ES2860299T3 - Inhibidores de DNA-PK - Google Patents

Inhibidores de DNA-PK Download PDF

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Publication number
ES2860299T3
ES2860299T3 ES18186230T ES18186230T ES2860299T3 ES 2860299 T3 ES2860299 T3 ES 2860299T3 ES 18186230 T ES18186230 T ES 18186230T ES 18186230 T ES18186230 T ES 18186230T ES 2860299 T3 ES2860299 T3 ES 2860299T3
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alkyl
group
ra1b
groups
hydrogen
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ES18186230T
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Spanish (es)
Inventor
Paul S Charifson
Kevin Michael Cottrell
Hongbo Deng
John P Duffy
Huai Gao
Simon Giroux
Jeremy Green
Katrina Lee Jackson
John Patrick Maxwell
Mark A Morris
Albert Charles Pierce
Nathan D Waal
Joseph M Kennedy
David J Lauffer
Mark Willem Ledeboer
Pan Li
Jinwang Xu
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • 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
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Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2694484T1 (sl) 2011-04-08 2018-10-30 Janssen Sciences Ireland Uc Derivati pirimidina za zdravljenje virusnih okužb
EA033830B1 (ru) 2011-11-09 2019-11-29 Janssen Sciences Ireland Uc Производные аденина в качестве активаторов толл-подобных рецепторов tlr7
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
UA115983C2 (uk) 2012-04-24 2018-01-25 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори днк-пк
AU2013288600B2 (en) 2012-07-13 2017-06-29 Janssen Sciences Ireland Uc Macrocyclic purines for the treatment of viral infections
NZ705589A (en) 2012-10-10 2019-05-31 Janssen Sciences Ireland Uc Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases
EA035431B1 (ru) 2012-11-16 2020-06-15 Янссен Сайенсиз Айрлэнд Юси Гетероциклические замещенные производные 2-амино-хиназолина в качестве модуляторов tlr7 и/или tlr8 для лечения вирусных инфекций
KR102300861B1 (ko) 2013-02-21 2021-09-10 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 바이러스 감염의 치료를 위한 2-아미노피리미딘 유도체
SG11201507203RA (en) 2013-03-12 2015-10-29 Vertex Pharma Dna-pk inhibitors
SG11201508078XA (en) 2013-03-29 2015-11-27 Janssen Sciences Ireland Uc Macrocyclic deaza-purinones for the treatment of viral infections
WO2014187932A1 (en) 2013-05-24 2014-11-27 Janssen R&D Ireland Pyridone derivatives for the treatment of viral infections and further diseases
ES2645950T3 (es) 2013-06-27 2017-12-11 Janssen Sciences Ireland Uc Derivados de pirrolo[3,2-d]pirimidina para el tratamiento de infecciones víricas y otras enfermedades
UA117253C2 (uk) 2013-07-30 2018-07-10 ЯНССЕН САЙЄНСЕЗ АЙРЛЕНД ЮСі ПОХІДНІ ТІЄНО[3,2-d]ПІРИМІДИНІВ ДЛЯ ЛІКУВАННЯ ВІРУСНИХ ІНФЕКЦІЙ
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
DK3057959T3 (en) * 2013-10-17 2018-06-06 Vertex Pharma INHIBITORS FOR DNA PK
US10287268B2 (en) * 2014-07-21 2019-05-14 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
CN104352488B (zh) * 2014-10-31 2016-08-31 厦门大学 一类取代杂环衍生物在制备治疗疼痛药物中的应用
WO2016066115A1 (zh) * 2014-10-31 2016-05-06 厦门大学 取代杂环衍生物、其制备方法和用途
CN104356082B (zh) * 2014-10-31 2016-07-13 厦门大学 一类取代杂环衍生物及其制备方法
AU2016334141B2 (en) * 2015-10-09 2019-12-19 ACEA Therapeutics, Inc. Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same
