JP2018058902A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2018058902A5 JP2018058902A5 JP2018000737A JP2018000737A JP2018058902A5 JP 2018058902 A5 JP2018058902 A5 JP 2018058902A5 JP 2018000737 A JP2018000737 A JP 2018000737A JP 2018000737 A JP2018000737 A JP 2018000737A JP 2018058902 A5 JP2018058902 A5 JP 2018058902A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- independently
- prodrug
- kit according
- 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
- 229940002612 prodrug Drugs 0.000 claims 20
- 239000000651 prodrug Substances 0.000 claims 20
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000003118 aryl group Chemical group 0.000 claims 16
- 229940079593 drug Drugs 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 8
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims 7
- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims 7
- 150000001875 compounds Chemical class 0.000 claims 7
- 150000001993 dienes Chemical class 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 102000004169 proteins and genes Human genes 0.000 claims 5
- 108090000623 proteins and genes Proteins 0.000 claims 5
- -1 CC1065 Chemical compound 0.000 claims 4
- 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 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 108090000765 processed proteins & peptides Proteins 0.000 claims 4
- 239000012190 activator Substances 0.000 claims 3
- 150000001720 carbohydrates Chemical class 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 239000003153 chemical reaction reagent Substances 0.000 claims 3
- 230000000873 masking effect Effects 0.000 claims 3
- 229960004857 mitomycin Drugs 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 229920000642 polymer Polymers 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 230000008685 targeting Effects 0.000 claims 3
- 229960004528 vincristine Drugs 0.000 claims 3
- 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 3
- 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 3
- 108010088751 Albumins Proteins 0.000 claims 2
- 102000009027 Albumins Human genes 0.000 claims 2
- FERIUCNNQQJTOY-UHFFFAOYSA-N Butyric acid Chemical compound CCCC(O)=O FERIUCNNQQJTOY-UHFFFAOYSA-N 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
- UHDGCWIWMRVCDJ-CCXZUQQUSA-N Cytarabine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O1 UHDGCWIWMRVCDJ-CCXZUQQUSA-N 0.000 claims 2
- 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 2
- 229930192392 Mitomycin Natural products 0.000 claims 2
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 2
- 108091034117 Oligonucleotide Proteins 0.000 claims 2
- 229930012538 Paclitaxel Natural products 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- WDLRUFUQRNWCPK-UHFFFAOYSA-N Tetraxetan Chemical compound OC(=O)CN1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1 WDLRUFUQRNWCPK-UHFFFAOYSA-N 0.000 claims 2
- 108010044540 auristatin Proteins 0.000 claims 2
- 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 2
- 229940127093 camptothecin Drugs 0.000 claims 2
- 239000003795 chemical substances by application Substances 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
- 239000012634 fragment Substances 0.000 claims 2
- 230000004927 fusion Effects 0.000 claims 2
- GLVAUDGFNGKCSF-UHFFFAOYSA-N mercaptopurine Chemical compound S=C1NC=NC2=C1NC=N2 GLVAUDGFNGKCSF-UHFFFAOYSA-N 0.000 claims 2
- 229960001592 paclitaxel Drugs 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 239000002534 radiation-sensitizing agent Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 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
- 229940063683 taxotere Drugs 0.000 claims 2
- KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical class CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims 1
- MCEHFIXEKNKSRW-LBPRGKRZSA-N (2s)-2-[[3,5-dichloro-4-[(2,4-diaminopteridin-6-yl)methyl-methylamino]benzoyl]amino]pentanedioic acid Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=C(Cl)C=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1Cl MCEHFIXEKNKSRW-LBPRGKRZSA-N 0.000 claims 1
- 125000001340 2-chloroethyl group Chemical group [H]C([H])(Cl)C([H])([H])* 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- QUHGSDZVAPFNLV-UHFFFAOYSA-N 4-[(5-acetamidofuran-2-carbonyl)amino]-n-[3-(dimethylamino)propyl]-1-propylpyrrole-2-carboxamide Chemical compound C1=C(C(=O)NCCCN(C)C)N(CCC)C=C1NC(=O)C1=CC=C(NC(C)=O)O1 QUHGSDZVAPFNLV-UHFFFAOYSA-N 0.000 claims 1
