AU2014259151B2 - Quinazolinone derivatives useful as FGFR kinase modulators - Google Patents
Quinazolinone derivatives useful as FGFR kinase modulators Download PDFInfo
- Publication number
- AU2014259151B2 AU2014259151B2 AU2014259151A AU2014259151A AU2014259151B2 AU 2014259151 B2 AU2014259151 B2 AU 2014259151B2 AU 2014259151 A AU2014259151 A AU 2014259151A AU 2014259151 A AU2014259151 A AU 2014259151A AU 2014259151 B2 AU2014259151 B2 AU 2014259151B2
- Authority
- AU
- Australia
- Prior art keywords
- alkyl
- substituted
- 6alkyl
- cancer
- haloci
- 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.)
- Active
Links
- ACODOYCXGPDFBE-UHFFFAOYSA-N CC(C)(C)OC(N(CC1)CCC1N(C=Nc(cc1)c2cc1N(CCCO[Si+](C)(C)C(C)(C)C)c1cc(OC)cc(OC)c1F)C2=O)=O Chemical compound CC(C)(C)OC(N(CC1)CCC1N(C=Nc(cc1)c2cc1N(CCCO[Si+](C)(C)C(C)(C)C)c1cc(OC)cc(OC)c1F)C2=O)=O ACODOYCXGPDFBE-UHFFFAOYSA-N 0.000 description 1
- QWVHOBYTLDLHTF-UHFFFAOYSA-N CC(C)(C)[Si+](C)(C)OCCN(c(cc12)ccc1N=CN(c1ccccc1)C2=O)c(c(Cl)c(cc1C)OC)c1Cl Chemical compound CC(C)(C)[Si+](C)(C)OCCN(c(cc12)ccc1N=CN(c1ccccc1)C2=O)c(c(Cl)c(cc1C)OC)c1Cl QWVHOBYTLDLHTF-UHFFFAOYSA-N 0.000 description 1
- XDPVLWNCYDPYAH-UHFFFAOYSA-N CC(C)(C)[Si+](C)(C)OCCN(c(cc12)ccc1N=CN(c1ccccc1)C2=O)c1cc(OC)cc(OC)c1 Chemical compound CC(C)(C)[Si+](C)(C)OCCN(c(cc12)ccc1N=CN(c1ccccc1)C2=O)c1cc(OC)cc(OC)c1 XDPVLWNCYDPYAH-UHFFFAOYSA-N 0.000 description 1
- PWSFDXONPLBLHU-UHFFFAOYSA-N CC(C)NCCN(c(cc12)ccc1N=CN(c1c[n](C)nc1)C2=O)c(cc(cc1OC)OC)c1F Chemical compound CC(C)NCCN(c(cc12)ccc1N=CN(c1c[n](C)nc1)C2=O)c(cc(cc1OC)OC)c1F PWSFDXONPLBLHU-UHFFFAOYSA-N 0.000 description 1
- UGUPRYFMMDMSOU-UHFFFAOYSA-N CCCN(c(cc12)ccc1N=CN(C1CCOCC1)C2=O)c(cc(C)cc1OC)c1F Chemical compound CCCN(c(cc12)ccc1N=CN(C1CCOCC1)C2=O)c(cc(C)cc1OC)c1F UGUPRYFMMDMSOU-UHFFFAOYSA-N 0.000 description 1
- WUWWAMGQOPNGLP-UHFFFAOYSA-N CCCN(c(cc12)ccc1N=CN(C1CCOCC1)C2=O)c1cc(OC)cc(C)c1 Chemical compound CCCN(c(cc12)ccc1N=CN(C1CCOCC1)C2=O)c1cc(OC)cc(C)c1 WUWWAMGQOPNGLP-UHFFFAOYSA-N 0.000 description 1
- UFGHTNSAWYXAJL-UHFFFAOYSA-N CCCN(c(cc12)ccc1N=CN(c1ccccc1)C2=O)c(c(F)c(cc1OC)OC)c1F Chemical compound CCCN(c(cc12)ccc1N=CN(c1ccccc1)C2=O)c(c(F)c(cc1OC)OC)c1F UFGHTNSAWYXAJL-UHFFFAOYSA-N 0.000 description 1
- PVKQCTPNZDAAAR-UHFFFAOYSA-N COc(c(F)c1N(CCCN)c(cc23)ccc2N=CN(C2CCNCC2)C3=O)cc(O)c1F Chemical compound COc(c(F)c1N(CCCN)c(cc23)ccc2N=CN(C2CCNCC2)C3=O)cc(O)c1F PVKQCTPNZDAAAR-UHFFFAOYSA-N 0.000 description 1
- GEQXWVAUEBANKR-UHFFFAOYSA-N COc(c(F)c1N(CCOS(C)(=C)=O)c(cc2)cc3c2N=CN(C2CCNCC2)C3=O)cc(OC)c1F Chemical compound COc(c(F)c1N(CCOS(C)(=C)=O)c(cc2)cc3c2N=CN(C2CCNCC2)C3=O)cc(OC)c1F GEQXWVAUEBANKR-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
- C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/80—Oxygen atoms
- C07D239/82—Oxygen atoms with an aryl radical attached in position 4
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/02—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
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- 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)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Toys (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1307577.5A GB201307577D0 (en) | 2013-04-26 | 2013-04-26 | New compounds |