FI3365334T3 (fi) * 2015-10-21 2024-09-19 Otsuka Pharma Co Ltd Bentsolaktaamiyhdisteitä proteiinikinaasin estäjinä
CR20180323A (es) 2015-11-20 2018-08-06 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituídos como moduladores de los receptores de pge2
KR102488323B1 (ko) 2015-12-10 2023-01-12 피티씨 테라퓨틱스, 인크. 헌팅턴병 치료 또는 개선을 위한 조성물
CN109476675B (zh) 2016-07-01 2022-12-09 爱尔兰詹森科学公司 用于治疗病毒性感染的二氢吡喃并嘧啶衍生物
EP3481830B1 (en) 2016-07-05 2022-02-16 The Broad Institute, Inc. Bicyclic urea kinase inhibitors and uses thereof
AU2017295720B2 (en) * 2016-07-13 2021-07-22 Vertex Pharmaceuticals Incorporated Methods, compositions and kits for increasing genome editing efficiency
WO2018053373A1 (en) 2016-09-16 2018-03-22 The General Hospital Corporation Uses of satl-inducible kinase (sik) inhibitors for treating osteoporosis
TW201815418A (zh) 2016-09-27 2018-05-01 Vertex Pharma 使用dna破壞劑及dna-pk抑制劑之組合治療癌症的方法
AU2017335205B2 (en) 2016-09-29 2021-11-04 Janssen Sciences Ireland Unlimited Company Pyrimidine prodrugs for the treatment of viral infections and further diseases
KR102607967B1 (ko) * 2016-12-19 2023-11-29 메르크 파텐트 게엠베하 단백질 키나제 억제제 및 추가 화학요법제의 조합물
EP3589284A4 (en) 2017-02-28 2020-12-16 The General Hospital Corporation USES OF PYRIMIDOPYRIMIDINONES AS SIK INHIBITORS
US20200101080A1 (en) * 2017-03-31 2020-04-02 Bioventures, Llc Inhibitors of dna pk and uses thereof
CN111212837A (zh) 2017-04-07 2020-05-29 艾森医药公司 吡咯并嘧啶激酶抑制剂的药用盐、物理形态和组合物及其制备方法
HUE056406T2 (hu) 2017-05-18 2022-02-28 Idorsia Pharmaceuticals Ltd N-szubsztituált indol származékok
ES2929309T3 (es) 2017-05-18 2022-11-28 Idorsia Pharmaceuticals Ltd Derivados de benzofurano y benzotiofeno como moduladores del receptor PGE2
EA201992677A1 (ru) * 2017-05-18 2020-04-23 Идорсия Фармасьютиклз Лтд Пиримидиновые производные в качестве модуляторов pge2 рецепторов
AU2018269666B2 (en) 2017-05-18 2022-02-03 Idorsia Pharmaceuticals Ltd Phenyl derivatives as PGE2 receptor modulators
CA3063788A1 (en) 2017-05-18 2018-11-22 Idorsia Pharmaceuticals Ltd Pyrimidine derivatives
EA201992878A1 (ru) 2017-06-05 2020-05-08 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Соединения для лечения болезни хантингтона
BR112019027719A2 (pt) 2017-06-28 2020-07-28 Ptc Therapeutics, Inc. métodos para tratar a doença de huntington
EP3644996B1 (en) 2017-06-28 2023-07-26 PTC Therapeutics, Inc. Methods for treating huntington's disease
US12121524B2 (en) 2018-01-17 2024-10-22 Vertex Pharmaceuticals Incorporated DNA-PK inhibitors
WO2019143677A1 (en) 2018-01-17 2019-07-25 Vertex Pharmaceuticals Incorporated Quinoxalinone compounds, compositions, methods, and kits for increasing genome editing efficiency
AU2019209293B2 (en) 2018-01-17 2023-07-27 Vertex Pharmaceuticals Incorporated DNA-PK inhibitors
TW202415645A (zh) 2018-03-01 2024-04-16 愛爾蘭商健生科學愛爾蘭無限公司 ２，４－二胺基喹唑啉衍生物及其醫學用途
BR112020019373A2 (pt) 2018-03-27 2020-12-29 Ptc Therapeutics, Inc. Compostos para o tratamento da doença de hutington
HUE068060T2 (hu) * 2018-06-27 2024-12-28 Ptc Therapeutics Inc Heterociklikus és heteroaril vegyületek Huntington-kór kezelésére
KR20210038845A (ko) 2018-06-27 2021-04-08 피티씨 테라퓨틱스, 인크. 헌팅턴병 치료를 위한 헤테로아릴 화합물
WO2020005882A1 (en) 2018-06-27 2020-01-02 Ptc Therapeutics, Inc. Heteroaryl compounds for treating huntington's disease
