CA2958095C - 2-(2,4,5-substituted aniline) pyrimidine derivative, pharmaceutical composition and use thereof - Google Patents
2-(2,4,5-substituted aniline) pyrimidine derivative, pharmaceutical composition and use thereof Download PDFInfo
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- CA2958095C CA2958095C CA2958095A CA2958095A CA2958095C CA 2958095 C CA2958095 C CA 2958095C CA 2958095 A CA2958095 A CA 2958095A CA 2958095 A CA2958095 A CA 2958095A CA 2958095 C CA2958095 C CA 2958095C
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- cancer
- methyl
- amino
- methoxy
- methy
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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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- 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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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/33—Heterocyclic compounds
- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
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- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410401604.7 | 2014-08-15 | ||
| CN201410401604.7A CN104140418B (zh) | 2014-08-15 | 2014-08-15 | 2-(2，4，5-取代苯胺)嘧啶衍生物及其用途 |
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| CN104140418B (zh) * | 2014-08-15 | 2016-08-24 | 常州润诺生物科技有限公司 | 2-(2，4，5-取代苯胺)嘧啶衍生物及其用途 |
| CN105237515B (zh) * | 2014-10-10 | 2018-06-05 | 益方生物科技（上海）有限公司 | 氘代嘧啶类化合物、其制备方法、药物组合物和用途 |
| ES2886887T3 (es) * | 2014-10-11 | 2021-12-21 | Shanghai Hansoh Biomedical Co Ltd | Inhibidor de EGFR y preparación y aplicación del mismo |
| CN111170998B (zh) * | 2014-11-05 | 2023-04-11 | 益方生物科技(上海)股份有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| CN105712998B (zh) * | 2014-12-05 | 2019-12-13 | 上海润诺生物科技有限公司 | 氮杂吲哚类衍生物、其制备方法及其在医药上的应用 |
| CN105001208A (zh) * | 2015-08-06 | 2015-10-28 | 南京雷科星生物技术有限公司 | 一种表皮生长因子受体egfr抑制剂及其制备方法与用途 |
| CN105153122B (zh) * | 2015-08-27 | 2018-07-20 | 上海圣考医药科技有限公司 | [(吲哚-3-基)嘧啶-2-基]氨基苯基丙-2-烯酰胺衍生物及盐、制备方法、应用 |
| KR102051609B1 (ko) * | 2015-08-31 | 2019-12-03 | 우시 상량 바이오테크놀로지 씨오., 엘티디. | 2-아릴아미노피리딘, 피리미딘 또는 트리아진 유도체 및 그 제조방법과 사용 |
| CN110483485A (zh) * | 2015-09-02 | 2019-11-22 | 益方生物科技（上海）有限公司 | 嘧啶类化合物、其制备方法和医药用途 |
| CN108779102B (zh) * | 2015-12-27 | 2020-04-21 | 纽弗姆制药有限公司 | 用于治疗癌症及相关疾病和病况的氘代化合物及其组合物和方法 |
| CN108610331A (zh) * | 2016-01-22 | 2018-10-02 | 焦玉奇 | 2-(2,4,5-取代苯胺)嘧啶衍生物 |
| CN107043369A (zh) * | 2016-02-06 | 2017-08-15 | 焦玉奇 | 2‑(2,4,5‑取代苯胺)嘧啶衍生物 |
| CA3016092C (en) * | 2016-03-22 | 2025-03-11 | Jiangsu Hansoh Pharmaceutical Group Co Ltd | POLYCRYSTALLINE FORM OF FREE BASIC OR SALT EGFR INHIBITOR ACID, PROCESS FOR ITS PREPARATION AND APPLICATION |
