JP2014527070A5 - - Google Patents
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- JP2014527070A5 JP2014527070A5 JP2014528600A JP2014528600A JP2014527070A5 JP 2014527070 A5 JP2014527070 A5 JP 2014527070A5 JP 2014528600 A JP2014528600 A JP 2014528600A JP 2014528600 A JP2014528600 A JP 2014528600A JP 2014527070 A5 JP2014527070 A5 JP 2014527070A5
- Authority
- JP
- Japan
- Prior art keywords
- fap
- prodrug
- group
- lower alkyl
- proteasome inhibitor
- 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 description 36
- 239000000651 prodrug Substances 0.000 claims description 36
- 229940079156 Proteasome inhibitor Drugs 0.000 claims description 18
- 239000003207 proteasome inhibitor Substances 0.000 claims description 18
- 239000000758 substrate Substances 0.000 claims description 12
- 238000003776 cleavage reaction Methods 0.000 claims description 11
- 230000007017 scission Effects 0.000 claims description 11
- 239000013543 active substance Substances 0.000 claims description 8
- 102000004169 proteins and genes Human genes 0.000 claims description 8
- 108090000623 proteins and genes Proteins 0.000 claims description 8
- 210000002536 stromal cell Anatomy 0.000 claims description 8
- 150000003839 salts Chemical class 0.000 claims description 7
- 230000004913 activation Effects 0.000 claims description 6
- 229940127089 cytotoxic agent Drugs 0.000 claims description 6
- 210000002950 fibroblast Anatomy 0.000 claims description 6
- 241000282326 Felis catus Species 0.000 claims description 5
- 206010028980 Neoplasm Diseases 0.000 claims description 5
- 102000056251 Prolyl Oligopeptidases Human genes 0.000 claims description 5
- 102100037838 Prolyl endopeptidase Human genes 0.000 claims description 5
- 101710178372 Prolyl endopeptidase Proteins 0.000 claims description 5
- 102000004245 Proteasome Endopeptidase Complex Human genes 0.000 claims description 5
- 108090000708 Proteasome Endopeptidase Complex Proteins 0.000 claims description 5
- 238000000034 method Methods 0.000 claims description 4
- 230000002797 proteolythic effect Effects 0.000 claims description 3
- 239000002254 cytotoxic agent Substances 0.000 claims description 2
- 231100000599 cytotoxic agent Toxicity 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 238000001727 in vivo Methods 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 230000028327 secretion Effects 0.000 claims description 2
- 231100000331 toxic Toxicity 0.000 claims description 2
- 230000002588 toxic effect Effects 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 claims 15
- 150000001875 compounds Chemical class 0.000 claims 11
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 210000004027 cell Anatomy 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 108090000765 processed proteins & peptides Proteins 0.000 claims 6
- 230000000903 blocking effect Effects 0.000 claims 5
- 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
- 239000002246 antineoplastic agent Substances 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- 125000004080 3-carboxypropanoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C(O[H])=O 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 3