| GB1307577.5 | 2013-04-26 | ||
| PCT/GB2014/051288 WO2014174307A1 (en) | 2013-04-26 | 2014-04-25 | Quinazolinone derivatives useful as fgfr kinase modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2014259151A1 AU2014259151A1 (en) | 2015-11-26 |
| AU2014259151B2 true AU2014259151B2 (en) | 2018-03-15 |
Family
ID=48626899
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2014259151A Active AU2014259151B2 (en) | 2013-04-26 | 2014-04-25 | Quinazolinone derivatives useful as FGFR kinase modulators |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9493426B2 (enExample) |
| EP (1) | EP2989092B1 (enExample) |
| JP (1) | JP6419784B2 (enExample) |
| KR (1) | KR102341202B1 (enExample) |
| CN (1) | CN105324378B (enExample) |
| AU (1) | AU2014259151B2 (enExample) |
| BR (1) | BR112015026830B1 (enExample) |
| CA (1) | CA2910142C (enExample) |
| DK (1) | DK2989092T3 (enExample) |
| ES (1) | ES2650312T3 (enExample) |
| GB (1) | GB201307577D0 (enExample) |
| MX (1) | MX366166B (enExample) |
| RU (1) | RU2701517C2 (enExample) |
| WO (1) | WO2014174307A1 (enExample) |
Families Citing this family (48)
| 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 |
| GB201118656D0 (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 |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| 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 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| 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 |
| EP3060563B1 (en) | 2013-10-25 | 2018-05-02 | Novartis AG | Ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors |
| 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. |
| HUE053653T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR inhibitor és IGF1R inhibitor kombinációi |
| PL3200786T3 (pl) | 2014-10-03 | 2020-03-31 | Novartis Ag | Zastosowanie pochodnych pirydylowych o skondensowanym układzie bicyklicznym jako inhibitorów fgfr4 |
| 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 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| SG10201913036RA (en) | 2015-02-20 | 2020-02-27 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| 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 |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy 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 |
| 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 |
| RU2732127C1 (ru) * | 2016-09-01 | 2020-09-11 | Наньцзин Транстера Биосайенсиз Ко. Лтд. | Ингибиторы рецептора фактора роста фибробластов и их применение |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| PL3788047T3 (pl) | 2018-05-04 | 2025-04-14 | Incyte Corporation | Stałe postacie inhibitora fgfr i sposoby ich otrzymywania |
| KR20210018264A (ko) | 2018-05-04 | 2021-02-17 | 인사이트 코포레이션 | Fgfr 억제제의 염 |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| CR20220169A (es) | 2019-10-14 | 2022-10-27 | Incyte Corp | Heterociclos bicíclicos como inhibidores de fgfr |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| JP7720840B2 (ja) | 2019-12-04 | 2025-08-08 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式複素環 |
