JP2017519753A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2017519753A5 JP2017519753A5 JP2016572687A JP2016572687A JP2017519753A5 JP 2017519753 A5 JP2017519753 A5 JP 2017519753A5 JP 2016572687 A JP2016572687 A JP 2016572687A JP 2016572687 A JP2016572687 A JP 2016572687A JP 2017519753 A5 JP2017519753 A5 JP 2017519753A5
- Authority
- JP
- Japan
- Prior art keywords
- prodrug
- fap
- drug
- cytotoxic
- cleavage
- 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 31
- 239000000651 prodrug Substances 0.000 claims 31
- 229940079593 drug Drugs 0.000 claims 22
- 239000003814 drug Substances 0.000 claims 22
- 238000003776 cleavage reaction Methods 0.000 claims 11
- 231100000433 cytotoxic Toxicity 0.000 claims 11
- 230000001472 cytotoxic effect Effects 0.000 claims 11
- 230000007017 scission Effects 0.000 claims 11
- 150000001875 compounds Chemical class 0.000 claims 10
- 239000000824 cytostatic agent Substances 0.000 claims 9
- 230000001085 cytostatic effect Effects 0.000 claims 9
- 239000000758 substrate Substances 0.000 claims 9
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 230000003827 upregulation Effects 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 102000056251 Prolyl Oligopeptidases Human genes 0.000 claims 4
- -1 biscartamide Chemical compound 0.000 claims 4
- 241000282326 Felis catus Species 0.000 claims 3
- 108010038807 Oligopeptides Proteins 0.000 claims 3
- 102000015636 Oligopeptides Human genes 0.000 claims 3
- 230000004913 activation Effects 0.000 claims 3
- 210000002950 fibroblast Anatomy 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 125000001165 hydrophobic group Chemical group 0.000 claims 3
- 235000018102 proteins Nutrition 0.000 claims 3
- 102000004169 proteins and genes Human genes 0.000 claims 3
- 108090000623 proteins and genes Proteins 0.000 claims 3
- 210000002536 stromal cell Anatomy 0.000 claims 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 2
- PAYRUJLWNCNPSJ-UHFFFAOYSA-N Aniline Chemical compound NC1=CC=CC=C1 PAYRUJLWNCNPSJ-UHFFFAOYSA-N 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- FRJIAZKQGSCKPQ-FSPLSTOPSA-N His-Ala Chemical group OC(=O)[C@H](C)NC(=O)[C@@H](N)CC1=CN=CN1 FRJIAZKQGSCKPQ-FSPLSTOPSA-N 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 102100037838 Prolyl endopeptidase Human genes 0.000 claims 2
- 101710178372 Prolyl endopeptidase Proteins 0.000 claims 2
- 229940100198 alkylating agent Drugs 0.000 claims 2
- 239000002168 alkylating agent Substances 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 230000001461 cytolytic effect Effects 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 230000004761 fibrosis Effects 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 108010040030 histidinoalanine Proteins 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 231100000682 maximum tolerated dose Toxicity 0.000 claims 2
- 230000035699 permeability Effects 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 231100001274 therapeutic index Toxicity 0.000 claims 2
- QVMPZNRFXAKISM-UHFFFAOYSA-N tirapazamine Chemical compound C1=CC=C2[N+]([O-])=NC(=N)N(O)C2=C1 QVMPZNRFXAKISM-UHFFFAOYSA-N 0.000 claims 2
- 229950002376 tirapazamine Drugs 0.000 claims 2
- 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
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 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
