JP2010503717A5 - - Google Patents
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- JP2010503717A5 JP2010503717A5 JP2009528693A JP2009528693A JP2010503717A5 JP 2010503717 A5 JP2010503717 A5 JP 2010503717A5 JP 2009528693 A JP2009528693 A JP 2009528693A JP 2009528693 A JP2009528693 A JP 2009528693A JP 2010503717 A5 JP2010503717 A5 JP 2010503717A5
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- Prior art keywords
- cancer
- inhibitors
- derivatives
- cell
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- Prior art date
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- -1 platinum compounds Compounds Chemical class 0.000 claims 24
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- 239000003112 inhibitor Substances 0.000 claims 18
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- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 8
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 8
- 150000003384 small molecules Chemical class 0.000 claims 8
- 150000001875 compounds Chemical class 0.000 claims 5
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- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 5
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 5
- 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
- 108091008605 VEGF receptors Proteins 0.000 claims 4
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- 229940079593 drug Drugs 0.000 claims 4
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 4
- 239000003102 growth factor Substances 0.000 claims 4
- VMMKGHQPQIEGSQ-UHFFFAOYSA-N minodronic acid Chemical compound C1=CC=CN2C(CC(O)(P(O)(O)=O)P(O)(O)=O)=CN=C21 VMMKGHQPQIEGSQ-UHFFFAOYSA-N 0.000 claims 4
- 108090000623 proteins and genes Proteins 0.000 claims 4
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- 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 3
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 3
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- 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
- OEWYWFJWBZNJJG-UHFFFAOYSA-N 1-(aziridin-1-yl)-3-(2-nitroimidazol-1-yl)propan-2-ol Chemical compound C1=CN=C([N+]([O-])=O)N1CC(O)CN1CC1 OEWYWFJWBZNJJG-UHFFFAOYSA-N 0.000 claims 2
- YZEUHQHUFTYLPH-UHFFFAOYSA-N 2-nitroimidazole Chemical compound [O-][N+](=O)C1=NC=CN1 YZEUHQHUFTYLPH-UHFFFAOYSA-N 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 2
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- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 2
- 101001059454 Homo sapiens Serine/threonine-protein kinase MARK2 Proteins 0.000 claims 2
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- GQYIWUVLTXOXAJ-UHFFFAOYSA-N Lomustine Chemical compound ClCCN(N=O)C(=O)NC1CCCCC1 GQYIWUVLTXOXAJ-UHFFFAOYSA-N 0.000 claims 2
- 102000005741 Metalloproteases Human genes 0.000 claims 2
- 108010006035 Metalloproteases Proteins 0.000 claims 2
- 229930192392 Mitomycin Natural products 0.000 claims 2
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 2
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- 102100028904 Serine/threonine-protein kinase MARK2 Human genes 0.000 claims 2
- 102100031463 Serine/threonine-protein kinase PLK1 Human genes 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims 2
- 208000024313 Testicular Neoplasms Diseases 0.000 claims 2
- 206010057644 Testis cancer Diseases 0.000 claims 2
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- 206010046431 Urethral cancer Diseases 0.000 claims 2
- 206010046458 Urethral neoplasms Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims 2
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims 2
- DZBUGLKDJFMEHC-UHFFFAOYSA-N acridine Chemical compound C1=CC=CC2=CC3=CC=CC=C3N=C21 DZBUGLKDJFMEHC-UHFFFAOYSA-N 0.000 claims 2
- RJURFGZVJUQBHK-UHFFFAOYSA-N actinomycin D Natural products CC1OC(=O)C(C(C)C)N(C)C(=O)CN(C)C(=O)C2CCCN2C(=O)C(C(C)C)NC(=O)C1NC(=O)C1=C(N)C(=O)C(C)=C2OC(C(C)=CC=C3C(=O)NC4C(=O)NC(C(N5CCCC5C(=O)N(C)CC(=O)N(C)C(C(C)C)C(=O)OC4C)=O)C(C)C)=C3N=C21 RJURFGZVJUQBHK-UHFFFAOYSA-N 0.000 claims 2
- 229940100198 alkylating agent Drugs 0.000 claims 2
- 239000002168 alkylating agent Substances 0.000 claims 2
- 229960003437 aminoglutethimide Drugs 0.000 claims 2
- ROBVIMPUHSLWNV-UHFFFAOYSA-N aminoglutethimide Chemical compound C=1C=C(N)C=CC=1C1(CC)CCC(=O)NC1=O ROBVIMPUHSLWNV-UHFFFAOYSA-N 0.000 claims 2
- 229960001220 amsacrine Drugs 0.000 claims 2
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- 239000003242 anti bacterial agent Substances 0.000 claims 2
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- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical group N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 claims 2
- 229950002826 canertinib Drugs 0.000 claims 2
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- 229960002584 gefitinib Drugs 0.000 claims 2
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 2
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- GFIJNRVAKGFPGQ-LIJARHBVSA-N leuprolide Chemical compound CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)[C@H](CC=1N=CNC=1)NC(=O)[C@H]1NC(=O)CC1)CC1=CC=C(O)C=C1 GFIJNRVAKGFPGQ-LIJARHBVSA-N 0.000 claims 2
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| EP2685980B1 (en) | 2011-03-17 | 2017-12-06 | The Trustees Of The University Of Pennsylvania | Methods and use of bifunctional enzyme-building clamp-shaped molecules |
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-
2007
- 2007-09-14 DK DK07820235.5T patent/DK2068880T3/da active
- 2007-09-14 MX MX2009002710A patent/MX2009002710A/es active IP Right Grant
- 2007-09-14 WO PCT/EP2007/059735 patent/WO2008034776A1/en not_active Ceased
- 2007-09-14 EP EP07820235A patent/EP2068880B1/en not_active Revoked
- 2007-09-14 ES ES07820235T patent/ES2385613T3/es active Active
- 2007-09-14 CA CA002663599A patent/CA2663599A1/en not_active Abandoned
- 2007-09-14 SI SI200730957T patent/SI2068880T1/sl unknown
- 2007-09-14 NZ NZ576065A patent/NZ576065A/en unknown
- 2007-09-14 PL PL07820235T patent/PL2068880T3/pl unknown
- 2007-09-14 AT AT07820235T patent/ATE552835T1/de active
- 2007-09-14 RU RU2009114414/15A patent/RU2492864C2/ru active
- 2007-09-14 JP JP2009528693A patent/JP2010503717A/ja active Pending
- 2007-09-14 BR BRPI0717586-8A patent/BRPI0717586A2/pt not_active IP Right Cessation
- 2007-09-14 KR KR1020097007757A patent/KR20090074202A/ko not_active Ceased
- 2007-09-14 AU AU2007299080A patent/AU2007299080B2/en active Active
- 2007-09-14 US US12/441,180 patent/US8877764B2/en active Active
- 2007-09-14 PT PT07820235T patent/PT2068880E/pt unknown
-
2009
- 2009-03-16 IL IL197605A patent/IL197605A0/en unknown
-
2012
- 2012-07-06 CY CY20121100603T patent/CY1112896T1/el unknown
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