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 (OSRAM) | 2020-10-22 |
Family
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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 (OSRAM) |
| EP (1) | EP3518931A4 (OSRAM) |
| JP (2) | JP2019529475A (OSRAM) |
| KR (1) | KR20190062485A (OSRAM) |
| AU (1) | AU2017335648B2 (OSRAM) |
| CA (1) | CA3038657A1 (OSRAM) |
| IL (1) | IL265523B (OSRAM) |
| MX (1) | MX394860B (OSRAM) |
| RU (1) | RU2758669C2 (OSRAM) |
| TW (1) | TW201815418A (OSRAM) |
| WO (1) | WO2018064092A1 (OSRAM) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018064092A1 (en) | 2016-09-27 | 2018-04-05 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of dna-damaging agents and dna-pk inhibitors |
| 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 |
| JP2025531951A (ja) * | 2022-07-20 | 2025-09-26 | カンバイダ (スーチュアン) バイオテクノロジー シーオー., エルティーディー. | 腫瘍の処置におけるドキソルビシンと組み合わせたイミダゾリノン誘導体の使用 |
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 |
| WO1991009594A1 (en) | 1989-12-28 | 1991-07-11 | Virginia Commonwealth University | Sigma receptor ligands and the use thereof |
| DK0498722T3 (da) | 1991-02-07 | 1998-03-09 | Roussel Uclaf | Nye bicycliske nitrogenforbindelser substitueret med en benzylgruppe, fremgangsmåde til deres fremstilling, de opnåede nye intermediærer, deres anvendelse som lægemidler og de pharmaceutiske præparater som de indgår i |
| 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 |
| DK0968206T3 (da) | 1997-02-19 | 2007-03-26 | Berlex Inc | N-heterocykliske derivater som NOS-inhibitorer |
| JPH10251255A (ja) | 1997-03-14 | 1998-09-22 | Nissan Chem Ind Ltd | アジン誘導体 |
| IL133009A0 (en) | 1997-05-28 | 2001-03-19 | Aventis Pharm Prod 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 |
| WO2000042026A1 (en) | 1999-01-15 | 2000-07-20 | Novo Nordisk A/S | Non-peptide glp-1 agonists |
| ES2306671T3 (es) | 1999-10-07 | 2008-11-16 | Amgen Inc. | Inhibidores de triazina quinasa. |
| 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 |
| CA2401778C (en) | 2000-02-29 | 2010-12-21 | 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 |
| WO2002020500A2 (en) * | 2000-09-01 | 2002-03-14 | Icos Corporation | Materials and methods to potentiate cancer treatment |
| US6610677B2 (en) | 2000-09-15 | 2003-08-26 | 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 |
| AU2001296871A1 (en) | 2000-09-15 | 2002-03-26 | 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 |
| US6613776B2 (en) | 2000-09-15 | 2003-09-02 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| ES2307667T3 (es) | 2000-12-05 | 2008-12-01 | Vertex Pharmaceuticals Incorporated | Inhibidires de quinasas terminales c-jun(jnk) y otras proteinas quinasas. |
| HUP0400639A3 (en) | 2000-12-21 | 2010-03-29 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them |
| US20040097502A1 (en) | 2001-02-02 | 2004-05-20 | Gellibert Francoise Jeanne | Pyrazoles as tgf inhibitors |
| MY130778A (en) | 2001-02-09 | 2007-07-31 | Vertex Pharma | Heterocyclic inhibitiors of erk2 and uses thereof |
| CA2441733A1 (en) | 2001-03-29 | 2002-10-10 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| JP2004535381A (ja) | 2001-04-13 | 2004-11-25 | 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 | c−JunN末端キナーゼ(JNK)および他のプロテインキナーゼのインヒビター |
