JO3419B1 - مركبات بيريدوبيرازين مضادة للسرطان من خلال تثبيط إنزيمات كيناز fgfr - Google Patents
مركبات بيريدوبيرازين مضادة للسرطان من خلال تثبيط إنزيمات كيناز fgfrInfo
- Publication number
- JO3419B1 JO3419B1 JOP/2012/0308A JOP20120308A JO3419B1 JO 3419 B1 JO3419 B1 JO 3419B1 JO P20120308 A JOP20120308 A JO P20120308A JO 3419 B1 JO3419 B1 JO 3419B1
- Authority
- JO
- Jordan
- Prior art keywords
- pyridopyrazine
- inhibition
- kinase enzymes
- fgfr kinase
- anticancer compounds
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 108091008794 FGF receptors Proteins 0.000 title 1
- 230000001093 anti-cancer Effects 0.000 title 1
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
- YEYHFKBVNARCNE-UHFFFAOYSA-N pyrido[2,3-b]pyrazine Chemical compound N1=CC=NC2=CC=CN=C21 YEYHFKBVNARCNE-UHFFFAOYSA-N 0.000 title 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- -1 pyridopyrazine derivative compounds Chemical class 0.000 abstract 1
Classifications
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- 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
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pulmonology (AREA)
- Gastroenterology & Hepatology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161552888P | 2011-10-28 | 2011-10-28 | |
| GBGB1118656.6A GB201118656D0 (en) | 2011-10-28 | 2011-10-28 | New compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JO3419B1 true JO3419B1 (ar) | 2019-10-20 |
Family
ID=45373584
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOP/2012/0308A JO3419B1 (ar) | 2011-10-28 | 2012-10-15 | مركبات بيريدوبيرازين مضادة للسرطان من خلال تثبيط إنزيمات كيناز fgfr |
Country Status (33)
| Country | Link |
|---|---|
| US (2) | US9309242B2 (e) |
| EP (1) | EP2776435B1 (e) |
| JP (1) | JP6169583B2 (e) |
| KR (1) | KR102066496B1 (e) |
| CN (1) | CN104011051B (e) |
| AP (1) | AP4060A (e) |
| AR (1) | AR088567A1 (e) |
| AU (1) | AU2012328170B2 (e) |
| BR (1) | BR112014010206B8 (e) |
| CA (1) | CA2853390C (e) |
| CL (1) | CL2014001065A1 (e) |
| CO (1) | CO6940422A2 (e) |
| CR (1) | CR20140190A (e) |
| DK (1) | DK2776435T3 (e) |
| EA (1) | EA027563B1 (e) |
| EC (1) | ECSP14013325A (e) |
| ES (1) | ES2688868T3 (e) |
| GB (1) | GB201118656D0 (e) |
| HR (1) | HRP20181533T1 (e) |
| IL (1) | IL232083B (e) |
| IN (1) | IN2014MN00948A (e) |
| JO (1) | JO3419B1 (e) |
| LT (1) | LT2776435T (e) |
| MX (1) | MX353654B (e) |
| MY (1) | MY185666A (e) |
| NI (1) | NI201400032A (e) |
| PH (1) | PH12014500867A1 (e) |
| SG (1) | SG11201401055XA (e) |
| SI (1) | SI2776435T1 (e) |
| TW (1) | TWI602814B (e) |
| UA (1) | UA111386C2 (e) |
| UY (1) | UY34418A (e) |
| WO (1) | WO2013061080A1 (e) |
Families Citing this family (43)
| 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 |
| GB201118654D0 (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 |
| 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 |
| 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 |
| AR098145A1 (es) * | 2013-10-25 | 2016-05-04 | Novartis Ag | Compuestos derivados de piridilo bicíclicos fusionados como inhibidores de fgfr4 |
| CA2927252C (en) * | 2013-10-25 | 2021-09-28 | 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 |
| EP3848034B1 (en) | 2014-03-26 | 2025-02-12 | Astex Therapeutics Limited | Cmet-inhibitors for use in delaying the emergence in resistance to fgfr inhibitors |
| DK3122359T3 (da) * | 2014-03-26 | 2021-03-08 | Astex Therapeutics Ltd | Kombinationer af en fgfr-inhibitor og en igf1r-hæmmer |
| SG11201700703XA (en) | 2014-08-18 | 2017-03-30 | Eisai R&D Man Co Ltd | Salt of monocyclic pyridine derivative and crystal thereof |
