JP2007516194A5 - - Google Patents
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- JP2007516194A5 JP2007516194A5 JP2006518329A JP2006518329A JP2007516194A5 JP 2007516194 A5 JP2007516194 A5 JP 2007516194A5 JP 2006518329 A JP2006518329 A JP 2006518329A JP 2006518329 A JP2006518329 A JP 2006518329A JP 2007516194 A5 JP2007516194 A5 JP 2007516194A5
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- JP
- Japan
- Prior art keywords
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- substituents
- optionally substituted
- groups
- 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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- 125000001424 substituent group Chemical group 0.000 claims 63
- -1 cyano, nitro, carboxy, amino Chemical group 0.000 claims 57
- 239000001257 hydrogen Substances 0.000 claims 40
- 229910052739 hydrogen Inorganic materials 0.000 claims 40
- 229910052760 oxygen Inorganic materials 0.000 claims 32
- 125000000623 heterocyclic group Chemical group 0.000 claims 30
- 229910052736 halogen Inorganic materials 0.000 claims 29
- 150000002367 halogens Chemical class 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 27
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 26
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 24
- 125000005842 heteroatom Chemical group 0.000 claims 22
- 229910052717 sulfur Inorganic materials 0.000 claims 22
- 150000002431 hydrogen Chemical class 0.000 claims 19
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 18
- 239000008194 pharmaceutical composition Substances 0.000 claims 18
- 229910052757 nitrogen Inorganic materials 0.000 claims 17
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 14
- 125000002837 carbocyclic group Chemical group 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 13
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 13
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 11
- 125000004432 carbon atom Chemical group C* 0.000 claims 11
- 125000002950 monocyclic group Chemical group 0.000 claims 11
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 125000000217 alkyl group Chemical group 0.000 claims 8
- 229910002091 carbon monoxide Inorganic materials 0.000 claims 8
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 7
- 229910052731 fluorine Inorganic materials 0.000 claims 7
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 7
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 6
- 239000000460 chlorine Substances 0.000 claims 6
- 229910052801 chlorine Inorganic materials 0.000 claims 6
- 239000011737 fluorine Substances 0.000 claims 6
- 125000001153 fluoro group Chemical group F* 0.000 claims 6
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 6
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 5
- 150000001204 N-oxides Chemical class 0.000 claims 5
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 5
- 125000001309 chloro group Chemical group Cl* 0.000 claims 5
- 239000001301 oxygen Chemical group 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 239000012453 solvate Substances 0.000 claims 5
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- 125000004423 acyloxy group Chemical group 0.000 claims 4
- 125000003282 alkyl amino group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 239000011593 sulfur Substances 0.000 claims 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 3
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 3
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 125000002541 furyl group Chemical group 0.000 claims 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 230000002265 prevention Effects 0.000 claims 3
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 2
- 102000003989 Aurora kinases Human genes 0.000 claims 2
- 108090000433 Aurora kinases Proteins 0.000 claims 2
- 102000003903 Cyclin-dependent kinases Human genes 0.000 claims 2
- 108090000266 Cyclin-dependent kinases Proteins 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000004442 acylamino group Chemical group 0.000 claims 2
- 125000004466 alkoxycarbonylamino group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 238000006243 chemical reaction Methods 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 125000000842 isoxazolyl group Chemical group 0.000 claims 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 2
