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
- use according
- 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.)
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- -1 platinum compounds Compounds Chemical class 0.000 claims 30
- 201000011510 cancer Diseases 0.000 claims 23
- 230000002401 inhibitory effect Effects 0.000 claims 22
- 239000003112 inhibitor Substances 0.000 claims 21
- 206010028980 Neoplasm Diseases 0.000 claims 15
- 108090001123 antibodies Proteins 0.000 claims 12
- 102000004965 antibodies Human genes 0.000 claims 12
- 230000035772 mutation Effects 0.000 claims 12
- 210000004027 cells Anatomy 0.000 claims 11
- 102000017256 epidermal growth factor-activated receptor activity proteins Human genes 0.000 claims 9
- 108040009258 epidermal growth factor-activated receptor activity proteins Proteins 0.000 claims 9
- 150000003384 small molecules Chemical class 0.000 claims 8
- 208000002154 Non-Small-Cell Lung Carcinoma Diseases 0.000 claims 5
- 230000003042 antagnostic Effects 0.000 claims 5
- 239000005557 antagonist Substances 0.000 claims 5
- 150000001875 compounds Chemical class 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- AOJJSUZBOXZQNB-TZSSRYMLSA-N ADRIAMYCIN 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
- 229960004679 Doxorubicin Drugs 0.000 claims 4
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- 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
- 208000000587 Small Cell Lung Carcinoma Diseases 0.000 claims 4
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- 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 3
- 229960004857 Mitomycin Drugs 0.000 claims 3
- 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 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
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- 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
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- 229940064005 Antibiotic throat preparations Drugs 0.000 claims 2
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- GQYIWUVLTXOXAJ-UHFFFAOYSA-N Belustine Chemical compound ClCCN(N=O)C(=O)NC1CCCCC1 GQYIWUVLTXOXAJ-UHFFFAOYSA-N 0.000 claims 2
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- VSJKWCGYPAHWDS-FQEVSTJZSA-N Camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims 2
- HAWPXGHAZFHHAD-UHFFFAOYSA-N Chlormethine Chemical compound ClCCN(C)CCCl HAWPXGHAZFHHAD-UHFFFAOYSA-N 0.000 claims 2
- IAKHMKGGTNLKSZ-INIZCTEOSA-N 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
