JP2012506408A5 - - Google Patents
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- JP2012506408A5 JP2012506408A5 JP2011532704A JP2011532704A JP2012506408A5 JP 2012506408 A5 JP2012506408 A5 JP 2012506408A5 JP 2011532704 A JP2011532704 A JP 2011532704A JP 2011532704 A JP2011532704 A JP 2011532704A JP 2012506408 A5 JP2012506408 A5 JP 2012506408A5
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- JP
- Japan
- Prior art keywords
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- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 21
- 235000001014 amino acid Nutrition 0.000 claims 9
- 229940024606 amino acid Drugs 0.000 claims 9
- 150000001413 amino acids Chemical class 0.000 claims 9
- 239000004066 vascular targeting agent Substances 0.000 claims 6
- 108010000684 Matrix Metalloproteinases Proteins 0.000 claims 5
- 102000002274 Matrix Metalloproteinases Human genes 0.000 claims 5
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 4
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 4
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 4
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 4
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 4
- 125000000539 amino acid group Chemical group 0.000 claims 4
- 235000005772 leucine Nutrition 0.000 claims 4
- 230000007026 protein scission Effects 0.000 claims 4
- 235000004400 serine Nutrition 0.000 claims 4
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 3
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims 3
- 239000004473 Threonine Substances 0.000 claims 3
- 102000004243 Tubulin Human genes 0.000 claims 3
- 108090000704 Tubulin Proteins 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 108090000765 processed proteins & peptides Proteins 0.000 claims 3
- 230000006337 proteolytic cleavage Effects 0.000 claims 3
- 235000008521 threonine Nutrition 0.000 claims 3
- IAKHMKGGTNLKSZ-INIZCTEOSA-N (S)-colchicine Chemical compound C1([C@@H](NC(C)=O)CC2)=CC(=O)C(OC)=CC=C1C1=C2C=C(OC)C(OC)=C1OC IAKHMKGGTNLKSZ-INIZCTEOSA-N 0.000 claims 2
- 239000004475 Arginine Substances 0.000 claims 2
- 239000004471 Glycine Substances 0.000 claims 2
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims 2
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 2
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims 2
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 2
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 2
- 239000004472 Lysine Substances 0.000 claims 2
- 235000004279 alanine Nutrition 0.000 claims 2
- 235000009697 arginine Nutrition 0.000 claims 2
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 2
- 235000003704 aspartic acid Nutrition 0.000 claims 2
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims 2
- 239000011230 binding agent Substances 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000002209 hydrophobic effect Effects 0.000 claims 2
- 229960000310 isoleucine Drugs 0.000 claims 2
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims 2
- 235000018977 lysine Nutrition 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 235000002374 tyrosine Nutrition 0.000 claims 2
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 2
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 1
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 claims 1
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 1
- JTTHKOPSMAVJFE-VIFPVBQESA-N L-homophenylalanine Chemical compound OC(=O)[C@@H](N)CCC1=CC=CC=C1 JTTHKOPSMAVJFE-VIFPVBQESA-N 0.000 claims 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 1
- FFEARJCKVFRZRR-BYPYZUCNSA-N L-methionine Chemical compound CSCC[C@H](N)C(O)=O FFEARJCKVFRZRR-BYPYZUCNSA-N 0.000 claims 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 1
