JP2006503919A5 - - Google Patents
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- JP2006503919A5 JP2006503919A5 JP2005501762A JP2005501762A JP2006503919A5 JP 2006503919 A5 JP2006503919 A5 JP 2006503919A5 JP 2005501762 A JP2005501762 A JP 2005501762A JP 2005501762 A JP2005501762 A JP 2005501762A JP 2006503919 A5 JP2006503919 A5 JP 2006503919A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- composition
- group
- drug
- topoisomerase
- 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
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- 206010028980 Neoplasm Diseases 0.000 claims description 7
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 5
- 201000011510 cancer Diseases 0.000 claims description 5
- 208000029742 colonic neoplasm Diseases 0.000 claims description 5
- 229960004768 irinotecan Drugs 0.000 claims description 5
- 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 description 5
- 238000002648 combination therapy Methods 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 claims description 4
- 201000005787 hematologic cancer Diseases 0.000 claims description 4
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims description 4
- 229960002949 fluorouracil Drugs 0.000 claims description 3
- 239000007787 solid Substances 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 10
- 229940079593 drug Drugs 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 206010006187 Breast cancer Diseases 0.000 claims 4
- 208000026310 Breast neoplasm Diseases 0.000 claims 4
- 206010009944 Colon cancer Diseases 0.000 claims 4
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin 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
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 4
- 206010033128 Ovarian cancer Diseases 0.000 claims 4
- 206010060862 Prostate cancer Diseases 0.000 claims 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 4
- 239000002246 antineoplastic agent Substances 0.000 claims 4
- 229940041181 antineoplastic drug Drugs 0.000 claims 4
- 201000005202 lung cancer Diseases 0.000 claims 4
- 208000020816 lung neoplasm Diseases 0.000 claims 4
- 230000009036 growth inhibition Effects 0.000 claims 3
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 2
- 229940123780 DNA topoisomerase I inhibitor Drugs 0.000 claims 2
- 229940124087 DNA topoisomerase II inhibitor Drugs 0.000 claims 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 208000007913 Pituitary Neoplasms Diseases 0.000 claims 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 239000000365 Topoisomerase I Inhibitor Substances 0.000 claims 2
- 239000000317 Topoisomerase II Inhibitor Substances 0.000 claims 2
- 229940100198 alkylating agent Drugs 0.000 claims 2
- 239000002168 alkylating agent Substances 0.000 claims 2
- 239000012635 anticancer drug combination Substances 0.000 claims 2
- 229940127093 camptothecin Drugs 0.000 claims 2
- 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
- 229960004316 cisplatin Drugs 0.000 claims 2
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 2
- 229940046044 combinations of antineoplastic agent Drugs 0.000 claims 2
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims 2
- 229960004679 doxorubicin Drugs 0.000 claims 2
- 238000007918 intramuscular administration Methods 0.000 claims 2
- 238000007912 intraperitoneal administration Methods 0.000 claims 2
- 238000001990 intravenous administration Methods 0.000 claims 2
- 201000002511 pituitary cancer Diseases 0.000 claims 2
- 229960000575 trastuzumab Drugs 0.000 claims 2
- 238000001959 radiotherapy Methods 0.000 claims 1
- LISFMEBWQUVKPJ-UHFFFAOYSA-N quinolin-2-ol Chemical compound C1=CC=C2NC(=O)C=CC2=C1 LISFMEBWQUVKPJ-UHFFFAOYSA-N 0.000 description 3