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N Docetaxel 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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- 206010051066 Gastrointestinal stromal tumour Diseases 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
- 229940093922 Gynecological Antibiotics Drugs 0.000 claims 2
- CGIGDMFJXJATDK-UHFFFAOYSA-N Indometacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims 2
- RCINICONZNJXQF-MZXODVADSA-N Intaxel 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 2
- UWKQSNNFCGGAFS-XIFFEERXSA-N Irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims 2
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 2
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- DLGOEMSEDOSKAD-UHFFFAOYSA-N Nitrumon Chemical compound ClCCNC(=O)N(N=O)CCCl DLGOEMSEDOSKAD-UHFFFAOYSA-N 0.000 claims 2
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- NOWKCMXCCJGMRR-UHFFFAOYSA-N aziridine Chemical class C1CN1 NOWKCMXCCJGMRR-UHFFFAOYSA-N 0.000 claims 2
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- OSQUFVVXNRMSHL-LTHRDKTGSA-M sodium;3-[(2Z)-2-[(E)-4-(1,3-dibutyl-4,6-dioxo-2-sulfanylidene-1,3-diazinan-5-ylidene)but-2-enylidene]-1,3-benzoxazol-3-yl]propane-1-sulfonate Chemical compound [Na+].O=C1N(CCCC)C(=S)N(CCCC)C(=O)C1=C\C=C\C=C/1N(CCCS([O-])(=O)=O)C2=CC=CC=C2O\1 OSQUFVVXNRMSHL-LTHRDKTGSA-M 0.000 claims 2
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- AIWRTTMUVOZGPW-HSPKUQOVSA-N abarelix Chemical compound C([C@@H](C(=O)N[C@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N[C@H](C)C(N)=O)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](CC=1C=NC=CC=1)NC(=O)[C@@H](CC=1C=CC(Cl)=CC=1)NC(=O)[C@@H](CC=1C=C2C=CC=CC2=CC=1)NC(C)=O)C1=CC=C(O)C=C1 AIWRTTMUVOZGPW-HSPKUQOVSA-N 0.000 claims 1
- 229960002184 abarelix Drugs 0.000 claims 1
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- ULXXDDBFHOBEHA-CWDCEQMOSA-N afatinib Chemical compound N1=CN=C2C=C(O[C@@H]3COCC3)C(NC(=O)/C=C/CN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-CWDCEQMOSA-N 0.000 claims 1
- 229960005142 alclofenac Drugs 0.000 claims 1
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- 230000002280 anti-androgenic Effects 0.000 claims 1
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- 230000001833 anti-estrogenic Effects 0.000 claims 1
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- 239000003816 antisense DNA Substances 0.000 claims 1
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- BSYNRYMUTXBXSQ-UHFFFAOYSA-N aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims 1
