JPWO2019149164A5 - - Google Patents
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- Publication number
- JPWO2019149164A5 JPWO2019149164A5 JP2020541535A JP2020541535A JPWO2019149164A5 JP WO2019149164 A5 JPWO2019149164 A5 JP WO2019149164A5 JP 2020541535 A JP2020541535 A JP 2020541535A JP 2020541535 A JP2020541535 A JP 2020541535A JP WO2019149164 A5 JPWO2019149164 A5 JP WO2019149164A5
- Authority
- JP
- Japan
- Prior art keywords
- egfr
- alkyl
- substituted
- halogen
- 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.)
- Granted
Links
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 48
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 48
- 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 48
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 229910052736 halogen Inorganic materials 0.000 claims 16
- 150000002367 halogens Chemical class 0.000 claims 16
- 239000008194 pharmaceutical composition Substances 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 12
- YZCKVEUIGOORGS-NJFSPNSNSA-N Tritium Chemical compound [3H] YZCKVEUIGOORGS-NJFSPNSNSA-N 0.000 claims 11
- 229910052722 tritium Inorganic materials 0.000 claims 11
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 10
- 229910052805 deuterium Inorganic materials 0.000 claims 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 101150029707 ERBB2 gene Proteins 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 229920006395 saturated elastomer Polymers 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 150000002148 esters Chemical class 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000004452 carbocyclyl group Chemical group 0.000 claims 3
- -1 cyano, hydroxyl Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 125000002950 monocyclic group Chemical group 0.000 claims 3
- 125000003367 polycyclic group Chemical group 0.000 claims 3
- 102200048955 rs121434569 Human genes 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- 125000004642 (C1-C12) alkoxy group Chemical group 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 102200048928 rs121434568 Human genes 0.000 claims 2
- 102200048795 rs121913428 Human genes 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 102200048929 rs121913444 Human genes 0.000 claims 1
- 102200048951 rs121913465 Human genes 0.000 claims 1
- 102220014448 rs1554350381 Human genes 0.000 claims 1
- 102200048796 rs28929495 Human genes 0.000 claims 1
- 102200048979 rs28929495 Human genes 0.000 claims 1
- 102220004843 rs397516975 Human genes 0.000 claims 1
- 102220014234 rs397516981 Human genes 0.000 claims 1
- 102200048801 rs397517085 Human genes 0.000 claims 1
- 102220014441 rs397517109 Human genes 0.000 claims 1
- 102220014444 rs397517111 Human genes 0.000 claims 1
- 102220014445 rs397517112 Human genes 0.000 claims 1
- 102220055972 rs397517115 Human genes 0.000 claims 1
- 102220014449 rs397517116 Human genes 0.000 claims 1
- 102220055958 rs727504263 Human genes 0.000 claims 1
- 102220055962 rs730880333 Human genes 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023180451A JP7738619B2 (ja) | 2018-01-31 | 2023-10-19 | Ｅｒｂｂ／ｂｔｋ阻害剤 |
| JP2025145276A JP2025179139A (ja) | 2018-01-31 | 2025-09-02 | Ｅｒｂｂ／ｂｔｋ阻害剤 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2018/074791 | 2018-01-31 | ||
| CN2018074791 | 2018-01-31 | ||
| CN2018118569 | 2018-11-30 | ||
| CNPCT/CN2018/118569 | 2018-11-30 | ||
