JP2019536767A5 - - Google Patents
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- Publication number
- JP2019536767A5 JP2019536767A5 JP2019523821A JP2019523821A JP2019536767A5 JP 2019536767 A5 JP2019536767 A5 JP 2019536767A5 JP 2019523821 A JP2019523821 A JP 2019523821A JP 2019523821 A JP2019523821 A JP 2019523821A JP 2019536767 A5 JP2019536767 A5 JP 2019536767A5
- Authority
- JP
- Japan
- Prior art keywords
- inhibitors
- inhibitor
- epicatechin
- compounds
- kinase
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 14
- 239000003112 inhibitor Substances 0.000 claims 14
- PFTAWBLQPZVEMU-ZFWWWQNUSA-N (+)-epicatechin Natural products C1([C@@H]2OC3=CC(O)=CC(O)=C3C[C@@H]2O)=CC=C(O)C(O)=C1 PFTAWBLQPZVEMU-ZFWWWQNUSA-N 0.000 claims 9
- PFTAWBLQPZVEMU-UKRRQHHQSA-N (-)-epicatechin Chemical compound C1([C@H]2OC3=CC(O)=CC(O)=C3C[C@H]2O)=CC=C(O)C(O)=C1 PFTAWBLQPZVEMU-UKRRQHHQSA-N 0.000 claims 6
- 230000001093 anti-cancer Effects 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- -1 nitoseurea Chemical compound 0.000 claims 4
- BASFCYQUMIYNBI-UHFFFAOYSA-N platinum Chemical compound [Pt] BASFCYQUMIYNBI-UHFFFAOYSA-N 0.000 claims 4
- PFTAWBLQPZVEMU-DZGCQCFKSA-N (+)-3',4',5,7-Tetrahydroxy-2,3-trans-flavan-3-ol Natural products C1([C@H]2OC3=CC(O)=CC(O)=C3C[C@@H]2O)=CC=C(O)C(O)=C1 PFTAWBLQPZVEMU-DZGCQCFKSA-N 0.000 claims 3
- 235000007246 (+)-epicatechin Nutrition 0.000 claims 3
- 235000007355 (-)-epicatechin Nutrition 0.000 claims 3
- 229930013783 (-)-epicatechin Natural products 0.000 claims 3
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 claims 3
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 claims 3
- 235000012734 epicatechin Nutrition 0.000 claims 3
- LPTRNLNOHUVQMS-UHFFFAOYSA-N epicatechin Natural products Cc1cc(O)cc2OC(C(O)Cc12)c1ccc(O)c(O)c1 LPTRNLNOHUVQMS-UHFFFAOYSA-N 0.000 claims 3
- 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 2
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 2
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 2
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 2
- 230000000259 anti-tumor effect Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229960004562 carboplatin Drugs 0.000 claims 2
- 190000008236 carboplatin Chemical compound 0.000 claims 2
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 2
- 229960004316 cisplatin Drugs 0.000 claims 2
- 229960002949 fluorouracil Drugs 0.000 claims 2
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound 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 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims 2
- 229960002411 imatinib Drugs 0.000 claims 2
- 229940124302 mTOR inhibitor Drugs 0.000 claims 2
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 2
- GLVAUDGFNGKCSF-UHFFFAOYSA-N mercaptopurine Chemical compound S=C1NC=NC2=C1NC=N2 GLVAUDGFNGKCSF-UHFFFAOYSA-N 0.000 claims 2
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims 2
- 229960001756 oxaliplatin Drugs 0.000 claims 2
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 claims 2
- 229910052697 platinum Inorganic materials 0.000 claims 2
- HKTBGLYNZWOCKW-NSHDSACASA-N 4-[[4-(2-amino-1,3-thiazol-5-yl)-6-[(3s)-3-methylmorpholin-4-yl]-1,3,5-triazin-2-yl]oxy]-3-fluoro-n,n-dimethylbenzamide Chemical compound C[C@H]1COCCN1C1=NC(OC=2C(=CC(=CC=2)C(=O)N(C)C)F)=NC(C=2SC(N)=NC=2)=N1 HKTBGLYNZWOCKW-NSHDSACASA-N 0.000 claims 1
- BQPZIYSVGQSCET-UHFFFAOYSA-N 4-[[4-(2-amino-1,3-thiazol-5-yl)-6-morpholin-4-yl-1,3,5-triazin-2-yl]oxy]-n,n-dimethylbenzamide Chemical compound C1=CC(C(=O)N(C)C)=CC=C1OC1=NC(N2CCOCC2)=NC(C=2SC(N)=NC=2)=N1 BQPZIYSVGQSCET-UHFFFAOYSA-N 0.000 claims 1
