AR097455A1 - Composición farmacéutica que contiene compuesto de pirimidina como un ingrediente activo - Google Patents
Composición farmacéutica que contiene compuesto de pirimidina como un ingrediente activoInfo
- Publication number
- AR097455A1 AR097455A1 ARP140103193A ARP140103193A AR097455A1 AR 097455 A1 AR097455 A1 AR 097455A1 AR P140103193 A ARP140103193 A AR P140103193A AR P140103193 A ARP140103193 A AR P140103193A AR 097455 A1 AR097455 A1 AR 097455A1
- Authority
- AR
- Argentina
- Prior art keywords
- pharmaceutical composition
- cancer
- fgfr4
- fgf19
- dimethoxybenzyl
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 6
- 239000004480 active ingredient Substances 0.000 title abstract 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 239000002131 composite material Substances 0.000 title 1
- 206010028980 Neoplasm Diseases 0.000 abstract 8
- 201000011510 cancer Diseases 0.000 abstract 8
- 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 abstract 6
- 101000917134 Homo sapiens Fibroblast growth factor receptor 4 Proteins 0.000 abstract 6
- 101150051399 FGF19 gene Proteins 0.000 abstract 3
- 102100031734 Fibroblast growth factor 19 Human genes 0.000 abstract 3
- 101000846394 Homo sapiens Fibroblast growth factor 19 Proteins 0.000 abstract 3
- 230000003321 amplification Effects 0.000 abstract 3
- 201000007270 liver cancer Diseases 0.000 abstract 3
- 208000014018 liver neoplasm Diseases 0.000 abstract 3
- 238000003199 nucleic acid amplification method Methods 0.000 abstract 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 2
- -1 pyrimidine compound Chemical class 0.000 abstract 2
- VTBMFHXAWLFGOI-GFCCVEGCSA-N (2r)-3-[4-[[5-[(2,6-difluoro-3,5-dimethoxyphenyl)methoxy]pyrimidin-2-yl]amino]pyrazol-1-yl]propane-1,2-diol Chemical compound COC1=CC(OC)=C(F)C(COC=2C=NC(NC3=CN(C[C@@H](O)CO)N=C3)=NC=2)=C1F VTBMFHXAWLFGOI-GFCCVEGCSA-N 0.000 abstract 1
- DTENMRBPRWLNIS-UHFFFAOYSA-N 5-[(2,6-difluoro-3,5-dimethoxyphenyl)methoxy]-n-[1-methyl-5-[(4-methylpiperazin-1-yl)methyl]pyrazol-3-yl]pyrimidin-2-amine Chemical compound COC1=CC(OC)=C(F)C(COC=2C=NC(NC3=NN(C)C(CN4CCN(C)CC4)=C3)=NC=2)=C1F DTENMRBPRWLNIS-UHFFFAOYSA-N 0.000 abstract 1
- SYBLMCUTGSQYDI-UHFFFAOYSA-N 5-[(2,6-difluoro-3,5-dimethoxyphenyl)methoxy]-n-[3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]pyrimidin-2-amine Chemical compound COC1=CC(OC)=C(F)C(COC=2C=NC(NC=3C=C(OC)C(N4CCC(CC4)N4CCN(C)CC4)=CC=3)=NC=2)=C1F SYBLMCUTGSQYDI-UHFFFAOYSA-N 0.000 abstract 1
- NRTXZTDLUSLCNB-UHFFFAOYSA-N 5-[(2,6-difluoro-3,5-dimethoxyphenyl)methoxy]-n-[4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine Chemical compound COC1=CC(OC)=C(F)C(COC=2C=NC(NC=3C=CC(=CC=3)N3CCN(C)CC3)=NC=2)=C1F NRTXZTDLUSLCNB-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Dermatology (AREA)
Abstract
Composición farmacéutica para el tratamiento de cáncer relacionado con FGFR4 ,cáncer relacionado con FGF19, o cáncer de hígado positivo para la amplificación del gen FGF19. Un compuesto de pirimidina específico tiene una acción inhibitoria sobre FGFR4, y una composición farmacéutica que tiene el compuesto como un ingrediente activo tiene un efecto de tratamiento de cáncer relacionado con FGFR4; en otra forma de realización, cáncer relacionado con FGF19, y en aun otra forma de realización, cáncer de hígado positivo para la amplificación del gen FGF19. Reivindicación 1: Una composición farmacéutica para el tratamiento de