| WO2016054483A1 (en) * | 2014-10-03 | 2016-04-07 | Novartis Ag | Use of ring-fused bicyclic pyridyl derivatives as fgfr4 inhibitors |
| TWI695837B (zh) | 2014-12-04 | 2020-06-11 | 比利時商健生藥品公司 | 作為激酶調節劑之三唑並嗒 |
| 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 |
| 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 |
| KR102691777B1 (ko) | 2015-09-23 | 2024-08-02 | 얀센 파마슈티카 엔브이 | 비-헤테로아릴 치환된 1,4-벤조디아제핀 및 암의 치료를 위한 이의 용도 |
| WO2017050864A1 (en) | 2015-09-23 | 2017-03-30 | Janssen Pharmaceutica Nv | New compounds |
| MX382526B (es) | 2015-10-23 | 2025-03-13 | Array Biopharma Inc | Compuestos de 2-piridazin-3(2h)-ona 2-aril sustituidas y 2-heteroaril sustituidas como inhibidores de las tirosina quinasas fgfr |
| SG10201913213WA (en) | 2015-12-17 | 2020-03-30 | Eisai R&D Man Co Ltd | Therapeutic agent for breast cancer |
| WO2017164705A1 (ko) * | 2016-03-24 | 2017-09-28 | 재단법인 대구경북첨단의료산업진흥재단 | 신규한 피리딘 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 fgfr 관련 질환의 예방 또는 치료용 약학적 조성물 |
| CN109563091B (zh) * | 2016-08-12 | 2022-04-29 | 江苏豪森药业集团有限公司 | Fgfr4抑制剂及其制备方法和应用 |
| CN108101857B (zh) * | 2016-11-24 | 2021-09-03 | 韶远科技(上海)有限公司 | 制取2-氨基-3-溴-6-氯吡嗪的可放大工艺 |
| 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 |
| EP3777860A4 (en) | 2018-03-28 | 2021-12-15 | Eisai R&D Management Co., Ltd. | THERAPEUTIC FOR HEPATOCELLULAR CARCINOMA |
| US12180207B2 (en) | 2018-12-19 | 2024-12-31 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of FGFR tyrosine kinases |
| JP2022515197A (ja) | 2018-12-19 | 2022-02-17 | アレイ バイオファーマ インコーポレイテッド | がんを治療するためのfgfr阻害剤としての7-((3,5-ジメトキシフェニル)アミノ)キノキサリン誘導体 |
| US12441707B2 (en) | 2019-12-30 | 2025-10-14 | Tyra Biosciences, Inc. | Indazole compounds |
| WO2021138392A1 (en) | 2019-12-30 | 2021-07-08 | Tyra Biosciences, Inc. | Aminopyrimidine compounds |
| EP4076449A4 (en) * | 2020-01-17 | 2023-12-06 | Beta Pharma, Inc. | PYRIDAZINE AND 1,2,4-TRIAZINE DERIVATIVES AS FGFR KINASE INHIBITORS |
| CR20230325A (es) | 2020-12-30 | 2023-12-11 | Tyra Biosciences Inc | Compuestos de indazol como inhibidores de cinasas |
| WO2022182972A1 (en) | 2021-02-26 | 2022-09-01 | Tyra Biosciences, Inc. | Aminopyrimidine compounds and methods of their use |
| US20250368666A1 (en) | 2022-06-29 | 2025-12-04 | 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 |
| WO2025129014A1 (en) | 2023-12-15 | 2025-06-19 | Tyra Biosciences, Inc. | Indazole compounds for the treatment of cancer |
| WO2025222097A1 (en) | 2024-04-19 | 2025-10-23 | Tyra Biosciences, Inc. | Indazole-based protac degraders and their anticancer activity |
Family Cites Families (117)
| 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 |
| WO1994026723A2 (en) | 1993-05-14 | 1994-11-24 | Genentech, Inc. | ras FARNESYL TRANSFERASE 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 |
| WO1998004689A1 (en) | 1995-07-31 | 1998-02-05 | 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 |
| WO1998054157A1 (en) | 1997-05-28 | 1998-12-03 | Rhône-Poulenc Rorer Pharmaceuticals Inc. | QUINOLINE AND QUINOXALINE COMPOUNDS WHICH INHIBIT PLATELET-DERIVED GROWTH FACTOR AND/OR p561ck 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 |
| AU3033500A (en) | 1999-01-15 | 2000-08-01 | Agouron Pharmaceuticals, Inc. | Non-peptide glp-1 agonists |
| SK3542002A3 (en) | 1999-09-15 | 2003-04-01 | Warner Lambert Co | 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 |
| WO2003051833A2 (en) | 2001-12-18 | 2003-06-26 | Merck & Co., Inc. | Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5 |
