JP2019178158A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2019178158A5 JP2019178158A5 JP2019117132A JP2019117132A JP2019178158A5 JP 2019178158 A5 JP2019178158 A5 JP 2019178158A5 JP 2019117132 A JP2019117132 A JP 2019117132A JP 2019117132 A JP2019117132 A JP 2019117132A JP 2019178158 A5 JP2019178158 A5 JP 2019178158A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- independently
- integer
- formula
- alkylene
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 55
- 125000005647 linker group Chemical group 0.000 claims 22
- 239000000178 monomer Substances 0.000 claims 20
- -1 heterocyclylene Chemical group 0.000 claims 18
- 239000008194 pharmaceutical composition Substances 0.000 claims 15
- 125000002947 alkylene group Chemical group 0.000 claims 14
- 239000003814 drug Substances 0.000 claims 14
- 229940124597 therapeutic agent Drugs 0.000 claims 14
- 125000000732 arylene group Chemical group 0.000 claims 12
- 125000002993 cycloalkylene group Chemical group 0.000 claims 12
- 125000004474 heteroalkylene group Chemical group 0.000 claims 12
- 125000005549 heteroarylene group Chemical group 0.000 claims 12
- 230000008685 targeting Effects 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- 108010044540 auristatin Proteins 0.000 claims 6
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims 6
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 5
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 5
- FWVCSXWHVOOTFJ-UHFFFAOYSA-N 1-(2-chloroethylsulfanyl)-2-[2-(2-chloroethylsulfanyl)ethoxy]ethane Chemical compound ClCCSCCOCCSCCCl FWVCSXWHVOOTFJ-UHFFFAOYSA-N 0.000 claims 4
- 101800002638 Alpha-amanitin Proteins 0.000 claims 4
- 102100024222 B-lymphocyte antigen CD19 Human genes 0.000 claims 4
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 4
- 101000980825 Homo sapiens B-lymphocyte antigen CD19 Proteins 0.000 claims 4
- 102100027212 Tumor-associated calcium signal transducer 2 Human genes 0.000 claims 4
- 239000000427 antigen Substances 0.000 claims 4
- 102000036639 antigens Human genes 0.000 claims 4
- 108091007433 antigens Proteins 0.000 claims 4
- 239000002246 antineoplastic agent Substances 0.000 claims 4
- 229940127089 cytotoxic agent Drugs 0.000 claims 4
- 239000003112 inhibitor Substances 0.000 claims 4
- YUOCYTRGANSSRY-UHFFFAOYSA-N pyrrolo[2,3-i][1,2]benzodiazepine Chemical compound C1=CN=NC2=C3C=CN=C3C=CC2=C1 YUOCYTRGANSSRY-UHFFFAOYSA-N 0.000 claims 4
- 229960000575 trastuzumab Drugs 0.000 claims 4
- AOSZTAHDEDLTLQ-AZKQZHLXSA-N (1S,2S,4R,8S,9S,11S,12R,13S,19S)-6-[(3-chlorophenyl)methyl]-12,19-difluoro-11-hydroxy-8-(2-hydroxyacetyl)-9,13-dimethyl-6-azapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one Chemical compound C([C@@H]1C[C@H]2[C@H]3[C@]([C@]4(C=CC(=O)C=C4[C@@H](F)C3)C)(F)[C@@H](O)C[C@@]2([C@@]1(C1)C(=O)CO)C)N1CC1=CC=CC(Cl)=C1 AOSZTAHDEDLTLQ-AZKQZHLXSA-N 0.000 claims 3
- ONBQEOIKXPHGMB-VBSBHUPXSA-N 1-[2-[(2s,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]oxy-4,6-dihydroxyphenyl]-3-(4-hydroxyphenyl)propan-1-one Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1OC1=CC(O)=CC(O)=C1C(=O)CCC1=CC=C(O)C=C1 ONBQEOIKXPHGMB-VBSBHUPXSA-N 0.000 claims 3
