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)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (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)
- Oncology (AREA)
- Pulmonology (AREA)
- Gastroenterology & Hepatology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
يتعلق الاختراع الحالي بمركبات جديدة مشتقة من البيريدوبيرازين، وبتركيبات صيدلانية تشتمل على هذه المركبات، وبعمليات لتحضير هذه المركبات وباستخدام هذه المركبات في علاج بعض الأمراض، مثل السرطان.
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 (ar) |
| EP (1) | EP2776435B1 (ar) |
| JP (1) | JP6169583B2 (ar) |
| KR (1) | KR102066496B1 (ar) |
| CN (1) | CN104011051B (ar) |
| AP (1) | AP4060A (ar) |
| AR (1) | AR088567A1 (ar) |
| AU (1) | AU2012328170B2 (ar) |
| BR (1) | BR112014010206B8 (ar) |
| CA (1) | CA2853390C (ar) |
| CL (1) | CL2014001065A1 (ar) |
| CO (1) | CO6940422A2 (ar) |
| CR (1) | CR20140190A (ar) |
| DK (1) | DK2776435T3 (ar) |
| EA (1) | EA027563B1 (ar) |
| EC (1) | ECSP14013325A (ar) |
| ES (1) | ES2688868T3 (ar) |
| GB (1) | GB201118656D0 (ar) |
| HR (1) | HRP20181533T1 (ar) |
| IL (1) | IL232083B (ar) |
| IN (1) | IN2014MN00948A (ar) |
| JO (1) | JO3419B1 (ar) |
| LT (1) | LT2776435T (ar) |
| MX (1) | MX353654B (ar) |
| MY (1) | MY185666A (ar) |
| NI (1) | NI201400032A (ar) |
| PH (1) | PH12014500867A1 (ar) |
| SG (1) | SG11201401055XA (ar) |
| SI (1) | SI2776435T1 (ar) |
| TW (1) | TWI602814B (ar) |
| UA (1) | UA111386C2 (ar) |
| UY (1) | UY34418A (ar) |
| WO (1) | WO2013061080A1 (ar) |
Families Citing this family (44)
| 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 |
| 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 |
| GB201118656D0 (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 |
| 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 |
| CN105683188B (zh) * | 2013-10-25 | 2018-02-09 | 诺华股份有限公司 | 作为fgfr4抑制剂的稠环二环吡啶基衍生物 |
| JP6752715B2 (ja) * | 2014-03-26 | 2020-09-09 | アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited | 組合せ |
| MX373150B (es) * | 2014-03-26 | 2020-04-21 | Astex Therapeutics Ltd | Combinaciones de un inhibidor del factor de crecimiento de fibroblasto (fgfr) y un inhibidor del receptor del factor de crecimiento 1 similar a insulina (igf1r). |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| KR102344105B1 (ko) | 2014-08-18 | 2021-12-29 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 모노시클릭 피리딘 유도체의 염 및 이의 결정 |
| JP6585167B2 (ja) * | 2014-10-03 | 2019-10-02 | ノバルティス アーゲー | Fgfr4阻害剤としての縮環二環式ピリジル誘導体の使用 |
| 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 |
| TWI719960B (zh) | 2015-02-10 | 2021-03-01 | 英商阿斯迪克治療公司 | 新穎組成物 |
| 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 |
| ES2887148T3 (es) | 2015-03-25 | 2021-12-21 | Nat Cancer Ct | Agente terapéutico contra el cáncer de vías biliares |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| AU2016328693B2 (en) | 2015-09-23 | 2021-03-11 | Janssen Pharmaceutica Nv | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| DK3353177T3 (da) | 2015-09-23 | 2020-08-24 | Janssen Pharmaceutica Nv | Tricykliske heterocykler til behandling af cancer |
| AU2016341445B2 (en) | 2015-10-23 | 2020-08-27 | Array Biopharma, Inc. | 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2H)-one compounds as inhibitors of FGFR tyrosine kinases |
| US12414945B2 (en) | 2015-12-17 | 2025-09-16 | Eisai R&D Management 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 |
| EP3498707A4 (en) * | 2016-08-12 | 2020-04-08 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | FGFR4 INHIBITOR, PREPARATION METHOD THEREOF AND USE THEREOF |
| 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 |
| SG11202007591RA (en) | 2018-03-28 | 2020-09-29 | Eisai R&D Man Co Ltd | Therapeutic agent for hepatocellular carcinoma |
| EP3898615A1 (en) | 2018-12-19 | 2021-10-27 | Array Biopharma, Inc. | 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer |
