CN111170998B - 嘧啶或吡啶类化合物、其制备方法和医药用途 - Google Patents

嘧啶或吡啶类化合物、其制备方法和医药用途 Download PDF

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CN111170998B
CN111170998B CN201910180890.1A CN201910180890A CN111170998B CN 111170998 B CN111170998 B CN 111170998B CN 201910180890 A CN201910180890 A CN 201910180890A CN 111170998 B CN111170998 B CN 111170998B
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CN111170998A (zh
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江岳恒
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Yifang Biotechnology Shanghai Co ltd
Betta Pharmaceuticals Co Ltd
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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
    • C07D403/02—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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

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  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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CN201510152615.0A CN105085489B (zh) 2014-11-05 2015-04-01 嘧啶或吡啶类化合物、其制备方法和医药用途

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CN201580060134.5A Expired - Fee Related CN107548391B (zh) 2014-11-05 2015-11-05 嘧啶或吡啶类化合物、其制备方法和医药用途

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CN202211200422.4A Active CN115403565B (zh) 2014-11-05 2015-11-05 嘧啶或吡啶类化合物、其制备方法和医药用途
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EP (2) EP3216786B1 (https=)
JP (1) JP6637058B2 (https=)
KR (1) KR102560052B1 (https=)
CN (5) CN111170998B (https=)
CA (1) CA2966376C (https=)
ES (1) ES2881622T3 (https=)
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Families Citing this family (93)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015188777A1 (en) * 2014-06-12 2015-12-17 Shanghai Fochon Pharmaceutical Co Ltd Certain protein kinase inhibitors
WO2016029839A1 (zh) * 2014-08-25 2016-03-03 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
CN117069700B (zh) * 2014-10-11 2026-01-30 上海翰森生物医药科技有限公司 Egfr抑制剂及其制备和应用
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
CN108024993B (zh) * 2014-12-11 2020-11-06 贝达医药公司 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂
CN113563332B (zh) 2014-12-23 2024-12-17 达纳－法伯癌症研究所公司 作为egfr抑制剂的新的嘧啶和治疗病症的方法
JP6970081B2 (ja) * 2015-07-16 2021-11-24 正大天晴▲藥▼▲業▼集▲団▼股▲フン▼有限公司 アニリンピリミジン誘導体及びその使用
US10377747B2 (en) 2015-08-31 2019-08-13 Wuxi Shuangliang Biotechnology Co., Ltd. 2-arylamino pyridine, pyrimidine or triazine derivatives, preparation method and use thereof
CN106117185B (zh) * 2015-08-31 2017-11-07 广州必贝特医药技术有限公司 2,4‑二含氮基团取代嘧啶类化合物及其制备方法和应用
