JP2017525755A5 - - Google Patents
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- JP2017525755A5 JP2017525755A5 JP2017519448A JP2017519448A JP2017525755A5 JP 2017525755 A5 JP2017525755 A5 JP 2017525755A5 JP 2017519448 A JP2017519448 A JP 2017519448A JP 2017519448 A JP2017519448 A JP 2017519448A JP 2017525755 A5 JP2017525755 A5 JP 2017525755A5
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- JP
- Japan
- Prior art keywords
- cancer
- amino acid
- linker
- compound according
- optionally
- 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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- 125000005647 linker group Chemical group 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 20
- 150000001413 amino acids Chemical group 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 10
- 239000012453 solvate Substances 0.000 claims 9
- 125000000539 amino acid group Chemical group 0.000 claims 7
- 108090000765 processed proteins & peptides Proteins 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 125000006850 spacer group Chemical group 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
- 239000004472 Lysine Substances 0.000 claims 4
- NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-N 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
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- 125000002252 acyl group Chemical group 0.000 claims 2
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- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
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- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
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- ALBODLTZUXKBGZ-JUUVMNCLSA-N (2s)-2-amino-3-phenylpropanoic acid;(2s)-2,6-diaminohexanoic acid Chemical compound NCCCC[C@H](N)C(O)=O.OC(=O)[C@@H](N)CC1=CC=CC=C1 ALBODLTZUXKBGZ-JUUVMNCLSA-N 0.000 claims 1
- DLGAUVSRZXNATA-DHYYHALDSA-N (2s,3s)-2-amino-3-methylpentanoic acid;(2s)-pyrrolidine-2-carboxylic acid Chemical compound OC(=O)[C@@H]1CCCN1.CC[C@H](C)[C@H](N)C(O)=O DLGAUVSRZXNATA-DHYYHALDSA-N 0.000 claims 1
- 239000004475 Arginine Substances 0.000 claims 1
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims 1
- KDXKERNSBIXSRK-RXMQYKEDSA-N D-lysine Chemical compound NCCCC[C@@H](N)C(O)=O KDXKERNSBIXSRK-RXMQYKEDSA-N 0.000 claims 1
- 108010016626 Dipeptides Proteins 0.000 claims 1
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-Ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 claims 1
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-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
- RHGKLRLOHDJJDR-BYPYZUCNSA-N L-citrulline Chemical compound NC(=O)NCCC[C@H]([NH3+])C([O-])=O RHGKLRLOHDJJDR-BYPYZUCNSA-N 0.000 claims 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 1
- AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims 1
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-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
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 1
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 1
- AHLPHDHHMVZTML-UHFFFAOYSA-N Orn-delta-NH2 Natural products NCCCC(N)C(O)=O AHLPHDHHMVZTML-UHFFFAOYSA-N 0.000 claims 1
- UTJLXEIPEHZYQJ-UHFFFAOYSA-N Ornithine Natural products OC(=O)C(C)CCCN UTJLXEIPEHZYQJ-UHFFFAOYSA-N 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 1
- 206010062122 Testicular choriocarcinoma Diseases 0.000 claims 1
- 206010057644 Testis cancer Diseases 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
- 239000008186 active pharmaceutical agent Substances 0.000 claims 1
- 235000004279 alanine Nutrition 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 229960003121 arginine Drugs 0.000 claims 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims 1
- 125000000637 arginyl group Chemical group N[C@@H](CCCNC(N)=N)C(=O)* 0.000 claims 1
- 229960001230 asparagine Drugs 0.000 claims 1
- 235000009582 asparagine Nutrition 0.000 claims 1
- 208000014911 choriocarcinoma of testis Diseases 0.000 claims 1
