JP2007509059A5 - - Google Patents
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- JP2007509059A5 JP2007509059A5 JP2006535368A JP2006535368A JP2007509059A5 JP 2007509059 A5 JP2007509059 A5 JP 2007509059A5 JP 2006535368 A JP2006535368 A JP 2006535368A JP 2006535368 A JP2006535368 A JP 2006535368A JP 2007509059 A5 JP2007509059 A5 JP 2007509059A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- heteroaryl
- compound
- aminoalkyl
- 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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- -1 heterocycloaryl Chemical group 0.000 claims 179
- 150000001875 compounds Chemical class 0.000 claims 79
- 125000000217 alkyl group Chemical group 0.000 claims 61
- 125000001072 heteroaryl group Chemical group 0.000 claims 47
- 125000004103 aminoalkyl group Chemical group 0.000 claims 40
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 37
- 229910052739 hydrogen Inorganic materials 0.000 claims 35
- 125000003118 aryl group Chemical group 0.000 claims 32
- 239000001257 hydrogen Substances 0.000 claims 31
- 125000000753 cycloalkyl group Chemical group 0.000 claims 29
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 21
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 20
- 125000003545 alkoxy group Chemical group 0.000 claims 20
- 239000000203 mixture Substances 0.000 claims 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 17
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 17
- 150000002431 hydrogen Chemical class 0.000 claims 14
- 206010028980 Neoplasm Diseases 0.000 claims 13
- 201000011510 cancer Diseases 0.000 claims 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 11
- 241001465754 Metazoa Species 0.000 claims 9
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 8
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 8
- 125000002252 acyl group Chemical group 0.000 claims 8
- ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 8
- 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 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000001624 naphthyl group Chemical group 0.000 claims 8
- 125000000068 chlorophenyl group Chemical group 0.000 claims 7
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 7
- 230000000694 effects Effects 0.000 claims 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 5
- 102000009929 raf Kinases Human genes 0.000 claims 5
- 108010077182 raf Kinases Proteins 0.000 claims 5
- FDKXTQMXEQVLRF-ZHACJKMWSA-N (E)-dacarbazine Chemical compound CN(C)\N=N\c1[nH]cnc1C(N)=O FDKXTQMXEQVLRF-ZHACJKMWSA-N 0.000 claims 4
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 4
- YBYIRNPNPLQARY-UHFFFAOYSA-N 1H-indene Natural products C1=CC=C2CC=CC2=C1 YBYIRNPNPLQARY-UHFFFAOYSA-N 0.000 claims 4
- VVIAGPKUTFNRDU-UHFFFAOYSA-N 6S-folinic acid Natural products C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)NC(CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-UHFFFAOYSA-N 0.000 claims 4
- GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims 4
- GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 claims 4
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims 4
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 4
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims 4
- 229940123237 Taxane Drugs 0.000 claims 4
- 229940122803 Vinca alkaloid Drugs 0.000 claims 4
- 125000005073 adamantyl group Chemical group C12(CC3CC(CC(C1)C3)C2)* 0.000 claims 4
- 229960005310 aldesleukin Drugs 0.000 claims 4
- 108700025316 aldesleukin Proteins 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000005036 alkoxyphenyl group Chemical group 0.000 claims 4
- 125000000278 alkyl amino alkyl group Chemical group 0.000 claims 4
- 125000005037 alkyl phenyl group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- 150000001413 amino acids Chemical class 0.000 claims 4
- HSMPSHPWCOOUJH-UHFFFAOYSA-N anilinyl Chemical group [NH]C1=CC=CC=C1 HSMPSHPWCOOUJH-UHFFFAOYSA-N 0.000 claims 4
- 229940045799 anthracyclines and related substance Drugs 0.000 claims 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims 4
- 125000005128 aryl amino alkyl group Chemical group 0.000 claims 4
- 125000001769 aryl amino group Chemical group 0.000 claims 4
- 125000005160 aryl oxy alkyl group Chemical group 0.000 claims 4
- 125000004104 aryloxy group Chemical group 0.000 claims 4
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims 4
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 4
- RWCCWEUUXYIKHB-UHFFFAOYSA-N benzophenone Chemical compound C=1C=CC=CC=1C(=O)C1=CC=CC=C1 RWCCWEUUXYIKHB-UHFFFAOYSA-N 0.000 claims 4
- 239000012965 benzophenone Substances 0.000 claims 4
- 150000005347 biaryls Chemical group 0.000 claims 4
- 235000010290 biphenyl Nutrition 0.000 claims 4