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- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound 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 1
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- 229960004316 cisplatin Drugs 0.000 claims 1
- 229960002436 cladribine Drugs 0.000 claims 1
- HJKBJIYDJLVSAO-UHFFFAOYSA-L clodronic acid disodium salt Chemical compound [Na+].[Na+].OP([O-])(=O)C(Cl)(Cl)P(O)([O-])=O HJKBJIYDJLVSAO-UHFFFAOYSA-L 0.000 claims 1
- 229960001338 colchicine Drugs 0.000 claims 1
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- GIUYCYHIANZCFB-FJFJXFQQSA-N fludarabine phosphate Chemical compound C1=NC=2C(N)=NC(F)=NC=2N1[C@@H]1O[C@H](COP(O)(O)=O)[C@@H](O)[C@@H]1O GIUYCYHIANZCFB-FJFJXFQQSA-N 0.000 claims 1
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- JBVNBBXAMBZTMQ-CEGNMAFCSA-N megestrol Chemical compound C1=CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)C)(O)[C@@]1(C)CC2 JBVNBBXAMBZTMQ-CEGNMAFCSA-N 0.000 claims 1
- 229960001924 melphalan Drugs 0.000 claims 1
- GLVAUDGFNGKCSF-UHFFFAOYSA-N mercaptopurine Chemical compound S=C1NC=NC2=C1NC=N2 GLVAUDGFNGKCSF-UHFFFAOYSA-N 0.000 claims 1
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- 229960004584 methylprednisolone Drugs 0.000 claims 1
- VAOCPAMSLUNLGC-UHFFFAOYSA-N metronidazole Chemical compound CC1=NC=C([N+]([O-])=O)N1CCO VAOCPAMSLUNLGC-UHFFFAOYSA-N 0.000 claims 1
- BLXXJMDCKKHMKV-UHFFFAOYSA-N nabumeton Chemical compound C1=C(CCC(C)=O)C=CC2=CC(OC)=CC=C21 BLXXJMDCKKHMKV-UHFFFAOYSA-N 0.000 claims 1
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- FXSKHQLAUMGYJK-UHFFFAOYSA-J platinum(4+);propan-2-amine;dichloride;dihydroxide Chemical compound [OH-].[OH-].[Cl-].[Cl-].[Pt+4].CC(C)N.CC(C)N FXSKHQLAUMGYJK-UHFFFAOYSA-J 0.000 claims 1
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- 102220052592 rs121913463 Human genes 0.000 claims 1
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- CKNPWBAXEKSCRG-UHFFFAOYSA-J satraplatin Chemical compound CC(=O)O[Pt-2]([NH3+])(Cl)(Cl)(OC(C)=O)[NH2+]C1CCCCC1 CKNPWBAXEKSCRG-UHFFFAOYSA-J 0.000 claims 1
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- 201000000849 skin cancer Diseases 0.000 claims 1
- VBDRTGFACFYFCT-UHFFFAOYSA-M sodium;hydroxy-[(1R)-1-hydroxy-3-[methyl(pentyl)amino]-1-phosphonopropyl]phosphinate;hydrate Chemical compound O.[Na+].CCCCCN(C)CCC(O)(P(O)(O)=O)P(O)([O-])=O VBDRTGFACFYFCT-UHFFFAOYSA-M 0.000 claims 1
- 229960003787 sorafenib Drugs 0.000 claims 1
