JP2013545757A5 - - Google Patents
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- JP2013545757A5 JP2013545757A5 JP2013539999A JP2013539999A JP2013545757A5 JP 2013545757 A5 JP2013545757 A5 JP 2013545757A5 JP 2013539999 A JP2013539999 A JP 2013539999A JP 2013539999 A JP2013539999 A JP 2013539999A JP 2013545757 A5 JP2013545757 A5 JP 2013545757A5
- Authority
- JP
- Japan
- Prior art keywords
- amino acid
- pharmaceutical composition
- acid change
- mutation
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- 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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- 150000001413 amino acids Chemical class 0.000 claims 48
- 239000008194 pharmaceutical composition Substances 0.000 claims 48
- 230000035772 mutation Effects 0.000 claims 31
- 102000016914 ras Proteins Human genes 0.000 claims 26
- 108010014186 ras Proteins Proteins 0.000 claims 26
- 102100026715 Serine/threonine-protein kinase STK11 Human genes 0.000 claims 16
- 206010028980 Neoplasm Diseases 0.000 claims 15
- 101710181599 Serine/threonine-protein kinase STK11 Proteins 0.000 claims 15
- JTSLALYXYSRPGW-UHFFFAOYSA-N n-[5-(4-cyanophenyl)-1h-pyrrolo[2,3-b]pyridin-3-yl]pyridine-3-carboxamide Chemical compound C=1C=CN=CC=1C(=O)NC(C1=C2)=CNC1=NC=C2C1=CC=C(C#N)C=C1 JTSLALYXYSRPGW-UHFFFAOYSA-N 0.000 claims 14
- 229940124647 MEK inhibitor Drugs 0.000 claims 12
- 230000037430 deletion Effects 0.000 claims 12
- 238000012217 deletion Methods 0.000 claims 12
- 230000037431 insertion Effects 0.000 claims 12
- 238000003780 insertion Methods 0.000 claims 12
- 229940124302 mTOR inhibitor Drugs 0.000 claims 12
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 12
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 12
- 108090000623 proteins and genes Proteins 0.000 claims 12
- 201000011510 cancer Diseases 0.000 claims 11
- 241000124008 Mammalia Species 0.000 claims 10
- 239000012453 solvate Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 7
- 150000001875 compounds Chemical class 0.000 claims 6
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 6
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 6
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 4
- 229960005167 everolimus Drugs 0.000 claims 4
- 108020004705 Codon Proteins 0.000 claims 3
- 229940126638 Akt inhibitor Drugs 0.000 claims 2
- 239000012823 PI3K/mTOR inhibitor Substances 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 102220530637 Putative apolipoprotein(a)-like protein 2_G12F_mutation Human genes 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 2
- 210000004369 blood Anatomy 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 239000003197 protein kinase B inhibitor Substances 0.000 claims 2
- 102200006657 rs104894228 Human genes 0.000 claims 2
- 102200006562 rs104894231 Human genes 0.000 claims 2
- 102200006534 rs104894365 Human genes 0.000 claims 2
- 102200006532 rs112445441 Human genes 0.000 claims 2
- 102220197780 rs121434596 Human genes 0.000 claims 2
- 102200006525 rs121913240 Human genes 0.000 claims 2
- 102200140160 rs121913322 Human genes 0.000 claims 2
- 102200006531 rs121913529 Human genes 0.000 claims 2
- 102200006537 rs121913529 Human genes 0.000 claims 2
- 102200006539 rs121913529 Human genes 0.000 claims 2
- 102200006538 rs121913530 Human genes 0.000 claims 2
- 102200006540 rs121913530 Human genes 0.000 claims 2
- 102200006541 rs121913530 Human genes 0.000 claims 2
- 102200155721 rs121918464 Human genes 0.000 claims 2
- 102220056962 rs121918464 Human genes 0.000 claims 2
- 102200155722 rs121918465 Human genes 0.000 claims 2
- 102200007373 rs17851045 Human genes 0.000 claims 2
- 102200097053 rs199473666 Human genes 0.000 claims 2
- 102200124922 rs267606920 Human genes 0.000 claims 2
- 102200006648 rs28933406 Human genes 0.000 claims 2
- 102200140141 rs59912467 Human genes 0.000 claims 2
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- BUROJSBIWGDYCN-GAUTUEMISA-N AP 23573 Chemical compound C1C[C@@H](OP(C)(C)=O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 BUROJSBIWGDYCN-GAUTUEMISA-N 0.000 claims 1
