JP2016528304A5 - - Google Patents
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- JP2016528304A5 JP2016528304A5 JP2016537780A JP2016537780A JP2016528304A5 JP 2016528304 A5 JP2016528304 A5 JP 2016528304A5 JP 2016537780 A JP2016537780 A JP 2016537780A JP 2016537780 A JP2016537780 A JP 2016537780A JP 2016528304 A5 JP2016528304 A5 JP 2016528304A5
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Claims (59)
- Lが、腫瘍関連抗原に特異的に結合する抗体又はその抗原結合断片であり、さらに、該腫瘍関連抗原が、AFP、ALK、BAGEタンパク質、β-カテニン、brc-abl、BRCA1、BORIS、CA9、炭酸脱水酵素IX、カスパーゼ-8、CD20、CD40、CDK4、CEA、CLEC12A、cMET、CTLA4、サイクリン-B1、CYP1B1、EGFR、EGFRvIII、ErbB2/Her2、ErbB3、ErbB4、ETV6-AML、EphA2、Fra-1、FOLR1、GAGEタンパク質、GD2、GD3、GloboH、グリピカン-3、GM3、gp100、HER2、HLA/B-raf、HLA/k-ras、HLA/MAGE-A3、hTERT、IGF1R、LGR5、LMP2、MAGEタンパク質、MART-1、メソセリン、ML-IAP、MUC1、MUC16又はCA-125、MUM1、NA17、NY-BR1、NY-BR62、NY-BR85、NY-ESO1、OX40、p15、p53、PAP、PAX3、PAX5、PCTA-1、PDGFR-α、PDGFR-β、PDGF-A、PDGF-B、PDGF-C、PDGF-D、PLAC1、PRLR、PRAME、PSMA、FOLH1、RAGEタンパク質、Ras、RGS5、Rho、SART-1、SART-3、Steap-1、Steap-2、サバイビン、TAG-72、TGF-β、TMPRSS2、Tn、TNFRSF17、TRP-1、TRP-2、チロシナーゼ、及びウロプラキン-3からなる群から選択される、請求項1記載の組成物。
- 前記腫瘍関連抗原が、EGFRvIII、HER2、及びMUC16からなる群から選択される、請求項2記載の組成物。
- 式IIa又はIIbの化合物が、95%より高いジアステレオマー過剰率で存在する、請求項3記載の組成物。
- 請求項1記載の組成物を含む、医薬組成物。
- 式IIa又はIIbの化合物が、95%より高いジアステレオマー過剰率で存在する、請求項8記載の医薬組成物。
- 請求項1〜6のいずれか1項記載の化合物、又は、請求項7〜11のいずれか1項記載の組成物を含む、疾患を治療するための医薬組成物であって、非経口投与用に製剤化されている、前記医薬組成物。
- 前記疾患が、癌、自己免疫疾患、及び炎症性疾患から選択される、請求項12記載の医薬組成物。
- 腫瘍関連抗原と関連した疾患又は障害を治療するための医薬組成物であって、該腫瘍関連抗原は、AFP、ALK、BAGEタンパク質、β-カテニン、brc-abl、BRCA1、BORIS、CA9、炭酸脱水酵素IX、カスパーゼ-8、CD20、CD40、CDK4、CEA、CLEC12A、cMET、CTLA4、サイクリン-B1、CYP1B1、EGFR、EGFRvIII、ErbB2/Her2、ErbB3、ErbB4、ETV6-AML、EphA2、Fra-1、FOLR1、GAGEタンパク質、GD2、GD3、GloboH、グリピカン-3、GM3、gp100、Her2、HLA/B-raf、HLA/k-ras、HLA/MAGE-A3、hTERT、IGF1R、LGR5、LMP2、MAGEタンパク質、MART-1、メソセリン、ML-IAP、Muc1、Muc16又はCA-125、MUM1、NA17、NY-BR1、NY-BR62、NY-BR85、NY-ESO1、OX40、p15、p53、PAP、PAX3、PAX5、PCTA-1、PDGFR-α、PDGFR-β、PDGF-A、PDGF-B、PDGF-C、PDGF-D、PLAC1、PRLR、PRAME、PSMA、FOLH1、RAGEタンパク質、Ras、RGS5、Rho、SART-1、SART-3、Steap-1、Steap-2、サバイビン、TAG-72、TGF-β、TMPRSS2、Tn、TNFRSF17、TRP-1、TRP-2、チロシナーゼ、及びウロプラキン-3からなる群から選択され、該医薬組成物は、請求項1〜6のいずれか1項記載の化合物、又は、請求項7〜11のいずれか1項記載の組成物を含み、該医薬組成物は、非経口投与用に製剤化されている、前記医薬組成物。
- 前記ジアステレオマー過剰率が、少なくとも95%である、請求項15又は16記載の組成物。
- 式Iの化合物が、実質的に図1に示される1H NMRによって特徴づけられる、請求項15又は16記載の組成物、又は、請求項58記載の化合物。
- 前記有機溶媒がアセトニトリルを含む、請求項24記載の方法。
- 前記有機溶媒及び水が、約1:1〜約4:1又は約1:1〜約10:1の有機溶媒:水の体積比で存在する、請求項24記載の方法。
- 式IIIの化合物と式IVの化合物のモル比が、約1:1〜約1:3である、請求項24記載の方法。
- 成分(i)〜(iv)が、約18時間接触される、請求項24〜28のいずれか1項記載の方法。
- 式IVの化合物が、式IIIの化合物に対して、化学量論的過剰で存在する、請求項24〜29のいずれか1項記載の方法。
- 工程(a)の後に追加的な量の式IVの化合物を接触させることをさらに含む、請求項24〜30のいずれか1項記載の方法。
- 工程(a)において、式IVの化合物と式IIIの化合物のモル比が、約2.3:1である、請求項24〜30のいずれか1項記載の方法。
- 工程(a)において、式IVの化合物と式IIIの化合物のモル比が、約1.5:1である、請求項24記載の方法。
