RU2602233C2 - Замещенные бензопиразиновые производные в качестве ингибиторов fgfr-киназ для лечения раковых заболеваний - Google Patents
Замещенные бензопиразиновые производные в качестве ингибиторов fgfr-киназ для лечения раковых заболеваний Download PDFInfo
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- RU2602233C2 RU2602233C2 RU2013129820/04A RU2013129820A RU2602233C2 RU 2602233 C2 RU2602233 C2 RU 2602233C2 RU 2013129820/04 A RU2013129820/04 A RU 2013129820/04A RU 2013129820 A RU2013129820 A RU 2013129820A RU 2602233 C2 RU2602233 C2 RU 2602233C2
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- 0 C[n]1ncc(-c2nc(cc(C(*)c3cc(*)cc(*)c3)cc3)c3nc2)c1 Chemical compound C[n]1ncc(-c2nc(cc(C(*)c3cc(*)cc(*)c3)cc3)c3nc2)c1 0.000 description 3
- WBPOSVOTKNOXMD-UHFFFAOYSA-N C[n]1ncc(-c2cnc(ccc(C(CC#N)c3cc(OC)cc(OC)c3)c3)c3n2)c1 Chemical compound C[n]1ncc(-c2cnc(ccc(C(CC#N)c3cc(OC)cc(OC)c3)c3)c3n2)c1 WBPOSVOTKNOXMD-UHFFFAOYSA-N 0.000 description 1
- SGRCPJXYTPOORE-UHFFFAOYSA-N C[n]1ncc(-c2nc(cc(cc3)C(c4cc(OC)cc(OC)c4)=O)c3nc2)c1 Chemical compound C[n]1ncc(-c2nc(cc(cc3)C(c4cc(OC)cc(OC)c4)=O)c3nc2)c1 SGRCPJXYTPOORE-UHFFFAOYSA-N 0.000 description 1
Classifications
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- 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
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (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 | |
| GB1020179.6 | 2010-11-29 | ||
| US61/417,744 | 2010-11-29 | ||
| GBGB1020179.6A GB201020179D0 (en) | 2010-11-29 | 2010-11-29 | New compounds |
| 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 |
|---|---|
| RU2013129820A RU2013129820A (ru) | 2015-01-10 |
| RU2602233C2 true RU2602233C2 (ru) | 2016-11-10 |
Family
ID=43500774
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2013129820/04A RU2602233C2 (ru) | 2010-11-29 | 2011-11-29 | Замещенные бензопиразиновые производные в качестве ингибиторов fgfr-киназ для лечения раковых заболеваний |
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) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2771526C1 (ru) * | 2018-09-14 | 2022-05-05 | Аббиско Терапеутикс Ко., Лтд. | Ингибитор fgfr, метод его получения и его применение |
Families Citing this family (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2013032951A1 (en) | 2011-08-26 | 2013-03-07 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| AU2012308238B2 (en) | 2011-09-14 | 2017-05-25 | 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 |
| 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 |
| 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 |
| 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 |
| CA2876689C (en) | 2012-06-13 | 2022-04-26 | Incyte Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| 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 |
| CN104812389B (zh) | 2012-09-24 | 2020-07-17 | 润新生物公司 | 某些化学实体、组合物及方法 |
| US9725421B2 (en) | 2012-11-12 | 2017-08-08 | Neupharma, Inc. | Substituted quinoxalines as B-raf kinase inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| 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 |
| BR112016022056B1 (pt) | 2014-03-26 | 2023-04-11 | Astex Therapeutics Limited | Combinação, composição farmacêutica, uso de uma combinação ou uma composição farmacêutica, e, produto farmacêutico |
| US10736900B2 (en) | 2014-03-26 | 2020-08-11 | Astex Therapeutics Ltd | Combinations of an FGFR inhibitor and an IGF1R inhibitor |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| WO2016027781A1 (ja) | 2014-08-18 | 2016-02-25 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 単環ピリジン誘導体の塩およびその結晶 |