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims 1
- 101710113436 GTPase KRas Proteins 0.000 claims 1
- 102100039788 GTPase NRas Human genes 0.000 claims 1
- 101000744505 Homo sapiens GTPase NRas Proteins 0.000 claims 1
- 101000628562 Homo sapiens Serine/threonine-protein kinase STK11 Proteins 0.000 claims 1
- 101000702545 Homo sapiens Transcription activator BRG1 Proteins 0.000 claims 1
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 1
- 108020004485 Nonsense Codon Proteins 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 102220580881 Serine/threonine-protein kinase STK11_D176Y_mutation Human genes 0.000 claims 1
- 102220580789 Serine/threonine-protein kinase STK11_D277Y_mutation Human genes 0.000 claims 1
- 102220584452 Serine/threonine-protein kinase STK11_E199Q_mutation Human genes 0.000 claims 1
- 102220584443 Serine/threonine-protein kinase STK11_H174R_mutation Human genes 0.000 claims 1
- 102220580788 Serine/threonine-protein kinase STK11_L285Q_mutation Human genes 0.000 claims 1
- CBPNZQVSJQDFBE-FUXHJELOSA-N Temsirolimus Chemical compound C1C[C@@H](OC(=O)C(C)(CO)CO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 CBPNZQVSJQDFBE-FUXHJELOSA-N 0.000 claims 1
- 102100031027 Transcription activator BRG1 Human genes 0.000 claims 1
- 102220350107 c.166G>T Human genes 0.000 claims 1
- 102220360834 c.724G>A Human genes 0.000 claims 1
- 230000003197 catalytic effect Effects 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229960002448 dasatinib Drugs 0.000 claims 1
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N dimethyl sulfoxide Natural products CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000037434 nonsense mutation Effects 0.000 claims 1
- CGBJSGAELGCMKE-UHFFFAOYSA-N omipalisib Chemical group COC1=NC=C(C=2C=C3C(C=4C=NN=CC=4)=CC=NC3=CC=2)C=C1NS(=O)(=O)C1=CC=C(F)C=C1F CGBJSGAELGCMKE-UHFFFAOYSA-N 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- -1 rapalog Chemical compound 0.000 claims 1
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 1
- 229960001302 ridaforolimus Drugs 0.000 claims 1
- 102200140795 rs1057520039 Human genes 0.000 claims 1
- 102200055464 rs113488022 Human genes 0.000 claims 1
- 102200014493 rs121909124 Human genes 0.000 claims 1
- 102220197819 rs121913227 Human genes 0.000 claims 1
- 102220197820 rs121913227 Human genes 0.000 claims 1
- 102200140257 rs121913315 Human genes 0.000 claims 1
- 102200140772 rs121913315 Human genes 0.000 claims 1
- 102200140256 rs121913316 Human genes 0.000 claims 1
- 102220197823 rs121913338 Human genes 0.000 claims 1
- 102200055449 rs121913341 Human genes 0.000 claims 1
- 102200055517 rs121913348 Human genes 0.000 claims 1
- 102200055523 rs121913348 Human genes 0.000 claims 1
- 102200055529 rs121913351 Human genes 0.000 claims 1
- 102200055532 rs121913355 Human genes 0.000 claims 1
- 102200055451 rs121913361 Human genes 0.000 claims 1
- 102200055461 rs121913366 Human genes 0.000 claims 1
- 102200055463 rs121913369 Human genes 0.000 claims 1
- 102220010949 rs121913375 Human genes 0.000 claims 1
- 102200055469 rs121913377 Human genes 0.000 claims 1
- 102200006533 rs121913535 Human genes 0.000 claims 1
- 102200055501 rs180177032 Human genes 0.000 claims 1
- 102200055521 rs180177033 Human genes 0.000 claims 1
- 102220041736 rs368466538 Human genes 0.000 claims 1
- 102200001486 rs397514547 Human genes 0.000 claims 1
- 102220044529 rs587781374 Human genes 0.000 claims 1
- 102220062377 rs587782687 Human genes 0.000 claims 1
- 102220198320 rs730881972 Human genes 0.000 claims 1
- 102200031604 rs750730042 Human genes 0.000 claims 1
- 102200140793 rs764449808 Human genes 0.000 claims 1
- 102220087511 rs864622488 Human genes 0.000 claims 1
- 102220090324 rs876657851 Human genes 0.000 claims 1
- 102220098666 rs878853247 Human genes 0.000 claims 1
- 229960002930 sirolimus Drugs 0.000 claims 1
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 1
