JP2019529475A5 - - Google Patents
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- JP2019529475A5 JP2019529475A5 JP2019516455A JP2019516455A JP2019529475A5 JP 2019529475 A5 JP2019529475 A5 JP 2019529475A5 JP 2019516455 A JP2019516455 A JP 2019516455A JP 2019516455 A JP2019516455 A JP 2019516455A JP 2019529475 A5 JP2019529475 A5 JP 2019529475A5
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Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022117973A JP2022136163A (ja) | 2016-09-27 | 2022-07-25 | Dna損傷剤とdna-pk阻害剤との組合せ物を使用する、がんを処置するための方法 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662400606P | 2016-09-27 | 2016-09-27 | |
| US62/400,606 | 2016-09-27 | ||
| US201662497943P | 2016-12-08 | 2016-12-08 | |
| US62/497,943 | 2016-12-08 | ||
| PCT/US2017/053589 WO2018064092A1 (en) | 2016-09-27 | 2017-09-27 | Method for treating cancer using a combination of dna-damaging agents and dna-pk inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022117973A Division JP2022136163A (ja) | 2016-09-27 | 2022-07-25 | Dna損傷剤とdna-pk阻害剤との組合せ物を使用する、がんを処置するための方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019529475A JP2019529475A (ja) | 2019-10-17 |
| JP2019529475A5 true JP2019529475A5 (enExample) | 2020-10-22 |
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Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019516455A Pending JP2019529475A (ja) | 2016-09-27 | 2017-09-27 | Dna損傷剤とdna−pk阻害剤との組合せ物を使用する、がんを処置するための方法 |
| JP2022117973A Pending JP2022136163A (ja) | 2016-09-27 | 2022-07-25 | Dna損傷剤とdna-pk阻害剤との組合せ物を使用する、がんを処置するための方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022117973A Pending JP2022136163A (ja) | 2016-09-27 | 2022-07-25 | Dna損傷剤とdna-pk阻害剤との組合せ物を使用する、がんを処置するための方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US11110108B2 (enExample) |
| EP (1) | EP3518931A4 (enExample) |
| JP (2) | JP2019529475A (enExample) |
| KR (1) | KR20190062485A (enExample) |
| AU (1) | AU2017335648B2 (enExample) |
| CA (1) | CA3038657A1 (enExample) |
| IL (1) | IL265523B (enExample) |
| MX (1) | MX394860B (enExample) |
| RU (1) | RU2758669C2 (enExample) |
| TW (1) | TW201815418A (enExample) |
| WO (1) | WO2018064092A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2758669C2 (ru) | 2016-09-27 | 2021-11-01 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с применением сочетания днк-поражающих агентов и ингибиторов днк-пк |
| CN112574179B (zh) * | 2019-09-29 | 2022-05-10 | 山东轩竹医药科技有限公司 | Dna-pk抑制剂 |
| CN112574211B (zh) * | 2019-09-29 | 2022-06-14 | 山东轩竹医药科技有限公司 | 杂环类激酶抑制剂 |
| CN111956639B (zh) * | 2020-09-03 | 2023-06-09 | 辽宁大学 | 有机硒化合物的神经炎症相关疾病治疗用途 |
| JP2023546159A (ja) * | 2020-10-19 | 2023-11-01 | バルーク エス.ブルームバーグ インスティテュート | がんを診断および治療するための方法およびキット |
| EP4559467A1 (en) * | 2022-07-20 | 2025-05-28 | Kangbaida (Sichuan) Biotechnology Co., Ltd. | Use of imidazolinone derivative combined with doxorubicin in treatment of tumors |
Family Cites Families (191)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5571506A (en) | 1989-08-14 | 1996-11-05 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Aromatic oligomeric compounds useful as mimics of bioactive macromolecules |
| AU658134B2 (en) | 1989-12-28 | 1995-04-06 | Virginia Commonwealth University | Sigma receptor ligands and the use thereof |
| EP0498722B1 (fr) | 1991-02-07 | 1997-07-30 | Roussel Uclaf | Dérivés bicycliques azotés, leur procédé de préparation, les intermédiaires obtenus, leur application comme médicaments et les compositions pharmaceutiques les renfermant |
| US6004979A (en) | 1991-02-07 | 1999-12-21 | Hoechst Marion Roussel | Nitrogenous bicycles |