- 201000000336 choriocarcinoma of the testis Diseases 0.000 claims 1
- ONCCWDRMOZMNSM-FBCQKBJTSA-N compound Z Chemical compound N1=C2C(=O)NC(N)=NC2=NC=C1C(=O)[C@H]1OP(O)(=O)OC[C@H]1O ONCCWDRMOZMNSM-FBCQKBJTSA-N 0.000 claims 1
- AMRJKAQTDDKMCE-UHFFFAOYSA-N dolastatin Chemical compound CC(C)C(N(C)C)C(=O)NC(C(C)C)C(=O)N(C)C(C(C)C)C(OC)CC(=O)N1CCCC1C(OC)C(C)C(=O)NC(C=1SC=CN=1)CC1=CC=CC=C1 AMRJKAQTDDKMCE-UHFFFAOYSA-N 0.000 claims 1
- 229930188854 dolastatin Natural products 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229940088679 drug related substance Drugs 0.000 claims 1
- VQNATVDKACXKTF-XELLLNAOSA-N duocarmycin Chemical compound COC1=C(OC)C(OC)=C2NC(C(=O)N3C4=CC(=O)C5=C([C@@]64C[C@@H]6C3)C=C(N5)C(=O)OC)=CC2=C1 VQNATVDKACXKTF-XELLLNAOSA-N 0.000 claims 1
- 229960005501 duocarmycin Drugs 0.000 claims 1
- 229930184221 duocarmycin Natural products 0.000 claims 1
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 claims 1
- 229960002743 glutamine Drugs 0.000 claims 1
- 229960002885 histidine Drugs 0.000 claims 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims 1
- 229960000310 isoleucine Drugs 0.000 claims 1
- AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims 1
- 229930182817 methionine Natural products 0.000 claims 1
- 229960003104 ornithine Drugs 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 229960002087 pertuzumab Drugs 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
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 239000002904 solvent Substances 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
- 201000003120 testicular cancer Diseases 0.000 claims 1
- 229960000575 trastuzumab Drugs 0.000 claims 1
- -1 tubricin Chemical compound 0.000 claims 1
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462014912P | 2014-06-20 | 2014-06-20 | |
| US62/014,912 | 2014-06-20 | ||
| US201462015661P | 2014-06-23 | 2014-06-23 | |
| US62/015,661 | 2014-06-23 | ||
| PCT/US2015/036414 WO2015195904A1 (en) | 2014-06-20 | 2015-06-18 | Her2 antibody-drug conjugates |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017525755A JP2017525755A (ja) | 2017-09-07 |
| JP2017525755A5 true JP2017525755A5 (cg-RX-API-DMAC7.html) | 2018-07-26 |
Family
ID=54936097
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017519448A Pending JP2017525755A (ja) | 2014-06-20 | 2015-06-18 | Ｈｅｒ２抗体−薬物抱合体 |
Country Status (16)
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10953106B2 (en) | 2015-02-16 | 2021-03-23 | Lonza Ltd | Antibodies |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6180408B2 (ja) | 2011-06-13 | 2017-08-16 | アブゲノミクス コーペラティフ ユー．エー． | 抗ｐｓｇｌ−１抗体およびその使用 |
| BR112015014712A2 (pt) | 2012-12-21 | 2017-07-11 | Abgenomics Int Inc | ligadores de autoimolação hidrofílicos e seus conjugados |
| AU2015276821A1 (en) | 2014-06-20 | 2017-01-12 | Abgenomics International Inc. | Anti-folate receptor aplha (FRA) antibody-drug conjugates and methods of using thereof |
| KR102793098B1 (ko) * | 2015-06-29 | 2025-04-09 | 이뮤노젠 아이엔씨 | 시스테인 조작된 항체의 콘주게이트 |
| AU2016363013B2 (en) | 2015-12-04 | 2022-03-10 | Seagen Inc. | Conjugates of quaternized tubulysin compounds |
| US11793880B2 (en) | 2015-12-04 | 2023-10-24 | Seagen Inc. | Conjugates of quaternized tubulysin compounds |
| ES2817751T3 (es) * | 2015-12-21 | 2021-04-08 | Pfizer | Purificación de conjugados de anticuerpo-fármaco mediante el uso de un gradiente de fosfato de sodio |
| IL260289B (en) | 2016-01-08 | 2022-08-01 | Bioalliance Cv | Tetravalent anti-psgl-1 antibodies and uses thereof |
| CN107029244B (zh) * | 2016-02-04 | 2021-04-27 | 浙江昭华生物医药有限公司 | 抗her2抗体-药物偶联物及其应用 |
| MX2019010028A (es) * | 2017-02-28 | 2019-10-14 | Seattle Genetics Inc | Anticuerpos con cisteina mutada por conjugacion. |
| KR20190125310A (ko) | 2017-03-10 | 2019-11-06 | 퀴아펙 파마슈티칼스 에이비 | 방출가능한 접합체 |
| JP7073487B2 (ja) * | 2017-06-16 | 2022-05-23 | イーライ リリー アンド カンパニー | 操作された抗体化合物およびこれらの抱合体 |
| SG10201801219VA (en) | 2018-02-13 | 2019-09-27 | Agency Science Tech & Res | Anti-HER2 Antibodies |
