proteins 0.000 claims 2
- 101000874179 Homo sapiens Syndecan-1 Proteins 0.000 claims 2
- 101000851376 Homo sapiens Tumor necrosis factor receptor superfamily member 8 Proteins 0.000 claims 2
- 101000622304 Homo sapiens Vascular cell adhesion protein 1 Proteins 0.000 claims 2
- 102100021435 Macrophage-stimulating protein receptor Human genes 0.000 claims 2
- 102100036735 Prostate stem cell antigen Human genes 0.000 claims 2
- 102100029198 SLAM family member 7 Human genes 0.000 claims 2
- 102100036427 Spondin-2 Human genes 0.000 claims 2
- 102100035721 Syndecan-1 Human genes 0.000 claims 2
- 102100033726 Tumor necrosis factor receptor superfamily member 17 Human genes 0.000 claims 2
- 102100036857 Tumor necrosis factor receptor superfamily member 8 Human genes 0.000 claims 2
- 102100038929 V-set domain-containing T-cell activation inhibitor 1 Human genes 0.000 claims 2
- 102100023543 Vascular cell adhesion protein 1 Human genes 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 108010074865 mindin Proteins 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- JPSHPWJJSVEEAX-OWPBQMJCSA-N (2s)-2-amino-4-fluoranylpentanedioic acid Chemical compound OC(=O)[C@@H](N)CC([18F])C(O)=O JPSHPWJJSVEEAX-OWPBQMJCSA-N 0.000 claims 1
- BGFTWECWAICPDG-UHFFFAOYSA-N 2-[bis(4-chlorophenyl)methyl]-4-n-[3-[bis(4-chlorophenyl)methyl]-4-(dimethylamino)phenyl]-1-n,1-n-dimethylbenzene-1,4-diamine Chemical compound C1=C(C(C=2C=CC(Cl)=CC=2)C=2C=CC(Cl)=CC=2)C(N(C)C)=CC=C1NC(C=1)=CC=C(N(C)C)C=1C(C=1C=CC(Cl)=CC=1)C1=CC=C(Cl)C=C1 BGFTWECWAICPDG-UHFFFAOYSA-N 0.000 claims 1
- 108090000663 Annexin A1 Proteins 0.000 claims 1
- 108010008014 B-Cell Maturation Antigen Proteins 0.000 claims 1
- 102100025218 B-cell differentiation antigen CD72 Human genes 0.000 claims 1
- 102100038080 B-cell receptor CD22 Human genes 0.000 claims 1
- 102100024222 B-lymphocyte antigen CD19 Human genes 0.000 claims 1
- 102100027052 Bone morphogenetic protein receptor type-1B Human genes 0.000 claims 1
- 108010085074 Brevican Proteins 0.000 claims 1
- 102100032312 Brevican core protein Human genes 0.000 claims 1
- 102100031658 C-X-C chemokine receptor type 5 Human genes 0.000 claims 1
- 102100032556 C-type lectin domain family 14 member A Human genes 0.000 claims 1
- 102100024217 CAMPATH-1 antigen Human genes 0.000 claims 1
- 102100024220 CD180 antigen Human genes 0.000 claims 1
- 108010065524 CD52 Antigen Proteins 0.000 claims 1
- 102100025221 CD70 antigen Human genes 0.000 claims 1
- 102100025475 Carcinoembryonic antigen-related cell adhesion molecule 5 Human genes 0.000 claims 1
- 102000000844 Cell Surface Receptors Human genes 0.000 claims 1
- 108010001857 Cell Surface Receptors Proteins 0.000 claims 1
- 102000002029 Claudin Human genes 0.000 claims 1
- 108050009302 Claudin Proteins 0.000 claims 1
- 102100032768 Complement receptor type 2 Human genes 0.000 claims 1
- 229940126062 Compound A Drugs 0.000 claims 1
- 102100030074 Dickkopf-related protein 1 Human genes 0.000 claims 1
- 101710099518 Dickkopf-related protein 1 Proteins 0.000 claims 1
- 101150076616 EPHA2 gene Proteins 0.000 claims 1
- 108010036395 Endoglin Proteins 0.000 claims 1
- 102100030340 Ephrin type-A receptor 2 Human genes 0.000 claims 1
- 102100031517 Fc receptor-like protein 1 Human genes 0.000 claims 1
- 101710120224 Fc receptor-like protein 1 Proteins 0.000 claims 1
- 102100031511 Fc receptor-like protein 2 Human genes 0.000 claims 1
- 102100031507 Fc receptor-like protein 5 Human genes 0.000 claims 1
- 102100035139 Folate receptor alpha Human genes 0.000 claims 1
- 102100022662 Guanylyl cyclase C Human genes 0.000 claims 1
- 102100030595 HLA class II histocompatibility antigen gamma chain Human genes 0.000 claims 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 1
- 101000959738 Homo sapiens Annexin A1 Proteins 0.000 claims 1
- 101000934359 Homo sapiens B-cell differentiation antigen CD72 Proteins 0.000 claims 1
- 101000884305 Homo sapiens B-cell receptor CD22 Proteins 0.000 claims 1
- 101000980825 Homo sapiens B-lymphocyte antigen CD19 Proteins 0.000 claims 1
- 101000984546 Homo sapiens Bone morphogenetic protein receptor type-1B Proteins 0.000 claims 1
- 101000922405 Homo sapiens C-X-C chemokine receptor type 5 Proteins 0.000 claims 1
- 101000942280 Homo sapiens C-type lectin domain family 14 member A Proteins 0.000 claims 1
- 101000980829 Homo sapiens CD180 antigen Proteins 0.000 claims 1
- 101000934356 Homo sapiens CD70 antigen Proteins 0.000 claims 1
- 101000914324 Homo sapiens Carcinoembryonic antigen-related cell adhesion molecule 5 Proteins 0.000 claims 1
- 101000941929 Homo sapiens Complement receptor type 2 Proteins 0.000 claims 1
- 101000846911 Homo sapiens Fc receptor-like protein 2 Proteins 0.000 claims 1
- 101000846908 Homo sapiens Fc receptor-like protein 5 Proteins 0.000 claims 1
- 101001023230 Homo sapiens Folate receptor alpha Proteins 0.000 claims 1
- 101000899808 Homo sapiens Guanylyl cyclase C Proteins 0.000 claims 1
- 101001082627 Homo sapiens HLA class II histocompatibility antigen gamma chain Proteins 0.000 claims 1
- 101000606465 Homo sapiens Inactive tyrosine-protein kinase 7 Proteins 0.000 claims 1
- 101001046677 Homo sapiens Integrin alpha-V Proteins 0.000 claims 1