- NMUSYJAQQFHJEW-UHFFFAOYSA-N 5-Azacytidine Natural products O=C1N=C(N)N=CN1C1C(O)C(O)C(CO)O1 NMUSYJAQQFHJEW-UHFFFAOYSA-N 0.000 claims 1
- NMUSYJAQQFHJEW-KVTDHHQDSA-N 5-azacytidine Chemical compound O=C1N=C(N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 NMUSYJAQQFHJEW-KVTDHHQDSA-N 0.000 claims 1
- 108010006654 Bleomycin Proteins 0.000 claims 1
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims 1
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 claims 1
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 claims 1
- 102000004190 Enzymes Human genes 0.000 claims 1
- 108090000790 Enzymes Proteins 0.000 claims 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-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
- 229930192392 Mitomycin Natural products 0.000 claims 1
- 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 1
- 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 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 1
- 229940123237 Taxane 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
- ZYJKONDZYOWOHE-UHFFFAOYSA-N [4-amino-3-(hydroxymethyl)phenyl]methanol Chemical compound NC1=CC=C(CO)C=C1CO ZYJKONDZYOWOHE-UHFFFAOYSA-N 0.000 claims 1
- 125000003275 alpha amino acid group Chemical group 0.000 claims 1
- 229960003896 aminopterin Drugs 0.000 claims 1
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 1
- 230000002280 anti-androgenic effect Effects 0.000 claims 1
- 230000003432 anti-folate effect Effects 0.000 claims 1
- 239000000051 antiandrogen Substances 0.000 claims 1
- 229940127074 antifolate Drugs 0.000 claims 1
- 229940041181 antineoplastic drug Drugs 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 229960002756 azacitidine Drugs 0.000 claims 1
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims 1
- XJHABGPPCLHLLV-UHFFFAOYSA-N benzo[de]isoquinoline-1,3-dione Chemical compound C1=CC(C(=O)NC2=O)=C3C2=CC=CC3=C1 XJHABGPPCLHLLV-UHFFFAOYSA-N 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
- 230000000903 blocking effect Effects 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical group OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 claims 1
- 229960004562 carboplatin Drugs 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 1
- 229960004397 cyclophosphamide Drugs 0.000 claims 1
- 229960000978 cyproterone acetate Drugs 0.000 claims 1
- UWFYSQMTEOIJJG-FDTZYFLXSA-N cyproterone acetate Chemical compound C1=C(Cl)C2=CC(=O)[C@@H]3C[C@@H]3[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 UWFYSQMTEOIJJG-FDTZYFLXSA-N 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 239000002254 cytotoxic agent Substances 0.000 claims 1
- 239000003534 dna topoisomerase inhibitor Substances 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 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
- 229960005420 etoposide Drugs 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
- 229960002949 fluorouracil Drugs 0.000 claims 1
- 229960002074 flutamide Drugs 0.000 claims 1
- MKXKFYHWDHIYRV-UHFFFAOYSA-N flutamide Chemical compound CC(C)C(=O)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 MKXKFYHWDHIYRV-UHFFFAOYSA-N 0.000 claims 1
- 239000004052 folic acid antagonist Substances 0.000 claims 1
- 150000002224 folic acids Chemical class 0.000 claims 1
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 1
