ES2661003T3 - Quinolinas como moduladores de FGFR quinasa - Google Patents
Quinolinas como moduladores de FGFR quinasa Download PDFInfo
- Publication number
- ES2661003T3 ES2661003T3 ES12794744.8T ES12794744T ES2661003T3 ES 2661003 T3 ES2661003 T3 ES 2661003T3 ES 12794744 T ES12794744 T ES 12794744T ES 2661003 T3 ES2661003 T3 ES 2661003T3
- Authority
- ES
- Spain
- Prior art keywords
- alkyl
- substituted
- ring
- groups
- 4alkyl
- 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
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/38—Nitrogen atoms
-
- 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
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D401/02—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
- C07D401/02—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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Quinoline Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161552880P | 2011-10-28 | 2011-10-28 | |
| US201161552880P | 2011-10-28 | ||
| GB201118652 | 2011-10-28 | ||
| GBGB1118652.5A GB201118652D0 (en) | 2011-10-28 | 2011-10-28 | New compounds |
| PCT/GB2012/052666 WO2013061074A1 (en) | 2011-10-28 | 2012-10-26 | Quinolines as fgfr kinase modulators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2661003T3 true ES2661003T3 (es) | 2018-03-27 |
Family
ID=45373580
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES12794744.8T Active ES2661003T3 (es) | 2011-10-28 | 2012-10-26 | Quinolinas como moduladores de FGFR quinasa |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US9439896B2 (index.php) |
| EP (1) | EP2776397B1 (index.php) |
| JP (1) | JP6067725B2 (index.php) |
| KR (1) | KR102072869B1 (index.php) |
| CN (1) | CN104011025B (index.php) |
| AU (1) | AU2012328164B2 (index.php) |
| BR (1) | BR112014010177B1 (index.php) |
| CA (1) | CA2853366C (index.php) |
| DK (1) | DK2776397T3 (index.php) |
| ES (1) | ES2661003T3 (index.php) |
| GB (1) | GB201118652D0 (index.php) |
| HU (1) | HUE037458T2 (index.php) |
| IN (1) | IN2014MN00988A (index.php) |
| MX (1) | MX353806B (index.php) |
| RU (1) | RU2625303C2 (index.php) |
| WO (1) | WO2013061074A1 (index.php) |
Families Citing this family (35)
| 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 |
| 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 |
| 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 |
| PE20151203A1 (es) | 2012-10-16 | 2015-08-31 | Janssen Pharmaceutica Nv | MODULADORES DE QUINOLINILO UNIDOS A FENILO DE ROR-GAMMA-t |
| AU2013331493A1 (en) | 2012-10-16 | 2015-04-09 | Janssen Pharmaceutica Nv | Heteroaryl linked quinolinyl modulators of RORyt |
| CN105209453B (zh) | 2012-10-16 | 2017-06-20 | 詹森药业有限公司 | ROR‑γ‑T的亚甲基连接的喹啉基调节剂 |
| AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| US9403816B2 (en) | 2013-10-15 | 2016-08-02 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of RORγt |
| JP6608358B2 (ja) | 2013-10-15 | 2019-11-20 | ヤンセン ファーマシューティカ エヌ.ベー. | RoRyTのキノリニルモジュレーター |
| WO2015057629A1 (en) * | 2013-10-15 | 2015-04-23 | Janssen Pharmaceutica Nv | ALKYL LINKED QUINOLINYL MODULATORS OF RORyt |
| US9284308B2 (en) | 2013-10-15 | 2016-03-15 | Janssen Pharmaceutica Nv | Methylene linked quinolinyl modulators of RORγt |
| US10555941B2 (en) | 2013-10-15 | 2020-02-11 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
| WO2015057206A1 (en) * | 2013-10-15 | 2015-04-23 | Janssen Pharmaceutica Nv | SECONDARY ALCOHOL QUINOLINYL MODULATORS OF RORyt |
| US9328095B2 (en) | 2013-10-15 | 2016-05-03 | Janssen Pharmaceutica Nv | Heteroaryl linked quinolinyl modulators of RORgammat |
| US9221804B2 (en) | 2013-10-15 | 2015-12-29 | Janssen Pharmaceutica Nv | Secondary alcohol quinolinyl modulators of RORγt |
