RU2675270C2 - Сокристаллы и содержащие их фармацевтические композиции - Google Patents

Сокристаллы и содержащие их фармацевтические композиции Download PDF

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RU2675270C2
RU2675270C2 RU2016118771A RU2016118771A RU2675270C2 RU 2675270 C2 RU2675270 C2 RU 2675270C2 RU 2016118771 A RU2016118771 A RU 2016118771A RU 2016118771 A RU2016118771 A RU 2016118771A RU 2675270 C2 RU2675270 C2 RU 2675270C2
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compound
crystal
day
adipic acid
cancer
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RU2016118771A
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RU2016118771A (ru
RU2016118771A3 (en
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Кваме Виреду НТИ-АДДАЕ
Саймон Адам О'НИЛ
Юэган Чжан
Майкл УОЛДО
Правин МУДУНУРИ
Бинь СУН
АЛСТЕН Джон Грегг ВАН
Марк ШТРОМАЙЕР
Кэти СТАВРОПУЛОС
Ирина Николаевна КАДИЯЛА
Меттачит НАВАМАЛ
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Вертекс Фармасьютикалз Инкорпорейтед
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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RU2016118771A 2013-10-17 2014-10-17 Сокристаллы и содержащие их фармацевтические композиции RU2675270C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361892002P 2013-10-17 2013-10-17
US61/892,002 2013-10-17
PCT/US2014/061102 WO2015058067A1 (en) 2013-10-17 2014-10-17 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

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RU2018143803A Division RU2823603C2 (ru) 2013-10-17 2014-10-17 Со-кристаллы и содержащие их фармацевтические композиции

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RU2016118771A RU2016118771A (ru) 2017-11-22
RU2016118771A3 RU2016118771A3 (en) 2018-07-10
RU2675270C2 true RU2675270C2 (ru) 2018-12-18

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CN (2) CN108771681B (enExample)
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Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS61664B1 (sr) 2012-04-24 2021-04-29 Vertex Pharma Inhibitori dna-pk
SI3527563T1 (sl) 2013-03-12 2022-01-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-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
MA39999A (fr) 2014-06-06 2015-12-10 Res Triangle Inst Agonistes du récepteur de l'apeline (apj) et leurs utilisations
JP6851989B2 (ja) 2015-05-18 2021-03-31 シン−ナット プロダクツ エンタープライズ エルエルシー 医薬用共結晶及びその用途
BR112017027285A2 (pt) * 2015-06-19 2018-09-11 Syn Nat Products Entpr Llc ?cocristal, composição farmacêutica e método para o tratamento de uma doença?
WO2016205782A1 (en) 2015-06-19 2016-12-22 Syn-Nat Products Enterprise LLC Composition containing carboplatin and use
CA2989001A1 (en) 2015-06-25 2016-12-29 Syn-Nat Products Enterprise LLC Pharmaceutical co-crystal composition and use thereof
CR20180323A (es) 2015-11-20 2018-08-06 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituídos como moduladores de los receptores de pge2
EP3386976A1 (en) 2015-12-09 2018-10-17 Research Triangle Institute, International Improved apelin receptor (apj) agonists and uses thereof
WO2017215593A1 (en) * 2016-06-13 2017-12-21 Syneurx International (Taiwan) Corp. Co-crystals of sodium benzoate and uses thereof
EP4219462A1 (en) * 2016-07-13 2023-08-02 Vertex Pharmaceuticals Incorporated Methods, compositions and kits for increasing genome editing efficiency
AU2017325870B2 (en) 2016-09-16 2021-07-22 Research Traingle Institute Tetrahydroisoquinoline kappa opioid antagonists
KR20190062485A (ko) * 2016-09-27 2019-06-05 버텍스 파마슈티칼스 인코포레이티드 Dna-손상제 및 dna-pk 저해제의 조합을 사용한 암 치료 방법
RU2764039C2 (ru) 2016-10-12 2022-01-14 Рисерч Трайэнгл Инститьют Гетероциклические агонисты рецептора апелина (apj) и их применение
ES3040063T3 (en) * 2016-12-19 2025-10-28 Merck Patent Gmbh Combination of a protein kinase inhibitor and an additional chemotherapeutic agent
US10696677B2 (en) 2016-12-21 2020-06-30 Research Triangle Institute Diaryl purine derivatives with improved bioavailability
CN110621671A (zh) 2017-05-18 2019-12-27 爱杜西亚药品有限公司 作为pge2受体调节剂的苯并呋喃及苯并噻吩衍生物
TW201900180A (zh) 2017-05-18 2019-01-01 瑞士商愛杜西亞製藥有限公司 嘧啶衍生物
PT3625228T (pt) 2017-05-18 2021-09-16 Idorsia Pharmaceuticals Ltd Derivados de pirimidina como moduladores dos recetores de pge2
LT3625222T (lt) 2017-05-18 2021-11-10 Idorsia Pharmaceuticals Ltd Fenilo dariniai, kaip pge2 receptoriaus moduliatoriai
ES2980444T3 (es) 2018-01-17 2024-10-01 Vertex Pharma Inhibidores de ADN-PK
US12121524B2 (en) 2018-01-17 2024-10-22 Vertex Pharmaceuticals Incorporated DNA-PK inhibitors
CN111770921B (zh) 2018-01-17 2024-03-22 沃泰克斯药物股份有限公司 用于提高基因组编辑效率的喹喔啉酮化合物，组合物，方法和试剂盒
CA3109809A1 (en) 2018-08-20 2020-02-27 Duke University Methods and compositions for drugs to treat ophthalmic diseases
MY204234A (en) 2018-08-27 2024-08-16 Regeneron Pharma Use of raman spectroscopy in downstream purification
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
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
CN114478399B (zh) * 2020-10-27 2024-10-29 华东理工大学 嘧菌酯低共熔混合物及其制备方法和应用
CN120555509B (zh) * 2025-07-30 2025-11-04 之江实验室 氨磷汀在提高基因组定点插入效率中的应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008042639A1 (en) * 2006-10-02 2008-04-10 Irm Llc Compounds and compositions as protein kinase inhibitors
RU2470922C2 (ru) * 2007-03-28 2012-12-27 Синджента Лимитед Сокристаллы
WO2013163190A1 (en) * 2012-04-24 2013-10-31 Vertex Pharmaceutical Incorporated Dna-pk inhibitors