| US20030096813A1 (en) | 2001-04-20 | 2003-05-22 | Jingrong Cao | Compositions useful 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. |
| JP4523271B2 (ja) | 2001-06-01 | 2010-08-11 | 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 | プロテインキナーゼのインヒビターとして有用なチアゾール化合物 |
| EP1399440B1 (en) | 2001-06-15 | 2009-06-03 | Vertex Pharmaceuticals Incorporated | 5-(2-aminopyrimidin-4-yl)benzisoxazoles as protein kinase inhibitors |
| DE60214198T2 (de) | 2001-07-03 | 2007-08-09 | Vertex Pharmaceuticals Inc., Cambridge | Isoxazolyl-pyrimidines als inhibitoren von src- und lck-protein-kinasen |
| MXPA04005510A (es) | 2001-12-07 | 2006-02-24 | Vertex Pharma | Compuestos basados en pirimidina utiles como inhibidores de gsk-3. |
| JP4656838B2 (ja) | 2002-02-06 | 2011-03-23 | 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 | Gsk−3の阻害剤として有用なヘテロアリール化合物 |
| 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 |
| WO2003091246A1 (en) | 2002-04-26 | 2003-11-06 | Vertex Pharmaceuticals Incorporated | Pyrrole derivatives as inhibitors of erk2 and uses thereof |
| CA2485429A1 (en) | 2002-05-06 | 2004-07-15 | Vertex Pharmaceuticals Incorporated | Thiadiazoles or oxadiazoles and their use as inhibitors of jak protein kinase |
| KR20050013562A (ko) | 2002-05-30 | 2005-02-04 | 버텍스 파마슈티칼스 인코포레이티드 | Jak 및 cdk2 프로테인 키나아제의 억제제 |
| MY141867A (en) | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| CA2491895C (en) | 2002-07-09 | 2011-01-18 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| RU2005106871A (ru) | 2002-08-14 | 2005-10-10 | Вертекс Фармасьютикалз Инкорпорейтед (Us) | Ингибиторы протеинкиназ и их применение |
| US7419984B2 (en) | 2002-10-17 | 2008-09-02 | Cell Therapeutics, Inc. | Pyrimidines and uses thereof |
| EP2172460A1 (en) | 2002-11-01 | 2010-04-07 | 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 |
| US7226919B2 (en) | 2002-12-18 | 2007-06-05 | Vertex Pharmaceuticals Inc. | Compositions useful as inhibitors of protein kinases |
| US7144911B2 (en) | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| JP5355842B2 (ja) * | 2002-12-31 | 2013-11-27 | ザイダス ビーエスヴィ ファーマ プライベート リミテッド | 非ペギレート化長循環性リポソーム |
| US7452555B2 (en) | 2003-01-21 | 2008-11-18 | S.S.C.I., Inc. | Cocrystallization |
| US7407962B2 (en) | 2003-02-07 | 2008-08-05 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds useful as inhibitors or protein kinases |
| US7456190B2 (en) | 2003-03-13 | 2008-11-25 | Vertex Pharmaceuticals Incorporated | Compositions useful as protein kinase inhibitors |
| US8404681B2 (en) | 2003-03-24 | 2013-03-26 | Luitpold Pharmaceuticals, Inc. | Xanthones, thioxanthones and acridinones as DNA-PK inhibitors |
| WO2004087698A2 (en) | 2003-03-25 | 2004-10-14 | Vertex Pharmaceuticals Incorporated | 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 |
| EP1678147B1 (en) | 2003-09-15 | 2012-08-08 | Lead Discovery Center GmbH | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
| CA2547080A1 (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 |
| AU2005222622B2 (en) | 2004-03-15 | 2011-04-07 | Dainippon Sumitomo Pharma Co., Ltd. | SNS-595 and methods of using the same |
| GB0405985D0 (en) | 2004-03-17 | 2004-04-21 | Novartis Forschungsstiftung | Kinase |
| MXPA06013208A (es) | 2004-05-14 | 2007-01-16 | Vertex Pharma | Profarmacos de pirrolipirimidina como inhibidotes de la proteina cinasa erk. |