| WO2020131627A1 (en) | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases |
| WO2021138391A1 (en) | 2019-12-30 | 2021-07-08 | Tyra Biosciences, Inc. | Indazole compounds |
| WO2021138392A1 (en) | 2019-12-30 | 2021-07-08 | Tyra Biosciences, Inc. | Aminopyrimidine compounds |
| CN114945367A (zh) * | 2020-01-17 | 2022-08-26 | 贝达医药公司 | 作为fgfr激酶抑制剂的哒嗪和1,2,4-三嗪衍生物 |
| CR20230325A (es) | 2020-12-30 | 2023-12-11 | Tyra Biosciences Inc | Compuestos de indazol como inhibidores de cinasas |
| BR112023016986A2 (pt) | 2021-02-26 | 2023-11-07 | Tyra Biosciences Inc | Compostos de aminopirimidina e métodos de seu uso |
| JP2025525433A (ja) | 2022-06-29 | 2025-08-05 | タイラ・バイオサイエンシーズ・インコーポレイテッド | インダゾール化合物 |
| EP4547670A1 (en) | 2022-06-29 | 2025-05-07 | 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 |
| WO2026035809A1 (en) | 2024-08-06 | 2026-02-12 | Tyra Biosciences, Inc. | Indazole compounds for the treatment of cancer |
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 |
| DE69828607T2 (de) | 1997-05-28 | 2006-01-05 | Aventis Pharmaceuticals Inc. | CHINOLIN- UND CHINOXALIN-VERBINDUNGEN DIE DEN VON BLUTPLÄTTCHEN ABSTAMMMENDEN WACHSTUMSFAKTOR UND/ODER PDGF- UND P56lck-TYROSIN-KINASE HEMMEN |
| 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 |
| EP1409487A1 (en) | 1999-09-15 | 2004-04-21 | Warner-Lambert Company Llc | 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 |
| DE60234125D1 (de) | 2001-12-24 | 2009-12-03 | Astrazeneca Ab | E inhibitoren |
| JP2003213463A (ja) | 2002-01-17 | 2003-07-30 | Sumitomo Chem Co Ltd | 金属腐食防止剤および洗浄液 |
| US7223738B2 (en) | 2002-04-08 | 2007-05-29 | Merck & Co., Inc. | 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 |
| KR20120032574A (ko) | 2002-10-03 | 2012-04-05 | 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 |
| US7098332B2 (en) | 2002-12-20 | 2006-08-29 | Hoffmann-La Roche Inc. | 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones |
| EP1590341B1 (en) | 2003-01-17 | 2009-06-17 | Warner-Lambert Company LLC | 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation |
| WO2004098494A2 (en) | 2003-04-30 | 2004-11-18 | Cytokinetics, Inc. | Compounds, compositions, and methods |
| JP4847868B2 (ja) | 2003-05-14 | 2011-12-28 | ニューロジェネティック ファーマシューティカルズ、 インコーポレイテッド | 化合物、及び、アミロイドベータの調節におけるその使用 |
| AU2004240747B2 (en) | 2003-05-23 | 2008-01-03 | Zentaris Gmbh | Novel pyridopyrazines and use thereof as kinase modulators |
| 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 |
| WO2005009437A1 (en) | 2003-07-21 | 2005-02-03 | Bethesda Pharmaceuticals, Inc. | Design and synthesis of optimized ligands for ppar |
| CA2534649A1 (en) | 2003-08-01 | 2005-02-10 | Genelabs Technologies, Inc. | Bicyclic imidazol derivatives against flaviviridae |
| CA2537224A1 (en) | 2003-10-17 | 2005-05-06 | 4 Aza Bioscience Nv | Heterocycle-substituted pteridine derivatives and their use in therapy |
| CN102225926A (zh) | 2003-11-07 | 2011-10-26 | 诺华疫苗和诊断公司 | 具有改进药物特性的喹啉酮类化合物的药学上可接受的盐 |
| EA009875B1 (ru) | 2003-11-20 | 2008-04-28 | Янссен Фармацевтика Н.В. | 6-алкенил и 6-фенилалкил замещенные 2-хинолиноны и 2-хиноксалиноны в качестве ингибиторов поли(адф-рибоза) полимеразы |
| 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 |
| BRPI0418078A8 (pt) | 2003-12-23 | 2018-01-02 | Astex Therapeutics Ltd | composto ou um seu sal, solvato, tautômero ou n-óxido, uso de um composto, métodos para a profilaxia ou tratamento de um estado ou condição doentia mediada pela proteína quinase b e mediada pela proteína quinase a, para tratar uma doença ou condição, para inibir uma proteína quinase b e uma proteína quinase a, para modular um processo celular, para tratar um distúrbio imune em um mamífero e para induzir apoptose em uma célula cancerosa, composição farmacêutica, e, processo para a preparação de um composto |
| 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 |
