CN105899490B - 嘧啶fgfr4抑制剂 - Google Patents
嘧啶fgfr4抑制剂 Download PDFInfo
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- CN105899490B CN105899490B CN201480056358.4A CN201480056358A CN105899490B CN 105899490 B CN105899490 B CN 105899490B CN 201480056358 A CN201480056358 A CN 201480056358A CN 105899490 B CN105899490 B CN 105899490B
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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
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0021—Intradermal administration, e.g. through microneedle arrays, needleless injectors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
- C07C53/15—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
- C07C53/16—Halogenated acetic acids
- C07C53/18—Halogenated acetic acids containing fluorine
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- 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
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D413/12—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 linked by a chain containing hetero atoms as chain links
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Dermatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Peptides Or Proteins (AREA)
- Biomedical Technology (AREA)
- Cell Biology (AREA)
- Oncology (AREA)
- Biotechnology (AREA)
- Hospice & Palliative Care (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Microbiology (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Food Science & Technology (AREA)
- Physics & Mathematics (AREA)
- Analytical Chemistry (AREA)
- Biochemistry (AREA)
- General Physics & Mathematics (AREA)
- Pathology (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910565163.7A CN110354128A (zh) | 2013-10-18 | 2014-10-16 | 嘧啶fgfr4抑制剂 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361892881P | 2013-10-18 | 2013-10-18 | |
| US61/892,881 | 2013-10-18 | ||
| PCT/US2014/060857 WO2015057938A1 (en) | 2013-10-18 | 2014-10-16 | Pyrimidine fgfr4 inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201910565163.7A Division CN110354128A (zh) | 2013-10-18 | 2014-10-16 | 嘧啶fgfr4抑制剂 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105899490A CN105899490A (zh) | 2016-08-24 |
| CN105899490B true CN105899490B (zh) | 2019-07-23 |
Family
ID=51842899
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480056358.4A Active CN105899490B (zh) | 2013-10-18 | 2014-10-16 | 嘧啶fgfr4抑制剂 |
| CN201910565163.7A Pending CN110354128A (zh) | 2013-10-18 | 2014-10-16 | 嘧啶fgfr4抑制剂 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201910565163.7A Pending CN110354128A (zh) | 2013-10-18 | 2014-10-16 | 嘧啶fgfr4抑制剂 |
Country Status (33)
Families Citing this family (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| SMT201700146T1 (it) | 2012-06-13 | 2017-05-08 | Incyte Holdings Corp | Composti triciclici sostituiti come inibitori di fgfr |
| CA2878412A1 (en) | 2012-07-11 | 2014-01-16 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| AR095464A1 (es) | 2013-03-15 | 2015-10-21 | Celgene Avilomics Res Inc | Compuestos de heteroarilo y usos de los mismos |
| UA120248C2 (uk) | 2013-03-15 | 2019-11-11 | Селджен Кар Ллс | Гетероарильні сполуки та їх застосування |
| MX374558B (es) | 2013-03-15 | 2025-03-06 | Sanofi Sa | Compuestos de heteroarilo y sus usos. |
