JP2012520321A5 - - Google Patents

Info

Publication number

JP2012520321A5

JP2012520321A5 JP2011554220A JP2011554220A JP2012520321A5 JP 2012520321 A5 JP2012520321 A5 JP 2012520321A5 JP 2011554220 A JP2011554220 A JP 2011554220A JP 2011554220 A JP2011554220 A JP 2011554220A JP 2012520321 A5 JP2012520321 A5 JP 2012520321A5

Authority

JP

Japan

Prior art keywords

effective amount

therapeutically effective

difluoro

pharmaceutical composition

iodophenylamino

Prior art date

2010-03-11

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

• Espacenet
• Global Dossier
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• 239000008194 pharmaceutical composition Substances 0.000 claims 32
• RDSACQWTXKSHJT-NSHDSACASA-N n-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2s)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide Chemical compound C1CC1(C[C@H](O)CO)S(=O)(=O)NC=1C(OC)=CC(F)=C(F)C=1NC1=CC=C(I)C=C1F RDSACQWTXKSHJT-NSHDSACASA-N 0.000 claims 24
• 150000003839 salts Chemical class 0.000 claims 24
• 239000011885 synergistic combination Substances 0.000 claims 16
• 239000000203 mixture Substances 0.000 claims 14
• 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 8
• -1 6,7-bis (2-methoxyethoxy) quinazolin-4-ylamino Chemical group 0.000 claims 6
• 125000004192 tetrahydrofuran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C1([H])[H] 0.000 claims 5
• 208000024770 Thyroid neoplasm Diseases 0.000 claims 4
• 201000002510 thyroid cancer Diseases 0.000 claims 4
• DYPIHQVLLQBLGP-UHFFFAOYSA-N 2-(3-morpholin-4-ylpropoxy)quinazolin-4-amine Chemical compound N=1C2=CC=CC=C2C(N)=NC=1OCCCN1CCOCC1 DYPIHQVLLQBLGP-UHFFFAOYSA-N 0.000 claims 3
• 206010006187 Breast cancer Diseases 0.000 claims 3
• 208000026310 Breast neoplasm Diseases 0.000 claims 3
• 239000004593 Epoxy Substances 0.000 claims 3
• UWYXLGUQQFPJRI-UHFFFAOYSA-N n-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine;4-methylbenzenesulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1.CC1=CC=C(S(O)(=O)=O)C=C1.O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 UWYXLGUQQFPJRI-UHFFFAOYSA-N 0.000 claims 3
• 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 3
• 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
• 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 3
• 206010028980 Neoplasm Diseases 0.000 claims 2
• 238000011374 additional therapy Methods 0.000 claims 2
• 239000002246 antineoplastic agent Substances 0.000 claims 2
• 201000011510 cancer Diseases 0.000 claims 2
• 229940127089 cytotoxic agent Drugs 0.000 claims 2
• 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
• 201000001441 melanoma Diseases 0.000 claims 2
• QJIHCROKGYMFNF-UHFFFAOYSA-N 3-[[6,7-bis(2-methoxyethoxy)quinazolin-4-yl]amino]benzonitrile Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#N)=C1 QJIHCROKGYMFNF-UHFFFAOYSA-N 0.000 claims 1
• 206010009944 Colon cancer Diseases 0.000 claims 1
• 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
• BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical compound O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 claims 1
• 208000009956 adenocarcinoma Diseases 0.000 claims 1
• 150000001412 amines Chemical class 0.000 claims 1
• 208000029742 colonic neoplasm Diseases 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• 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 1
• SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 1
• AKWHREAVLKZDDE-UHFFFAOYSA-N hexatriaconta-16,24,26,28-tetraene-2,3,10,14,20-pentone Chemical compound CCCCCCCC=CC=CC=CCCCC(=O)CCC=CCC(=O)CCCC(=O)CCCCCCC(=O)C(C)=O AKWHREAVLKZDDE-UHFFFAOYSA-N 0.000 claims 1
• 201000007270 liver cancer Diseases 0.000 claims 1
• 208000014018 liver neoplasm Diseases 0.000 claims 1
• 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
• 201000002528 pancreatic cancer Diseases 0.000 claims 1
• 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
• 238000001959 radiotherapy Methods 0.000 claims 1
• WAEXFXRVDQXREF-UHFFFAOYSA-N vorinostat Chemical compound ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1 WAEXFXRVDQXREF-UHFFFAOYSA-N 0.000 claims 1
• RFRJWGMOFBZAKC-DWCOZBPGSA-N CCC(/C=C\N([C@@H](C1(F)F)O[C@H](CO)C1O)C(N)=O)N Chemical compound CCC(/C=C\N([C@@H](C1(F)F)O[C@H](CO)C1O)C(N)=O)N RFRJWGMOFBZAKC-DWCOZBPGSA-N 0.000 description 1
• SSEZZHCCCUDIHL-UHFFFAOYSA-N CN(C([n]1c(N)c(C(N)=O)nc1)=O)N Chemical compound CN(C([n]1c(N)c(C(N)=O)nc1)=O)N SSEZZHCCCUDIHL-UHFFFAOYSA-N 0.000 description 1