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 (OSRAM) | 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 (OSRAM) |
| EP (2) | EP3204005A1 (OSRAM) |
| JP (1) | JP6784668B2 (OSRAM) |
| KR (1) | KR20170058432A (OSRAM) |
| CN (1) | CN107106685A (OSRAM) |
| AU (1) | AU2015329625B2 (OSRAM) |
| BR (1) | BR112017006113A8 (OSRAM) |
| CA (1) | CA2907878A1 (OSRAM) |
| IL (1) | IL251619B (OSRAM) |
| MX (1) | MX2017004580A (OSRAM) |
| RU (1) | RU2717570C2 (OSRAM) |
| WO (1) | WO2016055907A1 (OSRAM) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3019559A4 (en) | 2013-08-22 | 2017-04-05 | Sony Corporation | Water soluble fluorescent or colored dyes and methods for their use |
| KR102530707B1 (ko) | 2016-04-01 | 2023-05-11 | 소니그룹주식회사 | 초휘도 이량체성 또는 중합체성 염료 |
| KR20180133890A (ko) | 2016-04-06 | 2018-12-17 | 소니 주식회사 | 스페이싱 링커 그룹을 포함하는 초고명도 이량체성 또는 중합체성 염료 |
| EP3455300A1 (en) | 2016-05-11 | 2019-03-20 | Sony Corporation | Ultra bright dimeric or polymeric dyes |
| US12018159B2 (en) | 2016-07-29 | 2024-06-25 | Sony Group Corporation | Ultra bright dimeric or polymeric dyes and methods for preparation of the same |
| EP3691689A1 (en) | 2017-10-05 | 2020-08-12 | Sony Corporation | Programmable dendritic drugs |
| JP7551056B2 (ja) | 2017-10-05 | 2024-09-17 | ソニーグループ株式会社 | プログラマブルなポリマー薬物 |
| 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 |
| AU2018375787B2 (en) * | 2017-11-30 | 2023-02-23 | Ladrx Corporation | Albumin-binding prodrugs of auristatin E derivatives |
| WO2019140301A1 (en) | 2018-01-12 | 2019-07-18 | Sony Corporation | Polymers with rigid spacing groups comprising biologically active compounds |
| EP4616912A3 (en) | 2018-01-12 | 2025-11-19 | Sony Group Corporation | Phosphoalkyl ribose polymers comprising biologically active compounds |
| KR102742386B1 (ko) | 2018-03-19 | 2024-12-16 | 소니그룹주식회사 | 형광 신호 향상을 위한 2가 금속의 사용 |
| WO2019182766A1 (en) | 2018-03-21 | 2019-09-26 | Sony Corporation | Polymeric tandem dyes with linker groups |
| KR102854332B1 (ko) | 2018-06-27 | 2025-09-03 | 소니그룹주식회사 | 디옥시리보오스를 포함하는 링커 군을 갖는 중합체성 염료 |
| KR102486779B1 (ko) | 2019-09-26 | 2023-01-12 | 소니그룹주식회사 | 링커 그룹을 갖는 중합체성 탠덤 염료 |
| 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 |
| EP4256078A1 (en) | 2020-12-07 | 2023-10-11 | 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 |
|---|---|---|---|---|
| JP4846978B2 (ja) | 2001-10-30 | 2011-12-28 | メルク セローノ ソシエテ アノニム | タンパク質チロシンホスファターゼのオキシンドールヒドラジンモジュレータ |
| PA8577501A1 (es) | 2002-07-25 | 2004-02-07 | Warner Lambert Co | Inhibidores de quinasas |
| NZ583292A (en) * | 2003-11-06 | 2012-03-30 | Seattle Genetics Inc | Monomethylvaline compounds capable of conjugation to ligands |
| CA2621502A1 (en) * | 2005-09-07 | 2007-03-15 | Medimmune, Inc. | Toxin conjugated eph receptor antibodies |
| CN101542478B (zh) | 2006-06-26 | 2012-07-18 | 尼尔森（美国）有限公司 | 提高数据仓库性能的方法和装置 |
| HRP20110621T2 (hr) | 2006-09-15 | 2013-12-06 | Pfizer Products Inc. | SPOJEVI PIRIDO[2,3-d]PIRIMIDINONA I NJIHOVA UPOTREBA KAO INHIBITORI PI3 |
| CL2008001334A1 (es) * | 2007-05-08 | 2008-09-22 | Genentech Inc | Anticuerpo anti-muc16 disenado con cisteina; conjugado que lo comprende; metodo de produccion; formulacion farmaceutica que lo comprende; y su uso para tratar el cancer. |
| KR101601986B1 (ko) | 2007-10-02 | 2016-03-17 | 추가이 세이야쿠 가부시키가이샤 | 인터류킨 6 수용체 저해제를 유효 성분으로 하는 이식편대숙주병 치료제 |
| EP2300483A1 (en) * | 2008-05-23 | 2011-03-30 | Wyeth LLC | Triazine compounds as p13 kinase and mtor inhibitors |
| JP2013534520A (ja) * | 2010-06-08 | 2013-09-05 | ジェネンテック， インコーポレイテッド | システイン操作抗体及びコンジュゲート |
| ES3004351T3 (en) | 2010-10-22 | 2025-03-12 | Seagen Inc | Synergistic effects between auristatin-based antibody drug conjugates and inhibitors of the pi3k-akt mtor pathway |
| ES2596194T3 (es) | 2011-04-01 | 2017-01-05 | Wyeth Llc | Conjugados de anticuerpo-fármaco |
| CA2850034A1 (en) * | 2011-10-28 | 2013-05-02 | Genentech, Inc. | Therapeutic combinations and methods of treating melanoma |
| PT3327027T (pt) * | 2011-11-17 | 2021-02-15 | Pfizer | Péptidos citotóxicos e seus conjugados de anticorpos e fármacos |
| BR112015010436A2 (pt) * | 2012-11-07 | 2017-08-22 | Pfizer | Anticorpos anti-notch3 e conjugados anticorpo-fármaco |
| PT3137114T (pt) * | 2014-04-30 | 2021-02-26 | Pfizer | Conjugados anticorpo-fármaco anti-ptk7 |
-
2015
- 2015-09-29 US US15/516,780 patent/US10617670B2/en active Active
- 2015-09-29 CN CN201580054253.XA patent/CN107106685A/zh active Pending
- 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 JP JP2017518541A patent/JP6784668B2/ja active Active
- 2015-09-29 EP EP19170411.3A patent/EP3549583A1/en not_active Withdrawn
- 2015-09-29 WO PCT/IB2015/057457 patent/WO2016055907A1/en not_active Ceased
- 2015-09-29 MX MX2017004580A patent/MX2017004580A/es unknown
- 2015-09-29 KR KR1020177010980A patent/KR20170058432A/ko not_active Ceased
- 2015-09-29 AU AU2015329625A patent/AU2015329625B2/en not_active Ceased
- 2015-09-29 RU RU2017112048A patent/RU2717570C2/ru active
- 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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