Family Cites Families (180)

* 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
EP0507863A4 (en) 1989-12-28 1993-07-07 Virginia Commonwealth University Sigma receptor ligands and the use thereof
US6004979A (en) 1991-02-07 1999-12-21 Hoechst Marion Roussel Nitrogenous bicycles
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
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
EP1754703A3 (en) 1997-02-19 2007-02-28 Berlex, 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
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
AU3033500A (en) 1999-01-15 2000-08-01 Agouron Pharmaceuticals, Inc. Non-peptide glp-1 agonists
US6156373A (en) 1999-05-03 2000-12-05 Scimed Life Systems, Inc. Medical device coating methods and devices
US6258121B1 (en) 1999-07-02 2001-07-10 Scimed Life Systems, Inc. Stent coating
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
DK1259485T3 (da) 2000-02-29 2006-04-10 Millennium Pharm Inc Benzamider og beslægtede inhibitorer for faktor 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
US7419678B2 (en) 2000-05-12 2008-09-02 Cordis Corporation Coated medical devices for the prevention and treatment of vascular disease
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
US7473691B2 (en) 2000-09-15 2009-01-06 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
ATE346064T1 (de) 2000-09-15 2006-12-15 Vertex Pharma Pyrazolverbindungen als protein-kinasehemmer
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
US20040018228A1 (en) 2000-11-06 2004-01-29 Afmedica, Inc. Compositions and methods for reducing scar tissue formation
US20020111353A1 (en) 2000-12-05 2002-08-15 Mark Ledeboer Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
ATE354573T1 (de) 2000-12-21 2007-03-15 Vertex Pharma ßPYRAZOLVERBINDUNGEN, DIE SICH ALS PROTEINKINASEINHIBITOREN EIGNENß
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
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
US6762179B2 (en) 2001-05-31 2004-07-13 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinase
CA2446756C (en) 2001-06-01 2011-03-08 Vertex Pharmaceuticals Incorporated Thiazole compounds useful as inhibitors of protein kinase
CA2450769A1 (en) 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
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
US20030229390A1 (en) 2001-09-17 2003-12-11 Control Delivery Systems, Inc. On-stent delivery of pyrimidines and purine analogs
KR20040051618A (ko) 2001-10-25 2004-06-18 위스콘신 얼럼나이 리서어치 화운데이션 단백질 티로신 키나아제 저해제로 피복되거나 함침된 혈관스텐트 또는 이식물 및 그를 사용하는 방법
US6939376B2 (en) 2001-11-05 2005-09-06 Sun Biomedical, Ltd. Drug-delivery endovascular stent and method for treating restenosis
DE60236322D1 (de) 2001-12-07 2010-06-17 Vertex Pharma Verbindungen auf pyrimidin-basis als gsk-3-hemmer
SG159380A1 (en) 2002-02-06 2010-03-30 Vertex Pharma Heteroaryl compounds useful as inhibitors of 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
US20030204168A1 (en) 2002-04-30 2003-10-30 Gjalt Bosma Coated vascular devices
WO2004058753A1 (en) 2002-05-06 2004-07-15 Vertex Pharmaceuticals Incorporated Thiadiazoles or oxadiazoles and their use as inhibitors of jak protein kinase
MXPA04011956A (es) 2002-05-30 2005-03-31 Vertex Pharma Inhibidores de proteinas cinasas jak y cdk2.
US6835387B2 (en) 2002-06-11 2004-12-28 Scimed Life Systems, Inc. Sustained release of superoxide dismutase mimics from implantable or insertable medical devices
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
PL375447A1 (en) 2002-08-14 2005-11-28 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
US7419984B2 (en) 2002-10-17 2008-09-02 Cell Therapeutics, Inc. Pyrimidines and uses thereof
EP1562911B1 (en) 2002-11-01 2010-01-06 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of jak and other protein kinases
DE60316013T2 (de) 2002-11-04 2008-05-29 Vertex Pharmaceuticals Inc., Cambridge Heteroaryl-pyrimidinderivate als jak-inhibitoren