- 159000000000 sodium salts Chemical class 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 229960000235 temsirolimus Drugs 0.000 claims 1
- QFJCIRLUMZQUOT-UHFFFAOYSA-N temsirolimus Natural products C1CC(O)C(OC)CC1CC(C)C1OC(=O)C2CCCCN2C(=O)C(=O)C(O)(O2)C(C)CCC2CC(OC)C(C)=CC=CC=CC(C)CC(C)C(=O)C(OC)C(O)C(C)=CC(C)C(=O)C1 QFJCIRLUMZQUOT-UHFFFAOYSA-N 0.000 claims 1
- 210000004881 tumor cell Anatomy 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41452110P | 2010-11-17 | 2010-11-17 | |
| US61/414,521 | 2010-11-17 | ||
| PCT/US2011/061135 WO2012068339A2 (en) | 2010-11-17 | 2011-11-17 | Methods of treating cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013545757A JP2013545757A (ja) | 2013-12-26 |
| JP2013545757A5 true JP2013545757A5 (enExample) | 2015-01-08 |
Family
ID=46084636
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013539999A Pending JP2013545757A (ja) | 2010-11-17 | 2011-11-17 | 癌の治療方法 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20130231346A1 (enExample) |
| EP (1) | EP2640390A4 (enExample) |
| JP (1) | JP2013545757A (enExample) |
| WO (1) | WO2012068339A2 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2900301T3 (es) | 2013-03-15 | 2022-03-16 | Novartis Ag | Biomarcadores asociados con la inhibición de BRM |
| WO2015005473A1 (ja) * | 2013-07-12 | 2015-01-15 | 独立行政法人国立がん研究センター | がんの治療への応答性を予測する方法 |
| EP3074019A1 (en) * | 2013-11-27 | 2016-10-05 | Oncoethix GmbH | Method of treating non-small-cell lung cancer using pharmaceutical formulation containing thienotriazolodiazepine compounds |
| WO2015164743A2 (en) | 2014-04-24 | 2015-10-29 | Dana-Farber Cancer Institute, Inc. | Tumor suppressor and oncogene biomarkers predictive of anti-immune checkpoint inhibitor response |
| WO2016176338A1 (en) * | 2015-04-30 | 2016-11-03 | The Trustees Of Columbia University In The City Of New York | Small molecule ras ligands |
| CA2996513A1 (en) * | 2015-08-25 | 2018-03-02 | President And Fellows Of Harvard College | Methods and compositions relating to the diagnosis and treatment of cancer |
| US12246067B2 (en) | 2018-06-19 | 2025-03-11 | Biontech Us Inc. | Neoantigens and uses thereof |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| CN116355851B (zh) * | 2023-03-13 | 2023-09-08 | 广州医科大学附属第一医院（广州呼吸中心） | 一种来源于人非小细胞肺癌的原代细胞株及其制备方法与应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005121142A1 (en) * | 2004-06-11 | 2005-12-22 | Japan Tobacco Inc. | 5-amino-2,4,7-trioxo-3,4,7,8-tetrahydro-2h-pyrido’2,3-d! pyrimidine derivatives and related compounds for the treatment of cancer |
| US7378423B2 (en) * | 2004-06-11 | 2008-05-27 | Japan Tobacco Inc. | Pyrimidine compound and medical use thereof |
| KR20080108517A (ko) * | 2006-04-05 | 2008-12-15 | 노파르티스 아게 | 암을 치료하기 위한 치료제의 조합물 |
| US20090274698A1 (en) * | 2007-07-06 | 2009-11-05 | Shripad Bhagwat | Combination anti-cancer therapy |
| WO2009062199A1 (en) * | 2007-11-09 | 2009-05-14 | Fox Chase Cancer Center | EGFR/NEDD9/TGF-β LNTERACTOME AND METHODS OF USE THEREOF FOR THE IDENTIFICATION OF AGENTS HAVING EFFICACY IN THE TREATMENT OF HYPERPROLIFERATIVE DISORDERS |
| MX2010012064A (es) * | 2008-05-05 | 2010-12-06 | Schering Corp | Uso secuencial de agentes quimioterapeuticos citotoxicos para el tratamiento de cancer. |
| MX2011000440A (es) * | 2008-07-11 | 2011-02-24 | Novartis Ag | Combinacion de (a) un inhibidor de fosfoinositido 3-cinasa y (b) un modulador de la ruta de ras/raf/mek. |
| EA022637B1 (ru) * | 2009-11-17 | 2016-02-29 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | Комбинация |
| WO2012061683A2 (en) * | 2010-11-05 | 2012-05-10 | Glaxosmithkline Llc | Methods for treating cancer |
-
2011
- 2011-11-17 US US13/988,054 patent/US20130231346A1/en not_active Abandoned
- 2011-11-17 EP EP11841436.6A patent/EP2640390A4/en not_active Withdrawn
- 2011-11-17 JP JP2013539999A patent/JP2013545757A/ja active Pending
- 2011-11-17 WO PCT/US2011/061135 patent/WO2012068339A2/en not_active Ceased
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