- 229960005277 gemcitabine Drugs 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 229960001101 ifosfamide Drugs 0.000 claims 1
- HOMGKSMUEGBAAB-UHFFFAOYSA-N ifosfamide Chemical compound ClCCNP1(=O)OCCCN1CCCl HOMGKSMUEGBAAB-UHFFFAOYSA-N 0.000 claims 1
- 229960004768 irinotecan Drugs 0.000 claims 1
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims 1
- 229960004961 mechlorethamine Drugs 0.000 claims 1
- HAWPXGHAZFHHAD-UHFFFAOYSA-N mechlorethamine Chemical compound ClCCN(C)CCCl HAWPXGHAZFHHAD-UHFFFAOYSA-N 0.000 claims 1
- 229960001924 melphalan Drugs 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
- 229960000485 methotrexate Drugs 0.000 claims 1
- 229960004857 mitomycin Drugs 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 229960002653 nilutamide Drugs 0.000 claims 1
- XWXYUMMDTVBTOU-UHFFFAOYSA-N nilutamide Chemical compound O=C1C(C)(C)NC(=O)N1C1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 XWXYUMMDTVBTOU-UHFFFAOYSA-N 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 239000002777 nucleoside Substances 0.000 claims 1
- 150000003833 nucleoside derivatives Chemical class 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 229960001592 paclitaxel Drugs 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
- 125000001500 prolyl group Chemical group [H]N1C([H])(C(=O)[*])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- CPNGPNLZQNNVQM-UHFFFAOYSA-N pteridine Chemical compound N1=CN=CC2=NC=CN=C21 CPNGPNLZQNNVQM-UHFFFAOYSA-N 0.000 claims 1
- 239000002534 radiation-sensitizing agent Substances 0.000 claims 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 claims 1
- 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 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 229940044693 topoisomerase inhibitor Drugs 0.000 claims 1
- 229960000303 topotecan Drugs 0.000 claims 1
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims 1
- 210000004881 tumor cell Anatomy 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
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462011989P | 2014-06-13 | 2014-06-13 | |
| US62/011,989 | 2014-06-13 | ||
| US201462051033P | 2014-09-16 | 2014-09-16 | |
| US62/051,033 | 2014-09-16 | ||
| PCT/US2015/035798 WO2015192123A1 (en) | 2014-06-13 | 2015-06-15 | Fap-activated therapeutic agents, and uses related thereto |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020130483A Division JP7093912B2 (ja) | 2014-06-13 | 2020-07-31 | Ｆａｐ活性化治療剤及びそれに関連する使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017519753A JP2017519753A (ja) | 2017-07-20 |
| JP2017519753A5 true JP2017519753A5 (enExample) | 2018-02-01 |
| JP6744826B2 JP6744826B2 (ja) | 2020-08-19 |
Family
ID=54834485
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016572687A Expired - Fee Related JP6744826B2 (ja) | 2014-06-13 | 2015-06-15 | Ｆａｐ活性化治療剤及びそれに関連する使用 |
| JP2020130483A Active JP7093912B2 (ja) | 2014-06-13 | 2020-07-31 | Ｆａｐ活性化治療剤及びそれに関連する使用 |
| JP2022086532A Active JP7530111B2 (ja) | 2014-06-13 | 2022-05-27 | Ｆａｐ活性化治療剤及びそれに関連する使用 |
| JP2024115840A Pending JP2024150608A (ja) | 2014-06-13 | 2024-07-19 | Ｆａｐ活性化治療剤及びそれに関連する使用 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020130483A Active JP7093912B2 (ja) | 2014-06-13 | 2020-07-31 | Ｆａｐ活性化治療剤及びそれに関連する使用 |
| JP2022086532A Active JP7530111B2 (ja) | 2014-06-13 | 2022-05-27 | Ｆａｐ活性化治療剤及びそれに関連する使用 |
