JP2010534682A5 - - Google Patents
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- JP2010534682A5 JP2010534682A5 JP2010518424A JP2010518424A JP2010534682A5 JP 2010534682 A5 JP2010534682 A5 JP 2010534682A5 JP 2010518424 A JP2010518424 A JP 2010518424A JP 2010518424 A JP2010518424 A JP 2010518424A JP 2010534682 A5 JP2010534682 A5 JP 2010534682A5
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- JP
- Japan
- Prior art keywords
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- formula
- composition
- cancer
- alkyl
- 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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- 239000000203 mixture Substances 0.000 claims description 68
- 206010028980 Neoplasm Diseases 0.000 claims description 64
- 238000000034 method Methods 0.000 claims description 62
- -1 trifluoromethylcarbonyl Chemical group 0.000 claims description 60
- 201000011510 cancer Diseases 0.000 claims description 58
- 150000001875 compounds Chemical class 0.000 claims description 42
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 30
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 28
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 28
- 229940124647 MEK inhibitor Drugs 0.000 claims description 28
- 125000002883 imidazolyl group Chemical group 0.000 claims description 28
- 150000002148 esters Chemical class 0.000 claims description 24
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims description 24
- 230000035772 mutation Effects 0.000 claims description 24
- 150000003839 salts Chemical class 0.000 claims description 24
- 101150056950 Ntrk2 gene Proteins 0.000 claims description 21
- 102000004232 Mitogen-Activated Protein Kinase Kinases Human genes 0.000 claims description 18
- 230000000694 effects Effects 0.000 claims description 16
- 125000003545 alkoxy group Chemical group 0.000 claims description 14
- 125000000623 heterocyclic group Chemical group 0.000 claims description 14
- 229910052757 nitrogen Inorganic materials 0.000 claims description 14
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 14
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 14
- 125000004193 piperazinyl group Chemical group 0.000 claims description 14
- 125000003386 piperidinyl group Chemical group 0.000 claims description 14
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 14
- 102000018471 Proto-Oncogene Proteins B-raf Human genes 0.000 claims description 12
- 108010091528 Proto-Oncogene Proteins B-raf Proteins 0.000 claims description 12
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims description 10
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims description 10
- 102000009076 src-Family Kinases Human genes 0.000 claims description 8
- 108010087686 src-Family Kinases Proteins 0.000 claims description 8
- 206010009944 Colon cancer Diseases 0.000 claims description 6
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 6
- 206010029260 Neuroblastoma Diseases 0.000 claims description 6
- 230000008499 blood brain barrier function Effects 0.000 claims description 6
- 210000001218 blood-brain barrier Anatomy 0.000 claims description 6
- 201000007455 central nervous system cancer Diseases 0.000 claims description 6
- 208000025997 central nervous system neoplasm Diseases 0.000 claims description 6
- 208000032612 Glial tumor Diseases 0.000 claims description 5
- 206010018338 Glioma Diseases 0.000 claims description 5
- 230000001394 metastastic effect Effects 0.000 claims description 5
- 206010061289 metastatic neoplasm Diseases 0.000 claims description 5
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 4
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 4
- 102100031480 Dual specificity mitogen-activated protein kinase kinase 1 Human genes 0.000 claims description 4
- 101710146526 Dual specificity mitogen-activated protein kinase kinase 1 Proteins 0.000 claims description 4
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 4
- 206010033128 Ovarian cancer Diseases 0.000 claims description 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 4
- 201000000582 Retinoblastoma Diseases 0.000 claims description 4
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 4
- 210000004556 brain Anatomy 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- 230000001537 neural effect Effects 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 4
- 201000002510 thyroid cancer Diseases 0.000 claims description 4
- 125000000217 alkyl group Chemical group 0.000 claims description 3
- 239000002246 antineoplastic agent Substances 0.000 claims description 3
- 229940044683 chemotherapy drug Drugs 0.000 claims description 3
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 230000037396 body weight Effects 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 229960003685 imatinib mesylate Drugs 0.000 claims description 2
- YLMAHDNUQAMNNX-UHFFFAOYSA-N imatinib methanesulfonate Chemical compound CS(O)(=O)=O.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 YLMAHDNUQAMNNX-UHFFFAOYSA-N 0.000 claims description 2
- 230000005764 inhibitory process Effects 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 102220198325 rs1057520025 Human genes 0.000 claims description 2
- 102220198339 rs1057520026 Human genes 0.000 claims description 2
- 102200039431 rs121913488 Human genes 0.000 claims description 2
- 102220197934 rs376588714 Human genes 0.000 claims description 2
- 125000006559 (C1-C3) alkylamino group Chemical group 0.000 claims 1
- 206010027476 Metastases Diseases 0.000 claims 1
- 201000007983 brain glioma Diseases 0.000 claims 1
- 230000009401 metastasis Effects 0.000 claims 1
- 0 C*[C@]([C@](C)O1)OC1=O Chemical compound C*[C@]([C@](C)O1)OC1=O 0.000 description 5
- VWIIJDNADIEEDB-UHFFFAOYSA-N CN(CCO1)C1=O Chemical compound CN(CCO1)C1=O VWIIJDNADIEEDB-UHFFFAOYSA-N 0.000 description 2
- WEVYNIUIFUYDGI-UHFFFAOYSA-N 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide Chemical compound NC(=O)C1=CC=CC(C=2N=CN=C(NC=3C=CC(OC(F)(F)F)=CC=3)C=2)=C1 WEVYNIUIFUYDGI-UHFFFAOYSA-N 0.000 description 1
- JTPZTKBRUCILQD-UHFFFAOYSA-N CN(CCN1)C1=O Chemical compound CN(CCN1)C1=O JTPZTKBRUCILQD-UHFFFAOYSA-N 0.000 description 1
- 125000003282 alkyl amino group Chemical group 0.000 description 1
- 125000000031 ethylamino group Chemical group [H]C([H])([H])C([H])([H])N([H])[*] 0.000 description 1
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US95190607P | 2007-07-25 | 2007-07-25 | |
| US95190107P | 2007-07-25 | 2007-07-25 | |
| US60/951,906 | 2007-07-25 | ||
| US60/951,901 | 2007-07-25 | ||
| US2919608P | 2008-02-15 | 2008-02-15 | |
| US61/029,196 | 2008-02-15 | ||
| PCT/US2008/071256 WO2009015368A2 (en) | 2007-07-25 | 2008-07-25 | Multikinase inhibitors for use in the treatment of cancer |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013114011A Division JP2013189458A (ja) | 2007-07-25 | 2013-05-30 | 癌の処置において使用するための多キナーゼインヒビター |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010534682A JP2010534682A (ja) | 2010-11-11 |
| JP2010534682A5 true JP2010534682A5 (enExample) | 2011-08-25 |
| JP5484327B2 JP5484327B2 (ja) | 2014-05-07 |
Family
ID=40121184
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010518424A Active JP5484327B2 (ja) | 2007-07-25 | 2008-07-25 | 癌の処置において使用するための多キナーゼインヒビター |
| JP2013114011A Pending JP2013189458A (ja) | 2007-07-25 | 2013-05-30 | 癌の処置において使用するための多キナーゼインヒビター |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013114011A Pending JP2013189458A (ja) | 2007-07-25 | 2013-05-30 | 癌の処置において使用するための多キナーゼインヒビター |
Country Status (10)
| Country | Link |
|---|---|