US20220064146A1 (en) * 2018-12-31 2022-03-03 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
CN111909144A (zh) * 2019-05-10 2020-11-10 山东轩竹医药科技有限公司 喹唑啉类dna-pk抑制剂
TW202110849A (zh) * 2019-05-27 2021-03-16 大陸商迪哲（江蘇）醫藥股份有限公司 Ｄｎａ依賴性蛋白激酶抑制劑
EP3983542A2 (en) * 2019-06-17 2022-04-20 CRISPR Therapeutics AG Methods and compositions for improved homology directed repair
CN112300126A (zh) * 2019-07-31 2021-02-02 山东轩竹医药科技有限公司 杂环类dna-pk抑制剂
WO2021041546A1 (en) 2019-08-27 2021-03-04 Vertex Pharmaceuticals Incorporated Compositions and methods for treatment of disorders associated with repetitive dna
WO2021050059A1 (en) 2019-09-11 2021-03-18 Provincial Health Services Authority Dna-pk inhibiting compounds
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
US20220402920A1 (en) * 2019-12-31 2022-12-22 Chengdu Baiyu Pharmaceutical Co., Ltd. Purine derivative and medical use thereof
CN113372345B (zh) * 2020-02-25 2022-08-16 山东轩竹医药科技有限公司 氘代杂环类激酶抑制剂
CN114315834B (zh) * 2020-04-17 2024-01-05 成都百裕制药股份有限公司 咪唑啉酮衍生物及其在医药上的应用
US20220228142A1 (en) 2020-12-17 2022-07-21 Vertex Pharmaceuticals Incorporated Compositions and methods for editing beta-globin for treatment of hemaglobinopathies
WO2022182959A1 (en) 2021-02-26 2022-09-01 Vertex Pharmaceuticals Incorporated Compositions and methods for treatment of myotonic dystrophy type 1 with crispr/slucas9
TW202302848A (zh) 2021-02-26 2023-01-16 美商維泰克斯製藥公司 以crispr/sacas9治療第1型肌強直性營養不良之組合物及方法
WO2023018637A1 (en) 2021-08-09 2023-02-16 Vertex Pharmaceuticals Incorporated Gene editing of regulatory elements
AU2023397123A1 (en) * 2022-12-12 2025-02-13 Avelos Therapeutics Inc. Substituted heterocyclic compound derivatives and their pharmaceutical use
WO2025181336A1 (en) 2024-03-01 2025-09-04 Cellectis Sa Compositions and methods for hbb-editing in hspc

Family Cites Families (179)

* Cited by examiner, † Cited by third party
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
JPH05503517A (ja) 1989-12-18 1993-06-10 バージニア・コモンウェルス・ユニバーシティ シグマレセプターリガンド及びその用途
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
GB2338957B (en) 1997-02-19 2001-08-01 Berlex Lab N-heterocyclic derivatives as nos inhibitors
JPH10251255A (ja) 1997-03-14 1998-09-22 Nissan Chem Ind Ltd アジン誘導体
BR9809172A (pt) 1997-05-28 2000-08-01 Rhone Poulenc Rorer Pharma Composto, composição farmacêutica, e, processos de inibir a atividade da tirosina cinase pdgf, a atividade da tirosina cinase lck, a proliferação celular, diferenciação ou liberação de mediador em um paciente, para tratar uma patologia ligada a um distúrbio hiperproliferativo, para tratar restenose e para tratar a inflamação em um paciente
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
AU770600B2 (en) * 1999-10-07 2004-02-26 Amgen, Inc. Triazine kinase inhibitors
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
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
US6613776B2 (en) 2000-09-15 2003-09-02 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
NZ525008A (en) 2000-09-15 2004-12-24 Vertex Pharma 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
MXPA03005001A (es) 2000-12-05 2003-09-05 Vertex Pharma Inhibidores de n- terminal c-jun cinasas (jnk) y otras proteinas cinasas.
