IN2014KN02601A - - Google Patents

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Publication number
IN2014KN02601A
IN2014KN02601A IN2601KON2014A IN2014KN02601A IN 2014KN02601 A IN2014KN02601 A IN 2014KN02601A IN 2601KON2014 A IN2601KON2014 A IN 2601KON2014A IN 2014KN02601 A IN2014KN02601 A IN 2014KN02601A
Authority
IN
India
Prior art keywords
compounds
compositions
disorders
inhibitors
dna
Prior art date
Application number
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
Original Assignee
Vertex Pharma
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Vertex Pharma filed Critical Vertex Pharma
Publication of IN2014KN02601A publication Critical patent/IN2014KN02601A/en

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    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • 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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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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Abstract

The present invention relates to compounds of following formula (I) useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders, such as cancer.
IN2601KON2014 2012-04-24 2013-04-23 IN2014KN02601A (en)

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Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102024766B1 (en) 2011-04-08 2019-09-25 얀센 사이언시즈 아일랜드 언리미티드 컴퍼니 Pyrimidine derivatives for the treatment of viral infections
SG11201401244TA (en) 2011-11-09 2014-09-26 Janssen R & D Ireland Purine derivatives for the treatment of viral infections
US9034885B2 (en) 2012-01-13 2015-05-19 Acea Biosciences Inc. EGFR modulators and uses thereof
BR112014026703B1 (en) * 2012-04-24 2022-10-25 Vertex Pharmaceuticals Incorporated DNA-PK INHIBITORS AND THEIR USES, PHARMACEUTICAL COMPOSITION AND THEIR USES, AND METHOD OF SENSITIZING A CELL
JP6250046B2 (en) 2012-07-13 2017-12-20 ヤンセン・サイエンシズ・アイルランド・ユーシー Macrocyclic purines for the treatment of viral infections
WO2014056953A1 (en) 2012-10-10 2014-04-17 Janssen R&D Ireland Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases
SG11201503042QA (en) 2012-11-16 2015-06-29 Janssen Sciences Ireland Uc Heterocyclic substituted 2-amino-quinazoline derivatives for the treatment of viral infections
JP6404835B2 (en) 2013-02-21 2018-10-17 ヤンセン・サイエンシズ・アイルランド・ユーシー 2-Aminopyrimidine derivatives for the treatment of viral infections
PT3527563T (en) 2013-03-12 2021-12-09 Vertex Pharma Dna-pk inhibitors
WO2014154859A1 (en) 2013-03-29 2014-10-02 Janssen R&D Ireland Macrocyclic deaza-purinones for the treatment of viral infections
MY188071A (en) 2013-05-24 2021-11-16 Janssen Sciences Ireland Uc Pyridone derivatives for the treatment of viral infections and further diseases
AU2014301089B2 (en) 2013-06-27 2018-10-04 Janssen Sciences Ireland Uc Pyrrolo[3,2-d]pyrimidine derivatives for the treatment of viral infections and other diseases
MX368625B (en) 2013-07-30 2019-10-08 Janssen Sciences Ireland Uc THIENO[3,2-d]PYRIMIDINES DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS.
