JP2020523348A5 - - Google Patents
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- JP2020523348A5 JP2020523348A5 JP2019568372A JP2019568372A JP2020523348A5 JP 2020523348 A5 JP2020523348 A5 JP 2020523348A5 JP 2019568372 A JP2019568372 A JP 2019568372A JP 2019568372 A JP2019568372 A JP 2019568372A JP 2020523348 A5 JP2020523348 A5 JP 2020523348A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- alkyl
- cancer
- salt according
- halo
- 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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- 150000001875 compounds Chemical class 0.000 claims 31
- 150000003839 salts Chemical class 0.000 claims 23
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 125000005843 halogen group Chemical group 0.000 claims 14
- 125000003545 alkoxy group Chemical group 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 108091008606 PDGF receptors Proteins 0.000 claims 4
- 102000011653 Platelet-Derived Growth Factor Receptors Human genes 0.000 claims 4
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 4
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- -1 R c is H Chemical group 0.000 claims 3
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 3
- 108091008605 VEGF receptors Proteins 0.000 claims 3
- 102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 claims 3
- 108010003374 fms-Like Tyrosine Kinase 3 Proteins 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 229940124676 vascular endothelial growth factor receptor Drugs 0.000 claims 3
- 101000916644 Homo sapiens Macrophage colony-stimulating factor 1 receptor Proteins 0.000 claims 2
- 101000823316 Homo sapiens Tyrosine-protein kinase ABL1 Proteins 0.000 claims 2
- 102100028198 Macrophage colony-stimulating factor 1 receptor Human genes 0.000 claims 2
- 102100033116 Mitogen-activated protein kinase kinase kinase 20 Human genes 0.000 claims 2
- 108700020796 Oncogene Proteins 0.000 claims 2
- 102000001332 SRC Human genes 0.000 claims 2
- 108060006706 SRC Proteins 0.000 claims 2
- 102100022596 Tyrosine-protein kinase ABL1 Human genes 0.000 claims 2
- 241000700605 Viruses Species 0.000 claims 2
- 150000001721 carbon Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 102000005962 receptors Human genes 0.000 claims 2
- 108020003175 receptors Proteins 0.000 claims 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000003950 B-cell lymphoma Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 102100035080 BDNF/NT-3 growth factors receptor Human genes 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm 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
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 241000282326 Felis catus Species 0.000 claims 1
- 201000003741 Gastrointestinal carcinoma Diseases 0.000 claims 1
- 102100035108 High affinity nerve growth factor receptor Human genes 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 101000596896 Homo sapiens BDNF/NT-3 growth factors receptor Proteins 0.000 claims 1
- 101000596894 Homo sapiens High affinity nerve growth factor receptor Proteins 0.000 claims 1
- 101000977771 Homo sapiens Interleukin-1 receptor-associated kinase 4 Proteins 0.000 claims 1
- 101001018157 Homo sapiens Mitogen-activated protein kinase kinase kinase 20 Proteins 0.000 claims 1
- 101001047681 Homo sapiens Tyrosine-protein kinase Lck Proteins 0.000 claims 1
- 206010021042 Hypopharyngeal cancer Diseases 0.000 claims 1
- 206010056305 Hypopharyngeal neoplasm Diseases 0.000 claims 1
- 102100023533 Interleukin-1 receptor-associated kinase 4 Human genes 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 108010066373 MLK-like mitogen-activated protein triple kinase Proteins 0.000 claims 1