- TVZGACDUOSZQKY-LBPRGKRZSA-N 4-aminofolic acid Chemical compound C1=NC2=NC(N)=NC(N)=C2N=C1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 TVZGACDUOSZQKY-LBPRGKRZSA-N 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 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
- 108091023037 Aptamer Proteins 0.000 claims 1
- 108010006654 Bleomycin Proteins 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 102000009016 Cholera Toxin Human genes 0.000 claims 1
- 108010049048 Cholera Toxin Proteins 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 108090000695 Cytokines Proteins 0.000 claims 1
- 239000012624 DNA alkylating agent Substances 0.000 claims 1
- 229940126161 DNA alkylating agent Drugs 0.000 claims 1
- 239000012623 DNA damaging agent Substances 0.000 claims 1
- 239000012625 DNA intercalator Substances 0.000 claims 1
- 239000012626 DNA minor groove binder Substances 0.000 claims 1
- 108010092160 Dactinomycin Proteins 0.000 claims 1
- AUGQEEXBDZWUJY-ZLJUKNTDSA-N Diacetoxyscirpenol Chemical compound C([C@]12[C@]3(C)[C@H](OC(C)=O)[C@@H](O)[C@H]1O[C@@H]1C=C(C)CC[C@@]13COC(=O)C)O2 AUGQEEXBDZWUJY-ZLJUKNTDSA-N 0.000 claims 1
- AUGQEEXBDZWUJY-UHFFFAOYSA-N Diacetoxyscirpenol Natural products CC(=O)OCC12CCC(C)=CC1OC1C(O)C(OC(C)=O)C2(C)C11CO1 AUGQEEXBDZWUJY-UHFFFAOYSA-N 0.000 claims 1
- 229940117937 Dihydrofolate reductase inhibitor Drugs 0.000 claims 1
- 102000016607 Diphtheria Toxin Human genes 0.000 claims 1
- 108010053187 Diphtheria Toxin Proteins 0.000 claims 1
- 229930189413 Esperamicin Natural products 0.000 claims 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 1
- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical class OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 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
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 1
- LPGWZGMPDKDHEP-HLTPFJCJSA-N Leurosine Chemical compound C([C@]1([C@@H]2O1)CC)N(CCC=1C3=CC=CC=C3NC=11)C[C@H]2C[C@]1(C(=O)OC)C1=CC([C@]23[C@H]([C@@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC LPGWZGMPDKDHEP-HLTPFJCJSA-N 0.000 claims 1
- LPGWZGMPDKDHEP-GKWAKPNHSA-N Leurosine 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@]6(CC)O[C@@H]6[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C LPGWZGMPDKDHEP-GKWAKPNHSA-N 0.000 claims 1
- 229930126263 Maytansine Natural products 0.000 claims 1
- HYFMSAFINFJTFH-UHFFFAOYSA-N Mitomycin-A Natural products O=C1C(OC)=C(C)C(=O)C2=C1C(COC(N)=O)C1(OC)N2CC2NC21 HYFMSAFINFJTFH-UHFFFAOYSA-N 0.000 claims 1
- FONIWJIDLJEJTL-UHFFFAOYSA-N N(8)-acetylspermidine Chemical compound CC(=O)NCCCCNCCCN FONIWJIDLJEJTL-UHFFFAOYSA-N 0.000 claims 1
- ZAHXYMFVNNUHCP-UHFFFAOYSA-N Naphazoline nitrate Chemical group O[N+]([O-])=O.C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 ZAHXYMFVNNUHCP-UHFFFAOYSA-N 0.000 claims 1
- 108010038807 Oligopeptides Proteins 0.000 claims 1
- 102000015636 Oligopeptides Human genes 0.000 claims 1
- 108010043958 Peptoids Proteins 0.000 claims 1
- 108010039491 Ricin Proteins 0.000 claims 1
- 210000001744 T-lymphocyte Anatomy 0.000 claims 1
- 229940123237 Taxane Drugs 0.000 claims 1
- DPOPAJRDYZGTIR-UHFFFAOYSA-N Tetrazine Chemical compound C1=CN=NN=N1 DPOPAJRDYZGTIR-UHFFFAOYSA-N 0.000 claims 1
- 229940122149 Thymidylate synthase inhibitor Drugs 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
- 241000863480 Vinca Species 0.000 claims 1
- 241000700605 Viruses Species 0.000 claims 1
- 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 1
- 229930183665 actinomycin Natural products 0.000 claims 1
- 125000001931 aliphatic group Chemical group 0.000 claims 1
- SHGAZHPCJJPHSC-YCNIQYBTSA-N all-trans-retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 229960003896 aminopterin Drugs 0.000 claims 1
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 1
- 230000003276 anti-hypertensive effect Effects 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 230000001028 anti-proliverative effect Effects 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 229960001561 bleomycin Drugs 0.000 claims 1
- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 claims 1
- 229930195731 calicheamicin Natural products 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
- 239000013522 chelant Substances 0.000 claims 1
- 229960000684 cytarabine Drugs 0.000 claims 1
- 231100000433 cytotoxic Toxicity 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 239000002254 cytotoxic agent Substances 0.000 claims 1
- 230000001472 cytotoxic effect Effects 0.000 claims 1
- 229960000975 daunorubicin Drugs 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
- 239000000412 dendrimer Substances 0.000 claims 1
