WO2016023422A1 - 2-(2,4,5-取代苯胺)嘧啶衍生物、其药物组合物及其用途 - Google Patents

2-(2,4,5-取代苯胺)嘧啶衍生物、其药物组合物及其用途 Download PDF

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Publication number
WO2016023422A1
WO2016023422A1 PCT/CN2015/085714 CN2015085714W WO2016023422A1 WO 2016023422 A1 WO2016023422 A1 WO 2016023422A1 CN 2015085714 W CN2015085714 W CN 2015085714W WO 2016023422 A1 WO2016023422 A1 WO 2016023422A1
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methyl
cancer
amino
methoxy
substituted
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PCT/CN2015/085714
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English (en)
French (fr)
Chinese (zh)
Inventor
朱孝云
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Changzhou Runnor Biological Technology Co Ltd
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Changzhou Runnor Biological Technology Co Ltd
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Priority to JP2017527959A priority Critical patent/JP6418622B2/ja
Priority to EP15832588.6A priority patent/EP3181559B8/en
Priority to AU2015303641A priority patent/AU2015303641B2/en
Priority to CA2958095A priority patent/CA2958095C/en
Priority to US15/553,892 priority patent/US10414756B2/en
Priority to KR1020177007190A priority patent/KR101937704B1/ko
Publication of WO2016023422A1 publication Critical patent/WO2016023422A1/zh
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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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
    • 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
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • 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

Definitions

  • the detection data ( ⁇ M) in the embodiment of the present patent application is shown in the following table, and although the detection data is stated with a certain number of significant figures, the number indicating that the data has been determined to be an effective number should not be considered.
  • SD rats 24, half male and half female. Randomly divided into 4 groups, 6 in each group, half male and half

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • 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)
PCT/CN2015/085714 2014-08-15 2015-07-31 2-(2,4,5-取代苯胺)嘧啶衍生物、其药物组合物及其用途 Ceased WO2016023422A1 (zh)

Priority Applications (6)

Application Number Priority Date Filing Date Title
JP2017527959A JP6418622B2 (ja) 2014-08-15 2015-07-31 ２−（２，４，５−置換アニリン）ピリミジン誘導体、その薬物組成物及びその用途
EP15832588.6A EP3181559B8 (en) 2014-08-15 2015-07-31 2-(2,4,5-substituted aniline) pyrimidine derivative, pharmaceutical composition and use thereof
AU2015303641A AU2015303641B2 (en) 2014-08-15 2015-07-31 2-(2,4,5-substituted aniline) pyrimidine derivative, pharmaceutical composition and use thereof
CA2958095A CA2958095C (en) 2014-08-15 2015-07-31 2-(2,4,5-substituted aniline) pyrimidine derivative, pharmaceutical composition and use thereof
US15/553,892 US10414756B2 (en) 2014-08-15 2015-07-31 2-(2,4,5-substituted aniline) pyrimidine derivative, pharmaceutical composition and use thereof
KR1020177007190A KR101937704B1 (ko) 2014-08-15 2015-07-31 2-(2,4,5-치환 아닐린)피리미딘 유도체, 이의 약물 조성물 및 이의 용도

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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
CN201410401604.7 2014-08-15

Publications (1)

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WO2016023422A1 true WO2016023422A1 (zh) 2016-02-18

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PCT/CN2015/085714 Ceased WO2016023422A1 (zh) 2014-08-15 2015-07-31 2-(2,4,5-取代苯胺)嘧啶衍生物、其药物组合物及其用途

Country Status (8)

Country Link
US (1) US10414756B2 (https=)
EP (1) EP3181559B8 (https=)
JP (1) JP6418622B2 (https=)
KR (1) KR101937704B1 (https=)
CN (1) CN104140418B (https=)
AU (1) AU2015303641B2 (https=)
CA (1) CA2958095C (https=)
WO (1) WO2016023422A1 (https=)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9968606B2 (en) * 2015-12-27 2018-05-15 NeuForm Pharmaceuticals, Inc. Deuterated compounds for treating cancer and related diseases and conditions, and compositions and methods thereof
US10179784B2 (en) 2014-11-05 2019-01-15 Inventisbio Shanghai Ltd. Pyrimidine or pyridine compounds, preparation method therefor and pharmaceutical uses thereof
KR20190046875A (ko) * 2016-09-19 2019-05-07 난징 추앙트어 파마슈티컬 테크놀로지 컴퍼니 리미티드 중수소화 3-(4,5-치환 아미노피리미딘) 페닐 유도체 및 그의 응용
US10513509B2 (en) 2016-05-26 2019-12-24 Recurium Ip Holdings, Llc EGFR inhibitor compounds
CN110950847A (zh) * 2018-09-27 2020-04-03 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
JP2020521003A (ja) * 2017-05-24 2020-07-16 ティーワイケー メディシンズ インコーポレーテッドＴｙｋ Ｍｅｄｉｃｉｎｅｓ Ｉｎｃ． 重水素化ａｚｄ９２９１の結晶形、製造方法および使用