- QIVBCDIJIAJPQS-VIFPVBQESA-N L-tryptophane Chemical compound C1=CC=C2C(C[C@H](N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-VIFPVBQESA-N 0.000 claims 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 1
- 108010076557 Matrix Metalloproteinase 14 Proteins 0.000 claims 1
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 1
- QIVBCDIJIAJPQS-UHFFFAOYSA-N Tryptophan Natural products C1=CC=C2C(CC(N)C(O)=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-N 0.000 claims 1
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 1
- 230000002378 acidificating effect Effects 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 235000009582 asparagine Nutrition 0.000 claims 1
- 229960001230 asparagine Drugs 0.000 claims 1
- 229960001338 colchicine Drugs 0.000 claims 1
- 239000007822 coupling agent Substances 0.000 claims 1
- 235000018417 cysteine Nutrition 0.000 claims 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 235000013922 glutamic acid Nutrition 0.000 claims 1
- 239000004220 glutamic acid Substances 0.000 claims 1
- 229930182817 methionine Natural products 0.000 claims 1
- 230000000269 nucleophilic effect Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 239000004474 valine Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0819287.4A GB0819287D0 (en) | 2008-10-22 | 2008-10-22 | Compounds |
| GB0819287.4 | 2008-10-22 | ||
| PCT/GB2009/002484 WO2010046628A1 (en) | 2008-10-22 | 2009-10-20 | Compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012506408A JP2012506408A (ja) | 2012-03-15 |
| JP2012506408A5 true JP2012506408A5 (enExample) | 2012-12-06 |
| JP5820272B2 JP5820272B2 (ja) | 2015-11-24 |
Family
ID=40097772
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011532704A Expired - Fee Related JP5820272B2 (ja) | 2008-10-22 | 2009-10-20 | 化合物 |
Country Status (18)
| Country | Link |
|---|---|
| US (5) | US8927486B2 (enExample) |
| EP (2) | EP3446715A1 (enExample) |
| JP (1) | JP5820272B2 (enExample) |
| CN (2) | CN102143762B (enExample) |
| CA (1) | CA2741475A1 (enExample) |
| CY (1) | CY1121309T1 (enExample) |
| DK (1) | DK2349344T5 (enExample) |
| ES (1) | ES2714590T3 (enExample) |
| GB (1) | GB0819287D0 (enExample) |
| HR (1) | HRP20190437T8 (enExample) |
| HU (1) | HUE042688T2 (enExample) |
| LT (1) | LT2349344T (enExample) |
| PL (1) | PL2349344T3 (enExample) |
| PT (1) | PT2349344T (enExample) |
| SI (1) | SI2349344T1 (enExample) |
| SM (1) | SMT201900127T1 (enExample) |
| TR (1) | TR201902884T4 (enExample) |
| WO (1) | WO2010046628A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0707034D0 (en) | 2007-04-12 | 2007-05-23 | St Andrews The | Compounds |
| GB0819287D0 (en) | 2008-10-22 | 2008-11-26 | Univ Bradford | Compounds |
| JP6356684B2 (ja) | 2012-11-02 | 2018-07-11 | マレイ・アンド・プール・エンタープライゼズ・リミテッド | コルヒチン誘導体の投与による心血管イベントの処置または予防 |
| EA037375B1 (ru) | 2013-04-16 | 2021-03-22 | Марри Энд Пул Энтерпрайзес Лимитед | Составы с замедленным высвобождением, содержащие колхицин, и способы их применения |
| GB2516882A (en) * | 2013-08-02 | 2015-02-11 | Univ Bradford | Tumour-targeted theranostic |
| CA2925106C (en) | 2013-09-25 | 2023-11-14 | Cytomx Therapeutics, Inc. | Matrix metalloproteinase substrates and other cleavable moieties and methods of use thereof |
| EP4176896B1 (en) | 2014-01-31 | 2025-10-08 | Cytomx Therapeutics, Inc. | Matriptase and u-plasminogen activator substrates and other cleavable moieties and methods of use thereof |
| IL300408B2 (en) | 2015-01-20 | 2025-11-01 | Cytomx Therapeutics Inc | Matrix metalloprotease-cleavable and serine protease cleavable substrates and methods of use thereof |
| GB2545169B (en) * | 2015-12-01 | 2019-10-09 | Ellipses Pharma Ltd | Taxane Prodrug Comprising A Membrane Type Matrix Metalloproteinase Cleavage Site |