- 229920000736 dendritic polymer Polymers 0.000 claims 1
- 230000004069 differentiation Effects 0.000 claims 1
- 239000003166 dihydrofolate reductase inhibitor Substances 0.000 claims 1
- 239000003534 dna topoisomerase inhibitor Substances 0.000 claims 1
- 229930188854 dolastatin Natural products 0.000 claims 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- 229960005501 duocarmycin Drugs 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
- 229930184221 duocarmycin Natural products 0.000 claims 1
- 125000006575 electron-withdrawing group Chemical group 0.000 claims 1
- YJGVMLPVUAXIQN-UHFFFAOYSA-N epipodophyllotoxin Natural products COC1=C(OC)C(OC)=CC(C2C3=CC=4OCOC=4C=C3C(O)C3C2C(OC3)=O)=C1 YJGVMLPVUAXIQN-UHFFFAOYSA-N 0.000 claims 1
- LJQQFQHBKUKHIS-WJHRIEJJSA-N esperamicin Chemical compound O1CC(NC(C)C)C(OC)CC1OC1C(O)C(NOC2OC(C)C(SC)C(O)C2)C(C)OC1OC1C(\C2=C/CSSSC)=C(NC(=O)OC)C(=O)C(OC3OC(C)C(O)C(OC(=O)C=4C(=CC(OC)=C(OC)C=4)NC(=O)C(=C)OC)C3)C2(O)C#C\C=C/C#C1 LJQQFQHBKUKHIS-WJHRIEJJSA-N 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
- 229960000752 etoposide phosphate Drugs 0.000 claims 1
- LIQODXNTTZAGID-OCBXBXKTSA-N etoposide phosphate Chemical compound COC1=C(OP(O)(O)=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 LIQODXNTTZAGID-OCBXBXKTSA-N 0.000 claims 1
- 229960002949 fluorouracil Drugs 0.000 claims 1
- 239000002628 heparin derivative Substances 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 238000003384 imaging method Methods 0.000 claims 1
- 239000002596 immunotoxin Substances 0.000 claims 1
- 231100000608 immunotoxin Toxicity 0.000 claims 1
- 229940051026 immunotoxin Drugs 0.000 claims 1
- 230000002637 immunotoxin Effects 0.000 claims 1
- 239000000411 inducer Substances 0.000 claims 1
- 108700009084 lexitropsin Proteins 0.000 claims 1
- 239000002502 liposome Substances 0.000 claims 1
- WKPWGQKGSOKKOO-RSFHAFMBSA-N maytansine Chemical compound CO[C@@H]([C@@]1(O)C[C@](OC(=O)N1)([C@H]([C@@H]1O[C@@]1(C)[C@@H](OC(=O)[C@H](C)N(C)C(C)=O)CC(=O)N1C)C)[H])\C=C\C=C(C)\CC2=CC(OC)=C(Cl)C1=C2 WKPWGQKGSOKKOO-RSFHAFMBSA-N 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
- 229960001428 mercaptopurine Drugs 0.000 claims 1
- 229960000485 methotrexate Drugs 0.000 claims 1
- HYFMSAFINFJTFH-NGSRAFSJSA-N mitomycin A Chemical compound O=C1C(OC)=C(C)C(=O)C2=C1[C@@H](COC(N)=O)[C@]1(OC)N2C[C@@H]2N[C@@H]21 HYFMSAFINFJTFH-NGSRAFSJSA-N 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 239000002777 nucleoside Substances 0.000 claims 1
- 125000003835 nucleoside group Chemical group 0.000 claims 1
- 229920001542 oligosaccharide Polymers 0.000 claims 1
- 150000002482 oligosaccharides Chemical class 0.000 claims 1
- 239000002245 particle Substances 0.000 claims 1
- 239000000816 peptidomimetic Substances 0.000 claims 1
- 229910052697 platinum Inorganic materials 0.000 claims 1
- 229960001237 podophyllotoxin Drugs 0.000 claims 1
- YJGVMLPVUAXIQN-XVVDYKMHSA-N podophyllotoxin Chemical compound COC1=C(OC)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@H](O)[C@@H]3[C@@H]2C(OC3)=O)=C1 YJGVMLPVUAXIQN-XVVDYKMHSA-N 0.000 claims 1
- YVCVYCSAAZQOJI-UHFFFAOYSA-N podophyllotoxin Natural products COC1=C(O)C(OC)=CC(C2C3=CC=4OCOC=4C=C3C(O)C3C2C(OC3)=O)=C1 YVCVYCSAAZQOJI-UHFFFAOYSA-N 0.000 claims 1
- 229920000575 polymersome Polymers 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- CPNGPNLZQNNVQM-UHFFFAOYSA-N pteridine Chemical compound N1=CN=CC2=NC=CN=C21 CPNGPNLZQNNVQM-UHFFFAOYSA-N 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 229930002330 retinoic acid Natural products 0.000 claims 1
- 239000000523 sample Substances 0.000 claims 1
- 125000006850 spacer group Chemical group 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 239000003734 thymidylate synthase inhibitor Substances 0.000 claims 1
- 229940044693 topoisomerase inhibitor Drugs 0.000 claims 1
- 239000003053 toxin Substances 0.000 claims 1
- 231100000765 toxin Toxicity 0.000 claims 1
- 229960001727 tretinoin Drugs 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
Applications Claiming Priority (16)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP11166241.7 | 2011-05-16 | ||
| EP11166241 | 2011-05-16 | ||
| EP11166942 | 2011-05-20 | ||
| EP11166942.0 | 2011-05-20 | ||
| US201161515432P | 2011-08-05 | 2011-08-05 | |
| US201161515458P | 2011-08-05 | 2011-08-05 | |
| US61/515,458 | 2011-08-05 | ||
| EP11176736.4 | 2011-08-05 | ||
| EP11176736 | 2011-08-05 | ||
| EP11176741.4 | 2011-08-05 | ||
| US61/515,432 | 2011-08-05 | ||
| EP11176741 | 2011-08-05 | ||
| EP11192572.3 | 2011-12-08 | ||