- 125000001064 morpholinomethyl group Chemical group [H]C([H])(*)N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H] 0.000 claims 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- ABADUMLIAZCWJD-UHFFFAOYSA-N 1,3-dioxole Chemical class C1OC=CO1 ABADUMLIAZCWJD-UHFFFAOYSA-N 0.000 claims 1
- 125000006508 2,6-difluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C(F)=C1[H])C([H])([H])* 0.000 claims 1
- 125000002941 2-furyl group Chemical group O1C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- KTLZQGKPJPIMTM-UHFFFAOYSA-N C1CCCN1C1N(N2CCCCC2)CCNC1 Chemical compound C1CCCN1C1N(N2CCCCC2)CCNC1 KTLZQGKPJPIMTM-UHFFFAOYSA-N 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 108091007911 GSKs Proteins 0.000 claims 1
- 102000002254 Glycogen Synthase Kinase 3 Human genes 0.000 claims 1
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 claims 1
- 102000004103 Glycogen Synthase Kinases Human genes 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010061534 Oesophageal squamous cell carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000036765 Squamous cell carcinoma of the esophagus Diseases 0.000 claims 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000005605 benzo group Chemical group 0.000 claims 1
- BNBQRQQYDMDJAH-UHFFFAOYSA-N benzodioxan Chemical compound C1=CC=C2OCCOC2=C1 BNBQRQQYDMDJAH-UHFFFAOYSA-N 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 125000002527 bicyclic carbocyclic group Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 239000004202 carbamide Substances 0.000 claims 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 208000007276 esophageal squamous cell carcinoma Diseases 0.000 claims 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001041 indolyl group Chemical group 0.000 claims 1
- IQPQWNKOIGAROB-UHFFFAOYSA-N isocyanate group Chemical group [N-]=C=O IQPQWNKOIGAROB-UHFFFAOYSA-N 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000005647 linker group Chemical group 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000001620 monocyclic carbocycle group Chemical group 0.000 claims 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
- 125000006518 morpholino carbonyl group Chemical group [H]C1([H])OC([H])([H])C([H])([H])N(C(*)=O)C1([H])[H] 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001567 quinoxalinyl group Chemical group N1=C(C=NC2=CC=CC=C12)* 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 0 **Nc1c[n]nc1-c1nc(cc(*)c(*)c2)c2[n]1 Chemical compound **Nc1c[n]nc1-c1nc(cc(*)c(*)c2)c2[n]1 0.000 description 2
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US48468503P | 2003-07-03 | 2003-07-03 | |
| GBGB0315657.7A GB0315657D0 (en) | 2003-07-03 | 2003-07-03 | Pharmaceutical compounds |
| US60/484,685 | 2003-07-03 | ||
| GB0315657.7 | 2003-07-03 | ||
| US51437403P | 2003-10-24 | 2003-10-24 | |
| GB0324919A GB0324919D0 (en) | 2003-10-24 | 2003-10-24 | Pharmaceutical compounds |
| US60/514,374 | 2003-10-24 | ||
| GB0324919.0 | 2003-10-24 | ||
| PCT/GB2004/002824 WO2005002552A2 (en) | 2003-07-03 | 2004-07-05 | Benzimidazole derivatives and their use as protein kinases inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2007516194A JP2007516194A (ja) | 2007-06-21 |
| JP2007516194A5 true JP2007516194A5 (enExample) | 2007-10-04 |
| JP4833059B2 JP4833059B2 (ja) | 2011-12-07 |
Family
ID=46045485
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006518329A Expired - Fee Related JP4833059B2 (ja) | 2003-07-03 | 2004-07-05 | 医薬化合物 |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US7977477B2 (enExample) |
| EP (2) | EP2305250B1 (enExample) |
| JP (1) | JP4833059B2 (enExample) |
| CN (1) | CN1845734B (enExample) |
| AU (1) | AU2004253338B2 (enExample) |
| CA (1) | CA2531050C (enExample) |
| DK (2) | DK2305250T3 (enExample) |
| ES (2) | ES2457466T3 (enExample) |
| MX (1) | MXPA05014223A (enExample) |
| NZ (1) | NZ543959A (enExample) |
| PL (2) | PL2305250T3 (enExample) |
| PT (2) | PT2305250E (enExample) |
| SI (2) | SI1648426T1 (enExample) |
| TW (1) | TWI372050B (enExample) |
| WO (1) | WO2005002552A2 (enExample) |