| CN110903253B (zh) * | 2019-12-13 | 2020-12-25 | 西安交通大学医学院第一附属医院 | 一种喹唑啉酮类化合物及其制备方法和应用 |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JP7630801B2 (ja) * | 2020-07-13 | 2025-02-18 | 国立大学法人富山大学 | Ｎｒ４ａ１拮抗薬を用いた鎮痛薬 |
| CN112279834B (zh) * | 2020-12-29 | 2021-04-09 | 北京鑫开元医药科技有限公司 | 一种fgfr4抑制剂、制备方法、药物组合物及其应用 |
| 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 |
| CN115260164B (zh) * | 2021-05-01 | 2024-03-26 | 杭州星鳌生物科技有限公司 | 新型4(3h)-喹唑啉酮类似物的制备方法、结构组成及其在抗肿瘤药物中的应用 |
| US11939331B2 (en) | 2021-06-09 | 2024-03-26 | Incyte Corporation | Tricyclic heterocycles as FGFR inhibitors |
| EP4352060A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| KR102862736B1 (ko) | 2022-12-07 | 2025-09-22 | 부산대학교 산학협력단 | 신규 2-((트랜스-4-(4-아릴옥시)사이클로헥실)아미노)퀴나졸리논 유도체 및 이의 제조방법 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011135376A1 (en) * | 2010-04-30 | 2011-11-03 | Astex Therapeutics Limited | Pyrazolyl quinazoline kinase inhibitors |
| WO2012073017A1 (en) * | 2010-11-29 | 2012-06-07 | Astex Therapeutics Limited | Substituted benzopyrazin derivatives as fgfr kinase inhibitors for the treatment of cancer diseases |
Family Cites Families (102)
| 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 |
| CZ296845B6 (cs) | 1997-05-28 | 2006-07-12 | Aventis Pharmaceuticals Inc. | Derivát chinolinu a chinoxalinu, farmaceutický prostredek obsahující tento derivát a pouzití |
| UA71555C2 (en) | 1997-10-06 | 2004-12-15 | Zentaris Gmbh | Methods for modulating function of serine/threonine protein kinases by 5-azaquinoline derivatives |
| JP2002534512A (ja) | 1999-01-15 | 2002-10-15 | ノボ ノルディスク アクティーゼルスカブ | 非ペプチドｇｌｐ−１アゴニスト |
| CA2393896A1 (en) | 1999-09-15 | 2001-03-22 | Warner-Lambert Company | Pteridinones as kinase inhibitors |
| 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 |
| AU2002359714B2 (en) | 2001-12-18 | 2006-12-21 | Merck Sharp & Dohme Corp. | Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5 |
| ES2333702T3 (es) | 2001-12-24 | 2010-02-26 | Astrazeneca Ab | Derivados de quinazolina sustituidos que actuan como unhibidores de cinasas aurora. |
| 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 |
| US7265378B2 (en) | 2002-07-10 | 2007-09-04 | E. I. Du Pont De Nemours And Company | Electronic devices made with electron transport and/or anti-quenching layers |
| US7825132B2 (en) | 2002-08-23 | 2010-11-02 | Novartis Vaccines And Diagnostics, Inc. | Inhibition of FGFR3 and treatment of multiple myeloma |
| KR20050056227A (ko) | 2002-10-03 | 2005-06-14 | 탈자진 인코포레이티드 | 혈관항상성 유지제 및 그의 사용 방법 |
| AR043059A1 (es) | 2002-11-12 | 2005-07-13 | Bayer Pharmaceuticals Corp | Derivados de indolil pirazinona utiles para el tratamiento de trastornos hiper-proliferativos |
| MXPA05007503A (es) | 2003-01-17 | 2005-09-21 | Warner Lambert Co | Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular. |
| EP1620413A2 (en) | 2003-04-30 | 2006-02-01 | Cytokinetics, Inc. | Compounds, compositions, and methods |
| MXPA05012281A (es) | 2003-05-14 | 2006-05-19 | Torreypines Therapeutics Inc | Compuestos y uso de los mismos en la modulacion beta amiloide. |
