JP2020532581A5 - - Google Patents
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- JP2020532581A5 JP2020532581A5 JP2020533340A JP2020533340A JP2020532581A5 JP 2020532581 A5 JP2020532581 A5 JP 2020532581A5 JP 2020533340 A JP2020533340 A JP 2020533340A JP 2020533340 A JP2020533340 A JP 2020533340A JP 2020532581 A5 JP2020532581 A5 JP 2020532581A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- independently
- alkyl
- halogen
- haloalkyl
- 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.)
- Granted
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims description 85
- 229910052799 carbon Inorganic materials 0.000 claims description 66
- 229910052736 halogen Inorganic materials 0.000 claims description 62
- 150000002367 halogens Chemical class 0.000 claims description 62
- 150000001875 compounds Chemical class 0.000 claims description 46
- 125000000623 heterocyclic group Chemical group 0.000 claims description 46
- 239000000203 mixture Substances 0.000 claims description 41
- 229940002612 prodrug Drugs 0.000 claims description 37
- 239000000651 prodrug Substances 0.000 claims description 37
- 150000003839 salts Chemical class 0.000 claims description 37
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 36
- 239000012453 solvate Substances 0.000 claims description 36
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims description 26
- 229920002554 vinyl polymer Polymers 0.000 claims description 26
- 125000000843 phenylene group Chemical group C1(=C(C=CC=C1)*)* 0.000 claims description 24
- 125000001188 haloalkyl group Chemical group 0.000 claims description 22
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 22
- 150000004677 hydrates Chemical class 0.000 claims description 21
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 20
- 125000005549 heteroarylene group Chemical group 0.000 claims description 20
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 16
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 16
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 16
- -1 frill Chemical group 0.000 claims description 14
- 125000002568 propynyl group Chemical group [*]C#CC([H])([H])[H] 0.000 claims description 12
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 11
- 201000010099 disease Diseases 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 125000000732 arylene group Chemical group 0.000 claims description 6
- 125000002757 morpholinyl group Chemical group 0.000 claims description 6
- 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 claims description 5
- 101000917134 Homo sapiens Fibroblast growth factor receptor 4 Proteins 0.000 claims description 5
- 230000001404 mediated effect Effects 0.000 claims description 5
- 125000004406 C3-C8 cycloalkylene group Chemical group 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 125000004193 piperazinyl group Chemical group 0.000 claims description 4
- 206010061692 Benign muscle neoplasm Diseases 0.000 claims description 3
- 206010004593 Bile duct cancer Diseases 0.000 claims description 3
- 206010006187 Breast cancer Diseases 0.000 claims description 3
- 208000026310 Breast neoplasm Diseases 0.000 claims description 3
- 206010009944 Colon cancer Diseases 0.000 claims description 3
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 3
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 3
- 201000004458 Myoma Diseases 0.000 claims description 3
- 206010033128 Ovarian cancer Diseases 0.000 claims description 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 3
- 206010060862 Prostate cancer Diseases 0.000 claims description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 3
- 206010038389 Renal cancer Diseases 0.000 claims description 3
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 3
- 206010039491 Sarcoma Diseases 0.000 claims description 3
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 3
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 3
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 3
- 208000026900 bile duct neoplasm Diseases 0.000 claims description 3
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 3
- 206010017758 gastric cancer Diseases 0.000 claims description 3
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 3
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 3
- 208000020082 intraepithelial neoplasia Diseases 0.000 claims description 3
- 201000010982 kidney cancer Diseases 0.000 claims description 3
- 201000005249 lung adenocarcinoma Diseases 0.000 claims description 3
- 201000005202 lung cancer Diseases 0.000 claims description 3
- 208000020816 lung neoplasm Diseases 0.000 claims description 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 3
- 201000001441 melanoma Diseases 0.000 claims description 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 3
- 210000000496 pancreas Anatomy 0.000 claims description 3
- 201000002094 pancreatic adenocarcinoma Diseases 0.000 claims description 3
- 201000002528 pancreatic cancer Diseases 0.000 claims description 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 3
- 201000008129 pancreatic ductal adenocarcinoma Diseases 0.000 claims description 3
- 201000000849 skin cancer Diseases 0.000 claims description 3
- 201000011549 stomach cancer Diseases 0.000 claims description 3
- 201000002510 thyroid cancer Diseases 0.000 claims description 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 125000002993 cycloalkylene group Chemical group 0.000 claims description 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 2