| HUE053654T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR- és CMET-inhibitorok kombinációi a rák kezelésére |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| AU2015238305B2 (en) | 2014-03-26 | 2020-06-18 | Astex Therapeutics Ltd | Combinations of an FGFR inhibitor and an IGF1R inhibitor |
| JP5925978B1 (ja) | 2014-08-18 | 2016-05-25 | 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 |
| 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 |
| AU2016237222B2 (en) | 2015-03-25 | 2021-04-29 | Eisai R&D Management Co., Ltd. | Therapeutic agent for bile duct cancer |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| 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 |
| ES2811845T3 (es) | 2015-09-23 | 2021-03-15 | Janssen Pharmaceutica Nv | Heterociclos tricíclicos para el tratamiento del cáncer |
| US12414945B2 (en) | 2015-12-17 | 2025-09-16 | Eisai R&D Management Co., Ltd. | Therapeutic agent for breast cancer |
| CN108264510A (zh) * | 2017-01-02 | 2018-07-10 | 上海喆邺生物科技有限公司 | 一种选择性抑制激酶化合物及其用途 |
| MX2020008610A (es) | 2018-03-28 | 2020-09-21 | Eisai R&D Man Co Ltd | Agente terapeutico para carcinoma hepatocelular. |
| CN113087696A (zh) * | 2019-12-23 | 2021-07-09 | 江苏开元药业有限公司 | 喹啉类化合物及其应用 |
| EP4076449A4 (en) * | 2020-01-17 | 2023-12-06 | Beta Pharma, Inc. | PYRIDAZINE AND 1,2,4-TRIAZINE DERIVATIVES AS FGFR KINASE INHIBITORS |
Family Cites Families (118)
| 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 |
| EP0763537A3 (en) | 1993-05-14 | 1997-10-22 | Genentech Inc | Non-peptides farnesyl transfer inhibitors |
| 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 |
| CA2262403C (en) | 1995-07-31 | 2011-09-20 | Urocor, Inc. | 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 |
| EP1001945B1 (en) | 1997-05-28 | 2011-03-02 | Aventis Pharmaceuticals Inc. | QUINOLINE AND QUINOXALINE COMPOUNDS WHICH INHIBIT PLATELET-DERIVED GROWTH FACTOR AND/OR p56lck TYROSINE KINASES |
| 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 |
| WO2001019825A1 (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 |
| 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 |
| PL211694B1 (pl) | 2001-12-24 | 2012-06-29 | Astrazeneca Ab | Podstawiona pochodna chinazoliny, jej zastosowania oraz jej kompozycja farmaceutyczna |
| 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 |
| AU2003223467B2 (en) | 2002-04-08 | 2007-10-04 | Merck Sharp & Dohme Corp. | Inhibitors of Akt activity |
| US20040097725A1 (en) | 2002-07-10 | 2004-05-20 | Norman Herron | 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 |
| US7208493B2 (en) | 2002-10-03 | 2007-04-24 | Targegen, Inc. | Vasculostatic agents and methods of use thereof |
| 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 |
| BRPI0406809A (pt) | 2003-01-17 | 2005-12-27 | Warner Lambert Co | Heterociclos substituìdos de 2-aminopiridina como inibidores da proliferação celular |
| EP1620413A2 (en) | 2003-04-30 | 2006-02-01 | Cytokinetics, Inc. | Compounds, compositions, and methods |
| CA2525547C (en) | 2003-05-14 | 2012-07-03 | Torreypines Therapeutics, Inc. | Compounds and uses thereof in modulating amyloid beta |
| DE10323345A1 (de) | 2003-05-23 | 2004-12-16 | Zentaris Gmbh | Neue Pyridopyrazine und deren Verwendung als Kinase-Inhibitoren |
| PL1636228T3 (pl) | 2003-05-23 | 2009-04-30 | Aeterna Zentaris Gmbh | Nowe pirydopirazyny i ich zastosowanie jako modulatorów kinazy |
| WO2005007099A2 (en) | 2003-07-10 | 2005-01-27 | Imclone Systems Incorporated | Pkb inhibitors as anti-tumor agents |
| WO2005009437A1 (en) | 2003-07-21 | 2005-02-03 | Bethesda Pharmaceuticals, Inc. | Design and synthesis of optimized ligands for ppar |
| KR20060054410A (ko) | 2003-08-01 | 2006-05-22 | 제네랩스 테크놀로지스, 인코포레이티드 | 플라비비리다에에 대한 2고리 이미다졸 유도체 |
| JP2007508355A (ja) | 2003-10-17 | 2007-04-05 | 4・アー・ゼット・アー・バイオサイエンス・ナムローゼ・フエンノートシャップ | 複素環−置換プテリジン誘導体と治療におけるその利用 |