| EP1463506B1 (en) | 2001-12-24 | 2009-10-21 | Astrazeneca AB | Substituted quinazoline derivatives as inhibitors of aurora kinases |
| 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 |
| CA2480800C (en) | 2002-04-08 | 2008-09-23 | Mark T. Bilodeau | 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 |
| CA2500727A1 (en) | 2002-10-03 | 2004-04-15 | 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 |
| WO2004098494A2 (en) | 2003-04-30 | 2004-11-18 | Cytokinetics, Inc. | Compounds, compositions, and methods |
| BRPI0410348A (pt) | 2003-05-14 | 2006-05-30 | Torreypines Therapeutics Inc | compostos e usos dos mesmos na modulação de amilóide-beta |
| DK1636228T3 (da) * | 2003-05-23 | 2009-02-23 | Aeterna Zentaris Gmbh | Nye pyridopyraziner og deres anvendelse som kinasemodulatorer |
| 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 |
| AU2004259000A1 (en) | 2003-07-21 | 2005-02-03 | Bethesda Pharmaceuticals, Inc. | Design and synthesis of optimized ligands for PPAR |
| TW200517381A (en) | 2003-08-01 | 2005-06-01 | Genelabs Tech Inc | Bicyclic heteroaryl derivatives |
| ATE369862T1 (de) | 2003-10-17 | 2007-09-15 | 4 Aza Ip Nv | Heterocyclus-substituierte pteridin-derivate und ihre verwendung in der therapie |
| WO2005046590A2 (en) | 2003-11-07 | 2005-05-26 | Chiron Corporation | Methods for synthesizing quinolinone compounds |
| SG150533A1 (en) | 2003-11-20 | 2009-03-30 | Janssen Pharmaceutica Nv | 6-alkenyl and 6-phenylalkyl substituted 2-quinolinones and 2- quinoxalinones as poly(adp-ribose) polymerase inhibitors |
| BRPI0416853A (pt) | 2003-11-24 | 2007-02-13 | Hoffmann La Roche | pirazolila e imidazolila pirimidinas |
| EP1706385B1 (en) | 2003-12-23 | 2010-10-06 | Astex Therapeutics Limited | Pyrazole derivatives as protein kinase modulators |
| US7205316B2 (en) | 2004-05-12 | 2007-04-17 | Abbott Laboratories | Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands |
| US7098222B2 (en) | 2004-05-12 | 2006-08-29 | Abbott Laboratories | Bicyclic-substituted amines having cyclic-substituted monocyclic substituents |
| NZ553087A (en) | 2004-08-31 | 2010-12-24 | 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 |
| PT1830869E (pt) | 2004-12-24 | 2013-08-22 | Spinifex Pharm Pty Ltd | Método de tratamento ou profilaxia |
| AU2006212726C1 (en) | 2005-02-14 | 2013-05-16 | Bionomics Limited | Novel tubulin polymerisation inhibitors |
| US9271963B2 (en) | 2005-03-03 | 2016-03-01 | Universitat Des Saarlandes | Selective inhibitors of human corticosteroid synthases |
| US20090156617A1 (en) | 2005-05-12 | 2009-06-18 | Northrup Alan B | Tyrosine kinase inhibitors |
| AU2006247315A1 (en) | 2005-05-18 | 2006-11-23 | 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 |
| 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 |
| EP1790342A1 (de) * | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
| MY159523A (en) | 2005-12-21 | 2017-01-13 | Janssen Pharmaceutica Nv | Triazolopyridazines as tyrosine kinase modulators |
| EP2024342A2 (en) | 2006-05-01 | 2009-02-18 | Pfizer Products Incorporated | Substituted 2-amino-fused heterocyclic compounds |
| GB0609621D0 (en) | 2006-05-16 | 2006-06-21 | Astrazeneca Ab | Novel co-crystal |
| ATE549338T1 (de) | 2006-05-24 | 2012-03-15 | Boehringer Ingelheim Int | Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind |
| CA2657702A1 (en) | 2006-07-03 | 2008-01-10 | Vereniging Voor Christelijk Hoger Onderwijs Wetenschappelijk Onderzoek E N Patieentenzorg | Quinazolines and related heterocyclic comp0unds, 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 |
