JP2017504606A5 - - Google Patents

Info

Publication number

JP2017504606A5

JP2017504606A5 JP2016541497A JP2016541497A JP2017504606A5 JP 2017504606 A5 JP2017504606 A5 JP 2017504606A5 JP 2016541497 A JP2016541497 A JP 2016541497A JP 2016541497 A JP2016541497 A JP 2016541497A JP 2017504606 A5 JP2017504606 A5 JP 2017504606A5

Authority

JP

Japan

Prior art keywords

antibody

alkyl

alkylene

amino acid

acid sequence

Prior art date

2014-12-16

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

• Espacenet
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• 125000003275 alpha amino acid group Chemical group 0.000 claims 42
• 239000000611 antibody drug conjugate Substances 0.000 claims 41
• 229940049595 antibody-drug conjugate Drugs 0.000 claims 41
• 125000000217 alkyl group Chemical group 0.000 claims 24
• 150000001875 compounds Chemical class 0.000 claims 23
• 229910052739 hydrogen Inorganic materials 0.000 claims 21
• 125000003118 aryl group Chemical group 0.000 claims 20
• 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 19
• 125000001072 heteroaryl group Chemical group 0.000 claims 18
• 125000006832 (C1-C10) alkylene group Chemical group 0.000 claims 16
• 229910052799 carbon Inorganic materials 0.000 claims 14
• 125000002947 alkylene group Chemical group 0.000 claims 11
• 239000003814 drug Substances 0.000 claims 11
• 229940079593 drug Drugs 0.000 claims 11
• 125000004446 heteroarylalkyl group Chemical group 0.000 claims 8
• 239000000126 substance Substances 0.000 claims 8
• 102100038080 B-cell receptor CD22 Human genes 0.000 claims 7
• 101000884305 Homo sapiens B-cell receptor CD22 Proteins 0.000 claims 7
• 101000934338 Homo sapiens Myeloid cell surface antigen CD33 Proteins 0.000 claims 7
• 102100025243 Myeloid cell surface antigen CD33 Human genes 0.000 claims 7
• 125000003710 aryl alkyl group Chemical group 0.000 claims 7
• 125000000753 cycloalkyl group Chemical group 0.000 claims 7
• 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 6
• 101100279855 Arabidopsis thaliana EPFL5 gene Proteins 0.000 claims 6
• 102100026094 C-type lectin domain family 12 member A Human genes 0.000 claims 6
• 101150031358 COLEC10 gene Proteins 0.000 claims 6
• 101100496086 Homo sapiens CLEC12A gene Proteins 0.000 claims 6
• 108090000765 processed proteins & peptides Proteins 0.000 claims 6
• 125000001424 substituent group Chemical group 0.000 claims 6
• 125000006725 C1-C10 alkenyl group Chemical group 0.000 claims 5
• 125000000592 heterocycloalkyl group Chemical group 0.000 claims 5
• 125000006850 spacer group Chemical group 0.000 claims 5
• 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 4
• XTFIVUDBNACUBN-UHFFFAOYSA-N 1,3,5-trinitro-1,3,5-triazinane Chemical compound [O-][N+](=O)N1CN([N+]([O-])=O)CN([N+]([O-])=O)C1 XTFIVUDBNACUBN-UHFFFAOYSA-N 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
• 101150029707 ERBB2 gene Proteins 0.000 claims 4
• 125000004450 alkenylene group Chemical group 0.000 claims 4
• 125000003545 alkoxy group Chemical group 0.000 claims 4
• 125000003282 alkyl amino group Chemical group 0.000 claims 4
• 125000004414 alkyl thio group Chemical group 0.000 claims 4
• 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 4
• -1 cyano, sulfonyl Chemical group 0.000 claims 4
• 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims 4
• 150000002148 esters Chemical class 0.000 claims 4
• 125000005843 halogen group Chemical group 0.000 claims 4
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
• 229910052698 phosphorus Inorganic materials 0.000 claims 4
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
• 229940124530 sulfonamide Drugs 0.000 claims 4
• 150000003456 sulfonamides Chemical class 0.000 claims 4