ES2705342T3 (en) * 2013-10-17 2019-03-22 Vertex Pharma Co-crystals of (S) -N-methyl-8- (1 - ((2'-methyl- [4,5'-bipirimidin] -6-yl) amino) propan-2-yl) quinoline-4-carboxamide and deuterated derivatives thereof as DNA-PK inhibitors
JP6374959B2 (en) * 2013-10-17 2018-08-15 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ DNA-PK inhibitor
AU2015292818B2 (en) * 2014-07-21 2020-01-16 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
CN104352488B (en) * 2014-10-31 2016-08-31 厦门大学 The application in preparation treatment pain medication of the one class substituted heterocycle derivant
WO2016066115A1 (en) * 2014-10-31 2016-05-06 厦门大学 Substituted heterocyclic derivative, preparation method and use thereof
CN104356082B (en) * 2014-10-31 2016-07-13 厦门大学 One class substituted heterocycle derivant and preparation method thereof
US10533011B2 (en) * 2015-10-09 2020-01-14 ACEA Therapeutics, Inc. Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same
DK3365334T3 (en) * 2015-10-21 2024-09-23 Otsuka Pharma Co Ltd BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS
CR20180323A (en) 2015-11-20 2018-08-06 Idorsia Pharmaceuticals Ltd DERIVATIVES OF INDOL N-SUBSTITUTES AS MODULATORS OF PGE2 RECEIVERS
CA3119019C (en) 2015-12-10 2024-06-11 Ptc Therapeutics, Inc. Compounds and methods for treating huntington's disease
US11053256B2 (en) 2016-07-01 2021-07-06 Janssen Sciences Ireland Unlimited Company Dihydropyranopyrimidines for the treatment of viral infections
KR20190075043A (en) 2016-07-05 2019-06-28 더 브로드 인스티튜트, 인코퍼레이티드 Bicyclic urea kinase inhibitors and uses thereof
MA45670A (en) * 2016-07-13 2019-05-22 Vertex Pharma PROCESSES, COMPOSITIONS AND KITS TO INCREASE 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
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
EA038646B1 (en) 2016-09-29 2021-09-28 Янссен Сайенсиз Айрлэнд Анлимитед Компани Pyrimidine prodrugs for the treatment of viral infections and further diseases
EP3554495A1 (en) 2016-12-19 2019-10-23 Merck Patent GmbH Combination of a protein kinase inhibitor and an additional chemotherapeutic agent
US11285158B2 (en) 2017-02-28 2022-03-29 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
AU2017408099A1 (en) 2017-04-07 2019-11-07 ACEA Therapeutics, Inc. Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same
SI3625224T1 (en) 2017-05-18 2021-11-30 Idorsia Pharmaceuticals Ltd N-substituted indole derivatives
AR111874A1 (en) 2017-05-18 2019-08-28 Idorsia Pharmaceuticals Ltd PIRIMIDINE DERIVATIVES
WO2018210987A1 (en) 2017-05-18 2018-11-22 Idorsia Pharmaceuticals Ltd Benzofurane and benzothiophene derivatives as pge2 receptor modulators
LT3625228T (en) * 2017-05-18 2021-10-25 Idorsia Pharmaceuticals Ltd Pyrimidine derivatives as pge2 receptor modulators
PE20191814A1 (en) 2017-05-18 2019-12-27 Idorsia Pharmaceuticals Ltd PYRIMIDINE DERIVATIVES AS PGE2 RECEPTOR MODULATORS
SG11201911615WA (en) 2017-06-05 2020-01-30 Ptc Therapeutics Inc Compounds for treating huntington's disease
BR112019027717A2 (en) 2017-06-28 2020-07-28 Ptc Therapeutics, Inc. methods to treat huntington's disease
US11395822B2 (en) 2017-06-28 2022-07-26 Ptc Therapeutics, Inc. Methods for treating Huntington's disease
WO2019143678A1 (en) 2018-01-17 2019-07-25 Vertex Pharmaceuticals Incorporated Dna-pk inhibitors
WO2019143675A1 (en) 2018-01-17 2019-07-25 Vertex Pharmaceuticals Incorporated Dna-pk inhibitors
TW201945003A (en) 2018-03-01 2019-12-01 愛爾蘭商健生科學愛爾蘭無限公司 2,4-diaminoquinazoline derivatives and medical uses thereof
US12103926B2 (en) 2018-03-27 2024-10-01 Ptc Therapeutics, Inc. Compounds for treating huntington's disease
US11685746B2 (en) 2018-06-27 2023-06-27 Ptc Therapeutics, Inc. Heteroaryl compounds for treating Huntington's disease