| CN102123712B (zh) | 2006-12-13 | 2014-03-19 | 默沙东公司 | 使用igf1r抑制剂治疗癌症的方法 |
| US7872018B2 (en) | 2006-12-21 | 2011-01-18 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| JP5442448B2 (ja) | 2006-12-22 | 2014-03-12 | アステックス、セラピューティックス、リミテッド | Fgfrインヒビターとしての二環式ヘテロ環式化合物 |
| AU2007336893A1 (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 |
| PE20090288A1 (es) | 2007-05-10 | 2009-04-03 | Smithkline Beecham Corp | Derivados de quinoxalina como inhibidores de la pi3 quinasa |
| 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 |
| PT2172450E (pt) | 2007-06-20 | 2013-10-28 | Mitsubishi Tanabe Pharma Corp | Novo derivado sulfonamida de ácido malónico e sua utilização farmacêutica |
| 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 |
| 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 |
| KR101580482B1 (ko) | 2007-11-16 | 2015-12-28 | 인사이트 홀딩스 코포레이션 | 야누스 키나제 억제제로서의 4-피라졸릴-n-아릴피리미딘-2-아민 및 4-피라졸릴-n-헤테로아릴피리미딘-2-아민 |
| JP2011519868A (ja) | 2008-05-05 | 2011-07-14 | シェーリング コーポレイション | 癌を処置するための化学療法剤の連続投与 |
| GEP20125502B (en) | 2008-05-23 | 2012-04-25 | Novartis Ag | Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors |
| US8592448B2 (en) | 2008-11-20 | 2013-11-26 | OSI Pharmaceuticals, LLC | Substituted pyrrolo[2,3-b]-pyridines and -pyrazines |
| EP2389376A1 (en) | 2009-01-21 | 2011-11-30 | 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 |
| CU24245B1 (es) | 2009-06-12 | 2017-02-02 | Centre Nat Rech Scient | QUINOLIN-6 AMINA Y QUINOLINA-7-AMINA DERIVADOS DE LA FÓRMULA (Id) y (Ir), Y SALES DERIVADAS |
| ES2534226T3 (es) | 2009-09-03 | 2015-04-20 | Bioenergenix | Compuestos heterocíclicos para la inhibición de PASK |
| US9340528B2 (en) | 2009-09-04 | 2016-05-17 | Bayer Pharma Aktiengesellschaft | 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 |
| KR101955691B1 (ko) | 2010-03-30 | 2019-03-07 | 베르선 코포레이션 | 트롬빈 억제제로서의 다중치환된 방향족 화합물 |
| 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 |
| CA2804304C (en) | 2010-05-24 | 2020-02-25 | Intellikine, Llc | 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 |
| WO2012104776A1 (en) | 2011-01-31 | 2012-08-09 | Novartis Ag | Novel heterocyclic derivatives |
| CN103491962B (zh) | 2011-02-23 | 2016-10-12 | 因特利凯有限责任公司 | 激酶抑制剂的组合及其用途 |
| 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 |
| EP2757885B1 (en) | 2011-09-21 | 2017-03-15 | Neupharma, Inc. | Certain chemical entites, compositions, and methods |
| AU2012318580A1 (en) | 2011-10-04 | 2014-05-22 | Gilead Calistoga Llc | Novel quinoxaline inhibitors of PI3K |
| 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 |
| 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 |
| KR20140090218A (ko) | 2011-10-28 | 2014-07-16 | 노파르티스 아게 | 신규 퓨린 유도체 및 질환의 치료에서의 그의 용도 |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| US9481911B2 (en) | 2012-03-08 | 2016-11-01 | Astellas Pharma Inc. | Methods for detecting FGFR3/TACC3 fusion genes |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (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 |
| EP3848034B1 (en) | 2014-03-26 | 2025-02-12 | Astex Therapeutics Limited | Cmet-inhibitors for use in delaying the emergence in resistance to fgfr inhibitors |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| DK3122359T3 (da) | 2014-03-26 | 2021-03-08 | Astex Therapeutics Ltd | Kombinationer af en fgfr-inhibitor og en igf1r-hæmmer |
| 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 |
-
2011
- 2011-10-28 GB GBGB1118656.6A patent/GB201118656D0/en not_active Ceased
-
2012
- 2012-10-15 JO JOP/2012/0308A patent/JO3419B1/ar active