- 125000000539 amino acid group Chemical group 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 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
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000003275 alpha amino acid group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 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 2
- 238000001574 biopsy Methods 0.000 claims 2
- 229960004562 carboplatin Drugs 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 229960003668 docetaxel Drugs 0.000 claims 2
- 229960004679 doxorubicin Drugs 0.000 claims 2
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 2
- 125000000524 functional group Chemical group 0.000 claims 2
- 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 2
- 229960005277 gemcitabine Drugs 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 230000002209 hydrophobic effect Effects 0.000 claims 2
- -1 methoxysuccinyl Chemical group 0.000 claims 2
- 230000035699 permeability Effects 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- FWPWHHUJACGNMZ-NBBQQVJHSA-N (1s,2r,5r)-5-[(1s)-1-hydroxy-2-methylpropyl]-2-methyl-7-oxa-4-azabicyclo[3.2.0]heptane-3,6-dione Chemical compound N1C(=O)[C@H](C)[C@@H]2OC(=O)[C@@]21[C@@H](O)C(C)C FWPWHHUJACGNMZ-NBBQQVJHSA-N 0.000 claims 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 1
- 208000031886 HIV Infections Diseases 0.000 claims 1
- 208000037357 HIV infectious disease Diseases 0.000 claims 1
- 101001136986 Homo sapiens Proteasome subunit beta type-8 Proteins 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010062016 Immunosuppression Diseases 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
- 241000124008 Mammalia Species 0.000 claims 1
- 108010064641 ONX 0912 Proteins 0.000 claims 1
- 108010079844 PR-957 Proteins 0.000 claims 1
- KMXHEXRPYSXLRN-JDVQERKKSA-N PS-519 Chemical compound N1C(=O)[C@H](CCC)[C@@H]2OC(=O)[C@@]21[C@@H](O)C(C)C KMXHEXRPYSXLRN-JDVQERKKSA-N 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 102100035760 Proteasome subunit beta type-8 Human genes 0.000 claims 1
- 201000004681 Psoriasis Diseases 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
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 230000003213 activating effect Effects 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 230000030741 antigen processing and presentation Effects 0.000 claims 1
- 108010044540 auristatin Proteins 0.000 claims 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- 125000003180 beta-lactone group Chemical group 0.000 claims 1
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 1
- 229960001467 bortezomib Drugs 0.000 claims 1
- GXJABQQUPOEUTA-RDJZCZTQSA-N bortezomib Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)B(O)O)NC(=O)C=1N=CC=NC=1)C1=CC=CC=C1 GXJABQQUPOEUTA-RDJZCZTQSA-N 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- BLMPQMFVWMYDKT-NZTKNTHTSA-N carfilzomib Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CC(C)C)C(=O)[C@]1(C)OC1)NC(=O)CN1CCOCC1)CC1=CC=CC=C1 BLMPQMFVWMYDKT-NZTKNTHTSA-N 0.000 claims 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- SJFBTAPEPRWNKH-CCKFTAQKSA-N delanzomib Chemical compound CC(C)C[C@@H](B(O)O)NC(=O)[C@H]([C@@H](C)O)NC(=O)C1=CC=CC(C=2C=CC=CC=2)=N1 SJFBTAPEPRWNKH-CCKFTAQKSA-N 0.000 claims 1
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 claims 1
