CA2924206C - Pyrimidine fgfr4 inhibitors - Google Patents
Pyrimidine fgfr4 inhibitors Download PDFInfo
- Publication number
- CA2924206C CA2924206C CA2924206A CA2924206A CA2924206C CA 2924206 C CA2924206 C CA 2924206C CA 2924206 A CA2924206 A CA 2924206A CA 2924206 A CA2924206 A CA 2924206A CA 2924206 C CA2924206 C CA 2924206C
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Classifications
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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 or needleless injectors
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- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (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)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
- Urology & Nephrology (AREA)
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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2924206A1 CA2924206A1 (en) | 2015-04-23 |
| CA2924206C true CA2924206C (en) | 2022-10-25 |
Family
ID=51842899
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2924206A Active CA2924206C (en) | 2013-10-18 | 2014-10-16 | Pyrimidine fgfr4 inhibitors |
Country Status (33)
| Country | Link |
|---|---|
| US (4) | US9434697B2 (https=) |
| EP (2) | EP3057943B1 (https=) |
| JP (2) | JP6139788B2 (https=) |
| KR (1) | KR101826015B1 (https=) |
| CN (2) | CN105899490B (https=) |
| AR (1) | AR098048A1 (https=) |
| AU (2) | AU2014337291B9 (https=) |
| BR (1) | BR112016008110B1 (https=) |
| CA (1) | CA2924206C (https=) |
| CL (1) | CL2016000918A1 (https=) |
| CY (1) | CY1121129T1 (https=) |
| DK (1) | DK3057943T3 (https=) |
| ES (1) | ES2679521T3 (https=) |
| HR (1) | HRP20181129T1 (https=) |
| HU (1) | HUE039268T2 (https=) |
| IL (1) | IL244373B (https=) |
| JO (1) | JO3515B1 (https=) |
| LT (1) | LT3057943T (https=) |
| MX (1) | MX378288B (https=) |
| MY (1) | MY184733A (https=) |
| NZ (1) | NZ717559A (https=) |
| PE (1) | PE20160679A1 (https=) |
| PH (1) | PH12016500676B1 (https=) |
| PL (1) | PL3057943T3 (https=) |
| PT (1) | PT3057943T (https=) |
| RS (1) | RS57444B1 (https=) |
| RU (1) | RU2715708C2 (https=) |
| SG (1) | SG11201602069WA (https=) |
| SI (1) | SI3057943T1 (https=) |
| SM (1) | SMT201800379T1 (https=) |
| TW (1) | TWI597268B (https=) |
| UA (1) | UA116920C2 (https=) |
| WO (2) | WO2015057938A1 (https=) |
Families Citing this family (73)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| ES2704744T3 (es) | 2012-06-13 | 2019-03-19 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| SMT202100451T1 (it) | 2012-07-11 | 2021-09-14 | Blueprint Medicines Corp | Inibitori del recettore di crescita dei fibroblasti |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| TWI647220B (zh) | 2013-03-15 | 2019-01-11 | 美商西建卡爾有限責任公司 | 雜芳基化合物及其用途 |
| MY181020A (en) | 2013-03-15 | 2020-12-16 | Sanofi Sa | Heteroaryl compounds and uses thereof |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| MX378288B (es) | 2013-10-18 | 2025-03-10 | Eisai R&D Man Co Ltd | Inhibidores de pirimidina del fgfr4. |
| CA2928042C (en) | 2013-10-25 | 2022-05-10 | Blueprint Medicines Corporation | Inhibitors of the fibroblast growth factor receptor |
| CN105683188B (zh) | 2013-10-25 | 2018-02-09 | 诺华股份有限公司 | 作为fgfr4抑制剂的稠环二环吡啶基衍生物 |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| MA38393B1 (fr) | 2014-03-13 | 2018-11-30 | Sanofi Sa | Composés hétéroaryle et utilisations associées |
| JP6585167B2 (ja) | 2014-10-03 | 2019-10-02 | ノバルティス アーゲー | Ｆｇｆｒ４阻害剤としての縮環二環式ピリジル誘導体の使用 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MX373169B (es) | 2015-02-20 | 2020-04-24 | Incyte Holdings Corp | Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr). |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| 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 |
| SG10201810057UA (en) * | 2015-04-14 | 2018-12-28 | Eisai R&D Man Co Ltd | Crystalline fgfr4 inhibitor compound and uses thereof |
| US10550112B2 (en) | 2015-07-20 | 2020-02-04 | Dana-Farber Cancer Institute, Inc. | 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 |
| US10934311B2 (en) | 2016-01-08 | 2021-03-02 | Hangzhou Innogate Pharma Co., Ltd. | Heterocyclic compound used as FGFR inhibitor |
| EP3454898B1 (en) * | 2016-05-10 | 2021-11-10 | Eisai R&D Management Co., Ltd. | Drug combinations for reducing cell viability and/or cell proliferation |
| JP6667014B2 (ja) * | 2016-05-20 | 2020-03-18 | 浙江海正薬業股▲ふん▼有限公司Ｚｈｅｊｉａｎｇ Ｈｉｓｕｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌ ＣＯ．，ＬＴＤ． | ピリミジン誘導体、その調製方法および医療での使用 |
| 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 |
| CN109803684B (zh) * | 2016-08-23 | 2022-08-23 | 卫材 R&D 管理有限公司 | 用于治疗肝细胞癌的组合疗法 |
| 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 |
| SG11201903911UA (en) | 2016-11-02 | 2019-05-30 | Novartis Ag | Combinations of fgfr4 inhibitors and bile acid sequestrants |
| NZ754218A (en) * | 2016-11-17 | 2021-07-30 | 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 |
| JP6941900B2 (ja) * | 2017-08-04 | 2021-09-29 | アビスコ セラピューティクス カンパニー リミテッド | Ｆｇｆｒ４阻害活性が示されるアルデヒド基ピリジン誘導体、その製造方法および応用 |
| 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 |
| WO2019047826A1 (zh) | 2017-09-05 | 2019-03-14 | 博奥阿迪斯生物科技公司 | 芳香类衍生物、其制备方法及其在医药上的应用 |
| MA51570A (fr) | 2018-01-10 | 2020-11-18 | Eisai R&D Man Co Ltd | Polythérapies pour le traitement du carcinome hépatocellulaire |
| MA52493A (fr) | 2018-05-04 | 2021-03-10 | Incyte Corp | Sels d'un inhibiteur de fgfr |
| CR20200590A (es) | 2018-05-04 | 2021-04-26 | Incyte Corp | Formas sólidas de un inhibidor de fgfr y procesos para prepararlas |
| CN112313207B (zh) * | 2018-06-22 | 2023-02-14 | 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 |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
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| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
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| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US20230172867A1 (en) | 2020-05-15 | 2023-06-08 | Eisai R&D Management Co., Ltd. | A method for treating cancer with an oral dosage form of an fgfr4 inhibitor |
| JP2023533903A (ja) * | 2020-05-15 | 2023-08-07 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | Ｆｇｆｒ４阻害剤の経口製剤によるがんの治療方法 |
| CN113943251B (zh) * | 2020-07-16 | 2026-04-17 | 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 |
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