| EP11192572 | 2011-12-08 | ||
| EP11192577.2 | 2011-12-08 | ||
| EP11192577 | 2011-12-08 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016161617A Division JP2017014262A (ja) | 2011-05-16 | 2016-08-22 | 生体直交型薬物活性化 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018058902A JP2018058902A (ja) | 2018-04-12 |
| JP2018058902A5 true JP2018058902A5 (enExample) | 2018-05-31 |
| JP6608467B2 JP6608467B2 (ja) | 2019-11-20 |
Family
ID=47176369
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014510928A Active JP6215194B2 (ja) | 2011-05-16 | 2012-05-16 | 生体直交型薬物活性化 |
| JP2014510929A Active JP5993940B2 (ja) | 2011-05-16 | 2012-05-16 | 生体直交型薬物活性化 |
| JP2014510930A Active JP6482273B2 (ja) | 2011-05-16 | 2012-05-16 | 生体直交型薬物活性化 |
| JP2016161617A Ceased JP2017014262A (ja) | 2011-05-16 | 2016-08-22 | 生体直交型薬物活性化 |
| JP2018000737A Active JP6608467B2 (ja) | 2011-05-16 | 2018-01-05 | 生体直交型薬物活性化 |
Family Applications Before (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014510928A Active JP6215194B2 (ja) | 2011-05-16 | 2012-05-16 | 生体直交型薬物活性化 |
| JP2014510929A Active JP5993940B2 (ja) | 2011-05-16 | 2012-05-16 | 生体直交型薬物活性化 |
| JP2014510930A Active JP6482273B2 (ja) | 2011-05-16 | 2012-05-16 | 生体直交型薬物活性化 |
| JP2016161617A Ceased JP2017014262A (ja) | 2011-05-16 | 2016-08-22 | 生体直交型薬物活性化 |
Country Status (9)
| Country | Link |
|---|---|
| US (8) | US20160151505A1 (enExample) |
| EP (4) | EP2709668A1 (enExample) |
| JP (5) | JP6215194B2 (enExample) |
| CN (4) | CN103732256A (enExample) |
| AU (3) | AU2012257418B2 (enExample) |
| CA (3) | CA2836361C (enExample) |
| DK (1) | DK2709667T3 (enExample) |
| ES (1) | ES2920373T3 (enExample) |
| WO (3) | WO2012156919A1 (enExample) |
Families Citing this family (90)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6215194B2 (ja) * | 2011-05-16 | 2017-10-18 | コーニンクレッカ フィリップス エヌ ヴェＫｏｎｉｎｋｌｉｊｋｅ Ｐｈｉｌｉｐｓ Ｎ．Ｖ． | 生体直交型薬物活性化 |
| US10400280B2 (en) | 2012-08-14 | 2019-09-03 | 10X Genomics, Inc. | Methods and systems for processing polynucleotides |
| US9701998B2 (en) | 2012-12-14 | 2017-07-11 | 10X Genomics, Inc. | Methods and systems for processing polynucleotides |
| US10752949B2 (en) | 2012-08-14 | 2020-08-25 | 10X Genomics, Inc. | Methods and systems for processing polynucleotides |
| US11591637B2 (en) | 2012-08-14 | 2023-02-28 | 10X Genomics, Inc. | Compositions and methods for sample processing |
| US10323279B2 (en) | 2012-08-14 | 2019-06-18 | 10X Genomics, Inc. | Methods and systems for processing polynucleotides |
| CN111748607B (zh) | 2012-08-14 | 2024-04-30 | 10X基因组学有限公司 | 微胶囊组合物及方法 |
| WO2014065860A1 (en) * | 2012-10-24 | 2014-05-01 | The General Hospital Corporation | Functionalized 1,2,4,5-tetrazine compounds for use in bioorthogonal coupling reactions |
| WO2014081300A1 (en) * | 2012-11-22 | 2014-05-30 | Tagworks Pharmaceuticals B.V. | Channel protein activatable liposomes |
| US20150297741A1 (en) * | 2012-11-22 | 2015-10-22 | Tagworks Pharmaceuticals B.V. | Bio-orthogonal drug activation |
| FI2922574T3 (fi) * | 2012-11-22 | 2023-08-11 | Tagworks Pharmaceuticals B V | Kemiallisesti pilkkoutuva ryhmä |
| WO2014081299A1 (en) * | 2012-11-22 | 2014-05-30 | Tagworks Pharmaceuticals B.V. | Activatable liposomes |
| US9580553B2 (en) | 2012-12-07 | 2017-02-28 | University Of Washington Through Its Center For Commercialization | Thermally-activated self-immolative materials |
| US10533221B2 (en) | 2012-12-14 | 2020-01-14 | 10X Genomics, Inc. | Methods and systems for processing polynucleotides |
| WO2014124338A1 (en) | 2013-02-08 | 2014-08-14 | 10X Technologies, Inc. | Polynucleotide barcode generation |
| BR112015022585B1 (pt) | 2013-03-15 | 2023-04-04 | Regeneron Pharmaceuticals, Inc | Composto, composição farmacêutica, conjugado droga-anticorpo, e, uso dos mesmos |
| DK2968495T3 (da) | 2013-03-15 | 2019-10-14 | Daniel J Capon | Hybrid immunoglobulin indeholdende en ikke-peptid-bro |
| US20150087043A1 (en) * | 2013-04-11 | 2015-03-26 | Coferon, Inc | Monomers capable of multimerizing in an aqueous solution that employ bioorthogonal chemistries, and methods of using same |
| CN105611914B (zh) | 2013-06-19 | 2020-09-08 | 加利福尼亚大学董事会 | 局部递送治疗剂的化学构造物 |
| JP6608823B2 (ja) | 2013-08-26 | 2019-11-20 | レゲネロン ファーマシューティカルス，インコーポレーテッド | マクロライドジアステレオマーを含む医薬組成物、その合成方法、及び治療上の使用 |
| CN118146306A (zh) | 2013-09-25 | 2024-06-07 | 西托姆克斯治疗公司 | 基质金属蛋白酶底物和其它可切割部分及其使用方法 |
| JP6835586B2 (ja) * | 2014-01-31 | 2021-02-24 | シトムクス セラピューティクス，インコーポレイティド | マトリプターゼ及びｕ‐プラスミノーゲン活性化因子の基質及び他の切断可能部分、並びにその使用方法 |