cáncer relacionado con FGFR4, que comprende 5-[(2,6-difluoro-3,5-dimetoxibencil)oxi]-N-{3-metoxi-4-[4-(4-metilpiperazin-1-il)piperidin-1-il]fenil}pirimidin-2-amina, 2-[4-({5-[(2,6-difluoro-3,5-dimetoxibencil)oxi]pirimidin-2-il}amino)-1H-pirazol-1-il]etanol, (2R)-3[4-({5-[(2,6-difluoro-3,5dimetoxibencil)oxi]pirimidin-2-il}amino)-1H-pirazol-1-il]propano-1,2-diol, 5-[(2,6-difluoro-3,5-dimetoxibencil)oxi]-N-[4-(4-metilpiperazin-1-il)fenil]pirimidin-2-amina o 5-[(2,6-difluoro-3,5-dimetoxibencil)oxi]-N-{1-metil-5-[(4-metilpiperazin-1-il)metil]-1Hpirazol-3-il}pirimidin-2-amina, o una de sus sales farmacéuticamente aceptables, y un excipiente. Reivindicación 2: La composición farmacéutica de acuerdo con la reivindicación 1, donde el cáncer relacionado con FGFR4 es cáncer relacionado con FGF19. Reivindicación 3: La composición farmacéutica de acuerdo con la reivindicación 1,donde el cáncer relacionado con FGFR4 es cáncer de hígado positivo para la amplificación del gen FGF19.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2013176355 | 2013-08-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR097455A1 true AR097455A1 (es) | 2016-03-16 |
Family
ID=52586573
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP140103193A AR097455A1 (es) | 2013-08-28 | 2014-08-26 | Composición farmacéutica que contiene compuesto de pirimidina como un ingrediente activo |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20160199371A1 (es) |
| EP (1) | EP3040072A4 (es) |
| JP (1) | JPWO2015030021A1 (es) |
| KR (1) | KR20160040719A (es) |
| CN (1) | CN105492009A (es) |
| AR (1) | AR097455A1 (es) |
| AU (1) | AU2014312919A1 (es) |
| CA (1) | CA2922352A1 (es) |
| HK (1) | HK1219432A1 (es) |
| IL (1) | IL244206A0 (es) |
| MX (1) | MX2016002589A (es) |
| PH (1) | PH12016500372A1 (es) |
| RU (1) | RU2016106774A (es) |
| SG (1) | SG11201601461RA (es) |
| TW (1) | TW201605452A (es) |
| WO (1) | WO2015030021A1 (es) |
Families Citing this family (34)
| 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 |
| LT3495367T (lt) | 2012-06-13 | 2021-02-25 | Incyte Holdings Corporation | Pakeistieji tricikliniai junginiai, kaip fgfr inhibitoriai |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| LT2986610T (lt) | 2013-04-19 | 2018-04-10 | Incyte Holdings Corporation | Bicikliniai heterociklai, kaip fgfr inhibitoriai |
| SMT201800379T1 (it) | 2013-10-18 | 2018-09-13 | Eisai R&D Man Co Ltd | Inibitori di fgfr4 della pirimidina |
| BR112016008276B1 (pt) | 2013-10-25 | 2021-03-02 | Novartis Ag | derivados bicíclicos de piridila fundidos ao anel, seus usos e seu intermediário, e composição farmacêutica |
| WO2016054483A1 (en) | 2014-10-03 | 2016-04-07 | 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 |
| SG11201706287PA (en) | 2015-02-20 | 2017-09-28 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| 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 |
| CN107660200B (zh) | 2015-04-14 | 2022-01-11 | 卫材R&D管理有限公司 | 结晶fgfr4抑制剂化合物和其用途 |
| EP3454898B1 (en) | 2016-05-10 | 2021-11-10 | Eisai R&D Management Co., Ltd. | Drug combinations for reducing cell viability and/or cell proliferation |
| CN107541495B (zh) * | 2016-06-28 | 2022-04-26 | 上海市东方医院 | 一种fgf19过表达的人肝癌细胞系及其应用 |
| 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 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| ES3061844T3 (en) | 2018-05-04 | 2026-04-07 | Incyte Corp | Salts of an fgfr inhibitor |