| JP2024115840A Pending JP2024150608A (ja) | 2014-06-13 | 2024-07-19 | Ｆａｐ活性化治療剤及びそれに関連する使用 |
Country Status (15)
| Country | Link |
|---|---|
| US (6) | US10245248B2 (enExample) |
| EP (2) | EP3154594B1 (enExample) |
| JP (4) | JP6744826B2 (enExample) |
| CN (4) | CN113786495A (enExample) |
| CA (1) | CA2952051C (enExample) |
| DK (1) | DK3154594T3 (enExample) |
| ES (1) | ES2951596T3 (enExample) |
| FI (1) | FI3154594T3 (enExample) |
| HR (1) | HRP20230854T1 (enExample) |
| HU (1) | HUE063194T2 (enExample) |
| IL (3) | IL291922B2 (enExample) |
| PL (1) | PL3154594T3 (enExample) |
| PT (1) | PT3154594T (enExample) |
| SI (1) | SI3154594T1 (enExample) |
| WO (1) | WO2015192123A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015192123A1 (en) | 2014-06-13 | 2015-12-17 | Trustees Of Tufts College | Fap-activated therapeutic agents, and uses related thereto |
| US9737556B2 (en) | 2014-06-13 | 2017-08-22 | Trustees Of Tufts College | FAP-activated therapeutic agents, and uses related thereto |
| WO2017189569A1 (en) * | 2016-04-25 | 2017-11-02 | Trustees Of Tufts College | Multimediator dpp4 and fap inhibitors, and uses related thereto |
| AU2017348322B8 (en) | 2016-10-28 | 2021-12-23 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating EZH2-mediated cancer |
| AU2017370694A1 (en) | 2016-12-08 | 2019-07-25 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating CDK4/6-mediated cancer |
| US20200237936A1 (en) | 2016-12-14 | 2020-07-30 | Purdue Research Foundation | Fibroblast activation protein (fap)-targeted imaging and therapy |
| DK3391914T3 (da) * | 2017-04-21 | 2021-10-18 | Safe Implant Tech Aps | Guldpartikler til anvendelse i terapi til at forebygge eller mindske kapselkontraktur |
| GB201710973D0 (en) | 2017-07-07 | 2017-08-23 | Avacta Life Sciences Ltd | Scaffold proteins |
| WO2019154859A1 (en) * | 2018-02-06 | 2019-08-15 | Universität Heidelberg | Fap inhibitor |
| WO2019173516A1 (en) | 2018-03-06 | 2019-09-12 | Icahn School Of Medicine At Mount Sinai | Serine threonine kinase (akt) degradation / disruption compounds and methods of use |
| CN108864250A (zh) * | 2018-05-29 | 2018-11-23 | 北京大学 | 一种FAPα酶敏感的吉西他滨前体药物及其制备方法和应用 |
| US20210353652A1 (en) * | 2018-06-04 | 2021-11-18 | Trustees Of Tufts College | Tumor microenvironment-activated drug-binder conjugates, and uses related thereto |
| CA3104298A1 (en) | 2018-06-21 | 2019-12-26 | Icahn School Of Medicine At Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| EP3867648A4 (en) * | 2018-10-17 | 2022-06-22 | Purdue Research Foundation | FIBROBLAST ACTIVATING PROTEIN (FAP) TARGETED IMAGING AND FIBROSIS THERAPY |
| AU2020270908B2 (en) * | 2019-04-09 | 2025-09-25 | Beth Israel Deaconess Medical Center, Inc. | Degradation of AKT by conjugation of ATP-competitive AKT inhibitor GDC-0068 with E3 ligase ligands and methods of use |
| US12465648B2 (en) | 2019-05-06 | 2025-11-11 | Icahn School Of Medicine At Mount Sinai | Heterobifunctional compounds as degraders of HPK1 |
| AU2020316435A1 (en) * | 2019-07-22 | 2022-03-03 | Purdue Research Foundation | Multivalent fibroblast-targeted agents and methods of use |
| JP7638664B2 (ja) | 2020-01-31 | 2025-03-04 | キヤノン株式会社 | 光電変換装置、光電変換システム、および移動体 |
| CN111233955B (zh) * | 2020-02-28 | 2022-06-10 | 南京缘聚医药科技有限公司 | 一类噻唑酮甲酰胞嘧啶衍生物及其药物用途 |
