JP2019501222A - Ｅｇｆｒチロシンキナーゼの臨床的に重要な変異体の選択的阻害薬 - Google Patents

Ｅｇｆｒチロシンキナーゼの臨床的に重要な変異体の選択的阻害薬 Download PDF

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JP2019501222A
JP2019501222A JP2018554640A JP2018554640A JP2019501222A JP 2019501222 A JP2019501222 A JP 2019501222A JP 2018554640 A JP2018554640 A JP 2018554640A JP 2018554640 A JP2018554640 A JP 2018554640A JP 2019501222 A JP2019501222 A JP 2019501222A
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ユンタオ ソン，
ユンタオ ソン，
アレクサンダー ジェイムズ ブリッジス，
アレクサンダー ジェイムズ ブリッジス，
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シーエス ファーマテック リミテッド
シーエス ファーマテック リミテッド
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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
    • C07D401/02—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
    • 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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/136—Amines having aromatic rings, e.g. ketamine, nortriptyline having the amino group directly attached to the aromatic ring, e.g. benzeneamine
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D403/02—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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08F—MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
    • C08F20/00—Homopolymers and copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical or a salt, anhydride, ester, amide, imide or nitrile thereof
    • C08F20/02—Monocarboxylic acids having less than ten carbon atoms, Derivatives thereof
    • C08F20/52—Amides or imides
    • C08F20/54—Amides, e.g. N,N-dimethylacrylamide or N-isopropylacrylamide
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08F—MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
    • C08F20/00—Homopolymers and copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical or a salt, anhydride, ester, amide, imide or nitrile thereof
    • C08F20/02—Monocarboxylic acids having less than ten carbon atoms, Derivatives thereof
    • C08F20/52—Amides or imides
    • C08F20/54—Amides, e.g. N,N-dimethylacrylamide or N-isopropylacrylamide
    • C08F20/58—Amides, e.g. N,N-dimethylacrylamide or N-isopropylacrylamide containing oxygen in addition to the carbonamido oxygen, e.g. N-methylolacrylamide, N-acryloylmorpholine
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08F—MACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
    • C08F20/00—Homopolymers and copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical or a salt, anhydride, ester, amide, imide or nitrile thereof
    • C08F20/02—Monocarboxylic acids having less than ten carbon atoms, Derivatives thereof
    • C08F20/52—Amides or imides
    • C08F20/54—Amides, e.g. N,N-dimethylacrylamide or N-isopropylacrylamide
    • C08F20/60—Amides, e.g. N,N-dimethylacrylamide or N-isopropylacrylamide containing nitrogen in addition to the carbonamido nitrogen

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Polymers & Plastics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2018554640A 2016-01-07 2017-01-06 Ｅｇｆｒチロシンキナーゼの臨床的に重要な変異体の選択的阻害薬 Withdrawn JP2019501222A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662276221P 2016-01-07 2016-01-07
US62/276,221 2016-01-07
US201662399730P 2016-09-26 2016-09-26
US62/399,730 2016-09-26
PCT/US2017/012466 WO2017120429A1 (en) 2016-01-07 2017-01-06 Selective inhibitors of clinically important mutants of the egfr tyrosine kinase

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JP2021029700A Division JP2021091703A (ja) 2016-01-07 2021-02-26 Ｅｇｆｒチロシンキナーゼの臨床的に重要な変異体の選択的阻害薬

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JP2019501222A true JP2019501222A (ja) 2019-01-17
JP2019501222A5 JP2019501222A5 (OSRAM) 2020-01-23

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JP2021029700A Ceased JP2021091703A (ja) 2016-01-07 2021-02-26 Ｅｇｆｒチロシンキナーゼの臨床的に重要な変異体の選択的阻害薬

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US (1) US10435388B2 (OSRAM)
EP (1) EP3399968B8 (OSRAM)
JP (2) JP2019501222A (OSRAM)
KR (1) KR20180105161A (OSRAM)
CN (1) CN109328059B (OSRAM)
TW (1) TWI726968B (OSRAM)
WO (1) WO2017120429A1 (OSRAM)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022533473A (ja) * 2019-07-26 2022-07-22 メッドシャイン ディスカバリー インコーポレイテッド Ｅｇｆｒ及びｅｒｂｂ２に作用するピリミジン系化合物
JP2023545571A (ja) * 2020-12-02 2023-10-30 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
JP2024524262A (ja) * 2021-08-06 2024-07-05 上海和誉生物医薬科技有限公司 ピリミジンまたはピリジン誘導体およびその製造方法ならびに薬学上の応用

