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 |
|---|---|---|---|---|
| MX394860B (es) | 2016-09-27 | 2025-03-24 | Vertex Pharma | Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk). |
| 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 |
| US20240000977A1 (en) * | 2020-10-19 | 2024-01-04 | Baruch S. Blumberg Institute | Methods and kits for diagnosing and treating cancers |
| CN120129526A (zh) * | 2022-07-20 | 2025-06-10 | 成都百裕制药股份有限公司 | 咪唑啉酮衍生物联合多柔比星在治疗肿瘤中的应用 |
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 |
| CA2071897A1 (en) | 1989-12-28 | 1991-06-29 | Richard A. Glennon | Sigma receptor ligands and the use thereof |
| US6004979A (en) | 1991-02-07 | 1999-12-21 | Hoechst Marion Roussel | Nitrogenous bicycles |
| JP3531944B2 (ja) | 1991-02-07 | 2004-05-31 | アベンティス・ファーマ・ソシエテ・アノニム | 新規のベンジル基で置換された窒素系二環式誘導体及びその製造方法 |
| 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 |
| WO1993022291A1 (en) | 1992-04-24 | 1993-11-11 | 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 |
| CN1100777C (zh) | 1997-02-19 | 2003-02-05 | 伯莱克斯实验室公司 | 作为nos抑制剂的n－杂环衍生物 |
| JPH10251255A (ja) | 1997-03-14 | 1998-09-22 | Nissan Chem Ind Ltd | アジン誘導体 |
| EP1001945B1 (en) | 1997-05-28 | 2011-03-02 | Aventis Pharmaceuticals Inc. | QUINOLINE AND QUINOXALINE COMPOUNDS WHICH INHIBIT PLATELET-DERIVED GROWTH FACTOR AND/OR p56lck TYROSINE KINASES |
| 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 |
| 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 |
| MXPA02003436A (es) | 1999-10-07 | 2002-08-20 | Amgen Inc | Inhibidores de triazina cinasa. |
| 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 |
| EP1255741A2 (en) | 2000-02-01 | 2002-11-13 | Cor Therapeutics, Inc. | 2- 1H]-QUINOLONE AND 2- 1H]-QUINOXALONE INHIBITORS OF FACTOR Xa |
| WO2001064642A2 (en) | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| US6605615B2 (en) | 2000-03-01 | 2003-08-12 | 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 |
| AU2001288432A1 (en) | 2000-09-01 | 2002-03-22 | Icos Corporation | Materials and methods to potentiate cancer treatment |
| US6660731B2 (en) | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| CA2422367C (en) | 2000-09-15 | 2010-05-18 | 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 |
| US6613776B2 (en) | 2000-09-15 | 2003-09-02 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| WO2002046184A1 (en) | 2000-12-05 | 2002-06-13 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| KR100947185B1 (ko) | 2000-12-21 | 2010-03-15 | 버텍스 파마슈티칼스 인코포레이티드 | 단백질 키나제 억제제로서 유용한 피라졸 화합물 및 이를 포함하는 조성물 |
| JP2004521901A (ja) | 2001-02-02 | 2004-07-22 | グラクソ グループ リミテッド | Ｔｇｆ阻害剤としてのピラゾール |
| MY130778A (en) | 2001-02-09 | 2007-07-31 | Vertex Pharma | Heterocyclic inhibitiors of erk2 and uses thereof |
| US6949544B2 (en) | 2001-03-29 | 2005-09-27 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases |
| DE60214701T2 (de) | 2001-04-13 | 2007-09-13 | Vertex Pharmaceuticals Inc., Cambridge | Inhibitoren von c-jun-n-terminalen-kinasen (jnk) und anderen proteinkinasen |
| US20030096813A1 (en) | 2001-04-20 | 2003-05-22 | Jingrong Cao | Compositions useful as inhibitors of GSK-3 |
| EP1404669A2 (en) | 2001-05-16 | 2004-04-07 | 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. |
| EP1392684B1 (en) | 2001-06-01 | 2006-09-13 | Vertex Pharmaceuticals Incorporated | Thiazole compounds useful as inhibitors of protein kinases |
| CA2450769A1 (en) | 2001-06-15 | 2002-12-27 | Vertex Pharmaceuticals Incorporated | 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors |
| US6689778B2 (en) | 2001-07-03 | 2004-02-10 | Vertex Pharmaceuticals Incorporated | Inhibitors of Src and Lck protein kinases |
| 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 |
| AU2003237121A1 (en) | 2002-04-26 | 2003-11-10 | Vertex Pharmaceuticals Incorporated | Pyrrole derivatives as inhibitors of erk2 and uses thereof |
| JP4681302B2 (ja) | 2002-05-06 | 2011-05-11 | 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 | チアジアゾールまたはオキサジアゾール、およびこれらの、ｊａｋプロテインキナーゼのインヒビターとしての使用 |
| AU2003231880A1 (en) | 2002-05-30 | 2003-12-19 | Vertex Pharmaceuticals Incorporated | Inhibitors of jak and cdk2 protein kinases |
| MY141867A (en) | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| US7361665B2 (en) | 2002-07-09 | 2008-04-22 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases |
| KR20050042478A (ko) | 2002-08-14 | 2005-05-09 | 버텍스 파마슈티칼스 인코포레이티드 | 프로테인 키나아제 억제제 및 이의 용도 |
| US7419984B2 (en) | 2002-10-17 | 2008-09-02 | Cell Therapeutics, Inc. | Pyrimidines and uses thereof |
| US7312227B2 (en) | 2002-11-01 | 2007-12-25 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of JAK and other protein kinases |
| WO2004041814A1 (en) | 2002-11-04 | 2004-05-21 | Vertex Pharmaceuticals Incorporated | Heteroaryl-pyramidine derivatives as jak inhibitors |
| WO2004058749A1 (en) | 2002-12-18 | 2004-07-15 | Vertex Pharmaceuticals Incorporated | Benzisoxazole derivatives useful as inhibitors of protein kinases |
| US7144911B2 (en) | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| EA008930B1 (ru) * | 2002-12-31 | 2007-08-31 | Зайдус Би-Эс-Ви Рисерч Энд Дивелопмент Прайвит Лимитид | Непэгилированные, длительно циркулирующие липосомы |
| EP1596869B1 (en) | 2003-01-21 | 2014-06-04 | New Form Pharmaceuticals Inc. | Novel cocrystallization |
| JP2006518381A (ja) | 2003-02-07 | 2006-08-10 | 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インヒビターとして有用なヘテロアリール置換ピロール |
| WO2004083203A1 (en) | 2003-03-13 | 2004-09-30 | Vertex Pharmaceuticals Incorporated | Compositions useful as protein kinase inhibitors |
| JP2006523681A (ja) | 2003-03-24 | 2006-10-19 | ルイトポルド・ファーマシューティカルズ・インコーポレーテッド | Ｄｎａ−ｐｋ阻害剤としてのキサントン、チオキサントンおよびアクリジノン |
| 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 |
| WO2005026129A1 (en) | 2003-09-15 | 2005-03-24 | Gpc Biotech Ag | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
| AU2004313928A1 (en) | 2003-12-02 | 2005-07-28 | Vertex Pharmaceuticals, Inc. | Heterocyclic protein kinase inhibitors and uses thereof |
| CN1902193B (zh) | 2003-12-04 | 2011-07-13 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的喹喔啉 |
| 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 |
| DK1725233T3 (da) | 2004-03-15 | 2011-03-14 | Sunesis Pharmaceuticals Inc | Farmaceutisk sammensætning omfattende SNS-595 og anvendelse deraf |
| GB0405985D0 (en) | 2004-03-17 | 2004-04-21 | Novartis Forschungsstiftung | Kinase |
| ZA200610163B (en) | 2004-05-14 | 2008-02-27 | 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 |
| EP1756084B1 (en) | 2004-06-04 | 2008-11-26 | Arena Pharmaceuticals, Inc. | Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto |
| PT1791830E (pt) | 2004-09-17 | 2011-04-04 | Vertex Pharma | Compostos de diaminotriazole úteis como inibidores de proteína-quinase |
| CA2583976A1 (en) | 2004-10-13 | 2006-04-27 | Ptc Therapeutics, Inc. | Use of defined compounds for the manufacture of a medicament for preventing/treating diseases resulting from somatic mutations |