IL156408A0 (en) 2000-12-21 2004-01-04 Vertex Pharma Pyrazole derivatives and pharmaceutical compositions containing the same
WO2002062787A1 (en) 2001-02-02 2002-08-15 Glaxo Group Limited Pyrazoles as tgf inhibitors
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
ATE339416T1 (de) 2001-04-13 2006-10-15 Vertex Pharma Inhibitoren von c-jun-n-terminalen-kinasen (jnk) und anderen proteinkinasen
WO2002085909A1 (en) 2001-04-20 2002-10-31 Vertex Pharmaceuticals Incorporated 9-deazaguanine derivatives 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
US6762179B2 (en) 2001-05-31 2004-07-13 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinase
EP1392684B1 (en) 2001-06-01 2006-09-13 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinases
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
US20030199526A1 (en) 2001-12-07 2003-10-23 Deborah Choquette Pyrimidine-based compounds useful as GSK-3 inhibitors
RU2004126671A (ru) 2002-02-06 2005-04-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Гетероарилсоединения, полезные в качестве ингибиторов 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
WO2003091246A1 (en) 2002-04-26 2003-11-06 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
EP2316834A1 (en) 2002-05-06 2011-05-04 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
US20040208608A1 (en) 2002-06-24 2004-10-21 Alex Tager Dispersion compensation architecture for switch-ready optical networks
CA2491895C (en) 2002-07-09 2011-01-18 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
JP4741948B2 (ja) 2002-08-14 2011-08-10 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インヒビターおよびそれらの使用
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
ES2289349T3 (es) 2002-11-04 2008-02-01 Vertex Pharmaceuticals Incorporated Derivados de heteroaril-pirimidina como inhibidores de jak.
AU2003297160A1 (en) 2002-12-18 2004-07-22 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
JP5069905B2 (ja) 2003-01-21 2012-11-07 アプテュイト （ウエスト ラファイエット）、エルエルシー 新規な共結晶化
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
US7456190B2 (en) 2003-03-13 2008-11-25 Vertex Pharmaceuticals Incorporated Compositions useful as protein kinase inhibitors
WO2004085418A2 (en) 2003-03-24 2004-10-07 Luitpold Pharmaceuticals, Inc. Xanthones, thioxanthones and acridinones as dna-pk inhibitors
AU2004225965A1 (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
WO2005026129A1 (en) * 2003-09-15 2005-03-24 Gpc Biotech Ag 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
US7592340B2 (en) 2003-12-04 2009-09-22 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
CA2954578A1 (en) 2004-03-15 2005-09-29 Sunesis Pharmaceuticals, Inc. Methods of using sns-595 in treating cancer
GB0405985D0 (en) 2004-03-17 2004-04-21 Novartis Forschungsstiftung Kinase
US7358258B2 (en) 2004-05-14 2008-04-15 Vertex Pharmaceuticals Incorporated Prodrugs of an ERK protein kinase inhibitor
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
CN101870690A (zh) 2004-06-04 2010-10-27 艾尼纳制药公司 作为代谢调节剂的经取代芳基和杂芳基衍生物及其相关病症的预防和治疗
NZ580450A (en) 2004-09-17 2011-06-30 Vertex Pharma Diaminotriazole Compounds Useful as Protein Kinase Inhibitors
WO2006044502A2 (en) 2004-10-13 2006-04-27 Ptc Therapeutics, Inc. Pyrazole or triazole compounds and their use for the manufacture of a medicament for treating somatic mutation-related diseases
EP1828147A1 (en) 2004-10-15 2007-09-05 AstraZeneca AB Quinoxalines as b-raf inhibitors
GT200500284A (es) 2004-10-15 2006-03-27 Aventis Pharma Inc Pirimidinas como antagonistas del receptor de prostaglandina d2
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
US20060142572A1 (en) 2004-12-14 2006-06-29 Gabriel Martinez-Botella Inhibitors of ERK protein kinase and uses thereof