Families Citing this family (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JP2019501222A (ja) 2016-01-07 2019-01-17 シーエス ファーマテック リミテッド Ｅｇｆｒチロシンキナーゼの臨床的に重要な変異体の選択的阻害薬
EP3464275B1 (en) 2016-05-26 2024-05-08 Recurium IP Holdings, LLC Egfr inhibitor compounds
EP3492462B1 (en) * 2016-07-26 2023-08-30 Shenzhen TargetRx, Inc. Amino pyrimidine compound for inhibiting protein tyrosine kinase activity
IL292977A (en) 2016-09-09 2022-07-01 Incyte Corp Pyrazolopyridine derivatives as modulators of hpk1 and their use in cancer therapy
WO2018049214A1 (en) 2016-09-09 2018-03-15 Incyte Corporation Pyrazolopyridine derivatives as hpk1 modulators and uses thereof for the treatment of cancer
KR102388312B1 (ko) * 2017-06-13 2022-04-19 베이징 아다메이들 바이오테크놀로지 리미티드 라이어빌리티 컴퍼니 아미노피리미딘 화합물, 이의 제조방법 및 용도
EP3648753A4 (en) * 2017-07-05 2021-03-17 CS Pharmatech Limited SELECTIVE INHIBITORS OF CLINICALLY IMPORTANT MUTANTS OF EGFR TYROSINE KINASE
EP3659307A4 (en) * 2017-07-28 2021-09-22 Yale University ANTI-CANCER PRODUCTS AND METHOD FOR MANUFACTURING AND USING THEREOF
PT3658547T (pt) * 2017-07-28 2023-10-20 Yuhan Corp Processo de preparação de n -(5 -(4 -(4 -formil -3- fenil- 1h -pirazol- 1 -il)pirimidin -2- ilamino) -4 -metoxi 2- morfolinofenil) acrilamida
WO2019042187A1 (zh) * 2017-08-30 2019-03-07 深圳市塔吉瑞生物医药有限公司 一种氨基嘧啶类化合物及包含该化合物的组合物及其用途
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
CN107827875B (zh) * 2017-09-25 2021-07-09 文韬创新药物研究（北京）有限责任公司 一种苯并咪唑类衍生物作为周期蛋白依赖性激酶4/6抑制剂的应用
US20210101881A1 (en) * 2018-02-12 2021-04-08 Ancureall Pharmaceutical (Shanghai) Co., Ltd. Pyrimidine compound, preparation method thereof and medical use thereof
LT3755703T (lt) 2018-02-20 2022-10-10 Incyte Corporation N-(fenil)-2-(fenil)pirimidin-4-karboksamido dariniai ir susiję junginiai, kaip hpk1 inhibitoriai, skirti vėžio gydymui
WO2019164949A1 (en) * 2018-02-20 2019-08-29 Dana-Farber Cancer Institute, Inc. Pharmaceutical combinations of egfr inhibitors and methods of use thereof
EP3755338A4 (en) * 2018-02-20 2021-11-03 Dana-Farber Cancer Institute, Inc. PHARMACEUTICAL COMBINATIONS OF EGFR INHIBITORS AND THEIR METHODS OF USE
US12448374B2 (en) 2018-06-07 2025-10-21 Disarm Therapeutics, Inc. Inhibitors of SARM1
CN112543757A (zh) 2018-06-15 2021-03-23 卡迪拉保健有限公司 对结核菌具有抗菌活性的缩合氮杂杂芳基化合物
CN110790749B (zh) * 2018-08-03 2023-07-14 北京普祺医药科技股份有限公司 一种含氮杂环化合物、药物组合物以及其用途