LT3814357T (en) * 2018-06-27 2024-06-25 Ptc Therapeutics, Inc. Heterocyclic and heteroaryl compounds for treating huntington's disease
CN111909144A (en) * 2019-05-10 2020-11-10 山东轩竹医药科技有限公司 Quinazoline DNA-PK inhibitor
TW202110849A (en) * 2019-05-27 2021-03-16 大陸商迪哲（江蘇）醫藥股份有限公司 Dna-dependent protein kinase inhibitor
CA3142521A1 (en) 2019-06-17 2020-12-24 Vertex Pharmaceuticals Incorporated Compositions and methods for editing beta-globin for treatment of hemaglobinopathies
CN112300126A (en) * 2019-07-31 2021-02-02 山东轩竹医药科技有限公司 Heterocyclic DNA-PK inhibitors
TW202118873A (en) 2019-08-27 2021-05-16 美商維泰克斯製藥公司 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
CN112574211B (en) * 2019-09-29 2022-06-14 山东轩竹医药科技有限公司 Heterocyclic kinase inhibitors
CN112574179B (en) * 2019-09-29 2022-05-10 山东轩竹医药科技有限公司 DNA-PK inhibitors
WO2021136463A1 (en) * 2019-12-31 2021-07-08 成都百裕制药股份有限公司 Purine derivative and medical use thereof
CN113372345B (en) * 2020-02-25 2022-08-16 山东轩竹医药科技有限公司 Deuterated heterocyclic kinase inhibitors
JP7498795B2 (en) * 2020-04-17 2024-06-12 チェンドゥ バイユー ファーマシューティカル カンパニー リミテッド Imidazolidinone derivatives and their applications in medicine
WO2022133246A1 (en) 2020-12-17 2022-06-23 Vertex Pharmaceuticals Incorporated Compositions and methods for editing beta-globin for treatment of hemaglobinopathies
EP4298221A1 (en) 2021-02-26 2024-01-03 Vertex Pharmaceuticals Incorporated Compositions and methods for treatment of myotonic dystrophy type 1 with crispr/slucas9
TW202302848A (en) 2021-02-26 2023-01-16 美商維泰克斯製藥公司 Compositions and methods for treatment of myotonic dystrophy type 1 with crispr/sacas9
WO2023018637A1 (en) 2021-08-09 2023-02-16 Vertex Pharmaceuticals Incorporated Gene editing of regulatory elements
WO2024128741A1 (en) * 2022-12-12 2024-06-20 Avelos Therapeutics Inc. Substituted heterocyclic compound derivatives and their pharmaceutical use

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
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
ES2104862T3 (en) 1991-02-07 1997-10-16 Roussel Uclaf NITROGENATED BICYCLE DERIVATIVES, THEIR PREPARATION PROCEDURE, THEIR INTERMEDIATE PRODUCTS OBTAINED, THEIR APPLICATION AS DRUGS AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM.
EP0519211A1 (en) 1991-05-17 1992-12-23 Hoechst Schering AgrEvo GmbH Substituted 4-aminopyrimidine, process for their preparation and their use as parasiticide
DE4208254A1 (en) 1992-03-14 1993-09-16 Hoechst Ag SUBSTITUTED PYRIMIDINE, METHOD FOR THE PRODUCTION THEREOF AND THEIR USE AS A PEST CONTROL AND FUNGICIDE
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 (en) 1994-10-19 1996-04-25 Hoechst Ag Quinoxalines, process for their preparation and their use
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 (en) 1997-03-14 1998-09-22 Nissan Chem Ind Ltd Azine derivative
HUP0004807A3 (en) 1997-05-28 2001-12-28 Aventis Pharma Inc Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases, use of them for producing pharmaceutical compositions and pharmaceutical compositions containing them
DE19801598C2 (en) 1998-01-17 2000-05-11 Aventis Res & Tech Gmbh & Co Catalytic synthesis of N-alkylated anilines from olefins and anilines
DE19836697A1 (en) 1998-08-13 2000-02-17 Hoechst Marion Roussel De Gmbh New substituted 4-amino-2-aryl-pyrimidines, are soluble guanylate cyclase activators useful e.g. for treating atherosclerosis, hypertension, angina pectoris, thrombosis, asthma or diabetes
EP1147094A1 (en) 1999-01-15 2001-10-24 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
EP1255741A2 (en) 2000-02-01 2002-11-13 Cor Therapeutics, Inc. 2- 1H]-QUINOLONE AND 2- 1H]-QUINOXALONE INHIBITORS OF FACTOR Xa