| AU2015229186B2 (en) * | 2014-03-14 | 2021-01-28 | Biomolecular Holdings Llc | Hybrid immunoglobulin containing non-peptidyl linkage |
| CN106659796B (zh) | 2014-03-14 | 2021-04-30 | 加利福尼亚大学董事会 | Tco缀合物和治疗剂递送方法 |
| EP3125866B1 (en) * | 2014-04-04 | 2021-03-03 | President and Fellows of Harvard College | Refillable drug delivery devices and methods of use thereof |
| CN113249435B (zh) | 2014-06-26 | 2024-09-03 | 10X基因组学有限公司 | 分析来自单个细胞或细胞群体的核酸的方法 |
| US12312640B2 (en) | 2014-06-26 | 2025-05-27 | 10X Genomics, Inc. | Analysis of nucleic acid sequences |
| AU2015284236B2 (en) | 2014-06-30 | 2018-03-08 | Tva (Abc), Llc | Targeted conjugates and particles and formulations thereof |
| US10179775B2 (en) | 2014-08-11 | 2019-01-15 | The General Hospital Corporation | Cyclooctenes for bioorthogonol reactions |
| CN104356110B (zh) * | 2014-11-19 | 2018-01-23 | 西北大学 | 一种硫诱导3,6‑芳香杂环不对称取代‑1,2,4,5‑四嗪化合物及其合成方法 |
| MA41374A (fr) | 2015-01-20 | 2017-11-28 | Cytomx Therapeutics Inc | Substrats clivables par métalloprotéase matricielle et clivables par sérine protéase et procédés d'utilisation de ceux-ci |
| KR20240142591A (ko) | 2015-03-27 | 2024-09-30 | 리제너론 파아마슈티컬스, 인크. | 메이탄시노이드 유도체, 이의 컨주게이트, 및 사용 방법 |
| US20160331852A1 (en) * | 2015-05-11 | 2016-11-17 | Memorial Sloan Kettering Cancer Center | Radioligands for pretargeted pet imaging and methods of their therapeutic use |
| PT3319959T (pt) | 2015-07-06 | 2021-12-06 | Alkermes Inc | Inibidores hetero-halo de histona desacetilase |
| WO2017007755A1 (en) | 2015-07-06 | 2017-01-12 | Rodin Therapeutics, Inc. | Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase |
| CN117567535A (zh) * | 2015-09-10 | 2024-02-20 | 坦伯公司 | 生物正交组合物 |
| GB201516480D0 (en) | 2015-09-17 | 2015-11-04 | Univ Edinburgh | Tetrazine as a trigger to release caged cargo |
| EP3153155B1 (en) * | 2015-10-08 | 2021-03-03 | President and Fellows of Harvard College | Refillable drug delivery devices and methods of use thereof |
| EP3368546A4 (en) | 2015-10-28 | 2019-06-26 | Tarveda Therapeutics, Inc. | AGAINST SSTR CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF |
| US10875840B2 (en) * | 2015-12-15 | 2020-12-29 | University Of Delaware | Methods for inducing bioorthogonal reactivity |
| AU2017211120C1 (en) | 2016-01-25 | 2021-10-07 | Regeneron Pharmaceuticals, Inc. | Maytansinoid derivatives, conjugates thereof, and methods of use |
| US11690825B2 (en) | 2016-03-09 | 2023-07-04 | Board Of Regents, The University Of Texas System | 20-HETE receptor (GPR75) antagonists and methods of use |
| US10662157B2 (en) | 2016-04-06 | 2020-05-26 | Sumitomo Chemical Company, Limited | Heterocyclic compound |
| WO2018004338A1 (en) | 2016-06-27 | 2018-01-04 | Tagworks Pharmaceuticals B.V. | Cleavable tetrazine used in bio-orthogonal drug activation |
| MX394242B (es) | 2017-01-11 | 2025-03-24 | Rodin Therapeutics Inc | Inhibidores biciclicos de histona desacetilasa |
| EP3385779A1 (en) * | 2017-04-05 | 2018-10-10 | Koninklijke Philips N.V. | Multi-view display device and method |
| ES2983582T3 (es) | 2017-04-07 | 2024-10-23 | Tambo Inc | Composiciones bioortogonales |
| US11560384B2 (en) | 2017-05-04 | 2023-01-24 | University Of Utah Research Foundation | Benzonorbornadiene derivatives and reactions thereof |
| CN107281204A (zh) * | 2017-05-04 | 2017-10-24 | 北京大学 | 一种非对称的1，2，4，5‑四嗪分子的应用 |
| WO2019014549A1 (en) | 2017-07-14 | 2019-01-17 | The Penn State Research Foundation | Compositions and methods for targeted delivery of therapeutic and/or diagnostic species |
| MX2020001484A (es) | 2017-08-07 | 2020-08-20 | Rodin Therapeutics Inc | Inhibidores bicíclicos de la histona desacetilasa. |
| US10837047B2 (en) * | 2017-10-04 | 2020-11-17 | 10X Genomics, Inc. | Compositions, methods, and systems for bead formation using improved polymers |
| US10590244B2 (en) | 2017-10-04 | 2020-03-17 | 10X Genomics, Inc. | Compositions, methods, and systems for bead formation using improved polymers |
| WO2019084323A1 (en) | 2017-10-25 | 2019-05-02 | Georgia State University Research Foundation, Inc. | CHEMICAL RELEASE SYSTEM DELIVERED BY ENRICHMENT |
| CN111051523B (zh) | 2017-11-15 | 2024-03-19 | 10X基因组学有限公司 | 功能化凝胶珠 |
| US10829815B2 (en) | 2017-11-17 | 2020-11-10 | 10X Genomics, Inc. | Methods and systems for associating physical and genetic properties of biological particles |
| CN120365276A (zh) * | 2018-04-11 | 2025-07-25 | 透明医药有限公司 | 靶向化合物及其生产方法 |
| EP3787691A1 (en) | 2018-05-04 | 2021-03-10 | Tagworks Pharmaceuticals B.V. | Tetrazines for high click conjugation yield in vivo and high click release yield |