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
EP1596869B1 (en) * 2003-01-21 2014-06-04 New Form Pharmaceuticals Inc. Novel cocrystallization
WO2004072063A1 (en) 2003-02-07 2004-08-26 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
WO2004083203A1 (en) 2003-03-13 2004-09-30 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
EP1678147B1 (en) 2003-09-15 2012-08-08 Lead Discovery Center GmbH Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases
US7244735B2 (en) 2003-12-02 2007-07-17 Vertex Pharmaceuticals Inc. Heterocyclic protein kinase inhibitors and uses thereof
WO2005056547A2 (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
JP5317472B2 (ja) 2004-03-15 2013-10-16 サネシス ファーマシューティカルズ， インコーポレイテッド Ｓｎｓ−５９５、及びその使用方法
GB0405985D0 (en) 2004-03-17 2004-04-21 Novartis Forschungsstiftung Kinase
JP4993604B2 (ja) 2004-05-14 2012-08-08 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 ピロリルピリミジンｅｒｋプロテインキナーゼインヒビターのプロドラッグ
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
ATE415397T1 (de) 2004-06-04 2008-12-15 Arena Pharm Inc Substituierte aryl- und heteroarylderivate als modulatoren des stoffwechsels und für die prophylaxe und behandlung von damit in zusammenhang stehenden erkrankungen
NZ580450A (en) 2004-09-17 2011-06-30 Vertex Pharma Diaminotriazole Compounds Useful as Protein Kinase Inhibitors
WO2006044456A1 (en) 2004-10-13 2006-04-27 Ptc Therapeutics, Inc. Compounds for nonsense suppression, and methods for their use
HN2005000795A (es) 2004-10-15 2010-08-19 Aventis Pharma Inc Pirimidinas como antagonistas del receptor de prostaglandina d2
MX2007004480A (es) 2004-10-15 2007-05-08 Astrazeneca Ab Quinoxalinas como inhibidores b raf.
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
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
ZA200707482B (en) 2005-02-04 2008-12-31 Senomyx Inc Compounds comprising linked heteroaryl moieties and their use as novel umami flavour 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
US20090221581A1 (en) 2005-05-25 2009-09-03 Philipp Wabnitz Methods of 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
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
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
JP5249770B2 (ja) 2005-11-03 2013-07-31 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ジン
CA2629781A1 (en) 2005-11-16 2007-05-24 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
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
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
CA2657227A1 (en) 2006-07-14 2008-01-17 Novartis Ag Pyrimidine derivatives as alk-5 inhibitors
US7635683B2 (en) 2006-08-04 2009-12-22 Enanta Pharmaceuticals, Inc. Quinoxalinyl tripeptide hepatitis C virus inhibitors
CA2661307C (en) 2006-08-22 2016-07-19 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
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
WO2008070661A1 (en) 2006-12-04 2008-06-12 Neurocrine Biosciences, Inc. Substituted pyrimidines as adenosine receptor antagonists
DE602007007985D1 (de) 2006-12-19 2010-09-02 Vertex Pharma Als inhibitoren von proteinkinasen geeignete aminopyrimidine
EP2076500A4 (en) 2006-12-28 2009-12-09 Ambrx Inc AMINO ACIDS AND POLYPEPTIDES WITH PHENAZINE AND QUINOXALIN SUBSTITUTION
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
KR20090120510A (ko) 2007-03-09 2009-11-24 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제 억제제로서 유용한 아미노피리미딘
MX2009009592A (es) 2007-03-09 2009-11-10 Vertex Pharma Aminopiridinas utiles como inhibidores de proteinas cinasas.
CA2679884A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
CA2682195A1 (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
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
AU2008247592A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
JP5389786B2 (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 キナーゼ阻害として有用なアミノピリミジン
MX2009011811A (es) 2007-05-02 2010-01-14 Vertex Pharma Aminopirimidinas utiles como inhibidores de cinasa.