| PCT/CN2019/073355 WO2019149164A1 (en) | 2018-01-31 | 2019-01-28 | Erbb/btk inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023180451A Division JP7738619B2 (ja) | 2018-01-31 | 2023-10-19 | Ｅｒｂｂ／ｂｔｋ阻害剤 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021512087A JP2021512087A (ja) | 2021-05-13 |
| JP2021512087A5 JP2021512087A5 (https=) | 2022-02-02 |
| JPWO2019149164A5 true JPWO2019149164A5 (https=) | 2022-02-02 |
| JP7427597B2 JP7427597B2 (ja) | 2024-02-05 |
Family
ID=67478612
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020541535A Active JP7427597B2 (ja) | 2018-01-31 | 2019-01-28 | Ｅｒｂｂ／ｂｔｋ阻害剤 |
| JP2023180451A Active JP7738619B2 (ja) | 2018-01-31 | 2023-10-19 | Ｅｒｂｂ／ｂｔｋ阻害剤 |
| JP2025145276A Pending JP2025179139A (ja) | 2018-01-31 | 2025-09-02 | Ｅｒｂｂ／ｂｔｋ阻害剤 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023180451A Active JP7738619B2 (ja) | 2018-01-31 | 2023-10-19 | Ｅｒｂｂ／ｂｔｋ阻害剤 |
| JP2025145276A Pending JP2025179139A (ja) | 2018-01-31 | 2025-09-02 | Ｅｒｂｂ／ｂｔｋ阻害剤 |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US11007198B2 (https=) |
| EP (2) | EP4356975A3 (https=) |
| JP (3) | JP7427597B2 (https=) |
| KR (2) | KR20250046340A (https=) |
| CN (3) | CN111587244A (https=) |
| AU (2) | AU2019215538B2 (https=) |
| CA (1) | CA3086616A1 (https=) |
| DK (1) | DK3746424T3 (https=) |
| ES (1) | ES2977484T3 (https=) |
| MX (2) | MX2020007947A (https=) |
| PT (1) | PT3746424T (https=) |
| RU (2) | RU2764069C1 (https=) |
| TW (1) | TWI798334B (https=) |
| WO (1) | WO2019149164A1 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11896597B2 (en) * | 2018-01-31 | 2024-02-13 | Dizal (Jiangsu) Pharmaceutical Co., Ltd. | ErbB/BTK inhibitors |
| TWI798334B (zh) * | 2018-01-31 | 2023-04-11 | 大陸商迪哲（江蘇）醫藥股份有限公司 | Ｅｒｂｂ／ｂｔｋ抑制劑 |
| US12157730B2 (en) | 2019-03-19 | 2024-12-03 | Voronoi Inc. | Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component |
| AU2020240382B2 (en) | 2019-03-19 | 2022-08-25 | Voronoi Inc. | Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component |
| WO2021104305A1 (zh) * | 2019-11-26 | 2021-06-03 | 上海翰森生物医药科技有限公司 | 含氮多环类衍生物抑制剂、其制备方法和应用 |
| CN111057021B (zh) * | 2019-12-11 | 2023-05-23 | 中国药科大学 | 均三嗪类化合物及其制备方法和用途 |
| US20230137932A1 (en) * | 2020-01-07 | 2023-05-04 | Dana-Farber Cancer Institute, Inc. | Cyano-pyrimidine inhibitors of egfr/her2 |
| CN111470998B (zh) * | 2020-06-28 | 2020-09-25 | 上海皓元生物医药科技有限公司 | 用于合成喜树碱衍生物的中间体及其制备方法和用途 |
| CN112409281B (zh) * | 2020-08-20 | 2022-11-18 | 上海大学 | (e)-3-(3-氯-2-氟-6-(1h-四氮唑-1-基)苯基)丙烯酸的合成方法 |
| CN112679446A (zh) * | 2020-10-26 | 2021-04-20 | 都创(上海)医药科技有限公司 | 一种合成反式-3-(3-氯-2-氟-6-(1h-四氮唑-1-基)苯基)丙烯酸的方法 |
| WO2022206797A1 (zh) * | 2021-03-30 | 2022-10-06 | 贝达药业股份有限公司 | Egfr抑制剂及其组合物和用途 |
| EP4323356A1 (en) | 2021-04-13 | 2024-02-21 | Nuvalent, Inc. | Amino-substituted heterocycles for treating cancers with egfr mutations |
| AU2022303386A1 (en) * | 2021-07-02 | 2023-12-14 | Aldeyra Therapeutics, Inc. | Heterocyclic aldehyde trapping compounds and uses thereof |
| EP4380924A4 (en) * | 2021-08-02 | 2025-10-01 | Dizal Jiangsu Pharmaceutical Co Ltd | NEW PHARMACEUTICAL SALTS AND POLYMORPHIC FORMS OF AN ERBB AND BTK INHIBITOR |
| CN115181093B (zh) * | 2022-08-01 | 2023-04-25 | 重庆医科大学 | Sunvozertinib中间体的制备方法 |
| WO2024261740A1 (en) | 2023-06-23 | 2024-12-26 | Assia Chemical Industries, Ltd. | Solid state forms of sunvozertinib |
| WO2025247783A1 (en) | 2024-05-29 | 2025-12-04 | Syngenta Crop Protection Ag | Pesticidally active dihydro-benzoxazinone compounds |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1719762B1 (en) * | 2004-02-27 | 2012-06-27 | Eisai R&D Management Co., Ltd. | Novel pyridine derivative and pyrimidine derivative (1) |
