JP2018016629A5 - - Google Patents
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- JP2018016629A5 JP2018016629A5 JP2017170106A JP2017170106A JP2018016629A5 JP 2018016629 A5 JP2018016629 A5 JP 2018016629A5 JP 2017170106 A JP2017170106 A JP 2017170106A JP 2017170106 A JP2017170106 A JP 2017170106A JP 2018016629 A5 JP2018016629 A5 JP 2018016629A5
- Authority
- JP
- Japan
- Prior art keywords
- fap
- proteasome inhibitor
- inhibitor according
- lower alkyl
- pharmaceutical composition
- 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.)
- Pending
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- 229940079156 Proteasome inhibitor Drugs 0.000 claims 15
- 239000003207 proteasome inhibitor Substances 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 12
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 125000002252 acyl group Chemical group 0.000 claims 5
- 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
- 229940127089 cytotoxic agent Drugs 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 210000004027 cell Anatomy 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 125000004080 3-carboxypropanoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C(O[H])=O 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
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 230000004913 activation Effects 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
- 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
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 210000002950 fibroblast Anatomy 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
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- -1 methoxysuccinyl Chemical group 0.000 claims 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 108090000623 proteins and genes Proteins 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 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
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical group O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-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
- 102000004245 Proteasome Endopeptidase Complex Human genes 0.000 claims 1
- 108090000708 Proteasome Endopeptidase Complex Proteins 0.000 claims 1
- 102100035760 Proteasome subunit beta type-8 Human genes 0.000 claims 1
- 201000004681 Psoriasis Diseases 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
- 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
- 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
- 201000011510 cancer Diseases 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
- 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
- 229960002949 fluorouracil Drugs 0.000 claims 1
- 125000002485 formyl group Chemical group [H]C(*)=O 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
- 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
- 230000001404 mediated effect Effects 0.000 claims 1
- 229960000485 methotrexate Drugs 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
- 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
- 230000001603 reducing effect Effects 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 210000002536 stromal cell Anatomy 0.000 claims 1
- 229910052717 sulfur Inorganic materials 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
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161528824P | 2011-08-30 | 2011-08-30 | |
| US61/528,824 | 2011-08-30 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014528600A Division 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018016629A JP2018016629A (ja) | 2018-02-01 |
| JP2018016629A5 true JP2018016629A5 (enExample) | 2018-03-22 |
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 Before (1)
| 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 |
Country Status (14)
| Country | Link |
|---|---|
| US (6) | US9597410B2 (enExample) |
| EP (2) | EP4144354B1 (enExample) |
| JP (2) | JP6207509B2 (enExample) |
| CN (2) | CN108383893A (enExample) |
| AU (2) | AU2012301810B2 (enExample) |
| CA (1) | CA2846852C (enExample) |
| DK (1) | DK2753334T3 (enExample) |
| ES (1) | ES2929179T3 (enExample) |
| HR (1) | HRP20221320T1 (enExample) |
| HU (1) | HUE060305T2 (enExample) |
| PL (1) | PL2753334T3 (enExample) |
| PT (1) | PT2753334T (enExample) |
| SI (1) | SI2753334T1 (enExample) |
| WO (1) | WO2013033396A2 (enExample) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4144354B1 (en) | 2011-08-30 | 2025-11-26 | Trustees Of Tufts College | Fap-activated proteasome inhibitors for treating solid tumors |
| RU2015123982A (ru) * | 2012-12-03 | 2017-01-13 | Ф. Хоффманн-Ля Рош Аг | Соединения замещенных триазола и имидазола |
| US20170035917A1 (en) * | 2013-06-10 | 2017-02-09 | Millennium Pharmaceuticals, Inc. | Methods of treatment of cancer |
| WO2015076359A1 (ja) * | 2013-11-21 | 2015-05-28 | 国立大学法人北海道大学 | プロテアソーム阻害性化合物 |
| US9737556B2 (en) | 2014-06-13 | 2017-08-22 | Trustees Of Tufts College | FAP-activated therapeutic agents, and uses related thereto |
| FI3154594T3 (fi) | 2014-06-13 | 2023-08-07 | Bach Biosciences Llc | Fap-aktivoituja terapeuttisia aineita ja niihin liittyviä käyttöjä |
| DK3160513T3 (da) | 2014-06-30 | 2020-04-06 | Glykos Finland Oy | Saccharidderivat af en toksisk payload og antistofkonjugater deraf |
| EP3166933B1 (en) * | 2014-07-14 | 2018-08-01 | Centrax International Inc. | Epoxyketone compounds for enzyme inhibition |
| 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 |
| CA2958495C (en) * | 2014-08-22 | 2023-04-18 | 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 |
| WO2017156071A1 (en) | 2016-03-09 | 2017-09-14 | Blade Therapeutics, Inc. | Cyclic keto-amide compounds as calpain modulators and methods of production and use thereof |