| MX2020011718A (es) | 2018-05-04 | 2021-02-15 | Incyte Corp | Formas solidas de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr) y procesos para prepararlas. |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| TWI891666B (zh) | 2019-10-14 | 2025-08-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之雙環雜環 |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021113462A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Derivatives of an fgfr inhibitor |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| 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 |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法 |
| JP2024522189A (ja) | 2021-06-09 | 2024-06-11 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式ヘテロ環 |
| EP4352060A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| EP4509142A1 (en) | 2023-08-16 | 2025-02-19 | Ona Therapeutics S.L. | Fgfr4 as target in cancer treatment |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060247250A1 (en) | 2005-03-16 | 2006-11-02 | Targegen, Inc. | Pyrimidine inhibitors of kinases |
| US20070161645A1 (en) | 2005-11-02 | 2007-07-12 | Targegen, Inc. | Thiazole inhibitors targeting resistant kinase mutations |
| US8030487B2 (en) | 2006-07-07 | 2011-10-04 | Targegen, Inc. | 2-amino—5-substituted pyrimidine inhibitors |
| UA114501C2 (uk) | 2012-02-28 | 2017-06-26 | Астеллас Фарма Інк. | Азотовмісна ароматична гетероциклічна сполука |
| BR112014021897B1 (pt) * | 2012-03-08 | 2022-06-14 | Astellas Pharma Inc | Método, kit, conjunto de iniciadores e conjuntos de sondas para detectar um gene de fusão composto por um gene fgfr3 e um gene tacc3 |
-
2014
- 2014-08-26 AR ARP140103193A patent/AR097455A1/es unknown
- 2014-08-26 TW TW103129371A patent/TW201605452A/zh unknown
- 2014-08-27 EP EP14840047.6A patent/EP3040072A4/en not_active Withdrawn
- 2014-08-27 CA CA2922352A patent/CA2922352A1/en not_active Abandoned
- 2014-08-27 JP JP2015534246A patent/JPWO2015030021A1/ja active Pending
- 2014-08-27 US US14/914,955 patent/US20160199371A1/en not_active Abandoned
- 2014-08-27 SG SG11201601461RA patent/SG11201601461RA/en unknown
- 2014-08-27 AU AU2014312919A patent/AU2014312919A1/en not_active Abandoned
- 2014-08-27 RU RU2016106774A patent/RU2016106774A/ru not_active Application Discontinuation
- 2014-08-27 KR KR1020167007640A patent/KR20160040719A/ko not_active Withdrawn
- 2014-08-27 WO PCT/JP2014/072349 patent/WO2015030021A1/ja not_active Ceased
- 2014-08-27 MX MX2016002589A patent/MX2016002589A/es unknown
- 2014-08-27 CN CN201480047119.2A patent/CN105492009A/zh active Pending
- 2014-08-27 HK HK16107576.9A patent/HK1219432A1/zh unknown
-
2016
- 2016-02-21 IL IL244206A patent/IL244206A0/en unknown
- 2016-02-24 PH PH12016500372A patent/PH12016500372A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| RU2016106774A (ru) | 2017-10-03 |
| US20160199371A1 (en) | 2016-07-14 |
| HK1219432A1 (zh) | 2017-04-07 |
| EP3040072A1 (en) | 2016-07-06 |
| WO2015030021A1 (ja) | 2015-03-05 |
| EP3040072A4 (en) | 2017-03-29 |
| JPWO2015030021A1 (ja) | 2017-03-02 |
| KR20160040719A (ko) | 2016-04-14 |
| MX2016002589A (es) | 2016-06-14 |
| TW201605452A (zh) | 2016-02-16 |
| CA2922352A1 (en) | 2015-03-05 |
| PH12016500372A1 (en) | 2016-05-02 |
| CN105492009A (zh) | 2016-04-13 |
| IL244206A0 (en) | 2016-04-21 |
| AU2014312919A1 (en) | 2016-03-10 |
| SG11201601461RA (en) | 2016-03-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |