JP2016521707A5 - - Google Patents

Info

Publication number

JP2016521707A5

JP2016521707A5 JP2016517967A JP2016517967A JP2016521707A5 JP 2016521707 A5 JP2016521707 A5 JP 2016521707A5 JP 2016517967 A JP2016517967 A JP 2016517967A JP 2016517967 A JP2016517967 A JP 2016517967A JP 2016521707 A5 JP2016521707 A5 JP 2016521707A5

Authority

JP

Japan

Prior art keywords

activatable antibody

target

seq

activatable

optionally

Prior art date

2014-06-04

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
• Global Dossier
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• 238000000034 method Methods 0.000 claims 22
• 108090000765 processed proteins & peptides Proteins 0.000 claims 17
• 150000001413 amino acids Chemical group 0.000 claims 12
• 239000003795 chemical substances by application Substances 0.000 claims 10
• 229920001184 polypeptide Polymers 0.000 claims 10
• 102000004196 processed proteins & peptides Human genes 0.000 claims 10
• 108091005804 Peptidases Proteins 0.000 claims 9
• 239000004365 Protease Substances 0.000 claims 9
• 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 claims 9
• 239000012634 fragment Substances 0.000 claims 7
• 235000001014 amino acid Nutrition 0.000 claims 6
• 239000002131 composite material Substances 0.000 claims 6
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
• BLUGYPPOFIHFJS-UUFHNPECSA-N (2s)-n-[(2s)-1-[[(3r,4s,5s)-3-methoxy-1-[(2s)-2-[(1r,2r)-1-methoxy-2-methyl-3-oxo-3-[[(1s)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]-3-methyl-2-(methylamino)butanamid Chemical compound CN[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C=1SC=CN=1)CC1=CC=CC=C1 BLUGYPPOFIHFJS-UUFHNPECSA-N 0.000 claims 5
• 102000004190 Enzymes Human genes 0.000 claims 4
• 108090000790 Enzymes Proteins 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
• 238000010494 dissociation reaction Methods 0.000 claims 4
• 230000005593 dissociations Effects 0.000 claims 4
• 125000006850 spacer group Chemical group 0.000 claims 4
• 239000000758 substrate Substances 0.000 claims 4
• 108010075254 C-Peptide Proteins 0.000 claims 3
• 201000010099 disease Diseases 0.000 claims 3
• 208000035475 disorder Diseases 0.000 claims 3
• JARGNLJYKBUKSJ-KGZKBUQUSA-N (2r)-2-amino-5-[[(2r)-1-(carboxymethylamino)-3-hydroxy-1-oxopropan-2-yl]amino]-5-oxopentanoic acid;hydrobromide Chemical compound Br.OC(=O)[C@H](N)CCC(=O)N[C@H](CO)C(=O)NCC(O)=O JARGNLJYKBUKSJ-KGZKBUQUSA-N 0.000 claims 2
• 102000001706 Immunoglobulin Fab Fragments Human genes 0.000 claims 2
• 108010054477 Immunoglobulin Fab Fragments Proteins 0.000 claims 2
• 206010039509 Scab Diseases 0.000 claims 2
• IEDXPSOJFSVCKU-HOKPPMCLSA-N [4-[[(2S)-5-(carbamoylamino)-2-[[(2S)-2-[6-(2,5-dioxopyrrolidin-1-yl)hexanoylamino]-3-methylbutanoyl]amino]pentanoyl]amino]phenyl]methyl N-[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-N-methylcarbamate Chemical compound CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCc1ccc(NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](NC(=O)CCCCCN2C(=O)CCC2=O)C(C)C)cc1)C(C)C IEDXPSOJFSVCKU-HOKPPMCLSA-N 0.000 claims 2
• 239000003638 chemical reducing agent Substances 0.000 claims 2
• 108010044804 gamma-glutamyl-seryl-glycine Proteins 0.000 claims 2
• RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 claims 2
• 108700026078 glutathione trisulfide Proteins 0.000 claims 2
• 230000000873 masking effect Effects 0.000 claims 2
• 108010093470 monomethyl auristatin E Proteins 0.000 claims 2
• 210000001519 tissue Anatomy 0.000 claims 2
• WOWDZACBATWTAU-FEFUEGSOSA-N (2s)-2-[[(2s)-2-(dimethylamino)-3-methylbutanoyl]amino]-n-[(3r,4s,5s)-1-[(2s)-2-[(1r,2r)-3-[[(1s,2r)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-n,3-dimethylbutanamide Chemical compound CC(C)[C@H](N(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)C1=CC=CC=C1 WOWDZACBATWTAU-FEFUEGSOSA-N 0.000 claims 1
• 208000023275 Autoimmune disease Diseases 0.000 claims 1
• 108010024636 Glutathione Proteins 0.000 claims 1
• XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 1
• 206010028980 Neoplasm Diseases 0.000 claims 1
• PZBFGYYEXUXCOF-UHFFFAOYSA-N TCEP Chemical group OC(=O)CCP(CCC(O)=O)CCC(O)=O PZBFGYYEXUXCOF-UHFFFAOYSA-N 0.000 claims 1
• 108010044540 auristatin Proteins 0.000 claims 1
• 210000004899 c-terminal region Anatomy 0.000 claims 1
• 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 1
• 229930195731 calicheamicin Natural products 0.000 claims 1
• 201000011510 cancer Diseases 0.000 claims 1
• 230000000536 complexating effect Effects 0.000 claims 1
• 150000001875 compounds Chemical class 0.000 claims 1
• 230000001268 conjugating effect Effects 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
• 229940039227 diagnostic agent Drugs 0.000 claims 1
• 239000000032 diagnostic agent Substances 0.000 claims 1
• AMRJKAQTDDKMCE-UHFFFAOYSA-N dolastatin Chemical compound CC(C)C(N(C)C)C(=O)NC(C(C)C)C(=O)N(C)C(C(C)C)C(OC)CC(=O)N1CCCC1C(OC)C(C)C(=O)NC(C=1SC=CN=1)CC1=CC=CC=C1 AMRJKAQTDDKMCE-UHFFFAOYSA-N 0.000 claims 1
• 229930188854 dolastatin Natural products 0.000 claims 1
• 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 1
• 229960005501 duocarmycin Drugs 0.000 claims 1
• 229930184221 duocarmycin Natural products 0.000 claims 1
• 230000000694 effects Effects 0.000 claims 1
• 229960003180 glutathione Drugs 0.000 claims 1
• 208000027866 inflammatory disease Diseases 0.000 claims 1
• 230000002452 interceptive effect Effects 0.000 claims 1
• 231100000782 microtubule inhibitor Toxicity 0.000 claims 1
• 102000039446 nucleic acids Human genes 0.000 claims 1
• 108020004707 nucleic acids Proteins 0.000 claims 1
• 150000007523 nucleic acids Chemical class 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 150000003573 thiols Chemical class 0.000 claims 1
• 231100000765 toxin Toxicity 0.000 claims 1
• 239000003053 toxin Substances 0.000 claims 1