JP2008525461A (ja) 2004-12-23 2008-07-17 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 Ｅｒｋプロテインキナーゼの選択的阻害剤およびその使用
CA2597134C (en) 2005-02-04 2015-05-26 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
AR054438A1 (es) 2005-04-15 2007-06-27 Kudos Pharm Ltd Inhibidores de adn -pk
EP1901747A2 (en) 2005-05-25 2008-03-26 Ingenium Pharmaceuticals AG Pyrimidine-based cdk inhibitors for treating pain
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
US7874452B2 (en) 2005-07-22 2011-01-25 Berkeley Law & Technology Group, Llp Cup cover
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
US20070219192A1 (en) 2005-11-02 2007-09-20 Xiangping Qian Certain chemical entities, compositions, and methods
BRPI0619708A2 (pt) 2005-11-03 2011-10-11 Vertex Pharma composto, composição, método para inibir a atividade da proteìna aurora quinase numa amostra biológica, método para tratar distúrbio proliferativo e método para tratar cáncer
JP2009515992A (ja) 2005-11-16 2009-04-16 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アミノピリミジン
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
PE20071025A1 (es) 2006-01-31 2007-10-17 Mitsubishi Tanabe Pharma Corp Compuesto amina trisustituido
US8013153B2 (en) 2006-03-23 2011-09-06 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
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
RU2485115C2 (ru) 2006-07-14 2013-06-20 Новартис Аг Производные пиримидина в качестве ингибиторов alk-5
PE20080403A1 (es) * 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
US7635683B2 (en) 2006-08-04 2009-12-22 Enanta Pharmaceuticals, Inc. Quinoxalinyl tripeptide hepatitis C virus inhibitors
WO2008023357A1 (en) 2006-08-22 2008-02-28 Technion Research And Development Foundation Ltd. 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
KR101101675B1 (ko) * 2006-10-02 2011-12-30 노파르티스 아게 단백질 키나제 억제제로서의 화합물 및 조성물
DE102006050512A1 (de) 2006-10-26 2008-04-30 Bayer Healthcare Ag Substituierte heterocyclische Verbindungen und ihre Verwendung
AU2007317435A1 (en) 2006-11-02 2008-05-15 Vertex Pharmaceuticals Incorporated Aminopyridines and aminopyrimidines useful as inhibitors of protein kinases
WO2008070661A1 (en) 2006-12-04 2008-06-12 Neurocrine Biosciences, Inc. Substituted pyrimidines as adenosine receptor antagonists
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
JP2010514808A (ja) 2006-12-28 2010-05-06 アンブルックス，インコーポレイテッド フェナジンまたはキノキサリンで置換されたアミノ酸およびポリペプチド
CA2702647C (en) 2007-01-31 2016-03-22 Ym Biosciences Australia Pty Ltd Thiopyrimidine-based compounds and uses thereof
WO2008106202A1 (en) 2007-02-27 2008-09-04 Housey Gerard M Theramutein modulators
CA2680029A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
CN101663295B (zh) 2007-03-09 2014-11-05 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的氨基嘧啶类化合物
CA2679701A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyridines useful as inhibitors of protein kinases
JP2010522194A (ja) 2007-03-20 2010-07-01 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 キナーゼ阻害薬として有用なアミノピリミジン
DE102007015169A1 (de) 2007-03-27 2008-10-02 Universität des Saarlandes Campus Saarbrücken 17Beta-Hydroxysteroid-Dehydrogenase-Typ1-Inhibitoren zur Behandlung hormonabhängiger Erkrankungen
CN101679386A (zh) 2007-04-13 2010-03-24 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
US7910587B2 (en) 2007-04-26 2011-03-22 Enanta Pharmaceuticals, Inc. Quinoxalinyl dipeptide hepatitis C virus inhibitors
EP2152696B1 (en) 2007-05-02 2014-09-24 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase 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
CA2685876A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles 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