| EP0519211A1 (de) | 1991-05-17 | 1992-12-23 | Hoechst Schering AgrEvo GmbH | Substituierte 4-Aminopyrimidine, Verfahren zu ihrer Herstellung und ihre Verwendung als Schädlingsbekämpfungsmittel |
| DE4208254A1 (de) | 1992-03-14 | 1993-09-16 | Hoechst Ag | Substituierte pyrimidine, verfahren zu ihrer herstellung und ihre verwendung als schaedlingsbekaempfungsmittel und fungizid |
| AU3933493A (en) | 1992-04-24 | 1993-11-29 | E.I. Du Pont De Nemours And Company | Arthropodicidal and fungicidal aminopyrimidines |
| US5595756A (en) | 1993-12-22 | 1997-01-21 | Inex Pharmaceuticals Corporation | Liposomal compositions for enhanced retention of bioactive agents |
| DE4437406A1 (de) | 1994-10-19 | 1996-04-25 | Hoechst Ag | Chinoxaline, Verfahren zu ihrer Herstellung und ihre Verwendung |
| US5977117A (en) | 1996-01-05 | 1999-11-02 | Texas Biotechnology Corporation | Substituted phenyl compounds and derivatives thereof that modulate the activity of endothelin |
| WO1998037079A1 (en) | 1997-02-19 | 1998-08-27 | Berlex Laboratories, Inc. | N-heterocyclic derivatives as nos inhibitors |
| JPH10251255A (ja) | 1997-03-14 | 1998-09-22 | Nissan Chem Ind Ltd | アジン誘導体 |
| SK158099A3 (en) | 1997-05-28 | 2000-06-12 | Rhone Poulenc Rorer Pharma | Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases |
| DE19801598C2 (de) | 1998-01-17 | 2000-05-11 | Aventis Res & Tech Gmbh & Co | Katalytische Synthese von N-alkylierten Anilinen aus Olefinen und Anilinen |
| DE19836697A1 (de) | 1998-08-13 | 2000-02-17 | Hoechst Marion Roussel De Gmbh | Substituierte 4-Amino-2-aryl-pyrimidine, ihre Herstellung, ihre Verwendung und sie enthaltende pharmazeutische Präparate |
| AU3033500A (en) | 1999-01-15 | 2000-08-01 | Agouron Pharmaceuticals, Inc. | Non-peptide glp-1 agonists |
| ATE396978T1 (de) | 1999-10-07 | 2008-06-15 | Amgen Inc | Triazin-kinase-hemmer |
| GB9924092D0 (en) | 1999-10-13 | 1999-12-15 | Zeneca Ltd | Pyrimidine derivatives |
| US6552016B1 (en) | 1999-10-14 | 2003-04-22 | Curis, Inc. | Mediators of hedgehog signaling pathways, compositions and uses related thereto |
| AU2001234690A1 (en) | 2000-02-01 | 2001-08-14 | Cor Therapeutics, Inc. | 2-(1h)-quinolone and 2-(1h)-quinoxalone inhibitors of factor xa |
| WO2001064643A2 (en) | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | BENZAMIDES AND RELATED INHIBITORS OF FACTOR Xa |
| WO2001064646A2 (en) | 2000-03-01 | 2001-09-07 | Tularik Inc. | Hydrazones and analogs as cholesterol lowering agents |
| DE10013318A1 (de) | 2000-03-17 | 2001-09-20 | Merck Patent Gmbh | Formulierung enthaltend Chinoxalinderivate |
| US7498304B2 (en) | 2000-06-16 | 2009-03-03 | Curis, Inc. | Angiogenesis-modulating compositions and uses |
| EP1351946A2 (en) | 2000-09-01 | 2003-10-15 | Icos Corporation | Materials and methods to potentiate cancer treatment |
| US6613776B2 (en) | 2000-09-15 | 2003-09-02 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US7473691B2 (en) | 2000-09-15 | 2009-01-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6610677B2 (en) | 2000-09-15 | 2003-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| MXPA03002297A (es) | 2000-09-15 | 2003-06-06 | Vertex Pharma | Compuestos de triazol utiles como inhibidores de proteina cinasa. |
| US20020111353A1 (en) | 2000-12-05 | 2002-08-15 | Mark Ledeboer | Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases |
| ES2375491T3 (es) | 2000-12-21 | 2012-03-01 | Vertex Pharmaceuticals Incorporated | Compuestos de pirazol útiles como agentes inhibidores de las prote�?na-quinasas. |