| US20210308207A1 (en) | 2018-05-04 | 2021-10-07 | Tagworks Pharmaceuticals B.V. | Compounds comprising a linker for increasing transcyclooctene stability |
| WO2019231016A1 (ko) | 2018-05-31 | 2019-12-05 | (주)스파크바이오파마 | 신규한 형광체-테트라진 화합물 및 이의 용도 |
| KR102011772B1 (ko) * | 2018-05-31 | 2019-08-19 | (주)스파크바이오파마 | 신규한 형광체-테트라진 화합물 및 이의 용도 |
| EP3853234B1 (en) | 2018-09-18 | 2025-04-23 | Nikang Therapeutics, Inc. | Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors |
| CN119823023A (zh) | 2018-10-10 | 2025-04-15 | 坦博公司 | 制备官能化环辛烯的工艺 |
| AU2019394972A1 (en) | 2018-12-06 | 2021-06-03 | Cytomx Therapeutics, Inc. | Matrix metalloprotease-cleavable and serine or cysteine protease-cleavable substrates and methods of use thereof |
| EP3893935A4 (en) * | 2018-12-12 | 2022-12-28 | The General Hospital Corporation | PRODRUGS WITH TRIDENTATE SELF-IMMOLATING LINKER |
| CN112010817A (zh) * | 2019-05-31 | 2020-12-01 | 四川大学华西医院 | 一种制备四嗪类化合物的方法及其应用 |
| IL289095A (en) | 2019-06-17 | 2022-02-01 | Tagworks Pharmaceuticals B V | Activating components to cleave labels from biomolecules in vivo |
| JP7784899B2 (ja) * | 2019-06-17 | 2025-12-12 | タグワークス ファーマシューティカルス ビー．ブイ． | 高速で且つ効率的なクリック放出の為の化合物 |
| IL289094A (en) * | 2019-06-17 | 2022-02-01 | Tagworks Pharmaceuticals B V | Tetrazines for increasing the speed and yield of the "click release" reaction |
| CN113321698B (zh) * | 2020-02-28 | 2022-08-23 | 国家纳米科学中心 | 一种单甲基澳瑞他汀e前药及其制备方法和应用 |
| CN113321702B (zh) * | 2020-02-28 | 2022-08-05 | 国家纳米科学中心 | 一种单甲基澳瑞他汀f甲酯前药及其制备方法和应用 |
| CN113354657B (zh) * | 2020-03-05 | 2022-10-21 | 国家纳米科学中心 | 一种Mytoxin A前药及其制备方法和应用 |
| EP3909944A1 (en) * | 2020-05-14 | 2021-11-17 | Rigshospitalet | Nuclide labelled h-tetrazines and use thereof for pet and spect pretargeted imaging and radionuclide therapy |
| EP4295917A3 (en) * | 2020-08-07 | 2024-02-28 | Tambo, Inc. | Trans-cyclooctene bioorthogonal agents and uses in cancer and immunotherapy |
| US20230301988A1 (en) | 2020-08-27 | 2023-09-28 | The Texas A&M University System | Inhibitors of sars cov-2 infection and uses thereof |
| US20240058455A1 (en) * | 2020-10-02 | 2024-02-22 | The General Hospital Corporation | Bioorthogonal linkers and reactions |
| WO2022197877A1 (en) | 2021-03-19 | 2022-09-22 | Genentech, Inc. | Methods and compositions for time delayed bio-orthogonal release of cytotoxic agents |
| CA3226899A1 (en) * | 2021-08-25 | 2023-03-02 | R.P. Scherer Technologies, Llc | Methods of using antibody-drug-conjugates |
| WO2023081809A1 (en) * | 2021-11-05 | 2023-05-11 | Tambo, Inc. | Trans-cyclooctene-modified bispecific antibodies |
| EP4186529B1 (en) * | 2021-11-25 | 2025-07-09 | Veraxa Biotech GmbH | Improved antibody-payload conjugates (apcs) prepared by site-specific conjugation utilizing genetic code expansion |
| IL314951B2 (en) | 2022-02-15 | 2025-07-01 | Tagworks Pharmaceuticals B V | Masked il12 protein |
| CN114652857B (zh) * | 2022-03-31 | 2023-10-20 | 成都大学 | 一种用于修复内皮糖萼受损的靶向药物递送系统及其制备方法 |
| CN115974892B (zh) * | 2022-12-27 | 2023-09-08 | 四川大学华西医院 | 三氮唑四嗪类化合物及其制备方法、应用 |
| CN116370650B (zh) * | 2023-04-14 | 2024-03-22 | 四川大学华西医院 | 基于四嗪连接子的多肽药物偶联物及其制备方法、应用 |
| CN116675664B (zh) * | 2023-04-21 | 2025-06-24 | 苏州大学 | 一种生物正交断键反应体系及前药与应用 |
| WO2025043219A1 (en) * | 2023-08-24 | 2025-02-27 | The Regents Of The University Of California | Methods for uncaging tetrazines |
| US20250243238A1 (en) * | 2024-01-31 | 2025-07-31 | Oregon State University | Tetrazine amino acids and methods for their production and use |
| CN117700394B (zh) * | 2024-02-06 | 2024-05-28 | 南京大学 | 一类可与非张力烯基硼酸快速环加成反应的四嗪类化合物及其生物医药应用 |
| WO2025174248A1 (en) * | 2024-02-16 | 2025-08-21 | Tagworks Pharmaceuticals B.V. | Trans-cyclooctenes with "or gate" release |
| CN117752824A (zh) * | 2024-02-21 | 2024-03-26 | 中国医学科学院医学实验动物研究所 | 预靶向肿瘤免疫探针、生物正交制剂、试剂盒及应用 |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4826964A (en) | 1982-07-20 | 1989-05-02 | Sri International | Bridged oxygen analogs of daunorubcin and doxorubicin |
| US4486414A (en) | 1983-03-21 | 1984-12-04 | Arizona Board Of Reagents | Dolastatins A and B cell growth inhibitory substances |
| US4486444A (en) | 1983-06-20 | 1984-12-04 | Merck & Co., Inc. | (Hydroxybenzoyl)thiophenesulfonamide and acyl derivatives thereof for the topical treatment of elevated intraocular pressure |
| US4879278A (en) | 1989-05-16 | 1989-11-07 | Arizona Board Of Regents | Isolation and structural elucidation of the cytostatic linear depsipeptide dolastatin 15 |
| US4986988A (en) | 1989-05-18 | 1991-01-22 | Arizona Board Of Regents | Isolation and structural elucidation of the cytostatic linear depsipeptides dolastatin 13 and dehydrodolastatin 13 |