| RU2330851C9 (ru) | 2003-05-23 | 2008-10-20 | Центарис Гмбх | ПИРИДО[2,3-b]ПИРАЗИНОВЫЕ ПРОИЗВОДНЫЕ, ЛЕКАРСТВЕННОЕ СРЕДСТВО ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ ИЛИ НАРУШЕНИЯ, КОТОРЫЕ ОБУСЛОВЛЕНЫ НЕПРАВИЛЬНО НАПРАВЛЕННЫМИ ПРОЦЕССАМИ КЛЕТОЧНОЙ СИГНАЛЬНОЙ ТРАНСДУКЦИИ, СПОСОБ ПОЛУЧЕНИЯ ЛЕКАРСТВЕННОГО СРЕДСТВА |
| DE10323345A1 (de) | 2003-05-23 | 2004-12-16 | Zentaris Gmbh | Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren |
| 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 |
| JP4890255B2 (ja) | 2003-11-07 | 2012-03-07 | 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 | 改良された薬物特性を有するキノリノン化合物の薬学的に受容可能な塩 |
| MXPA06005687A (es) | 2003-11-20 | 2006-08-17 | Janssen Pharmaceutica Nv | 2-quinolinonas y 2-quinoxalinonas sustituidas con 6-alquenilo y 6-fenilalquilo como inhibidores de la poli(adenosin fosfato-ribosa)polimerasa. |
| JP2007512275A (ja) | 2003-11-24 | 2007-05-17 | エフ．ホフマン−ラ ロシュ アーゲー | ピラゾリルおよびイミダゾリルピリミジン |
| MXPA06007326A (es) | 2003-12-23 | 2007-01-26 | Astex Therapeutics Ltd | Derivados de pirazol como moduladores de proteina cinasa. |
| 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 |
| BRPI0514691A (pt) * | 2004-08-31 | 2008-06-17 | Astrazeneca Ab | composto ou um sal farmaceuticamente aceitável do mesmo, processo para preparar o mesmo, composição farmacêutica, e, uso de um composto ou um sal farmaceuticamente aceitável do mesmo |
| EP1830869B1 (en) | 2004-12-24 | 2013-05-22 | Spinifex Pharmaceuticals Pty Ltd | Method of treatment or prophylaxis |
| 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 |
| CA2606017A1 (en) | 2005-05-12 | 2006-11-23 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| GB0513692D0 (en) | 2005-07-04 | 2005-08-10 | Karobio Ab | Novel pharmaceutical compositions |
| EP1957487A1 (de) | 2005-11-11 | 2008-08-20 | AEterna Zentaris GmbH | Neue pyridopyrazine und deren verwendung als modulatoren von kinasen |
| 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 |
| EP1966214B9 (en) | 2005-12-21 | 2017-09-13 | Janssen Pharmaceutica N.V. | Triazolopyridazines as tyrosine kinase modulators |
| JP2009535393A (ja) | 2006-05-01 | 2009-10-01 | ファイザー・プロダクツ・インク | 置換２−アミノ縮合複素環式化合物 |
| GB0609621D0 (en) | 2006-05-16 | 2006-06-21 | Astrazeneca Ab | Novel co-crystal |
| CA2653117A1 (en) | 2006-05-24 | 2007-11-29 | Boehringer Ingelheim International Gmbh | Substituted pteridines substituted with a four-membered heterocycle |
| JP2009541460A (ja) | 2006-07-03 | 2009-11-26 | ベレナギング ヴォー クリスタラク ホガー オンダーヴェイル ヴェーテンザパーリク オンダージーク エン パシェンテンゾーク | ヒスタミンｈ４受容体と相互作用する縮合二環式化合物 |
| 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 |
| WO2008076278A2 (en) | 2006-12-13 | 2008-06-26 | Schering Corporation | Methods of cancer treatment with igf1r inhibitors |
| JP2010514695A (ja) | 2006-12-21 | 2010-05-06 | プレキシコン，インコーポレーテッド | キナーゼ調節のための化合物および方法およびそのための適応症 |
| CA2673003A1 (en) | 2006-12-22 | 2008-07-03 | Novartis Ag | Quinazolines for pdk1 inhibition |
| AU2007337886C1 (en) | 2006-12-22 | 2014-10-16 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as FGFR inhibitors |
| KR20080062876A (ko) | 2006-12-29 | 2008-07-03 | 주식회사 대웅제약 | 신규한 항진균성 트리아졸 유도체 |
| EP2150255A4 (en) | 2007-05-10 | 2011-10-05 | Glaxosmithkline Llc | CHINOXALINE DERIVATIVES AS P13 KINASE INHIBITORS |