| CA2909207C (en) | 2013-04-19 | 2021-11-02 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| HUE039268T2 (hu) * | 2013-10-18 | 2018-12-28 | Eisai R&D Man Co Ltd | Pirimidin FGFR4 inhibitorok |
| EP3060563B1 (en) | 2013-10-25 | 2018-05-02 | Novartis AG | Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors |
| LT3395814T (lt) | 2013-10-25 | 2022-07-25 | Blueprint Medicines Corporation | Fibroblastų augimo faktoriaus receptoriaus inhibitoriai |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| US20180185341A1 (en) | 2014-10-03 | 2018-07-05 | Novartis Ag | Use of ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| UA121669C2 (uk) | 2015-02-20 | 2020-07-10 | Інсайт Корпорейшн | Біциклічні гетероцикли як інгібітори fgfr |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US9802917B2 (en) | 2015-03-25 | 2017-10-31 | Novartis Ag | Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide |
| WO2016164703A1 (en) * | 2015-04-09 | 2016-10-13 | Eisai R & D Management Co., Ltd. | Fgfr4 inhibitors |
| JP6431622B2 (ja) * | 2015-04-14 | 2018-11-28 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 結晶性ｆｇｆｒ４阻害剤化合物およびその使用 |
| CA2991645A1 (en) | 2015-07-20 | 2017-01-26 | Dana-Farber Cancer Institute, Inc. | Novel pyrimidines as egfr inhibitors and methods of treating disorders |
| BR112018001053A2 (pt) | 2015-07-20 | 2018-09-11 | Univ Taipei Medical | compostos, composição farmacêutica e método para inibir, prevenir ou tratar um câncer em um indivíduo |
| CN105418441A (zh) * | 2015-12-22 | 2016-03-23 | 中国工程物理研究院化工材料研究所 | 2,3-二氯-4-羟基苯胺的制备方法 |
| CN109071521B (zh) * | 2016-01-08 | 2019-10-25 | 杭州英创医药科技有限公司 | 作为fgfr抑制剂的杂环化合物 |
| EP3454898B1 (en) * | 2016-05-10 | 2021-11-10 | Eisai R&D Management Co., Ltd. | Drug combinations for reducing cell viability and/or cell proliferation |
| TWI669300B (zh) * | 2016-05-20 | 2019-08-21 | 浙江海正藥業股份有限公司 | 嘧啶類衍生物、其製備方法、其藥物組合物以及其在醫藥上的用途 |
| CN107400092B (zh) * | 2016-05-20 | 2021-08-24 | 浙江海正药业股份有限公司 | 嘧啶类衍生物及其制备方法和其在医药上的用途 |
| CN105884760B (zh) * | 2016-06-13 | 2019-01-04 | 厦门市蔚嘉化学科技有限公司 | 一种可比司他中间体的制备方法 |
| JP7190425B2 (ja) * | 2016-08-23 | 2022-12-15 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 肝細胞癌の治療のための併用療法 |
| WO2018049233A1 (en) | 2016-09-08 | 2018-03-15 | Nicolas Stransky | Inhibitors of the fibroblast growth factor receptor in combination with cyclin-dependent kinase inhibitors |
| WO2018055503A1 (en) | 2016-09-20 | 2018-03-29 | Novartis Ag | Combination comprising a pd-1 antagonist and an fgfr4 inhibitor |
| US11229643B2 (en) | 2016-11-02 | 2022-01-25 | Novartis Ag | Combinations of FGFR4 inhibitors and bile acid sequestrants |
| CA3043948C (en) * | 2016-11-17 | 2021-08-31 | Guangdong Zhongsheng Pharmaceutical Co., Ltd | Fgfr4 inhibitor and preparation method and use thereof |
| KR101812266B1 (ko) | 2016-11-25 | 2017-12-27 | 한국과학기술연구원 | 4-((2-아크릴아미도페닐)아미노)티에노[3,2-d]피리미딘-7-카복스아미드 유도체 및 그의 약학적 활용 |
| CN108239069B (zh) * | 2016-12-26 | 2021-01-05 | 南京药捷安康生物科技有限公司 | 一种用于成纤维细胞生长因子受体的抑制剂及其用途 |
| CN108503593B (zh) * | 2017-02-28 | 2021-04-27 | 暨南大学 | 2-氨基嘧啶类化合物及其应用 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| WO2019024876A1 (zh) * | 2017-08-04 | 2019-02-07 | 上海和誉生物医药科技有限公司 | 一种具有fgfr4抑制活性的醛基吡啶衍生物、其制备方法和应用 |
| CN109422760B (zh) * | 2017-09-01 | 2022-05-27 | 南京圣和药物研发有限公司 | Fgfr4抑制剂及其应用 |
| CA3074885A1 (en) | 2017-09-05 | 2019-03-14 | Bioardis Llc | Aromatic derivative, preparation method for same, and medical applications thereof |