| SG11201702381QA (en) | 2014-09-26 | 2017-04-27 | Janssen Pharmaceutica Nv | Use of fgfr mutant gene panels in identifying cancer patients that will be responsive to treatment with an fgfr inhibitor |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| TWI719960B (zh) | 2015-02-10 | 2021-03-01 | 英商阿斯迪克治療公司 | 新穎組成物 |
| 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 |
| CN114984013A (zh) | 2015-03-25 | 2022-09-02 | 国立癌症研究中心 | 胆管癌治疗剂 |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| BR112018001438A2 (en) * | 2015-07-24 | 2018-12-04 | Debiopharm International S.A. | gffr expression and susceptibility to a gffr inhibitor |
| HUE050567T2 (hu) | 2015-09-23 | 2020-12-28 | Janssen Pharmaceutica Nv | Triciklusos heterociklusok rák kezelésére |
| 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 |
| EP3365335B1 (en) | 2015-10-23 | 2024-02-14 | Array Biopharma, Inc. | 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2h)-one compounds as inhibitors of fgfr tyrosine kinases |
| AU2016374441B2 (en) | 2015-12-17 | 2021-10-21 | Eisai R&D Management Co., Ltd. | Therapeutic agent for breast cancer |
| SG11201903091VA (en) * | 2016-10-10 | 2019-05-30 | Dev Ct Biotechnology | Quinoxaline compounds as type iii receptor tyrosine kinase inhibitors |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| BR112020017922A2 (pt) | 2018-03-28 | 2020-12-22 | Eisai R&D Management Co., Ltd. | Agente terapêutico para carcinoma hepatocelular |
| KR102956194B1 (ko) | 2018-05-04 | 2026-04-23 | 인사이트 코포레이션 | Fgfr 억제제의 염 |
| RS66310B1 (sr) | 2018-05-04 | 2025-01-31 | Incyte Corp | Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu |
| US12351571B2 (en) | 2018-12-19 | 2025-07-08 | Array Biopharma Inc. | Substituted quinoxaline compounds as inhibitors of FGFR tyrosine kinases |
| WO2020131627A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
| 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 |
| US11680061B2 (en) | 2019-08-08 | 2023-06-20 | Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. | Crystal forms C and E of pyrazin-2(1H)-one compound and preparation method therefor |
| 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 |
| WO2021113479A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| MX2022006691A (es) | 2019-12-04 | 2022-09-19 | Incyte Corp | Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr). |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| MX2023007793A (es) | 2020-12-30 | 2023-09-22 | Tyra Biosciences Inc | Compuestos de indazol como inhibidores de cinasas. |
| EP4297873A1 (en) | 2021-02-26 | 2024-01-03 | Tyra Biosciences, Inc. | Aminopyrimidine compounds and methods of their use |
| 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 |
| IL317558A (en) | 2022-06-29 | 2025-02-01 | Tyra Biosciences Inc | Indazole compounds |
| AU2023300357A1 (en) | 2022-06-29 | 2025-01-09 | Tyra Biosciences, Inc. | Polymorphic compounds and uses thereof |
| WO2024138112A1 (en) | 2022-12-22 | 2024-06-27 | Tyra Biosciences, Inc. | Indazole compounds |
| AU2024400764A1 (en) | 2023-12-15 | 2026-07-09 | Tyra Biosciences, Inc. | Indazole compounds for the treatment of cancer |
| WO2026035809A1 (en) | 2024-08-06 | 2026-02-12 | Tyra Biosciences, Inc. | Indazole compounds for the treatment of cancer |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008078091A1 (en) * | 2006-12-22 | 2008-07-03 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as fgfr inhibitors |
| WO2009019518A1 (en) * | 2007-08-09 | 2009-02-12 | Astrazeneca Ab | Pyrimidine compounds having a fgfr inhibitory effect |
| RU2377241C2 (ru) * | 2003-11-24 | 2009-12-27 | Ф.Хоффманн-Ля Рош Аг | Производные пиразоло-имидазопиримидина, обладающие антагонистической активностью в отношении кортикотропин-рилизинг фактора (crf) |