- POAZEDQQRWSVGZ-ZDUSSCGKSA-N 4-[[4-(6-aminopyridin-3-yl)-6-[(3s)-3-methylmorpholin-4-yl]-1,3,5-triazin-2-yl]oxy]-3-fluoro-n,n-dimethylbenzamide Chemical compound C[C@H]1COCCN1C1=NC(OC=2C(=CC(=CC=2)C(=O)N(C)C)F)=NC(C=2C=NC(N)=CC=2)=N1 POAZEDQQRWSVGZ-ZDUSSCGKSA-N 0.000 claims 1
- BQRTZZXEYYXREE-UHFFFAOYSA-N 4-[[4-(6-aminopyridin-3-yl)-6-morpholin-4-yl-1,3,5-triazin-2-yl]oxy]-n,n-dimethylbenzamide Chemical compound C1=CC(C(=O)N(C)C)=CC=C1OC1=NC(N2CCOCC2)=NC(C=2C=NC(N)=CC=2)=N1 BQRTZZXEYYXREE-UHFFFAOYSA-N 0.000 claims 1
- 229940122531 Anaplastic lymphoma kinase inhibitor Drugs 0.000 claims 1
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims 1
- 229940125431 BRAF inhibitor Drugs 0.000 claims 1
- 229940122361 Bisphosphonate Drugs 0.000 claims 1
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 1
- 101000997835 Homo sapiens Tyrosine-protein kinase JAK1 Proteins 0.000 claims 1
- 229940123241 Janus kinase 3 inhibitor Drugs 0.000 claims 1
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 1
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims 1
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims 1
- 102000043136 MAP kinase family Human genes 0.000 claims 1
- 108091054455 MAP kinase family Proteins 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 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
- 102100022596 Tyrosine-protein kinase ABL1 Human genes 0.000 claims 1
- 102100033438 Tyrosine-protein kinase JAK1 Human genes 0.000 claims 1
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims 1
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims 1
- 230000006682 Warburg effect Effects 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 239000012635 anticancer drug combination Substances 0.000 claims 1
- 238000011319 anticancer therapy Methods 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 150000004663 bisphosphonates Chemical class 0.000 claims 1
- 230000000973 chemotherapeutic effect Effects 0.000 claims 1
- 229940046044 combinations of antineoplastic agent Drugs 0.000 claims 1
- 229960004397 cyclophosphamide Drugs 0.000 claims 1
- 239000003534 dna topoisomerase inhibitor Substances 0.000 claims 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 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 claims 1
- 229960002584 gefitinib Drugs 0.000 claims 1
- 229960005277 gemcitabine Drugs 0.000 claims 1
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims 1
- 230000002414 glycolytic effect Effects 0.000 claims 1
- 239000003102 growth factor Substances 0.000 claims 1
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims 1
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims 1
- 230000028993 immune response Effects 0.000 claims 1
- 230000001024 immunotherapeutic effect Effects 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 229960004768 irinotecan Drugs 0.000 claims 1
- 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 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- 229960004891 lapatinib Drugs 0.000 claims 1
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims 1
- 229960001428 mercaptopurine Drugs 0.000 claims 1
- 230000002503 metabolic effect Effects 0.000 claims 1
- 229960000485 methotrexate Drugs 0.000 claims 1
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 230000037361 pathway Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 239000003197 protein kinase B inhibitor Substances 0.000 claims 1
- 230000011664 signaling Effects 0.000 claims 1