| WO2006040568A1 (en) | 2004-10-15 | 2006-04-20 | Astrazeneca Ab | Quinoxalines as b raf inhibitors |
| HN2005000795A (es) | 2004-10-15 | 2010-08-19 | Aventis Pharma Inc | Pirimidinas como antagonistas del receptor de prostaglandina d2 |
| ES2326825T3 (es) | 2004-10-26 | 2009-10-20 | Pharma Mar S.A., Sociedad Unipersonal | Doxorubicina liposomal pegilada en combinacion con ecteinascidina 743. |
| 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 |
| EP1850681B1 (en) | 2005-02-04 | 2019-12-18 | Firmenich Incorporated | Compounds comprising linked hetero aryl moieties and their use as novel umami flavor modifiers, tastants and taste enhancers for comestible compositions |
| BRPI0608934A2 (pt) | 2005-04-06 | 2010-02-17 | Irm Llc | compostos e composições contendo diarilamina, e seu uso como moduladores de receptores nucleares de hormÈnios esteróides |
| 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 |
| US20090221581A1 (en) | 2005-05-25 | 2009-09-03 | Philipp Wabnitz | Methods of treating pain |
| US20090035394A1 (en) * | 2005-05-26 | 2009-02-05 | Graeme Cameron Murray Smith | Use of dna-pk inhibition to sensitise atm deficient cancers to dna-damaging cancer therapies |
| 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 |
| US20090298844A1 (en) | 2005-07-26 | 2009-12-03 | John Pollard | Abl kinase inhibition |
| GB0520657D0 (en) | 2005-10-11 | 2005-11-16 | Ludwig Inst Cancer Res | Pharmaceutical compounds |
| JP2009514875A (ja) | 2005-11-02 | 2009-04-09 | サイトキネティクス・インコーポレーテッド | 化学物質、組成物、および方法 |
| CA2627808A1 (en) | 2005-11-03 | 2007-05-18 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| CN101360740A (zh) | 2005-11-16 | 2009-02-04 | 沃泰克斯药物股份有限公司 | 可用作激酶抑制剂的氨基嘧啶 |
| EP1983823A1 (en) | 2006-01-17 | 2008-10-29 | 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 |
| PE20071025A1 (es) | 2006-01-31 | 2007-10-17 | Mitsubishi Tanabe Pharma Corp | Compuesto 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 |
| JP2009542608A (ja) * | 2006-06-29 | 2009-12-03 | アステックス・セラピューティクス・リミテッド | 医薬組合せ剤 |
| 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 |
| PE20121506A1 (es) | 2006-07-14 | 2012-11-26 | Amgen Inc | Compuestos triazolopiridinas como inhibidores de c-met |
| BRPI0714409A2 (pt) | 2006-07-14 | 2013-03-12 | Novartis Ag | derivados de pirimidina como inibidores de alk-5 |
| US7635683B2 (en) | 2006-08-04 | 2009-12-22 | Enanta Pharmaceuticals, Inc. | Quinoxalinyl tripeptide hepatitis C virus inhibitors |
| US8541428B2 (en) | 2006-08-22 | 2013-09-24 | Technion Research And Development Foundation Ltd. | Heterocyclic derivatives, pharmaceutical compositions and methods of use thereof |
| 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 |
| NZ576750A (en) | 2006-11-02 | 2012-01-12 | Vertex Pharma | Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases |
| US20100234341A1 (en) | 2006-12-04 | 2010-09-16 | Marion Lanier | Substituted pyrimidines as adenosine receptor antagonists |
| CA2673353A1 (en) | 2006-12-19 | 2008-06-26 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| WO2008083346A1 (en) | 2006-12-28 | 2008-07-10 | Ambrx, Inc. | Phenazine and quinoxaline substituted amino acids and polypeptides |
| JP5539734B2 (ja) | 2007-01-31 | 2014-07-02 | ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド | チオピリミジンベースの化合物およびその使用 |
| WO2008106202A1 (en) | 2007-02-27 | 2008-09-04 | Housey Gerard M | Theramutein modulators |