CN106749193B (zh) * 2015-11-23 2020-11-20 南京圣和药业股份有限公司 吲唑取代的表皮生长因子受体抑制剂及其应用
CN113912648A (zh) * 2015-12-02 2022-01-11 深圳市塔吉瑞生物医药有限公司 一种二氨基嘧啶化合物及包含该化合物的组合物
KR102029135B1 (ko) * 2015-12-27 2019-10-07 뉴폼 파마슈티컬스, 아이엔씨. 암 및 관련 질병 및 상태 치료용 중수소화된 화합물, 그의 조성물 및 방법
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
EP3399968B8 (en) * 2016-01-07 2021-12-01 Xuanzhu Biopharmaceutical Co., Ltd. Selective inhibitors of clinically important mutants of the egfr tyrosine kinase
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
CN107188888A (zh) * 2016-03-15 2017-09-22 罗欣生物科技（上海）有限公司 一种制备甲磺酸迈瑞替尼的方法
CN106279160B (zh) * 2016-03-18 2017-09-26 海南越康生物医药有限公司 N‑苯基‑2‑氨基嘧啶类化合物制备方法和用途
CN105884687B (zh) * 2016-04-14 2018-06-22 梯尔希（南京）药物研发有限公司 一种5-苄基苄达明的制备方法
EP3454860B1 (en) * 2016-05-11 2025-09-17 Beta Pharma, Inc. 2-anilinopyrimidine derivatives as therapeutic agents for treatment of brain cancers
AU2017269335B2 (en) 2016-05-26 2021-07-01 Recurium Ip Holdings, Llc EGFR inhibitor compounds
BR112018075823A2 (pt) * 2016-06-17 2019-03-26 Beta Pharma, Inc. sais farmacêuticos de n-(2-(2-(dimetilamino)etoxi)-4-metoxi-5-((4-(1-metil-1h-indol-3-il)pirimidin-2-il)amino)fenil)acrilamida e suas formas cristalinas
CN107540661A (zh) * 2016-06-24 2018-01-05 正大天晴药业集团股份有限公司 作为egfr抑制剂的苯胺嘧啶化合物的结晶
JP6740452B2 (ja) * 2016-07-26 2020-08-12 深▲セン▼市塔吉瑞生物医▲薬▼有限公司Ｓｈｅｎｚｈｅｎ ＴａｒｇｅｔＲｘ，Ｉｎｃ． プロテインチロシンキナーゼの活性を阻害するためのアミノピリミジン系化合物
CN107840846B (zh) * 2016-09-19 2020-11-24 郑州泰基鸿诺医药股份有限公司 一种含嘧啶环的化合物、egfr抑制剂及其应用
CN107973783B (zh) * 2016-10-21 2024-09-06 正大天晴药业集团股份有限公司 作为erk抑制剂的苯胺嘧啶衍生物
CN107973782B (zh) * 2016-10-21 2021-11-02 正大天晴药业集团股份有限公司 一种三氟乙基取代吲哚的苯胺嘧啶化合物及其盐的结晶
CN108057036B (zh) * 2016-11-07 2023-06-13 正大天晴药业集团股份有限公司 一种egfr抑制剂的固体药物组合物
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
US11352352B2 (en) * 2017-06-13 2022-06-07 Beijing Adamadle Biotechnology Limited Liability Company Aminopyrimidine compound, preparation method therefor and use thereof
CN110799191B (zh) * 2017-06-16 2023-05-26 贝塔制药有限公司 N-(2-(2-(二甲氨基)乙氧基)-4-甲氧基-5-((4-(1-甲基-1h-吲哚-3-基)嘧啶-2-基)氨基)苯基)丙烯酰胺及其盐的药物制剂
CN107266437B (zh) * 2017-07-19 2019-08-30 海南越康生物医药有限公司 N-苯基-2-氨基嘧啶类化合物的晶型、盐型及其制备方法
CN107721991B (zh) * 2017-11-17 2019-10-18 南方医科大学中西医结合医院 一种6-(嘧啶-4-基)-1h-吲唑衍生物及其制备方法和应用
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
SG11202005468YA (en) 2017-12-20 2020-07-29 Basf Se Process for the generation of metal-containing films
CN108558832B (zh) * 2018-01-17 2021-04-30 浙江树人学院 一种新型抗肿瘤药物奥希替尼衍生物及其制备方法
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
CN112119074A (zh) * 2018-05-15 2020-12-22 益方生物科技（上海）有限公司 Egfr抑制剂
CN108675993A (zh) * 2018-06-14 2018-10-19 纽瑞森生物科技（北京）有限公司 氘代嘧啶类化合物、制备方法、药物组合物、制剂和用途