- PIQCTGMSNWUMAF-UHFFFAOYSA-N chembl522892 Chemical compound C1CN(C)CCN1C1=CC=C(NC(=N2)C=3C(NC4=CC=CC(F)=C4C=3N)=O)C2=C1 PIQCTGMSNWUMAF-UHFFFAOYSA-N 0.000 description 2
- 230000000694 effects Effects 0.000 description 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 description 2
- 230000002195 synergetic effect Effects 0.000 description 2
- 125000004174 2-benzimidazolyl group Chemical group [H]N1C(*)=NC2=C([H])C([H])=C([H])C([H])=C12 0.000 description 1
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 description 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 description 1
- 230000002730 additional effect Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 231100000599 cytotoxic agent Toxicity 0.000 description 1
- 239000002619 cytotoxin Substances 0.000 description 1
- 229940084651 iressa Drugs 0.000 description 1
- 230000000737 periodic effect Effects 0.000 description 1
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40572902P | 2002-08-23 | 2002-08-23 | |
| US42610702P | 2002-11-13 | 2002-11-13 | |
| US42622602P | 2002-11-13 | 2002-11-13 | |
| US42628202P | 2002-11-13 | 2002-11-13 | |
| US42821002P | 2002-11-21 | 2002-11-21 | |
| US46032803P | 2003-04-03 | 2003-04-03 | |
| US46049303P | 2003-04-03 | 2003-04-03 | |
| US46032703P | 2003-04-03 | 2003-04-03 | |
| US47891603P | 2003-06-16 | 2003-06-16 | |
| US48404803P | 2003-07-01 | 2003-07-01 | |
| PCT/US2003/025990 WO2004018419A2 (en) | 2002-08-23 | 2003-08-19 | Benzimidazole quinolinones and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2006503919A JP2006503919A (ja) | 2006-02-02 |
| JP2006503919A5 true JP2006503919A5 (https=) | 2010-10-28 |
| JP4613130B2 JP4613130B2 (ja) | 2011-01-12 |
Family
ID=31950997
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2005501762A Expired - Fee Related JP4613130B2 (ja) | 2002-08-23 | 2003-08-19 | ベンゾイミダゾールキノリノンおよびそれらの使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US7470709B2 (https=) |
| EP (2) | EP1539754A4 (https=) |
| JP (1) | JP4613130B2 (https=) |
| KR (1) | KR20050037585A (https=) |
| AU (1) | AU2003288899B2 (https=) |
| BR (1) | BR0313743A (https=) |
| CA (1) | CA2496164C (https=) |
| IL (1) | IL166932A (https=) |
| TW (1) | TWI345567B (https=) |
| WO (1) | WO2004018419A2 (https=) |
Families Citing this family (121)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE448226T1 (de) | 2000-09-01 | 2009-11-15 | Novartis Vaccines & Diagnostic | Aza heterocyclische derivate und ihre therapeutische verwendung |
| US20030028018A1 (en) * | 2000-09-11 | 2003-02-06 | Chiron Coporation | Quinolinone derivatives |
| DE60115069T2 (de) | 2000-09-11 | 2006-08-03 | Chiron Corp., Emeryville | Chinolinonderivate als tyrosin-kinase inhibitoren |
| US20090118139A1 (en) * | 2000-11-07 | 2009-05-07 | Caliper Life Sciences, Inc. | Microfluidic method and system for enzyme inhibition activity screening |
| EP1539754A4 (en) * | 2002-08-23 | 2009-02-25 | Novartis Vaccines & Diagnostic | BENZIMIDAZOCHINOLINONE AND ITS USE |
| US7825132B2 (en) * | 2002-08-23 | 2010-11-02 | Novartis Vaccines And Diagnostics, Inc. | Inhibition of FGFR3 and treatment of multiple myeloma |
| US20050256157A1 (en) * | 2002-08-23 | 2005-11-17 | Chiron Corporation | Combination therapy with CHK1 inhibitors |
| AU2003275282A1 (en) | 2002-09-30 | 2004-04-23 | Bristol-Myers Squibb Company | Novel tyrosine kinase inhibitors |
| SG148864A1 (en) * | 2002-11-13 | 2009-01-29 | Chiron Corp | Methods of treating cancer and related methods |
| EP1571146A4 (en) | 2002-12-10 | 2010-09-01 | Ono Pharmaceutical Co | NITROGENIC HETEROCYCLIC COMPOUNDS AND THEIR MEDICAL USE |
| WO2004087153A2 (en) * | 2003-03-28 | 2004-10-14 | Chiron Corporation | Use of organic compounds for immunopotentiation |