- QBWKPGNFQQJGFY-QLFBSQMISA-N 3-[(1r)-1-[(2r,6s)-2,6-dimethylmorpholin-4-yl]ethyl]-n-[6-methyl-3-(1h-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-1,2-thiazol-5-amine Chemical compound N1([C@H](C)C2=NSC(NC=3C4=NC=C(N4C=C(C)N=3)C3=CNN=C3)=C2)C[C@H](C)O[C@H](C)C1 QBWKPGNFQQJGFY-QLFBSQMISA-N 0.000 claims 3
- 229940126657 Compound 17 Drugs 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 210000004027 cell Anatomy 0.000 claims 3
- 229940126142 compound 16 Drugs 0.000 claims 3
- 229940125846 compound 25 Drugs 0.000 claims 3
- 125000004404 heteroalkyl group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- DLKUYSQUHXBYPB-NSSHGSRYSA-N (2s,4r)-4-[[2-[(1r,3r)-1-acetyloxy-4-methyl-3-[3-methylbutanoyloxymethyl-[(2s,3s)-3-methyl-2-[[(2r)-1-methylpiperidine-2-carbonyl]amino]pentanoyl]amino]pentyl]-1,3-thiazole-4-carbonyl]amino]-2-methyl-5-(4-methylphenyl)pentanoic acid Chemical compound N([C@@H]([C@@H](C)CC)C(=O)N(COC(=O)CC(C)C)[C@H](C[C@@H](OC(C)=O)C=1SC=C(N=1)C(=O)N[C@H](C[C@H](C)C(O)=O)CC=1C=CC(C)=CC=1)C(C)C)C(=O)[C@H]1CCCCN1C DLKUYSQUHXBYPB-NSSHGSRYSA-N 0.000 claims 2
- WVHGJJRMKGDTEC-WCIJHFMNSA-N 2-[(1R,4S,8R,10S,13S,16S,27R,34S)-34-[(2S)-butan-2-yl]-8,22-dihydroxy-13-[(2R,3S)-3-hydroxybutan-2-yl]-2,5,11,14,27,30,33,36,39-nonaoxo-27lambda4-thia-3,6,12,15,25,29,32,35,38-nonazapentacyclo[14.12.11.06,10.018,26.019,24]nonatriaconta-18(26),19(24),20,22-tetraen-4-yl]acetamide Chemical compound CC[C@H](C)[C@@H]1NC(=O)CNC(=O)[C@@H]2Cc3c([nH]c4cc(O)ccc34)[S@](=O)C[C@H](NC(=O)CNC1=O)C(=O)N[C@@H](CC(N)=O)C(=O)N1C[C@H](O)C[C@H]1C(=O)N[C@@H]([C@@H](C)[C@H](C)O)C(=O)N2 WVHGJJRMKGDTEC-WCIJHFMNSA-N 0.000 claims 2
- 102100033400 4F2 cell-surface antigen heavy chain Human genes 0.000 claims 2
- 102100038080 B-cell receptor CD22 Human genes 0.000 claims 2
- 101800001350 Beta-amanitin Proteins 0.000 claims 2
- 102100025221 CD70 antigen Human genes 0.000 claims 2
- 102000000905 Cadherin Human genes 0.000 claims 2
- 108050007957 Cadherin Proteins 0.000 claims 2
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims 2
- 102100025475 Carcinoembryonic antigen-related cell adhesion molecule 5 Human genes 0.000 claims 2
- 102100039496 Choline transporter-like protein 4 Human genes 0.000 claims 2
- 102000008186 Collagen Human genes 0.000 claims 2
- 108010035532 Collagen Proteins 0.000 claims 2
- 239000012623 DNA damaging agent Substances 0.000 claims 2
- 102000000820 Enterotoxin Receptors Human genes 0.000 claims 2
- 108010001687 Enterotoxin Receptors Proteins 0.000 claims 2
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 claims 2
- 239000005977 Ethylene Substances 0.000 claims 2
- 108010067306 Fibronectins Proteins 0.000 claims 2
- 102000016359 Fibronectins Human genes 0.000 claims 2
- 102100041003 Glutamate carboxypeptidase 2 Human genes 0.000 claims 2
- 102100030595 HLA class II histocompatibility antigen gamma chain Human genes 0.000 claims 2