| 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 |
| UA92150C2 (ru) | 2004-06-04 | 2010-10-11 | Арена Фармасьютикалз, Инк. | Замещенные производные арила и гетероарила как модуляторы метаболизма и для профилактики и лечения связанных с ним расстройств |
| ATE493401T1 (de) | 2004-09-17 | 2011-01-15 | Vertex Pharma | Als proteinkinaseinhibitoren geeignete diaminotriazolverbindungen |
| EP2402323A3 (en) | 2004-10-13 | 2012-05-30 | PTC Therapeutics, Inc. | Pyrazole or triazole compounds and their use for the manufacture of a medicament for treating somatic mutation-related diseases |
| JP2008516939A (ja) | 2004-10-15 | 2008-05-22 | アストラゼネカ アクチボラグ | 化学化合物 |
| HN2005000795A (es) | 2004-10-15 | 2010-08-19 | Aventis Pharma Inc | Pirimidinas como antagonistas del receptor de prostaglandina d2 |
| PL1827500T3 (pl) * | 2004-10-26 | 2009-09-30 | Pharma Mar Sa | Pegylowana liposomalna doksorubicyna w kombinacji z ekteinascydyną 743 |
| US20060166936A1 (en) | 2004-10-29 | 2006-07-27 | Hayley Binch | 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 |
| AU2005316599A1 (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 |
| EP1901747A2 (en) | 2005-05-25 | 2008-03-26 | 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 |
| AU2006272609A1 (en) | 2005-07-26 | 2007-02-01 | Vertex Pharmaceuticals Incorporated | Abl kinase inhibition |
| GB0520657D0 (en) | 2005-10-11 | 2005-11-16 | Ludwig Inst Cancer Res | Pharmaceutical compounds |
| US20070219192A1 (en) | 2005-11-02 | 2007-09-20 | Xiangping Qian | Certain chemical entities, compositions, and methods |
| CN101316597B (zh) | 2005-11-03 | 2013-04-17 | 顶点医药品公司 | 用作激酶抑制剂的氨基嘧啶 |
| DE602006021776D1 (de) | 2005-11-16 | 2011-06-16 | Vertex Pharma | Als kinaseinhibitoren geeignete aminopyrimidine |
| 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 |
| AR061974A1 (es) | 2006-07-14 | 2008-08-10 | Novartis Ag | Derivados de pirimidina como inhibidores de alk, composiciones farmaceuticas y procesos de obtencion |
| 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 |
| CN103739595A (zh) | 2006-10-02 | 2014-04-23 | Irm责任有限公司 | 作为蛋白激酶抑制剂的化合物和组合物 |
| 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 |
| AU2007333650A1 (en) | 2006-12-19 | 2008-06-26 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as inhibitors of protein kinases |
| KR20090102838A (ko) | 2006-12-28 | 2009-09-30 | 암브룩스, 인코포레이티드 | 페나진 및 퀴녹살린 치환된 아미노산 및 폴리펩티드 |
| AU2008210266B2 (en) | 2007-01-31 | 2013-09-05 | Ym Biosciences Australia Pty Ltd | Thiopyrimidine-based compounds and uses thereof |
| WO2008106202A1 (en) | 2007-02-27 | 2008-09-04 | Housey Gerard M | Theramutein modulators |
| JP2010520887A (ja) | 2007-03-09 | 2010-06-17 | 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ジン |
| JP5393489B2 (ja) | 2007-03-09 | 2014-01-22 | 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 |
| MX2009009590A (es) | 2007-03-09 | 2009-11-10 | Vertex Pharma | Aminopirimidinas utiles como inhibidores de proteinas cinasas. |
| 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 |
| JP5389785B2 (ja) | 2007-05-02 | 2014-01-15 | 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 | キナーゼ阻害剤として有用なチアゾールおよびピラゾール |