| EP1692085A4 (en) | 2003-11-07 | 2010-10-13 | Novartis Vaccines & Diagnostic | INHIBITION OF FGFR3 AND TREATMENT OF MULTIPLE MYELOMA |
| ES2670349T3 (es) * | 2003-11-20 | 2018-05-30 | Janssen Pharmaceutica Nv | 2-Quinolinonas y 2-quinoxalinonas sustituidas con 6-alquenilo y 6-fenilalquilo como inhibidores de poli(ADP-ribosa) polimerasa |
| KR101118582B1 (ko) | 2003-11-20 | 2012-02-27 | 얀센 파마슈티카 엔.브이. | 폴리(adp-리보스)폴리머라제 저해제로서의 6-알케닐 및6-페닐알킬 치환된 2-퀴놀리논 및 2-퀴녹살리논 |
| WO2005054231A1 (en) | 2003-11-24 | 2005-06-16 | F.Hoffmann-La Roche Ag | Pyrazolyl and imidazolyl pyrimidines |
| 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 |
| EP1789399A1 (en) | 2004-08-31 | 2007-05-30 | AstraZeneca AB | Quinazolinone derivatives and their use as b-raf inhibitors |
| JP2008516905A (ja) | 2004-10-14 | 2008-05-22 | エフ.ホフマン−ラ ロシュ アーゲー | Cdk1抗増殖活性を有する1,5−ナフチリジンアゾリジノン |
| EP1830869B1 (en) | 2004-12-24 | 2013-05-22 | Spinifex Pharmaceuticals Pty Ltd | Method of treatment or prophylaxis |
| JP2008530030A (ja) | 2005-02-14 | 2008-08-07 | バイオノミックス リミテッド | 新規なチューブリン重合阻害剤 |
| EP1853261B1 (de) | 2005-03-03 | 2017-01-11 | Universität des Saarlandes | Selektive hemmstoffe humaner corticoidsynthasen |
| JP2008540535A (ja) | 2005-05-12 | 2008-11-20 | メルク エンド カムパニー インコーポレーテッド | チロシンキナーゼ阻害剤 |
| EP1881981A1 (en) | 2005-05-18 | 2008-01-30 | Wyeth | 4, 6-diamino-[1,7] naphthyridine-3-carbonitrile inhibitors of tpl2 kinase and methods of making and using the same |
| GB0513692D0 (en) | 2005-07-04 | 2005-08-10 | Karobio Ab | Novel pharmaceutical compositions |
| BRPI0615233A2 (pt) | 2005-08-26 | 2011-05-10 | Serono Lab | derivados de pirazina e uso dos mesmos como inibidores p13k |
| EP1790342A1 (de) | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
| CA2628039A1 (en) | 2005-11-11 | 2007-05-18 | 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 |
| ME02736B (me) | 2005-12-21 | 2017-10-20 | Janssen Pharmaceutica Nv | Triazolopiridazini kao modulatori tirozin kinaze |
| US7998978B2 (en) | 2006-05-01 | 2011-08-16 | Pfizer Inc. | Substituted 2-amino-fused heterocyclic compounds |
| GB0609621D0 (en) | 2006-05-16 | 2006-06-21 | Astrazeneca Ab | Novel co-crystal |
| JP2009537590A (ja) | 2006-05-24 | 2009-10-29 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 四員複素環で置換された置換プテリジン |
| US20100016293A1 (en) | 2006-07-03 | 2010-01-21 | Rogier Adriaan Smits | Quinazolines and Related Heterocyclic Compounds, and Their Therapeutic Use |
| 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 |
| CN101641351A (zh) | 2006-12-21 | 2010-02-03 | 普莱希科公司 | 用于激酶调节的化合物和方法及其适应症 |
| AU2007336893A1 (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 |
| EP1990342A1 (en) | 2007-05-10 | 2008-11-12 | AEterna Zentaris GmbH | Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof |
| WO2008141065A1 (en) | 2007-05-10 | 2008-11-20 | Smithkline Beecham Corporation | Quinoxaline derivatives as p13 kinase inhibitors |
| US20100179143A1 (en) | 2007-05-29 | 2010-07-15 | Smithkline Beecham Corporation | 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 |
| PL2172450T3 (pl) | 2007-06-20 | 2014-03-31 | Mitsubishi Tanabe Pharma Corp | Nowe pochodne sulfonamidowe kwasu malonowego i ich zastosowanie farmaceutyczne |
| 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 |
| 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 |
| EP2282739A2 (en) | 2008-05-05 | 2011-02-16 | Schering Corporation | Sequential administration of chemotherapeutic agents for treatment of cancer |
| GEP20125502B (en) | 2008-05-23 | 2012-04-25 | Novartis Ag | Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors |
| WO2010059771A1 (en) | 2008-11-20 | 2010-05-27 | Osi Pharmaceuticals, Inc. | Substituted pyrrolo[2,3-b]-pyridines and-pyrazines |