- 101000800023 Homo sapiens 4F2 cell-surface antigen heavy chain Proteins 0.000 claims 2
- 101000884305 Homo sapiens B-cell receptor CD22 Proteins 0.000 claims 2
- 101000934356 Homo sapiens CD70 antigen Proteins 0.000 claims 2
- 101000914324 Homo sapiens Carcinoembryonic antigen-related cell adhesion molecule 5 Proteins 0.000 claims 2
- 101000892862 Homo sapiens Glutamate carboxypeptidase 2 Proteins 0.000 claims 2
- 101001082627 Homo sapiens HLA class II histocompatibility antigen gamma chain Proteins 0.000 claims 2
- 101000605020 Homo sapiens Large neutral amino acids transporter small subunit 1 Proteins 0.000 claims 2
- 101000777628 Homo sapiens Leukocyte antigen CD37 Proteins 0.000 claims 2
- 101000628547 Homo sapiens Metalloreductase STEAP1 Proteins 0.000 claims 2
- 101000934338 Homo sapiens Myeloid cell surface antigen CD33 Proteins 0.000 claims 2
- 101000581981 Homo sapiens Neural cell adhesion molecule 1 Proteins 0.000 claims 2
- 101000897042 Homo sapiens Nucleotide pyrophosphatase Proteins 0.000 claims 2
- 101000874179 Homo sapiens Syndecan-1 Proteins 0.000 claims 2
- 101000904724 Homo sapiens Transmembrane glycoprotein NMB Proteins 0.000 claims 2
- 101000801433 Homo sapiens Trophoblast glycoprotein Proteins 0.000 claims 2
- 101000851376 Homo sapiens Tumor necrosis factor receptor superfamily member 8 Proteins 0.000 claims 2
- 101000851007 Homo sapiens Vascular endothelial growth factor receptor 2 Proteins 0.000 claims 2
- 101000685848 Homo sapiens Zinc transporter ZIP6 Proteins 0.000 claims 2
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims 2
- 102100031586 Leukocyte antigen CD37 Human genes 0.000 claims 2
- 229940124647 MEK inhibitor Drugs 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 102000003735 Mesothelin Human genes 0.000 claims 2
- 108090000015 Mesothelin Proteins 0.000 claims 2
- 102100026712 Metalloreductase STEAP1 Human genes 0.000 claims 2
- 108010008707 Mucin-1 Proteins 0.000 claims 2
- 102000007298 Mucin-1 Human genes 0.000 claims 2
- 102100025243 Myeloid cell surface antigen CD33 Human genes 0.000 claims 2
- 102100035486 Nectin-4 Human genes 0.000 claims 2
- 101710043865 Nectin-4 Proteins 0.000 claims 2
- 102100027347 Neural cell adhesion molecule 1 Human genes 0.000 claims 2
- 102100021969 Nucleotide pyrophosphatase Human genes 0.000 claims 2
- 229930012538 Paclitaxel Natural products 0.000 claims 2
- 102100037765 Periostin Human genes 0.000 claims 2
- 101710199268 Periostin Proteins 0.000 claims 2
- LOUPRKONTZGTKE-WZBLMQSHSA-N Quinine Chemical group C([C@H]([C@H](C1)C=C)C2)C[N@@]1[C@@H]2[C@H](O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-WZBLMQSHSA-N 0.000 claims 2
- RXGJTYFDKOHJHK-UHFFFAOYSA-N S-deoxo-amaninamide Natural products CCC(C)C1NC(=O)CNC(=O)C2Cc3c(SCC(NC(=O)CNC1=O)C(=O)NC(CC(=O)N)C(=O)N4CC(O)CC4C(=O)NC(C(C)C(O)CO)C(=O)N2)[nH]c5ccccc35 RXGJTYFDKOHJHK-UHFFFAOYSA-N 0.000 claims 2
- 108091007561 SLC44A4 Proteins 0.000 claims 2
- 102100035721 Syndecan-1 Human genes 0.000 claims 2
- 108700012457 TACSTD2 Proteins 0.000 claims 2
- 101150117918 Tacstd2 gene Proteins 0.000 claims 2
- 102000007000 Tenascin Human genes 0.000 claims 2
- 108010008125 Tenascin Proteins 0.000 claims 2
- 102100023935 Transmembrane glycoprotein NMB Human genes 0.000 claims 2
- 102100033579 Trophoblast glycoprotein Human genes 0.000 claims 2
- 102100036857 Tumor necrosis factor receptor superfamily member 8 Human genes 0.000 claims 2
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims 2
- 102100023144 Zinc transporter ZIP6 Human genes 0.000 claims 2
- 229930013930 alkaloid Natural products 0.000 claims 2
- 150000003797 alkaloid derivatives Chemical class 0.000 claims 2
- 239000004007 alpha amanitin Substances 0.000 claims 2
- CIORWBWIBBPXCG-SXZCQOKQSA-N alpha-amanitin Chemical compound O=C1N[C@@H](CC(N)=O)C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H]([C@@H](C)[C@@H](O)CO)C(=O)N[C@@H](C2)C(=O)NCC(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@H]1C[S@@](=O)C1=C2C2=CC=C(O)C=C2N1 CIORWBWIBBPXCG-SXZCQOKQSA-N 0.000 claims 2
- CIORWBWIBBPXCG-UHFFFAOYSA-N alpha-amanitin Natural products O=C1NC(CC(N)=O)C(=O)N2CC(O)CC2C(=O)NC(C(C)C(O)CO)C(=O)NC(C2)C(=O)NCC(=O)NC(C(C)CC)C(=O)NCC(=O)NC1CS(=O)C1=C2C2=CC=C(O)C=C2N1 CIORWBWIBBPXCG-UHFFFAOYSA-N 0.000 claims 2
- 239000004080 beta amanitin Substances 0.000 claims 2
- IEQCUEXVAPAFMQ-UHFFFAOYSA-N beta-amanitin Natural products O=C1NC(CC(O)=O)C(=O)N2CC(O)CC2C(=O)NC(C(C)C(O)CO)C(=O)NC(C2)C(=O)NCC(=O)NC(C(C)CC)C(=O)NCC(=O)NC1CS(=O)C1=C2C2=CC=C(O)C=C2N1 IEQCUEXVAPAFMQ-UHFFFAOYSA-N 0.000 claims 2
- 229930195731 calicheamicin Natural products 0.000 claims 2
- HXCHCVDVKSCDHU-LULTVBGHSA-N calicheamicin Chemical compound C1[C@H](OC)[C@@H](NCC)CO[C@H]1O[C@H]1[C@H](O[C@@H]2C\3=C(NC(=O)OC)C(=O)C[C@](C/3=C/CSSSC)(O)C#C\C=C/C#C2)O[C@H](C)[C@@H](NO[C@@H]2O[C@H](C)[C@@H](SC(=O)C=3C(=C(OC)C(O[C@H]4[C@@H]([C@H](OC)[C@@H](O)[C@H](C)O4)O)=C(I)C=3C)OC)[C@@H](O)C2)[C@@H]1O HXCHCVDVKSCDHU-LULTVBGHSA-N 0.000 claims 2
- 229940127093 camptothecin Drugs 0.000 claims 2
- 229920001436 collagen Polymers 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims 2
- 229960004679 doxorubicin Drugs 0.000 claims 2
- 229960005501 duocarmycin Drugs 0.000 claims 2
- VQNATVDKACXKTF-XELLLNAOSA-N duocarmycin Chemical compound COC1=C(OC)C(OC)=C2NC(C(=O)N3C4=CC(=O)C5=C([C@@]64C[C@@H]6C3)C=C(N5)C(=O)OC)=CC2=C1 VQNATVDKACXKTF-XELLLNAOSA-N 0.000 claims 2
- 229930184221 duocarmycin Natural products 0.000 claims 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 2
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 2
- 229940014144 folate Drugs 0.000 claims 2
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 claims 2
- 235000019152 folic acid Nutrition 0.000 claims 2
- 239000011724 folic acid Substances 0.000 claims 2
- IEQCUEXVAPAFMQ-SXZCQOKQSA-N g729ypp47l Chemical compound O=C1N[C@@H](CC(O)=O)C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H]([C@@H](C)[C@@H](O)CO)C(=O)N[C@@H](C2)C(=O)NCC(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@H]1C[S@@](=O)C1=C2C2=CC=C(O)C=C2N1 IEQCUEXVAPAFMQ-SXZCQOKQSA-N 0.000 claims 2
