ES2756748T3 - Uso de derivados de piridilo bicíclicos de anillo fusionado como inhibidores de fgfr4 - Google Patents
Uso de derivados de piridilo bicíclicos de anillo fusionado como inhibidores de fgfr4 Download PDFInfo
- Publication number
- ES2756748T3 ES2756748T3 ES15781518T ES15781518T ES2756748T3 ES 2756748 T3 ES2756748 T3 ES 2756748T3 ES 15781518 T ES15781518 T ES 15781518T ES 15781518 T ES15781518 T ES 15781518T ES 2756748 T3 ES2756748 T3 ES 2756748T3
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- Prior art keywords
- alkyl
- fgfr4
- ring
- dihydro
- carboxamide
- Prior art date
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- 101150082429 FGFR4 gene Proteins 0.000 title 1
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- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 42
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- 150000001860 citric acid derivatives Chemical class 0.000 claims description 3
- HXNZAVZZAPTZBP-UHFFFAOYSA-N N-(5-cyanopyridin-2-yl)-7-formyl-6-(hydroxymethyl)-3,4-dihydro-2H-1,8-naphthyridine-1-carboxamide Chemical compound OCc1cc2CCCN(C(=O)Nc3ccc(cn3)C#N)c2nc1C=O HXNZAVZZAPTZBP-UHFFFAOYSA-N 0.000 claims 1
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- BJEPYKJPYRNKOW-UHFFFAOYSA-L malate(2-) Chemical group [O-]C(=O)C(O)CC([O-])=O BJEPYKJPYRNKOW-UHFFFAOYSA-L 0.000 claims 1
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 abstract description 5
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Classifications
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Life Sciences & Earth Sciences (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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| PCT/US2015/053677 WO2016054483A1 (en) | 2014-10-03 | 2015-10-02 | Use of ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors |
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| CN113105454B (zh) * | 2016-05-20 | 2022-10-11 | 江苏豪森药业集团有限公司 | Fgfr4抑制剂、其制备方法和应用 |
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| US11229643B2 (en) * | 2016-11-02 | 2022-01-25 | Novartis Ag | Combinations of FGFR4 inhibitors and bile acid sequestrants |
| TWI723480B (zh) * | 2018-07-27 | 2021-04-01 | 大陸商北京加科思新藥研發有限公司 | 用作fgfr4抑制劑的稠環衍生物 |
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| JP6576325B2 (ja) | 2013-03-15 | 2019-09-18 | セルジーン シーエーアール エルエルシー | ヘテロアリール化合物およびそれらの使用 |
| LT2986610T (lt) | 2013-04-19 | 2018-04-10 | Incyte Holdings Corporation | Bicikliniai heterociklai, kaip fgfr inhibitoriai |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| AU2014287209B2 (en) | 2013-07-09 | 2019-01-24 | Dana-Farber Cancer Institute, Inc. | Kinase inhibitors for the treatment of disease |
| AR097455A1 (es) | 2013-08-28 | 2016-03-16 | Astellas Pharma Inc | Composición farmacéutica que contiene compuesto de pirimidina como un ingrediente activo |
| SMT201800379T1 (it) | 2013-10-18 | 2018-09-13 | Eisai R&D Man Co Ltd | Inibitori di fgfr4 della pirimidina |
| DK3395814T3 (da) | 2013-10-25 | 2022-07-04 | Blueprint Medicines Corp | Hæmmere af fibroblastvækstfaktorreceptoren |
| 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 |
| WO2015195509A2 (en) | 2014-06-16 | 2015-12-23 | Ngm Biopharmaceuticals, Inc. | Methods and uses for modulating bile acid homeostasis and treatment of bile acid disorders and diseases |
| WO2016054483A1 (en) * | 2014-10-03 | 2016-04-07 | Novartis Ag | Use of ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors |
| CN107787226A (zh) * | 2015-03-25 | 2018-03-09 | 诺华股份有限公司 | 药物组合 |
| 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 |
| US11229643B2 (en) | 2016-11-02 | 2022-01-25 | Novartis Ag | Combinations of FGFR4 inhibitors and bile acid sequestrants |
-
2015
- 2015-10-02 WO PCT/US2015/053677 patent/WO2016054483A1/en not_active Ceased
- 2015-10-02 JP JP2017517705A patent/JP6585167B2/ja active Active
- 2015-10-02 EP EP15781518.4A patent/EP3200786B1/en active Active
- 2015-10-02 ES ES15781518T patent/ES2756748T3/es active Active
- 2015-10-02 US US15/516,443 patent/US20180185341A1/en not_active Abandoned
- 2015-10-02 PL PL15781518T patent/PL3200786T3/pl unknown
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2018
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2019
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- 2019-09-04 JP JP2019161051A patent/JP6794514B2/ja active Active
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| US20190231760A1 (en) | 2019-08-01 |
| PL3200786T3 (pl) | 2020-03-31 |
| US10507201B2 (en) | 2019-12-17 |
| US20180185341A1 (en) | 2018-07-05 |
| US10463653B2 (en) | 2019-11-05 |
| JP2019218398A (ja) | 2019-12-26 |
| WO2016054483A1 (en) | 2016-04-07 |
| JP6585167B2 (ja) | 2019-10-02 |
| EP3200786A1 (en) | 2017-08-09 |
| JP6794514B2 (ja) | 2020-12-02 |
| JP2017530154A (ja) | 2017-10-12 |
| EP3200786B1 (en) | 2019-08-28 |
| US20190076412A1 (en) | 2019-03-14 |
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