- 239000004305 biphenyl Substances 0.000 claims 4
- 125000004799 bromophenyl group Chemical group 0.000 claims 4
- 229960004117 capecitabine Drugs 0.000 claims 4
- 229960004562 carboplatin Drugs 0.000 claims 4
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 4
- 229960004316 cisplatin Drugs 0.000 claims 4
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 4
- 125000004858 cycloalkoxyalkyl group Chemical group 0.000 claims 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 4
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims 4
- 125000004367 cycloalkylaryl group Chemical group 0.000 claims 4
- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 4
- WVIIMZNLDWSIRH-UHFFFAOYSA-N cyclohexylcyclohexane Chemical group C1CCCCC1C1CCCCC1 WVIIMZNLDWSIRH-UHFFFAOYSA-N 0.000 claims 4
- 229960004397 cyclophosphamide Drugs 0.000 claims 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 4
- 229960003901 dacarbazine Drugs 0.000 claims 4
- 125000004985 dialkyl amino alkyl group Chemical group 0.000 claims 4
- 125000004986 diarylamino group Chemical group 0.000 claims 4
- 125000004188 dichlorophenyl group Chemical group 0.000 claims 4
- 125000004212 difluorophenyl group Chemical group 0.000 claims 4
- 125000005240 diheteroarylamino group Chemical group 0.000 claims 4
- 229960002949 fluorouracil Drugs 0.000 claims 4
- VVIAGPKUTFNRDU-ABLWVSNPSA-N folinic acid Chemical compound C1NC=2NC(N)=NC(=O)C=2N(C=O)C1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 VVIAGPKUTFNRDU-ABLWVSNPSA-N 0.000 claims 4
- 235000008191 folinic acid Nutrition 0.000 claims 4
- 239000011672 folinic acid Substances 0.000 claims 4
- 125000002541 furyl group Chemical group 0.000 claims 4
- 229960002584 gefitinib Drugs 0.000 claims 4
- 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 4
- 229960005277 gemcitabine Drugs 0.000 claims 4
- 125000006485 halo alkoxy phenyl group Chemical group 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- 125000005059 halophenyl group Chemical group 0.000 claims 4
- 125000005241 heteroarylamino group Chemical group 0.000 claims 4
- 125000005326 heteroaryloxy alkyl group Chemical group 0.000 claims 4
- 125000005553 heteroaryloxy group Chemical group 0.000 claims 4
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 4
- 125000004464 hydroxyphenyl group Chemical group 0.000 claims 4
- 229960002411 imatinib Drugs 0.000 claims 4
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims 4
- 125000002883 imidazolyl group Chemical group 0.000 claims 4
- 125000003454 indenyl group Chemical group C1(C=CC2=CC=CC=C12)* 0.000 claims 4
- 125000001041 indolyl group Chemical group 0.000 claims 4
- 125000006303 iodophenyl group Chemical group 0.000 claims 4
- 229940084651 iressa Drugs 0.000 claims 4
- 229960004768 irinotecan Drugs 0.000 claims 4
- 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 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims 4
- 229960001691 leucovorin Drugs 0.000 claims 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
- 125000002757 morpholinyl group Chemical group 0.000 claims 4
- 125000006501 nitrophenyl group Chemical group 0.000 claims 4
- 125000003884 phenylalkyl group Chemical group 0.000 claims 4
- 125000003170 phenylsulfonyl group Chemical group C1(=CC=CC=C1)S(=O)(=O)* 0.000 claims 4
- NAYYNDKKHOIIOD-UHFFFAOYSA-N phthalamide Chemical compound NC(=O)C1=CC=CC=C1C(N)=O NAYYNDKKHOIIOD-UHFFFAOYSA-N 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 229940002612 prodrug Drugs 0.000 claims 4
- 239000000651 prodrug Substances 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 4
- 125000004621 quinuclidinyl group Chemical group N12C(CC(CC1)CC2)* 0.000 claims 4
- 229960004641 rituximab Drugs 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000005329 tetralinyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 claims 4
- 229950006410 tezacitabine Drugs 0.000 claims 4
- GFFXZLZWLOBBLO-ASKVSEFXSA-N tezacitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(=C/F)/[C@H](O)[C@@H](CO)O1 GFFXZLZWLOBBLO-ASKVSEFXSA-N 0.000 claims 4
- 229930192474 thiophene Natural products 0.000 claims 4
- QERYCTSHXKAMIS-UHFFFAOYSA-M thiophene-2-carboxylate Chemical compound [O-]C(=O)C1=CC=CS1 QERYCTSHXKAMIS-UHFFFAOYSA-M 0.000 claims 4
- 229960000303 topotecan Drugs 0.000 claims 4
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims 4
- 229960000575 trastuzumab Drugs 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- DLAHAXOYRFRPFQ-UHFFFAOYSA-N dodecyl benzoate Chemical compound CCCCCCCCCCCCOC(=O)C1=CC=CC=C1 DLAHAXOYRFRPFQ-UHFFFAOYSA-N 0.000 claims 3
- 125000001207 fluorophenyl group Chemical group 0.000 claims 3
- HKIOYBQGHSTUDB-UHFFFAOYSA-N folpet Chemical group C1=CC=C2C(=O)N(SC(Cl)(Cl)Cl)C(=O)C2=C1 HKIOYBQGHSTUDB-UHFFFAOYSA-N 0.000 claims 3