- WVHGJJRMKGDTEC-UHFFFAOYSA-N gamma-amanitin Natural products O=C1NC(CC(N)=O)C(=O)N2CC(O)CC2C(=O)NC(C(C)C(C)O)C(=O)NC(C2)C(=O)NCC(=O)NC(C(C)CC)C(=O)NCC(=O)NC1CS(=O)C1=C2C2=CC=C(O)C=C2N1 WVHGJJRMKGDTEC-UHFFFAOYSA-N 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 229940043355 kinase inhibitor Drugs 0.000 claims 2
- 239000003446 ligand Substances 0.000 claims 2
- 229960000485 methotrexate Drugs 0.000 claims 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 2
- 231100000782 microtubule inhibitor Toxicity 0.000 claims 2
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 2
- 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 2
- 229960001592 paclitaxel Drugs 0.000 claims 2
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 2
- 229920001481 poly(stearyl methacrylate) Polymers 0.000 claims 2
- 102000004196 processed proteins & peptides Human genes 0.000 claims 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims 2
- 229930002341 quinoline alkaloid Natural products 0.000 claims 2
- UOWVMDUEMSNCAV-WYENRQIDSA-N rachelmycin Chemical class C1([C@]23C[C@@H]2CN1C(=O)C=1NC=2C(OC)=C(O)C4=C(C=2C=1)CCN4C(=O)C1=CC=2C=4CCN(C=4C(O)=C(C=2N1)OC)C(N)=O)=CC(=O)C1=C3C(C)=CN1 UOWVMDUEMSNCAV-WYENRQIDSA-N 0.000 claims 2
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 2
- 230000035897 transcription Effects 0.000 claims 2
- 238000013518 transcription Methods 0.000 claims 2
- 229930184737 tubulysin Natural products 0.000 claims 2
- 229960005502 α-amanitin Drugs 0.000 claims 2
- OFILNAORONITPV-ZUROAWGWSA-N ε-amanitin Chemical compound O=C1N[C@@H](CC(O)=O)C(=O)N2C[C@H](O)C[C@H]2C(=O)N[C@@H]([C@@H](C)[C@H](C)O)C(=O)N[C@@H](C2)C(=O)NCC(=O)N[C@@H]([C@@H](C)CC)C(=O)NCC(=O)N[C@H]1CS(=O)C1=C2C2=CC=C(O)C=C2N1 OFILNAORONITPV-ZUROAWGWSA-N 0.000 claims 2
- WZZBNLYBHUDSHF-DHLKQENFSA-N 1-[(3s,4s)-4-[8-(2-chloro-4-pyrimidin-2-yloxyphenyl)-7-fluoro-2-methylimidazo[4,5-c]quinolin-1-yl]-3-fluoropiperidin-1-yl]-2-hydroxyethanone Chemical compound CC1=NC2=CN=C3C=C(F)C(C=4C(=CC(OC=5N=CC=CN=5)=CC=4)Cl)=CC3=C2N1[C@H]1CCN(C(=O)CO)C[C@@H]1F WZZBNLYBHUDSHF-DHLKQENFSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 238000007913 intrathecal administration Methods 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 230000002685 pulmonary effect Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 238000011255 standard chemotherapy Methods 0.000 claims 1
- 239000008223 sterile water Substances 0.000 claims 1
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 230000000699 topical effect Effects 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 0 CC(C)(C)N(C(CC1*)=O)C1=O Chemical compound CC(C)(C)N(C(CC1*)=O)C1=O 0.000 description 39
- HRDWHBMAXHWZBF-UHFFFAOYSA-N CC(C)C(C(C(C)C)=O)N Chemical compound CC(C)C(C(C(C)C)=O)N HRDWHBMAXHWZBF-UHFFFAOYSA-N 0.000 description 1
- CWPHAVLGPBXYCF-UHFFFAOYSA-N CC(C1CNCCC1)=[O]=C Chemical compound CC(C1CNCCC1)=[O]=C CWPHAVLGPBXYCF-UHFFFAOYSA-N 0.000 description 1
- FSFHCYNAHIWOBP-UHFFFAOYSA-N CSC(C1NCCC1)=O Chemical compound CSC(C1NCCC1)=O FSFHCYNAHIWOBP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662345557P | 2016-06-03 | 2016-06-03 | |