- 工程(b)における式Iの化合物の単離が、濾過により達成される、請求項24〜29のいずれか1項記載の方法。
- 式Iの化合物を抗体又はその抗原結合断片と結合させて抗体-薬剤コンジュゲートを作製することをさらに含む、請求項24〜34のいずれか1項記載の方法。
- 式Iの化合物が、S、O、又はNR3を介して前記抗体又は抗原結合断片に結合され、R3がH又はアルキルである、請求項35記載の方法。
- 前記抗体又はその抗原結合断片が、腫瘍関連抗原に特異的に結合することができ、さらに、該腫瘍関連抗原が、AFP、ALK、BAGEタンパク質、β-カテニン、brc-abl、BRCA1、BORIS、CA9、炭酸脱水酵素IX、カスパーゼ-8、CD20、CD40、CDK4、CEA、CLEC12A、cMET、CTLA4、サイクリン-B1、CYP1B1、EGFR、EGFRvIII、ErbB2/Her2、ErbB3、ErbB4、ETV6-AML、EphA2、Fra-1、FOLR1、GAGEタンパク質、GD2、GD3、GloboH、グリピカン-3、GM3、gp100、Her2、HLA/B-raf、HLA/k-ras、HLA/MAGE-A3、hTERT、IGF1R、LGR5、LMP2、MAGEタンパク質、MART-1、メソセリン、ML-IAP、Muc1、Muc16又はCA-125、MUM1、NA17、NY-BR1、NY-BR62、NY-BR85、NY-ESO1、OX40、p15、p53、PAP、PAX3、PAX5、PCTA-1、PDGFR-α、PDGFR-β、PDGF-A、PDGF-B、PDGF-C、PDGF-D、PLAC1、PRLR、PRAME、PSMA、FOLH1、RAGEタンパク質、Ras、RGS5、Rho、SART-1、SART-3、Steap-1、Steap-2、サバイビン、TAG-72、TGF-β、TMPRSS2、Tn、TNFRSF17、TRP-1、TRP-2、チロシナーゼ、及びウロプラキン-3からなる群から選択される、請求項35又は36記載の方法。
- 前記腫瘍関連抗原が、EGFRvIII、Her2、及びMuc16からなる群から選択される、請求項40記載の方法。
- Lが、腫瘍関連抗原に特異的に結合する抗体又はその抗原結合断片であり、さらに、該腫瘍関連抗原が、AFP、ALK、BAGEタンパク質、β-カテニン、brc-abl、BRCA1、BORIS、CA9、炭酸脱水酵素IX、カスパーゼ-8、CD20、CD40、CDK4、CEA、CLEC12A、cMET、CTLA4、サイクリン-B1、CYP1B1、EGFR、EGFRvIII、ErbB2/Her2、ErbB3、ErbB4、ETV6-AML、EphA2、Fra-1、FOLR1、GAGEタンパク質、GD2、GD3、GloboH、グリピカン-3、GM3、gp100、Her2、HLA/B-raf、HLA/k-ras、HLA/MAGE-A3、hTERT、IGF1R、LGR5、LMP2、MAGEタンパク質(例えば、MAGE-1、-2、-3、-4、-6、及び-12)、MART-1、メソセリン、ML-IAP、Muc1、Muc16又はCA-125、MUM1、NA17、NY-BR1、NY-BR62、NY-BR85、NY-ESO1、OX40、p15、p53、PAP、PAX3、PAX5、PCTA-1、PDGFR-α、PDGFR-β、PDGF-A、PDGF-B、PDGF-C、PDGF-D、PLAC1、PRLR、PRAME、PSMA、FOLH1、RAGEタンパク質、Ras、RGS5、Rho、SART-1、SART-3、Steap-1、Steap-2、サバイビン、TAG-72、TGF-β、TMPRSS2、Tn、TNFRSF17、TRP-1、TRP-2、チロシナーゼ、及びウロプラキン-3からなる群から選択される、請求項42記載の方法。
- 前記腫瘍関連抗原が、EGFRvIII、Her2、及びMuc16からなる群から選択される、請求項43記載の方法。
- 式IIa又はIIbの化合物が、95%より高いジアステレオマー過剰率で存在する、請求項42記載の方法。
- 式Iの化合物が、95%より高いジアステレオマー過剰率で存在する、請求項42記載の方法。
- 請求項24〜34及び37〜39のいずれか1項記載の方法によって製造される、式Iの化合物。
- 請求項35〜55のいずれか1項記載の方法によって製造される、式IIa又はIIbの化合物。
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- 2014-08-26 JP JP2016537780A patent/JP6608823B2/ja active Active
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- 2014-08-26 US US14/913,965 patent/US20160354482A1/en not_active Abandoned
- 2014-08-26 MX MX2016002149A patent/MX2016002149A/es active IP Right Grant
- 2014-08-26 BR BR112016004023A patent/BR112016004023A2/pt not_active Application Discontinuation
- 2014-08-26 WO PCT/US2014/052757 patent/WO2015031396A1/en active Application Filing
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2018
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP7084938B2 (ja) | 2016-11-16 | 2022-06-15 | リジェネロン・ファーマシューティカルズ・インコーポレイテッド | 抗met抗体、metに結合する二重特異性抗原結合分子およびその使用方法 |
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