| EP3762037B1 (en) * | 2018-03-09 | 2023-12-27 | QuiaPEG Pharmaceuticals AB | Releasable antibody conjugates |
| EP3833690B1 (en) * | 2018-08-08 | 2024-03-27 | ImmuneOnco Biopharmaceuticals (Shanghai) Inc. | Recombinant bifunctional protein targeting cd47 and her2 |
| CA3112043A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| TWI834720B (zh) | 2018-09-12 | 2024-03-11 | 瑞典商奎亞培格製藥公司 | 可釋放glp-1共軛物 |
| KR20220003506A (ko) * | 2019-03-22 | 2022-01-10 | 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 | 표적 분자의 변형을 위한 조성물 및 방법 |
| AU2021232625A1 (en) * | 2020-03-05 | 2022-09-29 | Umc Utrecht Holding B.V. | Membrane ubiquitin ligases to target protein degradation |
| IL303350A (en) | 2020-12-04 | 2023-08-01 | Macrogenics Inc | Pharmaceutical compositions of a her2/neu antibody and use of the same |
| CN112618726B (zh) * | 2020-12-21 | 2022-11-11 | 江南大学 | 一种抗体缀合物、增强抗体分子免疫效应功能的方法 |
| WO2022198231A1 (en) | 2021-03-18 | 2022-09-22 | Seagen Inc. | Selective drug release from internalized conjugates of biologically active compounds |
| AU2024256916A1 (en) | 2023-04-18 | 2025-12-04 | Astrazeneca Ab | Conjugates comprising cleavable linkers |
| WO2025059190A2 (en) * | 2023-09-11 | 2025-03-20 | Catena Biosciences, Inc. | Polypeptide conjugation compositions and methods of use |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101520209B1 (ko) * | 2003-11-06 | 2015-05-13 | 시애틀 지네틱스, 인크. | 리간드에 접합될 수 있는 모노메틸발린 화합물 |
| JP4861308B2 (ja) * | 2004-04-07 | 2012-01-25 | ジェネンテック， インコーポレイテッド | 抗体結合体の質量分析 |
| AU2010229192A1 (en) * | 2009-03-06 | 2011-09-29 | Agensys, Inc. | Antibody drug conjugates (ADC) that bind to 24P4C12 proteins |
| WO2011005481A1 (en) * | 2009-06-22 | 2011-01-13 | Medimmune, Llc | ENGINEERED Fc REGIONS FOR SITE-SPECIFIC CONJUGATION |
| GB0920127D0 (en) * | 2009-11-17 | 2009-12-30 | Ucb Pharma Sa | Antibodies |
| RS52983B (sr) * | 2010-04-15 | 2014-02-28 | Spirogen Sárl | Pirolobenzodiazepini i njihovi konjugati |
| DK3108886T3 (da) * | 2010-04-21 | 2020-08-10 | Syntarga Bv | Konjugater af CC-1065-analoger og bifunktionelle linkere |
| CN103566377A (zh) * | 2012-07-18 | 2014-02-12 | 上海博笛生物科技有限公司 | 癌症的靶向免疫治疗 |
| BR112015014712A2 (pt) * | 2012-12-21 | 2017-07-11 | Abgenomics Int Inc | ligadores de autoimolação hidrofílicos e seus conjugados |
| AU2014214751B2 (en) * | 2013-02-08 | 2017-06-01 | Novartis Ag | Specific sites for modifying antibodies to make immunoconjugates |
| PT2948184T (pt) * | 2014-01-10 | 2016-07-08 | Synthon Biopharmaceuticals Bv | Conjugados de anticorpo-fármaco de duocarmicina apresentando uma melhor atividade antitumoral in vivo. |
-
2015
- 2015-06-18 TW TW104119839A patent/TW201625315A/zh unknown
- 2015-06-18 WO PCT/US2015/036414 patent/WO2015195904A1/en not_active Ceased
- 2015-06-18 AU AU2015277100A patent/AU2015277100A1/en not_active Abandoned
- 2015-06-18 CN CN201580043407.5A patent/CN106659783A/zh active Pending
- 2015-06-18 US US14/743,351 patent/US20160051695A1/en not_active Abandoned
- 2015-06-18 KR KR1020177001643A patent/KR20170063507A/ko not_active Withdrawn
- 2015-06-18 SG SG10201811124YA patent/SG10201811124YA/en unknown
- 2015-06-18 MX MX2016017117A patent/MX2016017117A/es unknown
- 2015-06-18 RU RU2017101331A patent/RU2017101331A/ru not_active Application Discontinuation
- 2015-06-18 EP EP15809482.1A patent/EP3157560A4/en not_active Withdrawn
- 2015-06-18 CA CA2952834A patent/CA2952834A1/en not_active Abandoned
- 2015-06-18 SG SG11201610468XA patent/SG11201610468XA/en unknown
- 2015-06-18 BR BR112016029588A patent/BR112016029588A2/pt not_active IP Right Cessation
- 2015-06-18 JP JP2017519448A patent/JP2017525755A/ja active Pending
-
2016
- 2016-12-15 PH PH12016502509A patent/PH12016502509A1/en unknown
- 2016-12-18 IL IL249626A patent/IL249626A0/en unknown
-
2017
- 2017-01-13 ZA ZA2017/00306A patent/ZA201700306B/en unknown
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10953106B2 (en) | 2015-02-16 | 2021-03-23 | Lonza Ltd | Antibodies |
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