JP2016528209A5 - - Google Patents
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- JP2016528209A5 JP2016528209A5 JP2016525833A JP2016525833A JP2016528209A5 JP 2016528209 A5 JP2016528209 A5 JP 2016528209A5 JP 2016525833 A JP2016525833 A JP 2016525833A JP 2016525833 A JP2016525833 A JP 2016525833A JP 2016528209 A5 JP2016528209 A5 JP 2016528209A5
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- Prior art keywords
- alkyl
- optionally substituted
- halo
- cancer
- independently
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 87
- 150000001875 compounds Chemical class 0.000 claims 49
- 125000001475 halogen functional group Chemical group 0.000 claims 30
- 125000004122 cyclic group Chemical group 0.000 claims 29
- 125000003545 alkoxy group Chemical group 0.000 claims 19
- -1 where Z Chemical compound 0.000 claims 19
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 18
- 206010028980 Neoplasm Diseases 0.000 claims 16
- 150000003973 alkyl amines Chemical class 0.000 claims 13
- 208000035475 disorder Diseases 0.000 claims 10
- 230000002062 proliferating effect Effects 0.000 claims 9
- 208000023275 Autoimmune disease Diseases 0.000 claims 8
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 8
- 206010013774 Dry eye Diseases 0.000 claims 8
- 201000004681 Psoriasis Diseases 0.000 claims 8
- 201000011510 cancer Diseases 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 8
- 208000027866 inflammatory disease Diseases 0.000 claims 8
- 206010025135 lupus erythematosus Diseases 0.000 claims 8
- 238000000034 method Methods 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 108010024121 Janus Kinases Proteins 0.000 claims 6
- 102000015617 Janus Kinases Human genes 0.000 claims 6
- 238000004519 manufacturing process Methods 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 201000008808 Fibrosarcoma Diseases 0.000 claims 2
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 claims 2
- 101000932478 Homo sapiens Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 2
- 101000997835 Homo sapiens Tyrosine-protein kinase JAK1 Proteins 0.000 claims 2
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims 2
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 2
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 206010039491 Sarcoma Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 102100033438 Tyrosine-protein kinase JAK1 Human genes 0.000 claims 2
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims 2
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 201000007455 central nervous system cancer Diseases 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 2
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 208000010749 gastric carcinoma Diseases 0.000 claims 2
- 201000010536 head and neck cancer Diseases 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 230000037361 pathway Effects 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 230000000069 prophylactic effect Effects 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 2
- 201000000498 stomach carcinoma Diseases 0.000 claims 2
- 229940124597 therapeutic agent Drugs 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361845342P | 2013-07-11 | 2013-07-11 | |
| US61/845,342 | 2013-07-11 | ||
| US201461923179P | 2014-01-02 | 2014-01-02 | |
| US61/923,179 | 2014-01-02 | ||
| PCT/US2014/046442 WO2015006754A2 (en) | 2013-07-11 | 2014-07-11 | Heterocyclic compounds and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016528209A JP2016528209A (ja) | 2016-09-15 |
| JP2016528209A5 true JP2016528209A5 (https=) | 2017-08-17 |
| JP6564771B2 JP6564771B2 (ja) | 2019-08-21 |
Family
ID=51298956
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016525833A Active JP6564771B2 (ja) | 2013-07-11 | 2014-07-11 | キナーゼ阻害剤としてのピリミジン誘導体 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US10562918B2 (https=) |
| EP (1) | EP3019496B1 (https=) |
| JP (1) | JP6564771B2 (https=) |
| KR (1) | KR102173433B1 (https=) |
| CN (3) | CN112592334B (https=) |
| AU (1) | AU2014287016B2 (https=) |
| BR (1) | BR112016000195A8 (https=) |
| CA (1) | CA2917364C (https=) |
| DK (1) | DK3019496T3 (https=) |
| ES (1) | ES2761572T3 (https=) |
| IL (1) | IL243420A0 (https=) |
| MX (1) | MX368491B (https=) |
| NZ (1) | NZ715687A (https=) |
| RU (1) | RU2677653C2 (https=) |
| SG (1) | SG11201600062RA (https=) |
| WO (1) | WO2015006754A2 (https=) |
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| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| US9034885B2 (en) | 2012-01-13 | 2015-05-19 | Acea Biosciences Inc. | EGFR modulators and uses thereof |
| US9464089B2 (en) | 2012-01-13 | 2016-10-11 | Acea Biosciences Inc. | Heterocyclic compounds and uses thereof |
| CA2861010A1 (en) | 2012-01-13 | 2013-07-18 | Xiao Xu | Heterocyclic compounds and uses as anticancer agents |
| ES2704744T3 (es) | 2012-06-13 | 2019-03-19 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
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| AU2014308616B2 (en) | 2013-08-23 | 2018-12-06 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
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