- 229960003957 dexamethasone Drugs 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- AFOSIXZFDONLBT-UHFFFAOYSA-N divinyl sulfone Chemical compound C=CS(=O)(=O)C=C AFOSIXZFDONLBT-UHFFFAOYSA-N 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 108700002672 epoxomicin Proteins 0.000 claims 1
- DOGIDQKFVLKMLQ-JTHVHQAWSA-N epoxomicin Chemical compound CC[C@H](C)[C@H](N(C)C(C)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1 DOGIDQKFVLKMLQ-JTHVHQAWSA-N 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 229960002949 fluorouracil Drugs 0.000 claims 1
- 210000005260 human cell Anatomy 0.000 claims 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 229960003685 imatinib mesylate Drugs 0.000 claims 1
- YLMAHDNUQAMNNX-UHFFFAOYSA-N imatinib methanesulfonate Chemical compound CS(O)(=O)=O.C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 YLMAHDNUQAMNNX-UHFFFAOYSA-N 0.000 claims 1
- 230000001506 immunosuppresive effect Effects 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000001678 irradiating effect Effects 0.000 claims 1
- MXAYKZJJDUDWDS-LBPRGKRZSA-N ixazomib Chemical compound CC(C)C[C@@H](B(O)O)NC(=O)CNC(=O)C1=CC(Cl)=CC=C1Cl MXAYKZJJDUDWDS-LBPRGKRZSA-N 0.000 claims 1
- MBOMYENWWXQSNW-AWEZNQCLSA-N ixazomib citrate Chemical compound N([C@@H](CC(C)C)B1OC(CC(O)=O)(CC(O)=O)C(=O)O1)C(=O)CNC(=O)C1=CC(Cl)=CC=C1Cl MBOMYENWWXQSNW-AWEZNQCLSA-N 0.000 claims 1
- GOTYRUGSSMKFNF-UHFFFAOYSA-N lenalidomide Chemical compound C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O GOTYRUGSSMKFNF-UHFFFAOYSA-N 0.000 claims 1
- 229960004942 lenalidomide Drugs 0.000 claims 1
- 229960000485 methotrexate Drugs 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- SWZXEVABPLUDIO-WSZYKNRRSA-N n-[(2s)-3-methoxy-1-[[(2s)-3-methoxy-1-[[(2s)-1-[(2r)-2-methyloxiran-2-yl]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]-2-methyl-1,3-thiazole-5-carboxamide Chemical compound N([C@@H](COC)C(=O)N[C@@H](COC)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)[C@]1(C)OC1)C(=O)C1=CN=C(C)S1 SWZXEVABPLUDIO-WSZYKNRRSA-N 0.000 claims 1
- 229950005750 oprozomib Drugs 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 229960005079 pemetrexed Drugs 0.000 claims 1
- QOFFJEBXNKRSPX-ZDUSSCGKSA-N pemetrexed Chemical compound C1=N[C]2NC(N)=NC(=O)C2=C1CCC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 QOFFJEBXNKRSPX-ZDUSSCGKSA-N 0.000 claims 1
- 125000001151 peptidyl group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000004437 phosphorous atom Chemical group 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 230000008093 supporting effect Effects 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
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 claims 1
- 0 CC(C)[C@@](C([C@@]([C@]1C)O2)(C2=O)NC1=O)O* Chemical compound CC(C)[C@@](C([C@@]([C@]1C)O2)(C2=O)NC1=O)O* 0.000 description 2
- FTCFXJNXQMLMCC-ZQQDZYSUSA-N CC(C)C[C@@H](/C=C/S(C)(=O)=O)NC([C@H](CC(C)C)NC([C@H](CC(C)C)NC)=O)=O Chemical compound CC(C)C[C@@H](/C=C/S(C)(=O)=O)NC([C@H](CC(C)C)NC([C@H](CC(C)C)NC)=O)=O FTCFXJNXQMLMCC-ZQQDZYSUSA-N 0.000 description 1
- SHFYIABOLDVYDL-XEVUQIKYSA-N CC(C)C[C@@H](B(OC(CC(O)=O)C1C(O)=O)OC1=O)NC(CNC)=O Chemical compound CC(C)C[C@@H](B(OC(CC(O)=O)C1C(O)=O)OC1=O)NC(CNC)=O SHFYIABOLDVYDL-XEVUQIKYSA-N 0.000 description 1