AU2008257044A1 (en) 2007-05-24 2008-12-04 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
AU2008257559B2 (en) 2007-05-25 2013-10-10 AbbVie Deutschland 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
WO2009008991A2 (en) 2007-07-06 2009-01-15 Government Of The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services National Institutes Of Health 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
PT2174934E (pt) 2007-08-01 2012-08-08 Ihara Chemical Ind Co Derivado de oxopirazina e herbicida
CA2696113A1 (en) 2007-08-10 2009-04-02 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
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
WO2009061761A2 (en) 2007-11-06 2009-05-14 E. I. Du Pont De Nemours And Company Fungicidal heterocyclic amines
WO2009091388A2 (en) 2007-12-21 2009-07-23 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
JPWO2009107391A1 (ja) 2008-02-27 2011-06-30 武田薬品工業株式会社 ６員芳香環含有化合物
EA021904B1 (ru) 2008-03-05 2015-09-30 Мерк Патент Гмбх Производные хиноксалинона в качестве стимуляторов секреции инсулина, способы их получения и их применение для лечения диабета
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
CA2728018C (en) 2008-06-16 2016-10-11 Merck Patent Gmbh Quinoxalinedione derivatives
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
NZ590784A (en) 2008-07-23 2012-12-21 Vertex Pharma Pyrazolopyridine kinase inhibitors
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
WO2010065899A2 (en) 2008-12-05 2010-06-10 Molecular Insight Pharmaceuticals, Inc. Technetium-and rhenium-bis(heteroaryl)complexes and methods of use thereof
PL2376485T3 (pl) 2008-12-19 2018-05-30 Vertex Pharmaceuticals Incorporated Pochodne pirazyny użyteczne jako inhibitory kinazy ATR
WO2010093808A1 (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
CN102574843B (zh) 2009-10-22 2015-06-17 法博太科制药有限公司 抗纤维化剂的稠环类似物
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
EA201290574A1 (ru) 2009-12-25 2012-12-28 Мотида Фармасьютикал Ко., Лтд. Новое производное 3-гидрокси-5-арилизотиазола
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
MX2012010557A (es) 2010-03-16 2012-10-05 Merck Patent Gmbh Morfolinilquinazolinas.
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
DE102010025786A1 (de) 2010-07-01 2012-01-05 Merck Patent Gmbh Pyrazolochinoline
DE102010035744A1 (de) 2010-08-28 2012-03-01 Merck Patent Gmbh Imidazolonylchinoline
US9464065B2 (en) 2011-03-24 2016-10-11 The Scripps Research Institute Compounds and methods for inducing chondrogenesis
JP2014510151A (ja) 2011-04-05 2014-04-24 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 Ａｔｒキナーゼ（ｔｒａｋｉｎａｓｅ）阻害剤として有用なアミノピラジン化合物
GB201114051D0 (en) 2011-08-15 2011-09-28 Domainex Ltd Compounds and their uses
JP6002223B2 (ja) 2011-08-26 2016-10-05 ニューファーマ， インコーポレイテッド 特定の化学的実体、組成物、および方法
CN115403531A (zh) 2011-09-14 2022-11-29 润新生物公司 作为激酶抑制剂的化学实体、组合物及方法
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
UA115983C2 (uk) * 2012-04-24 2018-01-25 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори днк-пк
WO2014075077A1 (en) 2012-11-12 2014-05-15 Neupharma, Inc. Certain chemical entities, compositions, and methods
SG11201507203RA (en) 2013-03-12 2015-10-29 Vertex Pharma Dna-pk inhibitors
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

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HRP20210365T1 (hr) 2021-04-16
KR20150005645A (ko) 2015-01-14
EP2841428A1 (en) 2015-03-04
DK2841428T3 (da) 2018-12-10
PL2841428T3 (pl) 2019-07-31
TR201816379T4 (tr) 2018-11-21
CY1124311T1 (el) 2022-07-22
BR112014026703A2 (pt) 2017-06-27
US9925188B2 (en) 2018-03-27
AU2017239481B2 (en) 2019-05-16
RU2638540C1 (ru) 2017-12-14

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