- 101001015064 Homo sapiens Integrin beta-6 Proteins 0.000 claims 1
- 101001055144 Homo sapiens Interleukin-2 receptor subunit alpha Proteins 0.000 claims 1
- 101000777628 Homo sapiens Leukocyte antigen CD37 Proteins 0.000 claims 1
- 101000628547 Homo sapiens Metalloreductase STEAP1 Proteins 0.000 claims 1
- 101000628535 Homo sapiens Metalloreductase STEAP2 Proteins 0.000 claims 1
- 101001133056 Homo sapiens Mucin-1 Proteins 0.000 claims 1
- 101000934338 Homo sapiens Myeloid cell surface antigen CD33 Proteins 0.000 claims 1
- 101001023705 Homo sapiens Nectin-4 Proteins 0.000 claims 1
- 101000581981 Homo sapiens Neural cell adhesion molecule 1 Proteins 0.000 claims 1
- 101000897042 Homo sapiens Nucleotide pyrophosphatase Proteins 0.000 claims 1
- 101000610548 Homo sapiens Proline-rich protein 4 Proteins 0.000 claims 1
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 1
- 101000829127 Homo sapiens Somatostatin receptor type 2 Proteins 0.000 claims 1
- 101000829138 Homo sapiens Somatostatin receptor type 3 Proteins 0.000 claims 1
- 101000829153 Homo sapiens Somatostatin receptor type 5 Proteins 0.000 claims 1
- 101000834948 Homo sapiens Tomoregulin-2 Proteins 0.000 claims 1
- 101000904724 Homo sapiens Transmembrane glycoprotein NMB Proteins 0.000 claims 1
- 101000801255 Homo sapiens Tumor necrosis factor receptor superfamily member 17 Proteins 0.000 claims 1
- 101000955999 Homo sapiens V-set domain-containing T-cell activation inhibitor 1 Proteins 0.000 claims 1
- 102100039813 Inactive tyrosine-protein kinase 7 Human genes 0.000 claims 1
- 102100022337 Integrin alpha-V Human genes 0.000 claims 1
- 102100033011 Integrin beta-6 Human genes 0.000 claims 1
- 102100026878 Interleukin-2 receptor subunit alpha Human genes 0.000 claims 1
- 102100031586 Leukocyte antigen CD37 Human genes 0.000 claims 1
- 102100026712 Metalloreductase STEAP1 Human genes 0.000 claims 1
- 102100026711 Metalloreductase STEAP2 Human genes 0.000 claims 1
- 102100034256 Mucin-1 Human genes 0.000 claims 1
- 101100042271 Mus musculus Sema3b gene Proteins 0.000 claims 1
- 102100025243 Myeloid cell surface antigen CD33 Human genes 0.000 claims 1
- 102100035486 Nectin-4 Human genes 0.000 claims 1
- 102100027347 Neural cell adhesion molecule 1 Human genes 0.000 claims 1
- 102100021969 Nucleotide pyrophosphatase Human genes 0.000 claims 1
- 102100037603 P2X purinoceptor 5 Human genes 0.000 claims 1
- 101710189969 P2X purinoceptor 5 Proteins 0.000 claims 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 1
- 108091006938 SLC39A6 Proteins 0.000 claims 1
- 101100111629 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) KAR2 gene Proteins 0.000 claims 1
- 102100029329 Somatostatin receptor type 1 Human genes 0.000 claims 1
- 102100023802 Somatostatin receptor type 2 Human genes 0.000 claims 1
- 102100023803 Somatostatin receptor type 3 Human genes 0.000 claims 1
- 102100023801 Somatostatin receptor type 4 Human genes 0.000 claims 1
- 102100023806 Somatostatin receptor type 5 Human genes 0.000 claims 1
- 102000007000 Tenascin Human genes 0.000 claims 1
- 102100038126 Tenascin Human genes 0.000 claims 1
- 108010008125 Tenascin Proteins 0.000 claims 1
- 102100026160 Tomoregulin-2 Human genes 0.000 claims 1
- 102100023935 Transmembrane glycoprotein NMB Human genes 0.000 claims 1
- 102100029690 Tumor necrosis factor receptor superfamily member 13C Human genes 0.000 claims 1
- 101710178300 Tumor necrosis factor receptor superfamily member 13C Proteins 0.000 claims 1
- 108010079206 V-Set Domain-Containing T-Cell Activation Inhibitor 1 Proteins 0.000 claims 1
- 102100023144 Zinc transporter ZIP6 Human genes 0.000 claims 1
- 239000000611 antibody drug conjugate Substances 0.000 claims 1
- 229940049595 antibody-drug conjugate Drugs 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000012829 chemotherapy agent Substances 0.000 claims 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 1
- 235000018417 cysteine Nutrition 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 108010087914 epidermal growth factor receptor VIII Proteins 0.000 claims 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 1
- 101150028578 grp78 gene Proteins 0.000 claims 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000023958 prostate neoplasm Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 108010064556 somatostatin receptor subtype-4 Proteins 0.000 claims 1
- 108010082379 somatostatin receptor type 1 Proteins 0.000 claims 1
- 210000000130 stem cell Anatomy 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K47/68035—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a pyrrolobenzodiazepine
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Cell Biology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Toxicology (AREA)
- Peptides Or Proteins (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Claims (14)
1. Spoj, naznačen time, da je A:
[image]
i njegove soli i njegovi solvati.
2. Konjugat, naznačen time, da ima formulu KonjA:
[image]
u kojoj CBA predstavlja sredstvo za vezanje stanice.
3. Konjugat prema patentnom zahtjevu 2, naznačen time, da se kod sredstva za vezanje stanice radi o protutijelu ili fragmentu protutijela za antigen koji je povezan s tumorom.