- 125000004956 cyclohexylene group Chemical group 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 125000002883 imidazolyl group Chemical group 0.000 claims description 2
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 2
- 125000002971 oxazolyl group Chemical group 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims description 2
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 2
- 208000015347 renal cell adenocarcinoma Diseases 0.000 claims description 2
- 239000000126 substance Substances 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 125000005247 tetrazinyl group Chemical group N1=NN=NC(=C1)* 0.000 claims description 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- 125000004306 triazinyl group Chemical group 0.000 claims description 2
- 125000001425 triazolyl group Chemical group 0.000 claims description 2
- 125000000217 alkyl group Chemical group 0.000 description 55
- 125000003545 alkoxy group Chemical group 0.000 description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 125000000304 alkynyl group Chemical group 0.000 description 4
- 238000000034 method Methods 0.000 description 3
- 0 *C(NC(CCCCC1)CC1c1n[n]c(**c2c(*)c(*)c(*)c(*)c2*)c1*)=O Chemical compound *C(NC(CCCCC1)CC1c1n[n]c(**c2c(*)c(*)c(*)c(*)c2*)c1*)=O 0.000 description 1
- 125000004404 heteroalkyl group Chemical group 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023144389A JP2023158113A (ja) | 2017-09-05 | 2023-09-06 | 芳香族誘導体、その調製方法、およびその医学的適用 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710791233 | 2017-09-05 | ||
| CN201710791233.1 | 2017-09-05 | ||
| PCT/CN2018/104007 WO2019047826A1 (zh) | 2017-09-05 | 2018-09-04 | 芳香类衍生物、其制备方法及其在医药上的应用 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023144389A Division JP2023158113A (ja) | 2017-09-05 | 2023-09-06 | 芳香族誘導体、その調製方法、およびその医学的適用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020532581A JP2020532581A (ja) | 2020-11-12 |
| JP2020532581A5 true JP2020532581A5 (enExample) | 2021-10-14 |
| JP7346420B2 JP7346420B2 (ja) | 2023-09-19 |
Family
ID=65634601
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020533340A Active JP7346420B2 (ja) | 2017-09-05 | 2018-09-04 | 芳香族誘導体、その調製方法、およびその医学的適用 |
| JP2023144389A Pending JP2023158113A (ja) | 2017-09-05 | 2023-09-06 | 芳香族誘導体、その調製方法、およびその医学的適用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023144389A Pending JP2023158113A (ja) | 2017-09-05 | 2023-09-06 | 芳香族誘導体、その調製方法、およびその医学的適用 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US11279697B2 (enExample) |
| EP (1) | EP3680236A4 (enExample) |
| JP (2) | JP7346420B2 (enExample) |
| KR (1) | KR102677016B1 (enExample) |
| CN (1) | CN110997637B (enExample) |
| CA (1) | CA3074885A1 (enExample) |
| PH (1) | PH12020500436A1 (enExample) |
| SG (1) | SG11202001979PA (enExample) |
| TW (1) | TWI817955B (enExample) |
| WO (1) | WO2019047826A1 (enExample) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020177067A1 (en) | 2019-03-05 | 2020-09-10 | Bioardis Llc | Aromatic derivatives, preparation methods, and medical uses thereof |
| WO2021060307A1 (ja) * | 2019-09-25 | 2021-04-01 | 富士フイルム株式会社 | イミダゾピリジン化合物またはその塩および医薬組成物 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| CA2839437A1 (en) | 2011-06-16 | 2012-12-20 | Isis Pharmaceuticals, Inc. | Antisense modulation of fibroblast growth factor receptor 4 expression |
| US8802697B2 (en) | 2012-07-11 | 2014-08-12 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| US10124003B2 (en) * | 2013-07-18 | 2018-11-13 | Taiho Pharmaceutical Co., Ltd. | Therapeutic agent for FGFR inhibitor-resistant cancer |
| CN110354128A (zh) | 2013-10-18 | 2019-10-22 | 卫材R&D管理有限公司 | 嘧啶fgfr4抑制剂 |
| AU2014339972B9 (en) | 2013-10-25 | 2019-05-30 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| MX367723B (es) | 2013-10-25 | 2019-09-03 | Novartis Ag | Compuestos de anillos fusionados bicíclicos derivados de piridilo como inhibidores de fgfr4. |
| JP6655559B2 (ja) | 2014-06-24 | 2020-02-26 | コベストロ、ドイチュラント、アクチエンゲゼルシャフトＣｏｖｅｓｔｒｏ Ｄｅｕｔｓｃｈｌａｎｄ Ａｇ | ジフェニルメタン系ジアミンおよびポリアミンの製造方法 |
| WO2016064960A1 (en) * | 2014-10-22 | 2016-04-28 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| EP3029864B1 (en) | 2014-12-01 | 2020-11-18 | Harman Becker Automotive Systems GmbH | Fast representation of station information in a fm receiver using a single tuner |
| ES2895769T3 (es) | 2015-02-20 | 2022-02-22 | Incyte Corp | Heterociclos bicíclicos como inhibidores de FGFR |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US9580423B2 (en) * | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CN105906630B (zh) * | 2015-04-06 | 2018-10-23 | 四川百利药业有限责任公司 | 用作fgfr抑制剂的n-(1h-吡唑-5-基)嘧啶并吡唑-4,6-二取代胺类化合物 |
| WO2016164703A1 (en) * | 2015-04-09 | 2016-10-13 | Eisai R & D Management Co., Ltd. | Fgfr4 inhibitors |
| CN109224235B (zh) | 2018-10-23 | 2020-05-19 | 孙喜家 | 一种双腔管 |
| CN109331654A (zh) | 2018-10-26 | 2019-02-15 | 高邮高和光电器材有限公司 | 一种有机废气光催化氧化装置 |
-
2018
- 2018-09-04 SG SG11202001979PA patent/SG11202001979PA/en unknown
- 2018-09-04 EP EP18854268.2A patent/EP3680236A4/en not_active Withdrawn
- 2018-09-04 US US16/644,919 patent/US11279697B2/en active Active
- 2018-09-04 CN CN201880034411.9A patent/CN110997637B/zh active Active
- 2018-09-04 JP JP2020533340A patent/JP7346420B2/ja active Active
- 2018-09-04 CA CA3074885A patent/CA3074885A1/en active Pending
- 2018-09-04 WO PCT/CN2018/104007 patent/WO2019047826A1/zh not_active Ceased
- 2018-09-04 KR KR1020207009736A patent/KR102677016B1/ko active Active
- 2018-09-05 TW TW107131186A patent/TWI817955B/zh active
-
2020
- 2020-03-04 PH PH12020500436A patent/PH12020500436A1/en unknown
-
2023
- 2023-09-06 JP JP2023144389A patent/JP2023158113A/ja active Pending