JP2017530983A5 - - Google Patents
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- Publication number
- JP2017530983A5 JP2017530983A5 JP2017518541A JP2017518541A JP2017530983A5 JP 2017530983 A5 JP2017530983 A5 JP 2017530983A5 JP 2017518541 A JP2017518541 A JP 2017518541A JP 2017518541 A JP2017518541 A JP 2017518541A JP 2017530983 A5 JP2017530983 A5 JP 2017530983A5
- Authority
- JP
- Japan
- Prior art keywords
- auristatin
- pharmaceutically acceptable
- phenyl
- methyl
- acceptable salt
- 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
- DWZAEMINVBZMHQ-UHFFFAOYSA-N 1-[4-[4-(dimethylamino)piperidine-1-carbonyl]phenyl]-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea Chemical compound C1CC(N(C)C)CCN1C(=O)C(C=C1)=CC=C1NC(=O)NC1=CC=C(C=2N=C(N=C(N=2)N2CCOCC2)N2CCOCC2)C=C1 DWZAEMINVBZMHQ-UHFFFAOYSA-N 0.000 claims description 7
- 108010044540 auristatin Proteins 0.000 claims 14
- 150000003839 salts Chemical class 0.000 claims 13
- 229940124302 mTOR inhibitor Drugs 0.000 claims 11
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 11
- -1 1,3-thiazol-2-yl Chemical group 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 239000000611 antibody drug conjugate Substances 0.000 claims 5
- 229940049595 antibody-drug conjugate Drugs 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 4
- 239000003085 diluting agent Substances 0.000 claims 4
- 239000002552 dosage form Substances 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- QAAFNSMAIAVCHE-BZLYQNAUSA-N (2s)-2-[(2-amino-2-methylpropanoyl)amino]-n-[(3r,4s,5s)-3-methoxy-1-[(2s)-2-[(1r,2r)-1-methoxy-2-methyl-3-oxo-3-[[(1s)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-n,3-dimethylbutanamide Chemical compound CC(N)(C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C=1SC=CN=1)CC1=CC=CC=C1 QAAFNSMAIAVCHE-BZLYQNAUSA-N 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 1
- 239000004202 carbamide Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- NRMQEWBZFDNUHD-VKRRFRHLSA-N CC[C@H](C)[C@@H]([C@@H](CC(N(CCC1)[C@@H]1[C@@H]([C@@H](C)C(N[C@H](C)[C@H](c1ccccc1)O)=O)OC)=O)OC)N(C)C([C@@H](C(C)C)NC(C(C)(C)N)=O)=O Chemical compound CC[C@H](C)[C@@H]([C@@H](CC(N(CCC1)[C@@H]1[C@@H]([C@@H](C)C(N[C@H](C)[C@H](c1ccccc1)O)=O)OC)=O)OC)N(C)C([C@@H](C(C)C)NC(C(C)(C)N)=O)=O NRMQEWBZFDNUHD-VKRRFRHLSA-N 0.000 description 3
- BYZVPLCBAAEVLB-JQWMWWJASA-N CC[C@H](C)C(C(CC(N(CCC1)[C@@H]1/C(/C(C)C(NC(C)C(C)(c1ccccc1)O)=O)=[O]/C)=O)OC)N(C)C(/C(/C(C)C)=N/C(C(C)(C)N)=O)=O Chemical compound CC[C@H](C)C(C(CC(N(CCC1)[C@@H]1/C(/C(C)C(NC(C)C(C)(c1ccccc1)O)=O)=[O]/C)=O)OC)N(C)C(/C(/C(C)C)=N/C(C(C)(C)N)=O)=O BYZVPLCBAAEVLB-JQWMWWJASA-N 0.000 description 1
- MUJOCDBVNQNVSF-YIBJTWMJSA-N CC[C@H](C)[C@@H]([C@@H](CC(N(CCC1)[C@@H]1[C@@H]([C@@H](C)C(N[C@H](C)[C@H](c1ccccc1)O)=O)OC)=O)OC)N(C)C(CC(C)C/[O]=C(/C(C)(C)N)\N)=O Chemical compound CC[C@H](C)[C@@H]([C@@H](CC(N(CCC1)[C@@H]1[C@@H]([C@@H](C)C(N[C@H](C)[C@H](c1ccccc1)O)=O)OC)=O)OC)N(C)C(CC(C)C/[O]=C(/C(C)(C)N)\N)=O MUJOCDBVNQNVSF-YIBJTWMJSA-N 0.000 description 1