- YVEKBPJIQYLZDU-KTUBMRJJSA-N CC(C)C[C@@H](C([C@]1(C)OC1)=O)NC(CNC(C(CC(C)C)NC([C@H](CCc1ccccc1)NC)=O)=O)=O Chemical compound CC(C)C[C@@H](C([C@]1(C)OC1)=O)NC(CNC(C(CC(C)C)NC([C@H](CCc1ccccc1)NC)=O)=O)=O YVEKBPJIQYLZDU-KTUBMRJJSA-N 0.000 description 1
- HEZVRGZEVQVONT-VRKAVTRVSA-N CC(C)[C@@H]([C@@]([C@H]([C@H]1C)OC)(C(SC[C@@H](C(O)=O)NC(C)=O)=O)NC1=O)O Chemical compound CC(C)[C@@H]([C@@]([C@H]([C@H]1C)OC)(C(SC[C@@H](C(O)=O)NC(C)=O)=O)NC1=O)O HEZVRGZEVQVONT-VRKAVTRVSA-N 0.000 description 1
- RMAVNBWCMCLWKH-GJZGRUSLSA-N CCN[C@@H](Cc1ccccc1)C(N[C@H](B(O)O)CC(C)C)=O Chemical compound CCN[C@@H](Cc1ccccc1)C(N[C@H](B(O)O)CC(C)C)=O RMAVNBWCMCLWKH-GJZGRUSLSA-N 0.000 description 1
- JRUYKTCURFJCJI-DDASBUEYSA-N CC[C@H](C)[C@@H]([C@H](C(N[C@@H]1[C@@H](C[C@@H](C(O)=O)NC([C@H](C)NC)=O)C1)=O)O1)C1=O Chemical compound CC[C@H](C)[C@@H]([C@H](C(N[C@@H]1[C@@H](C[C@@H](C(O)=O)NC([C@H](C)NC)=O)C1)=O)O1)C1=O JRUYKTCURFJCJI-DDASBUEYSA-N 0.000 description 1
- 230000008629 immune suppression Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161528824P | 2011-08-30 | 2011-08-30 | |
| US61/528,824 | 2011-08-30 | ||
| PCT/US2012/053140 WO2013033396A2 (en) | 2011-08-30 | 2012-08-30 | Fap-activated proteasome inhibitors for treating solid tumors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017170106A Division JP2018016629A (ja) | 2011-08-30 | 2017-09-05 | 固形腫瘍を治療するためのｆａｐ活性化プロテアソーム阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014527070A JP2014527070A (ja) | 2014-10-09 |
| JP2014527070A5 true JP2014527070A5 (cg-RX-API-DMAC7.html) | 2015-10-15 |
| JP6207509B2 JP6207509B2 (ja) | 2017-10-04 |
Family
ID=47757170
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014528600A Active JP6207509B2 (ja) | 2011-08-30 | 2012-08-30 | 固形腫瘍を治療するためのｆａｐ活性化プロテアソーム阻害剤 |
| JP2017170106A Pending JP2018016629A (ja) | 2011-08-30 | 2017-09-05 | 固形腫瘍を治療するためのｆａｐ活性化プロテアソーム阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017170106A Pending JP2018016629A (ja) | 2011-08-30 | 2017-09-05 | 固形腫瘍を治療するためのｆａｐ活性化プロテアソーム阻害剤 |
Country Status (14)
| Country | Link |
|---|---|
| US (6) | US9597410B2 (cg-RX-API-DMAC7.html) |
| EP (2) | EP2753334B1 (cg-RX-API-DMAC7.html) |
| JP (2) | JP6207509B2 (cg-RX-API-DMAC7.html) |
| CN (2) | CN103945856A (cg-RX-API-DMAC7.html) |
| AU (2) | AU2012301810B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2846852C (cg-RX-API-DMAC7.html) |
| DK (1) | DK2753334T3 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2929179T3 (cg-RX-API-DMAC7.html) |
| HR (1) | HRP20221320T1 (cg-RX-API-DMAC7.html) |
| HU (1) | HUE060305T2 (cg-RX-API-DMAC7.html) |
| PL (1) | PL2753334T3 (cg-RX-API-DMAC7.html) |
| PT (1) | PT2753334T (cg-RX-API-DMAC7.html) |
| SI (1) | SI2753334T1 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2013033396A2 (cg-RX-API-DMAC7.html) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2753334T (pt) | 2011-08-30 | 2022-11-03 | Tufts College | Inibidores de proteassoma ativados por fap utilizados para o tratamento de tumores sólidos |
| BR112015012885A2 (pt) * | 2012-12-03 | 2017-07-11 | Hoffmann La Roche | composições triazol e imidazol substituídas |
| WO2014200969A2 (en) * | 2013-06-10 | 2014-12-18 | Millennium Pharmaceuticals, Inc. | Methods of treatment of cancer |