4. Konjugat prema patentnom zahtjevu 3, naznačen time, da protutijelo ili fragment protutijela je jedno protutijelo koje se veže na jedan ili više antigena povezanih s tumorom ili na receptore stanične površine koji su odabrani od (1) do (88):
(1) BMPR1B;
(2) E16;
(3) STEAP1;
(4) 0772P;
(5) MPF;
(6) Napi3b;
(7) Sema 5b;
(8) PSCA hlg;
(9) ETBR;
(10) MSG783;
(11) STEAP2;
(12) TrpM4;
(13) CRIPTO;
(14) CD21;
(15) CD79b;
(16) FcRH2;
(17) HER2;
(18) NCA;
(19) MDP;
(20) IL20R-alfa;
(21) Brevikan;
(22) EphB2R;
(23) ASLG659;
(24) PSCA;
(25) GEDA;
(26) BAFF-R;
(27) CD22;
(28) CD79a;
(29) CXCR5;
(30) HLA-DOB;
(31) P2X5;
(32) CD72;
(33) LY64;
(34) FcRH1;
(35) IRTA2;
(36) TENB2;
(37) PSMA-FOLH1;
(38) SST;
(38.1) SSTR2;
(38.2) SSTR5;
(38.3) SSTR1;
(38.4) SSTR3;
(38.5) SSTR4;
(39) ITGAV;
(40) ITGB6;
(41) CEACAM5;
(42) MET;
(43) MUC1;
(44) CA9;
(45) EGFRvIII;
(46) CD33;
(47) CD19;
(48) IL2RA;
(49) AXL;
(50) CD30 - TNFRSF8;
(51) BCMA - TNFRSF17;
(52) CT Ags - CTA;
(53) CD174 (Lewis Y) – FUT3;
(54) CLEC14A;
(55) GRP78 – HSPA5;
(56) CD70;
(57) specifični antigeni matične stanice;
(58) ASG-5;
(59) ENPP3;
(60) PRR4;
(61) GCC – GUCY2C;
(62) Liv-1 – SLC39A6;
(63) 5T4;
(64) CD56 – NCMA1;
(65) CanAg;
(66) FOLR1;
(67) GPNMB;
(68) TIM-1 – HAVCR1;
(69) RG-1/Mindin, meta za tumor prostate – Mindin/RG-1;
(70) B7-H4 – VTCN1;
(71) PTK7;
(72) CD37;
(73) CD138 – SDC1;
(74) CD74;
(75) Klaudini - CLs;
(76) EGFR;
(77) Her3;
(78) RON – MST1R;
(79) EPHA2;
(80) CD20 – MS4A1;
(81) Tenascin C - TNC;
(82) FAP;
(83) DKK-1;
(84) CD52;
(85) CS1 – SLAMF7;
(86) Endoglin - ENG;
(87) Aneksin A1 – ANXA1;
(88) V-CAM (CD106) – VCAM1.
5. Konjugat prema bilo kojem od patentnih zahtjeva 2 do 4, naznačen time, da protutijelo ili fragment protutijela je protutijelo modificirano cisteinskim inženjeringom.
6. Konjugat prema bilo kojem od patentnih zahtjeva 2 do 5, naznačen time, da opterećenost lijekom (p) od lijekova (D) prema protutijelu (Ab), iznosi cijeli broj od 1 do oko 8.
7. Konjugat prema patentnom zahtjevu 6, naznačen time, da p je 1, 2, 3 ili 4.
8. Pripravak, naznačen time, da obuhvaća mješavinu spojeva lijeka i konjugata u skladu s bilo kojim od zahtjeva 2 do 7, pri čemu prosječna opterećenost lijekom po protutijelu u mješavini spojeva konjugata protutijelo-lijek, iznosi od oko 1 do oko 8.
9. Konjugat prema bilo kojem od patentnih zahtjeva 2 do 7, ili pripravak prema patentnom zahtjevu 8, naznačen time, da je za uporabu u liječenju.
10. Konjugat prema bilo kojem od patentnih zahtjeva 2 do 7, ili pripravak prema patentnom zahtjevu 8, naznačen time, da je za uporabu u liječenju proliferativne bolesti kod pojedinca.
11. Konjugat ili pripravak za uporabu prema patentnom zahtjevu 10, naznačen time, da bolest jest rak.
12. Farmaceutski pripravak, naznačen time, da sadrži konjugat u skladu s bilo kojim od patentnih zahtjeva 2 do 7, ili pripravak u skladu s patentnim zahtjevom 8, te farmaceutski prihvatljiv razrjeđivač, nosač ili pomoćnu tvar.
13. Farmaceutski pripravak prema patentnom zahtjevu 12, naznačen time, da dodatno sadrži terapijski učinkovitu količinu kemoterapijskog sredstva.
14. Postupak proizvodnje konjugata u skladu s bilo kojim od patentnih zahtjeva 2 do 7, naznačen time, da postupak obuhvaća korak reakcije sredstva za vezanje stanice sa spojem A koji je definiran u patentnom zahtjevu 1.
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US201261712924P | 2012-10-12 | 2012-10-12 | |
EP18187765.5A EP3470086B1 (en) | 2012-10-12 | 2013-10-11 | Pyrrolobenzodiazepines and conjugates thereof |
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HRP20190366TT HRP20190366T1 (hr) | 2012-10-12 | 2019-02-26 | Pirolobenzodiazepini i njihovi konjugati |
HRP20210126TT HRP20210126T1 (hr) | 2012-10-12 | 2021-01-22 | Pirolobenzodiazepini i njihovi konjugati |
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Families Citing this family (73)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB0819095D0 (en) | 2008-10-17 | 2008-11-26 | Spirogen Ltd | Pyrrolobenzodiazepines |
AU2011239522B2 (en) | 2010-04-15 | 2014-10-23 | Medimmune Limited | Targeted pyrrolobenzodiazapine conjugates |
AU2011239525B2 (en) | 2010-04-15 | 2015-04-09 | Medimmune Limited | Pyrrolobenzodiazepines used to treat proliferative diseases |
CA2849039C (en) | 2011-09-20 | 2018-09-18 | Spirogen Sarl | Pyrrolobenzodiazepines as unsymmetrical dimeric pbd compounds for inclusion in targeted conjugates |
US9388187B2 (en) | 2011-10-14 | 2016-07-12 | Medimmune Limited | Pyrrolobenzodiazepines |
BR112014008888A2 (pt) | 2011-10-14 | 2017-04-18 | Seattle Genetics Inc | pirrolobenzodiazepinas |