| EP1990342A1 (en) | 2007-05-10 | 2008-11-12 | AEterna Zentaris GmbH | Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof |
| JP2010529031A (ja) | 2007-05-29 | 2010-08-26 | 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キナーゼ阻害剤としてのナフチリジン誘導体 |
| 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 |
| EP2172450B9 (en) * | 2007-06-20 | 2014-10-08 | Mitsubishi Tanabe Pharma Corporation | Novel malonic acid sulfonamide derivative and pharmaceutical use thereof |
| WO2008155378A1 (en) | 2007-06-21 | 2008-12-24 | Janssen Pharmaceutica Nv | 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 |
| EP2173354A4 (en) | 2007-08-09 | 2011-10-05 | Glaxosmithkline Llc | CHINOXALIN DERIVATIVES AS PI3 KINASE INHIBITORS |
| WO2009019518A1 (en) | 2007-08-09 | 2009-02-12 | Astrazeneca Ab | Pyrimidine compounds having a fgfr inhibitory effect |
| US20090054304A1 (en) | 2007-08-23 | 2009-02-26 | Kalypsys, Inc. | Heterocyclic modulators of tgr5 for treatment of disease |
| WO2009064835A1 (en) | 2007-11-16 | 2009-05-22 | Incyte Corporation | 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors |
| EP2282995B1 (en) | 2008-05-23 | 2015-08-26 | Novartis AG | Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors |
| JP2012509342A (ja) | 2008-11-20 | 2012-04-19 | オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド | 置換ピロロ［２，３−ｂ］−ピリジンおよび−ピラジン |
| CA2750047A1 (en) | 2009-01-21 | 2010-07-29 | Basilea Pharmaceutica Ag | Novel bicyclic antibiotics |
| EP2391623A4 (en) | 2009-02-02 | 2012-09-05 | Merck Sharp & Dohme | HAMMER OF ACT ACTIVITY |
| TW201041888A (en) | 2009-05-06 | 2010-12-01 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| HRP20230248T1 (hr) | 2009-06-12 | 2023-04-14 | Abivax | Spojevi korisni za liječenje preranog starenja, te naročito progerije |
| CA2772714C (en) | 2009-09-03 | 2017-09-26 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| 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 |
| RU2017144535A (ru) | 2010-03-30 | 2019-02-18 | Версеон Корпорейшн | Мультизамещенные ароматические соединения в качестве ингибиторов тромбина |
| US8513421B2 (en) | 2010-05-19 | 2013-08-20 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
| WO2011149937A1 (en) | 2010-05-24 | 2011-12-01 | Intellikine, Inc. | Heterocyclic compounds and uses thereof |
| 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 |
| EP2670753B1 (en) | 2011-01-31 | 2016-10-19 | 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 |
| 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 |
| EP2763994A4 (en) | 2011-10-04 | 2015-08-26 | Gilead Calistoga Llc | NEW QUINOXALINE INHIBITORS OF THE PI3K PATH |
| 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 |
| PH12014500912A1 (en) | 2011-10-28 | 2014-06-09 | Novartis Ag | Novel purine derivatives and their use in the treatment of disease |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| JO3210B1 (ar) | 2011-10-28 | 2018-03-08 | Merck Sharp & Dohme | مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| 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 |
| 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. |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| HUE053653T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR inhibitor és IGF1R inhibitor kombinációi |