- 102100027754 Mast/stem cell growth factor receptor Kit Human genes 0.000 claims 1
- 101710087603 Mast/stem cell growth factor receptor Kit Proteins 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 102100029166 NT-3 growth factor receptor Human genes 0.000 claims 1
- 101150117329 NTRK3 gene Proteins 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010030155 Oesophageal carcinoma 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
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000007452 Plasmacytoma Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 102100028286 Proto-oncogene tyrosine-protein kinase receptor Ret Human genes 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 101710083476 Tyrosine-protein kinase Blk Proteins 0.000 claims 1
- 102100027053 Tyrosine-protein kinase Blk Human genes 0.000 claims 1
- 102100024036 Tyrosine-protein kinase Lck Human genes 0.000 claims 1
- 102100026857 Tyrosine-protein kinase Lyn Human genes 0.000 claims 1
- 101710088331 Tyrosine-protein kinase Lyn Proteins 0.000 claims 1
- 102100021788 Tyrosine-protein kinase Yes Human genes 0.000 claims 1
- 101710107570 Tyrosine-protein kinase Yes Proteins 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 102000009520 Vascular Endothelial Growth Factor C Human genes 0.000 claims 1
- 108010073923 Vascular Endothelial Growth Factor C Proteins 0.000 claims 1
- 108010053100 Vascular Endothelial Growth Factor Receptor-3 Proteins 0.000 claims 1
- 102100033179 Vascular endothelial growth factor receptor 3 Human genes 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 210000000941 bile Anatomy 0.000 claims 1
- 201000009036 biliary tract cancer Diseases 0.000 claims 1
- 208000020790 biliary tract neoplasm Diseases 0.000 claims 1
- 206010006007 bone sarcoma Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 208000024519 eye neoplasm Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 210000004907 gland Anatomy 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 201000006866 hypopharynx cancer Diseases 0.000 claims 1
- 230000037431 insertion Effects 0.000 claims 1
- 238000003780 insertion Methods 0.000 claims 1
- 201000002313 intestinal cancer Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 201000005831 male reproductive organ cancer Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000009826 neoplastic cell growth Effects 0.000 claims 1
- 210000005036 nerve Anatomy 0.000 claims 1
- 201000002120 neuroendocrine carcinoma Diseases 0.000 claims 1
- 201000008106 ocular cancer Diseases 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 102200039431 rs121913488 Human genes 0.000 claims 1
- 102200006095 rs77724903 Human genes 0.000 claims 1
- 102200006097 rs79658334 Human genes 0.000 claims 1
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000004001 thioalkyl group Chemical group 0.000 claims 1
- 238000001890 transfection Methods 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
- 108010002164 tyrosine receptor Proteins 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762518855P | 2017-06-13 | 2017-06-13 | |
| US62/518,855 | 2017-06-13 | ||
| PCT/US2018/037221 WO2018231910A1 (en) | 2017-06-13 | 2018-06-13 | Aminothiazole compounds as protein kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020523348A JP2020523348A (ja) | 2020-08-06 |
| JP2020523348A5 true JP2020523348A5 (https=) | 2021-07-26 |
| JP6979595B2 JP6979595B2 (ja) | 2021-12-15 |
Family
ID=64562741