EA036202B1 (ru) | 2011-10-14 | 2020-10-14 | Сиэтл Дженетикс, Инк. | Пирролбензодиазепины и конъюгаты направленного действия |
EP3388435B1 (en) | 2011-10-14 | 2023-05-03 | Seagen Inc. | Pyrrolobenzodiazepines and targeted conjugates |
BR112015002193A2 (pt) * | 2012-08-02 | 2017-07-04 | Genentech Inc | anticorpos anti-etbr e imunoconjugados |
WO2014057114A1 (en) | 2012-10-12 | 2014-04-17 | Adc Therapeutics Sàrl | Pyrrolobenzodiazepine-anti-psma antibody conjugates |
NZ707534A (en) | 2012-10-12 | 2018-08-31 | Adc Therapeutics Sa | Pyrrolobenzodiazepine-antibody conjugates |
CA3060520C (en) | 2012-10-12 | 2022-05-17 | Medimmune Limited | Pyrrolobenzodiazepines and conjugates thereof |
PL2766048T3 (pl) | 2012-10-12 | 2015-05-29 | Medimmune Ltd | Pirolobenzodiazepiny i ich koniugaty |
MX364328B (es) | 2012-10-12 | 2019-04-23 | Medimmune Ltd | Conjugados del anticuerpo pirrolobenzodiazepina. |
DK2906251T3 (da) | 2012-10-12 | 2017-11-20 | Adc Therapeutics Sa | Pyrrolobenzodiazepin-anti-CD22-antistofkonjugater |
AU2013328673B2 (en) | 2012-10-12 | 2017-07-13 | Medimmune Limited | Synthesis and intermediates of pyrrolobenzodiazepine derivatives for conjugation |
EP2906297B1 (en) | 2012-10-12 | 2017-12-06 | ADC Therapeutics SA | Pyrrolobenzodiazepine-antibody conjugates |
NZ707486A (en) | 2012-10-12 | 2018-09-28 | Adc Therapeutics Sa | Pyrrolobenzodiazepine - anti-psma antibody conjugates |
CN110452242A (zh) | 2012-12-21 | 2019-11-15 | 麦迪穆有限责任公司 | 吡咯并苯并二氮杂卓及其结合物 |
CA2894959C (en) | 2012-12-21 | 2022-01-11 | Spirogen Sarl | Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases |
AU2014244245C1 (en) | 2013-03-13 | 2018-04-19 | Genentech, Inc. | Pyrrolobenzodiazepines and conjugates thereof |
CN105142674B (zh) | 2013-03-13 | 2018-11-13 | 麦迪穆有限责任公司 | 吡咯并苯并二氮杂卓和其结合物 |
JP6744212B2 (ja) * | 2013-06-21 | 2020-08-19 | イナート・ファルマ・ソシエテ・アノニムInnate Pharma Pharma S.A. | ポリペプチドの酵素的結合 |
EP3054986B1 (en) | 2013-10-11 | 2019-03-20 | Medimmune Limited | Pyrrolobenzodiazepine-antibody conjugates |
GB201317981D0 (en) | 2013-10-11 | 2013-11-27 | Spirogen Sarl | Pyrrolobenzodiazepines and conjugates thereof |
GB201317982D0 (en) | 2013-10-11 | 2013-11-27 | Spirogen Sarl | Pyrrolobenzodiazepines and conjugates thereof |
US10010624B2 (en) | 2013-10-11 | 2018-07-03 | Medimmune Limited | Pyrrolobenzodiazepine-antibody conjugates |
WO2015052534A1 (en) | 2013-10-11 | 2015-04-16 | Spirogen Sàrl | Pyrrolobenzodiazepine-antibody conjugates |
TW201617368A (zh) | 2014-09-05 | 2016-05-16 | 史坦森特瑞斯公司 | 新穎抗mfi2抗體及使用方法 |
EP3193940A1 (en) | 2014-09-10 | 2017-07-26 | Medimmune Limited | Pyrrolobenzodiazepines and conjugates thereof |
TWI758784B (zh) | 2014-09-12 | 2022-03-21 | 美商建南德克公司 | 抗her2抗體及免疫結合物 |
GB201416112D0 (en) | 2014-09-12 | 2014-10-29 | Medimmune Ltd | Pyrrolobenzodiazepines and conjugates thereof |
KR20170101895A (ko) | 2014-11-25 | 2017-09-06 | 에이디씨 테라퓨틱스 에스에이 | 피롤로벤조디아제핀-항체 접합체 |
WO2016115201A1 (en) | 2015-01-14 | 2016-07-21 | Bristol-Myers Squibb Company | Heteroarylene-bridged benzodiazepine dimers, conjugates thereof, and methods of making and using |
CN107428780B (zh) | 2015-01-14 | 2020-09-04 | 百时美施贵宝公司 | 苯并二氮杂*二聚体、其缀合物及制备和使用方法 |
GB201506394D0 (en) * | 2015-04-15 | 2015-05-27 | Berkel Patricius H C Van And Howard Philip W | Site-specific antibody-drug conjugates |
GB201506405D0 (en) * | 2015-04-15 | 2015-05-27 | Berkel Patricius H C Van And Howard Philip W | Site-specific antibody-drug conjugates |
GB201506389D0 (en) | 2015-04-15 | 2015-05-27 | Berkel Patricius H C Van And Howard Philip W | Site-specific antibody-drug conjugates |
GB201506411D0 (en) | 2015-04-15 | 2015-05-27 | Bergenbio As | Humanized anti-axl antibodies |
GB201506402D0 (en) | 2015-04-15 | 2015-05-27 | Berkel Patricius H C Van And Howard Philip W | Site-specific antibody-drug conjugates |
KR20180019592A (ko) | 2015-06-23 | 2018-02-26 | 브리스톨-마이어스 스큅 컴퍼니 | 마크로시클릭 벤조디아제핀 이량체, 그의 접합체, 제조법 및 용도 |
MA43345A (fr) | 2015-10-02 | 2018-08-08 | Hoffmann La Roche | Conjugués anticorps-médicaments de pyrrolobenzodiazépine et méthodes d'utilisation |
TWI726942B (zh) | 2015-11-30 | 2021-05-11 | 美商輝瑞股份有限公司 | 位點專一性her2抗體藥物共軛體 |
GB201601431D0 (en) | 2016-01-26 | 2016-03-09 | Medimmune Ltd | Pyrrolobenzodiazepines |
GB201602356D0 (en) | 2016-02-10 | 2016-03-23 | Medimmune Ltd | Pyrrolobenzodiazepine Conjugates |
GB201602359D0 (en) | 2016-02-10 | 2016-03-23 | Medimmune Ltd | Pyrrolobenzodiazepine Conjugates |
AU2017254674A1 (en) | 2016-04-21 | 2018-11-01 | Abbvie Stemcentrx Llc | Novel anti-BMPR1B antibodies and methods of use |