| EP1363904A1 (en) | 2001-02-02 | 2003-11-26 | Glaxo Group Limited | Pyrazoles as tgf inhibitors |
| MY130778A (en) | 2001-02-09 | 2007-07-31 | Vertex Pharma | Heterocyclic inhibitiors of erk2 and uses thereof |
| EP1373257B9 (en) | 2001-03-29 | 2008-10-15 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| US6642227B2 (en) | 2001-04-13 | 2003-11-04 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases |
| WO2002085909A1 (en) | 2001-04-20 | 2002-10-31 | Vertex Pharmaceuticals Incorporated | 9-deazaguanine derivatives as inhibitors of gsk-3 |
| AU2002308748A1 (en) | 2001-05-16 | 2002-11-25 | Vertex Pharmaceuticals Incorporated | Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases |
| MXPA03010961A (es) | 2001-05-31 | 2004-02-27 | Vertex Pharma | Compuestos de tiazol utiles como inhibidores de proteinas cinasas. |
| ES2274035T3 (es) | 2001-06-01 | 2007-05-16 | Vertex Pharmaceuticals Incorporated | Compuestos de tiazol utiles como inhibidores de proteina quinasas. |
| MXPA03011652A (es) | 2001-06-15 | 2004-05-31 | Vertex Pharma | 5-(2-aminopirimidin-4-il) benzioxazoles como inhibidores de proteinas cinasa. |
| JP4342937B2 (ja) | 2001-07-03 | 2009-10-14 | バーテックス ファーマシューティカルズ インコーポレイテッド | SrcおよびLckタンパク質キナーゼの阻害剤としてのイソキサゾールピリミジン |
| US20030199526A1 (en) | 2001-12-07 | 2003-10-23 | Deborah Choquette | Pyrimidine-based compounds useful as GSK-3 inhibitors |
| ES2437391T3 (es) | 2002-02-06 | 2014-01-10 | Vertex Pharmaceuticals, Inc. | Compuestos de heteroarilo útiles como inhibidores de GSK-3 |
| US20030199525A1 (en) | 2002-03-21 | 2003-10-23 | Hirst Gavin C. | Kinase inhibitors |
| US20030207873A1 (en) | 2002-04-10 | 2003-11-06 | Edmund Harrington | Inhibitors of Src and other protein kinases |
| EP1506189A1 (en) | 2002-04-26 | 2005-02-16 | Vertex Pharmaceuticals Incorporated | Pyrrole derivatives as inhibitors of erk2 and uses thereof |
| ATE489384T1 (de) | 2002-05-06 | 2010-12-15 | Vertex Pharma | Thiadiazole oder oxadiazole und ihre verwendung als jak proteinkinaseinhibitoren |
| MXPA04011956A (es) | 2002-05-30 | 2005-03-31 | Vertex Pharma | Inhibidores de proteinas cinasas jak y cdk2. |
| MY141867A (en) | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| EP1554269A1 (en) | 2002-07-09 | 2005-07-20 | Vertex Pharmaceuticals Incorporated | Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities |
| US7304071B2 (en) | 2002-08-14 | 2007-12-04 | Vertex Pharmaceuticals Incorporated | Protein kinase inhibitors and uses thereof |
| US7419984B2 (en) | 2002-10-17 | 2008-09-02 | Cell Therapeutics, Inc. | Pyrimidines and uses thereof |
| WO2004041789A1 (en) | 2002-11-01 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of jak and other protein kinases |
| US7259161B2 (en) | 2002-11-04 | 2007-08-21 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of JAK and other protein kinases |
| AU2003297160A1 (en) | 2002-12-18 | 2004-07-22 | Vertex Pharmaceuticals Incorporated | Benzisoxazole derivatives useful as inhibitors of protein kinases |
| BR0317882A (pt) * | 2002-12-31 | 2005-12-13 | Bharat Serums & Vaccines Ltd | Processo para fabricação de lipossomas de longa circulação não tratados com peg; lipossoma; composição de doxorrubicina lipossomal de longa duração não tratada com peg; e método |
| US7144911B2 (en) | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| CA2514092C (en) | 2003-01-21 | 2013-03-19 | S.S.C.I., Inc. | Novel cocrystallization of hydrochloric acid salt of an active agent |
| WO2004072063A1 (en) | 2003-02-07 | 2004-08-26 | Vertex Pharmaceuticals Incorporated | Heteroaryl substituted pyrolls useful as inhibitors of protein kinases |