| US62/345,557 | 2016-06-03 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018569182A Division JP6548843B1 (ja) | 2016-06-03 | 2017-06-02 | ポリマーリンカーおよびそれらの使用法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019178158A JP2019178158A (ja) | 2019-10-17 |
| JP2019178158A5 true JP2019178158A5 (https=) | 2020-08-06 |
| JP7144681B2 JP7144681B2 (ja) | 2022-09-30 |
Family
ID=60477864
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018569182A Active JP6548843B1 (ja) | 2016-06-03 | 2017-06-02 | ポリマーリンカーおよびそれらの使用法 |
| JP2019117132A Active JP7144681B2 (ja) | 2016-06-03 | 2019-06-25 | ポリマーリンカーおよびそれらの使用法 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018569182A Active JP6548843B1 (ja) | 2016-06-03 | 2017-06-02 | ポリマーリンカーおよびそれらの使用法 |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US10583196B2 (https=) |
| EP (2) | EP4094778B1 (https=) |
| JP (2) | JP6548843B1 (https=) |
| KR (2) | KR102283536B1 (https=) |
| CN (1) | CN109563215B (https=) |
| AU (1) | AU2017273871B2 (https=) |
| WO (1) | WO2017210566A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4094778B1 (en) | 2016-06-03 | 2024-05-15 | Novacyte Therapeutics Company.,LTD | Polymer linkers and their uses |
| CN109796537A (zh) * | 2019-02-28 | 2019-05-24 | 中国农业大学 | 一种β-鹅膏毒肽人工抗原及其制备方法与应用 |
| WO2022155362A1 (en) * | 2021-01-15 | 2022-07-21 | R.P. Scherer Technologies, Llc | Dual-cleavage ester linkers for antibody-drug conjugates |
| KR102895959B1 (ko) * | 2021-07-28 | 2025-12-04 | 성균관대학교산학협력단 | 엑소좀 분비 억제제와 면역관문 억제제를 이용한 병용 치료 요법 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4256108A (en) | 1977-04-07 | 1981-03-17 | Alza Corporation | Microporous-semipermeable laminated osmotic system |
| US4160452A (en) | 1977-04-07 | 1979-07-10 | Alza Corporation | Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina |
| US4265874A (en) | 1980-04-25 | 1981-05-05 | Alza Corporation | Method of delivering drug with aid of effervescent activity generated in environment of use |
| US5169645A (en) | 1989-10-31 | 1992-12-08 | Duquesne University Of The Holy Ghost | Directly compressible granules having improved flow properties |
| US6323219B1 (en) | 1998-04-02 | 2001-11-27 | Ortho-Mcneil Pharmaceutical, Inc. | Methods for treating immunomediated inflammatory disorders |
| AU2003209227A1 (en) * | 2002-01-14 | 2003-07-30 | The General Hospital Corporation | Biodegradable polyketal polymers and methods for their formation and use |
| AU2004270251B2 (en) * | 2003-09-05 | 2011-03-31 | The General Hospital Corporation | Polyacetal drug conjugates as release system |
| US7498298B2 (en) | 2003-11-06 | 2009-03-03 | Seattle Genetics, Inc. | Monomethylvaline compounds capable of conjugation to ligands |
| WO2010068759A1 (en) * | 2008-12-10 | 2010-06-17 | Mersana Therapeutics, Inc. | Pharmaceutical formulations of biodegradable biocompatible camptothecin-polymer conjugates |
