JP2018511556A5 - - Google Patents
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- Publication number
- JP2018511556A5 JP2018511556A5 JP2017538686A JP2017538686A JP2018511556A5 JP 2018511556 A5 JP2018511556 A5 JP 2018511556A5 JP 2017538686 A JP2017538686 A JP 2017538686A JP 2017538686 A JP2017538686 A JP 2017538686A JP 2018511556 A5 JP2018511556 A5 JP 2018511556A5
- Authority
- JP
- Japan
- Prior art keywords
- item
- compound
- compound according
- quencher
- alkyl
- 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
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- 150000001875 compounds Chemical class 0.000 claims description 86
- 239000007850 fluorescent dye Substances 0.000 claims description 25
- ANRHNWWPFJCPAZ-UHFFFAOYSA-M thionine Chemical compound [Cl-].C1=CC(N)=CC2=[S+]C3=CC(N)=CC=C3N=C21 ANRHNWWPFJCPAZ-UHFFFAOYSA-M 0.000 claims description 19
- -1 heterocyclylamino Chemical group 0.000 claims description 18
- 125000005842 heteroatom Chemical group 0.000 claims description 9
- 125000003342 alkenyl group Chemical group 0.000 claims description 8
- 125000000217 alkyl group Chemical group 0.000 claims description 8
- 125000000304 alkynyl group Chemical group 0.000 claims description 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 8
- JPBGLQJDCUZXEF-UHFFFAOYSA-N chromenylium Chemical compound [O+]1=CC=CC2=CC=CC=C21 JPBGLQJDCUZXEF-UHFFFAOYSA-N 0.000 claims description 8
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 8
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 8
- 125000004475 heteroaralkyl group Chemical group 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 125000000623 heterocyclic group Chemical group 0.000 claims description 8
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 8
- 125000003275 alpha amino acid group Chemical group 0.000 claims description 6
- 230000008685 targeting Effects 0.000 claims description 6
- VGIRNWJSIRVFRT-UHFFFAOYSA-N 2',7'-difluorofluorescein Chemical compound OC(=O)C1=CC=CC=C1C1=C2C=C(F)C(=O)C=C2OC2=CC(O)=C(F)C=C21 VGIRNWJSIRVFRT-UHFFFAOYSA-N 0.000 claims description 5
- 235000001014 amino acid Nutrition 0.000 claims description 5
- 125000001691 aryl alkyl amino group Chemical group 0.000 claims description 5
- 229910052799 carbon Inorganic materials 0.000 claims description 5
- 125000004432 carbon atom Chemical group C* 0.000 claims description 5
- GNBHRKFJIUUOQI-UHFFFAOYSA-N fluorescein Chemical compound O1C(=O)C2=CC=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 GNBHRKFJIUUOQI-UHFFFAOYSA-N 0.000 claims description 5
- PYWVYCXTNDRMGF-UHFFFAOYSA-N rhodamine B Chemical compound [Cl-].C=12C=CC(=[N+](CC)CC)C=C2OC2=CC(N(CC)CC)=CC=C2C=1C1=CC=CC=C1C(O)=O PYWVYCXTNDRMGF-UHFFFAOYSA-N 0.000 claims description 5
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims description 4
- 108010084457 Cathepsins Proteins 0.000 claims description 4
- 102000005600 Cathepsins Human genes 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 4
- 125000005236 alkanoylamino group Chemical group 0.000 claims description 4
- 125000003545 alkoxy group Chemical group 0.000 claims description 4
- 125000003282 alkyl amino group Chemical group 0.000 claims description 4
- 125000005157 alkyl carboxy group Chemical group 0.000 claims description 4
- 125000001769 aryl amino group Chemical group 0.000 claims description 4
- 125000004104 aryloxy group Chemical group 0.000 claims description 4
- 239000004202 carbamide Substances 0.000 claims description 4
- 125000001589 carboacyl group Chemical group 0.000 claims description 4
- 125000000000 cycloalkoxy group Chemical group 0.000 claims description 4
- 125000005843 halogen group Chemical group 0.000 claims description 4
- 125000005241 heteroarylamino group Chemical group 0.000 claims description 4
- 125000005553 heteroaryloxy group Chemical group 0.000 claims description 4
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 4