GB201607478D0 (en) * | 2016-04-29 | 2016-06-15 | Medimmune Ltd | Pyrrolobenzodiazepine Conjugates |
TW201808936A (zh) | 2016-05-18 | 2018-03-16 | 美商梅爾莎納醫療公司 | 吡咯并苯并二氮呯類及其共軛物 |
US10526294B2 (en) | 2016-06-24 | 2020-01-07 | Mersana Therapeutics, Inc. | Pyrrolobenzodiazepines and conjugates thereof |
GB201617466D0 (en) | 2016-10-14 | 2016-11-30 | Medimmune Ltd | Pyrrolobenzodiazepine conjugates |
GB201619490D0 (en) * | 2016-11-17 | 2017-01-04 | Medimmune Ltd | Pyrrolobenzodiazepine conjugates |
EP3348560A1 (en) | 2017-01-16 | 2018-07-18 | Spago Nanomedical AB | Chemical compounds for coating of nanostructures |
GB201702031D0 (en) | 2017-02-08 | 2017-03-22 | Medlmmune Ltd | Pyrrolobenzodiazepine-antibody conjugates |
AU2018217926B2 (en) | 2017-02-08 | 2019-10-03 | Adc Therapeutics Sa | Pyrrolobenzodiazepine-antibody conjugates |
EP3612537B1 (en) | 2017-04-18 | 2022-07-13 | Medimmune Limited | Pyrrolobenzodiazepine conjugates |
US20200129637A1 (en) | 2017-04-20 | 2020-04-30 | Adc Therapeutics Sa | Combination therapy with an anti-axl antibody-drug conjugate |
KR102442736B1 (ko) | 2017-06-14 | 2022-09-16 | 에이디씨 테라퓨틱스 에스에이 | 항-cd19 adc의 투여를 위한 투약량 체제 |
JP7220203B2 (ja) | 2017-08-18 | 2023-02-09 | メドイミューン・リミテッド | ピロロベンゾジアゼピン複合体 |
US11628223B2 (en) | 2017-09-29 | 2023-04-18 | Daiichi Sankyo Company, Limited | Antibody-drug conjugates comprising substituted benzo[e]pyrrolo[1,2-α][1,4]diazepines |
ES2920123T3 (es) | 2017-11-14 | 2022-08-01 | Medimmune Ltd | Conjugados de pirrolobenzodiazepina |
EP3717021A1 (en) | 2017-11-27 | 2020-10-07 | Mersana Therapeutics, Inc. | Pyrrolobenzodiazepine antibody conjugates |
CU24558B1 (es) * | 2017-11-28 | 2021-12-08 | Ct Inmunologia Molecular | Anticuerpos monoclonales que reconocen al receptor del factor de crecimiento epidérmico y sus fragmentos derivados |
US20220305127A1 (en) | 2017-12-21 | 2022-09-29 | Mersana Therapeutics, Inc. | Pyrrolobenzodiazepine antibody conjugates |
GB201803342D0 (en) | 2018-03-01 | 2018-04-18 | Medimmune Ltd | Methods |
GB201806022D0 (en) | 2018-04-12 | 2018-05-30 | Medimmune Ltd | Pyrrolobenzodiazepines and conjugates thereof |
GB201902495D0 (en) | 2019-02-25 | 2019-04-10 | Medimmune Ltd | Methods of synthesis and intermediates |
CN114007642A (zh) | 2019-04-30 | 2022-02-01 | 森迪生物科学公司 | 嵌合受体及其使用方法 |
EP4013494A1 (en) | 2019-08-12 | 2022-06-22 | Regeneron Pharmaceuticals, Inc. | Macrophage stimulating 1 receptor (mst1r) variants and uses thereof |
WO2021080608A1 (en) | 2019-10-25 | 2021-04-29 | Medimmune, Llc | Branched moiety for use in conjugates |
US20220267456A1 (en) * | 2021-02-19 | 2022-08-25 | Janssen Biotech, Inc. | Materials and methods for targeting regulatory t cells for enhancing immune surveillance |
KR102285542B1 (ko) | 2021-03-09 | 2021-08-04 | 주식회사 레젠 | 투광등용 리플렉터 및 이를 가진 투광등 |
WO2023173096A1 (en) * | 2022-03-11 | 2023-09-14 | Sigma-Aldrich Co. Llc | Pyrrolobenzodiazepine intermediates and uses thereof |
Family Cites Families (130)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3361742A (en) | 1964-12-07 | 1968-01-02 | Hoffmann La Roche | 5-oxo-1h-pyrrolo-[2, 1-c][1, 4]-benzodiazepin-2-crylamides |
US3523941A (en) | 1967-03-06 | 1970-08-11 | Hoffmann La Roche | Benzodiazepine compounds and process for their preparation |
US3524849A (en) | 1967-10-27 | 1970-08-18 | Hoffmann La Roche | Process for the preparation of pyrrolo-benzodiazepine acrylamides and intermediates useful therein |
DE1965304A1 (de) | 1968-12-30 | 1970-07-23 | Fujisawa Pharmaceutical Co | Benzdiazepinon-Verbindungen und Verfahren zu ihrer Herstellung |
IL33558A (en) | 1968-12-30 | 1973-10-25 | Fujisawa Pharmaceutical Co | Antibiotic pyrrolo-benzodiazepine compound,its derivatives and processes for their production |
JPS4843755B1 (hr) | 1969-06-26 | 1973-12-20 | ||
JPS5382792U (hr) | 1976-12-10 | 1978-07-08 | ||
JPS585916B2 (ja) | 1977-12-27 | 1983-02-02 | 株式会社ミドリ十字 | 新規ベンゾジアゼピン系化合物 |
JPS5615289A (en) | 1979-07-17 | 1981-02-14 | Green Cross Corp:The | Novel benzodiazepinnbased compound 3 |
JPH0353356Y2 (hr) | 1981-02-06 | 1991-11-21 | ||
CA1185602A (en) | 1981-02-27 | 1985-04-16 | Emilio Kyburz | Imidazodiazepines |
CA1184175A (en) | 1981-02-27 | 1985-03-19 | Walter Hunkeler | Imidazodiazepines |
CA1173441A (en) | 1981-02-27 | 1984-08-28 | Hoffmann-La Roche Limited | Imidazodiazepines |
JPS58180487A (ja) | 1982-04-16 | 1983-10-21 | Kyowa Hakko Kogyo Co Ltd | 抗生物質dc−81およびその製造法 |
JPS58180487U (ja) | 1982-05-28 | 1983-12-02 | 松下電工株式会社 | 光線式報知器の組立体 |
US4427588A (en) | 1982-11-08 | 1984-01-24 | Bristol-Myers Company | Process for conversion of oxotomaymycin to tomaymycin |