| 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 |
| MX2007004276A (es) | 2004-10-14 | 2007-05-16 | Hoffmann La Roche | 1,5-naftiridin-azolidinonas que tienen actividad antiproliferativa de cdk-1. |
| PT1830869E (pt) | 2004-12-24 | 2013-08-22 | Spinifex Pharm Pty Ltd | Método de tratamento ou profilaxia |
| US8278290B2 (en) | 2005-02-14 | 2012-10-02 | Biononics Limited | Tubulin polymerisation inhibitors |
| WO2006092430A1 (de) | 2005-03-03 | 2006-09-08 | Universität des Saarlandes | Selektive hemmstoffe humaner corticoidsynthasen |
| US20090156617A1 (en) | 2005-05-12 | 2009-06-18 | Northrup Alan B | Tyrosine kinase inhibitors |
| WO2006124944A1 (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 |
| AU2006283846B2 (en) | 2005-08-26 | 2012-04-05 | Merck Serono Sa | Pyrazine derivatives and use as PI3K inhibitors |
| EP1790342A1 (de) * | 2005-11-11 | 2007-05-30 | Zentaris GmbH | Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege |
| AU2006313701B2 (en) | 2005-11-11 | 2012-05-31 | Aeterna Zentaris Gmbh | Novel pyridopyrazines and their use as modulators of kinases |
| US8217042B2 (en) | 2005-11-11 | 2012-07-10 | Zentaris Gmbh | Pyridopyrazines and their use as modulators of kinases |
| HUE030390T2 (en) | 2005-12-21 | 2017-05-29 | Janssen Pharmaceutica Nv | Triazolopyridazines as tyrosine kinase modulators |
| CA2651072A1 (en) | 2006-05-01 | 2007-11-08 | Pfizer Products Inc. | Substituted 2-amino-fused heterocyclic compounds |
| GB0609621D0 (en) | 2006-05-16 | 2006-06-21 | Astrazeneca Ab | Novel co-crystal |
| EP2029600B1 (de) | 2006-05-24 | 2012-03-14 | Boehringer Ingelheim International GmbH | Substituierte pteridine, die mit einem viergliedrigen heterocyclus substituiert sind |
| 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 |
| CA2672828A1 (en) | 2006-12-13 | 2008-06-26 | Schering Corporation | Methods of treatment |
| AU2007336811A1 (en) | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| WO2008078091A1 (en) | 2006-12-22 | 2008-07-03 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as fgfr inhibitors |
| CA2673003A1 (en) | 2006-12-22 | 2008-07-03 | Novartis Ag | Quinazolines for pdk1 inhibition |
| KR20080062876A (ko) | 2006-12-29 | 2008-07-03 | 주식회사 대웅제약 | 신규한 항진균성 트리아졸 유도체 |
| PE20090288A1 (es) | 2007-05-10 | 2009-04-03 | Smithkline Beecham Corp | Derivados de quinoxalina como inhibidores de la pi3 quinasa |
| EP1990342A1 (en) * | 2007-05-10 | 2008-11-12 | AEterna Zentaris GmbH | Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof |
| WO2008150827A1 (en) | 2007-05-29 | 2008-12-11 | 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 |
| US8461209B2 (en) | 2007-06-20 | 2013-06-11 | Mitsubishi Tanabe Pharma Corporation | Malonic acid sulfonamide derivative and pharmaceutical use thereof |
| 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 |
| WO2009019518A1 (en) | 2007-08-09 | 2009-02-12 | Astrazeneca Ab | Pyrimidine compounds having a fgfr inhibitory effect |
| WO2009021083A1 (en) | 2007-08-09 | 2009-02-12 | Smithkline Beecham Corporation | Quinoxaline derivatives as pi3 kinase inhibitors |
| 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 |
| 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 |
| 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 |
| 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 |
| SI2440547T1 (sl) | 2009-06-12 | 2023-05-31 | Abivax | Nove kemične molekule, ki zavirajo mehanizem spajanja za zdravljenje bolezni, ki so posledica napak pri spajanju |
| PH12012500382A1 (en) | 2009-09-03 | 2012-10-22 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| 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 |
| JP6155187B2 (ja) | 2010-03-30 | 2017-06-28 | ヴァーセオン コーポレイション | トロンビンの阻害剤としての多置換芳香族化合物 |
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| WO2011146591A1 (en) | 2010-05-19 | 2011-11-24 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