US10899755B2 (en) 2018-08-08 2021-01-26 Incyte Corporation Benzothiazole compounds and uses thereof
CN110857292A (zh) * 2018-08-22 2020-03-03 上海艾力斯医药科技有限公司 一种egfr激酶抑制剂及其制备方法和应用
EP3897670A4 (en) 2018-12-19 2022-09-07 Disarm Therapeutics, Inc. MRSA1 INHIBITORS IN COMBINATION WITH NEUROPROTECTIVE AGENTS
CN113227073B (zh) * 2019-01-05 2022-09-16 山东轩竹医药科技有限公司 Egfr酪氨酸激酶的选择性抑制剂的盐及其晶型
CN111410651B (zh) * 2019-01-05 2021-06-04 山东轩竹医药科技有限公司 酪氨酸激酶抑制剂的盐及其晶型
US12157730B2 (en) 2019-03-19 2024-12-03 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
PL3943491T3 (pl) 2019-03-19 2025-11-17 Voronoi Inc. Pochodna heteroarylowa, sposób jej wytwarzania i kompozycja farmaceutyczna zawierająca ją jako skuteczny składnik
CN111825658B (zh) * 2019-04-18 2024-11-08 华东理工大学 Egfr三突变抑制剂及其应用
CN112174961A (zh) * 2019-07-04 2021-01-05 微境生物医药科技(上海)有限公司 一类抑制egfr激酶的化合物及其制备方法和用途
EP4010338A1 (en) 2019-08-06 2022-06-15 Incyte Corporation Solid forms of an hpk1 inhibitor
TW202128670A (zh) * 2019-11-26 2021-08-01 大陸商上海翰森生物醫藥科技有限公司 含氮多環類衍生物抑制劑、其製備方法和應用
CN113045475A (zh) * 2019-12-27 2021-06-29 上海泓博智源医药股份有限公司 一种5-溴-7-甲基吲哚的制备方法
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
WO2021243596A1 (en) * 2020-06-03 2021-12-09 InventisBio Co., Ltd. Aminopyrimidine compounds, preparation methods and uses thereof
TW202214600A (zh) * 2020-09-24 2022-04-16 大陸商廣州費米子科技有限責任公司 嘧啶基衍生物、其製備方法及其用途
WO2022081478A1 (en) * 2020-10-12 2022-04-21 Dana-Farber Cancer Institute, Inc. Covalent egfr inhibitors and methods of use thereof
JP2023550591A (ja) * 2020-11-02 2023-12-04 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ＥＧＦＲ阻害薬としての置換１Ｈ－ピラゾロ［４，３－ｃ］及び誘導体
CN114539269B (zh) * 2020-11-19 2023-04-28 上海医药工业研究院有限公司 一种含氮大环化合物、其制备方法及其应用
WO2022115753A1 (en) * 2020-11-30 2022-06-02 H. Lee Moffitt Cancer Center And Research Institute, Inc. Merged scaffold taf1 inhibitors
EP4359400B1 (en) * 2021-06-23 2025-07-02 Blueprint Medicines Corporation Salt and crystal form of an azetidinyl substituted isoquinline acting as epidermal growth factor receptor inhibitor for the treatment of cancer
TW202317542A (zh) * 2021-06-23 2023-05-01 美商纜圖藥品公司 製備egfr抑制劑的方法
CN115701429B (zh) * 2021-08-02 2024-03-12 上海和誉生物医药科技有限公司 4-(1h-吲哚-1-基)嘧啶-2-氨基衍生物及其制备方法和应用
CN115703760B (zh) * 2021-08-11 2024-05-31 山东大学 2,4-二取代嘧啶类细胞周期蛋白依赖性激酶酶抑制剂及其制备方法和应用
CN116283914A (zh) * 2021-12-01 2023-06-23 上海艾力斯医药科技股份有限公司 一类嘧啶类化合物、其制备方法及应用