| JP6468562B2 (ja) * | 2013-11-21 | 2019-02-13 | 国立大学法人北海道大学 | プロテアソーム阻害性化合物 |
| EP4299134A3 (en) * | 2014-06-13 | 2024-03-27 | Bach Biosciences, LLC | Fap-activated therapeutic agents, and uses related thereto |
| WO2015192124A1 (en) | 2014-06-13 | 2015-12-17 | Trustees Of Tufts College | Fap-activated therapeutic agents, and uses related thereto |
| DK3160513T3 (da) | 2014-06-30 | 2020-04-06 | Glykos Finland Oy | Saccharidderivat af en toksisk payload og antistofkonjugater deraf |
| KR102462240B1 (ko) | 2014-07-14 | 2022-11-03 | 센트랙스 인터내셔널, 아이엔씨. | 효소 억제를 위한 에폭시케톤 화합물 |
| CN104231047B (zh) * | 2014-08-22 | 2017-06-16 | 亚飞（上海）生物医药科技有限公司 | 水溶性靶向激活的紫杉醇衍生物及其制备和用途 |
| US10682371B2 (en) | 2014-08-22 | 2020-06-16 | Yafei Shanghai Biolog Medicine Science & Technology Co. Ltd. | Small molecule conjugates specifically activated in tumor microenvironment for targeting and use thereof |
| WO2016210054A1 (en) * | 2015-06-23 | 2016-12-29 | The Board Of Trustees Of The Leland Stanford Junior University | Novel rhodol fluorophores for near-infrared imaging |
| CN106588965A (zh) * | 2015-10-15 | 2017-04-26 | 北京大学 | 脲拟肽硼酸化合物及其药物组合物、制备方法和用途 |
| CN105938123B (zh) * | 2015-12-18 | 2018-09-14 | 重庆两江药物研发中心有限公司 | 一种卡非佐米中间体中杂质的检测方法 |
| US10590084B2 (en) | 2016-03-09 | 2020-03-17 | Blade Therapeutics, Inc. | Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof |
| WO2017222914A1 (en) | 2016-06-21 | 2017-12-28 | Inception 4, Inc. | Carbocyclic prolinamide derivatives |
| KR102595723B1 (ko) | 2016-06-21 | 2023-10-27 | 오리온 옵탈몰로지 엘엘씨 | 헤테로시클릭 프롤린아미드 유도체 |
| AU2017292646A1 (en) | 2016-07-05 | 2019-02-07 | Blade Therapeutics, Inc. | Calpain modulators and therapeutic uses thereof |
| MX2019003425A (es) | 2016-09-28 | 2019-08-16 | Blade Therapeutics Inc | Moduladores de calpainas y usos terapeuticos de los mismos. |
| JP7162592B2 (ja) | 2016-12-14 | 2022-10-28 | パーデュー・リサーチ・ファウンデイション | 線維芽細胞活性化タンパク質（ｆａｐ）標的イメージングおよび治療 |
| MA47215A (fr) | 2017-01-09 | 2019-11-13 | Bioxcel Therapeutics Inc | Procédés prédictifs et diagnostiques pour le cancer de la prostate |
| WO2018187418A1 (en) * | 2017-04-04 | 2018-10-11 | Genentech, Inc. | Substrates recognized by fibroblast activation protein (fap) and methods of using the same |
| GB201710973D0 (en) | 2017-07-07 | 2017-08-23 | Avacta Life Sciences Ltd | Scaffold proteins |
| KR102005030B1 (ko) * | 2017-10-31 | 2019-07-29 | 충북대학교 산학협력단 | 프로테아좀 억제제를 유효성분으로 포함하는 신경퇴행성 질환의 예방 또는 치료용 약학적 조성물 |
| CN108191957B (zh) * | 2017-12-30 | 2021-05-04 | 浙江大学 | 三肽大环衍生物及其制备方法和应用 |
| JP2021512165A (ja) | 2018-01-29 | 2021-05-13 | コグノス・セラピューティクス・インコーポレイテッド | ボルテゾミブの腫瘍内送達 |
| JP2021512949A (ja) * | 2018-02-06 | 2021-05-20 | ウニベルジテート ハイデルベルク | Ｆａｐ阻害物質 |
| CA3107925A1 (en) * | 2018-08-02 | 2020-02-06 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Borate of azetidine derivative |
| WO2020033437A1 (en) * | 2018-08-06 | 2020-02-13 | University Of Kentucky Research Foundation | Proteasome inhibitors |
| GB201820320D0 (en) * | 2018-12-13 | 2019-01-30 | Bicyclerd Ltd | Bicyclic peptide ligands specific for FAPalpha |
| EP4041747A4 (en) * | 2019-10-11 | 2023-10-18 | Mayo Foundation for Medical Education and Research | PROTEASOME HIBITORS |
| CN111235221B (zh) * | 2020-01-22 | 2022-08-05 | 北京大学第一医院 | 一种fap抑制剂的活性检测方法 |