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019568372A Active JP6979595B2 (ja) | 2017-06-13 | 2018-06-13 | プロテインキナーゼ阻害剤としてのアミノチアゾール化合物 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US10300061B2 (https=) |
| EP (1) | EP3638237B1 (https=) |
| JP (1) | JP6979595B2 (https=) |
| KR (1) | KR102372288B1 (https=) |
| CN (1) | CN110831596B (https=) |
| AU (1) | AU2018284249B2 (https=) |
| CA (1) | CA3064081C (https=) |
| ES (1) | ES2949616T3 (https=) |
| MX (1) | MX393992B (https=) |
| MY (1) | MY201291A (https=) |
| TW (1) | TWI667236B (https=) |
| WO (1) | WO2018231910A1 (https=) |
| ZA (1) | ZA202000107B (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102797697B1 (ko) | 2018-05-25 | 2025-04-22 | 에이2에이 파마수티칼스, 잉크. | 신종 항암제 후보로서, 매우 강력한 tacc3 억제제 |
| JP7681018B2 (ja) * | 2019-11-14 | 2025-05-21 | エーツーエー ファーマシューティカルズ インコーポレーテッド | 抗がん剤としてｔａｃｃ３を標的とするイソオキサゾール誘導体 |
| EP4087574A4 (en) * | 2020-03-06 | 2024-01-17 | National Health Research Institutes | PYRIMIDINE COMPOUNDS AND THEIR PHARMACEUTICAL USES |
| US11299489B1 (en) | 2020-11-19 | 2022-04-12 | National Health Research Institutes | Thiazole compounds as protein kinase inhibitors |
| KR20240005751A (ko) * | 2021-04-12 | 2024-01-12 | 에이2에이 파마수티칼스, 잉크. | 암 치료를 위한 조성물 및 방법 |
| EP4499625A4 (en) | 2022-03-24 | 2026-03-18 | A2A Pharmaceuticals Inc | CANCER COMPOSITIONS AND TREATMENT METHODS |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2503715A1 (en) * | 2002-10-30 | 2004-05-21 | Merck & Co., Inc. | Kinase inhibitors |
| AU2006231929B2 (en) * | 2005-04-04 | 2012-09-06 | Ab Science | Substituted oxazole derivatives and their use as tyrosine kinase inhibitors |
| AU2006258101A1 (en) * | 2005-06-09 | 2006-12-21 | Merck Sharp & Dohme Corp. | Inhibitors of checkpoint kinases |
| GB0610909D0 (en) * | 2006-06-05 | 2006-07-12 | Merck Sharp & Dohme | Therapeutic treatment |
| AU2007296743B2 (en) | 2006-09-11 | 2012-02-16 | Curis, Inc. | Tyrosine kinase inhibitors containing a zinc binding moiety |
| TW200906825A (en) * | 2007-05-30 | 2009-02-16 | Scripps Research Inst | Inhibitors of protein kinases |
| US9255072B2 (en) * | 2011-03-04 | 2016-02-09 | National Health Rsearch Institutes | Pyrazole compounds and thiazole compounds as protein kinases inhibitors |
| EP2736904B1 (en) * | 2011-07-27 | 2016-03-16 | AB Science | Oxazole and thiazole derivatives as selective protein kinase inhibitors (c-kit) |
| WO2013143466A1 (zh) * | 2012-03-27 | 2013-10-03 | 广东东阳光药业有限公司 | 作为欧若拉激酶抑制剂的取代嘧啶衍生物 |
| CN106279143A (zh) * | 2015-05-11 | 2017-01-04 | 天津国际生物医药联合研究院 | 噻唑杂环类化合物及其制备方法和应用 |
| WO2018106643A1 (en) | 2016-12-06 | 2018-06-14 | Vertex Pharmaceuticals Incorporated | Heterocyclic azoles for the treatment of demyelinating diseases |
-
2018
- 2018-06-11 TW TW107120014A patent/TWI667236B/zh active
- 2018-06-13 ES ES18817380T patent/ES2949616T3/es active Active
- 2018-06-13 CA CA3064081A patent/CA3064081C/en active Active
- 2018-06-13 US US16/007,417 patent/US10300061B2/en active Active
- 2018-06-13 EP EP18817380.1A patent/EP3638237B1/en active Active
- 2018-06-13 MX MX2019014845A patent/MX393992B/es unknown
- 2018-06-13 AU AU2018284249A patent/AU2018284249B2/en active Active
- 2018-06-13 KR KR1020197038421A patent/KR102372288B1/ko active Active
- 2018-06-13 JP JP2019568372A patent/JP6979595B2/ja active Active
- 2018-06-13 MY MYPI2019006791A patent/MY201291A/en unknown
- 2018-06-13 CN CN201880039827.XA patent/CN110831596B/zh active Active
- 2018-06-13 WO PCT/US2018/037221 patent/WO2018231910A1/en not_active Ceased
-
2020
- 2020-01-08 ZA ZA2020/00107A patent/ZA202000107B/en unknown
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