JP2022515197A - がんを治療するためのfgfr阻害剤としての7-((3,5-ジメトキシフェニル)アミノ)キノキサリン誘導体 - Google Patents
がんを治療するためのfgfr阻害剤としての7-((3,5-ジメトキシフェニル)アミノ)キノキサリン誘導体 Download PDFInfo
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- JP2022515197A JP2022515197A JP2021536037A JP2021536037A JP2022515197A JP 2022515197 A JP2022515197 A JP 2022515197A JP 2021536037 A JP2021536037 A JP 2021536037A JP 2021536037 A JP2021536037 A JP 2021536037A JP 2022515197 A JP2022515197 A JP 2022515197A
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- Prior art keywords
- fgfr
- cancer
- subject
- ring
- kinase
- 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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- 0 CC(C=C(C=C1)N(*)c2cc(O)cc(*)c2)C1=NC=C(C(CC=C12)=CC1=C2I)N Chemical compound CC(C=C(C=C1)N(*)c2cc(O)cc(*)c2)C1=NC=C(C(CC=C12)=CC1=C2I)N 0.000 description 30
- XJAPOARONZGMMH-UHFFFAOYSA-N C/[O]=C(\C1)/C=CCC1N Chemical compound C/[O]=C(\C1)/C=CCC1N XJAPOARONZGMMH-UHFFFAOYSA-N 0.000 description 1
- DTHSTXQPBHBITL-UHFFFAOYSA-N C=C(C(N=C)=O)C#N Chemical compound C=C(C(N=C)=O)C#N DTHSTXQPBHBITL-UHFFFAOYSA-N 0.000 description 1
- LBLTVIVLHICKBS-VMPITWQZSA-N CC(C)(C)/C=C(/C(C)=O)\C#N Chemical compound CC(C)(C)/C=C(/C(C)=O)\C#N LBLTVIVLHICKBS-VMPITWQZSA-N 0.000 description 1
- NBORFPQARHGRIV-UHFFFAOYSA-N CC(C)(C)OC(N(C1)CC1(C=O)OC)=O Chemical compound CC(C)(C)OC(N(C1)CC1(C=O)OC)=O NBORFPQARHGRIV-UHFFFAOYSA-N 0.000 description 1
- CQYHKQXSKLVNHE-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCN1c1ncc(B2OC(C)(C)C(C)(C)O2)c(C)c1)=O Chemical compound CC(C)(C)OC(N(CC1)CCN1c1ncc(B2OC(C)(C)C(C)(C)O2)c(C)c1)=O CQYHKQXSKLVNHE-UHFFFAOYSA-N 0.000 description 1
- ISDZPKWRXRFDGU-UHFFFAOYSA-N CC(C1)CN1I Chemical compound CC(C1)CN1I ISDZPKWRXRFDGU-UHFFFAOYSA-N 0.000 description 1
- XQOPUMVIPGTSNN-UHFFFAOYSA-N CC(CCC1)N1C#N Chemical compound CC(CCC1)N1C#N XQOPUMVIPGTSNN-UHFFFAOYSA-N 0.000 description 1
- DCTJGUZYXXIDRB-UHFFFAOYSA-N CCC(C(C(N)=C1N)=O)C1=O Chemical compound CCC(C(C(N)=C1N)=O)C1=O DCTJGUZYXXIDRB-UHFFFAOYSA-N 0.000 description 1
- IKLVINQONMOKIJ-UHFFFAOYSA-N CCCNC(C(C)Cl)=O Chemical compound CCCNC(C(C)Cl)=O IKLVINQONMOKIJ-UHFFFAOYSA-N 0.000 description 1
- MMOOOQAABWPBQJ-UHFFFAOYSA-N CCc1nc(C)c(C)cc1 Chemical compound CCc1nc(C)c(C)cc1 MMOOOQAABWPBQJ-UHFFFAOYSA-N 0.000 description 1
- IOKLYXDNQOPONA-BQYQJAHWSA-N CN(C)C/C=C/C(N(C1)CC1(C(N(CC1)CCC1[n]1ncc(-c2cnc(ccc(N(CC#C)c3cc(OC)cc(OC)c3)c3)c3n2)c1)=O)F)=O Chemical compound CN(C)C/C=C/C(N(C1)CC1(C(N(CC1)CCC1[n]1ncc(-c2cnc(ccc(N(CC#C)c3cc(OC)cc(OC)c3)c3)c3n2)c1)=O)F)=O IOKLYXDNQOPONA-BQYQJAHWSA-N 0.000 description 1
- FKDGWAOITYMYJG-UHFFFAOYSA-N CN(C)C1(CC1)[Zn] Chemical compound CN(C)C1(CC1)[Zn] FKDGWAOITYMYJG-UHFFFAOYSA-N 0.000 description 1
- RMDBTAYWYWJRIC-UHFFFAOYSA-N COC(CN(CC1)CCC1[n]1ncc(-c2cnc(ccc(Nc3cc(OC)cc(OC)c3)c3)c3n2)c1)(C1)CN1C(C=C)=O Chemical compound COC(CN(CC1)CCC1[n]1ncc(-c2cnc(ccc(Nc3cc(OC)cc(OC)c3)c3)c3n2)c1)(C1)CN1C(C=C)=O RMDBTAYWYWJRIC-UHFFFAOYSA-N 0.000 description 1
- HLRBIOMHENPNQT-UHFFFAOYSA-N COc1cc(Nc2cc3nc(-c4c[n](C(CC5)CCN5C(C(C5)CN5C(C=C)=O)=O)nc4)cnc3cc2)cc(OC)c1 Chemical compound COc1cc(Nc2cc3nc(-c4c[n](C(CC5)CCN5C(C(C5)CN5C(C=C)=O)=O)nc4)cnc3cc2)cc(OC)c1 HLRBIOMHENPNQT-UHFFFAOYSA-N 0.000 description 1
- BUHWDTBBHCMMON-UHFFFAOYSA-N COc1cc(OC)cc(Nc2cc3nc(-c4c[n](C5CCNCC5)nc4)cnc3cc2)c1 Chemical compound COc1cc(OC)cc(Nc2cc3nc(-c4c[n](C5CCNCC5)nc4)cnc3cc2)c1 BUHWDTBBHCMMON-UHFFFAOYSA-N 0.000 description 1
- XMXBFJRKSZEPNE-UHFFFAOYSA-N CSCCNC(CCl)=O Chemical compound CSCCNC(CCl)=O XMXBFJRKSZEPNE-UHFFFAOYSA-N 0.000 description 1
- MHXRWANRWZZMHA-UHFFFAOYSA-N NC(CCC=C1)C1=O Chemical compound NC(CCC=C1)C1=O MHXRWANRWZZMHA-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- 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