| CZ309380B6 (cs) * | 2020-03-30 | 2022-10-26 | Ústav organické chemie a biochemie AV ČR v. v. i | Sloučeniny pro inhibici fibroblastového aktivačního proteinu |
| EP4168123B1 (en) * | 2020-06-17 | 2025-08-27 | University of Utah Research Foundation | Biomarker based patient selection for proteasome inhibitor treatment |
| EP4262878A1 (en) * | 2020-12-17 | 2023-10-25 | Trustees Of Tufts College | Fap-activated radiotheranostics, and uses related thereto |
| US20240101549A1 (en) | 2020-12-17 | 2024-03-28 | Astrazeneca Ab | N-(2-(4-cyanothiazolidin-3-yl)-2-oxoethyl)-quinoline-4-carboxamides |
| AU2022238571A1 (en) | 2021-03-18 | 2023-09-14 | Seagen Inc. | Selective drug release from internalized conjugates of biologically active compounds |
| US11806405B1 (en) | 2021-07-19 | 2023-11-07 | Zeno Management, Inc. | Immunoconjugates and methods |
| WO2024140736A1 (zh) * | 2022-12-27 | 2024-07-04 | 上海美悦生物科技发展有限公司 | 三肽环氧酮化合物、药物组合物及其制备方法和用途 |
| WO2025159301A1 (ko) * | 2024-01-24 | 2025-07-31 | 서울대학교산학협력단 | 섬유아세포 활성화 단백질에 의해 활성화되는 프로드러그 화합물 |
Family Cites Families (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4499082A (en) | 1983-12-05 | 1985-02-12 | E. I. Du Pont De Nemours And Company | α-Aminoboronic acid peptides |
| AU600226B2 (en) | 1985-02-04 | 1990-08-09 | Merrell Pharmaceuticals Inc. | Novel peptidase inhibitors |
| US4935493A (en) | 1987-10-06 | 1990-06-19 | E. I. Du Pont De Nemours And Company | Protease inhibitors |
| US5462928A (en) | 1990-04-14 | 1995-10-31 | New England Medical Center Hospitals, Inc. | Inhibitors of dipeptidyl-aminopeptidase type IV |
| US6825169B1 (en) | 1991-10-22 | 2004-11-30 | Trustees Of Tufts College | Inhibitors of dipeptidyl-aminopeptidase type IV |
| WO1995025223A1 (en) | 1994-03-11 | 1995-09-21 | Wilson Greatbatch Ltd. | Low power electromagnetic pump |
| US5580979A (en) | 1994-03-15 | 1996-12-03 | Trustees Of Tufts University | Phosphotyrosine peptidomimetics for inhibiting SH2 domain interactions |
| US6083903A (en) * | 1994-10-28 | 2000-07-04 | Leukosite, Inc. | Boronic ester and acid compounds, synthesis and uses |
| US6180402B1 (en) | 1996-11-20 | 2001-01-30 | Qlt Inc. | Method for inhibiting apoptosis induced by photodynamic therapy using a cysteine or serine protease inhibitor |
| BR9813233A (pt) | 1997-09-29 | 2000-08-22 | Point Therapeutics Inc | Estimulação de células hematopoéticas in vitro |
| WO1999038501A2 (en) | 1998-02-02 | 1999-08-05 | Trustees Of Tufts College | Method of regulating glucose metabolism, and reagents related thereto |
| AU770319C (en) | 1998-05-04 | 2004-11-25 | Point Therapeutics, Inc. | Hematopoietic stimulation |
| KR100704814B1 (ko) | 1998-06-05 | 2007-04-10 | 포인트 써러퓨틱스, 인크. | 시클릭 보로프롤린 화합물 |
| US6979697B1 (en) | 1998-08-21 | 2005-12-27 | Point Therapeutics, Inc. | Regulation of substrate activity |
| US6285178B1 (en) | 1999-02-11 | 2001-09-04 | Battelle Memorial Institute | Power supply |
| US6890904B1 (en) | 1999-05-25 | 2005-05-10 | Point Therapeutics, Inc. | Anti-tumor agents |
| CA2837936A1 (en) | 2001-11-26 | 2003-06-05 | Trustees Of Tufts College | Peptidomimetic inhibitors of post-proline cleaving enzymes |
| JP2005511636A (ja) | 2001-11-26 | 2005-04-28 | トラスティーズ オブ タフツ カレッジ | 自己免疫疾患の治療方法及びそれに関する試薬 |