| WO2010138719A1 (en) | 2009-05-28 | 2010-12-02 | Mersana Therapeutics, Inc. | Polyal drug conjugates comprising variable rate-releasing linkers |
| US8349308B2 (en) * | 2010-03-26 | 2013-01-08 | Mersana Therapeutics, Inc. | Modified polymers for delivery of polynucleotides, method of manufacture, and methods of use thereof |
| WO2012171020A1 (en) | 2011-06-10 | 2012-12-13 | Mersana Therapeutics, Inc. | Protein-polymer-drug conjugates |
| EP2794582A1 (en) * | 2011-12-23 | 2014-10-29 | Mersana Therapeutics, Inc. | Pharmaceutical formulations for fumagillin derivative-phf conjugates |
| US20160022829A1 (en) | 2013-03-14 | 2016-01-28 | Mersana Therapeutics, Inc. | Tubulysin compounds and conjugates thereof |
| WO2014152850A1 (en) * | 2013-03-14 | 2014-09-25 | The University Of Akron | Densely functionalized polymers derived from baylis-hillman adducts |
| CA2927022C (en) * | 2013-10-11 | 2018-08-21 | Asana Biosciences, Llc | Protein-polymer-drug conjugates |
| EA032231B1 (ru) * | 2013-10-11 | 2019-04-30 | Мерсана Терапьютикс, Инк. | Конъюгаты белок-полимер-лекарственное средство |
| WO2015195925A1 (en) * | 2014-06-18 | 2015-12-23 | Mersana Therapeutics, Inc. | Protein-polymer-drug conjugates and methods of using same |
| EP4094778B1 (en) | 2016-06-03 | 2024-05-15 | Novacyte Therapeutics Company.,LTD | Polymer linkers and their uses |
-
2017
- 2017-06-02 EP EP22166800.7A patent/EP4094778B1/en active Active
- 2017-06-02 US US15/572,720 patent/US10583196B2/en active Active
- 2017-06-02 KR KR1020197030061A patent/KR102283536B1/ko active Active
- 2017-06-02 EP EP17807574.3A patent/EP3464400B1/en active Active
- 2017-06-02 JP JP2018569182A patent/JP6548843B1/ja active Active
- 2017-06-02 AU AU2017273871A patent/AU2017273871B2/en active Active
- 2017-06-02 CN CN201780046754.2A patent/CN109563215B/zh active Active
- 2017-06-02 WO PCT/US2017/035698 patent/WO2017210566A1/en not_active Ceased
- 2017-06-02 KR KR1020187037645A patent/KR102034697B1/ko active Active
-
2019
- 2019-06-25 JP JP2019117132A patent/JP7144681B2/ja active Active
-
2020
- 2020-01-28 US US16/774,829 patent/US11529422B2/en active Active
-
2022
- 2022-11-16 US US17/988,595 patent/US12343399B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2019178158A5 (https=) | ||
| JP6193433B2 (ja) | Ｃｃ−１０６５類似体の新規の複合体および二官能性リンカー | |
| AU2010306917B2 (en) | Polymeric systems for the delivery of anticancer agents | |
| AU2009302387B2 (en) | HPMA - docetaxel or gemcitabine conjugates and uses therefore | |
| KR20230008723A (ko) | 전하 변이체 링커 | |
| JP2012528240A5 (https=) | ||
| AU2003230852B2 (en) | TNP-470 polymer conjugates and use thereof | |
| US20110319570A1 (en) | Polyesters with grafted zwitterions | |
| JP7144681B2 (ja) | ポリマーリンカーおよびそれらの使用法 | |
| WO2025064427A1 (en) | Dual-payload antibody-drug conjugates and uses thereof | |
| WO2024056101A9 (zh) | 用于抗体药物偶联物的连接子及其应用 | |
| WO2023158305A1 (en) | Masked il12 protein | |
| CA3026434C (en) | Polymer linkers and their uses | |
| AU2015200291A1 (en) | Polymeric systems for the delivery of anticancer agents | |
| Cateni et al. | PEG–Anticancer Drugs |