Family Cites Families (105)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2940972A (en) | 1957-06-27 | 1960-06-14 | Thomae Gmbh Dr K | Tri-and tetra-substituted pteridine derivatives |
| US4666828A (en) | 1984-08-15 | 1987-05-19 | The General Hospital Corporation | Test for Huntington's disease |
| US4683202A (en) | 1985-03-28 | 1987-07-28 | Cetus Corporation | Process for amplifying nucleic acid sequences |
| US4801531A (en) | 1985-04-17 | 1989-01-31 | Biotechnology Research Partners, Ltd. | Apo AI/CIII genomic polymorphisms predictive of atherosclerosis |
| US5272057A (en) | 1988-10-14 | 1993-12-21 | Georgetown University | Method of detecting a predisposition to cancer by the use of restriction fragment length polymorphism of the gene for human poly (ADP-ribose) polymerase |
| US5192659A (en) | 1989-08-25 | 1993-03-09 | Genetype Ag | Intron sequence analysis method for detection of adjacent and remote locus alleles as haplotypes |
| GB9125001D0 (en) | 1991-11-25 | 1992-01-22 | Ici Plc | Heterocyclic compounds |
| US5700823A (en) * | 1994-01-07 | 1997-12-23 | Sugen, Inc. | Treatment of platelet derived growth factor related disorders such as cancers |
| US6331555B1 (en) | 1995-06-01 | 2001-12-18 | University Of California | Treatment of platelet derived growth factor related disorders such as cancers |
| US6218529B1 (en) | 1995-07-31 | 2001-04-17 | Urocor, Inc. | Biomarkers and targets for diagnosis, prognosis and management of prostate, breast and bladder cancer |
| CA2744096C (en) | 1996-07-31 | 2013-07-30 | Laboratory Corporation Of America Holdings | Biomarkers and targets for diagnosis, prognosis and management of prostate disease |
| TW472045B (en) | 1996-09-25 | 2002-01-11 | Astra Ab | Protein kinase C inhibitor compounds, method for their preparation, pharmaceutical composition thereof and intermediate used for their preparation |
| ES2235331T3 (es) | 1997-05-28 | 2005-07-01 | Aventis Pharmaceuticals Inc | Compuestos quinolina y quinoxalina que inhiben el factor de crecimiento derivado de plaquetas y/o tirosina quinasas p561ck. |
| UA71555C2 (en) | 1997-10-06 | 2004-12-15 | Zentaris Gmbh | Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives |
| AU3033500A (en) | 1999-01-15 | 2000-08-01 | Agouron Pharmaceuticals, Inc. | Non-peptide glp-1 agonists |
| JP2003509425A (ja) | 1999-09-15 | 2003-03-11 | ワーナー−ランバート・カンパニー | キナーゼ阻害剤としてのプテリジノン |
| DE10013318A1 (de) | 2000-03-17 | 2001-09-20 | Merck Patent Gmbh | Formulierung enthaltend Chinoxalinderivate |
| WO2002076985A1 (en) | 2001-03-23 | 2002-10-03 | Smithkline Beecham Corporation | Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases |
| JP4286146B2 (ja) | 2001-12-18 | 2009-06-24 | メルク エンド カムパニー インコーポレーテッド | メタボトロピックグルタミン酸受容体−５のヘテロアリール置換ピラゾール系調節剤 |
| ATE446093T1 (de) | 2001-12-24 | 2009-11-15 | Astrazeneca Ab | Substituierte chinazolin-derivate als aurora- kinase inhibitoren |
| JP2003213463A (ja) | 2002-01-17 | 2003-07-30 | Sumitomo Chem Co Ltd | 金属腐食防止剤および洗浄液 |
| US6962995B2 (en) | 2002-07-10 | 2005-11-08 | E. I. Du Pont De Nemours And Company | Charge transport compositions and electronic devices made with such compositions |
| US7825132B2 (en) | 2002-08-23 | 2010-11-02 | Novartis Vaccines And Diagnostics, Inc. | Inhibition of FGFR3 and treatment of multiple myeloma |
| MXPA05003477A (es) | 2002-10-03 | 2005-07-22 | Targegen Inc | Agentes vasculo-estaticos y metodos de uso de los mismos. |
| AR043059A1 (es) | 2002-11-12 | 2005-07-13 | Bayer Pharmaceuticals Corp | Derivados de indolil pirazinona utiles para el tratamiento de trastornos hiper-proliferativos |