| WO2010084152A1 (en) | 2009-01-21 | 2010-07-29 | Basilea Pharmaceutica Ag | Novel bicyclic antibiotics |
| JP2012516847A (ja) | 2009-02-02 | 2012-07-26 | メルク・シャープ・エンド・ドーム・コーポレイション | Akt活性の阻害剤 |
| TW201041888A (en) | 2009-05-06 | 2010-12-01 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| KR101789275B1 (ko) * | 2009-06-12 | 2017-11-20 | 아비박스 | 에이즈 치료에 유용한 화합물 |
| CN102656163B (zh) | 2009-09-03 | 2016-01-13 | 拜奥埃内杰尼克斯公司 | 抑制pask的杂环化合物 |
| CA2772790C (en) | 2009-09-04 | 2017-06-27 | Benjamin Bader | Substituted aminoquinoxalines as tyrosine threonine kinase inhibitors |
| US20110123545A1 (en) | 2009-11-24 | 2011-05-26 | Bristol-Myers Squibb Company | Combination of vegfr2 and igf1r inhibitors for the treatment of proliferative diseases |
| EP2332939A1 (en) | 2009-11-26 | 2011-06-15 | Æterna Zentaris GmbH | Novel Naphthyridine derivatives and the use thereof as kinase inhibitors |
| MX355038B (es) | 2010-03-30 | 2018-03-28 | Verseon Corp | Compuestos aromáticos multisustituidos como inhibidores de trombina. |
| 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 |
| WO2011149937A1 (en) | 2010-05-24 | 2011-12-01 | Intellikine, Inc. | Heterocyclic compounds and uses thereof |
| 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 |
| KR101928116B1 (ko) | 2011-01-31 | 2018-12-11 | 노파르티스 아게 | 신규 헤테로시클릭 유도체 |
| JP6130305B2 (ja) | 2011-02-23 | 2017-05-17 | インテリカイン, エルエルシー | キナーゼ阻害剤の組み合わせおよびそれらの使用 |
| WO2012118492A1 (en) | 2011-03-01 | 2012-09-07 | Array Biopharma Inc. | Heterocyclic sulfonamides as raf inhibitors |
| CN107245056A (zh) | 2011-08-26 | 2017-10-13 | 润新生物公司 | 化学实体、组合物及方法 |
| JP6093768B2 (ja) | 2011-09-14 | 2017-03-08 | 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 |
| WO2013043935A1 (en) | 2011-09-21 | 2013-03-28 | Neupharma, Inc. | Certain chemical entites, compositions, and methods |
| EP2763994A4 (en) | 2011-10-04 | 2015-08-26 | Gilead Calistoga Llc | NEW QUINOXALINE INHIBITORS OF THE PI3K PATH |
| 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 |
| CA2853256C (en) | 2011-10-28 | 2019-05-14 | 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 |
| GB201118654D0 (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 |
| BR112014021897B1 (pt) | 2012-03-08 | 2022-06-14 | Astellas Pharma Inc | Método, kit, conjunto de iniciadores e conjuntos de sondas para detectar um gene de fusão composto por um gene fgfr3 e um gene tacc3 |
| 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 |
| US20150203589A1 (en) | 2012-07-24 | 2015-07-23 | The Trustees Of Columbia University In The City Of New York | Fusion proteins and methods thereof |
| 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 |
| AU2015238305B2 (en) | 2014-03-26 | 2020-06-18 | 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 |
| HUE053654T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR- és CMET-inhibitorok kombinációi a rák kezelésére |
| 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 |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
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| EP2776397A1 (en) | 2014-09-17 |
| RU2625303C2 (ru) | 2017-07-13 |
| MX2014004857A (es) | 2014-08-26 |
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| CN104011025A (zh) | 2014-08-27 |
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| US9439896B2 (en) | 2016-09-13 |
| MX353806B (es) | 2018-01-30 |
| KR20140093665A (ko) | 2014-07-28 |
| WO2013061074A1 (en) | 2013-05-02 |
| HUE037458T2 (hu) | 2018-09-28 |
| IN2014MN00988A (index.php) | 2015-04-24 |
| CA2853366A1 (en) | 2013-05-02 |
| BR112014010177A2 (pt) | 2017-04-25 |
| CA2853366C (en) | 2021-04-20 |
| US10039759B2 (en) | 2018-08-07 |
| AU2012328164A1 (en) | 2014-05-15 |
| EP2776397B1 (en) | 2017-11-29 |
| JP2014530896A (ja) | 2014-11-20 |
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