- 125000006239 protecting group Chemical group 0.000 claims description 4
- 239000000941 radioactive substance Substances 0.000 claims description 4
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims description 4
- 229940124530 sulfonamide Drugs 0.000 claims description 4
- 150000003456 sulfonamides Chemical class 0.000 claims description 4
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 125000004953 trihalomethyl group Chemical group 0.000 claims description 4
- 238000002372 labelling Methods 0.000 claims description 3
- 108010005843 Cysteine Proteases Proteins 0.000 claims description 2
- 102000005927 Cysteine Proteases Human genes 0.000 claims description 2
- 108091005804 Peptidases Proteins 0.000 claims description 2
- 239000004365 Protease Substances 0.000 claims description 2
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 claims description 2
- 150000001540 azides Chemical class 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 238000012800 visualization Methods 0.000 claims 1
- 238000000034 method Methods 0.000 description 8
- 108090000624 Cathepsin L Proteins 0.000 description 1
- 102000004172 Cathepsin L Human genes 0.000 description 1
- 102100026540 Cathepsin L2 Human genes 0.000 description 1
- 101000983577 Homo sapiens Cathepsin L2 Proteins 0.000 description 1
- 125000000539 amino acid group Chemical group 0.000 description 1
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022010930A JP2022044770A (ja) | 2015-01-22 | 2022-01-27 | ｉｎ ｖｉｖｏ画像化のためのプロテアーゼ活性化コントラスト剤 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562106400P | 2015-01-22 | 2015-01-22 | |
| US62/106,400 | 2015-01-22 | ||
| PCT/US2016/014606 WO2016118910A1 (en) | 2015-01-22 | 2016-01-22 | Protease-activated contrast agents for in vivo imaging |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022010930A Division JP2022044770A (ja) | 2015-01-22 | 2022-01-27 | ｉｎ ｖｉｖｏ画像化のためのプロテアーゼ活性化コントラスト剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018511556A JP2018511556A (ja) | 2018-04-26 |
| JP2018511556A5 true JP2018511556A5 (enExample) | 2019-03-07 |
| JP7017410B2 JP7017410B2 (ja) | 2022-02-08 |
Family
ID=56417841
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017538686A Active JP7017410B2 (ja) | 2015-01-22 | 2016-01-22 | ｉｎ ｖｉｖｏ画像化のためのプロテアーゼ活性化コントラスト剤 |
| JP2022010930A Pending JP2022044770A (ja) | 2015-01-22 | 2022-01-27 | ｉｎ ｖｉｖｏ画像化のためのプロテアーゼ活性化コントラスト剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022010930A Pending JP2022044770A (ja) | 2015-01-22 | 2022-01-27 | ｉｎ ｖｉｖｏ画像化のためのプロテアーゼ活性化コントラスト剤 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US10570173B2 (enExample) |
| EP (1) | EP3247802B1 (enExample) |
| JP (2) | JP7017410B2 (enExample) |
| KR (1) | KR102668593B1 (enExample) |
| CN (1) | CN107406872B (enExample) |
| WO (1) | WO2016118910A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107406872B (zh) * | 2015-01-22 | 2023-03-28 | 里兰斯坦福初级大学理事会 | 用于标记动物组织的化合物、组合物及其应用 |
| GB201617935D0 (en) | 2016-10-24 | 2016-12-07 | Queens University Of Belfast The | Binding compound and uses thereof |
| EP3510380B1 (en) | 2016-12-23 | 2023-11-08 | The Board of Trustees of the Leland Stanford Junior University | Activity-based probe compounds, compositions, and methods of use |
| EP3601261A4 (en) * | 2017-03-30 | 2021-07-14 | The Board of Trustees of the Leland Stanford Junior University | CONTRAST AGENTS ACTIVATED BY A PROTEASE FOR IN VIVO IMAGING |
| US20220105206A1 (en) * | 2020-10-02 | 2022-04-07 | Board Of Regents, The University Of Texas System | Sensitivity advances in ultrasound switchable fluorescence systems and techniques |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL60888A (en) * | 1978-06-16 | 1984-07-31 | Yeda Res & Dev | Substrates and process for the quantitative assay of enzymes |
| AU2704395A (en) | 1995-06-13 | 1997-01-09 | Sanofi Winthrop, Inc. | Calpain inhibitors for the treatment of neurodegenerative di seases |