| JP7352569B2 (ja) | 2018-01-10 | 2023-09-28 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 肝細胞癌の治療のための併用療法 |
| SMT202400507T1 (it) | 2018-05-04 | 2025-01-14 | Incyte Corp | Forme solide di un inibitore di fgfr e procedimenti per preparare le stesse |
| SG11202010882XA (en) | 2018-05-04 | 2020-11-27 | Incyte Corp | Salts of an fgfr inhibitor |
| WO2019242689A1 (zh) * | 2018-06-22 | 2019-12-26 | 北京赛特明强医药科技有限公司 | 一种氰基取代吡啶及氰基取代嘧啶类化合物、制备方法及其应用 |
| WO2020177067A1 (en) | 2019-03-05 | 2020-09-10 | Bioardis Llc | Aromatic derivatives, preparation methods, and medical uses thereof |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| CN118930524A (zh) | 2019-05-10 | 2024-11-12 | 德西费拉制药有限责任公司 | 苯基氨基嘧啶酰胺自噬抑制剂及其使用方法 |
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| PE20221083A1 (es) | 2019-06-17 | 2022-07-05 | Deciphera Pharmaceuticals Llc | Inhibidores de la autofagia de la amida aminopirimidina y sus metodos de uso |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
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| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CA3157361A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US11897891B2 (en) | 2019-12-04 | 2024-02-13 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
| WO2021113462A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Derivatives of an fgfr inhibitor |
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| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021231928A1 (en) | 2020-05-15 | 2021-11-18 | Eisai R&D Management Co., Ltd. | A method for treating cancer with an oral dosage form of an fgfr4 inhibitor |
| WO2021230886A1 (en) | 2020-05-15 | 2021-11-18 | Eisai R&D Management Co., Ltd. | A method for treating cancer with an oral dosage form of an fgfr4 inhibitor |
| CN113943251A (zh) * | 2020-07-16 | 2022-01-18 | 正大天晴药业集团股份有限公司 | 双环庚烯基氨基取代的氮杂芳环类化合物及其医药用途 |
| CN116406298A (zh) | 2020-10-05 | 2023-07-07 | 凯奥目生物科学株式会社 | 癌治疗用药物 |
| CN114621106A (zh) * | 2020-12-11 | 2022-06-14 | 重庆医药工业研究院有限责任公司 | 一种酪氨酸激酶药物中间体的制备方法 |
| CA3215903A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| EP4352060A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| CN115490670A (zh) * | 2021-06-17 | 2022-12-20 | 浙江海正药业股份有限公司 | Fgfr4选择性抑制剂的盐及其制备方法和用途 |
| CN115504965A (zh) | 2021-06-23 | 2022-12-23 | 浙江海正药业股份有限公司 | 嘧啶类衍生物的晶型及其制备方法 |
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| CN114560815A (zh) * | 2022-03-04 | 2022-05-31 | 北京工业大学 | (2-((5-氯-取代苯基氨基嘧啶-2-基)氨基)苯基)氨基甲酸叔丁酯类衍生物 |
| CN116947825B (zh) * | 2022-04-14 | 2025-11-28 | 浙江海正药业股份有限公司 | Fgfr4选择性抑制剂化合物的晶型及其制备方法和用途 |
| CN114835640B (zh) * | 2022-05-24 | 2024-02-13 | 中国药科大学 | 成纤维细胞生长因子受体抑制剂、制备方法及应用 |
| EP4509142A1 (en) | 2023-08-16 | 2025-02-19 | Ona Therapeutics S.L. | Fgfr4 as target in cancer treatment |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102083800A (zh) * | 2008-06-27 | 2011-06-01 | 阿维拉制药公司 | 杂芳基化合物和其用途 |
| CN102639510A (zh) * | 2009-12-07 | 2012-08-15 | 诺瓦提斯公司 | 3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲及其盐的晶型 |
| CN103121972A (zh) * | 2004-06-24 | 2013-05-29 | 诺瓦提斯公司 | 作为激酶抑制剂的嘧啶脲衍生物 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3881320D1 (de) * | 1987-09-28 | 1993-07-01 | Ciba Geigy Ag | Schaedlingsbekaempfungsmittel. |
| IL139599A0 (en) | 1998-05-26 | 2002-02-10 | Warner Lambert Co | Bicyclic pyrimidines and bicyclic 3,4-dihydropyrimidines as inhibitors of cellular proliferation |