| US5138036A (en) | 1989-11-13 | 1992-08-11 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Isolation and structural elucidation of the cytostatic cyclodepsipeptide dolastatin 14 |
| US5198560A (en) | 1990-04-27 | 1993-03-30 | Bristol-Myers Squibb Company | Cytotoxic bicyclo[7.3.1]tridec-4-ene-2,6-diyne compounds and process for the preparation thereof |
| US5635483A (en) | 1992-12-03 | 1997-06-03 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Tumor inhibiting tetrapeptide bearing modified phenethyl amides |
| US6034065A (en) | 1992-12-03 | 2000-03-07 | Arizona Board Of Regents | Elucidation and synthesis of antineoplastic tetrapeptide phenethylamides of dolastatin 10 |
| US5410024A (en) | 1993-01-21 | 1995-04-25 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Human cancer inhibitory pentapeptide amides |
| US5780588A (en) | 1993-01-26 | 1998-07-14 | Arizona Board Of Regents | Elucidation and synthesis of selected pentapeptides |
| US5504191A (en) | 1994-08-01 | 1996-04-02 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Human cancer inhibitory pentapeptide methyl esters |
| US5521284A (en) | 1994-08-01 | 1996-05-28 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Human cancer inhibitory pentapeptide amides and esters |
| US5530097A (en) | 1994-08-01 | 1996-06-25 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Human cancer inhibitory peptide amides |
| US5599902A (en) | 1994-11-10 | 1997-02-04 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Cancer inhibitory peptides |
| US5663149A (en) | 1994-12-13 | 1997-09-02 | Arizona Board Of Regents Acting On Behalf Of Arizona State University | Human cancer inhibitory pentapeptide heterocyclic and halophenyl amides |
| AU702976B2 (en) | 1996-05-03 | 1999-03-11 | Roger S. Cubicciotti | Prodrug compositions and drug delivery methods using synthetic receptors |
| DE69832158T2 (de) | 1997-02-25 | 2006-08-10 | Arizona Board Of Regents, Tempe | Isolierung und strukturelle aufklärung der kryostatischen linearen und cyclo-depsipeptide dolastatin 16, dolastatin 17, und dolastatin 18 |
| US6323315B1 (en) | 1999-09-10 | 2001-11-27 | Basf Aktiengesellschaft | Dolastatin peptides |
| US8236949B2 (en) * | 2007-07-17 | 2012-08-07 | University Of Delaware | Tetrazine-based bio-orthogonal coupling reagents and methods |
| WO2009109998A1 (en) | 2008-03-03 | 2009-09-11 | Lupin Limited | Novel protein tyrosine phosphatase - ib inhibitors |
| EP2361098B1 (en) | 2008-10-31 | 2019-08-28 | The General Hospital Corporation | Compositions and methods for delivering a substance to a biological target |
| GB0906379D0 (en) * | 2009-04-14 | 2009-05-20 | Kencryst Ltd | Reduced sodium salt |
| RU2011146362A (ru) * | 2009-04-16 | 2013-05-27 | Конинклейке Филипс Электроникс Н.В. | Набор для предварительного таргетинга, способ и средства, используемые в нем |
| DK2419142T3 (da) * | 2009-04-16 | 2020-02-10 | Tagworks Pharmaceuticals B V | Præmålretningskit, fremgangsmåde og deri anvendte midler |
| EP2595967B1 (en) | 2010-07-23 | 2016-03-23 | University Of Delaware | Tetrazine-trans-cyclooctene ligation for the rapid construction of radionuclide labeled probes |
| JP6063384B2 (ja) | 2010-10-14 | 2017-01-18 | コーニンクレッカ フィリップス エヌ ヴェＫｏｎｉｎｋｌｉｊｋｅ Ｐｈｉｌｉｐｓ Ｎ．Ｖ． | プレターゲットキット、プレターゲット方法及びその使用試薬 |
| WO2012085789A1 (en) | 2010-12-21 | 2012-06-28 | Koninklijke Philips Electronics N.V. | Agents for clearing biomolecules from circulation |
| EP2522369A1 (en) * | 2011-05-09 | 2012-11-14 | Koninklijke Philips Electronics N.V. | Pretargeting kit, method and agents used therein |
| JP6215194B2 (ja) | 2011-05-16 | 2017-10-18 | コーニンクレッカ フィリップス エヌ ヴェＫｏｎｉｎｋｌｉｊｋｅ Ｐｈｉｌｉｐｓ Ｎ．Ｖ． | 生体直交型薬物活性化 |
| WO2014065860A1 (en) | 2012-10-24 | 2014-05-01 | The General Hospital Corporation | Functionalized 1,2,4,5-tetrazine compounds for use in bioorthogonal coupling reactions |
| US20150297741A1 (en) | 2012-11-22 | 2015-10-22 | Tagworks Pharmaceuticals B.V. | Bio-orthogonal drug activation |
| FI2922574T3 (fi) | 2012-11-22 | 2023-08-11 | Tagworks Pharmaceuticals B V | Kemiallisesti pilkkoutuva ryhmä |
| US10179775B2 (en) | 2014-08-11 | 2019-01-15 | The General Hospital Corporation | Cyclooctenes for bioorthogonol reactions |
| WO2018004338A1 (en) | 2016-06-27 | 2018-01-04 | Tagworks Pharmaceuticals B.V. | Cleavable tetrazine used in bio-orthogonal drug activation |
| EP3787691A1 (en) * | 2018-05-04 | 2021-03-10 | Tagworks Pharmaceuticals B.V. | Tetrazines for high click conjugation yield in vivo and high click release yield |