PL3806898T3 (pl) * 2018-06-18 2026-02-23 UCB Biopharma SRL Antagonista gremlin-1 do zastosowania w leczeniu nowotworu
CN110698461B (zh) * 2018-07-09 2024-04-05 上海翰森生物医药科技有限公司 第三代egfr抑制剂的制备方法
KR101954370B1 (ko) 2018-07-25 2019-03-05 한미약품 주식회사 피리미딘 화합물 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물
US10376512B1 (en) 2018-08-09 2019-08-13 Chia Tai Tianqing Pharmaeutical Group Co., Ltd. Crystal of aniline pyrimidine compound of trifluoroethyl substituted indole and salt thereof
CN113166110B (zh) * 2018-12-12 2023-08-11 暨南大学 2-氨基嘧啶类化合物及其应用
CN111410667B (zh) * 2019-01-08 2024-11-22 武汉宇科源医药生物科技有限公司 新型(1,2,4)三唑并(1,5-a)吡啶基磷氧化物及其用途
PH12021551985A1 (en) 2019-02-22 2022-08-22 Hanmi Pharmaceutical Co Ltd Pharmaceutical composition comprising flt3 inhibitor and hypomethylating agent for treating acute myeloid leukemia
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
CN111747950B (zh) * 2019-03-29 2024-01-23 深圳福沃药业有限公司 用于治疗癌症的嘧啶衍生物
CN110016017A (zh) * 2019-05-16 2019-07-16 益方生物科技（上海）有限公司 一类嘧啶化合物的盐、多晶型物及其药物组合物、制备方法和应用
WO2020245208A1 (en) 2019-06-04 2020-12-10 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of cd9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis
AU2020296620B2 (en) * 2019-06-20 2023-07-13 Oncobix Co.Ltd. Pyrimidine derivative inhibiting growth of cancer cell and medicinal use thereof
CN110229143A (zh) * 2019-06-21 2019-09-13 益方生物科技（上海）有限公司 一类嘧啶化合物的盐、多晶型物及其药物组合物、制备方法和应用
EA202290154A1 (ru) 2019-06-27 2022-03-29 Ханми Фарм. Ко., Лтд. Фармацевтическая композиция для лечения острого миелоидного лейкоза, содержащая ингибитор flt3 и химиотерапевтические агенты
JP2022549272A (ja) * 2019-09-23 2022-11-24 ベータ・ファーマ・インコーポレイテッド Ｅｇｆｒ阻害剤とｃｄｋ４／６阻害剤の組み合わせを用いたｅｇｆｒ変異に関連する癌の治療
WO2021066443A1 (ko) * 2019-09-30 2021-04-08 한미약품 주식회사 Flt3 저해제 및 mdm2 저해제를 포함하는 급성 골수성 백혈병 치료용 약학적 조성물
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
US20210161897A1 (en) 2019-11-12 2021-06-03 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
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
CN110898026A (zh) * 2019-12-11 2020-03-24 倍而达药业（苏州）有限公司 包含bpi-7711的药用组合物及其制备方法
CN111100117B (zh) * 2019-12-18 2021-02-19 上海倍而达药业有限公司 氨基嘧啶类化合物甲磺酸盐的晶型a及其制备方法和应用
CN111057073A (zh) * 2019-12-26 2020-04-24 浙江工业大学 一种4-吲哚-2-芳胺基嘧啶化合物及其在炎症治疗中的应用
JP2023510426A (ja) 2020-01-20 2023-03-13 アストラゼネカ・アクチエボラーグ 癌を治療するための上皮細胞増殖因子受容体チロシンキナーゼ阻害剤
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN113354622B (zh) * 2020-03-06 2022-11-01 沈阳药科大学 对苯二胺类lsd1抑制剂及其制备方法
CN115175902B (zh) * 2020-03-13 2024-07-26 郑州同源康医药有限公司 一类用作激酶抑制剂的化合物及其应用
CN113493419A (zh) * 2020-03-18 2021-10-12 南京药石科技股份有限公司 Egfr酪氨酸激酶抑制剂及其用途