| US (4) | US8609640B2 (enExample) |
| EP (1) | EP2182941B1 (enExample) |
| JP (2) | JP5484327B2 (enExample) |
| KR (3) | KR101667960B1 (enExample) |
| CN (2) | CN105748465A (enExample) |
| AU (1) | AU2008279027B8 (enExample) |
| CA (1) | CA2698271C (enExample) |
| ES (1) | ES2670423T3 (enExample) |
| IL (2) | IL202307A (enExample) |
| WO (1) | WO2009015368A2 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4575667B2 (ja) * | 2002-03-08 | 2010-11-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 医薬として有用な大環状化合物 |
| ES2670423T3 (es) | 2007-07-25 | 2018-05-30 | Eisai R&D Management Co., Ltd. | Inhibidores de multicinasas para uso en el tratamiento de cáncer |
| CA2704048A1 (en) * | 2007-10-29 | 2009-05-07 | Eisai R & D Management Co., Ltd. | Methods for prognosing the ability of a zearalenone analog compound to treat cancer |
| CA2708143C (en) | 2007-12-07 | 2016-10-11 | Francis G. Fang | Intermediates in the synthesis of zearalenone macrolide analogs |
| US8426418B2 (en) | 2010-08-27 | 2013-04-23 | CollabRx Inc. | Method to treat melanoma in BRAF inhibitor-resistant subjects |
| AU2014299699B2 (en) * | 2013-06-26 | 2019-10-10 | Eisai R&D Management Co., Ltd. | Use of eribulin and lenvatinib as combination therapy for treatment of cancer |
| DK3039424T3 (da) * | 2013-08-28 | 2020-08-31 | Crown Bioscience Inc Taicang | Genekspressionssignaturer, der er prædiktive for et individs respons på en multikinaseinhibitor, og fremgangsmåder til anvendelse af disse |
| WO2015181628A1 (en) * | 2014-05-27 | 2015-12-03 | Eisai R&D Management Co., Ltd. | Treatment of acute myeloid leukemia with an hck inhibitor |
| WO2022053130A1 (en) * | 2020-09-09 | 2022-03-17 | Sid Alex Group, S.R.O. | Antago-mir-155 for treatment of v-src, c-src-tyrosine kinase-induced cancers |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9225396D0 (en) | 1992-12-04 | 1993-01-27 | Sandoz Ltd | Improvements in or relating to organic compounds |
| JPH0840893A (ja) | 1993-08-31 | 1996-02-13 | Takeda Chem Ind Ltd | インターロイキン−１産生抑制剤 |
| DE4420930C2 (de) | 1994-06-16 | 1997-05-22 | Daimler Benz Ag | Vorrichtung und Verfahren zum Steuern einer selbsttätigen Schaltvorrichtung eines Gangwechselgetriebes eines Kraftfahrzeuges |
| US5795910A (en) | 1994-10-28 | 1998-08-18 | Cor Therapeutics, Inc. | Method and compositions for inhibiting protein kinases |
| US5727726A (en) * | 1996-06-14 | 1998-03-17 | Newco Pneumatic Corp. | Cassette assembly for a stapling mechanism |
| AU6678398A (en) | 1997-02-27 | 1998-09-18 | Ana Maria Garcia | Inhibitors of isoprenyl transferase |
| GB2323845A (en) | 1997-03-31 | 1998-10-07 | Merck & Co Inc | MEK inhibiting lactones |
| GB9828709D0 (en) | 1998-12-24 | 1999-02-17 | Novartis Ag | Assay |
| US6635671B1 (en) | 1998-12-24 | 2003-10-21 | Novation Pharmaceuticals Inc. | Compounds which affect mRNA stability and uses therefor |
| JP2002540142A (ja) * | 1999-03-29 | 2002-11-26 | シャイアー・バイオケム・インコーポレイテッド | 白血病の処置方法 |
| WO2001036003A2 (en) | 1999-11-15 | 2001-05-25 | Drug Innovation & Design, Inc. | Selective cellular targeting: multifunctional delivery vehicles |
| MXPA02006778A (es) | 2000-01-12 | 2004-04-05 | Ventana Inc | Metodo para determinar la respuesta a una terapia de cancer. |
| JP2001294527A (ja) | 2000-04-14 | 2001-10-23 | Ajinomoto Co Inc | Ｔｈ２反応に特異的な免疫寛容誘導剤 |
| AU5352901A (en) | 2000-04-14 | 2001-10-30 | Ventana Med Syst Inc | Method for quantification of akt protein expression |
| JP2004292315A (ja) | 2000-12-14 | 2004-10-21 | Chugai Pharmaceut Co Ltd | Ｔａｋ１阻害剤 |
| JP2004292314A (ja) | 2000-12-14 | 2004-10-21 | Chugai Pharmaceut Co Ltd | ケラチノサイト増殖抑制剤 |
| US7071164B2 (en) | 2001-08-16 | 2006-07-04 | Kimberly-Clark Worldwide, Inc. | Anti-cancer and wound healing compounds |