- 125000004360 trifluorophenyl group Chemical group 0.000 claims 3
- 230000001419 dependent effect Effects 0.000 claims 2
- 229940088597 hormone Drugs 0.000 claims 2
- 239000005556 hormone Substances 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002489 hematologic effect Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US51185103P | 2003-10-16 | 2003-10-16 | |
| PCT/US2004/034185 WO2005037285A1 (en) | 2003-10-16 | 2004-10-15 | 2,6-disubstituted quinazolines, quinoxalines, quinolines and isoquinolines as inhibitors of raf kinase for treatment of cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007509059A JP2007509059A (ja) | 2007-04-12 |
| JP2007509059A5 true JP2007509059A5 (cg-RX-API-DMAC7.html) | 2007-09-06 |
Family
ID=34465285
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006535368A Pending JP2007509059A (ja) | 2003-10-16 | 2004-10-15 | 癌の処置のためのＲａｆキナーゼのインヒビターとしての、２，６−二置換キナゾリン、キノキサリン、キノリンおよびイソキノリン |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US20050084835A1 (cg-RX-API-DMAC7.html) |
| EP (1) | EP1680122A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2007509059A (cg-RX-API-DMAC7.html) |
| KR (1) | KR20070029110A (cg-RX-API-DMAC7.html) |
| CN (1) | CN1882345A (cg-RX-API-DMAC7.html) |
| AU (1) | AU2004281154A1 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2542329A1 (cg-RX-API-DMAC7.html) |
| IL (1) | IL174470A0 (cg-RX-API-DMAC7.html) |
| MX (1) | MXPA06003607A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2005037285A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (65)
| Publication number | Priority date | Publication date | Assignee | Title |
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| ME00275B (me) | 1999-01-13 | 2011-02-10 | Bayer Corp | ω-KARBOKSIARIL SUPSTITUISANI DIFENIL KARBAMIDI KAO INHIBITORI RAF KINAZE |
| JP2002534468A (ja) | 1999-01-13 | 2002-10-15 | バイエル コーポレイション | ｐ３８キナーゼ阻害剤としてのω−カルボキシアリール置換ジフェニル尿素 |
| US8124630B2 (en) | 1999-01-13 | 2012-02-28 | Bayer Healthcare Llc | ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors |
| PT1478358E (pt) | 2002-02-11 | 2013-09-11 | Bayer Healthcare Llc | Tosilato de sorafenib para o tratamento de doenças caracterizadas por angiogénese anormal |
| US20030216396A1 (en) | 2002-02-11 | 2003-11-20 | Bayer Corporation | Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors |
| US7557129B2 (en) | 2003-02-28 | 2009-07-07 | Bayer Healthcare Llc | Cyanopyridine derivatives useful in the treatment of cancer and other disorders |
| PL1626714T3 (pl) | 2003-05-20 | 2007-12-31 | Bayer Healthcare Llc | Diarylowe pochodne mocznika do schorzeń, w których pośredniczy PDGFR |
| CN102816113B (zh) | 2003-07-23 | 2015-05-13 | 拜耳医药保健有限责任公司 | 用于治疗和预防疾病和疾病症状的氟代ω-羧芳基二苯基脲 |
| BRPI0507373A (pt) * | 2004-01-23 | 2007-07-10 | Amgen Inc | compostos e método de uso |
| US20070054916A1 (en) * | 2004-10-01 | 2007-03-08 | Amgen Inc. | Aryl nitrogen-containing bicyclic compounds and methods of use |
| MX2007006230A (es) | 2004-11-30 | 2007-07-25 | Amgen Inc | Quinolinas y analogos de quinazolinas y su uso como medicamentos para tratar cancer. |
| JO2787B1 (en) | 2005-04-27 | 2014-03-15 | امجين إنك, | Alternative amide derivatives and methods of use |
| US20060292537A1 (en) * | 2005-06-27 | 2006-12-28 | Arcturus Media, Inc. | System and method for conducting multimedia karaoke sessions |
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| NZ587907A (en) | 2008-03-17 | 2012-09-28 | Ambit Biosciences Corp | Quinazoline derivatives as RAF kinase modulators and methods of use thereof |
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| US10253020B2 (en) | 2009-06-12 | 2019-04-09 | Abivax | Compounds for preventing, inhibiting, or treating cancer, AIDS and/or premature aging |
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-
2004
- 2004-10-15 AU AU2004281154A patent/AU2004281154A1/en not_active Abandoned
- 2004-10-15 EP EP04795363A patent/EP1680122A1/en not_active Withdrawn
- 2004-10-15 JP JP2006535368A patent/JP2007509059A/ja active Pending
- 2004-10-15 CA CA002542329A patent/CA2542329A1/en not_active Abandoned
- 2004-10-15 WO PCT/US2004/034185 patent/WO2005037285A1/en not_active Ceased
- 2004-10-15 CN CNA200480030549XA patent/CN1882345A/zh active Pending
- 2004-10-15 KR KR1020067007130A patent/KR20070029110A/ko not_active Ceased
- 2004-10-15 US US10/966,073 patent/US20050084835A1/en not_active Abandoned
- 2004-10-15 MX MXPA06003607A patent/MXPA06003607A/es unknown
- 2004-10-15 US US10/966,358 patent/US7691866B2/en not_active Expired - Fee Related
-
2006
- 2006-03-21 IL IL174470A patent/IL174470A0/en unknown
-
2009
- 2009-09-04 US US12/554,748 patent/US20090317359A1/en not_active Abandoned
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