EP2150255A4 (en) 2007-05-10 2011-10-05 Glaxosmithkline Llc CHINOXALINE DERIVATIVES AS P13 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
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)
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
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
ES2389320T3 (es) 2007-08-01 2012-10-25 Kumiai Chemical Industry Co., Ltd. Derivado de oxopirazina y herbicida
WO2009042294A2 (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
CN101889004B (zh) 2007-10-12 2014-09-10 阿斯利康公司 蛋白激酶抑制剂
KR20100088150A (ko) 2007-11-06 2010-08-06 이 아이 듀폰 디 네모아 앤드 캄파니 살진균성 복소환식 아민
EP2231624A4 (en) 2007-12-21 2011-07-06 Progenics Pharm Inc TRIAZINE AND CORRESPONDING COMPOUNDS WITH ANTIVIRAL EFFECT, COMPOSITIONS AND METHOD THEREFOR
CA2714743C (en) 2008-02-19 2017-01-17 Janssen Pharmaceutica N.V. Aryl-hydroxyethylamino-pyrimidines and triazines as modulators of fatty acid amide hydrolase
EP2253618A1 (en) 2008-02-27 2010-11-24 Takeda Pharmaceutical Company Limited Compound having 6-membered aromatic ring
JP5618837B2 (ja) 2008-03-05 2014-11-05 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ インスリン分泌刺激剤としてのキノキサリノン誘導体、それらを得る方法および糖尿病を治療するためのそれらの使用
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
BRPI0915064B8 (pt) 2008-06-16 2021-05-25 Merck Patent Gmbh derivados de quinoxalinadiona, seus usos, e medicamentos
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
KR20110039563A (ko) 2008-07-23 2011-04-19 버텍스 파마슈티칼스 인코포레이티드 피라졸로피리딘 키나제 억제제
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
ES2548141T3 (es) 2008-11-20 2015-10-14 Glaxosmithkline Llc Compuestos químicos
WO2010065899A2 (en) 2008-12-05 2010-06-10 Molecular Insight Pharmaceuticals, Inc. Technetium-and rhenium-bis(heteroaryl)complexes and methods of use thereof
EP2376485B1 (en) 2008-12-19 2017-12-06 Vertex Pharmaceuticals Incorporated Pyrazine derivatives useful as inhibitors of atr kinase
US8592415B2 (en) 2009-02-11 2013-11-26 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
EP2491030B1 (en) 2009-10-22 2015-07-15 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
PE20121639A1 (es) 2009-12-25 2012-12-02 Mochida Pharm Co Ltd Derivados de 3-hidroxi-5-arilizotiazol como moduladores de gpr40
UY33213A (es) 2010-02-18 2011-09-30 Almirall Sa Derivados de pirazol como inhibidores de jak
WO2011113512A1 (de) 2010-03-16 2011-09-22 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
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
CA2846574C (en) 2011-08-26 2020-07-07 Neupharma, Inc. Quinoxaline sulfonamide derivates for use as kinase inhibitors
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
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
EP2916838B1 (en) 2012-11-12 2019-03-13 Neupharma, Inc. Certain chemical entities, compositions, and methods
SI3527563T1 (sl) 2013-03-12 2022-01-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-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

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008042639A1 (en) * 2006-10-02 2008-04-10 Irm Llc Compounds and compositions as protein kinase inhibitors
RU2470922C2 (ru) * 2007-03-28 2012-12-27 Синджента Лимитед Сокристаллы
WO2013163190A1 (en) * 2012-04-24 2013-10-31 Vertex Pharmaceutical Incorporated Dna-pk inhibitors
RU2638540C1 (ru) * 2012-04-24 2017-12-14 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы днк-пк

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
KASHISHIAN a et al., DNA-dependent Protein Kinase Inhibitors as Drug Candidates for the treatment of Cancer, Molecular Cancer Therapeutics, 2003, Vol: 2, Nr: 12, страницы: 1257 - 1264. *
Scott L.Childs et al., The Salt-Cocrystal Continuum: The Influence of Crystal Structure on ionisation State, Molecular Pharmaceutics, 2007, v.4, no.3, pp.323-338. *
приоритет 13.11.2012, 12.03.2013 и 24.04.2013 & *

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