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105085489A (zh) * 2014-11-05 2015-11-25 上海页岩科技有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途

Family Cites Families (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
KR0166088B1 (ko) 1990-01-23 1999-01-15 . 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도
GB9518953D0 (en) 1995-09-15 1995-11-15 Pfizer Ltd Pharmaceutical formulations
WO2000035298A1 (en) 1996-11-27 2000-06-22 Wm. Wrigley Jr. Company Chewing gum containing medicament active agents
CA2280515A1 (en) 1997-03-11 1998-09-17 E.I. Du Pont De Nemours And Company Heteroaryl azole herbicides
GB9711643D0 (en) 1997-06-05 1997-07-30 Janssen Pharmaceutica Nv Glass thermoplastic systems
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
US6897208B2 (en) * 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
US7582631B2 (en) * 2004-01-14 2009-09-01 Amgen Inc. Substituted heterocyclic compounds and methods of use
ATE502920T1 (de) 2007-12-14 2011-04-15 Pulmagen Therapeutics Asthma Ltd Indole und ihre therapeutische verwendung
TWI458721B (zh) 2008-06-27 2014-11-01 Celgene Avilomics Res Inc 雜芳基化合物及其用途
WO2010142934A1 (en) 2009-06-12 2010-12-16 Pulmagen Therapeutics (Asthma) Limited Indole derivatives as ligands of crth2 receptors
ES2654177T3 (es) 2011-07-27 2018-02-12 Astrazeneca Ab Derivados de 2-(2,4,5-anilino sustituido)pirimidina como moduladores de EGFR útiles para tratar el cáncer
EP2763976B1 (en) * 2011-10-05 2016-05-18 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
NZ703162A (en) 2012-07-03 2017-05-26 3-V Biosciences Inc Heterocyclic modulators of lipid synthesis
CN104513253A (zh) * 2013-10-01 2015-04-15 南京波尔泰药业科技有限公司 用于治疗增殖性疾病的大环化合物
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
US20170166598A1 (en) 2014-05-13 2017-06-15 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
CN111892579B (zh) * 2014-06-12 2023-07-25 上海艾力斯医药科技股份有限公司 一类激酶抑制剂
BR112016029662B1 (pt) * 2014-06-19 2023-10-24 Takeda Pharmaceutical Company Limited COMPOSTO DE FÓRMULA Bf OU UMA FORMA FARMACEUTICAMENTE ACEITÁVEL DO MESMO, COMPOSIÇÃO FARMACÊUTICA COMPREENDENDO O MESMO E SEU USO
CN105315259B (zh) 2014-07-29 2018-03-09 上海艾力斯医药科技有限公司 吡啶胺基嘧啶衍生物、其制备方法及应用
CN113121575A (zh) 2014-08-25 2021-07-16 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
SI3205650T1 (sl) * 2014-10-11 2021-10-29 Shanghai Hansoh Biomedical Co Ltd Zaviralec EGFR-ja in priprava ter uporaba le-tega
HRP20250213T1 (hr) 2014-10-13 2025-04-25 Yuhan Corporation Spojevi i pripravci za modulaciju aktivnosti egfr mutantne kinaze
KR102387699B1 (ko) 2014-12-23 2022-04-18 미츠비시 하이텍 페이퍼 유럽 게엠베하 오프셋 인쇄용 감열 기록 재료
WO2016105525A2 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Novel pyrimidines as egfr inhibitors and methods of treating disorders
CN104788427B (zh) 2015-02-05 2017-05-31 上海泓博智源医药股份有限公司 3‑(2‑嘧啶氨基)苯基丙烯酰胺类化合物及其应用
CN104844580B (zh) 2015-04-17 2017-10-20 中国药科大学 嘧啶类化合物、其制备方法及医药用途
JP6457697B2 (ja) 2015-04-29 2019-01-23 カントン チョンション ファーマシューティカル カンパニー，リミティド キナーゼ阻害剤としての縮合環式または三環式アリールピリミジン化合物
WO2016183278A1 (en) 2015-05-13 2016-11-17 Ariad Pharmaceuticals, Inc. Heteroaryl compounds for kinase inhibition
KR102666414B1 (ko) 2015-07-16 2024-05-17 치아타이 티안큉 파마수티컬 그룹 주식회사 아닐린 피리미딘 유도체 및 그의 용도
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
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
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
JP2019501222A (ja) 2016-01-07 2019-01-17 シーエス ファーマテック リミテッド Ｅｇｆｒチロシンキナーゼの臨床的に重要な変異体の選択的阻害薬
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
WO2017190637A1 (zh) 2016-05-06 2017-11-09 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稠合嘧啶类化合物
KR20190006991A (ko) 2016-05-11 2019-01-21 베타 파마, 인크. 뇌암의 치료를 위한 치료제로서의 2-아닐리노피리미딘 유도체
EP3492462B1 (en) 2016-07-26 2023-08-30 Shenzhen TargetRx, Inc. Amino pyrimidine compound for inhibiting protein tyrosine kinase activity
EP3648753A4 (en) 2017-07-05 2021-03-17 CS Pharmatech Limited SELECTIVE INHIBITORS OF CLINICALLY IMPORTANT MUTANTS OF EGFR TYROSINE KINASE

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105085489A (zh) * 2014-11-05 2015-11-25 上海页岩科技有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2022533473A (ja) * 2019-07-26 2022-07-22 メッドシャイン ディスカバリー インコーポレイテッド Ｅｇｆｒ及びｅｒｂｂ２に作用するピリミジン系化合物
JP7154455B2 (ja) 2019-07-26 2022-10-17 チャイナ・リソースズ・ファーマシューティカル・ホールディングス・カンパニー・リミテッド Ｅｇｆｒ及びｅｒｂｂ２に作用するピリミジン系化合物
JP2023545571A (ja) * 2020-12-02 2023-10-30 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
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
JP2024524262A (ja) * 2021-08-06 2024-07-05 上海和誉生物医薬科技有限公司 ピリミジンまたはピリジン誘導体およびその製造方法ならびに薬学上の応用
JP7734995B2 (ja) 2021-08-06 2025-09-08 上海和誉生物医薬科技有限公司 ピリミジンまたはピリジン誘導体およびその製造方法ならびに薬学上の応用

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