| US9096590B2 (en) | 2010-05-24 | 2015-08-04 | Intellikine Llc | Substituted benzoxazoles as PI3 kinase inhibitors |
| 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 |
| JP5963777B2 (ja) | 2011-01-31 | 2016-08-03 | ノバルティス アーゲー | 新規ヘテロ環誘導体 |
| US9295673B2 (en) | 2011-02-23 | 2016-03-29 | Intellikine Llc | Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof |
| WO2012118492A1 (en) | 2011-03-01 | 2012-09-07 | Array Biopharma Inc. | Heterocyclic sulfonamides as raf inhibitors |
| CA2846574C (en) | 2011-08-26 | 2020-07-07 | Neupharma, Inc. | Quinoxaline sulfonamide derivates for use as kinase inhibitors |
| CN108794411B (zh) | 2011-09-14 | 2022-06-07 | 润新生物公司 | 某些化学实体、组合物及方法 |
| US9249110B2 (en) | 2011-09-21 | 2016-02-02 | Neupharma, Inc. | Substituted quinoxalines as B-raf kinase inhibitors |
| JP2014528451A (ja) | 2011-10-04 | 2014-10-27 | ギリアード カリストガ エルエルシー | Pi3kの新規キノキサリン阻害剤 |
| 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 |
| JO3210B1 (ar) | 2011-10-28 | 2018-03-08 | Merck Sharp & Dohme | مثبط منصهر لبروتين نقل الكوليسترليستير اوكسازوليدينون ثمائي الحلقة |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| CN104039790B (zh) | 2011-10-28 | 2016-04-13 | 诺华股份有限公司 | 嘌呤衍生物及它们在治疗疾病中的应用 |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| HK1205528A1 (en) | 2012-03-08 | 2015-12-18 | Astellas Pharma Inc. | Novel fgfr3 fusion product |
| 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 |
| MX373150B (es) | 2014-03-26 | 2020-04-21 | Astex Therapeutics Ltd | Combinaciones de un inhibidor del factor de crecimiento de fibroblasto (fgfr) y un inhibidor del receptor del factor de crecimiento 1 similar a insulina (igf1r). |
| JP6752715B2 (ja) | 2014-03-26 | 2020-09-09 | アステックス、セラピューティックス、リミテッドAstex Therapeutics Limited | 組合せ |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| TWI719960B (zh) | 2015-02-10 | 2021-03-01 | 英商阿斯迪克治療公司 | 新穎組成物 |
| 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 AP AP2014007540A patent/AP4060A/en active
- 2012-10-26 IN IN948MUN2014 patent/IN2014MN00948A/en unknown
- 2012-10-26 CN CN201280065190.4A patent/CN104011051B/zh active Active
- 2012-10-26 MY MYPI2014001207A patent/MY185666A/en unknown
- 2012-10-26 BR BR112014010206A patent/BR112014010206B8/pt active IP Right Grant
- 2012-10-26 LT LTEP12794745.5T patent/LT2776435T/lt unknown
- 2012-10-26 SG SG11201401055XA patent/SG11201401055XA/en unknown
- 2012-10-26 MX MX2014004855A patent/MX353654B/es active IP Right Grant
- 2012-10-26 AR ARP120104039A patent/AR088567A1/es active IP Right Grant
- 2012-10-26 AU AU2012328170A patent/AU2012328170B2/en active Active
- 2012-10-26 CA CA2853390A patent/CA2853390C/en active Active
- 2012-10-26 SI SI201231385T patent/SI2776435T1/sl unknown
- 2012-10-26 EA EA201490891A patent/EA027563B1/ru unknown
- 2012-10-26 UY UY0001034418A patent/UY34418A/es active IP Right Grant
- 2012-10-26 DK DK12794745.5T patent/DK2776435T3/en active
- 2012-10-26 HR HRP20181533TT patent/HRP20181533T1/hr unknown
- 2012-10-26 ES ES12794745.5T patent/ES2688868T3/es active Active
- 2012-10-26 WO PCT/GB2012/052672 patent/WO2013061080A1/en not_active Ceased
- 2012-10-26 UA UAA201405742A patent/UA111386C2/uk unknown
- 2012-10-26 EP EP12794745.5A patent/EP2776435B1/en 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 US US14/354,832 patent/US9309242B2/en active Active
- 2012-10-26 KR KR1020147010849A patent/KR102066496B1/ko active 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 NI NI201400032A patent/NI201400032A/es unknown
- 2014-04-25 CR CR20140190A patent/CR20140190A/es unknown
- 2014-04-25 CL CL2014001065A patent/CL2014001065A1/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 | |
| MX2014004861A (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 (ar) | ||
| UA110793C2 (uk) | Піразолілхіноксалінові інгібітори кінази | |
| PH12016502133A1 (en) | Substituted tricycle compounds as fgfr inhibitors |