US4427587A (en) | 1982-11-10 | 1984-01-24 | Bristol-Myers Company | Total synthesis of antitumor antibiotics BBM-2040A and BBM-2040B |
JPS59152329A (ja) | 1983-02-17 | 1984-08-31 | Green Cross Corp:The | 局所障害抑制剤 |
US4816567A (en) | 1983-04-08 | 1989-03-28 | Genentech, Inc. | Recombinant immunoglobin preparations |
FR2586683B1 (fr) | 1985-08-29 | 1988-07-01 | Centre Nat Rech Scient | Nouveaux derives de neothramycine, leur procede de preparation et leur application en tant que medicaments |
US5583024A (en) | 1985-12-02 | 1996-12-10 | The Regents Of The University Of California | Recombinant expression of Coleoptera luciferase |
JP2660201B2 (ja) | 1988-08-05 | 1997-10-08 | 塩野義製薬株式会社 | 新規ピロロ[1,4]ベンゾジアゼピン誘導体および老人性痴呆薬 |
FR2676230B1 (fr) | 1991-05-07 | 1993-08-27 | Centre Nat Rech Scient | Nouveaux derives de pyrrolo [1,4]-benzodiazepines, leur procede de preparation et medicaments les contenant. |
GB9205051D0 (en) | 1992-03-09 | 1992-04-22 | Cancer Res Campaign Tech | Pyrrolobenzodiazepine derivatives,their preparation,and compositions containing them |
FR2696176B1 (fr) | 1992-09-28 | 1994-11-10 | Synthelabo | Dérivés de pipéridine, leur préparation et leur application en thérapeutique. |
US6214345B1 (en) | 1993-05-14 | 2001-04-10 | Bristol-Myers Squibb Co. | Lysosomal enzyme-cleavable antitumor drug conjugates |
GB9316162D0 (en) | 1993-08-04 | 1993-09-22 | Zeneca Ltd | Fungicides |
JPH08336393A (ja) | 1995-04-13 | 1996-12-24 | Mitsubishi Chem Corp | 光学活性なγ−置換−β−ヒドロキシ酪酸エステルの製造法 |
US6602677B1 (en) | 1997-09-19 | 2003-08-05 | Promega Corporation | Thermostable luciferases and methods of production |
ATE349722T1 (de) | 1998-07-08 | 2007-01-15 | E Ink Corp | Verbesserte farbige mikroverkapselte elektrophoretische anzeige |
GB9818730D0 (en) | 1998-08-27 | 1998-10-21 | Univ Portsmouth | Collections of compounds |
GB9818732D0 (en) | 1998-08-27 | 1998-10-21 | Univ Portsmouth | Collection of compounds |
GB9818731D0 (en) | 1998-08-27 | 1998-10-21 | Univ Portsmouth | Compounds |
PT1413582E (pt) | 1998-08-27 | 2006-07-31 | Spirogen Ltd | Pirrolobenzodiazepinas dimericas |
US6909006B1 (en) | 1999-08-27 | 2005-06-21 | Spirogen Limited | Cyclopropylindole derivatives |
JP2003518075A (ja) | 1999-12-24 | 2003-06-03 | ジェネンテック・インコーポレーテッド | 生理活性化合物の消失半減期延長のための方法及び組成物 |
US20040001827A1 (en) | 2002-06-28 | 2004-01-01 | Dennis Mark S. | Serum albumin binding peptides for tumor targeting |
DK1320522T3 (da) | 2000-09-19 | 2006-04-03 | Moses Lee | Achirale analoger af CC-1065 og af duocarmyciner samt præparater og metoder til anvendelse deraf |
US6362331B1 (en) | 2001-03-30 | 2002-03-26 | Council Of Scientific And Industrial Research | Process for the preparation of antitumor agents |
US6660856B2 (en) | 2002-03-08 | 2003-12-09 | Kaohsiung Medical University | Synthesis of pyrrolo[2,1-c][1,4]benzodiazepine analogues |
AU2003263964C1 (en) | 2002-07-31 | 2010-08-19 | Seagen Inc. | Drug conjugates and their use for treating cancer, an autoimmune disease or an infectious disease |
US20040138269A1 (en) | 2002-10-11 | 2004-07-15 | Sugen, Inc. | Substituted pyrroles as kinase inhibitors |
GB0226593D0 (en) | 2002-11-14 | 2002-12-24 | Consultants Ltd | Compounds |
DE60326060D1 (de) | 2003-03-31 | 2009-03-19 | Council Scient Ind Res | Nichtvernetzende pyrroloä2,1-cüä1,4übenzodiazepine als potentielle antitumor-agentien und ihre herstellung |
GB0321295D0 (en) | 2003-09-11 | 2003-10-15 | Spirogen Ltd | Synthesis of protected pyrrolobenzodiazepines |
ATE516288T1 (de) | 2003-10-22 | 2011-07-15 | Us Gov Health & Human Serv | Pyrrolobenzodiazepinderivate, zusammensetzungen, die diese enthalten, und damit in zusammenhang stehende verfahren |
GB0416511D0 (en) | 2003-10-22 | 2004-08-25 | Spirogen Ltd | Pyrrolobenzodiazepines |
SI1725249T1 (sl) | 2003-11-06 | 2014-04-30 | Seattle Genetics, Inc. | Spojine monometilvalina, sposobne konjugacije na ligande |
AU2005214988A1 (en) | 2004-02-17 | 2005-09-01 | Absalus, Inc. | Super-humanized antibodies against respiratory syncytial virus |
WO2005082023A2 (en) | 2004-02-23 | 2005-09-09 | Genentech, Inc. | Heterocyclic self-immolative linkers and conjugates |
GB0404578D0 (en) | 2004-03-01 | 2004-04-07 | Spirogen Ltd | Pyrrolobenzodiazepines |
GB0404577D0 (en) | 2004-03-01 | 2004-04-07 | Spirogen Ltd | Pyrrolobenzodiazepines |
GB0404574D0 (en) | 2004-03-01 | 2004-04-07 | Spirogen Ltd | Amino acids |
SI1720881T1 (sl) | 2004-03-01 | 2013-04-30 | Spirogen Sarl | 11-hidroksi-5H-pirolo(2,1-c)(1,4)benzodiazepin-5onski derivati kot ključni intermediati za pipravo C2 substituiranih pirolobenzodiazepinov |