US20210369709A1 (en) 2020-05-27 2021-12-02 Astrazeneca Ab EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER
WO2021243596A1 (en) * 2020-06-03 2021-12-09 InventisBio Co., Ltd. Aminopyrimidine compounds, preparation methods and uses thereof
TW202220976A (zh) * 2020-09-08 2022-06-01 大陸商貝達藥業股份有限公司 Cd73抑制劑及其在醫藥上的應用
CN112079728B (zh) * 2020-09-17 2022-08-19 苏州昊帆生物股份有限公司 氘代n,n,n’-三甲基乙二胺类化合物及其制备方法
CN112174870B (zh) * 2020-10-12 2023-07-21 蔡霈 (r)-1-烷烃酰基-2-取代吡咯烷-2-甲酰胺的制备方法及其药用用途
CN112451527B (zh) * 2020-12-02 2022-08-16 北京鞍石生物科技有限责任公司 氨基嘧啶类化合物的用途
JP7628729B2 (ja) * 2020-12-02 2025-02-12 上海和誉生物医薬科技有限公司 ２，３－ジヒドロ－１Ｈ－ピロロ［３，２－ｂ］ピリジン誘導体、その製造方法および使用
CN115073426A (zh) * 2021-03-16 2022-09-20 上海科州药物研发有限公司 嘧啶杂环化合物及其制备方法和应用
CN117561254A (zh) * 2021-04-30 2024-02-13 苏州浦合医药科技有限公司 用于肺癌治疗的嘧啶基氨基苯
CN116670126A (zh) * 2021-05-13 2023-08-29 上海和誉生物医药科技有限公司 具有egfr抑制活性的氮杂芳基衍生物、其制备方法和应用
WO2023287783A1 (en) * 2021-07-13 2023-01-19 ACEA Therapeutics, Inc. Heterocyclic compounds and uses thereof
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
WO2023011415A1 (zh) * 2021-08-02 2023-02-09 贝达药业股份有限公司 Egfr抑制剂的药物组合及其应用
MX2024000261A (es) * 2021-08-06 2024-03-14 Abbisko Therapeutics Co Ltd Derivado de pirimidina o piridina, metodo de preparacion del mismo y aplicacion del mismo en la industria farmaceutica.
KR20240055046A (ko) * 2021-09-02 2024-04-26 신톤 비.브이. 오시머티닙을 제조하는 방법
CN117137919A (zh) * 2021-09-16 2023-12-01 中国人民解放军军事科学院军事医学研究院 一种氨基嘧啶衍生物及其作为egfr酪氨酸激酶抑制剂的应用
IL315848A (en) 2022-03-31 2024-11-01 Astrazeneca Ab Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in combination with an AKT inhibitor for cancer treatment
EP4543920A1 (en) 2022-06-27 2025-04-30 Astrazeneca AB Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
WO2024008048A1 (zh) * 2022-07-04 2024-01-11 杭州德睿智药科技有限公司 新型嘧啶或三嗪取代吡啶并杂环化合物
CN119654152A (zh) 2022-07-08 2025-03-18 阿斯利康(瑞典)有限公司 与hgf-受体抑制剂组合用于治疗癌症的表皮生长因子受体酪氨酸激酶抑制剂
CN117430600A (zh) * 2022-07-20 2024-01-23 上海和誉生物医药科技有限公司 一种选择性egfr抑制剂及其制备方法和在药学上的应用
WO2024094064A1 (en) * 2022-11-02 2024-05-10 Suzhou Puhe Biopharma Co., Ltd Pyrimidinylaminobenzenes for treating lung cancer with distant metastasis
CN115925687B (zh) * 2022-12-29 2024-04-02 广东省人民医院 靶向egfr的化合物、pet分子探针及其制备方法与应用
CN117623937A (zh) * 2023-10-20 2024-03-01 金凯(辽宁)生命科技股份有限公司 一种n,n,n'-三甲基乙二胺的制备方法
WO2026009146A1 (en) 2024-07-01 2026-01-08 Hetero Labs Limited Benzimidazole compounds as egfr inhibitors
WO2026047630A1 (en) 2024-08-31 2026-03-05 Hetero Labs Limited Heterocyclic compounds as egfr inhibitors
WO2026053183A1 (en) 2024-09-09 2026-03-12 Hetero Labs Limited Benzothiazole and benzoxazole compounds as egfr inhibitors