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- 108010042747 stallimycin Proteins 0.000 claims 1
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- 201000011549 stomach cancer Diseases 0.000 claims 1
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- 229960004964 temozolomide Drugs 0.000 claims 1
- RYYWUUFWQRZTIU-UHFFFAOYSA-K thiophosphate Chemical class [O-]P([O-])([O-])=S RYYWUUFWQRZTIU-UHFFFAOYSA-K 0.000 claims 1
- 229960001312 tiaprofenic acid Drugs 0.000 claims 1
- 229910052718 tin Inorganic materials 0.000 claims 1
- ATJFFYVFTNAWJD-UHFFFAOYSA-N tin hydride Chemical compound [Sn] ATJFFYVFTNAWJD-UHFFFAOYSA-N 0.000 claims 1
- 210000001519 tissues Anatomy 0.000 claims 1
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- LXZZYRPGZAFOLE-UHFFFAOYSA-L transplatin Chemical compound [H][N]([H])([H])[Pt](Cl)(Cl)[N]([H])([H])[H] LXZZYRPGZAFOLE-UHFFFAOYSA-L 0.000 claims 1
- 229960005294 triamcinolone Drugs 0.000 claims 1
- VXKHXGOKWPXYNA-PGBVPBMZSA-N triptorelin Chemical compound C([C@@H](C(=O)N[C@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1[C@@H](CCC1)C(=O)NCC(N)=O)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)C1=CC=C(O)C=C1 VXKHXGOKWPXYNA-PGBVPBMZSA-N 0.000 claims 1
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- 229960000604 valproic acid Drugs 0.000 claims 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims 1
- 229960002066 vinorelbine Drugs 0.000 claims 1
- CILBMBUYJCWATM-IJDPFCGHSA-N vinorelbine L-tartrate Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.OC(=O)[C@H](O)[C@@H](O)C(O)=O.C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC CILBMBUYJCWATM-IJDPFCGHSA-N 0.000 claims 1
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Claims (14)
- 癌を患う患者、および、腫瘍にEGFR遺伝子の変異を有する患者の治療用の医薬組成物を製造するための、さらに化学療法薬剤(2)と併用してもよい、BIBW2992(1)の使用。
- 癌が、以下からなる群から選ばれる請求項1に記載の使用:
・頭頸部腫瘍:SCC、AC、移行細胞癌、粘液性類表皮癌、未分化癌;
・中枢神経系腫瘍:星状細胞腫、グリア芽腫、髄膜腫、神経線維腫、神経鞘腫、上衣細胞腫、下垂体腫瘍、乏突起膠腫、髄芽細胞腫;
・気管支および縦隔の腫瘍:
気管支腫瘍:
○小細胞肺癌(SCLC):燕麦細胞肺癌、中間細胞癌、混合型燕麦細胞肺癌;
○非小細胞肺癌(NSCLC):SCC、紡錐体細胞癌、AC、細気管支癌、大型細胞NSCLC、明細胞NSCLC;
中皮腫;
胸線腫;
甲状腺癌:乳頭、小胞、未分化、延髄;
・消化管の腫瘍:
食道癌:SCC、AC、未分化、カルチノイド、肉腫;
胃癌:AC、腺扁平上皮、未分化;
結腸直腸癌:AC(ACの遺伝型を含む)カルチノイド、肉腫;
肛門癌:SSC、移行上皮腫、AC、基底細胞癌;
膵臓癌:AC(管状腺および腺房の癌を含む)、乳頭、腺扁平上皮、未分化、膵臓内分泌部の腫瘍;
肝細胞癌、胆管癌、血管肉腫、肝芽腫;
胆汁性癌腫症:AC、SCC、小細胞、未分化;
消化管間質腫瘍(GIST);
・婦人科の癌:
乳癌:AC(湿潤性腺管、小葉および延髄癌を含む)、管状腺、粘液性癌、パジェット病、炎症性癌、非湿潤性乳管および上皮内小葉癌;
卵巣癌:上皮腫瘍、間質腫瘍、生殖細胞腫瘍、未分化腫瘍;
子宮頸癌:SCC、AC、混合および未分化腫瘍;
子宮内膜癌:AC、SCC、混合、未分化腫瘍;
外陰癌:SCC、AC;
膣癌:SCC、AC;
・尿道および精巣癌:
精巣癌:精上皮腫;
非精上皮生殖細胞:奇形腫、胎児性癌、絨毛腫、卵黄嚢腫、混合型セルトリおよびライディッヒ腫瘍;
性腺外胚細胞腫瘍;