| US8338439B2 (en) | 2008-06-27 | 2012-12-25 | Celgene Avilomics Research, Inc. | 2,4-disubstituted pyrimidines useful as kinase inhibitors |
| TWI546290B (zh) * | 2008-06-27 | 2016-08-21 | 賽基艾維洛米斯研究股份有限公司 | 雜芳基化合物及其用途 |
| PL2805940T3 (pl) | 2012-01-17 | 2017-06-30 | Astellas Pharma Inc. | Związek pirazynokarboksyamidowy |
| PL2825042T3 (pl) * | 2012-03-15 | 2019-02-28 | Celgene Car Llc | Sole inhibitora kinazy receptora czynnika wzrostu naskórka |
| US20150166591A1 (en) * | 2012-05-05 | 2015-06-18 | Ariad Pharmaceuticals, Inc. | Methods and compositions for raf kinase mediated diseases |
| BR112015010221B1 (pt) | 2012-11-06 | 2022-09-13 | Shanghai Fochon Pharmaceutical Co., Ltd. | Inibidores de quinase alk, seus usos, composição farmacêutica, e método para fabricação de medicamento |
| SG11201600055PA (en) * | 2013-07-11 | 2016-02-26 | Betta Pharmaceuticals Co Ltd | Protein tyrosine kinase modulators and methods of use |
| CN105377835B (zh) * | 2013-07-11 | 2018-08-17 | 贝达药业股份有限公司 | 酪氨酸蛋白激酶调节剂及其应用方法 |
| US9415050B2 (en) | 2013-08-12 | 2016-08-16 | Pharmacyclics Llc | Methods for the treatment of HER2 amplified cancer |
| CN105384694B (zh) * | 2014-08-22 | 2020-09-04 | 四川海思科制药有限公司 | 一种取代的氨基嘧啶衍生物及其制备方法和药物用途 |
| CN106883213B (zh) * | 2015-12-15 | 2021-04-20 | 合肥中科普瑞昇生物医药科技有限公司 | 一种egfr和alk激酶的双重抑制剂 |
| CN106905245B (zh) * | 2015-12-23 | 2021-06-25 | 正大天晴药业集团股份有限公司 | 2,4-二取代的嘧啶类化合物 |
| CN106928150B (zh) * | 2015-12-31 | 2020-07-31 | 恩瑞生物医药科技（上海）有限公司 | 丙烯酰胺苯胺衍生物及其药学上的应用 |
| CN106083736A (zh) * | 2016-06-21 | 2016-11-09 | 郑州泰基鸿诺医药股份有限公司 | 一种嘧啶类化合物、egfr抑制剂及其应用 |
| TWI798334B (zh) * | 2018-01-31 | 2023-04-11 | 大陸商迪哲（江蘇）醫藥股份有限公司 | Ｅｒｂｂ／ｂｔｋ抑制劑 |
| KR102782739B1 (ko) * | 2018-03-13 | 2025-03-20 | 보로노이 주식회사 | 2,4,5-치환된 피리미딘 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 암의 예방 또는 치료용 약학적 조성물 |
-
2019
- 2019-01-17 TW TW108101860A patent/TWI798334B/zh active
- 2019-01-28 EP EP24161138.3A patent/EP4356975A3/en active Pending
- 2019-01-28 RU RU2020127393A patent/RU2764069C1/ru active
- 2019-01-28 CN CN201980006427.3A patent/CN111587244A/zh active Pending
- 2019-01-28 EP EP19748259.9A patent/EP3746424B1/en active Active
- 2019-01-28 KR KR1020257009058A patent/KR20250046340A/ko active Pending
- 2019-01-28 RU RU2021139070A patent/RU2021139070A/ru unknown
- 2019-01-28 CN CN202010659802.9A patent/CN111747934A/zh active Pending
- 2019-01-28 AU AU2019215538A patent/AU2019215538B2/en active Active
- 2019-01-28 JP JP2020541535A patent/JP7427597B2/ja active Active
- 2019-01-28 MX MX2020007947A patent/MX2020007947A/es unknown
- 2019-01-28 CN CN202010660882.XA patent/CN111909131B/zh active Active
- 2019-01-28 DK DK19748259.9T patent/DK3746424T3/da active
- 2019-01-28 CA CA3086616A patent/CA3086616A1/en active Pending
- 2019-01-28 WO PCT/CN2019/073355 patent/WO2019149164A1/en not_active Ceased
- 2019-01-28 KR KR1020207025029A patent/KR102786279B1/ko active Active
- 2019-01-28 ES ES19748259T patent/ES2977484T3/es active Active
- 2019-01-28 PT PT197482599T patent/PT3746424T/pt unknown
-
2020
- 2020-06-24 US US16/910,208 patent/US11007198B2/en active Active
- 2020-07-28 MX MX2023010411A patent/MX2023010411A/es unknown
-
2021
- 2021-04-07 US US17/224,121 patent/US11504375B2/en active Active
-
2023
- 2023-04-06 AU AU2023202151A patent/AU2023202151B2/en active Active
- 2023-10-19 JP JP2023180451A patent/JP7738619B2/ja active Active
-
2025
- 2025-09-02 JP JP2025145276A patent/JP2025179139A/ja active Pending
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