| JP2006522814A (ja) * | 2003-04-11 | 2006-10-05 | タイゲン・バイオテクノロジー | アミノキノリン化合物 |
| EP1660087A2 (en) * | 2003-07-22 | 2006-05-31 | Janssen Pharmaceutica N.V. | Quinolinone derivatives as inhibitors of c-fms kinase |
| AU2004274013A1 (en) * | 2003-09-17 | 2005-03-31 | Icos Corporation | Use of Chk1 inhibitors to control cell proliferation |
| US20050209247A1 (en) * | 2003-11-07 | 2005-09-22 | Chiron Corporation | Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties |
| US20050171182A1 (en) * | 2003-12-11 | 2005-08-04 | Roger Briesewitz | Methods and compositions for use in the treatment of mutant receptor tyrosine kinase driven cellular proliferative diseases |
| TW200533657A (en) * | 2004-02-17 | 2005-10-16 | Esteve Labor Dr | Substituted pyrazoline compounds, their preparation and use as medicaments |
| EP1718306A2 (en) | 2004-02-20 | 2006-11-08 | Chiron Corporation | Modulation of inflammatory and metastatic processes |
| US20050276765A1 (en) * | 2004-06-10 | 2005-12-15 | Paul Nghiem | Preventing skin damage |
| US7850960B2 (en) * | 2004-12-30 | 2010-12-14 | University Of Washington | Methods for regulation of stem cells |
| EP2301546B1 (en) * | 2005-01-27 | 2014-09-10 | Novartis AG | Treatment of metastasized tumors |
| US20060223849A1 (en) * | 2005-03-14 | 2006-10-05 | Mjalli Adnan M | Benzazole derivatives, compositions, and methods of use as beta-secretase inhibitors |
| HRP20100678T1 (hr) | 2005-03-29 | 2011-02-28 | Icos Corporation | Derivati heteroariluree korisni kao inhibitori chk1 |
| EP1869052A1 (en) * | 2005-04-06 | 2007-12-26 | AstraZeneca AB | Substituted heterocycles and their use as chk1, pdk1 and pak inhibitors |
| EP1885187B1 (en) * | 2005-05-13 | 2013-09-25 | Novartis AG | Methods for treating drug resistant cancer |
| EP2465857B1 (en) * | 2005-05-17 | 2014-06-04 | Novartis AG | Methods for synthesizing heterocyclic compounds |
| BRPI0611375A2 (pt) * | 2005-05-23 | 2010-08-31 | Novartis Ag | formas cristalinas e outras de sais de ácido láctico de 4-amino-5-flúor-3-[6-(4-metilpiperazin-1-il)-1h-benzimid azol-2-il]-1h-quinolin-2-ona |
| EP1898903B8 (en) * | 2005-06-10 | 2013-05-15 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| US8071768B2 (en) | 2005-06-10 | 2011-12-06 | Janssen Pharmaceutica, N.V. | Alkylquinoline and alkylquinazoline kinase modulators |
| US7825244B2 (en) | 2005-06-10 | 2010-11-02 | Janssen Pharmaceutica Nv | Intermediates useful in the synthesis of alkylquinoline and alkylquinazoline kinase modulators, and related methods of synthesis |
| US20060281788A1 (en) | 2005-06-10 | 2006-12-14 | Baumann Christian A | Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor |
| JP5301987B2 (ja) * | 2005-06-20 | 2013-09-25 | デコード・ジェネティクス・イーエイチエフ | ２型糖尿病のリスクの診断マーカーとしてのｔｃｆ７ｌ２遺伝子中の遺伝子変異体 |
| US7897589B2 (en) * | 2005-07-15 | 2011-03-01 | Laboratorios Del Dr. Esteve, S.A. | Substituted pyrazoline compounds, their preparation and use as medicaments |
| EP1743890A1 (en) * | 2005-07-15 | 2007-01-17 | Laboratorios Del Dr. Esteve, S.A. | 4,5-Dihydro-1H-pyrazole derivatives, their preparation and use as medicaments |
| EP1743892A1 (en) * | 2005-07-15 | 2007-01-17 | Laboratorios del Dr. Esteve S.A. | Substituted pyrazoline compounds, their preparation and use as medicaments |
| EP1757587A1 (en) * | 2005-07-15 | 2007-02-28 | Laboratorios Del Dr. Esteve, S.A. | Substituted pyrazoline compounds, their preparation and use as medicaments |
| EP1749523A1 (en) | 2005-07-29 | 2007-02-07 | Neuropharma, S.A. | GSK-3 inhibitors |
| AU2006304897B2 (en) | 2005-10-18 | 2012-07-12 | Janssen Pharmaceutica N.V. | Method of inhibiting FLT3 kinase |
| WO2007056317A2 (en) * | 2005-11-07 | 2007-05-18 | Novartis Vaccines & Diagnostics, Inc. | Methods for assaying an active pharmaceutical ingredient |