| DE602004024374D1 (de) | 2003-03-13 | 2010-01-14 | Vertex Pharma | Zusammensetzungen zur verwendung als protein-kinase-inhibitoren |
| EP1660473A2 (en) | 2003-03-24 | 2006-05-31 | Luitpold Pharmaceuticals, Inc. | Xanthones, thioxanthones and acridinones as dna-pk inhibitors |
| US20040235834A1 (en) | 2003-03-25 | 2004-11-25 | Farmer Luc J. | Thiazoles useful as inhibitors of protein kinases |
| US6875781B2 (en) | 2003-04-04 | 2005-04-05 | Cell Therapeutics, Inc. | Pyridines and uses thereof |
| US7189724B2 (en) | 2003-04-15 | 2007-03-13 | Valeant Research And Development | Quinoxaline derivatives having antiviral activity |
| US8084457B2 (en) | 2003-09-15 | 2011-12-27 | Lead Discovery Center Gmbh | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
| WO2005068468A2 (en) | 2003-12-02 | 2005-07-28 | Vertex Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors and uses thereof |
| CA2548172A1 (en) | 2003-12-04 | 2005-06-23 | Vertex Pharmaceuticals Incorporated | Quinoxalines useful as inhibitors of protein kinases |
| TW200533357A (en) | 2004-01-08 | 2005-10-16 | Millennium Pharm Inc | 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases |
| WO2005089757A1 (en) | 2004-03-15 | 2005-09-29 | Sunesis Pharmaceuticals, Inc. | Sns-595 and methods of using the same |
| GB0405985D0 (en) | 2004-03-17 | 2004-04-21 | Novartis Forschungsstiftung | Kinase |
| NZ551583A (en) | 2004-05-14 | 2009-05-31 | Vertex Pharma | Prodrugs of pyrrolylpyrimidine ERK protein kinase inhibitors |
| JP4449580B2 (ja) | 2004-05-31 | 2010-04-14 | 宇部興産株式会社 | 4−アラルキルアミノピリミジン誘導体及び抗菌剤 |
| DK1756084T3 (da) | 2004-06-04 | 2009-03-23 | Arena Pharm Inc | Substituerede aryl- og heteroarylderivater som modulatorer af metabolisme og forebyggelse og behandling af forstyrrelser beslægtet dermed |
| DE602005025655D1 (de) | 2004-09-17 | 2011-02-10 | Vertex Pharma | Als proteinkinaseinhibitoren geeignete diaminotriazolverbindungen |
| CA2583177A1 (en) | 2004-10-13 | 2006-04-27 | Ptc Therapeutics, Inc. | Compounds for nonsense suppression, and methods for their use |
| BRPI0518126A (pt) | 2004-10-15 | 2008-10-28 | Astrazeneca Ab | composto, processo para preparar o mesmo, composição farmacêutica, uso de um composto, e, métodos para produzir um efeito inibitório de b-raf e um efeito anti-cáncer em um animal de sangue quente, e para tratar uma doença ou condição |
| HN2005000795A (es) | 2004-10-15 | 2010-08-19 | Aventis Pharma Inc | Pirimidinas como antagonistas del receptor de prostaglandina d2 |
| US20090117176A1 (en) * | 2004-10-26 | 2009-05-07 | Pharma Mar, S.A. Sociedad Unipersonal | Anticancer Treatments |
| WO2006050249A1 (en) | 2004-10-29 | 2006-05-11 | Vertex Pharmaceuticals Incorporated | Diaminotriazole compounds useful as inhibitors of protein kinases |
| US7517870B2 (en) | 2004-12-03 | 2009-04-14 | Fondazione Telethon | Use of compounds that interfere with the hedgehog signaling pathway for the manufacture of a medicament for preventing, inhibiting, and/or reversing ocular diseases related with ocular neovascularization |
| WO2006065820A2 (en) | 2004-12-14 | 2006-06-22 | Vertex Pharmaceuticals Incorporated | Pyrimidine inhibitors of erk protein kinase and uses therof |
| US7501415B2 (en) | 2004-12-23 | 2009-03-10 | Vertex Pharmaceuticals Incorporated | Selective inhibitors of ERK protein kinase and uses thereof |
| MY158077A (en) | 2005-02-04 | 2016-08-30 | Senomyx Inc | Compounds comprising linked heteroaryl moieties and their use as novel umami flavor modifiers tastants and taste enhancers for comestible compositions |