| CA2679701A1 (en) | 2007-03-09 | 2008-09-18 | Vertex Pharmaceuticals Incorporated | Aminopyridines useful as inhibitors of protein kinases |
| JP5520057B2 (ja) | 2007-03-09 | 2014-06-11 | 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 | 蛋白キナーゼの阻害剤として有用なアミノピリミジン |
| NZ579485A (en) | 2007-03-09 | 2012-02-24 | Vertex Pharma | Aminopyrimidines useful as inhibitors of protein kinases |
| WO2008115973A2 (en) | 2007-03-20 | 2008-09-25 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| 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 |
| JP2010523700A (ja) | 2007-04-13 | 2010-07-15 | 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 | キナーゼインヒビターとして有用なアミノピリミジン |
| US7910587B2 (en) | 2007-04-26 | 2011-03-22 | Enanta Pharmaceuticals, Inc. | Quinoxalinyl dipeptide hepatitis C virus inhibitors |
| JP5572087B2 (ja) | 2007-05-02 | 2014-08-13 | 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 | キナーゼ阻害として有用なアミノピリミジン |
| AU2008247592A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Thiazoles and pyrazoles useful as kinase inhibitors |
| CN101801959A (zh) | 2007-05-02 | 2010-08-11 | 沃泰克斯药物股份有限公司 | 可用作激酶抑制剂的氨基嘧啶类化合物 |
| PE20090288A1 (es) | 2007-05-10 | 2009-04-03 | Smithkline Beecham Corp | Derivados de quinoxalina como inhibidores de la pi3 quinasa |
| WO2008144253A1 (en) | 2007-05-14 | 2008-11-27 | Irm Llc | Protein kinase inhibitors and methods for using thereof |
| JP2010528021A (ja) | 2007-05-24 | 2010-08-19 | 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 | キナーゼのインヒビターとして有用なチアゾールおよびピラゾール |
| MX2009012749A (es) | 2007-05-25 | 2010-03-10 | Abbott Gmbh & Co Kg | Compuestos heterociclicos como moduladores positivos del receptor de glutamato metabotropico 2 (receptor mglu2). |
| EP2170274A1 (en) | 2007-07-02 | 2010-04-07 | Technion Research and 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 | |
| BRPI0813863B1 (pt) | 2007-08-01 | 2016-09-27 | Ihara Chemical Ind Co | derivado de oxopirazina ou um sal agroquimicamente aceitável do mesmo, herbicida, e, método para usar um herbicida |
| US20090053192A1 (en) | 2007-08-10 | 2009-02-26 | Burnham Institute For Medical Research | Tissue-nonspecific alkaline phosphatase (tnap) activators and uses thereof |
| DE102007044032A1 (de) | 2007-09-14 | 2009-03-19 | Bayer Healthcare Ag | Substituierte heterocyclische Verbindungen und ihre Verwendung |
| ATE510827T1 (de) | 2007-10-12 | 2011-06-15 | Ingenium Pharmaceuticals Gmbh | Inhibitoren von proteinkinasen |
| KR20100088150A (ko) | 2007-11-06 | 2010-08-06 | 이 아이 듀폰 디 네모아 앤드 캄파니 | 살진균성 복소환식 아민 |
| 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 |
| CA2716898A1 (en) | 2008-02-27 | 2009-09-03 | Takeda Pharmaceutical Company Limited | Compound having 6-membered aromatic ring |
| HUE027811T2 (en) | 2008-03-05 | 2016-11-28 | Merck Patent Gmbh | Quinoxalinone derivatives as stimulators of insulin secretion, methods for their preparation and their use in the treatment of diabetes |
| US8268834B2 (en) | 2008-03-19 | 2012-09-18 | Novartis Ag | Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme |
| CA2725316A1 (en) | 2008-06-02 | 2009-12-10 | Banyu Pharmaceutical Co., Ltd. | Novel isoxazole derivative |
| KR101641391B1 (ko) | 2008-06-16 | 2016-07-20 | 메르크 파텐트 게엠베하 | 퀴녹살린디온 유도체 |
| 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 |
| US8697685B2 (en) | 2008-11-20 | 2014-04-15 | Glaxosmithkline Llc | Chemical compounds |
| PT3354650T (pt) | 2008-12-19 | 2022-06-20 | Vertex Pharma | Compostos úteis como inibidores da cinase atr |