| US20210308207A1 (en) * | 2018-05-04 | 2021-10-07 | Tagworks Pharmaceuticals B.V. | Compounds comprising a linker for increasing transcyclooctene stability |
| JP7784899B2 (ja) * | 2019-06-17 | 2025-12-12 | タグワークス ファーマシューティカルス ビー．ブイ． | 高速で且つ効率的なクリック放出の為の化合物 |
| IL289095A (en) * | 2019-06-17 | 2022-02-01 | Tagworks Pharmaceuticals B V | Activating components to cleave labels from biomolecules in vivo |
| IL289094A (en) * | 2019-06-17 | 2022-02-01 | Tagworks Pharmaceuticals B V | Tetrazines for increasing the speed and yield of the "click release" reaction |
-
2012
- 2012-05-16 JP JP2014510928A patent/JP6215194B2/ja active Active
- 2012-05-16 EP EP12725516.4A patent/EP2709668A1/en not_active Withdrawn
- 2012-05-16 US US14/117,125 patent/US20160151505A1/en not_active Abandoned
- 2012-05-16 US US14/117,246 patent/US9421274B2/en active Active
- 2012-05-16 EP EP12725515.6A patent/EP2709667B1/en active Active
- 2012-05-16 AU AU2012257418A patent/AU2012257418B2/en active Active
- 2012-05-16 CA CA2836361A patent/CA2836361C/en active Active
- 2012-05-16 AU AU2012257416A patent/AU2012257416B8/en active Active
- 2012-05-16 AU AU2012257417A patent/AU2012257417B2/en active Active
- 2012-05-16 DK DK12725515.6T patent/DK2709667T3/da active
- 2012-05-16 CA CA2836365A patent/CA2836365C/en active Active
- 2012-05-16 ES ES12725515T patent/ES2920373T3/es active Active
- 2012-05-16 JP JP2014510929A patent/JP5993940B2/ja active Active
- 2012-05-16 EP EP21208293.7A patent/EP3973993A1/en active Pending
- 2012-05-16 WO PCT/IB2012/052446 patent/WO2012156919A1/en not_active Ceased
- 2012-05-16 CN CN201280024028.8A patent/CN103732256A/zh active Pending
- 2012-05-16 CN CN201280035091.1A patent/CN103732257A/zh active Pending
- 2012-05-16 CN CN201280035096.4A patent/CN103889459B/zh active Active
- 2012-05-16 US US14/117,655 patent/US9931408B2/en active Active
- 2012-05-16 WO PCT/IB2012/052447 patent/WO2012156920A1/en not_active Ceased
- 2012-05-16 WO PCT/IB2012/052445 patent/WO2012156918A1/en not_active Ceased
- 2012-05-16 JP JP2014510930A patent/JP6482273B2/ja active Active
- 2012-05-16 EP EP12725514.9A patent/EP2709666B1/en active Active
- 2012-05-16 CN CN201810251663.9A patent/CN108524510A/zh active Pending
- 2012-05-16 CA CA2836338A patent/CA2836338C/en active Active
-
2015
- 2015-12-30 US US14/983,858 patent/US10376594B2/en active Active
-
2016
- 2016-08-22 JP JP2016161617A patent/JP2017014262A/ja not_active Ceased
- 2016-11-23 US US15/233,283 patent/US10004810B2/en active Active
-
2018
- 2018-01-05 JP JP2018000737A patent/JP6608467B2/ja active Active
-
2019
- 2019-07-15 US US16/512,038 patent/US10967069B2/en active Active
-
2021
- 2021-02-05 US US17/169,217 patent/US11857636B2/en active Active
-
2023
- 2023-10-30 US US18/497,645 patent/US20240091371A1/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2018058902A5 (enExample) | ||
| JP2014513717A5 (enExample) | ||
| JP6608467B2 (ja) | 生体直交型薬物活性化 | |
| EP3546448B1 (en) | Di-substituted maleic amide linker for antibody-drug conjugating and preparation method and use thereof | |
| US10780179B2 (en) | Conjugates for the treatment of cancer targeted at intracellular tumor-associated antigens | |
| EP3102606B1 (en) | Antibody-drug conjugates and immunotoxins | |
| US10029014B2 (en) | Synthesis of novel asymmetric bow-tie PAMAM dendrimer-based conjugates for tumor-targeting drug delivery | |
| JP2019535731A5 (enExample) | ||
| US20230330258A1 (en) | Conjugates comprising a phosphorus (v) and a drug moiety | |
| JP2016528183A (ja) | ポリペプチドの酵素的結合 | |
| RU2019129839A (ru) | Производные майтанзиноида с саморасщепляющимися пептидными линкерами и их конъюгаты | |
| KR20230088346A (ko) | 용해도 태그가 있는 분자 및 관련 방법들 | |
| JP2019534889A (ja) | 抗体−ポリマー−薬物コンジュゲート | |
| IL308504A (en) | Anti-ror2 antibodies, antibody fragments, their immunoconjugates and uses thereof | |
| FI3773735T3 (fi) | Sytotoksisen lääkkeen konjugaatti ja mainitun konjugaatin aihiolääkemuoto | |
| IL273384B2 (en) | Methods of preventing methionine oxidation in immunoconjugates | |
| US20240269313A1 (en) | Conjugates comprising a phosphorus(v) moiety and a drug | |
| KR20250163875A (ko) | 핵 위치화 폴리펩타이드 및 컨주게이트 및 이의 용도 | |
| McCombs | Exploring the Effects of HSP90 Inhibition on HER2-Directed Antibody Drug Conjugates | |
| KR20250034273A (ko) | 항-도펠 항체-약물 접합체 | |
| JP2025542295A (ja) | リン（ｖ）部分および薬物を含むコンジュゲート | |
| Vlashi | Real time, non-invasive, in vivo imaging of targeted drugs to solid tumors via a high affinity ligand: Implications to improving targeted-drug delivery |