| MX2009011811A (es) | 2007-05-02 | 2010-01-14 | Vertex Pharma | Aminopirimidinas utiles como inhibidores de cinasa. |
| CA2694381A1 (en) | 2007-05-02 | 2008-11-13 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| JP2010526823A (ja) | 2007-05-10 | 2010-08-05 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Pi3キナーゼ阻害物質としてのキノキサリン誘導体 |
| 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 |
| WO2008145616A1 (en) | 2007-05-25 | 2008-12-04 | Abbott Gmbh & Co. Kg | Heterocyclic compounds as positive modulators of metabotropic glutamate receptor 2 (mglu2 receptor) |
| 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 |
| EP2170338A2 (en) | 2007-07-06 | 2010-04-07 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | 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 | |
| EP2174934B1 (en) | 2007-08-01 | 2012-06-06 | Kumiai Chemical Industry Co., Ltd. | Oxopyrazine derivative and herbicide |
| 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 |
| NZ584454A (en) | 2007-10-12 | 2011-09-30 | Ingenium Pharmaceuticals Gmbh | N-[6-phenyl-pyrimidin-4-yl]-amides and urea derivatives as inhibitors of protein kinases |
| CN101902912A (zh) | 2007-11-06 | 2010-12-01 | 纳幕尔杜邦公司 | 杀真菌杂环胺 |
| US20120009151A1 (en) | 2007-12-21 | 2012-01-12 | Progenics Pharmaceuticals, Inc. | Triazines And Related Compounds Having Antiviral Activity, Compositions And Methods Thereof |
| CA2714743C (en) | 2008-02-19 | 2017-01-17 | Janssen Pharmaceutica N.V. | Aryl-hydroxyethylamino-pyrimidines and triazines as modulators of fatty acid amide hydrolase |
| US20110009421A1 (en) | 2008-02-27 | 2011-01-13 | Takeda Pharmaceutical Company Limited | Compound having 6-membered aromatic ring |
| 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 |
| CA2725316A1 (en) | 2008-06-02 | 2009-12-10 | Banyu Pharmaceutical Co., Ltd. | Novel isoxazole derivative |
| MX2010013577A (es) | 2008-06-16 | 2010-12-21 | Merck Patent Gmbh | Derivados de quinoxalindiona. |
| 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 |
| WO2010011756A1 (en) | 2008-07-23 | 2010-01-28 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridine kinase inhibitors |
| WO2010048149A2 (en) | 2008-10-20 | 2010-04-29 | Kalypsys, Inc. | Heterocyclic modulators of gpr119 for treatment of disease |
| EP2362775B1 (en) | 2008-11-20 | 2015-08-05 | GlaxoSmithKline LLC | Chemical compounds |
| WO2010065899A2 (en) | 2008-12-05 | 2010-06-10 | Molecular Insight Pharmaceuticals, Inc. | Technetium-and rhenium-bis(heteroaryl)complexes and methods of use thereof |
| AU2009327357C1 (en) | 2008-12-19 | 2017-02-02 | Vertex Pharmaceuticals Incorporated | Pyrazine derivatives useful as inhibitors of ATR kinase |
| 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 |
| WO2011022348A1 (en) | 2009-08-18 | 2011-02-24 | Janssen Pharmaceutica Nv | Ethylene diamine modulators of fatty acid amide hydrolase |
| AR077999A1 (es) | 2009-09-02 | 2011-10-05 | Vifor Int Ag | Antagonistas de pirimidin y triazin-hepcidina |
| IN2012DN03312A (OSRAM) | 2009-10-22 | 2015-10-23 | Fibrotech Therapeutics Pty Ltd | |
| 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 |
| EP2495238A4 (en) | 2009-10-30 | 2013-04-24 | Mochida Pharm Co Ltd | NEW 3-HYDROXY-5-ARYLISOXAZOLE DERIVATIVE |
| MX2012007474A (es) | 2009-12-25 | 2012-08-01 | Mochida Pharm Co Ltd | Derivados de 3-hidroxi-5-arilisotiazol novedosos. |