DE102004010943A1 (de) | 2004-03-03 | 2005-09-29 | Degussa Ag | Verfahren zur Herstellung von N-geschützten 4-Ketprolinderivaten |
JP5166861B2 (ja) | 2004-03-09 | 2013-03-21 | スピロゲン リミティッド | ピロロベンゾジアゼピン |
FR2869231B1 (fr) | 2004-04-27 | 2008-03-14 | Sod Conseils Rech Applic | Composition therapeutique contenant au moins un derive de la pyrrolobenzodiazepine et la fludarabine |
GB0410725D0 (en) | 2004-05-13 | 2004-06-16 | Spirogen Ltd | Pyrrolobenzodiazepine therapeutic agents |
WO2006034488A2 (en) | 2004-09-23 | 2006-03-30 | Genentech, Inc. | Cysteine engineered antibodies and conjugates |
CN101080506B (zh) | 2004-12-24 | 2012-06-13 | 昭和电工株式会社 | 热电半导体合金的制造方法、热电转换模块以及热电发电设备 |
US20080206239A1 (en) | 2005-02-03 | 2008-08-28 | Antitope Limited | Human Antibodies And Proteins |
JP5122441B2 (ja) | 2005-04-19 | 2013-01-16 | シアトル ジェネティックス, インコーポレイテッド | ヒト化抗cd70結合剤およびその使用 |
NZ563136A (en) | 2005-04-21 | 2009-11-27 | Spirogen Ltd | Pyrrolobenzodiazepines |
WO2007039752A1 (en) | 2005-10-05 | 2007-04-12 | Spirogen Limited | Alkyl 4- [4- (5-oxo-2, 3, 5, 11a-tetrahyd0-5h-pyrr0l0 [2, 1-c] [1, 4] benzodiazepine-8-yloxy) -butyrylamino]-1h-pyrrole-2-carboxylate derivatives and related compounds for the treatment of a proliferative disease |
US20070154906A1 (en) | 2005-10-05 | 2007-07-05 | Spirogen Ltd. | Methods to identify therapeutic candidates |
JP5129143B2 (ja) | 2005-10-07 | 2013-01-23 | エグゼリクシス, インコーポレイテッド | Mekインヒビターおよびその使用方法 |
ATE527262T1 (de) | 2006-01-25 | 2011-10-15 | Sanofi Sa | Neue tomaymycin derivate enhaltende zytotoxische mittel |
ES2673822T3 (es) | 2006-07-18 | 2018-06-25 | Sanofi | Anticuerpo antagonista contra EphA2 para el tratamiento de cáncer |
EP1914242A1 (en) | 2006-10-19 | 2008-04-23 | Sanofi-Aventis | Novel anti-CD38 antibodies for the treatment of cancer |
WO2008050140A2 (en) | 2006-10-27 | 2008-05-02 | Spirogen Limited | Compounds for treatment of parasitic infection |
PL2099823T5 (pl) | 2006-12-01 | 2023-02-20 | Seagen Inc. | Wariant środków wiążących cel i jego zastosowania |
PE20090245A1 (es) | 2007-05-08 | 2009-03-17 | Genentech Inc | Anticuerpos anti-muc16 disenados con cisteina y conjugados de anticuerpos y farmacos |
ES2435779T3 (es) | 2007-07-19 | 2013-12-23 | Sanofi | Agentes citotóxicos que comprenden nuevos derivados de tomaimicina y su uso terapéutico |
WO2009052249A1 (en) | 2007-10-19 | 2009-04-23 | Genentech, Inc. | Cysteine engineered anti-tenb2 antibodies and antibody drug conjugates |
GB0722087D0 (en) | 2007-11-09 | 2007-12-19 | Spirogen Ltd | Polyamides |
GB0722088D0 (en) | 2007-11-09 | 2007-12-19 | Spirogen Ltd | Pyrrolobenzodiazepines |
MX2010007767A (es) * | 2008-01-18 | 2010-08-09 | Medimmune Llc | Anticuerpos manipulados con cisteina para conjugacion especifica de sitio. |
US8609105B2 (en) | 2008-03-18 | 2013-12-17 | Seattle Genetics, Inc. | Auristatin drug linker conjugates |
GB0813432D0 (en) | 2008-07-22 | 2008-08-27 | Spirogen Ltd | Pyrrolobenzodiazepines |
EP2349040B9 (en) | 2008-10-15 | 2014-12-17 | Zimmer GmbH | Intramedullary nail |
GB0819095D0 (en) | 2008-10-17 | 2008-11-26 | Spirogen Ltd | Pyrrolobenzodiazepines |
GB0819097D0 (en) | 2008-10-17 | 2008-11-26 | Spirogen Ltd | Pyrrolobenzodiazepines |
IL271761B (en) | 2009-02-05 | 2022-09-01 | Immunogen Inc | (12as)-8-methoxy-9-benzyloxy-11,12,12a,13-tetrahydro-6h-indolo[2,1-c][1,4]benzodiazepine-6-one, 4-benzyloxy-5-methoxy -2-nitrobenzoic acid and a process for their preparation |
FR2949469A1 (fr) | 2009-08-25 | 2011-03-04 | Sanofi Aventis | Derives anticancereux, leur preparation et leur application en therapeutique |
JP2013505944A (ja) | 2009-09-24 | 2013-02-21 | シアトル ジェネティックス, インコーポレイテッド | Dr5リガンド薬物結合体 |
ES2449379T3 (es) | 2010-02-09 | 2014-03-19 | Bristol-Myers Squibb Company | Derivados de bencilpirrolidinona como moduladores de la actividad de receptores de quimiocinas |
GB201006340D0 (en) | 2010-04-15 | 2010-06-02 | Spirogen Ltd | Synthesis method and intermediates |
AU2011239525B2 (en) | 2010-04-15 | 2015-04-09 | Medimmune Limited | Pyrrolobenzodiazepines used to treat proliferative diseases |
PE20130342A1 (es) | 2010-04-15 | 2013-04-20 | Spirogen Sarl | Pirrolobenzodiacepinas y conjugados de las mismas |
WO2011130615A2 (en) | 2010-04-15 | 2011-10-20 | Dr. Reddy's Laboratories Ltd. | Preparation of lacosamide |
AU2011239522B2 (en) * | 2010-04-15 | 2014-10-23 | Medimmune Limited | Targeted pyrrolobenzodiazapine conjugates |
US9534000B2 (en) | 2011-02-15 | 2017-01-03 | Immunogen, Inc. | Cytotoxic benzodiazepine derivatives and methods of preparation |