- C07D401/14—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 three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D403/14—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 three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862781977P | 2018-12-19 | 2018-12-19 | |
| US62/781,977 | 2018-12-19 | ||
| PCT/US2019/066478 WO2020131674A1 (en) | 2018-12-19 | 2019-12-16 | 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022515197A true JP2022515197A (ja) | 2022-02-17 |
| JP2022515197A5 JP2022515197A5 (https=) | 2022-12-20 |
| JPWO2020131674A5 JPWO2020131674A5 (https=) | 2022-12-20 |
Family
ID=69165616
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021536037A Ceased JP2022515197A (ja) | 2018-12-19 | 2019-12-16 | がんを治療するためのfgfr阻害剤としての7-((3,5-ジメトキシフェニル)アミノ)キノキサリン誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US12351571B2 (https=) |
| EP (1) | EP3898615A1 (https=) |
| JP (1) | JP2022515197A (https=) |
| CN (1) | CN113474337A (https=) |
| WO (1) | WO2020131674A1 (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2704744T3 (es) | 2012-06-13 | 2019-03-19 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| MX373169B (es) | 2015-02-20 | 2020-04-24 | Incyte Holdings Corp | Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr). |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| 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 |
| 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 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | 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 |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021153703A1 (ja) * | 2020-01-31 | 2021-08-05 | 国立大学法人京都大学 | 軟骨形成異常症の治療 |
| 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 |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2023175185A1 (en) | 2022-03-17 | 2023-09-21 | Forx Therapeutics Ag | 2,4-dioxo-1,4-dihydroquinazoline derivatives as parg inhibitors for the treatment of cancer |
| JP2025537185A (ja) * | 2022-11-10 | 2025-11-14 | アジレント・テクノロジーズ・インク | 生細胞を分析するための機器および方法 |
| CN116159142B (zh) * | 2023-03-23 | 2026-02-17 | 上海市光华中西医结合医院(上海市光华医院) | 一组fgfr抑制剂在制备治疗类风湿性关节炎药物中的应用 |
| WO2025046148A1 (en) | 2023-09-01 | 2025-03-06 | Forx Therapeutics Ag | Novel parg inhibitors |
| CN120860030B (zh) * | 2025-09-29 | 2026-01-27 | 四川大学华西医院 | Fgfr抑制剂在制备治疗颅咽管瘤的药物中的用途 |
Citations (3)
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| JP2013528580A (ja) * | 2010-04-30 | 2013-07-11 | アステックス、セラピューティックス、リミテッド | ピラゾリルキナゾリンキナーゼ阻害剤 |
| JP2014534212A (ja) * | 2011-10-28 | 2014-12-18 | アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited | Fgfrキナーゼ阻害を介した抗癌ベンゾピラジン |
| WO2018040885A1 (zh) * | 2016-09-01 | 2018-03-08 | 南京药捷安康生物科技有限公司 | 成纤维细胞生长因子受体抑制剂及其用途 |
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- 2019-12-16 CN CN201980092586.XA patent/CN113474337A/zh active Pending
- 2019-12-16 JP JP2021536037A patent/JP2022515197A/ja not_active Ceased
- 2019-12-16 US US17/416,119 patent/US12351571B2/en active Active
- 2019-12-16 WO PCT/US2019/066478 patent/WO2020131674A1/en not_active Ceased
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| JP2013528580A (ja) * | 2010-04-30 | 2013-07-11 | アステックス、セラピューティックス、リミテッド | ピラゾリルキナゾリンキナーゼ阻害剤 |
| JP2014534212A (ja) * | 2011-10-28 | 2014-12-18 | アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited | Fgfrキナーゼ阻害を介した抗癌ベンゾピラジン |
| WO2018040885A1 (zh) * | 2016-09-01 | 2018-03-08 | 南京药捷安康生物科技有限公司 | 成纤维细胞生长因子受体抑制剂及其用途 |
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| EP3898615A1 (en) | 2021-10-27 |
| CN113474337A (zh) | 2021-10-01 |
| US12351571B2 (en) | 2025-07-08 |
| WO2020131674A1 (en) | 2020-06-25 |
| US20220041579A1 (en) | 2022-02-10 |
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