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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
WO2016054987A1 (zh) * 2014-10-11 2016-04-14 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
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
WO2017035753A1 (zh) * 2015-08-31 2017-03-09 无锡双良生物科技有限公司 2-芳胺基吡啶、嘧啶或三嗪衍生物及其制备方法和用途
CN106478605A (zh) * 2015-09-02 2017-03-08 上海页岩科技有限公司 嘧啶类化合物、其制备方法和医药用途
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
CN112645932B (zh) * 2016-03-22 2022-01-14 江苏豪森药业集团有限公司 Egfr抑制剂游离碱或其酸式盐的多晶型、其制备方法和应用
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
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
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
WO2022146201A1 (en) * 2020-12-30 2022-07-07 Joint Stock Company "Biocad" Epidermal growth factor receptor inhibitors
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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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
CN104140418A (zh) * 2014-08-15 2014-11-12 朱孝云 新的2-(2,4,5-取代苯胺)嘧啶衍生物及其用途

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KR20110048571A (ko) * 2008-09-03 2011-05-11 테바 파마슈티컬 인더스트리즈 리미티드 면역 기능을 지닌 ２―옥소―１,２―다이하이드로―퀴놀린 조절제
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

Patent Citations (2)

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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
CN104140418A (zh) * 2014-08-15 2014-11-12 朱孝云 新的2-(2,4,5-取代苯胺)嘧啶衍生物及其用途

Cited By (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10179784B2 (en) 2014-11-05 2019-01-15 Inventisbio Shanghai Ltd. Pyrimidine or pyridine compounds, preparation method therefor and pharmaceutical uses thereof
US11498921B1 (en) 2014-11-05 2022-11-15 InventisBio Co., Ltd. Pyrimidine or pyridine compounds, preparation method therefor and pharmaceutical uses thereof
US11203589B2 (en) 2014-11-05 2021-12-21 InventisBio Co., Ltd. Pyrimidine or pyridine compounds, preparation method therefor and pharmaceutical uses thereof
US9968606B2 (en) * 2015-12-27 2018-05-15 NeuForm Pharmaceuticals, Inc. Deuterated compounds for treating cancer and related diseases and conditions, and compositions and methods thereof
US11098030B2 (en) 2016-05-26 2021-08-24 Recurium Ip Holdings, Llc EGFR inhibitor compounds
US12049460B2 (en) 2016-05-26 2024-07-30 Recurium Ip Holdings, Llc EGFR inhibitor compounds
US10513509B2 (en) 2016-05-26 2019-12-24 Recurium Ip Holdings, Llc EGFR inhibitor compounds
EP3498708A4 (en) * 2016-09-19 2019-08-21 Nanjing Chuangte Pharmaceutical Technology Co., Ltd DEUTERATED 3- (4,5-SUBSTITUTED PYRIMIDINAMINE) PHENYL DERIVATIVES AND APPLICATIONS THEREOF
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
JP2019529551A (ja) * 2016-09-19 2019-10-17 南京創特医薬科技有限公司Ｎａｎｊｉｎｇ Ｃｈｕａｎｇｔｅ Ｐｈａｒｍａｃｅｕｔｉｃａｌ Ｔｅｃｈｎｏｌｏｇｙ Ｃｏ．， Ｌｔｄ 重水素化３−（４，５−置換アミノピリミジン）フェニル誘導体及びその使用
KR20190046875A (ko) * 2016-09-19 2019-05-07 난징 추앙트어 파마슈티컬 테크놀로지 컴퍼니 리미티드 중수소화 3-(4,5-치환 아미노피리미딘) 페닐 유도체 및 그의 응용
JP2020521003A (ja) * 2017-05-24 2020-07-16 ティーワイケー メディシンズ インコーポレーテッドＴｙｋ Ｍｅｄｉｃｉｎｅｓ Ｉｎｃ． 重水素化ａｚｄ９２９１の結晶形、製造方法および使用
CN110950847A (zh) * 2018-09-27 2020-04-03 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
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

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Publication number Publication date
JP2017523247A (ja) 2017-08-17
KR101937704B1 (ko) 2019-01-14
EP3181559B8 (en) 2018-11-14
CN104140418B (zh) 2016-08-24
EP3181559A4 (en) 2017-06-21
CA2958095C (en) 2023-09-26
JP6418622B2 (ja) 2018-11-07
AU2015303641B2 (en) 2018-04-12
KR20170036107A (ko) 2017-03-31
CN104140418A (zh) 2014-11-12
US10414756B2 (en) 2019-09-17
EP3181559B1 (en) 2018-10-03
US20180016258A1 (en) 2018-01-18
CA2958095A1 (en) 2016-02-18
AU2015303641A1 (en) 2017-03-23
EP3181559A1 (en) 2017-06-21

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