CA2849039C (en) | 2011-09-20 | 2018-09-18 | Spirogen Sarl | Pyrrolobenzodiazepines as unsymmetrical dimeric pbd compounds for inclusion in targeted conjugates |
BR112014008888A2 (pt) | 2011-10-14 | 2017-04-18 | Seattle Genetics Inc | pirrolobenzodiazepinas |
EA036202B1 (ru) | 2011-10-14 | 2020-10-14 | Сиэтл Дженетикс, Инк. | Пирролбензодиазепины и конъюгаты направленного действия |
EP3388435B1 (en) | 2011-10-14 | 2023-05-03 | Seagen Inc. | Pyrrolobenzodiazepines and targeted conjugates |
EA029046B1 (ru) | 2011-10-14 | 2018-02-28 | Медимьюн Лимитед | Пирролобензодиазепины и промежуточные соединения для их получения, способы их синтеза |
US9388187B2 (en) | 2011-10-14 | 2016-07-12 | Medimmune Limited | Pyrrolobenzodiazepines |
HUE025661T2 (en) | 2011-10-14 | 2016-04-28 | Medimmune Ltd | Pyrrolobenzodiazepines and their conjugates |
BR112014027190B1 (pt) | 2012-04-30 | 2020-03-03 | Medimmune Limited | Composto de pirrolobenzodiazepinas, sua composição farmacêutica e seu uso |
EP2855482B1 (en) | 2012-04-30 | 2017-03-01 | MedImmune Limited | Pyrrolobenzodiazepines |
CA2873889A1 (en) | 2012-07-09 | 2014-01-16 | Genentech, Inc. | Anti-cd22 antibodies and immunoconjugates |
MA37840B1 (fr) | 2012-07-09 | 2020-05-29 | Genentech Inc | Immunoconjugués comprenant des anticorps anti-cd79b |
BR112015002193A2 (pt) | 2012-08-02 | 2017-07-04 | Genentech Inc | anticorpos anti-etbr e imunoconjugados |
NZ707486A (en) | 2012-10-12 | 2018-09-28 | Adc Therapeutics Sa | Pyrrolobenzodiazepine - anti-psma antibody conjugates |
CA2887896A1 (en) | 2012-10-12 | 2014-04-17 | Adc Therapeutics Sarl | Pyrrolobenzodiazepine-anti-her2 antibody conjugates |
MX364328B (es) | 2012-10-12 | 2019-04-23 | Medimmune Ltd | Conjugados del anticuerpo pirrolobenzodiazepina. |
WO2014057114A1 (en) | 2012-10-12 | 2014-04-17 | Adc Therapeutics Sàrl | Pyrrolobenzodiazepine-anti-psma antibody conjugates |
WO2014057118A1 (en) | 2012-10-12 | 2014-04-17 | Adc Therapeutics Sarl | Pyrrolobenzodiazepine-anti-cd22 antibody conjugates |
AU2013328673B2 (en) | 2012-10-12 | 2017-07-13 | Medimmune Limited | Synthesis and intermediates of pyrrolobenzodiazepine derivatives for conjugation |
EP2906297B1 (en) | 2012-10-12 | 2017-12-06 | ADC Therapeutics SA | Pyrrolobenzodiazepine-antibody conjugates |
PL2766048T3 (pl) | 2012-10-12 | 2015-05-29 | Medimmune Ltd | Pirolobenzodiazepiny i ich koniugaty |
DK2906251T3 (da) | 2012-10-12 | 2017-11-20 | Adc Therapeutics Sa | Pyrrolobenzodiazepin-anti-CD22-antistofkonjugater |
NZ707534A (en) | 2012-10-12 | 2018-08-31 | Adc Therapeutics Sa | Pyrrolobenzodiazepine-antibody conjugates |
CA3060520C (en) | 2012-10-12 | 2022-05-17 | Medimmune Limited | Pyrrolobenzodiazepines and conjugates thereof |
CA2894959C (en) | 2012-12-21 | 2022-01-11 | Spirogen Sarl | Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases |
CN110452242A (zh) | 2012-12-21 | 2019-11-15 | 麦迪穆有限责任公司 | 吡咯并苯并二氮杂卓及其结合物 |
CN105164159A (zh) | 2013-02-22 | 2015-12-16 | 施特姆森特克斯股份有限公司 | 新的抗体缀合物及其用途 |
US20160031887A1 (en) | 2013-03-13 | 2016-02-04 | Medimmune Limited | Pyrrolobenzodiazepines and conjugates thereof |
CN105142674B (zh) | 2013-03-13 | 2018-11-13 | 麦迪穆有限责任公司 | 吡咯并苯并二氮杂卓和其结合物 |
AU2014244245C1 (en) | 2013-03-13 | 2018-04-19 | Genentech, Inc. | Pyrrolobenzodiazepines and conjugates thereof |
WO2014174111A1 (en) | 2013-04-26 | 2014-10-30 | Pierre Fabre Medicament | Axl antibody-drug conjugate and its use for the treatment of cancer |
GB201317981D0 (en) | 2013-10-11 | 2013-11-27 | Spirogen Sarl | Pyrrolobenzodiazepines and conjugates thereof |
US10010624B2 (en) | 2013-10-11 | 2018-07-03 | Medimmune Limited | Pyrrolobenzodiazepine-antibody conjugates |
GB201317982D0 (en) | 2013-10-11 | 2013-11-27 | Spirogen Sarl | Pyrrolobenzodiazepines and conjugates thereof |
EP3054986B1 (en) | 2013-10-11 | 2019-03-20 | Medimmune Limited | Pyrrolobenzodiazepine-antibody conjugates |
US20160256561A1 (en) | 2013-10-11 | 2016-09-08 | Medimmune Limited | Pyrrolobenzodiazepine-antibody conjugates |
WO2015052534A1 (en) | 2013-10-11 | 2015-04-16 | Spirogen Sàrl | Pyrrolobenzodiazepine-antibody conjugates |
BR112016014126B1 (pt) | 2013-12-16 | 2023-02-14 | Medimmune Limited | Composto não-peptídico, conjugados de anticorpo-fármaco do mesmo, uso dos ditos conjugados para o tratamento de câncer e composição farmacêutica que compreende os mesmos |
GB201406767D0 (en) | 2014-04-15 | 2014-05-28 | Cancer Rec Tech Ltd | Humanized anti-Tn-MUC1 antibodies anf their conjugates |
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