| US7419777B2 (en) | 2001-08-21 | 2008-09-02 | Ventana Medical Systems, Inc. | Method and quantification assay for determining c-kit/SCF/pAKT status |
| NZ532780A (en) | 2001-12-21 | 2006-10-27 | Wellcome Trust | Isolated naturally occurring mutant human B-Raf polypeptides and nucleic acids encoding them |
| US20040096855A1 (en) | 2001-12-24 | 2004-05-20 | Michael Stratton | Genes |
| JP4575667B2 (ja) * | 2002-03-08 | 2010-11-04 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 医薬として有用な大環状化合物 |
| US7915306B2 (en) | 2002-03-08 | 2011-03-29 | Eisai Co., Ltd. | Macrocyclic compounds useful as pharmaceuticals |
| EA010485B1 (ru) | 2003-07-23 | 2008-10-30 | Байер Фамэсьютиклс Копэрейшн | Производное n,n'-дифенилмочевины, фармацевтическая композиция (варианты) и способ лечения и предупреждения заболеваний и состояний с его использованием (варианты) |
| AU2003286447A1 (en) | 2003-10-16 | 2004-06-06 | The Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services | Treatments for inhibiting development and progression of nevi and melanoma having braf mutations |
| US20050214325A1 (en) | 2004-03-26 | 2005-09-29 | Vvii Newco 2003, Inc. | Compositions and methods to increase the effect of a neurotoxin treatment |
| AU2005223649A1 (en) | 2004-03-19 | 2005-09-29 | The Penn State Research Foundation | Combinatorial methods and compositions for treatment of melanoma |
| WO2005094830A1 (en) | 2004-03-30 | 2005-10-13 | Pfizer Products Inc. | Combinations of signal transduction inhibitors |
| CA2569277A1 (en) | 2004-06-04 | 2005-12-15 | Pfizer Products Inc. | Method for treating abnormal cell growth |
| EP1794137A4 (en) * | 2004-09-27 | 2009-12-02 | Kosan Biosciences Inc | SPECIFIC KINASE INHIBITORS |
| US20060216288A1 (en) | 2005-03-22 | 2006-09-28 | Amgen Inc | Combinations for the treatment of cancer |
| US7812143B2 (en) | 2006-03-31 | 2010-10-12 | Memorial Sloan-Kettering Cancer Center | Biomarkers for cancer treatment |
| ES2670423T3 (es) | 2007-07-25 | 2018-05-30 | Eisai R&D Management Co., Ltd. | Inhibidores de multicinasas para uso en el tratamiento de cáncer |
| CA2704048A1 (en) | 2007-10-29 | 2009-05-07 | Eisai R & D Management Co., Ltd. | Methods for prognosing the ability of a zearalenone analog compound to treat cancer |
| CA2708143C (en) | 2007-12-07 | 2016-10-11 | Francis G. Fang | Intermediates in the synthesis of zearalenone macrolide analogs |
| US8578879B2 (en) * | 2009-07-29 | 2013-11-12 | Applied Materials, Inc. | Apparatus for VHF impedance match tuning |
-
2008
- 2008-07-25 ES ES08796672.7T patent/ES2670423T3/es active Active
- 2008-07-25 KR KR1020157033387A patent/KR101667960B1/ko active Active
- 2008-07-25 WO PCT/US2008/071256 patent/WO2009015368A2/en not_active Ceased
- 2008-07-25 CN CN201610165747.1A patent/CN105748465A/zh active Pending
- 2008-07-25 KR KR1020167028439A patent/KR101721161B1/ko active Active
- 2008-07-25 CN CN200880023760.7A patent/CN101778627B/zh active Active
- 2008-07-25 EP EP08796672.7A patent/EP2182941B1/en active Active
- 2008-07-25 KR KR1020107004170A patent/KR101573026B1/ko active Active
- 2008-07-25 CA CA2698271A patent/CA2698271C/en active Active
- 2008-07-25 AU AU2008279027A patent/AU2008279027B8/en active Active
- 2008-07-25 US US12/180,408 patent/US8609640B2/en active Active
- 2008-07-25 JP JP2010518424A patent/JP5484327B2/ja active Active
-
2009
- 2009-11-24 IL IL202307A patent/IL202307A/en active IP Right Grant
-
2013
- 2013-03-11 US US13/794,635 patent/US8937056B2/en active Active
- 2013-05-30 JP JP2013114011A patent/JP2013189458A/ja active Pending
-
2015
- 2015-01-13 US US14/595,746 patent/US20150182496A1/en not_active Abandoned
-
2016
- 2016-08-11 IL IL247230A patent/IL247230A/en active IP Right Grant
-
2018
- 2018-04-23 US US15/960,259 patent/US11160783B2/en active Active
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