| CA2752150A1 (en) | 2009-02-11 | 2010-08-19 | Reaction Biology Corp. | Selective kinase inhibitors |
| 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 |
| US9062076B2 (en) | 2009-10-22 | 2015-06-23 | Fibrotech Therapeutics Pty Ltd | Fused ring analogues of anti-fibrotic agents |
| 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 |
| AU2010312365A1 (en) | 2009-10-30 | 2012-06-07 | Mochida Pharmaceutical Co.,Ltd. | Novel 3-hydroxy-5-arylisoxazole derivative |
| AU2010336225A1 (en) | 2009-12-25 | 2012-08-16 | Mochida Pharmaceutical Co.,Ltd. | Novel 3-hydroxy-5-arylisothiazole derivative |
| UY33213A (es) | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| EP2547664B1 (de) | 2010-03-16 | 2016-05-04 | Merck Patent GmbH | Morpholinylchinazoline |
| 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 |
| CA2832100A1 (en) | 2011-04-05 | 2012-10-11 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of tra kinase |
| GB201114051D0 (en) | 2011-08-15 | 2011-09-28 | Domainex Ltd | Compounds and their uses |
| US9295671B2 (en) | 2011-08-26 | 2016-03-29 | Neupharma, Inc. | Benzenesulfonamide derivatives of quinoxaline, pharmaceutical compositions thereof, and their use in methods for treating cancer |
| 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 |
| US9670180B2 (en) | 2012-01-25 | 2017-06-06 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| SI3459942T1 (sl) | 2012-04-24 | 2021-05-31 | Vertex Pharmaceuticals Incorporated | Inhibitorji DNA-PK |
| EP2916838B1 (en) | 2012-11-12 | 2019-03-13 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| HRP20211855T1 (hr) | 2013-03-12 | 2022-03-04 | Vertex Pharmaceuticals Incorporated | Inhibitori dnk-pk |
| SI3424920T1 (sl) | 2013-10-17 | 2020-08-31 | Vertex Pharmaceuticals Incorporated | Kokristali (s)-n-metil-8-(1-((2'-metil-(4,5'-bipirimidin)-6-il)amino)propan-2-il) kinolin-4-karboksamida in devterirani derivati le-teh kot inhibitorji dna-pk |
| WO2015058031A1 (en) * | 2013-10-17 | 2015-04-23 | Vertex Pharmaceuticals Incorporated | Dna-pk inhibitors |
| EP3131552B1 (en) * | 2014-04-16 | 2020-07-15 | Signal Pharmaceuticals, LLC | Methods for treating cancer using tor kinase inhibitor combination therapy |
| WO2016014148A1 (en) * | 2014-07-23 | 2016-01-28 | Mayo Foundation For Medical Education 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 |
| HK1258570A1 (zh) | 2015-09-30 | 2019-11-15 | Vertex Pharmaceuticals Inc. | 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法 |
| MX394860B (es) | 2016-09-27 | 2025-03-24 | Vertex Pharma | Metodo para tratar cancer usando una combinacion de agentes que dañan adn e inhibidores de proteina cinasa dependiente de adn (adn-pk). |
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2017
- 2017-09-27 MX MX2019003317A patent/MX394860B/es unknown
- 2017-09-27 AU AU2017335648A patent/AU2017335648B2/en active Active
- 2017-09-27 CA CA3038657A patent/CA3038657A1/en active Pending
- 2017-09-27 JP JP2019516455A patent/JP2019529475A/ja active Pending
- 2017-09-27 KR KR1020197012307A patent/KR20190062485A/ko not_active Ceased
- 2017-09-27 RU RU2019112863A patent/RU2758669C2/ru active
- 2017-09-27 EP EP17857298.8A patent/EP3518931A4/en active Pending
- 2017-09-27 US US16/336,195 patent/US11110108B2/en active Active
- 2017-09-27 WO PCT/US2017/053589 patent/WO2018064092A1/en not_active Ceased
- 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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