| US12103924B2 (en) | 2020-06-01 | 2024-10-01 | Icahn School Of Medicine At Mount Sinai | Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use |
| WO2022026729A1 (en) * | 2020-07-31 | 2022-02-03 | The Johns Hopkins University | Fap-activated compounds for treatment of cancer |
| WO2022094237A1 (en) * | 2020-10-30 | 2022-05-05 | Avacta Life Sciences Limited | Enzyme activated serum extended half-life therapeutic conjugates |
| EP4237012A1 (en) * | 2020-10-30 | 2023-09-06 | Avacta Life Sciences Limited | Fap-activated serum extended half-life therapeutic conjugates |
| CN116981479A (zh) * | 2020-12-17 | 2023-10-31 | 塔夫茨大学信托人 | Fap激活的放射治疗诊断法以及与之相关的用途 |
| JP2024510267A (ja) * | 2021-03-16 | 2024-03-06 | パーデュー・リサーチ・ファウンデーション | 線維芽細胞活性化タンパク質を標的とする化合物、およびその使用方法 |
| CN113018450B (zh) * | 2021-05-24 | 2021-08-06 | 潍坊中医药产业技术研究院 | 一种具有肿瘤细胞和肿瘤相关成纤维细胞双靶向功能的药物载体、制备方法及应用 |
| CN113845563B (zh) * | 2021-09-28 | 2024-02-20 | 遵义医药高等专科学校 | 一种FAPα酶激活式鬼臼毒素衍生物及其制备方法与应用 |
| JP2025521779A (ja) | 2022-07-05 | 2025-07-10 | ゾウネック、アレックス | 多段階化学療法用のプロドラッグキット |
| EP4615521A1 (en) * | 2022-11-09 | 2025-09-17 | Purdue Research Foundation | Keto-amide-based fibroblast activation protein-targeted ligand linked to an imaging or therapeutic agent, compositions and methods of use |
| WO2025159301A1 (ko) * | 2024-01-24 | 2025-07-31 | 서울대학교산학협력단 | 섬유아세포 활성화 단백질에 의해 활성화되는 프로드러그 화합물 |
| WO2025259682A1 (en) * | 2024-06-10 | 2025-12-18 | Trustees Of Tufts College | Enzyme-activated prodrugs with small molecule-mediated extended serum half-life |
| WO2026002988A1 (en) | 2024-06-24 | 2026-01-02 | Avacta Life Sciences Limited | Fibroblast activation protein alpha binder proteins |
| WO2026074156A1 (en) * | 2024-10-04 | 2026-04-09 | Avacta Life Sciences Limited | Fap-activated camptothecin conjugates and uses thereof |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3719667A (en) | 1970-08-24 | 1973-03-06 | Lilly Co Eli | Epimerization of 6-acylamido and 6-imido penicillin sulfoxide esters |
| US3840556A (en) | 1971-05-28 | 1974-10-08 | Lilly Co Eli | Penicillin conversion by halogen electrophiles and anti-bacterials derived thereby |
| NO812612L (no) | 1980-08-06 | 1982-02-08 | Ferring Pharma Ltd | Enzym-inhibitorer. |
| US5433955A (en) | 1989-01-23 | 1995-07-18 | Akzo N.V. | Site specific in vivo activation of therapeutic drugs |
| NZ241954A (en) | 1991-03-15 | 1994-01-26 | Amgen Inc | Compositions of g-csf for pulmonary administration. |
| GB9309663D0 (en) | 1993-05-11 | 1993-06-23 | Erba Carlo Spa | Biologically active compounds |
| US5451569A (en) | 1994-04-19 | 1995-09-19 | Hong Kong University Of Science And Technology R & D Corporation Limited | Pulmonary drug delivery system |
| US5767242A (en) | 1994-04-20 | 1998-06-16 | Boehringer Ingelheim Int'l Gmbh | Isolated dimeric fibroblast activation protein alpha, and uses thereof |
| CA2324226C (en) | 1998-03-19 | 2012-06-05 | Vertex Pharmaceuticals Incorporated | Inhibitors of caspases |
| US6613879B1 (en) | 1999-05-14 | 2003-09-02 | Boehringer Ingelheim Pharma Kg | FAP-activated anti-tumour compounds |
| AU2001266853B2 (en) * | 2000-06-14 | 2005-02-17 | Medarex, Inc. | Prodrug compounds with an oligopeptide having an isoleucine residue |
| GB0027552D0 (en) * | 2000-11-10 | 2000-12-27 | Boehringer Ingelheim Pharma | Anti-tumor compounds |
| US20030232742A1 (en) * | 2000-11-10 | 2003-12-18 | Stefan Peters | FAP-activated anti-tumor compounds |