| UY33213A (es) | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| EA201201289A1 (ru) | 2010-03-16 | 2013-08-30 | Мерк Патент Гмбх | Морфолинилхиназолины |
| 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 |
| CA2817250A1 (en) | 2010-11-18 | 2012-05-24 | The General Hospital Corporation | Novel compositions and uses of anti-hypertension agents for cancer therapy |
| 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 |
| ES2725790T3 (es) | 2011-08-26 | 2019-09-27 | Neupharma Inc | Algunas entidades químicas, composiciones, y métodos |
| WO2013040515A1 (en) | 2011-09-14 | 2013-03-21 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| WO2013043935A1 (en) | 2011-09-21 | 2013-03-28 | Neupharma, Inc. | Certain chemical entites, compositions, and methods |
| US9249111B2 (en) | 2011-09-30 | 2016-02-02 | Neupharma, Inc. | Substituted quinoxalines as B-RAF kinase inhibitors |
| 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 |
| EP2841428B1 (en) | 2012-04-24 | 2018-08-22 | Vertex Pharmaceuticals Incorporated | Dna-pk inhibitors |
| EP2916838B1 (en) | 2012-11-12 | 2019-03-13 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| WO2014159690A1 (en) | 2013-03-12 | 2014-10-02 | Vertex Pharmaceuticals Incorporated | Dna-pk inhibitors |
| RS57306B1 (sr) | 2013-10-17 | 2018-08-31 | Vertex Pharma | Inhibitori dnk-pk |
| PL3424920T3 (pl) | 2013-10-17 | 2020-11-16 | Vertex Pharmaceuticals Incorporated | Kokryształy (S)-N-metylo-8-(1-((2'-metylo-4’,6'-dideutero-[4,5'-bipirymidyn]-6-ylo)amino)propan-2-ylo)chinolino-4-karboksyamidu i ich deuterowane pochodne jako inhibitory DNA-PK |
| US9737535B2 (en) * | 2014-04-16 | 2017-08-22 | Signal Pharmaceuticals, Llc | Methods for treating cancer using TOR kinase inhibitor combination therapy comprising administering substituted pyrazino[2,3-b]pyrazines |
| US10517875B2 (en) | 2014-07-23 | 2019-12-31 | Mayo Foundation for Medical Engineering and Research | Targeting DNA-PKcs and B7-H1 to treat cancer |
| WO2016022723A1 (en) * | 2014-08-05 | 2016-02-11 | Merrimack Pharmaceuticals, Inc. | Combination therapies for treating her2-positive cancers that are resistant to her2-targeted therapies |
| AU2016331955B2 (en) * | 2015-09-30 | 2022-07-21 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors |
| WO2018064092A1 (en) | 2016-09-27 | 2018-04-05 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of dna-damaging agents and dna-pk inhibitors |
-
2017
- 2017-09-27 WO PCT/US2017/053589 patent/WO2018064092A1/en not_active Ceased
- 2017-09-27 AU AU2017335648A patent/AU2017335648B2/en active Active
- 2017-09-27 RU RU2019112863A patent/RU2758669C2/ru active
- 2017-09-27 KR KR1020197012307A patent/KR20190062485A/ko not_active Ceased
- 2017-09-27 TW TW106133237A patent/TW201815418A/zh unknown
- 2017-09-27 MX MX2019003317A patent/MX394860B/es unknown
- 2017-09-27 JP JP2019516455A patent/JP2019529475A/ja active Pending
- 2017-09-27 CA CA3038657A patent/CA3038657A1/en active Pending
- 2017-09-27 EP EP17857298.8A patent/EP3518931A4/en active Pending
- 2017-09-27 US US16/336,195 patent/US11110108B2/en active Active
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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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