| US10513509B2 (en) | 2016-05-26 | 2019-12-24 | Recurium Ip Holdings, Llc | EGFR inhibitor compounds |
| KR102245280B1 (ko) * | 2016-09-19 | 2021-04-27 | 난징 추앙트어 파마슈티컬 테크놀로지 컴퍼니 리미티드 | 중수소화 3-(4,5-치환 아미노피리미딘) 페닐 유도체 및 그의 응용 |
| CN108129342A (zh) * | 2016-11-30 | 2018-06-08 | 浙江九洲药物科技有限公司 | 一种奥希替尼中间体及其制备方法 |
| CN108047205B (zh) * | 2016-12-14 | 2019-08-27 | 河南真实生物科技有限公司 | 2-(2，4，5-取代苯氨基)嘧啶衍生物、其制备方法及其在制备抗肿瘤药物中的应用 |
| CN106957304B (zh) * | 2017-04-25 | 2017-12-01 | 孔令廷 | 一种石墨烯负载FeCl3催化剂的制备方法及其在制备抗癌药物中间体的用途 |
| CN107192773B (zh) * | 2017-05-17 | 2019-09-27 | 张家港威胜生物医药有限公司 | 一种检测奥希替尼含量和有关物质的高效液相法 |
| CN108929311B (zh) * | 2017-05-22 | 2020-07-28 | 焦玉奇 | 2-(2,4,5-取代苯胺)嘧啶衍生物 |
| ES2956943T3 (es) * | 2017-05-24 | 2024-01-05 | Tyk Medicines Inc | Forma cristalina de AZD9291 deuterado, procedimiento de preparación para la misma y uso de la misma |
| WO2019001425A1 (zh) * | 2017-06-27 | 2019-01-03 | 浙江同源康医药股份有限公司 | 一种氘代奥斯替尼衍生物及其应用 |
| TWI702205B (zh) * | 2017-10-06 | 2020-08-21 | 俄羅斯聯邦商拜奧卡德聯合股份公司 | 表皮生長因子受體抑制劑 |
| CN107954918B (zh) * | 2017-11-30 | 2022-01-25 | 郑州泰基鸿诺医药股份有限公司 | 一种n-氘代甲基吲哚类化合物的合成方法 |
| CN108047207A (zh) * | 2018-01-30 | 2018-05-18 | 天津大学 | N-[5-(嘧啶-2-氨基)-2,4-二取代苯基]-2-氟代丙烯酰胺氘代物及应用 |
| CN110272420A (zh) * | 2018-03-16 | 2019-09-24 | 江苏正大丰海制药有限公司 | 氘代3-(4,5-取代氨基嘧啶)苯基化合物单甲磺酸盐晶型及其制备方法 |
| CN110950847B (zh) * | 2018-09-27 | 2022-11-01 | 浙江同源康医药股份有限公司 | 氘代azd9291化合物的新晶型及其用途 |
| CN110003183A (zh) * | 2019-04-09 | 2019-07-12 | 河南真实生物科技有限公司 | 2-（2，4，5-取代苯氨基）嘧啶衍生物及其晶形b |
| CN111909135A (zh) * | 2020-08-15 | 2020-11-10 | 天津大学 | 一种azd9291氘代物甲磺酸盐新盐型及其制备方法 |
| TW202241890A (zh) * | 2020-12-30 | 2022-11-01 | 俄羅斯聯邦商拜奧卡德聯合股份公司 | 表皮生長因子受體之抑制劑 |
| CN113387935B (zh) * | 2021-07-23 | 2022-06-10 | 苏州雅深智慧科技有限公司 | 抑制三突变表皮生长因子受体酪氨酸激酶的化合物及用途 |
| CN113582976B (zh) * | 2021-08-24 | 2023-03-17 | 郑州大学 | 氘代2-取代苯胺-4-吲哚基嘧啶类衍生物及其制备方法和应用 |
| WO2025092926A1 (zh) * | 2023-10-31 | 2025-05-08 | 浙江同源康医药股份有限公司 | 一种嘧啶类衍生物的药物组合物 |
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| AU2009288108B2 (en) | 2008-09-03 | 2013-10-17 | Teva Pharmaceutical Industries, Ltd. | 2-oxo-1,2-dihydro-quinoline modulators of immune function |
| CN101676266B (zh) * | 2008-09-19 | 2011-10-26 | 苏州泽璟生物制药有限公司 | 氘代的ω-二苯基脲及衍生物以及包含该化合物的药物组合物 |
| EP3333161B1 (en) * | 2011-07-27 | 2020-02-19 | Astrazeneca AB | 2-(2,4,5-substituted-anilino)pyrimidine derivatives as egfr modulators useful for treating cancer |
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| WO2016023422A1 (zh) | 2016-02-18 |
| CA2958095A1 (en) | 2016-02-18 |
| KR101937704B1 (ko) | 2019-01-14 |
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