| CN101184395A (zh) | 2005-04-06 | 2008-05-21 | Irm责任有限公司 | 包含二芳基胺的化合物和组合物及其作为类固醇激素核受体调节剂的用途 |
| AR053358A1 (es) | 2005-04-15 | 2007-05-02 | Cancer Rec Tech Ltd | Inhibidores de adn - pk |
| JP2006316040A (ja) * | 2005-05-13 | 2006-11-24 | Genentech Inc | Herceptin(登録商標)補助療法 |
| WO2006125616A2 (en) | 2005-05-25 | 2006-11-30 | Ingenium Pharmaceuticals Ag | Pyrimidine-based cdk inhibitors for treating pain |
| JP2008542253A (ja) * | 2005-05-26 | 2008-11-27 | クドス ファーマシューティカルズ リミテッド | Dna損傷癌療法に対してatm欠損癌を感作するためのdna−pk阻害の使用 |
| WO2006138418A2 (en) | 2005-06-14 | 2006-12-28 | President And Fellows Of Harvard College | Improvement of cognitive performance with sirtuin activators |
| JP2007008045A (ja) | 2005-06-30 | 2007-01-18 | Mitsui Chemicals Inc | 光記録媒体および1h−キノキサリン−2−オン誘導体 |
| EP1906967A4 (en) | 2005-07-26 | 2010-07-28 | Vertex Pharma | ABL Kinase Inhibition |
| GB0520657D0 (en) | 2005-10-11 | 2005-11-16 | Ludwig Inst Cancer Res | Pharmaceutical compounds |
| EP1942732A2 (en) | 2005-11-02 | 2008-07-16 | Cytokinetics, Inc. | Certain chemical entities, compositions, and methods |
| NZ606263A (en) | 2005-11-03 | 2014-03-28 | Vertex Pharma | Sliding panel suspension system |
| AU2006315334B2 (en) | 2005-11-16 | 2011-05-19 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| WO2007082899A1 (en) | 2006-01-17 | 2007-07-26 | Vib Vzw | Inhibitors of prolyl-hydroxylase 1 for the treatment of skeletal muscle degeneration |
| JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| UY30118A1 (es) | 2006-01-31 | 2007-06-29 | Tanabe Seiyaku Co | Compueto amina trisustituido |
| WO2007109783A2 (en) | 2006-03-23 | 2007-09-27 | Janssen Pharmaceutica, N.V. | Substituted pyrimidine kinase inhibitors |
| US20080280891A1 (en) | 2006-06-27 | 2008-11-13 | Locus Pharmaceuticals, Inc. | Anti-cancer agents and uses thereof |
| EP2043635A2 (en) * | 2006-06-29 | 2009-04-08 | Astex Therapeutics Limited | Pharmaceutical combinations |
| WO2008008852A2 (en) | 2006-07-11 | 2008-01-17 | Emory University | Cxcr4 antagonists including heteroatoms for the treatment of medical disorders |
| TW200811134A (en) | 2006-07-12 | 2008-03-01 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| PE20080403A1 (es) | 2006-07-14 | 2008-04-25 | Amgen Inc | Derivados heterociclicos fusionados y metodos de uso |
| JP4960450B2 (ja) | 2006-07-14 | 2012-06-27 | ノバルティス アーゲー | Alk−5阻害剤としてのピリミジン誘導体 |
| US7635683B2 (en) | 2006-08-04 | 2009-12-22 | Enanta Pharmaceuticals, Inc. | Quinoxalinyl tripeptide hepatitis C virus inhibitors |
| EP2589597B1 (en) | 2006-08-22 | 2019-03-06 | Technion Research & Development Foundation | Heterocyclic derivatives binding to the peripheral-type benzodiazepine receptor (PBR) |
| EP1903038A1 (de) | 2006-09-07 | 2008-03-26 | Bayer Schering Pharma Aktiengesellschaft | N-(1-Hetaryl-piperidin-4-yl)-(het)arylamide als EP2-Rezeptor Modulatoren |
| US7875603B2 (en) | 2006-09-21 | 2011-01-25 | Nova Southeastern University | Specific inhibitors for vascular endothelial growth factor receptors |
| MX2009003456A (es) | 2006-10-02 | 2009-04-14 | Irm Llc | Compuestos y composiciones como inhibidores de proteina cinasa. |
| DE102006050512A1 (de) | 2006-10-26 | 2008-04-30 | Bayer Healthcare Ag | Substituierte heterocyclische Verbindungen und ihre Verwendung |
| EP2086965B1 (en) | 2006-11-02 | 2010-02-10 | Vertex Pharmaceuticals, Inc. | Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases |
| JP2010511727A (ja) | 2006-12-04 | 2010-04-15 | ニューロクライン バイオサイエンシーズ,インコーポレイテッド | アデノシン受容体アンタゴニストとしての置換ピリミジン |