| GB0103926D0 (en) | 2001-02-17 | 2001-04-04 | Astrazeneca Ab | Chemical compounds |
| AU2003285012A1 (en) | 2002-10-24 | 2004-05-13 | Sepracor, Inc. | Compositions comprising zopiclone derivatives and methods of making and using the same |
| JP2007500725A (ja) | 2003-07-29 | 2007-01-18 | アイアールエム・リミテッド・ライアビリティ・カンパニー | プロテインキナーゼ阻害剤としての化合物および組成物 |
| WO2006038112A1 (en) | 2004-10-01 | 2006-04-13 | Warner-Lambert Company Llc | Use of kinase inhibitors to promote neochondrogenesis |
| BRPI0620408B8 (pt) | 2005-12-21 | 2021-05-25 | Novartis Ag | derivados de pirimidinil aril uréia sendo inibidores de fgf, seus usos, e preparação farmacêutica |
| EP1918376A1 (en) | 2006-11-03 | 2008-05-07 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. | FGFR4 promotes cancer cell resistance in response to chemotherapeutic drugs |
| PT2114900T (pt) * | 2007-01-31 | 2019-01-17 | Ym Biosciences Australia Pty | Compostos à base de tiopirimidina e as suas utilizações |
| US20090062320A1 (en) | 2007-08-28 | 2009-03-05 | Vito Guagnano | Method of Treating Disorders Mediated by the Fibroblast Growth Factor Receptor |
| WO2011090738A2 (en) | 2009-12-29 | 2011-07-28 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
| IN2012DN05017A (enExample) | 2010-01-14 | 2015-10-02 | Univ Yale | |
| WO2011153553A2 (en) | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
| WO2012136732A1 (en) | 2011-04-08 | 2012-10-11 | Ab Science | Treatment of multiple myeloma with masitinib |
| CN102816162B (zh) | 2011-06-10 | 2016-04-27 | 中国科学院广州生物医药与健康研究院 | 嘧啶并嘧啶酮类化合物及其药用组合物和应用 |
| CA2862424A1 (en) | 2012-01-18 | 2013-07-25 | Genentech, Inc. | Methods of using fgf19 modulators |
| MX349120B (es) | 2012-02-28 | 2017-07-12 | Astellas Pharma Inc | Compuesto heterociclico aromatico que contiene nitrogeno. |
| CA2878412A1 (en) | 2012-07-11 | 2014-01-16 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| CA2908098A1 (en) * | 2013-03-15 | 2014-09-25 | Celgene Avilomics Research, Inc. | Mk2 inhibitors and uses thereof |
| MX374558B (es) * | 2013-03-15 | 2025-03-06 | Sanofi Sa | Compuestos de heteroarilo y sus usos. |
| AU2014287209B2 (en) | 2013-07-09 | 2019-01-24 | Dana-Farber Cancer Institute, Inc. | Kinase inhibitors for the treatment of disease |
| TW201605452A (zh) | 2013-08-28 | 2016-02-16 | 安斯泰來製藥股份有限公司 | 以嘧啶化合物作爲有效成分之醫藥組成物 |
| HUE039268T2 (hu) * | 2013-10-18 | 2018-12-28 | Eisai R&D Man Co Ltd | Pirimidin FGFR4 inhibitorok |
| LT3395814T (lt) | 2013-10-25 | 2022-07-25 | Blueprint Medicines Corporation | Fibroblastų augimo faktoriaus receptoriaus inhibitoriai |
| US9695165B2 (en) | 2014-01-15 | 2017-07-04 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| EP3444250A4 (en) | 2016-05-20 | 2019-09-25 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | FGFR4 INHIBITOR, MANUFACTURING METHOD AND APPLICATIONS THEREOF |
| TWI669300B (zh) | 2016-05-20 | 2019-08-21 | 浙江海正藥業股份有限公司 | 嘧啶類衍生物、其製備方法、其藥物組合物以及其在醫藥上的用途 |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103121972A (zh) * | 2004-06-24 | 2013-05-29 | 诺瓦提斯公司 | 作为激酶抑制剂的嘧啶脲衍生物 |
| CN102083800A (zh) * | 2008-06-27 | 2011-06-01 | 阿维拉制药公司 | 杂芳基化合物和其用途 |
| CN102639510A (zh) * | 2009-12-07 | 2012-08-15 | 诺瓦提斯公司 | 3-(2,6-二氯-3,5-二甲氧基-苯基)-1-{6-[4-(4-乙基-哌嗪-1-基)-苯基氨基]-嘧啶-4-基}-1-甲基-脲及其盐的晶型 |
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