KR101914720B1 - 암 질환의 치료를 위한 fgfr 키나제 억제제로서의 치환된 벤조피라진 유도체 - Google Patents
암 질환의 치료를 위한 fgfr 키나제 억제제로서의 치환된 벤조피라진 유도체 Download PDFInfo
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- KR101914720B1 KR101914720B1 KR1020137016924A KR20137016924A KR101914720B1 KR 101914720 B1 KR101914720 B1 KR 101914720B1 KR 1020137016924 A KR1020137016924 A KR 1020137016924A KR 20137016924 A KR20137016924 A KR 20137016924A KR 101914720 B1 KR101914720 B1 KR 101914720B1
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- 0 C*1*=CC(C(*2)=C*c(cc3)c2cc3C(c2cc([*+])cc(*)c2)=O)=C1 Chemical compound C*1*=CC(C(*2)=C*c(cc3)c2cc3C(c2cc([*+])cc(*)c2)=O)=C1 0.000 description 10
- PZRCRLJNTJXTCR-UHFFFAOYSA-N CC(C)NC(CC(c1cc2nc(-c3c[n](C)nc3)cnc2cc1)c1cc(OC)cc(OC)c1)=O Chemical compound CC(C)NC(CC(c1cc2nc(-c3c[n](C)nc3)cnc2cc1)c1cc(OC)cc(OC)c1)=O PZRCRLJNTJXTCR-UHFFFAOYSA-N 0.000 description 1
- RNXYZEKEIBUPMY-CIAFOILYSA-N CCOC(/C=C(\c1cc2nc(-c3c[n](C)nc3)cnc2cc1)/c1cc(OC)cc(OC)c1)=O Chemical compound CCOC(/C=C(\c1cc2nc(-c3c[n](C)nc3)cnc2cc1)/c1cc(OC)cc(OC)c1)=O RNXYZEKEIBUPMY-CIAFOILYSA-N 0.000 description 1
- MOHAWXZSVRDMSN-UHFFFAOYSA-N CCOC(CC(c1cc2nc(-c3c[n](C)nc3)cnc2cc1)c1cc(OC)cc(OC)c1)=O Chemical compound CCOC(CC(c1cc2nc(-c3c[n](C)nc3)cnc2cc1)c1cc(OC)cc(OC)c1)=O MOHAWXZSVRDMSN-UHFFFAOYSA-N 0.000 description 1
- NGBKIVOMFTXPDW-GZIVZEMBSA-N CN(C)C/C=C(\c(cc1)cc2c1ncc(-c1c[n](C)nc1)n2)/c1cc(OC)cc(OC)c1 Chemical compound CN(C)C/C=C(\c(cc1)cc2c1ncc(-c1c[n](C)nc1)n2)/c1cc(OC)cc(OC)c1 NGBKIVOMFTXPDW-GZIVZEMBSA-N 0.000 description 1
- WNNUUWUDLSDDIG-IOXNKQMXSA-N C[n]1ncc(-c2nc(cc(cc3)/C(/c4cc(OC)cc(OC)c4)=C/C#N)c3nc2)c1 Chemical compound C[n]1ncc(-c2nc(cc(cc3)/C(/c4cc(OC)cc(OC)c4)=C/C#N)c3nc2)c1 WNNUUWUDLSDDIG-IOXNKQMXSA-N 0.000 description 1
Classifications
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines 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
- A61K31/495—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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- 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
- 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
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41774410P | 2010-11-29 | 2010-11-29 | |
| US61/417,744 | 2010-11-29 | ||
| GBGB1020179.6A GB201020179D0 (en) | 2010-11-29 | 2010-11-29 | New compounds |
| GB1020179.6 | 2010-11-29 | ||
| PCT/GB2011/052356 WO2012073017A1 (en) | 2010-11-29 | 2011-11-29 | Substituted benzopyrazin derivatives as fgfr kinase inhibitors for the treatment of cancer diseases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20130132509A KR20130132509A (ko) | 2013-12-04 |
| KR101914720B1 true KR101914720B1 (ko) | 2018-11-05 |
Family
ID=43500774
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020137016924A Active KR101914720B1 (ko) | 2010-11-29 | 2011-11-29 | 암 질환의 치료를 위한 fgfr 키나제 억제제로서의 치환된 벤조피라진 유도체 |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US9290478B2 (enExample) |
| EP (1) | EP2646432B1 (enExample) |
| JP (1) | JP5868992B2 (enExample) |
| KR (1) | KR101914720B1 (enExample) |
| CN (1) | CN103370314B (enExample) |
| AU (1) | AU2011334624B2 (enExample) |
| BR (1) | BR112013013435B1 (enExample) |
| CA (1) | CA2819009C (enExample) |
| DK (1) | DK2646432T3 (enExample) |
| ES (1) | ES2541493T3 (enExample) |
| GB (1) | GB201020179D0 (enExample) |
| HR (1) | HRP20150692T8 (enExample) |
| HU (1) | HUE025091T2 (enExample) |
| MX (1) | MX2013005897A (enExample) |
| RU (1) | RU2602233C2 (enExample) |
| SI (1) | SI2646432T1 (enExample) |
| SM (1) | SMT201500191B (enExample) |
| WO (1) | WO2012073017A1 (enExample) |
