JP6716586B2 - Ｆｇｆｒ４阻害剤としての二環式複素環 - Google Patents
Ｆｇｆｒ４阻害剤としての二環式複素環 Download PDFInfo
- Publication number
- JP6716586B2 JP6716586B2 JP2017543981A JP2017543981A JP6716586B2 JP 6716586 B2 JP6716586 B2 JP 6716586B2 JP 2017543981 A JP2017543981 A JP 2017543981A JP 2017543981 A JP2017543981 A JP 2017543981A JP 6716586 B2 JP6716586 B2 JP 6716586B2
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- JP
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- Prior art keywords
- methyl
- difluoro
- dimethoxyphenyl
- alkyl
- oxo
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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Classifications
-
- 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
-
- 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
- A61K31/4353—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
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D471/10—Spiro-condensed systems
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)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2020100899A JP6903796B2 (ja) | 2015-02-20 | 2020-06-10 | Ｆｇｆｒ４阻害剤としての二環式複素環 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562118699P | 2015-02-20 | 2015-02-20 | |
| US62/118,699 | 2015-02-20 | ||
| US201562192661P | 2015-07-15 | 2015-07-15 | |
| US62/192,661 | 2015-07-15 | ||
| PCT/US2016/018770 WO2016134314A1 (en) | 2015-02-20 | 2016-02-19 | Bicyclic heterocycles as fgfr4 inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020100899A Division JP6903796B2 (ja) | 2015-02-20 | 2020-06-10 | Ｆｇｆｒ４阻害剤としての二環式複素環 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018507214A JP2018507214A (ja) | 2018-03-15 |
| JP2018507214A5 JP2018507214A5 (enExample) | 2019-04-11 |
| JP6716586B2 true JP6716586B2 (ja) | 2020-07-01 |
Family
ID=55697447
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017543981A Active JP6716586B2 (ja) | 2015-02-20 | 2016-02-19 | Ｆｇｆｒ４阻害剤としての二環式複素環 |
| JP2020100899A Active JP6903796B2 (ja) | 2015-02-20 | 2020-06-10 | Ｆｇｆｒ４阻害剤としての二環式複素環 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020100899A Active JP6903796B2 (ja) | 2015-02-20 | 2020-06-10 | Ｆｇｆｒ４阻害剤としての二環式複素環 |
Country Status (23)
| Country | Link |
|---|---|
| US (5) | US9890156B2 (enExample) |
| EP (1) | EP3259270A1 (enExample) |
| JP (2) | JP6716586B2 (enExample) |
| KR (1) | KR102643180B1 (enExample) |
| CN (2) | CN107438608B (enExample) |
| AU (2) | AU2016219816B2 (enExample) |
| BR (1) | BR112017017727B1 (enExample) |
| CA (1) | CA2976788C (enExample) |
| CL (1) | CL2017002122A1 (enExample) |
| CO (1) | CO2017008824A2 (enExample) |
| CR (1) | CR20170388A (enExample) |
| EA (1) | EA201791867A1 (enExample) |
| EC (1) | ECSP17062716A (enExample) |
| IL (1) | IL253869B (enExample) |
| MA (1) | MA41551A (enExample) |
| MX (2) | MX2021006443A (enExample) |
| MY (1) | MY187265A (enExample) |
| PE (1) | PE20180050A1 (enExample) |
| PH (2) | PH12021550394A1 (enExample) |
| SG (2) | SG10201907582WA (enExample) |
| TW (2) | TWI740818B (enExample) |
| UA (1) | UA121492C2 (enExample) |
| WO (1) | WO2016134314A1 (enExample) |
Families Citing this family (40)
| 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 |
| CA2876689C (en) | 2012-06-13 | 2022-04-26 | Incyte Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| NZ703495A (en) | 2012-07-11 | 2018-02-23 | Blueprint Medicines Corp | Inhibitors of the fibroblast growth factor receptor |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| PT3395814T (pt) | 2013-10-25 | 2022-07-27 | Blueprint Medicines Corp | Inibidores do recetor do fator de crescimento de fibroblastos |
| WO2015108992A1 (en) | 2014-01-15 | 2015-07-23 | Blueprint Medicines Corporation | Heterobicyclic compounds and their use as fgfr4 receptor inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CA2976790C (en) | 2015-02-20 | 2024-02-27 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CN110022900A (zh) | 2016-09-08 | 2019-07-16 | 蓝图药品公司 | 成纤维细胞生长因子受体4抑制剂与细胞周期蛋白依赖性激酶抑制剂的组合 |
| WO2018055503A1 (en) | 2016-09-20 | 2018-03-29 | Novartis Ag | Combination comprising a pd-1 antagonist and an fgfr4 inhibitor |
| JP7394623B2 (ja) | 2016-11-02 | 2023-12-08 | ノバルティス アーゲー | Ｆｇｆｒ４インヒビターおよび胆汁酸捕捉薬の組合せ |
| AR111960A1 (es) * | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| CN110997637B (zh) | 2017-09-05 | 2022-09-27 | 保仕健生物科技(上海)有限公司 | 芳香类衍生物、其制备方法及其在医药上的应用 |
| HUE066282T2 (hu) * | 2018-03-30 | 2024-07-28 | Servier Lab | Heterobiciklusos MAT2A-gátlók és eljárások rák kezelésében történõ alkalmazásukra |
| RS66310B1 (sr) | 2018-05-04 | 2025-01-31 | Incyte Corp | Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu |
| KR102956194B1 (ko) | 2018-05-04 | 2026-04-23 | 인사이트 코포레이션 | Fgfr 억제제의 염 |
| 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 |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| GEP20247679B (en) | 2019-10-14 | 2024-10-10 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| GB201915828D0 (en) * | 2019-10-31 | 2019-12-18 | Cancer Research Tech Ltd | Compounds, compositions and therapeutic uses thereof |
| CN112759593A (zh) | 2019-11-01 | 2021-05-07 | 北京伯汇生物技术有限公司 | 桥环并醛基吡啶衍生物及其应用 |
| MX2022006691A (es) | 2019-12-04 | 2022-09-19 | Incyte Corp | Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr). |
| WO2021113479A1 (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 |
| EP4178955A1 (en) | 2020-07-11 | 2023-05-17 | Pfizer Inc. | Antiviral heteroaryl ketone derivatives |
| US11351149B2 (en) | 2020-09-03 | 2022-06-07 | Pfizer Inc. | Nitrile-containing antiviral compounds |
| AU2021436754B2 (en) * | 2021-03-26 | 2024-11-07 | Apeloa Pharmaceutical Co., Ltd. | Bicyclic heterocyclic fgfr4 inhibitor, pharmaceutical composition and preparation comprising same, and application thereof |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313610A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之三環雜環 |
| MX2024006113A (es) | 2021-11-22 | 2024-07-29 | Incyte Corp | Terapia de combinación que comprende un inhibidor del receptor del factor de crecimiento de fibroblastos (fgfr) y un inhibidor del sarcoma de rata de kirsten (kras). |
| TW202442224A (zh) * | 2023-03-20 | 2024-11-01 | 香港商英矽智能科技知識產權有限公司 | Fgfr2與fgfr3之抑制劑及其用途 |
| WO2024242495A1 (ko) * | 2023-05-25 | 2024-11-28 | 주식회사 매직불릿테라퓨틱스 | 단백질 키나아제 억제용 신규 화합물 및 이를 포함하는 약학조성물 |
| EP4509142A1 (en) | 2023-08-16 | 2025-02-19 | Ona Therapeutics S.L. | Fgfr4 as target in cancer treatment |
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