JP2009502921A5 - - Google Patents
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- Publication number
- JP2009502921A5 JP2009502921A5 JP2008523972A JP2008523972A JP2009502921A5 JP 2009502921 A5 JP2009502921 A5 JP 2009502921A5 JP 2008523972 A JP2008523972 A JP 2008523972A JP 2008523972 A JP2008523972 A JP 2008523972A JP 2009502921 A5 JP2009502921 A5 JP 2009502921A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- independently
- composition
- cancer
- substituted
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 43
- 239000000203 mixture Substances 0.000 claims 28
- 125000001931 aliphatic group Chemical group 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 230000002401 inhibitory effect Effects 0.000 claims 9
- 238000000034 method Methods 0.000 claims 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 201000011510 cancer Diseases 0.000 claims 6
- 230000000694 effects Effects 0.000 claims 6
- 229920006395 saturated elastomer Polymers 0.000 claims 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 5
- 239000012472 biological sample Substances 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 5
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 239000001301 oxygen Substances 0.000 claims 5
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- 229910052739 hydrogen Inorganic materials 0.000 claims 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 4
- 229910052717 sulfur Chemical group 0.000 claims 4
- 239000011593 sulfur Chemical group 0.000 claims 4
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 3
- 101710151245 Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 3
- 125000002723 alicyclic group Chemical group 0.000 claims 3
- 239000005441 aurora Substances 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 101000600756 Homo sapiens 3-phosphoinositide-dependent protein kinase 1 Proteins 0.000 claims 2
- 101001117146 Homo sapiens [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial Proteins 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 102000001253 Protein Kinase Human genes 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 210000003169 central nervous system Anatomy 0.000 claims 2
- 229940125782 compound 2 Drugs 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 230000011278 mitosis Effects 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 108060006633 protein kinase Proteins 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- FSPQCTGGIANIJZ-UHFFFAOYSA-N 2-[[(3,4-dimethoxyphenyl)-oxomethyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide Chemical compound C1=C(OC)C(OC)=CC=C1C(=O)NC1=C(C(N)=O)C(CCCC2)=C2S1 FSPQCTGGIANIJZ-UHFFFAOYSA-N 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- ZADPBFCGQRWHPN-UHFFFAOYSA-N boronic acid Chemical compound OBO ZADPBFCGQRWHPN-UHFFFAOYSA-N 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 230000008878 coupling Effects 0.000 claims 1
- 238000010168 coupling process Methods 0.000 claims 1
- 238000005859 coupling reaction Methods 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 238000006073 displacement reaction Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 229960005235 piperonyl butoxide Drugs 0.000 claims 1
- 125000004591 piperonyl group Chemical group C(C1=CC=2OCOC2C=C1)* 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 238000007363 ring formation reaction Methods 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 0 *Nc1nc2ccccc2[n]1* Chemical compound *Nc1nc2ccccc2[n]1* 0.000 description 9