| JP2010513567A (ja) | 2006-12-19 | 2010-04-30 | バーテックス ファーマシューティカルズ インコーポレイテッド | プロテインキナーゼの阻害剤として有用なアミノピリミジン |
| CA2671851A1 (en) | 2006-12-28 | 2008-07-10 | Ambrx, Inc. | Phenazine and quinoxaline substituted amino acids and polypeptides |
| EP2114900B1 (en) | 2007-01-31 | 2018-10-10 | YM BioSciences Australia Pty Ltd | Thiopyrimidine-based compounds and uses thereof |
| WO2008106202A1 (en) | 2007-02-27 | 2008-09-04 | Housey Gerard M | Theramutein modulators |
| NZ579483A (en) | 2007-03-09 | 2012-07-27 | Vertex Pharma | Aminopyridines useful as inhibitors of protein kinases |
| ES2435997T3 (es) | 2007-03-09 | 2013-12-26 | Vertex Pharmaceuticals, Inc. | Aminopirimidinas útiles como inhibidores de las proteínas cinasas |
| EP2137183B1 (en) | 2007-03-09 | 2011-09-28 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| MX2009010037A (es) | 2007-03-20 | 2009-11-05 | Vertex Pharma | Aminopirimidinas utiles como inhibidores de cinasas. |
| DE102007015169A1 (de) | 2007-03-27 | 2008-10-02 | Universität des Saarlandes Campus Saarbrücken | 17Beta-Hydroxysteroid-Dehydrogenase-Typ1-Inhibitoren zur Behandlung hormonabhängiger Erkrankungen |
| GB0706044D0 (en) | 2007-03-28 | 2007-05-09 | Syngenta Ltd | C0-Crystals |
| CA2683785A1 (en) | 2007-04-13 | 2008-10-23 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| US7910587B2 (en) | 2007-04-26 | 2011-03-22 | Enanta Pharmaceuticals, Inc. | Quinoxalinyl dipeptide hepatitis C virus inhibitors |
| NZ580884A (en) | 2007-05-02 | 2012-02-24 | Vertex Pharma | Thiazoles and pyrazoles useful as kinase inhibitors |
| EP2152696B1 (en) | 2007-05-02 | 2014-09-24 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| AU2008247595A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| US20100234386A1 (en) | 2007-05-10 | 2010-09-16 | Chaudhari Amita | Quinoxaline derivatives as pi3 kinase inhibitors |
| WO2008144253A1 (en) | 2007-05-14 | 2008-11-27 | Irm Llc | Protein kinase inhibitors and methods for using thereof |
| CN101687852A (zh) | 2007-05-24 | 2010-03-31 | 沃泰克斯药物股份有限公司 | 可用作激酶抑制剂的噻唑类和吡唑类化合物 |
| KR20100017372A (ko) | 2007-05-25 | 2010-02-16 | 애보트 게엠베하 운트 콤파니 카게 | 향대사성 글루타메이트 수용체 2(mglu2 수용체)의 포지티브 조절자로서의 헤테로사이클릭 화합물 |
| WO2009004621A1 (en) | 2007-07-02 | 2009-01-08 | Technion Research & Development Foundation Ltd. | Compositions, articles and methods comprising tspo ligands for preventing or reducing tobacco-associated damage |
| US20100130597A1 (en) | 2007-07-06 | 2010-05-27 | The United State Of America, As Represented By The Secretary Of The Dept Of Health And Human Service | Dna-pkcs modulates energy regulation and brain function |
| UY31232A1 (es) | 2007-07-19 | 2009-03-02 | Compuestos derivados de dibenzotifenilamino-cromen-4-onas activas sustituidas y sus isomeros y aplicaciones | |
| UA100242C2 (uk) | 2007-08-01 | 2012-12-10 | Куміаі Кемікал Індастрі Ко., Лтд. | Похідна оксопіразину, проміжні сполуки, гербіцид на основі похідної оксопіразину та спосіб боротьби з небажаною рослинністю |
| EP2190466A4 (en) | 2007-08-10 | 2011-12-21 | Burnham Inst Medical Research | Tissue-specific alkaline phosphatase (TNAP) activators and their use |
| DE102007044032A1 (de) | 2007-09-14 | 2009-03-19 | Bayer Healthcare Ag | Substituierte heterocyclische Verbindungen und ihre Verwendung |
| HRP20110470T1 (hr) | 2007-10-12 | 2011-07-31 | Ingenium Pharmaceuticals Gmbh | Inhibitori proteinskih kinaza |
| CN101902912A (zh) | 2007-11-06 | 2010-12-01 | 纳幕尔杜邦公司 | 杀真菌杂环胺 |