- 0 CN(C)C(CC1)CCN1C(C(C=C1)=CCC1NC(Nc(cc1)ccc1-c1nc(N2CCOCC2)nc(N2CCOCC2)n1)=O)=* Chemical compound CN(C)C(CC1)CCN1C(C(C=C1)=CCC1NC(Nc(cc1)ccc1-c1nc(N2CCOCC2)nc(N2CCOCC2)n1)=O)=* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462062192P | 2014-10-10 | 2014-10-10 | |
| US62/062,192 | 2014-10-10 | ||
| PCT/IB2015/057457 WO2016055907A1 (en) | 2014-10-10 | 2015-09-29 | Synergistic auristatin combinations |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017530983A JP2017530983A (ja) | 2017-10-19 |
| JP2017530983A5 true JP2017530983A5 (Direct) | 2018-11-08 |
| JP6784668B2 JP6784668B2 (ja) | 2020-11-11 |
Family
ID=54288858
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017518541A Active JP6784668B2 (ja) | 2014-10-10 | 2015-09-29 | 相乗的オーリスタチン組合せ |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US10617670B2 (Direct) |
| EP (2) | EP3204005A1 (Direct) |
| JP (1) | JP6784668B2 (Direct) |
| KR (1) | KR20170058432A (Direct) |
| CN (1) | CN107106685A (Direct) |
| AU (1) | AU2015329625B2 (Direct) |
| BR (1) | BR112017006113A8 (Direct) |
| CA (1) | CA2907878A1 (Direct) |
| IL (1) | IL251619B (Direct) |
| MX (1) | MX2017004580A (Direct) |
| RU (1) | RU2717570C2 (Direct) |
| WO (1) | WO2016055907A1 (Direct) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9765220B2 (en) | 2013-08-22 | 2017-09-19 | Sony Corporation | Water soluble fluorescent or colored dyes and methods for their use |
| RU2762328C2 (ru) | 2016-04-01 | 2021-12-17 | Сони Корпорейшн | Ультраяркие димерные или полимерные красители |
| KR20180133890A (ko) | 2016-04-06 | 2018-12-17 | 소니 주식회사 | 스페이싱 링커 그룹을 포함하는 초고명도 이량체성 또는 중합체성 염료 |
| US11685835B2 (en) | 2016-05-11 | 2023-06-27 | Sony Corporation | Ultra bright dimeric or polymeric dyes |
| JP7312929B2 (ja) | 2016-07-29 | 2023-07-24 | ソニーグループ株式会社 | 超明色二量体またはポリマー色素およびその調製のための方法 |
| CN111315415A (zh) * | 2017-10-05 | 2020-06-19 | 索尼公司 | 可编程的聚合药物 |
| WO2019071153A1 (en) | 2017-10-05 | 2019-04-11 | Sony Corporation | PROGRAMMABLE DENDRITIC MEDICINES |
| WO2019088176A1 (ja) * | 2017-10-31 | 2019-05-09 | 国立大学法人神戸大学 | 抗体薬物複合体効果増強剤 |
| CN111836645A (zh) | 2017-11-16 | 2020-10-27 | 索尼公司 | 可编程的聚合药物 |
| CN111712511B (zh) * | 2017-11-30 | 2024-07-16 | 拉德克斯公司 | 澳瑞他汀e衍生物的白蛋白结合产物 |
| JP7515785B2 (ja) | 2018-01-12 | 2024-07-16 | ソニーグループ株式会社 | 生物学的に活性な化合物を含むホスホアルキルポリマー |
| EP4616912A3 (en) | 2018-01-12 | 2025-11-19 | Sony Group Corporation | Phosphoalkyl ribose polymers comprising biologically active compounds |
| US12076407B2 (en) | 2018-01-12 | 2024-09-03 | Sony Group Corporation | Polymers with rigid spacing groups comprising biologically active compounds |
| US11874280B2 (en) | 2018-03-19 | 2024-01-16 | Sony Group Corporation | Use of divalent metals for enhancement of fluorescent signals |
| WO2019182766A1 (en) | 2018-03-21 | 2019-09-26 | Sony Corporation | Polymeric tandem dyes with linker groups |
| EP3814366A1 (en) | 2018-06-27 | 2021-05-05 | Sony Corporation | Polymeric dyes with linker groups comprising deoxyribose |
| EP3861074A2 (en) | 2019-09-26 | 2021-08-11 | Sony Group Corporation | Polymeric tandem dyes with linker groups |
| JP7556194B2 (ja) * | 2019-12-13 | 2024-09-26 | Ｔｏｐｐａｎホールディングス株式会社 | 細胞構造体及びその使用 |