- RHCPXBWBWPXEFT-UHFFFAOYSA-N C(C1)C1c1ncncc1 Chemical compound C(C1)C1c1ncncc1 RHCPXBWBWPXEFT-UHFFFAOYSA-N 0.000 description 1
- MXDRPNGTQDRKQM-UHFFFAOYSA-N Cc1nnccc1 Chemical compound Cc1nnccc1 MXDRPNGTQDRKQM-UHFFFAOYSA-N 0.000 description 1
- NOKGKKJGXQXNTO-UHFFFAOYSA-N Cc1nncnc1 Chemical compound Cc1nncnc1 NOKGKKJGXQXNTO-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US70239905P | 2005-07-26 | 2005-07-26 | |
| US60/702,399 | 2005-07-26 | ||
| PCT/US2006/028149 WO2007015923A2 (en) | 2005-07-26 | 2006-07-21 | Benzimidazoles useful as inhibitors of protein kinases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013025417A Division JP2013082757A (ja) | 2005-07-26 | 2013-02-13 | プロテインキナーゼ阻害薬として有用なベンズイミダゾール |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009502921A JP2009502921A (ja) | 2009-01-29 |
| JP2009502921A5 true JP2009502921A5 (enExample) | 2009-09-03 |
| JP5255438B2 JP5255438B2 (ja) | 2013-08-07 |
Family
ID=37680602
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008523972A Expired - Fee Related JP5255438B2 (ja) | 2005-07-26 | 2006-07-21 | プロテインキナーゼ阻害薬として有用なベンズイミダゾール |
| JP2013025417A Withdrawn JP2013082757A (ja) | 2005-07-26 | 2013-02-13 | プロテインキナーゼ阻害薬として有用なベンズイミダゾール |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013025417A Withdrawn JP2013082757A (ja) | 2005-07-26 | 2013-02-13 | プロテインキナーゼ阻害薬として有用なベンズイミダゾール |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8076343B2 (enExample) |
| EP (2) | EP1937667B1 (enExample) |
| JP (2) | JP5255438B2 (enExample) |
| KR (1) | KR20080034483A (enExample) |
| CN (1) | CN101291927A (enExample) |
| AT (1) | ATE484501T1 (enExample) |
| AU (1) | AU2006276088A1 (enExample) |
| CA (1) | CA2616159A1 (enExample) |
| DE (1) | DE602006017574D1 (enExample) |
| ES (1) | ES2351357T3 (enExample) |
| IL (1) | IL188942A0 (enExample) |
| NO (1) | NO20080967L (enExample) |
| NZ (1) | NZ566021A (enExample) |
| RU (1) | RU2415853C2 (enExample) |
| TW (1) | TW200745088A (enExample) |
| WO (1) | WO2007015923A2 (enExample) |
| ZA (1) | ZA200800992B (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7989465B2 (en) | 2007-10-19 | 2011-08-02 | Avila Therapeutics, Inc. | 4,6-disubstituted pyrimidines useful as kinase inhibitors |
| CA2920996A1 (en) | 2007-10-19 | 2009-04-23 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| US9273077B2 (en) | 2008-05-21 | 2016-03-01 | Ariad Pharmaceuticals, Inc. | Phosphorus derivatives as kinase inhibitors |
| AU2009248923B2 (en) | 2008-05-21 | 2015-01-29 | Takeda Pharmaceutical Company Limited | Phosphorous derivatives as kinase inhibitors |
| US9834518B2 (en) | 2011-05-04 | 2017-12-05 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| JP6469567B2 (ja) | 2012-05-05 | 2019-02-13 | アリアド・ファーマシューティカルズ・インコーポレイテッド | Egfr発動性がんの細胞増殖阻害用化合物 |
| US9336046B2 (en) | 2012-06-15 | 2016-05-10 | International Business Machines Corporation | Transaction abort processing |
| US9512136B2 (en) * | 2012-11-26 | 2016-12-06 | Universal Display Corporation | Organic electroluminescent materials and devices |
| WO2014147203A1 (en) * | 2013-03-21 | 2014-09-25 | Bayer Pharma Aktiengesellschaft | 3-heteroaryl substituted indazoles |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| WO2014170421A1 (en) * | 2013-04-19 | 2014-10-23 | F. Hoffmann-La Roche Ag | Serine/threonine kinase inhibitors |