• 150000003462 sulfoxides Chemical class 0.000 claims 4
• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
• 229910052760 oxygen Inorganic materials 0.000 claims 3
• 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims 2
• 102100025218 B-cell differentiation antigen CD72 Human genes 0.000 claims 2
• 102100024220 CD180 antigen Human genes 0.000 claims 2
• 102100032768 Complement receptor type 2 Human genes 0.000 claims 2
• 102100031511 Fc receptor-like protein 2 Human genes 0.000 claims 2
• 101000934359 Homo sapiens B-cell differentiation antigen CD72 Proteins 0.000 claims 2
• 101000980829 Homo sapiens CD180 antigen Proteins 0.000 claims 2
• 101000941929 Homo sapiens Complement receptor type 2 Proteins 0.000 claims 2
• 101000846911 Homo sapiens Fc receptor-like protein 2 Proteins 0.000 claims 2
• 101000628547 Homo sapiens Metalloreductase STEAP1 Proteins 0.000 claims 2
• 101000628535 Homo sapiens Metalloreductase STEAP2 Proteins 0.000 claims 2
• 101000623901 Homo sapiens Mucin-16 Proteins 0.000 claims 2
• 101001136592 Homo sapiens Prostate stem cell antigen Proteins 0.000 claims 2
• 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 2
• 101000835745 Homo sapiens Teratocarcinoma-derived growth factor 1 Proteins 0.000 claims 2
• 102100026712 Metalloreductase STEAP1 Human genes 0.000 claims 2
• 102100026711 Metalloreductase STEAP2 Human genes 0.000 claims 2
• 102100023123 Mucin-16 Human genes 0.000 claims 2
• NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-N 0.000 claims 2
• 102100036735 Prostate stem cell antigen Human genes 0.000 claims 2
• 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 2
• 102100026404 Teratocarcinoma-derived growth factor 1 Human genes 0.000 claims 2
• 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
• 239000000539 dimer Substances 0.000 claims 2
• 125000005842 heteroatom Chemical group 0.000 claims 2
• 229940127121 immunoconjugate Drugs 0.000 claims 2
• 229920001184 polypeptide Polymers 0.000 claims 2
• 102000004196 processed proteins & peptides Human genes 0.000 claims 2
• 229910052717 sulfur Inorganic materials 0.000 claims 2
• RZRJACCZWZTYJY-UHFFFAOYSA-N tert-butylsulfanyl n,n-dimethylcarbamodithioate Chemical compound CN(C)C(=S)SSC(C)(C)C RZRJACCZWZTYJY-UHFFFAOYSA-N 0.000 claims 2
• FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 1
• STQGQHZAVUOBTE-UHFFFAOYSA-N 7-Cyan-hept-2t-en-4,6-diinsaeure Natural products C1=2C(O)=C3C(=O)C=4C(OC)=CC=CC=4C(=O)C3=C(O)C=2CC(O)(C(C)=O)CC1OC1CC(N)C(O)C(C)O1 STQGQHZAVUOBTE-UHFFFAOYSA-N 0.000 claims 1
• 102100020998 Aspartate beta-hydroxylase domain-containing protein 1 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
• 102100031517 Fc receptor-like protein 1 Human genes 0.000 claims 1
• 101710120224 Fc receptor-like protein 1 Proteins 0.000 claims 1
• 102100031507 Fc receptor-like protein 5 Human genes 0.000 claims 1
• 102100031546 HLA class II histocompatibility antigen, DO beta chain Human genes 0.000 claims 1
• 101000783987 Homo sapiens Aspartate beta-hydroxylase domain-containing protein 1 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
• 101000846908 Homo sapiens Fc receptor-like protein 5 Proteins 0.000 claims 1
• 101000866281 Homo sapiens HLA class II histocompatibility antigen, DO beta chain Proteins 0.000 claims 1
• 101001091205 Homo sapiens KiSS-1 receptor Proteins 0.000 claims 1
• 101001063456 Homo sapiens Leucine-rich repeat-containing G-protein coupled receptor 5 Proteins 0.000 claims 1
• 101001065550 Homo sapiens Lymphocyte antigen 6K Proteins 0.000 claims 1
• 101000620359 Homo sapiens Melanocyte protein PMEL Proteins 0.000 claims 1
• 101000829779 Homo sapiens Probable G-protein coupled receptor 19 Proteins 0.000 claims 1
• 101000825475 Homo sapiens Protein shisa-2 homolog Proteins 0.000 claims 1