| US7098332B2 (en) | 2002-12-20 | 2006-08-29 | Hoffmann-La Roche Inc. | 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones |
| EP1590341B1 (en) | 2003-01-17 | 2009-06-17 | Warner-Lambert Company LLC | 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation |
| WO2004098494A2 (en) | 2003-04-30 | 2004-11-18 | Cytokinetics, Inc. | Compounds, compositions, and methods |
| CN102584813B (zh) | 2003-05-14 | 2016-07-06 | Ngc药物公司 | 化合物及其在调节淀粉样蛋白β中的用途 |
| DE10323345A1 (de) | 2003-05-23 | 2004-12-16 | Zentaris Gmbh | Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren |
| WO2004104003A1 (de) | 2003-05-23 | 2004-12-02 | Zentaris Gmbh | Neue pyridopyrazine und deren verwendung als modulatoren von kinasen |
| WO2005007099A2 (en) | 2003-07-10 | 2005-01-27 | Imclone Systems Incorporated | Pkb inhibitors as anti-tumor agents |
| EP1646383A4 (en) | 2003-07-21 | 2009-03-25 | Bethesda Pharmaceuticals Inc | DESIGN AND SYNTHESIS OF OPTIMIZED LIGANDS FOR PPAR |
| PT1673092E (pt) | 2003-10-17 | 2007-11-23 | 4 Aza Ip Nv | ''derivados de pteridina substituídos com heterociclos e sua utilização em terapia'' |
| JP4823914B2 (ja) | 2003-11-07 | 2011-11-24 | ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド | Ｆｇｆｒ３の阻害および多発性骨髄腫の治療 |
| NZ546991A (en) | 2003-11-20 | 2010-01-29 | Janssen Pharmaceutica Nv | 6-Alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2-quinoxalinones as PARP inhibitors |
| EP2228369A1 (en) | 2003-12-23 | 2010-09-15 | Astex Therapeutics Ltd. | Pyrazole derivatives as protein kinase modulators |
| US7098222B2 (en) | 2004-05-12 | 2006-08-29 | Abbott Laboratories | Bicyclic-substituted amines having cyclic-substituted monocyclic substituents |
| US7205316B2 (en) | 2004-05-12 | 2007-04-17 | Abbott Laboratories | Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands |
| US20090118261A1 (en) | 2004-08-31 | 2009-05-07 | Astrazeneca Ab | Quinazolinone derivatives and their use as b-raf inhibitors |
| KR20080075235A (ko) | 2004-10-14 | 2008-08-14 | 에프. 호프만-라 로슈 아게 | Ｃｄｋ1 항증식성 활성을 갖는 1,5-나프티리딘 아졸리디논 |
| NZ555334A (en) | 2004-12-24 | 2010-05-28 | Spinifex Pharm Pty Ltd | Method of treatment or prophylaxis of a neuropathic condition using AT2 receptor antagonist |
| CA2597447C (en) | 2005-02-14 | 2014-03-25 | Bionomics Limited | Novel tubulin polymerisation inhibitors |
| EP1853261B1 (de) | 2005-03-03 | 2017-01-11 | Universität des Saarlandes | Selektive hemmstoffe humaner corticoidsynthasen |
| AU2006247833A1 (en) | 2005-05-12 | 2006-11-23 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| BRPI0611521A2 (pt) | 2005-05-18 | 2010-09-14 | Wyeth Corp | inibidores de 4,6-diamino-[1,7]naftiridina-3-carbonitrila de quìnase tpl2 e métodos de fabricação e uso dos mesmos |
| GB0513692D0 (en) | 2005-07-04 | 2005-08-10 | Karobio Ab | Novel pharmaceutical compositions |
| AU2006313701B2 (en) | 2005-11-11 | 2012-05-31 | Aeterna Zentaris Gmbh | Novel pyridopyrazines and their use as modulators of kinases |
| US8217042B2 (en) | 2005-11-11 | 2012-07-10 | Zentaris Gmbh | Pyridopyrazines and their use as modulators of kinases |
| EP1790342A1 (de) | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
| RS55630B1 (sr) | 2005-12-21 | 2017-06-30 | Janssen Pharmaceutica Nv | Triazolopiridazini kao modulatori tirozin kinaze |
| WO2007125405A2 (en) | 2006-05-01 | 2007-11-08 | Pfizer Products Inc. | Substituted 2-amino-fused heterocyclic compounds |
| GB0609621D0 (en) | 2006-05-16 | 2006-06-21 | Astrazeneca Ab | Novel co-crystal |
| WO2007135027A1 (de) | 2006-05-24 | 2007-11-29 | Boehringer Ingelheim International Gmbh | Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind |
| AU2007271187A1 (en) | 2006-07-03 | 2008-01-10 | Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek En Patientenzorg | Fused bicyclic compounds interacting with the histamine H4 receptor |
| JP2008127446A (ja) | 2006-11-20 | 2008-06-05 | Canon Inc | １，５−ナフチリジン化合物及び有機発光素子 |
| EP2104501B1 (en) | 2006-12-13 | 2014-03-12 | Merck Sharp & Dohme Corp. | Methods of cancer treatment with igf1r inhibitors |
| RU2009122670A (ru) * | 2006-12-21 | 2011-01-27 | Плекссикон, Инк. (Us) | Соединения и способы для модуляции киназ и показания к их применению |
| CA2673003A1 (en) | 2006-12-22 | 2008-07-03 | Novartis Ag | Quinazolines for pdk1 inhibition |
| KR20080062876A (ko) | 2006-12-29 | 2008-07-03 | 주식회사 대웅제약 | 신규한 항진균성 트리아졸 유도체 |
| EP1990342A1 (en) | 2007-05-10 | 2008-11-12 | AEterna Zentaris GmbH | Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof |
| TW200902008A (en) * | 2007-05-10 | 2009-01-16 | Smithkline Beecham Corp | Quinoxaline derivatives as PI3 kinase inhibitors |
| EP2154965A4 (en) | 2007-05-29 | 2011-08-17 | Glaxosmithkline Llc | NAPHTHYRIDINE DERIVATIVES AS P13 KINASE INHIBITORS |
| AR066879A1 (es) | 2007-06-08 | 2009-09-16 | Novartis Ag | Derivados de quinoxalina como inhibidores de la actividad de cinasa de tirosina de las cinasas janus |
| EP2170894A1 (en) | 2007-06-21 | 2010-04-07 | Janssen Pharmaceutica N.V. | Polymorphic and hydrate forms, salts and process for preparing 6-{difluoro[6-(1-methyl-1h-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]methyl}quinoline |
| JP2010535804A (ja) * | 2007-08-09 | 2010-11-25 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Ｐｉ３キナーゼ阻害薬としてのキノキサリン誘導体 |
| US20090054304A1 (en) | 2007-08-23 | 2009-02-26 | Kalypsys, Inc. | Heterocyclic modulators of tgr5 for treatment of disease |
| EA020777B1 (ru) | 2007-11-16 | 2015-01-30 | Инсайт Корпорейшн | 4-пиразолил-n-арилпиримидин-2-амины, 4-пиразолил-n-пиразолилпиримидин-2-амины и 4-пиразолил-n-пиридилпиримидин-2-амины в качестве ингибиторов киназ janus |
| US20110129456A1 (en) | 2008-05-05 | 2011-06-02 | Yaolin Wang | Sequential Administration of Chemotherapeutic Agents for Treatment of Cancer |
| AU2009248774B2 (en) | 2008-05-23 | 2012-05-31 | Novartis Ag | Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors |
| EP2356116A1 (en) | 2008-11-20 | 2011-08-17 | OSI Pharmaceuticals, Inc. | Substituted pyrroloý2,3-b¨-pyridines and-pyrazines |
| US8716280B2 (en) | 2009-01-21 | 2014-05-06 | Basilea Pharmaceutica Ag | Bicyclic antibiotics |
| WO2010088177A1 (en) | 2009-02-02 | 2010-08-05 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| TW201041888A (en) | 2009-05-06 | 2010-12-01 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| CN102625804B (zh) | 2009-06-12 | 2015-04-08 | Abivax公司 | 用于治疗aids的化合物 |
| DK2473504T3 (en) | 2009-09-03 | 2015-03-16 | Bioenergenix | Heterocyclic Compounds for Inhibition of Passover |
| WO2011026579A1 (en) | 2009-09-04 | 2011-03-10 | Bayer Schering Pharma Aktiengesellschaft | Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors |
| EP2332939A1 (en) | 2009-11-26 | 2011-06-15 | Æterna Zentaris GmbH | Novel Naphthyridine derivatives and the use thereof as kinase inhibitors |
| SG10201502484SA (en) | 2010-03-30 | 2015-05-28 | Verseon Corp | Multisubstituted aromatic compounds as inhibitors of thrombin |
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| US8513421B2 (en) | 2010-05-19 | 2013-08-20 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
| JP5894980B2 (ja) | 2010-05-24 | 2016-03-30 | インテリカイン， エルエルシー | 複素環式化合物およびその使用 |