| US10526315B2 (en) | 2016-06-21 | 2020-01-07 | Orion Ophthalmology LLC | Carbocyclic prolinamide derivatives |
| PT3472149T (pt) | 2016-06-21 | 2023-11-23 | Orion Opthalmology Llc | Derivados de prolinamida heterocíclicos |
| EP3481835A4 (en) | 2016-07-05 | 2020-02-26 | Blade Therapeutics, Inc. | CALPAIN MODULATORS AND THEIR THERAPEUTIC USES |
| WO2018064119A1 (en) | 2016-09-28 | 2018-04-05 | Blade Therapeutics, Inc. | Calpain modulators and therapeutic uses thereof |
| 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 |
| US11613785B2 (en) | 2017-01-09 | 2023-03-28 | Onkosxcel Therapeutics, Llc | Predictive and diagnostic methods for prostate cancer |
| CN110461863A (zh) * | 2017-04-04 | 2019-11-15 | 豪夫迈·罗氏有限公司 | 成纤维细胞活化蛋白(fap)识别的底物及其使用方法 |
| 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 |
| WO2019148181A1 (en) | 2018-01-29 | 2019-08-01 | Cognos Therapeutics, Inc. | Intratumoral delivery of bortezomib |
| 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 |
| US11466036B2 (en) * | 2018-08-02 | 2022-10-11 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Borate of azetidine derivative |
| US11578101B2 (en) * | 2018-08-06 | 2023-02-14 | University Of Kentucky Research Foundation | Proteasome inhibitors |
| GB201820320D0 (en) * | 2018-12-13 | 2019-01-30 | Bicyclerd Ltd | Bicyclic peptide ligands specific for FAPalpha |
| US20240092831A1 (en) * | 2019-10-11 | 2024-03-21 | Mayo Foundation For Medical Education And Research | Proteasome Inhibitors |
| 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 |
| CN115968411A (zh) * | 2020-06-17 | 2023-04-14 | 犹他大学研究基金会 | 基于生物标记的用于蛋白酶体抑制剂治疗的患者选择 |
| KR20230121800A (ko) * | 2020-12-17 | 2023-08-21 | 트러스티즈 오브 터프츠 칼리지 | Fap-활성화된 래디오테라노스틱스, 및 이와 관련된용도 |
| KR20230122080A (ko) | 2020-12-17 | 2023-08-22 | 아스트라제네카 아베 | N-(2-(4-시아노티아졸리딘-3-일)-2-옥소에틸)-퀴놀린-4-카르복스아미드 |
| US12036286B2 (en) | 2021-03-18 | 2024-07-16 | 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 |
| CN118255835A (zh) * | 2022-12-27 | 2024-06-28 | 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 |
|---|---|---|---|---|
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| US6825169B1 (en) | 1991-10-22 | 2004-11-30 | Trustees Of Tufts College | Inhibitors of dipeptidyl-aminopeptidase type IV |
| DE69535019T2 (de) | 1994-03-11 | 2007-01-04 | Wilson Greatbatch, Ltd. | Elektromagnetische pumpe mit geringem vermögen |
| US5580979A (en) | 1994-03-15 | 1996-12-03 | Trustees Of Tufts University | Phosphotyrosine peptidomimetics for inhibiting SH2 domain interactions |
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| ES2179022T3 (es) | 1999-02-11 | 2003-01-16 | Battelle Memorial Institute | Fuente de alimentacion. |
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| US7727964B2 (en) | 2001-11-26 | 2010-06-01 | Trustees Of Tufts College | Peptidomimetic inhibitors of post-proline cleaving enzymes |
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| RU2379315C2 (ru) | 2004-02-23 | 2010-01-20 | Трастиз Оф Тафтс Колледж | Ингибиторы дипептидилпептидазы iv |
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| BRPI0620027A2 (pt) * | 2005-12-19 | 2011-10-25 | Tufts College | inibidores da protease soft e formas pró-soft |
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| US20100184706A1 (en) * | 2007-03-20 | 2010-07-22 | Bachovchin William W | Fap-activated chemotherapeutic compounds, and methods of use thereof |
| US20100105753A1 (en) * | 2007-03-20 | 2010-04-29 | 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 |
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| MX2010009766A (es) | 2008-03-03 | 2010-09-28 | Univ Kansas State | Ensayo de proteasa. |
| 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 |
| EP4144354B1 (en) | 2011-08-30 | 2025-11-26 | Trustees Of Tufts College | Fap-activated proteasome inhibitors for treating solid tumors |
-
2012
- 2012-08-30 EP EP22201696.6A patent/EP4144354B1/en active Active
- 2012-08-30 PT PT128276862T patent/PT2753334T/pt unknown
- 2012-08-30 CN CN201810059355.6A patent/CN108383893A/zh active Pending
- 2012-08-30 DK DK12827686.2T patent/DK2753334T3/da active
- 2012-08-30 HU HUE12827686A patent/HUE060305T2/hu unknown
- 2012-08-30 HR HRP20221320TT patent/HRP20221320T1/hr unknown
- 2012-08-30 CN CN201280052940.4A patent/CN103945856A/zh active Pending
- 2012-08-30 JP JP2014528600A patent/JP6207509B2/ja active Active
- 2012-08-30 PL PL12827686.2T patent/PL2753334T3/pl unknown
- 2012-08-30 US US14/241,666 patent/US9597410B2/en active Active
- 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 EP EP12827686.2A patent/EP2753334B1/en active Active
- 2012-08-30 AU AU2012301810A patent/AU2012301810B2/en active Active
- 2012-08-30 SI SI201232012T patent/SI2753334T1/sl unknown
- 2012-08-30 ES ES12827686T patent/ES2929179T3/es active Active
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2016
- 2016-05-27 US US15/167,109 patent/US9956297B2/en active Active
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2017
- 2017-06-19 AU AU2017204121A patent/AU2017204121A1/en not_active Abandoned
- 2017-09-05 JP JP2017170106A patent/JP2018016629A/ja active Pending
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2018
- 2018-04-13 US US15/952,648 patent/US10517955B2/en active Active
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2019
- 2019-11-19 US US16/688,574 patent/US11065339B2/en active Active
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2021
- 2021-06-15 US US17/348,043 patent/US12214047B2/en active Active
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2025
- 2025-02-03 US US19/044,150 patent/US20250367304A1/en active Pending
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