- 2012-10-24 TW TW101139220A patent/TWI602814B/zh active
- 2012-10-26 AU AU2012328170A patent/AU2012328170B2/en active Active
- 2012-10-26 SG SG11201401055XA patent/SG11201401055XA/en unknown
- 2012-10-26 BR BR112014010206A patent/BR112014010206B8/pt active IP Right Grant
- 2012-10-26 SI SI201231385T patent/SI2776435T1/sl unknown
- 2012-10-26 UA UAA201405742A patent/UA111386C2/uk unknown
- 2012-10-26 CN CN201280065190.4A patent/CN104011051B/zh active Active
- 2012-10-26 US US14/354,832 patent/US9309242B2/en active Active
- 2012-10-26 MX MX2014004855A patent/MX353654B/es active IP Right Grant
- 2012-10-26 EP EP12794745.5A patent/EP2776435B1/en active Active
- 2012-10-26 UY UY0001034418A patent/UY34418A/es active IP Right Grant
- 2012-10-26 ES ES12794745.5T patent/ES2688868T3/es active Active
- 2012-10-26 EA EA201490891A patent/EA027563B1/ru unknown
- 2012-10-26 LT LTEP12794745.5T patent/LT2776435T/lt unknown
- 2012-10-26 AP AP2014007540A patent/AP4060A/en active
- 2012-10-26 IN IN948MUN2014 patent/IN2014MN00948A/en unknown
- 2012-10-26 AR ARP120104039A patent/AR088567A1/es active IP Right Grant
- 2012-10-26 MY MYPI2014001207A patent/MY185666A/en unknown
- 2012-10-26 WO PCT/GB2012/052672 patent/WO2013061080A1/en not_active Ceased
- 2012-10-26 CA CA2853390A patent/CA2853390C/en active Active
- 2012-10-26 KR KR1020147010849A patent/KR102066496B1/ko active Active
- 2012-10-26 PH PH1/2014/500867A patent/PH12014500867A1/en unknown
- 2012-10-26 JP JP2014537730A patent/JP6169583B2/ja active Active
- 2012-10-26 HR HRP20181533TT patent/HRP20181533T1/hr unknown
- 2012-10-26 DK DK12794745.5T patent/DK2776435T3/en active
-
2014
- 2014-04-10 IL IL232083A patent/IL232083B/en active IP Right Grant
- 2014-04-23 CO CO14086785A patent/CO6940422A2/es not_active Application Discontinuation
- 2014-04-25 CL CL2014001065A patent/CL2014001065A1/es unknown
- 2014-04-25 CR CR20140190A patent/CR20140190A/es unknown
- 2014-04-25 NI NI201400032A patent/NI201400032A/es unknown
- 2014-04-28 EC ECSP14013325 patent/ECSP14013325A/es unknown
-
2016
- 2016-02-09 US US15/019,563 patent/US10045982B2/en active Active
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JO3419B1 (ar) | مركبات بيريدوبيرازين مضادة للسرطان من خلال تثبيط إنزيمات كيناز fgfr | |
| MX356205B (es) | Benzopirazinas anticancerigenas via la inhibicion de cinasas del receptor del factor de crecimiento de fibroblasto (fgfr). | |
| MX359418B (es) | Pteridinas como inhibidores del receptor del factor de crecimiento de fribroblasto (fgfr). | |
| MX349004B (es) | Nuevos compuestos. | |
| MX366899B (es) | Nuevos compuestos. | |
| JO3366B1 (ar) | مثبطات بيرازوليل كوينوكزالين كاينيز | |
| MX353806B (es) | Quinolinas como moduladores de cinasas del receptor del factor de crecimiento de fibroblasto (fgfr). | |
| PH12016501898B1 (en) | Quinoxaline derivatives useful as fgfr kinase modulators | |
| PH12014502772A1 (en) | Substituted tricyclic compounds as fgfr inhibitors | |
| TR201816379T4 (tr) | DNA-PK inhibitörleri. | |
| EA201200473A1 (ru) | Замещенные (гетероарилметил)тиогидантоины | |
| EA201691032A1 (ru) | Производные изохромена в качестве ингибиторов фосфоинозитид-3-киназ | |
| EA201692313A1 (ru) | Производные индолизина в качестве ингибиторов фосфоинозитид-3-киназ | |
| WO2012162513A3 (en) | Alcohol-, diol-, and carbohydrate-substituted indenoisoquinolines as topoisomerase i inhibitors | |
| IN2014DN03010A (e) | ||
| UA110793C2 (uk) | Піразолілхіноксалінові інгібітори кінази | |
| PH12016502133A1 (en) | Substituted tricycle compounds as fgfr inhibitors |