| WO2009091388A2 (en) | 2007-12-21 | 2009-07-23 | Progenics Pharmaceuticals, Inc. | Triazines and related compounds having antiviral activity, compositions and methods thereof |
| US8562945B2 (en) | 2008-01-09 | 2013-10-22 | Molecular Insight Pharmaceuticals, Inc. | Technetium- and rhenium-bis(heteroaryl) complexes and methods of use thereof |
| US8598202B2 (en) | 2008-02-19 | 2013-12-03 | Janssen Pharmaceutica Nv | Aryl-hydroxyethylamino-pyrimidines and triazines as modulators of fatty acid amide hydrolase |
| WO2009107391A1 (ja) | 2008-02-27 | 2009-09-03 | 武田薬品工業株式会社 | 6員芳香環含有化合物 |
| CN101952258B (zh) | 2008-03-05 | 2014-03-19 | 默克专利有限公司 | 作为胰岛素分泌刺激剂的喹喔啉酮衍生物、获得它们的方法及其在治疗糖尿病中的用途 |
| US8268834B2 (en) | 2008-03-19 | 2012-09-18 | Novartis Ag | Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme |
| AU2009255183A1 (en) | 2008-06-02 | 2009-12-10 | Msd K.K. | Novel isoxazole derivative |
| ES2436195T3 (es) | 2008-06-16 | 2013-12-27 | Merck Patent Gmbh | Derivados de la quinoxalinadiona |
| EP2138488A1 (en) | 2008-06-26 | 2009-12-30 | sanofi-aventis | 4-(pyridin-4-yl)-1H-[1,3,5]triazin-2-one derivatives as GSK3-beta inhibitors for the treatment of neurodegenerative diseases |
| MX2011000839A (es) | 2008-07-23 | 2011-04-05 | Vertex Pharma | Inhibidores de pirazolpiridina cinasa. |
| WO2010048149A2 (en) | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| AR074199A1 (es) | 2008-11-20 | 2010-12-29 | Glaxosmithkline Llc | Compuesto de 6-(4-pirimidinil)-1h-indazol, composiciones farmaceuticas que lo comprenden y su uso para preparar un medicamento util para el tratamiento o disminucion de la gravedad del cancer. |
| EP2376485B1 (en) | 2008-12-19 | 2017-12-06 | Vertex Pharmaceuticals Incorporated | Pyrazine derivatives useful as inhibitors of atr kinase |
| EP2396004A4 (en) | 2009-02-11 | 2012-07-25 | Reaction Biology Corp | SELECTIVE KINASE HEMMER |
| JP2010111702A (ja) | 2009-02-16 | 2010-05-20 | Tetsuya Nishio | 複素環化合物、その製造法および用途 |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| US8906914B2 (en) | 2009-08-18 | 2014-12-09 | Janssen Pharmaceutica Nv | Ethylene diamine modulators of fatty acid hydrolase |
| AR077999A1 (es) | 2009-09-02 | 2011-10-05 | Vifor Int Ag | Antagonistas de pirimidin y triazin-hepcidina |
| JP5904944B2 (ja) | 2009-10-22 | 2016-04-20 | フィブロテック セラピューティクス プロプライエタリー リミテッド | 縮合環類似体の抗線維症剤 |
| ES2360333B1 (es) | 2009-10-29 | 2012-05-04 | Consejo Superior De Investigaciones Cientificas (Csic) (70%) | Derivados de bis (aralquil) amino y sistemas (hetero) aromaticos de seis miembros y su uso en el tratamiento de patologias neurodegenerativas, incluida la enfermedad de alzheimer |
| WO2011052756A1 (ja) | 2009-10-30 | 2011-05-05 | 持田製薬株式会社 | 新規3-ヒドロキシ-5-アリールイソキサゾール誘導体 |
| WO2011078371A1 (ja) | 2009-12-25 | 2011-06-30 | 持田製薬株式会社 | 新規3-ヒドロキシ-5-アリールイソチアゾール誘導体 |
| UY33213A (es) | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| CN102803227B (zh) | 2010-03-16 | 2016-01-20 | 默克专利有限公司 | 吗啉基喹唑啉 |
| TWI516264B (zh) | 2010-05-06 | 2016-01-11 | 臺北醫學大學 | 芳香醯喹啉化合物 |
| JP2011246389A (ja) | 2010-05-26 | 2011-12-08 | Oncotherapy Science Ltd | Ttk阻害作用を有する縮環ピラゾール誘導体 |
| SA111320519B1 (ar) * | 2010-06-11 | 2014-07-02 | Astrazeneca Ab | مركبات بيريميدينيل للاستخدام كمثبطات atr |
| DE102010025786A1 (de) | 2010-07-01 | 2012-01-05 | Merck Patent Gmbh | Pyrazolochinoline |
| DE102010035744A1 (de) | 2010-08-28 | 2012-03-01 | Merck Patent Gmbh | Imidazolonylchinoline |
| EP2640359A4 (en) * | 2010-11-18 | 2015-11-04 | Gen Hospital Corp | NOVEL COMPOSITIONS AND USES OF HYPOTENSE AGENTS IN THE TREATMENT OF CANCER |