| MY205459A (en) | 2018-12-06 | 2024-10-22 | Cytomx Therapeutics Inc | Matrix metalloprotease-cleavable and serine or cysteine protease-cleavable substrates and methods of use thereof |
| CN115353534B (zh) * | 2021-12-31 | 2024-06-07 | 郑州大学第一附属医院 | 一种秋水仙碱衍生物及其制备和其应用 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US819287A (en) * | 1905-09-11 | 1906-05-01 | Caesar Klaus | Automatic brake. |
| US5595756A (en) * | 1993-12-22 | 1997-01-21 | Inex Pharmaceuticals Corporation | Liposomal compositions for enhanced retention of bioactive agents |
| US6844318B2 (en) * | 2000-03-15 | 2005-01-18 | Bristol Myers Squibb Pharma Company | Peptidase-cleavable, targeted antineoplastic drugs and their therapeutic use |
| GB0018240D0 (en) | 2000-07-25 | 2000-09-13 | Pharmacia & Upjohn Spa | Polymeric conjugates of antitumor agents |
| GB0105929D0 (en) | 2001-03-09 | 2001-04-25 | Btg Int Ltd | Physiologically activated prodrugs |
| SI1545613T1 (sl) | 2002-07-31 | 2011-11-30 | Seattle Genetics Inc | Avristatinski konjugati in njihova uporaba za zdravljenje raka avtoimunske bolezni ali infekcijskebolezni |
| US20050106100A1 (en) * | 2003-09-03 | 2005-05-19 | Harris Thomas D. | Compounds containing matrix metalloproteinase substrates and methods of their use |
| GB0320691D0 (en) * | 2003-09-04 | 2003-10-01 | Smith & Nephew | Use of joint lining cells for articular cartilage repair |
| US8420603B2 (en) * | 2004-05-14 | 2013-04-16 | Abraxis Bioscience, Llc | SPARC and methods of use thereof |
| CN101146826A (zh) | 2005-01-24 | 2008-03-19 | 得克萨斯大学体系董事会 | 与磷脂酰丝氨酸结合的fc融合构建体及其治疗用途 |
| WO2006090813A1 (ja) | 2005-02-25 | 2006-08-31 | National University Corporation Hokkaido University | 腫瘍組織で選択的に分解性を示す血中滞留性素子 |
| US7714016B2 (en) * | 2005-04-08 | 2010-05-11 | Medarex, Inc. | Cytotoxic compounds and conjugates with cleavable substrates |
| GB0707034D0 (en) | 2007-04-12 | 2007-05-23 | St Andrews The | Compounds |
| GB0819287D0 (en) | 2008-10-22 | 2008-11-26 | Univ Bradford | Compounds |
-
2008
- 2008-10-22 GB GBGB0819287.4A patent/GB0819287D0/en not_active Ceased
-
2009
- 2009-10-20 LT LTEP09760548.9T patent/LT2349344T/lt unknown
- 2009-10-20 PL PL09760548T patent/PL2349344T3/pl unknown
- 2009-10-20 HU HUE09760548A patent/HUE042688T2/hu unknown
- 2009-10-20 WO PCT/GB2009/002484 patent/WO2010046628A1/en not_active Ceased
- 2009-10-20 JP JP2011532704A patent/JP5820272B2/ja not_active Expired - Fee Related
- 2009-10-20 CA CA2741475A patent/CA2741475A1/en not_active Abandoned
- 2009-10-20 TR TR2019/02884T patent/TR201902884T4/tr unknown
- 2009-10-20 CN CN200980141703.3A patent/CN102143762B/zh not_active Expired - Fee Related
- 2009-10-20 EP EP18194638.5A patent/EP3446715A1/en not_active Withdrawn
- 2009-10-20 DK DK09760548.9T patent/DK2349344T5/en active
- 2009-10-20 EP EP09760548.9A patent/EP2349344B1/en active Active
- 2009-10-20 HR HRP20190437TT patent/HRP20190437T8/hr unknown
- 2009-10-20 SI SI200931938T patent/SI2349344T1/sl unknown
- 2009-10-20 CN CN201410401756.7A patent/CN104193802B/zh not_active Expired - Fee Related
- 2009-10-20 ES ES09760548T patent/ES2714590T3/es active Active
- 2009-10-20 PT PT09760548T patent/PT2349344T/pt unknown
- 2009-10-20 SM SM20190127T patent/SMT201900127T1/it unknown
- 2009-10-20 US US13/125,732 patent/US8927486B2/en not_active Expired - Fee Related
-
2014
- 2014-11-25 US US14/553,803 patent/US20150196658A1/en not_active Abandoned
-
2016
- 2016-10-19 US US15/297,649 patent/US9937267B2/en active Active
-
2018
- 2018-03-01 US US15/909,475 patent/US10912839B2/en not_active Expired - Fee Related
-
2019
- 2019-02-27 CY CY20191100241T patent/CY1121309T1/el unknown
-
2020
- 2020-06-19 US US16/946,391 patent/US20200316212A1/en not_active Abandoned
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