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| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| JP6002223B2 (ja) * | 2011-08-26 | 2016-10-05 | ニューファーマ, インコーポレイテッド | 特定の化学的実体、組成物、および方法 |
| EP3332785B1 (en) | 2011-09-14 | 2020-05-06 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| US9249110B2 (en) | 2011-09-21 | 2016-02-02 | Neupharma, Inc. | Substituted quinoxalines as B-raf kinase inhibitors |
| WO2013049701A1 (en) | 2011-09-30 | 2013-04-04 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| EP2806874B1 (en) | 2012-01-25 | 2017-11-15 | Neupharma, Inc. | Quinoxaline-oxy-phenyl derivatives as kinase inhibitors |
| GB201209609D0 (en) * | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| SI2861595T1 (sl) | 2012-06-13 | 2017-04-26 | Incyte Holdings Corporation | Substituirane triciklične spojine kot inhibitorji fgfr |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| WO2014047648A1 (en) | 2012-09-24 | 2014-03-27 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| WO2014044846A1 (en) | 2012-09-24 | 2014-03-27 | Evotec (Uk) Ltd. | 3-(aryl- or heteroaryl-amino)-7-(3,5-dimethoxyphenyl)isoquinoline derivatives as fgfr inhibitors useful for the treatment of proliferative disorders or dysplasia |
| WO2014075077A1 (en) | 2012-11-12 | 2014-05-15 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
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| 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 |
| EP2924038A1 (en) | 2014-03-24 | 2015-09-30 | Evotec (UK) Ltd. | Preparation of pyrrolo[2,3-b]pyrazine and pyrrolo[2,3-b]pyridine derivatives as FGFR inhibitors |
| HUE053653T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR inhibitor és IGF1R inhibitor kombinációi |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| MX370099B (es) | 2014-03-26 | 2019-12-02 | Astex Therapeutics Ltd | Combinación que comprende un inhibidor de fgfr y un inhibidor de cmet para el tratamiento del cáncer. |
| MX369646B (es) | 2014-08-18 | 2019-11-15 | Eisai R&D Man Co Ltd | Sal de derivado de piridina monociclico y su cristal. |
| CN113957146A (zh) * | 2014-09-26 | 2022-01-21 | 詹森药业有限公司 | 使用fgfr突变基因组鉴定将对用fgfr抑制剂进行治疗有反应的癌症患者 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
| SG10201913036RA (en) | 2015-02-20 | 2020-02-27 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016152907A1 (ja) | 2015-03-25 | 2016-09-29 | 国立研究開発法人国立がん研究センター | 胆管癌治療剤 |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| JP2018524010A (ja) * | 2015-07-24 | 2018-08-30 | デバイオファーム インターナショナル エスエイ | Fgfr発現とfgfr阻害剤に対する感受性 |
| WO2017050865A1 (en) * | 2015-09-23 | 2017-03-30 | Janssen Pharmaceutica Nv | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| JP6898919B2 (ja) | 2015-09-23 | 2021-07-07 | ヤンセン ファーマシューティカ エヌ.ベー. | 新規化合物 |
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| KR20130132509A (ko) | 2013-12-04 |
| SI2646432T1 (sl) | 2015-08-31 |
| CN103370314B (zh) | 2015-10-21 |
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| BR112013013435A2 (pt) | 2016-10-11 |
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| DK2646432T3 (en) | 2015-07-13 |
| MX2013005897A (es) | 2013-10-25 |
| CN103370314A (zh) | 2013-10-23 |
| US20160031856A1 (en) | 2016-02-04 |
| US9856236B2 (en) | 2018-01-02 |
| HRP20150692T1 (hr) | 2015-08-14 |
| WO2012073017A1 (en) | 2012-06-07 |
| HUE025091T2 (en) | 2016-01-28 |
| SMT201500191B (it) | 2015-09-07 |
| JP5868992B2 (ja) | 2016-02-24 |
| US20130267525A1 (en) | 2013-10-10 |
| ES2541493T3 (es) | 2015-07-21 |
| JP2013543883A (ja) | 2013-12-09 |
| EP2646432A1 (en) | 2013-10-09 |
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