前立腺癌:AC、小細胞、SCC;
腎細胞癌:AC(明細胞、乳頭および嫌色素性細胞腫を含む)、遺伝型(たとえばフォンヒッペルリンドウ病)、腎芽細胞腫;
膀胱癌:移行細胞(尿路上皮)癌、SCC、AC;
尿道癌:SCC、移行細胞癌、AC;
陰茎癌:SCC;
・内分泌組織の腫瘍
甲状腺癌:乳頭、小胞、未分化、延髄の癌(多発性内分泌腺腫症候群を含む);
膵臓内分泌部の腫瘍;
カルチノイド;
褐色細胞腫。 - 癌が、上皮細胞癌である請求項1に記載の使用。
- 癌が、消化管癌、前立腺癌、卵巣癌、乳癌、頭頸部癌、食道癌、肺癌、非小細胞肺癌、神経系癌、腎臓癌、網膜癌、皮膚癌、肝臓癌、膵臓癌、性器−泌尿器癌および膀胱癌である請求項1に記載の使用。
- 化学療法薬剤(2)は以下からなる群から選ばれる請求項1〜4のいずれかに記載の使用:
・合成小分子VEGF受容体アンタゴニスト
・小分子成長因子(GF)受容体アンタゴニスト
・EGF受容体および/またはHER2受容体および/またはVEGF受容体および/またはインテグリン受容体またはそのほかのタンパク質チロシンキナーゼ受容体の合成小分子に分類されない阻害剤
・小分子Polo様キナーゼ−1(PLK−1)阻害剤
・Ras/Raf/MAPKまたはPI3K/AKT経路または、そのほかのセリン/スレオニンキナーゼの小分子阻害剤
・Ras/Raf/MAPKまたはPI3K/AKT経路または、そのほかのセリン/スレオニンキナーゼの合成小分子に分類されない阻害剤
・EGF受容体および/またはVEGF受容体および/またはインテグリン受容体またはそのほかのタンパク質チロシンキナーゼ受容体を対象とする合成的に作られた抗体、抗体断片または融合タンパク質である阻害剤
・循環VEGFを対象とする合成的に作られた抗体、抗体断片または融合タンパク質である阻害剤
・IGF1受容体および/またはIGF1またはIGF2成長因子を対象とする合成的に作られた化学物質、抗体、抗体断片または融合タンパク質である阻害剤
・核酸と相互作用し、かつ、アルキル化剤またはプラチナ化合物として分類される化合物・核酸と相互作用し、かつ、アントラサイクリンとして、DNA挿入剤として、またはDNA架橋剤として分類される化合物
・抗代謝産物
・自然発生、半合成または合成ブレオマイシン型抗生物質(BLM群抗生物質)
・DNA転写酵素の阻害剤、特にトポイソメラーゼIまたはトポイソメラーゼII阻害剤・クロマチン修飾薬剤
・有糸分裂阻害剤、抗有糸分裂薬剤、または、細胞周期阻害剤
・チューブリンと相互作用または結合する化合物
・有糸分裂キネシン、またはEg5、CENP−E、MCAK、Kid、MKLP−1を含むほかのモータータンパク質(限定されない)を阻害する化合物
・プロテアーゼ阻害剤
・ヒートショックタンパク質阻害剤
・Bcl−2、Bcl−xlおよび類似分子の抗アポトーシス機能を標的とする化合物
・酵素、ホルモン、ホルモンアンタゴニスト、またはホルモン阻害剤、またはステロイド生合成の阻害剤
・ステロイド
・サイトカイン、低酸素選択的なサイトトキシン、サイトカインの阻害剤、リンフォカイン、サイトカインを対象とした抗体、または、経口および非経口トレランス誘導ストラテジー
・支持薬
・COX−2阻害剤(限定されない)のような抗炎症性化合物
・化学放射線感光薬およびプロテクター
・光化学的に活性な薬
・合成ポリ−またはオリゴヌクレオチド
・細胞障害性抗生物質、癌細胞の表面分子をターゲットとする抗体、成長因子またはそれらの受容体をターゲットとする抗体、メタロプロテイナーゼの阻害剤、癌遺伝子の阻害剤、遺伝子の転写またはRNA翻訳またはタンパク質発現の阻害剤、または、希土類元素の複合体のような他の化学療法のまたは自然発生、半合成または合成治療薬。 - 化学療法薬剤(2)は以下からなる群から選ばれる請求項1〜4のいずれかに記載の使用:
小分子VEGF受容体アンタゴニスト、たとえばバタラニブ(PTK−787/ZK222584)、SU−5416、SU−6668、SU−11248、SU−14813、AZD−6474、AZD−2171、CP−547632、CEP−7055、AG−013736、IM−842またはGW−786034、2重EGFR/HER2アンタゴニスト、たとえばHKI−272、CI−1033またはGW−2016、EGFRアンタゴニスト、たとえばタルセバ(OSI−774)、PKI−166、EKB−569またはハーセプチン、分裂促進因子活性化タンパク質キナーゼのアンタゴニスト、たとえば、BAY−43−9006またはBAY−57−9006、合成小分子に分類されないタンパク質キナーゼ受容体アンタゴニスト、たとえばアトラセンタン、リツキシマブ、セテュキマブ、アバスチンTM(ベバシズマブ)、ビバツズマブマータンシン、IMC−1C11、エルビタックス(C−225)、DC−101、EMD−72000、バイタクシン、イマチニブ、融合タンパク質であるタンパク質チロシンキナーゼ阻害剤、たとえばVEGFtrap、アルキル化剤またはプラチナ化合物、たとえばメルファラン、シクロホスミド、オキサザホスホリン、シスプラチン、カルボプラチン、オキサリプラチン、サトラプラチン、テトラプラチン、イプロプラチン、マイトマイシン、ストレプトゾシン、カルムスチン(BCNU)、ロムスチン(CCNU)、ブスルファン、イホスファミド、ストレプトゾシン、チオテパ、クロラムブシル、ナイトロジェンマスタード、たとえばメクロメタミン、エチレンイミン化合物、アルキルスルホナート、ダウノルビシン、ドキソルビシン(アドリアマイシン)、リポソームのドキソルビシン(ドキシル)、エピルビシン、イダルビシン、ミトキサントロン、アムサクリン、ダクチノマイシン、ジスタマイシンまたはそれらの誘導体、ネトロプシン、ピベンジモル、マイトマイシン、CC−1065、デュオカルマイシン、ミトラマイシン、クロモマイシン、オリボマイシン、フタラニリド、たとえばプロパミジンまたはスチルバミジン、アントラマイシン、アジリジン、ニトロソウレアまたは、それらの誘導体、ピリミジンまたはプリン類似体またはアンタゴニストまたはヌクレオシドジホスファートレダクターゼの阻害剤、たとえばシタラビン、5−フルオロウラシル(5−FU)、ペメトレキセド、テガフール/ウラシル、ウラシルマスタード、フルダラビン、ゲムシタビン、カペシタビン、メルカプトプリン、クラドリビン、チオグアニン、メトトレキサート、ペントスタチン、ヒドロキシウレアまたは葉酸、フレオマイシン、ブレオマイシンまたはそれらの誘導体もしくは塩、CHPP、BZPP、MTPP、BAPP、リブロマイシン、アクリジンまたはそれらの誘導体、リファマイシン、アクチノマイシン、アドリアマイシン、カンプトセシン、たとえばイリノテカン(カンプトサール)またはトポテカン、アムサクリンまたはそれらの類似体、三環式カルボキサミド、ヒストンデアセチラーゼ阻害剤、たとえばSAHA、MD−275、トリコスタチンA、CBHA、LAQ824、またはバルプロ酸、植物由来抗癌剤、たとえばパクリタキセル(タキソール)、ドセタキセルまたはタキソテール、ビンカアルカロイドたとえばナベルビン、ビンブラスチン、ビンクリスチン、ビンデシンまたは酒石酸ビノレルビン、トロポロンアルカロイドたとえばコルヒチンまたはそれらの誘導体、マクロライドたとえばマイタンシン、アンサミトシンまたはライゾシン、抗有糸系分裂性ペプチドたとえばホモプシンまたはドラスタチン、エピポドフィロトキシンまたはポドフィロトキシンの誘導体、たとえばエトポシド、またはテニポシド、ステガナシン、抗有糸分裂性カルバマート誘導体、たとえばコンブレタスタチンまたはアンフェチニル、プロカルバジン、プロテアソーム阻害剤、たとえばボルテゾミブ、酵素、たとえばアスパラギナーゼ、ペグ化されたアスパラギナーゼ(ぺガスパルガーゼ)またはチミジンホスホリラーゼ阻害剤、ゲスターゲンまたはエストロゲン、たとえばエストラムスチン(T−66)またはメゲストロール、抗アンドロゲン、たとえばフルタミド、カソデックス、アナンドロンまたは酢酸シプロテロン、アロマターゼ阻害剤、たとえばアミノグルテチミド、アナストロゾール、フォルメスタンまたはレトロゾール、GNrH類似体、たとえばリュープロレリン、ブセレリン、ゴセレリンまたはトリプトレリン、抗エストロゲン剤、たとえばタモキシフェンまたはそのクエン酸塩、ドロロキシフェン、トリオキシフェン、ラロキシフェンまたはジンドキシフェン、17βエストラジオールの誘導体、たとえばICI164,384またはICI182,780、アミノグルテチミド、フォルメスタン、ファドロゾール、フィナステライド、ケトコナゾール、LH−RHアンタゴニスト、たとえばロイプロリド、ステロイド、たとえばブレドニゾン、プレドニゾロン、メチルプレドニゾロン、デキサメタゾン、ブデノシド、フルオコルトロンまたはトリアムシノロン、インターフェロン、たとえばインターフェロンβ、インターロイキン、たとえばIL−10またはIL−12、抗TNFα抗体、たとえばエタネルセプト、TNF−α(タソネルミン)、免疫調整薬、たとえばサリドマイド、そのR−およびS−エナンチオマーおよびその誘導体、またはレビミッド(CC−5013)、ロイコトリエンアンタゴニスト、マイトマイシンC、アジリドキノン、たとえばBMY−42355、AZQまたはEO−9、2−ニトロイミダゾール、たとえばミソニダゾール、NLP−1またはNLA−1、ニトロアクリジン、ニトロキノリン、ニトロピラゾロアクリジン、「二官能」ニトロ芳香族化合物、たとえばRSU−1069またはRB−6145、CB−1954、ナイトロジェンマスタードのN−オキシド、たとえばナイトロミン、ナイトロジェンマスタードの金属複合体、抗CD3または抗CD25抗体、耐性誘導薬、ビスホスホナートまたはそれらの誘導体、たとえばミノドロン酸またはその誘導体(YM−529、Ono−5920、YH−529)、ゾレドロン酸一水和物、イバンドロン酸ナトリウム水和物またはクロドロナート二ナトリウム、ニトロイミダゾール、たとえばメトロニダゾール、ミソニダゾール、ベンズニダゾールまたはニモラゾール、ニトロアクリル組成物、たとえばRSU−1069、ニトロキシルまたはN−オキシド、たとえばSR−4233、ハロゲン化したピリミジン類似体、たとえばブロモデオキシウリジン、ヨードデオキシウリジン、チオホスファート、たとえばWR−2721、光化学活性化薬、たとえばポルフィマー、フォトフリン、ベンゾポルフィン誘導体、フェオフォルバイド誘導体、メロシアニン540(MC−540)またはスズエチオポルフィリン、アンチテンプレートまたはアンチセンスRNAまたはDNA、たとえばオブリメルセン、非ステロイド系炎症薬、たとえばアセチルサリチル酸、メサラジン、イブプロフェン、ナプロキセン、フルルビプロフェン、フェノプロフェン、フェンブフェン、ケトプロフェン、インドプロフェン、ピルプロフェン、カルプロフェン、オキサプロジン、プラノプロフェン、ミロプロフェン、チオキサプロフェン、スプロフェン、アルミノプロフェン、チアプロフェン酸、フルプロフェン、インドメタシン、スリンダク、トルメチン、ゾメピラク、ナブメトン、ジクロフェナク、フェンクロフェナック、アルクロフェナク、ブロムフェナク、イブフェナク、アセクロフェナク、アセメタシン、フェンチアザク、クリダナク、エトドラク、オキシピナク、メフェナム酸、メクロフェナム酸、フルフェナム酸、ニフルミン酸、トルフェナム酸、ジフルニサル、フルフェニサル、ピロキシカム、テノキシカム、ロルノキシカム、ニメスリド、メロキシカム、セレコクシブ、ロフェコキシブ、または非ステロイド系炎症薬の医薬的に許容される塩、細胞損害性抗生物質、癌細胞の表面分子をターゲットとする抗体、たとえばアポリズマブまたは1D09C3、メタロプロテイナーゼの阻害剤、たとえばTIMP−1またはTIMP−2、亜鉛、癌遺伝子の阻害剤、たとえばP53およびRb、希土類元素の複合体、たとえばランタノイドの複素環複合体、光化学治療薬、たとえばPUVA、転写因子複合体ESX/DRIP130/Sur−2の阻害剤、HER−2発現阻害剤、たとえばヒートショックタンパク質HSP90分子ゲルダナマイシンおよびその誘導体17−アリルアミノゲルダナマイシンまたは17−AAG、またはIM−842、テトラチオモリビダード、スクアラミン、コンブレスタチンA4、TNP−470、マリマスタット、ネオバスタット、ビカルタミド、アバレリクス、オルゴボマブ、ミツモマブ、TLK−286、アレムツズマブ、イブリツモマブ、テモゾロマイド、デニロイキンジフチトクス、アルデスロイキン、ダカルバジン、フロクスウリジン、プリカマイシン、ミトタン、ピポブロマン、プリカマイシン、タモキシフェンおよびテストラクトンから選ばれる治療薬。 - 癌が、ゲフィチニブまたはエルロチニブのような可逆EGFRおよびHER2阻害剤による治療、またはCI−1033、EKB−569、HKI−272またはHKI−357のような他の不可逆阻害剤による治療に対して耐性または獲得耐性を示す請求項1〜6のいずれかに記載の使用。
- 癌が、ゲフィチニブおよび/またはエルロチニブでの治療に対して耐性または獲得耐性を示す請求項1〜6のいずれかに記載の使用。
- EGFR変異が、表1に載せた変異からなる群から選ばれる請求項1〜6のいずれかに記載の使用。
- EGFR変異が、表1のNo.1〜91で同定された変異からなる群から選ばれる請求項1〜6のいずれかに記載の使用。
- EGFR変異が、表1のNo.1〜29、57〜65、73、75、76、77、79および80〜91で同定された変異からなる群から選ばれる活性化変異である請求項1〜6のいずれかに記載の使用。
- EGFR変異が、表1のNo.92〜97で同定された変異からなる群から選ばれる請求項1〜6のいずれかに記載の使用。
- EGFR変異が、表1のNo.92、93、96、96−aおよび97で同定された変異からなる群から選ばれる請求項1〜6のいずれかに記載の使用。
- EGFR変異が、T790M、E746_A750del、E746_S752>V、L747_P753>S、L858R、L747_A750>P、S752_I759delからなる群から選ばれる請求項1〜6のいずれかに記載の使用。
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-
2007
- 2007-09-14 AU AU2007299080A patent/AU2007299080B2/en active Active
- 2007-09-14 EP EP07820235A patent/EP2068880B1/en not_active Revoked
- 2007-09-14 KR KR1020097007757A patent/KR20090074202A/ko not_active Application Discontinuation
- 2007-09-14 BR BRPI0717586-8A patent/BRPI0717586A2/pt not_active IP Right Cessation
- 2007-09-14 MX MX2009002710A patent/MX2009002710A/es active IP Right Grant
- 2007-09-14 RU RU2009114414/15A patent/RU2492864C2/ru active
- 2007-09-14 CA CA002663599A patent/CA2663599A1/en not_active Abandoned
- 2007-09-14 ES ES07820235T patent/ES2385613T3/es active Active
- 2007-09-14 JP JP2009528693A patent/JP2010503717A/ja active Pending
- 2007-09-14 PT PT07820235T patent/PT2068880E/pt unknown
- 2007-09-14 AT AT07820235T patent/ATE552835T1/de active
- 2007-09-14 PL PL07820235T patent/PL2068880T3/pl unknown
- 2007-09-14 WO PCT/EP2007/059735 patent/WO2008034776A1/en active Application Filing
- 2007-09-14 DK DK07820235.5T patent/DK2068880T3/da active
- 2007-09-14 SI SI200730957T patent/SI2068880T1/sl unknown
- 2007-09-14 US US12/441,180 patent/US8877764B2/en active Active
- 2007-09-14 NZ NZ576065A patent/NZ576065A/en unknown
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2009
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- 2012-07-06 CY CY20121100603T patent/CY1112896T1/el unknown
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