| US20240132725A1 (en) | 2020-12-07 | 2024-04-25 | Sony Group Corporation | Spacing linker group design for brightness enhancement in dimeric or polymeric dyes |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7696231B2 (en) | 2001-10-30 | 2010-04-13 | Laboratoires Serono Sa | Oxindole hydrazide modulators of protein tyrosine phosphatases (PTPs) |
| US7196090B2 (en) | 2002-07-25 | 2007-03-27 | Warner-Lambert Company | Kinase inhibitors |
| PT1725249E (pt) * | 2003-11-06 | 2014-04-10 | Seattle Genetics Inc | Compostos de monometilvalina capazes de conjugação a ligandos |
| JP2009506790A (ja) * | 2005-09-07 | 2009-02-19 | メディミューン，エルエルシー | 毒素とコンジュゲートしたｅｐｈ受容体抗体 |
| WO2008002578A2 (en) | 2006-06-26 | 2008-01-03 | Nielsen Media Research, Inc. | Methods and apparatus for improving data warehouse performance |
| ES2366489T3 (es) | 2006-09-15 | 2011-10-20 | Pfizer Products Inc. | Compuesto de pirido (2,3-d) piridinona y sus uso como inhibidores de pi3. |
| EP2144628B1 (en) * | 2007-05-08 | 2012-10-17 | Genentech, Inc. | Cysteine engineered anti-muc16 antibodies and antibody drug conjugates |
| CN101815532B (zh) | 2007-10-02 | 2012-08-15 | 中外制药株式会社 | 以白细胞介素6受体抑制剂为有效成分的移植物抗宿主病治疗剂 |
| WO2009143313A1 (en) | 2008-05-23 | 2009-11-26 | Wyeth | Triazine compounds as p13 kinase and mtor inhibitors |
| CN103068406B (zh) * | 2010-06-08 | 2017-06-30 | 基因泰克公司 | 半胱氨酸改造的抗体和偶联物 |
| ES2730941T7 (es) * | 2010-10-22 | 2020-05-27 | Seattle Genetics Inc | Efectos sinérgicos entre los conjugados de conjugados anticuerpo-fármaco a base de auristatina e inhibidores de la ruta PI3K-AKT-mTOR |
| JP5925875B2 (ja) | 2011-04-01 | 2016-05-25 | ワイス・エルエルシー | 抗体−薬剤コンジュゲート |
| AU2012328980A1 (en) * | 2011-10-28 | 2014-04-24 | Genentech, Inc. | Therapeutic combinations and methods of treating melanoma |
| ES2657014T3 (es) * | 2011-11-17 | 2018-03-01 | Pfizer Inc. | Péptidos citotóxicos y conjugados de fármaco anticuerpo de los mismos |
| EP2917240A1 (en) * | 2012-11-07 | 2015-09-16 | Pfizer Inc. | Anti-notch3 antibodies and antibody-drug conjugates |
| EP3711780A3 (en) * | 2014-04-30 | 2020-12-09 | Pfizer Inc | Anti-ptk7 antibody-drug conjugates |
-
2015
- 2015-09-29 AU AU2015329625A patent/AU2015329625B2/en not_active Ceased
- 2015-09-29 WO PCT/IB2015/057457 patent/WO2016055907A1/en not_active Ceased
- 2015-09-29 US US15/516,780 patent/US10617670B2/en active Active
- 2015-09-29 BR BR112017006113A patent/BR112017006113A8/pt not_active Application Discontinuation
- 2015-09-29 EP EP15778051.1A patent/EP3204005A1/en not_active Withdrawn
- 2015-09-29 CN CN201580054253.XA patent/CN107106685A/zh active Pending
- 2015-09-29 JP JP2017518541A patent/JP6784668B2/ja active Active
- 2015-09-29 KR KR1020177010980A patent/KR20170058432A/ko not_active Ceased
- 2015-09-29 RU RU2017112048A patent/RU2717570C2/ru active
- 2015-09-29 MX MX2017004580A patent/MX2017004580A/es unknown
- 2015-09-29 EP EP19170411.3A patent/EP3549583A1/en not_active Withdrawn
- 2015-10-07 CA CA2907878A patent/CA2907878A1/en active Pending
-
2017
- 2017-04-06 IL IL251619A patent/IL251619B/en active IP Right Grant
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