Families Citing this family (132)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI372050B (en) * | 2003-07-03 | 2012-09-11 | Astex Therapeutics Ltd | (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles |
| NZ544756A (en) | 2003-07-22 | 2009-09-25 | Astex Therapeutics Ltd | 3,4-Disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators |
| JP2007514759A (ja) | 2003-12-19 | 2007-06-07 | タケダ サン ディエゴ インコーポレイテッド | キナーゼ阻害剤 |
| US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
| CN1938279B (zh) * | 2004-01-30 | 2011-09-14 | 沃泰克斯药物股份有限公司 | Atp-结合弹夹转运蛋白调控剂 |
| EP1781653A1 (en) * | 2004-07-05 | 2007-05-09 | Astex Therapeutics Limited | 3,4-disubstituted pyrazoles as cyclin dependent kinases (cdk) or aurora kinase or glycogen synthase 3 (gsk-3) inhibitors |
| WO2006023931A2 (en) | 2004-08-18 | 2006-03-02 | Takeda San Diego, Inc. | Kinase inhibitors |
| ATE479687T1 (de) | 2004-10-15 | 2010-09-15 | Takeda Pharmaceutical | Kinaseinhibitoren |
| US7816369B2 (en) | 2004-11-03 | 2010-10-19 | Curis, Inc. | Mediators of hedgehog signaling pathways, compositions and uses related thereto |
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| JP5507049B2 (ja) * | 2004-12-30 | 2014-05-28 | アステックス、セラピューティックス、リミテッド | 医薬品 |
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| US8404718B2 (en) | 2005-01-21 | 2013-03-26 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors |
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| AR054425A1 (es) | 2005-01-21 | 2007-06-27 | Astex Therapeutics Ltd | Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico. |
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| WO2005047266A1 (en) | 2003-11-14 | 2005-05-26 | Lorus Therapeutics Inc. | Aryl imidazoles and their use as anti-cancer agents |
| US7932281B2 (en) * | 2004-03-10 | 2011-04-26 | Kureha Corporation | Amine-based compound and use thereof |
| US20080312223A1 (en) * | 2004-12-30 | 2008-12-18 | Astex Therapeutics Limited | Thiazole And Isothiazole Derivatives That Modulate The Activity Of CDK, GSK And Aurora Kinases |
| JP5507049B2 (ja) * | 2004-12-30 | 2014-05-28 | アステックス、セラピューティックス、リミテッド | 医薬品 |
| JP5474354B2 (ja) | 2005-12-30 | 2014-04-16 | アステックス、セラピューティックス、リミテッド | 医薬化合物 |
| US20110159111A1 (en) * | 2006-06-29 | 2011-06-30 | Astex Therapeutics Limited | Pharmaceutical combinations |
| JP5523829B2 (ja) | 2006-06-29 | 2014-06-18 | アステックス、セラピューティックス、リミテッド | 複合薬剤 |
| JP5528807B2 (ja) * | 2006-10-12 | 2014-06-25 | アステックス、セラピューティックス、リミテッド | 複合薬剤 |
-
2004
- 2004-07-02 TW TW093120042A patent/TWI372050B/zh not_active IP Right Cessation
- 2004-07-05 PL PL10195498T patent/PL2305250T3/pl unknown
- 2004-07-05 WO PCT/GB2004/002824 patent/WO2005002552A2/en not_active Ceased
- 2004-07-05 ES ES10195498.0T patent/ES2457466T3/es not_active Expired - Lifetime
- 2004-07-05 CN CN2004800249288A patent/CN1845734B/zh not_active Expired - Fee Related
- 2004-07-05 PL PL04743172T patent/PL1648426T3/pl unknown
- 2004-07-05 EP EP10195498.0A patent/EP2305250B1/en not_active Expired - Lifetime
- 2004-07-05 US US10/564,166 patent/US7977477B2/en not_active Expired - Fee Related
- 2004-07-05 CA CA2531050A patent/CA2531050C/en not_active Expired - Fee Related
- 2004-07-05 PT PT101954980T patent/PT2305250E/pt unknown
- 2004-07-05 DK DK10195498.0T patent/DK2305250T3/da active
- 2004-07-05 SI SI200432125T patent/SI1648426T1/sl unknown
- 2004-07-05 MX MXPA05014223A patent/MXPA05014223A/es active IP Right Grant
- 2004-07-05 AU AU2004253338A patent/AU2004253338B2/en not_active Ceased
- 2004-07-05 PT PT47431721T patent/PT1648426E/pt unknown
- 2004-07-05 JP JP2006518329A patent/JP4833059B2/ja not_active Expired - Fee Related
- 2004-07-05 NZ NZ543959A patent/NZ543959A/en not_active IP Right Cessation
- 2004-07-05 EP EP04743172.1A patent/EP1648426B1/en not_active Expired - Lifetime
- 2004-07-05 SI SI200432146T patent/SI2305250T1/sl unknown
- 2004-07-05 DK DK04743172.1T patent/DK1648426T3/da active
- 2004-07-05 ES ES04743172.1T patent/ES2443995T3/es not_active Expired - Lifetime
-
2011
- 2011-05-26 US US13/116,121 patent/US20110224203A1/en not_active Abandoned
-
2013
- 2013-05-24 US US13/902,325 patent/US20140010892A1/en not_active Abandoned
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