| WO2003092605A2 (en) | 2002-04-30 | 2003-11-13 | Trustees Of Tufts College | Protease inhibitors |
| WO2004004658A2 (en) | 2002-07-09 | 2004-01-15 | Point Therapeutics, Inc. | Methods and compositions relating to isoleucine boroproline compounds |
| AU2004240630B2 (en) | 2003-05-15 | 2010-10-07 | Trustees Of Tufts College | Stable analogs of peptide and polypeptide therapeutics |
| AU2005216970B2 (en) | 2004-02-23 | 2011-07-07 | Trustees Of Tufts College | Inhibitors of dipeptidylpeptidase IV for regulating glucose metabolism |
| US20060063719A1 (en) | 2004-09-21 | 2006-03-23 | Point Therapeutics, Inc. | Methods for treating diabetes |
| WO2006125227A2 (en) | 2005-05-19 | 2006-11-23 | Genentech, Inc. | Fibroblast activation protein inhibitor compounds and methods |
| KR20080030079A (ko) * | 2005-07-05 | 2008-04-03 | 트러스티즈 오브 터프츠 칼리지 | 섬유아세포 활성 단백질 알파의 억제제 |
| AU2006201635A1 (en) * | 2005-10-20 | 2007-05-10 | Ludwig Institute For Cancer Research | Novel inhibitors and methods for their preparation |
| CA2633803A1 (en) * | 2005-12-19 | 2007-09-07 | Trustees Of Tufts College | Soft protease inhibitors and pro-soft forms thereof |
| US20080004286A1 (en) * | 2006-06-30 | 2008-01-03 | Schering Corporation | Method of Using Substituted Piperidines that Increase P53 Activity |
| US20100184706A1 (en) * | 2007-03-20 | 2010-07-22 | Bachovchin William W | Fap-activated chemotherapeutic compounds, and methods of use thereof |
| CA2681351A1 (en) * | 2007-03-20 | 2008-09-25 | Trustees Of Tufts College | Inhibitors of fibroblast activation protein, and methods of use thereof |
| WO2009006473A2 (en) * | 2007-07-05 | 2009-01-08 | Trustees Of Tufts College | Pro-soft polypeptide proteasome inhibitors, and methods of use thereof |
| RS52435B (sr) * | 2007-08-06 | 2013-02-28 | Millennium Pharmaceuticals Inc. | Inhibitori proteazoma |
| ES2733348T3 (es) * | 2007-08-17 | 2019-11-28 | Boehringer Ingelheim Int | Derivados de purina para uso en el tratamiento de enfermedades relacionadas con FAP |
| JP2011517934A (ja) * | 2008-03-03 | 2011-06-23 | カンザス ステイト ユニバーシティ リサーチ ファウンデーション | プロテアーゼアッセイ |
| JP5801585B2 (ja) | 2011-03-30 | 2015-10-28 | 株式会社ケーヒン | 燃料噴射制御システム |
| PT2753334T (pt) | 2011-08-30 | 2022-11-03 | Tufts College | Inibidores de proteassoma ativados por fap utilizados para o tratamento de tumores sólidos |
-
2012
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- 2012-08-30 DK DK12827686.2T patent/DK2753334T3/da active
- 2012-08-30 EP EP12827686.2A patent/EP2753334B1/en active Active
- 2012-08-30 CN CN201280052940.4A patent/CN103945856A/zh active Pending
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- 2012-08-30 CN CN201810059355.6A patent/CN108383893A/zh active Pending
- 2012-08-30 PL PL12827686.2T patent/PL2753334T3/pl unknown
- 2012-08-30 JP JP2014528600A patent/JP6207509B2/ja active Active
- 2012-08-30 SI SI201232012T patent/SI2753334T1/sl unknown
- 2012-08-30 WO PCT/US2012/053140 patent/WO2013033396A2/en not_active Ceased
- 2012-08-30 CA CA2846852A patent/CA2846852C/en active Active
- 2012-08-30 ES ES12827686T patent/ES2929179T3/es active Active
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- 2025-02-03 US US19/044,150 patent/US20250367304A1/en active Pending
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