| ITUA20164278A1 (it) * | 2016-06-10 | 2017-12-10 | International Soc For Drug Development S R L | COMPOSTI 2-OXO-1,2-DIIDROPIRIDIN-3-CARBOSSAMMIDE E LORO USO COME INIBITORI DUALI DI PDK1/AurA |
| US10793551B2 (en) | 2017-10-19 | 2020-10-06 | Effector Therapeutics Inc. | Benzimidazole-indole inhibitors of Mnk1 and Mnk2 |
| CN112552287B (zh) * | 2020-12-16 | 2021-11-30 | 北京华氏精恒医药科技有限公司 | 一种吲哚类衍生物药物制剂及其制备方法 |
| WO2023116888A1 (zh) * | 2021-12-23 | 2023-06-29 | 杭州多域生物技术有限公司 | 一种五元并六元化合物、制备方法、药物组合物和应用 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL143157A0 (en) | 1998-11-17 | 2002-04-21 | Kumiai Chemical Industry Co | Pyrimidinylbenzimidazole and triazinylbenzimidazole derivatives and agricultural/horticultural bactericides |
| JP4535350B2 (ja) * | 1998-11-17 | 2010-09-01 | クミアイ化学工業株式会社 | ピリミジニルベンズイミダゾール誘導体及び農園芸用殺菌剤 |
| CA2386218A1 (en) | 1999-10-07 | 2001-04-12 | Amgen Inc. | Triazine kinase inhibitors |
| CA2400447C (en) * | 2000-02-17 | 2008-04-22 | Amgen Inc. | Kinase inhibitors |
| DE60217322T2 (de) * | 2001-04-27 | 2007-10-04 | Zenyaku Kogyo K.K. | Heterocyclische verbindung und antitumormittel, das diese als wirkstoff enthält |
| FR2833948B1 (fr) * | 2001-12-21 | 2004-02-06 | Sod Conseils Rech Applic | Nouveaux derives de benzimidazole et leur utilisation en tant que medicament |
| WO2003099811A1 (en) * | 2002-05-23 | 2003-12-04 | Cytopia Pty Ltd | Kinase inhibitors |
| CL2003002353A1 (es) * | 2002-11-15 | 2005-02-04 | Vertex Pharma | Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic |
| UA80767C2 (en) * | 2002-12-20 | 2007-10-25 | Pfizer Prod Inc | Pyrimidine derivatives for the treatment of abnormal cell growth |
| GB2432834A (en) * | 2004-01-12 | 2007-06-06 | Cytopia Res Pty Ltd | Selective Kinase Inhibitors |
-
2006
- 2006-07-21 CN CNA2006800343024A patent/CN101291927A/zh active Pending
- 2006-07-21 JP JP2008523972A patent/JP5255438B2/ja not_active Expired - Fee Related
- 2006-07-21 ES ES06787944T patent/ES2351357T3/es active Active
- 2006-07-21 EP EP06787944A patent/EP1937667B1/en not_active Not-in-force
- 2006-07-21 KR KR1020087004634A patent/KR20080034483A/ko not_active Ceased
- 2006-07-21 ZA ZA200800992A patent/ZA200800992B/xx unknown
- 2006-07-21 CA CA002616159A patent/CA2616159A1/en not_active Abandoned
- 2006-07-21 RU RU2008106949/04A patent/RU2415853C2/ru not_active IP Right Cessation
- 2006-07-21 US US11/492,643 patent/US8076343B2/en not_active Expired - Fee Related
- 2006-07-21 NZ NZ566021A patent/NZ566021A/en not_active IP Right Cessation
- 2006-07-21 EP EP10185388.5A patent/EP2336122B1/en not_active Not-in-force
- 2006-07-21 DE DE602006017574T patent/DE602006017574D1/de active Active
- 2006-07-21 AT AT06787944T patent/ATE484501T1/de not_active IP Right Cessation
- 2006-07-21 WO PCT/US2006/028149 patent/WO2007015923A2/en not_active Ceased
- 2006-07-21 AU AU2006276088A patent/AU2006276088A1/en not_active Abandoned
- 2006-07-26 TW TW095127328A patent/TW200745088A/zh unknown
-
2008
- 2008-01-22 IL IL188942A patent/IL188942A0/en unknown
- 2008-02-26 NO NO20080967A patent/NO20080967L/no not_active Application Discontinuation
-
2013
- 2013-02-13 JP JP2013025417A patent/JP2013082757A/ja not_active Withdrawn
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