CA2970185C - Substituted 2-anilinopyrimidine derivatives as egfr modulators - Google Patents
Substituted 2-anilinopyrimidine derivatives as egfr modulators Download PDFInfo
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- CA2970185C CA2970185C CA2970185A CA2970185A CA2970185C CA 2970185 C CA2970185 C CA 2970185C CA 2970185 A CA2970185 A CA 2970185A CA 2970185 A CA2970185 A CA 2970185A CA 2970185 C CA2970185 C CA 2970185C
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- compound
- cancer
- pharmaceutically acceptable
- solvate
- acceptable salt
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61P35/00—Antineoplastic agents
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| US62/166,883 | 2015-05-27 | ||
| PCT/US2015/065286 WO2016094821A2 (en) | 2014-12-11 | 2015-12-11 | Substituted 2-anilinopyrimidine derivatives as egfr modulators |
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| CA2970185C true CA2970185C (en) | 2023-10-17 |
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| US10590111B2 (en) * | 2014-12-11 | 2020-03-17 | Beta Pharma, Inc. | Substituted 2-anilinopyrimidine derivatives as EGFR modulators |
| US11052086B2 (en) * | 2016-05-11 | 2021-07-06 | Beta Pharma, Inc. | 2-anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers |
| CN109311858B (zh) | 2016-05-26 | 2021-12-03 | 里科瑞尔姆Ip控股有限责任公司 | Egfr抑制剂化合物 |
| EP3471730B1 (en) | 2016-06-17 | 2021-10-20 | Beta Pharma, Inc. | Pharmaceutical salts of n-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1h-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide and crystalline forms thereof |
| CN106243044A (zh) * | 2016-06-30 | 2016-12-21 | 浙江大学 | 含卤代丙烯酰胺侧链的嘧啶类衍生物及制备和应用 |
| CN108602802B (zh) * | 2016-07-26 | 2020-01-21 | 深圳市塔吉瑞生物医药有限公司 | 用于抑制蛋白酪氨酸激酶活性的氨基嘧啶类化合物 |
| MX2019015177A (es) * | 2017-06-16 | 2020-02-07 | Beta Pharma Inc | Formulaciones farmaceuticas de n-(2-(2-(dimetilamino)etoxi)-4-meto xi-5((4-(1-metil-1h-indol-3-il)pirimidin-2-il)amino)fenil)acrilam ida y las sales de ellas. |
| CN109503573A (zh) * | 2017-09-14 | 2019-03-22 | 昆明圣加南生物科技有限公司 | 2-取代苯胺基嘧啶衍生物及其用途 |
| CN107935995A (zh) * | 2017-11-28 | 2018-04-20 | 中山大学 | 一种新型2‑苯胺基嘧啶衍生物及其在制备抗肿瘤药物中的应用 |
| CN108017633A (zh) * | 2018-01-30 | 2018-05-11 | 天津大学 | N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-2-氟代丙烯酰胺衍生物及应用 |
| PT3806898T (pt) * | 2018-06-18 | 2025-12-02 | UCB Biopharma SRL | Antagonista de gremlin-1 para utilização no tratamento do cancro |
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| US12390464B2 (en) | 2019-09-23 | 2025-08-19 | Beta Pharma, Inc. | Treatment of EGFR mutant-related cancers using a combination of EGFR and CDK4/6 inhibitors |
| WO2021094379A1 (en) | 2019-11-12 | 2021-05-20 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| CA3166980A1 (en) | 2020-01-20 | 2021-07-29 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| US20210369709A1 (en) | 2020-05-27 | 2021-12-02 | Astrazeneca Ab | EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER |
| US20250136576A1 (en) * | 2021-07-13 | 2025-05-01 | ACEA Therapeutics, Inc. | Heterocyclic Compounds and Uses Thereof |
| CN119278041A (zh) | 2022-03-31 | 2025-01-07 | 阿斯利康(瑞典)有限公司 | 用于治疗癌症的与akt抑制剂组合的表皮生长因子受体（egfr）酪氨酸激酶抑制剂 |
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| WO2010059711A1 (en) * | 2008-11-18 | 2010-05-27 | Wisconsin Alumni Research Foundation | Sigma-1 receptor ligands and methods of use |
| JP5918693B2 (ja) | 2009-05-05 | 2016-05-18 | ダナ ファーバー キャンサー インスティテュート インコーポレイテッド | Ｅｇｆｒ阻害剤及び疾患の治療方法 |
| BR112013027734A2 (pt) * | 2011-05-04 | 2017-08-08 | Ariad Pharma Inc | compostos para a inibição de proliferação celular em cânceres impulsionados pelo egfr, método e composição farmacêutica |
| EP2736895B1 (en) * | 2011-07-27 | 2016-01-06 | Astrazeneca AB | 2-(2,4,5-substituted-anilino) pyrimidine derivatives as egfr modulators useful for treating cancer |
| AU2013204563B2 (en) * | 2012-05-05 | 2016-05-19 | Takeda Pharmaceutical Company Limited | Compounds for inhibiting cell proliferation in EGFR-driven cancers |
| CN104860941B (zh) | 2014-02-25 | 2017-03-22 | 上海海雁医药科技有限公司 | 2,4‑二取代苯‑1,5‑二胺衍生物及其应用以及由其制备的药物组合物和药用组合物 |
| PE20170268A1 (es) | 2014-06-19 | 2017-04-21 | Ariad Pharma Inc | Compuestos de heteroarilo para la inhibicion de cinasa |
| CN106458969A (zh) * | 2014-08-25 | 2017-02-22 | 四川海思科制药有限公司 | 一种(取代的苯基)(取代的嘧啶)胺基衍生物及其制备方法和药物用途 |
| CN105461695B (zh) * | 2014-09-29 | 2018-03-27 | 齐鲁制药有限公司 | 嘧啶或三嗪衍生物及其制备方法和用途 |
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| US10590111B2 (en) * | 2014-12-11 | 2020-03-17 | Beta Pharma, Inc. | Substituted 2-anilinopyrimidine derivatives as EGFR modulators |
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