| US20020155565A1 (en) | 2000-11-10 | 2002-10-24 | Pilar Garin-Chesa | FAP-activated anti-tumor compounds |
| US20030055052A1 (en) | 2000-11-10 | 2003-03-20 | Stefan Peters | FAP-activated anti-tumor compounds |
| EP1238678A1 (en) | 2001-03-08 | 2002-09-11 | Bayer Aktiengesellschaft | Enzyme-activated cytostatic conjugates with integrin ligands |
| US6897034B2 (en) | 2001-06-11 | 2005-05-24 | Medarex, Inc. | CD10-activated prodrug compounds |
| EP1333033A1 (en) | 2002-01-30 | 2003-08-06 | Boehringer Ingelheim Pharma GmbH & Co.KG | FAP-activated anti-tumor compounds |
| US20040033957A1 (en) | 2002-05-10 | 2004-02-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | FAP-activated anti-tumor prodrugs |
| WO2003094972A2 (en) | 2002-05-10 | 2003-11-20 | Boehringer Ingelheim Pharma Gmbh & Co Kg | Fap-activated anti-tumor prodrugs |
| EP1718667B1 (en) | 2004-02-23 | 2013-01-09 | Genentech, Inc. | Heterocyclic self-immolative linkers and conjugates |
| CA2582552A1 (en) * | 2004-10-21 | 2006-05-04 | Igf Oncology, Llc | Toxins and radionuclides coupled to igf-1 receptor ligands for treatment of cancer |
| WO2007087131A2 (en) | 2006-01-05 | 2007-08-02 | The Johns Hopkins University | Peptide prodrugs |
| WO2008011157A2 (en) | 2006-07-20 | 2008-01-24 | The General Hospital Corporation | Methods, compositions, and kits for the selective activation of protoxins through combinatorial targeting |
| WO2008116053A2 (en) | 2007-03-20 | 2008-09-25 | Trustees Of Tufts College | Fap-activated chemotherapeutic compounds, and methods of use thereof |
| EP2753334B1 (en) | 2011-08-30 | 2022-10-19 | Trustees Of Tufts College | Fap-activated proteasome inhibitors for treating solid tumors |
| HK1204294A1 (en) | 2012-03-21 | 2015-11-13 | 拜耳知识产权有限责任公司 | Use of (rs)-s-cyclopropyl-s-(4-{[4-{[1r, 2r)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide for treating specific tumours |
| MX2015004703A (es) | 2012-10-16 | 2015-10-12 | Genspera Inc | Composiciones cancerigenas inyectables. |
| JP6386467B2 (ja) | 2012-11-16 | 2018-09-05 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | キナーゼ活性のモジュレーターとしての新規複素環式誘導体 |
| JP6523965B2 (ja) * | 2012-12-28 | 2019-06-05 | コビオレス エヌヴイＣｏｂｉｏｒｅｓ Ｎｖ | 最小毒性プロドラッグ |
| US9737556B2 (en) | 2014-06-13 | 2017-08-22 | Trustees Of Tufts College | FAP-activated therapeutic agents, and uses related thereto |
| WO2015192123A1 (en) | 2014-06-13 | 2015-12-17 | Trustees Of Tufts College | Fap-activated therapeutic agents, and uses related thereto |
| WO2016046778A2 (en) | 2014-09-25 | 2016-03-31 | Amgen Inc | Protease-activatable bispecific proteins |
| US11351264B2 (en) | 2016-04-01 | 2022-06-07 | Arizona Board Of Regents On Behalf Of The University Of Arizona | PAR2 mimetic peptides and uses thereof |
| WO2017189569A1 (en) | 2016-04-25 | 2017-11-02 | Trustees Of Tufts College | Multimediator dpp4 and fap inhibitors, and uses related thereto |
-
2015
- 2015-06-15 WO PCT/US2015/035798 patent/WO2015192123A1/en not_active Ceased
- 2015-06-15 SI SI201531956T patent/SI3154594T1/sl unknown
- 2015-06-15 CN CN202111061513.XA patent/CN113786495A/zh active Pending
- 2015-06-15 US US15/318,627 patent/US10245248B2/en active Active
- 2015-06-15 JP JP2016572687A patent/JP6744826B2/ja not_active Expired - Fee Related
- 2015-06-15 PT PT158070490T patent/PT3154594T/pt unknown