• 101000853730 Homo sapiens RING finger and transmembrane domain-containing protein 2 Proteins 0.000 claims 1
• 101000713169 Homo sapiens Solute carrier family 52, riboflavin transporter, member 2 Proteins 0.000 claims 1
• 101000834937 Homo sapiens Tomoregulin-1 Proteins 0.000 claims 1
• 101000834948 Homo sapiens Tomoregulin-2 Proteins 0.000 claims 1
• 102100034845 KiSS-1 receptor Human genes 0.000 claims 1
• 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 1
• 102100031036 Leucine-rich repeat-containing G-protein coupled receptor 5 Human genes 0.000 claims 1
• 102100032129 Lymphocyte antigen 6K Human genes 0.000 claims 1
• 102100022430 Melanocyte protein PMEL Human genes 0.000 claims 1
• 101100042271 Mus musculus Sema3b gene Proteins 0.000 claims 1
• 102100037603 P2X purinoceptor 5 Human genes 0.000 claims 1
• 101710189969 P2X purinoceptor 5 Proteins 0.000 claims 1
• 102100023417 Probable G-protein coupled receptor 19 Human genes 0.000 claims 1
• 102100022938 Protein shisa-2 homolog Human genes 0.000 claims 1
• 102100035928 RING finger and transmembrane domain-containing protein 2 Human genes 0.000 claims 1
• 102100036862 Solute carrier family 52, riboflavin transporter, member 2 Human genes 0.000 claims 1
• 102100026159 Tomoregulin-1 Human genes 0.000 claims 1
• 102100026160 Tomoregulin-2 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
• 102000003425 Tyrosinase Human genes 0.000 claims 1
• 108060008724 Tyrosinase Proteins 0.000 claims 1
• JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims 1
• 229940009456 adriamycin Drugs 0.000 claims 1
• 125000003342 alkenyl group Chemical group 0.000 claims 1
• 239000003242 anti bacterial agent Substances 0.000 claims 1
• 239000002246 antineoplastic agent Substances 0.000 claims 1
• 230000003115 biocidal effect Effects 0.000 claims 1
• JCKYGMPEJWAADB-UHFFFAOYSA-N chlorambucil Chemical compound OC(=O)CCCC1=CC=C(N(CCCl)CCCl)C=C1 JCKYGMPEJWAADB-UHFFFAOYSA-N 0.000 claims 1
• 229960004630 chlorambucil Drugs 0.000 claims 1
• 239000000562 conjugate Substances 0.000 claims 1
• 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
• 235000018417 cysteine Nutrition 0.000 claims 1
• XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 1
• STQGQHZAVUOBTE-VGBVRHCVSA-N daunorubicin 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(C)=O)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 STQGQHZAVUOBTE-VGBVRHCVSA-N 0.000 claims 1
• 229960000975 daunorubicin Drugs 0.000 claims 1
• 201000010099 disease Diseases 0.000 claims 1
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
• 229960004679 doxorubicin Drugs 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 VJJPUSNTGOMMGY-MRVIYFEKSA-N 0.000 claims 1
• 229960005420 etoposide Drugs 0.000 claims 1
• 125000005647 linker group Chemical group 0.000 claims 1
• SGDBTWWWUNNDEQ-LBPRGKRZSA-N melphalan Chemical compound OC(=O)[C@@H](N)CC1=CC=C(N(CCCl)CCCl)C=C1 SGDBTWWWUNNDEQ-LBPRGKRZSA-N 0.000 claims 1
• 229960001924 melphalan Drugs 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1
• 229960000485 methotrexate Drugs 0.000 claims 1
• 229960004857 mitomycin Drugs 0.000 claims 1
• 229910052757 nitrogen Inorganic materials 0.000 claims 1
• UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical group [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 1
• 239000000816 peptidomimetic Substances 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 229960003048 vinblastine Drugs 0.000 claims 1
• JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 claims 1
• 229960004528 vincristine Drugs 0.000 claims 1
• OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims 1
• OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims 1