| GB201020179D0 (en) * | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| CN102532141A (zh) | 2010-12-08 | 2012-07-04 | 中国科学院上海药物研究所 | [1，2，4]三唑并[4，3-b][1，2，4]三嗪类化合物、其制备方法和用途 |
| WO2012104776A1 (en) | 2011-01-31 | 2012-08-09 | Novartis Ag | Novel heterocyclic derivatives |
| TWI592411B (zh) | 2011-02-23 | 2017-07-21 | 英特爾立秦有限責任公司 | 激酶抑制劑之組合及其用途 |
| WO2012118492A1 (en) | 2011-03-01 | 2012-09-07 | Array Biopharma Inc. | Heterocyclic sulfonamides as raf inhibitors |
| WO2013032951A1 (en) | 2011-08-26 | 2013-03-07 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| AU2012308238B2 (en) | 2011-09-14 | 2017-05-25 | 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 |
| EP2763994A4 (en) | 2011-10-04 | 2015-08-26 | Gilead Calistoga Llc | NEW QUINOXALINE INHIBITORS OF THE PI3K PATH |
| 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 |
| SG11201401716XA (en) | 2011-10-28 | 2014-05-29 | Novartis Ag | Novel purine derivatives and their use in the treatment of disease |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| JO3210B1 (ar) | 2011-10-28 | 2018-03-08 | Merck Sharp & Dohme | مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة |
| 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 |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| US9221804B2 (en) | 2013-10-15 | 2015-12-29 | Janssen Pharmaceutica Nv | Secondary alcohol quinolinyl modulators of RORγt |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| US10736900B2 (en) | 2014-03-26 | 2020-08-11 | Astex Therapeutics Ltd | Combinations of an FGFR inhibitor and an IGF1R inhibitor |
| BR112016022056B1 (pt) | 2014-03-26 | 2023-04-11 | Astex Therapeutics Limited | Combinação, composição farmacêutica, uso de uma combinação ou uma composição farmacêutica, e, produto farmacêutico |
| TWI719960B (zh) | 2015-02-10 | 2021-03-01 | 英商阿斯迪克治療公司 | 新穎組成物 |
-
2010
- 2010-11-29 GB GBGB1020179.6A patent/GB201020179D0/en not_active Ceased
-
2011
- 2011-11-29 WO PCT/GB2011/052356 patent/WO2012073017A1/en not_active Ceased
- 2011-11-29 AU AU2011334624A patent/AU2011334624B2/en active Active
- 2011-11-29 JP JP2013540440A patent/JP5868992B2/ja active Active
- 2011-11-29 RU RU2013129820/04A patent/RU2602233C2/ru active
- 2011-11-29 MX MX2013005897A patent/MX2013005897A/es active IP Right Grant
- 2011-11-29 US US13/990,193 patent/US9290478B2/en active Active
- 2011-11-29 SI SI201130534T patent/SI2646432T1/sl unknown
- 2011-11-29 EP EP11805567.2A patent/EP2646432B1/en active Active
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-
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- 2015-08-03 US US14/816,565 patent/US9856236B2/en active Active
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2377241C2 (ru) * | 2003-11-24 | 2009-12-27 | Ф.Хоффманн-Ля Рош Аг | Производные пиразоло-имидазопиримидина, обладающие антагонистической активностью в отношении кортикотропин-рилизинг фактора (crf) |
| WO2008078091A1 (en) * | 2006-12-22 | 2008-07-03 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as fgfr inhibitors |
| WO2009019518A1 (en) * | 2007-08-09 | 2009-02-12 | Astrazeneca Ab | Pyrimidine compounds having a fgfr inhibitory effect |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2771526C1 (ru) * | 2018-09-14 | 2022-05-05 | Аббиско Терапеутикс Ко., Лтд. | Ингибитор fgfr, метод его получения и его применение |
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| CA2819009C (en) | 2020-02-25 |
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| HRP20150692T1 (hr) | 2015-08-14 |
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| KR101914720B1 (ko) | 2018-11-05 |
| SI2646432T1 (sl) | 2015-08-31 |
| SMT201500191B (it) | 2015-09-07 |
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