| 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 |
-
2013
- 2013-04-26 GB GBGB1307577.5A patent/GB201307577D0/en not_active Ceased
-
2014
- 2014-04-25 AU AU2014259151A patent/AU2014259151B2/en active Active
- 2014-04-25 CN CN201480036664.1A patent/CN105324378B/zh active Active
- 2014-04-25 WO PCT/GB2014/051288 patent/WO2014174307A1/en not_active Ceased
- 2014-04-25 BR BR112015026830-7A patent/BR112015026830B1/pt active IP Right Grant
- 2014-04-25 KR KR1020157033349A patent/KR102341202B1/ko active Active
- 2014-04-25 US US14/787,089 patent/US9493426B2/en active Active
- 2014-04-25 EP EP14725756.2A patent/EP2989092B1/en active Active
- 2014-04-25 DK DK14725756.2T patent/DK2989092T3/da active
- 2014-04-25 MX MX2015014471A patent/MX366166B/es active IP Right Grant
- 2014-04-25 RU RU2015150417A patent/RU2701517C2/ru active
- 2014-04-25 JP JP2016509551A patent/JP6419784B2/ja active Active
- 2014-04-25 ES ES14725756.2T patent/ES2650312T3/es active Active
- 2014-04-25 CA CA2910142A patent/CA2910142C/en active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011135376A1 (en) * | 2010-04-30 | 2011-11-03 | Astex Therapeutics Limited | Pyrazolyl quinazoline kinase inhibitors |
| WO2012073017A1 (en) * | 2010-11-29 | 2012-06-07 | Astex Therapeutics Limited | Substituted benzopyrazin derivatives as fgfr kinase inhibitors for the treatment of cancer diseases |
Also Published As
| Publication number | Publication date |
|---|---|
| BR112015026830A2 (pt) | 2017-07-25 |
| MX366166B (es) | 2019-07-01 |
| EP2989092A1 (en) | 2016-03-02 |
| GB201307577D0 (en) | 2013-06-12 |
| BR112015026830B1 (pt) | 2022-11-16 |
| US20160075666A1 (en) | 2016-03-17 |
| EP2989092B1 (en) | 2017-08-30 |
| ES2650312T3 (es) | 2018-01-17 |
| CA2910142C (en) | 2021-08-10 |
| CN105324378A (zh) | 2016-02-10 |
| US9493426B2 (en) | 2016-11-15 |
| CA2910142A1 (en) | 2014-10-30 |
| JP2016521276A (ja) | 2016-07-21 |
| BR112015026830A8 (pt) | 2019-12-24 |
| CN105324378B (zh) | 2017-10-24 |
| WO2014174307A1 (en) | 2014-10-30 |
| AU2014259151A1 (en) | 2015-11-26 |
| MX2015014471A (es) | 2016-06-28 |
| KR102341202B1 (ko) | 2021-12-20 |
| RU2015150417A3 (enExample) | 2018-03-29 |
| RU2015150417A (ru) | 2017-06-06 |
| DK2989092T3 (da) | 2017-11-13 |
| JP6419784B2 (ja) | 2018-11-07 |
| KR20160003035A (ko) | 2016-01-08 |
| RU2701517C2 (ru) | 2019-09-27 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2014259151B2 (en) | Quinazolinone derivatives useful as FGFR kinase modulators | |
| AU2013269316C1 (en) | Pteridines as FGFR inhibitors | |
| EP2646432B1 (en) | Substituted benzopyrazin derivatives as fgfr kinase inhibitors for the treatment of cancer diseases | |
| AU2013269317B2 (en) | New compounds | |
| AU2012328167B9 (en) | New compounds | |
| AU2012328171B2 (en) | Anticancer benzopyrazines via the inhibition of FGFR kinases | |
| DK2776397T3 (en) | QUINOLINES AS FGFR CHINA MODULATORS | |
| HK1187916B (en) | Substituted benzopyrazin derivatives as fgfr kinase inhibitors for the treatment of cancer diseases |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) |