| NZ567550A (en) | 2005-11-29 | 2011-08-26 | Novartis Ag | Formulations of lactic acid salts of 4-amino-5-fluoro-3-[6-(4-methyl-piperazin-1-yl)-1 H-benzimidazol-2-yl]1H-quinolin-2-one |
| KR20080080525A (ko) | 2005-12-08 | 2008-09-04 | 노파르티스 아게 | 유전자 전사에 대한 ｆｇｆｒ３의 억제제의 효과 |
| PL2021335T3 (pl) | 2006-04-20 | 2011-10-31 | Janssen Pharmaceutica Nv | Związki heterocykliczne jako inhibitory kinazy C-FMS |
| WO2007124319A1 (en) | 2006-04-20 | 2007-11-01 | Janssen Pharmaceutica N.V. | Inhibitors of c-fms kinase |
| US8697716B2 (en) | 2006-04-20 | 2014-04-15 | Janssen Pharmaceutica Nv | Method of inhibiting C-KIT kinase |
| FR2902100A1 (fr) * | 2006-06-13 | 2007-12-14 | Sanofi Aventis Sa | Molecules duales contenant un derive peroxydique, leur synthese et leurs applications en therapeutique |
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| RU2009112496A (ru) * | 2006-10-19 | 2010-11-27 | Ф. Хоффманн-Ля Рош Аг (Ch) | Аминометил-4-имидазолы |
| EP2170859A1 (en) | 2007-06-25 | 2010-04-07 | F. Hoffmann-Roche AG | Benzimidazole amido derivatives as kinase inhibitors |
| ES2799897T3 (es) | 2007-08-31 | 2020-12-22 | Whitehead Inst Biomedical Res | Estimulación de la vía wnt en la reprogramación de células somáticas |
| JO3240B1 (ar) | 2007-10-17 | 2018-03-08 | Janssen Pharmaceutica Nv | c-fms مثبطات كيناز |
| GB0800855D0 (en) | 2008-01-17 | 2008-02-27 | Syngenta Ltd | Herbicidal compounds |
| US9000027B2 (en) * | 2008-02-04 | 2015-04-07 | Dana-Farber Cancer Institute, Inc. | Chk1 suppresses a caspase-2 apoptotic response to DNA damage that bypasses p53, bcl-2 and caspase-3 |
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| DE102008022221A1 (de) | 2008-05-06 | 2009-11-12 | Universität des Saarlandes | Inhibitoren der humanen Aldosteronsynthase CYP11B2 |
| EP2151234A1 (en) * | 2008-07-28 | 2010-02-10 | Laboratorios Del. Dr. Esteve, S.A. | Pharmaceutical formulation comprising a CB1-receptor compound in a solid solution and/or solid dispersion |
| JP5564045B2 (ja) * | 2008-09-02 | 2014-07-30 | ノバルティス アーゲー | 二環式キナーゼ阻害剤 |
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| US8492374B2 (en) | 2009-04-29 | 2013-07-23 | Industrial Technology Research Institute | Azaazulene compounds |
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| KR101127161B1 (ko) * | 2009-07-13 | 2012-03-20 | 한국화학연구원 | 테트라히드로이미다조피리딘기가 치환된 퀴놀리논 화합물 |
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| HUE045270T2 (hu) | 2010-01-05 | 2019-12-30 | Inst Nat Sante Rech Med | FLT3 receptor anatgonisták fájdalom rendellenességek kezelésére |
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| BR112012026289A2 (pt) | 2010-04-16 | 2016-07-12 | Novartis Ag | composto orgânico para uso no tratamento de câncer do fígado |
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| JP2014526506A (ja) | 2011-09-15 | 2014-10-06 | ノバルティス アーゲー | 中等度肝障害患者の癌治療における４−アミノ−５−フルオロ−３−［６−（４−メチルピペラジン−１−イル）−１ｈ−ベンゾイミダゾール−２−イル］−１ｈ−キノリン−２−オンの使用 |
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- 2003-08-19 AU AU2003288899A patent/AU2003288899B2/en not_active Ceased
- 2003-08-19 US US10/644,055 patent/US7470709B2/en not_active Expired - Fee Related
- 2003-08-19 EP EP12186782.4A patent/EP2573079A3/en not_active Withdrawn
- 2003-08-19 CA CA2496164A patent/CA2496164C/en not_active Expired - Fee Related
- 2003-08-19 WO PCT/US2003/025990 patent/WO2004018419A2/en not_active Ceased
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2004
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2005
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2008
- 2008-12-23 US US12/317,493 patent/US20090281100A1/en not_active Abandoned
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