- 229960003787 sorafenib Drugs 0.000 claims 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 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
- 229940044693 topoisomerase inhibitor Drugs 0.000 claims 1
- 229960000303 topotecan Drugs 0.000 claims 1
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims 1
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 claims 1
- JXLYSJRDGCGARV-CFWMRBGOSA-N vinblastine Chemical compound C([C@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-CFWMRBGOSA-N 0.000 claims 1
- 229960003048 vinblastine Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN201611037375 | 2016-11-01 | ||
| IN201611037375 | 2016-11-01 | ||
| PCT/IN2017/050506 WO2018083713A1 (en) | 2016-11-01 | 2017-11-01 | Composition comprising combination of epicatechin and anti-cancer compound |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019536767A JP2019536767A (ja) | 2019-12-19 |
| JP2019536767A5 true JP2019536767A5 (enExample) | 2020-12-03 |
Family
ID=62076542
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019523821A Pending JP2019536767A (ja) | 2016-11-01 | 2017-11-01 | エピカテキン及び抗癌化合物の組合せを含む組成物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20190262347A1 (enExample) |
| EP (1) | EP3535252A4 (enExample) |
| JP (1) | JP2019536767A (enExample) |
| CN (1) | CN110312709A (enExample) |
| WO (1) | WO2018083713A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2718277A4 (en) | 2011-06-06 | 2015-02-11 | Cardero Therapeutics Inc | METHOD AND COMPOSITIONS FOR TREATING MITOCHONDRIAL TOXICITY |
| US20180193306A1 (en) | 2012-03-23 | 2018-07-12 | Cardero Therapeutics, Inc. | Compounds and compositions for the treatment of muscular disorders and bone disorders |
| CN106714770B (zh) | 2014-07-23 | 2024-04-19 | 斯法尔制药私人有限公司 | 羟基类固醇化合物、其中间体、制备方法、组合物及其用途 |
| WO2017221269A1 (en) | 2016-06-21 | 2017-12-28 | Sphaera Pharma Pvt. Ltd., | Utility of (+) epicatechin and their analogs |
| JP2022512811A (ja) | 2018-10-24 | 2022-02-07 | エピリウム バイオ インコーポレイテッド | エピカテキンとカルボキシ－ｎ－複素環式共結晶形成剤とを含む共結晶 |
| JP6746022B1 (ja) * | 2020-02-13 | 2020-08-26 | シーシーアイホールディングス株式会社 | 腫瘍細胞におけるアスパラギン酸合成の阻害剤、腫瘍細胞のスフェロイド形成阻害剤、腫瘍細胞の転移抑制剤、解糖系阻害剤の作用増強剤、並びに腫瘍の転移の抑制および／または予防用医薬組成物 |
| CN115025236B (zh) * | 2022-05-09 | 2024-03-08 | 聊城大学 | 一种加载化疗药物-茶多酚联合药物的pH响应型靶向DNA纳米载药体系 |
| WO2024036225A1 (en) | 2022-08-10 | 2024-02-15 | Epirium Bio Inc. | Epicatechin for inhibiting glutamate toxicity |
| WO2024036223A1 (en) | 2022-08-10 | 2024-02-15 | Epirium Bio Inc. | Epicatechin inhibiting atp hydrolysis |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2011105763A (ja) * | 2000-06-21 | 2011-06-02 | Kao Corp | Ｐｐａｒ依存的遺伝子転写活性化剤 |
| US7192612B2 (en) * | 2001-02-22 | 2007-03-20 | Purdue Research Foundation | Compositions and methods based on synergies between capsicum extracts and tea catechins for prevention and treatment of cancer |
| US20070054868A1 (en) * | 2005-06-20 | 2007-03-08 | The Trustees Of Columbia University In The City Of New York | Synergistic polyphenol compounds, compositions thereof, and uses thereof |
| US9630958B2 (en) * | 2012-07-23 | 2017-04-25 | Sphaera Pharma Pte. Ltd. | Triazine compounds |
-
2017
- 2017-11-01 JP JP2019523821A patent/JP2019536767A/ja active Pending
- 2017-11-01 WO PCT/IN2017/050506 patent/WO2018083713A1/en not_active Ceased
- 2017-11-01 EP EP17867283.8A patent/EP3535252A4/en not_active Withdrawn
- 2017-11-01 CN CN201780081834.1A patent/CN110312709A/zh active Pending
- 2017-11-01 US US16/345,790 patent/US20190262347A1/en not_active Abandoned
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