| US9464065B2 (en) | 2011-03-24 | 2016-10-11 | The Scripps Research Institute | Compounds and methods for inducing chondrogenesis |
| MX2013011450A (es) | 2011-04-05 | 2014-02-03 | Vertex Pharma | Compuestos de aminopirazina utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr). |
| GB201114051D0 (en) | 2011-08-15 | 2011-09-28 | Domainex Ltd | Compounds and their uses |
| AU2012300317B2 (en) | 2011-08-26 | 2016-12-01 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| US9518029B2 (en) | 2011-09-14 | 2016-12-13 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| EP2757885B1 (en) | 2011-09-21 | 2017-03-15 | Neupharma, Inc. | Certain chemical entites, compositions, and methods |
| WO2013049701A1 (en) | 2011-09-30 | 2013-04-04 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| DE102011118830A1 (de) | 2011-11-18 | 2013-05-23 | Merck Patent Gmbh | Morpholinylbenzotriazine |
| GB201120993D0 (en) | 2011-12-06 | 2012-01-18 | Imp Innovations Ltd | Novel compounds and their use in therapy |
| WO2013112950A2 (en) | 2012-01-25 | 2013-08-01 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| IN2014KN02601A (enExample) | 2012-04-24 | 2015-05-08 | Vertex Pharma | |
| WO2014075077A1 (en) | 2012-11-12 | 2014-05-15 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| ES2900061T3 (es) | 2013-03-12 | 2022-03-15 | Vertex Pharma | Inhibidores de DNA-PK |
| RS57306B1 (sr) * | 2013-10-17 | 2018-08-31 | Vertex Pharma | Inhibitori dnk-pk |
| SG11201602962PA (en) * | 2013-10-17 | 2016-05-30 | Vertex Pharma | Co-crystals of (s)-n-methyl-8-(1-((2'-methyl-[4,5'-bipyrimidin]-6-yl)amino)propan-2-yl)quinoline-4-carboxamide and deuterated derivatives thereof as dna-pk inhibitors |
| JP2017514806A (ja) * | 2014-04-16 | 2017-06-08 | シグナル ファーマシューティカルズ,エルエルシー | Torキナーゼ阻害剤組み合わせ療法を使用して癌を治療する方法 |
| US10517875B2 (en) * | 2014-07-23 | 2019-12-31 | Mayo Foundation for Medical Engineering and Research | Targeting DNA-PKcs and B7-H1 to treat cancer |
| US20160045596A1 (en) * | 2014-08-05 | 2016-02-18 | Merrimack Pharmaceuticals, Inc. | Combination therapies for treating her2-positive cancers that are resistant to her2-targeted therapies |
| WO2017059357A1 (en) * | 2015-09-30 | 2017-04-06 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of dna damaging agents and atr inhibitors |
| RU2758669C2 (ru) | 2016-09-27 | 2021-11-01 | Вертекс Фармасьютикалз Инкорпорейтед | Способ лечения рака с применением сочетания днк-поражающих агентов и ингибиторов днк-пк |
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2017
- 2017-09-27 RU RU2019112863A patent/RU2758669C2/ru active
- 2017-09-27 KR KR1020197012307A patent/KR20190062485A/ko not_active Ceased
- 2017-09-27 MX MX2019003317A patent/MX394860B/es unknown
- 2017-09-27 WO PCT/US2017/053589 patent/WO2018064092A1/en not_active Ceased
- 2017-09-27 EP EP17857298.8A patent/EP3518931A4/en active Pending
- 2017-09-27 CA CA3038657A patent/CA3038657A1/en active Pending
- 2017-09-27 AU AU2017335648A patent/AU2017335648B2/en active Active
- 2017-09-27 US US16/336,195 patent/US11110108B2/en active Active
- 2017-09-27 JP JP2019516455A patent/JP2019529475A/ja active Pending
- 2017-09-27 TW TW106133237A patent/TW201815418A/zh unknown
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2019
- 2019-03-20 IL IL265523A patent/IL265523B/en unknown
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2021
- 2021-07-29 US US17/444,033 patent/US11980633B2/en active Active
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2022
- 2022-07-25 JP JP2022117973A patent/JP2022136163A/ja active Pending
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