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011140338A1 (en) * 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
CN103702990A (zh) * 2011-07-27 2014-04-02 阿斯利康(瑞典)有限公司 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症

Family Cites Families (46)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1257546A1 (en) * 2000-02-17 2002-11-20 Amgen Inc. Kinase inhibitors
ES2364495T3 (es) 2005-02-03 2011-09-05 The General Hospital Corporation Método para tratar cáncer resistente a gefitinib.
EA200900573A1 (ru) * 2006-10-20 2009-10-30 АйАрЭм ЭлЭлСи Композиции и способы для модуляции рецепторов c-kit и pdgfr
WO2008058037A1 (en) * 2006-11-03 2008-05-15 Irm Llc Compounds and compositions as protein kinase inhibitors
EP2103620A1 (en) * 2006-12-12 2009-09-23 Takeda Pharmaceutical Company Limited Fused heterocyclic compound
JP2010514688A (ja) * 2006-12-22 2010-05-06 ノバルティス アーゲー インドール−４−イルピリミジニル−２−イル−アミン誘導体およびサイクリン依存性キナーゼ阻害剤としてのその使用
CA2672518A1 (en) 2006-12-22 2008-07-03 Novartis Ag Organic compounds and their uses
CN105367503A (zh) * 2007-10-19 2016-03-02 阿维拉制药公司 杂芳基化合物和其用途
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
US9155422B1 (en) * 2008-09-24 2015-10-13 Susan M. Wohld Turkey flipper and method for making and using
CN101723936B (zh) * 2008-10-27 2014-01-15 上海睿星基因技术有限公司 激酶抑制剂及其在药学中的用途
EP4585589A3 (en) * 2008-12-03 2025-11-19 The Scripps Research Institute Stem cell cultures
KR101705158B1 (ko) * 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
PL2470173T3 (pl) * 2009-08-25 2016-11-30 Leczenie skojarzone nanocząstkowymi kompozycjami taksanu i inhibitorów hedgehog
US8916577B2 (en) 2011-01-26 2014-12-23 Nerviano Medical Sciences S.R.L. Tricyclic derivatives, process for their preparation and their use as kinase inhibitors
WO2012126181A1 (en) * 2011-03-24 2012-09-27 Ying Luo Use of kinase inhibitors in preventing and treating inflammatory disorder
US9834518B2 (en) * 2011-05-04 2017-12-05 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in EGFR-driven cancers
CN102363618A (zh) 2011-07-04 2012-02-29 华东理工大学 一种表皮生长因子受体的新型抑制剂及其应用
KR20140059246A (ko) * 2011-09-22 2014-05-15 화이자 인코포레이티드 피롤로피리미딘 및 퓨린 유도체
PL2805940T3 (pl) 2012-01-17 2017-06-30 Astellas Pharma Inc. Związek pirazynokarboksyamidowy
CN103360407B (zh) 2012-04-10 2016-06-22 上海希迈医药科技有限公司 一种噻吩并嘧啶类衍生物、其制备方法及其在医药上的应用
CN103374000B (zh) 2012-04-13 2015-11-11 中国科学院广州生物医药与健康研究院 嘧啶并二氮杂卓类化合物及其药用组合物和应用
CN104520291A (zh) 2012-06-06 2015-04-15 Irm责任有限公司 用于调节egfr活性的化合物和组合物
EP2909194A1 (en) * 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
RU2015118647A (ru) * 2012-11-20 2017-01-10 Дженентек, Инк. Аминопиримидиновые соединения в качестве ингибиторов содержащих т790м мутантных egfr
US9695228B2 (en) 2012-11-21 2017-07-04 Janssen Biotech, Inc. EGFR and c-Met fibronectin type III domain binding molecules
CN104761544B (zh) 2014-01-03 2019-03-15 北京轩义医药科技有限公司 Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂
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
CN103804303B (zh) 2014-03-13 2015-04-08 山东理工大学 Egfr小分子抑制剂嘧啶衍生物及其制备方法与用途
EP3143015B1 (en) 2014-05-13 2019-02-20 ARIAD Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
WO2015188777A1 (en) 2014-06-12 2015-12-17 Shanghai Fochon Pharmaceutical Co Ltd Certain protein kinase inhibitors
CN110526912B (zh) 2014-06-19 2023-02-14 武田药品工业株式会社 用于激酶抑制的杂芳基化合物
CN105254615B (zh) 2014-07-11 2017-02-22 杭州华东医药集团新药研究院有限公司 苯胺嘧啶衍生物及其在制备抗恶性肿瘤药物中的用途
CN105315285B (zh) 2014-07-25 2017-12-08 上海海雁医药科技有限公司 2,4‑二取代7H‑吡咯并[2,3‑d]嘧啶衍生物、其制法与医药上的用途
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
WO2016029839A1 (zh) * 2014-08-25 2016-03-03 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
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
CN117069700B (zh) * 2014-10-11 2026-01-30 上海翰森生物医药科技有限公司 Egfr抑制剂及其制备和应用
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
CN108024993B (zh) * 2014-12-11 2020-11-06 贝达医药公司 取代的2-苯胺基嘧啶衍生物及其作为表皮生长因子受体调节剂
CN113563332B (zh) 2014-12-23 2024-12-17 达纳－法伯癌症研究所公司 作为egfr抑制剂的新的嘧啶和治疗病症的方法
JP6970081B2 (ja) 2015-07-16 2021-11-24 正大天晴▲藥▼▲業▼集▲団▼股▲フン▼有限公司 アニリンピリミジン誘導体及びその使用
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
CN107540661A (zh) 2016-06-24 2018-01-05 正大天晴药业集团股份有限公司 作为egfr抑制剂的苯胺嘧啶化合物的结晶

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011140338A1 (en) * 2010-05-05 2011-11-10 Gatekeeper Pharmaceuticals, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
CN103702990A (zh) * 2011-07-27 2014-04-02 阿斯利康(瑞典)有限公司 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Discovery of a Potent and Selective EGFR Inhibitor (AZD9291) of Both Sensitizing and T790M Resistance Mutations That Spares the Wild Type Form of the Receptor;M. Raymond V. Finlay et al.;《Journal of Medicinal Chemistry》;20141001;第57卷;第8249-8267页 *

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