- 2015-06-15 IL IL291922A patent/IL291922B2/en unknown
- 2015-06-15 ES ES15807049T patent/ES2951596T3/es active Active
- 2015-06-15 HR HRP20230854TT patent/HRP20230854T1/hr unknown
- 2015-06-15 HU HUE15807049A patent/HUE063194T2/hu unknown
- 2015-06-15 CN CN201580043350.9A patent/CN106573073B/zh active Active
- 2015-06-15 EP EP15807049.0A patent/EP3154594B1/en active Active
- 2015-06-15 CN CN202111061659.4A patent/CN113956325A/zh active Pending
- 2015-06-15 FI FIEP15807049.0T patent/FI3154594T3/fi active
- 2015-06-15 DK DK15807049.0T patent/DK3154594T3/da active
- 2015-06-15 CA CA2952051A patent/CA2952051C/en active Active
- 2015-06-15 IL IL325256A patent/IL325256A/en unknown
- 2015-06-15 EP EP23185698.0A patent/EP4299134A3/en active Pending
- 2015-06-15 PL PL15807049.0T patent/PL3154594T3/pl unknown
- 2015-06-15 IL IL249370A patent/IL249370B/en unknown
- 2015-06-15 CN CN202111061534.1A patent/CN113967258B/zh active Active
-
2019
- 2019-02-13 US US16/274,387 patent/US11033525B2/en active Active
-
2020
- 2020-07-31 JP JP2020130483A patent/JP7093912B2/ja active Active
-
2021
- 2021-04-01 US US17/220,635 patent/US12121505B2/en active Active
- 2021-04-01 US US17/220,675 patent/US12023316B2/en active Active
- 2021-05-26 US US17/330,848 patent/US12053450B2/en active Active
-
2022
- 2022-05-27 JP JP2022086532A patent/JP7530111B2/ja active Active
-
2024
- 2024-07-19 JP JP2024115840A patent/JP2024150608A/ja active Pending
- 2024-09-09 US US18/828,942 patent/US20250108031A1/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP7784142B2 (ja) | Ｆａｐ標的化放射性医薬品およびイメージング剤、ならびにそれらに関連する使用 | |
| ES2705342T3 (es) | Co-cristales de (S)-N-metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propan-2-il)quinolin-4-carboxamida y derivados deuterados de la misma como inhibidores de DNA-PK | |
| EP2879677B1 (en) | Substituted pyrazolone compounds and methods of use | |
| US20190375704A1 (en) | Modulators of the eif2alpha pathway | |
| JP2013107903A (ja) | 化学療法の強化方法 | |
| Kuhn et al. | Beta-lactams and their potential use as novel anticancer chemotherapeutics drugs | |
| KR102148681B1 (ko) | Pi3 키나제 모듈레이터로서의 헤테로방향족 화합물 | |
| US8975282B2 (en) | Substituted pyrazolone compounds and methods of use | |
| RU2017104909A (ru) | Лечение рака комбинацией лучевой терапии, наночастиц оксида церия и химиотерапевтического средства | |
| Apostolidou et al. | Treatment of acute lymphoblastic leukaemia: a new era | |
| JP2014040437A5 (enExample) | ||
| CN107027291A (zh) | 用谷氨酰胺酶抑制剂的组合疗法 | |
| WO2019236631A1 (en) | Pyrazolo-pyrimidin-amino-cycloalkyl compounds and their therapeutic uses | |
| TW201244714A (en) | PARP inhibitors for the treatment of CIPN | |
| US20220211883A1 (en) | Fap-activated radiotheranostics and uses related thereto | |
| ES2960601T3 (es) | Composiciones y métodos para el tratamiento del cáncer | |
| RU2019142111A (ru) | Усилитель противоопухолевого эффекта с применением нового соединения бифенила | |
| JP5113038B2 (ja) | 癌治療用キットおよび癌治療用医薬組成物 | |
| JP5642892B2 (ja) | 多形膠芽腫の治療のためのマシテンタンを含有する組み合わせ剤 | |
| JP6422936B2 (ja) | ５−ブロモ−インジルビン | |
| JP2009510165A5 (enExample) | ||
| AR049136A1 (es) | Composicion y metodo con irinotecan (cpt-11) y un inhibidor del egfr,como erlotinib | |
| ES2671730T3 (es) | Terapia de combinación para el cáncer de ovario | |
| KR102687556B1 (ko) | 종양 전이를 억제하는 방법 | |
| JP2024511054A (ja) | ボロン酸化合物、組成物および方法 |