| US7303741B2 (en) | 2002-09-23 | 2007-12-04 | General Electric Company | Systems and methods for high-resolution in vivo imaging of biochemical activity in a living organism |
| US8133482B2 (en) * | 2003-11-14 | 2012-03-13 | The Trustees Of The University Of Pennsylvania | Activatable photodynamic therapy agents |
| US20060148014A1 (en) * | 2004-12-09 | 2006-07-06 | Sergei Agoulnik | Tubulin isotype screening in cancer therapy using hemiasterlin analogs |
| US8968700B2 (en) | 2005-08-11 | 2015-03-03 | The Board Of Trustees Of The Leland Stanford Junior University | Imaging of protease activity in live cells using activity based probes |
| JP5437790B2 (ja) * | 2006-04-28 | 2014-03-12 | チルドレンズ ホスピタル メディカル センター | 膜貫通薬物送達システムに適用するためのプロサポシン由来の融合タンパク質又はポリペプチドを含む組成物 |
| CN101652149B (zh) * | 2007-02-28 | 2012-11-14 | 塞诺菲-安万特股份有限公司 | 成像探针 |
| MY162041A (en) | 2007-02-28 | 2017-05-31 | Sanofi Aventis | Imaging probes |
| WO2008139206A2 (en) * | 2007-05-16 | 2008-11-20 | Ge Healthcare As | Optical imaging agents |
| CA2695244A1 (en) * | 2007-08-03 | 2009-02-12 | Sanofi-Aventis | Caspase imaging probes |
| WO2009124265A1 (en) | 2008-04-03 | 2009-10-08 | The Board Of Trustees Of The Leland Stanford Junior University | Probes for in vivo targeting of active cysteine proteases |
| BRPI0917478A8 (pt) * | 2008-08-06 | 2017-05-23 | Univ Leland Stanford Junior | uso de beta-lactamase bacteriana para diagnóstico in vitroe geração de imagem, diagnóstico e terapêutica in vivo |
| WO2010053489A1 (en) * | 2008-11-07 | 2010-05-14 | Children's Hospital Medical Center | Fusogenic properties of saposin c and related proteins and peptides for application to transmembrane drug delivery systems |
| US9155471B2 (en) * | 2009-05-27 | 2015-10-13 | Lumicell, Inc'. | Methods and systems for spatially identifying abnormal cells |
| WO2012021800A2 (en) | 2010-08-13 | 2012-02-16 | Banyan Biomarkers | Caspase inhibitors as therapeutics for neural and organ injury and imaging |
| WO2012118715A2 (en) | 2011-02-28 | 2012-09-07 | The Board Of Trustees Of Leland Stanford Junior University | Non-peptidic quenched fluorescent imaging probes |
| US8709830B2 (en) * | 2011-03-18 | 2014-04-29 | Biotium, Inc. | Fluorescent dyes, fluorescent dye kits, and methods of preparing labeled molecules |
| WO2013036743A1 (en) | 2011-09-09 | 2013-03-14 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Imaging agents for imaging protease activity and uses thereof |
| US20140180073A1 (en) | 2012-12-24 | 2014-06-26 | Anticancer, Inc. | Portable digital imaging system for fluorescence-guided surgery |
| KR20160037834A (ko) | 2013-03-14 | 2016-04-06 | 루미셀, 아이엔씨. | 의료 이미징 장치 및 사용 방법 |
| WO2014145257A2 (en) * | 2013-03-15 | 2014-09-18 | The Board Of Trustees Of The Leland Stanford Junior University | Activity-based probe compounds, compositions, and methods of use |
| WO2014171899A1 (en) * | 2013-04-19 | 2014-10-23 | Agency For Science, Technology And Research | Tunable fluorescence using cleavable linkers |
| CN107406872B (zh) * | 2015-01-22 | 2023-03-28 | 里兰斯坦福初级大学理事会 | 用于标记动物组织的化合物、组合物及其应用 |
| EP3601261A4 (en) * | 2017-03-30 | 2021-07-14 | The Board of Trustees of the Leland Stanford Junior University | CONTRAST AGENTS ACTIVATED BY A PROTEASE FOR IN VIVO IMAGING |
-
2016
- 2016-01-22 CN CN201680017762.XA patent/CN107406872B/zh active Active
- 2016-01-22 US US15/545,689 patent/US10570173B2/en active Active
- 2016-01-22 KR KR1020177023302A patent/KR102668593B1/ko active Active
- 2016-01-22 JP JP2017538686A patent/JP7017410B2/ja active Active
- 2016-01-22 WO PCT/US2016/014606 patent/WO2016118910A1/en not_active Ceased
- 2016-01-22 EP EP16740869.9A patent/EP3247802B1/en active Active
-
2020
- 2020-02-14 US US16/792,142 patent/US20200299327A1/en not_active Abandoned
-
2022
- 2022-01-27 JP JP2022010930A patent/JP2022044770A/ja active Pending
- 2022-11-08 US US18/053,682 patent/US12459972B2/en active Active
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