DE60115394T2 (en) 2000-02-29 2006-10-19 Millennium Pharmaceuticals, Inc., Cambridge BENZAMID AND SIMILAR INHIBITORS FROM FACTOR XA
AU2001245401A1 (en) 2000-03-01 2001-09-12 Sumitomo Pharmaceuticals Company, Limited Hydrazones and analogs as cholesterol lowering agents
DE10013318A1 (en) 2000-03-17 2001-09-20 Merck Patent Gmbh Quinoxaline derivatives are used as photo-stable UV filters in cosmetic or pharmaceutical sunscreens for the hair or skin
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
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
US7473691B2 (en) 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
EP1317448B2 (en) 2000-09-15 2011-05-04 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
ATE407132T1 (en) 2000-12-05 2008-09-15 Vertex Pharma INHIBITORS OF C-JUN N-TERMINAL KINASES (JNK) AND OTHER PROTEIN KINASES
JP4160395B2 (en) 2000-12-21 2008-10-01 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 Pyrazole compounds useful as protein kinase inhibitors
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
DE60214701T2 (en) 2001-04-13 2007-09-13 Vertex Pharmaceuticals Inc., Cambridge INHIBITORS OF C-JUN-N TERMINAL KINASES (JNK) AND OTHER PROTEIN KINASES
WO2002085909A1 (en) 2001-04-20 2002-10-31 Vertex Pharmaceuticals Incorporated 9-deazaguanine derivatives as inhibitors of gsk-3
JP4316893B2 (en) 2001-05-16 2009-08-19 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 Inhibitors of Src and other protein kinases
MXPA03010961A (en) 2001-05-31 2004-02-27 Vertex Pharma Thiazole compounds useful as inhibitors of protein kinases.
JP4523271B2 (en) 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 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
ATE337312T1 (en) 2001-07-03 2006-09-15 Vertex Pharma ISOXAZOLYL PYRIMIDINES AS 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
PL372198A1 (en) 2002-02-06 2005-07-11 Vertex Pharmaceuticals Incorporated 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
US7304061B2 (en) 2002-04-26 2007-12-04 Vertex Pharmaceuticals Incorporated Heterocyclic 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
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
US20040208608A1 (en) 2002-06-24 2004-10-21 Alex Tager Dispersion compensation architecture for switch-ready optical networks
AU2003247959B2 (en) 2002-07-09 2010-07-29 Vertex Pharmaceuticals Incorporated Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities
US7304071B2 (en) 2002-08-14 2007-12-04 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
US7419984B2 (en) 2002-10-17 2008-09-02 Cell Therapeutics, Inc. Pyrimidines and uses thereof
AU2003286876A1 (en) 2002-11-01 2004-06-07 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of jak and other protein kinases
DE60316013T2 (en) 2002-11-04 2008-05-29 Vertex Pharmaceuticals Inc., Cambridge HETEROARYL PYRIMIDINE DERIVATIVES AS JAK INHIBITORS
DE60326646D1 (en) 2002-12-18 2009-04-23 Vertex Pharma BENZINE OXAZOLE DERIVATIVES PROPER AS INHIBITORS OF PROTEIN KINASES
US7144911B2 (en) 2002-12-31 2006-12-05 Deciphera Pharmaceuticals Llc Anti-inflammatory medicaments
WO2004064762A2 (en) 2003-01-21 2004-08-05 S.S.C.I. Inc. Novel cocrystallization
WO2004072063A1 (en) 2003-02-07 2004-08-26 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
EP1606284B1 (en) 2003-03-13 2009-12-02 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
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
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
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
BRPI0511124A (en) 2004-05-14 2007-11-27 Vertex Pharma erk inhibitors prodrugs pyrrolylpyrimidine protein kinase
JP4449580B2 (en) 2004-05-31 2010-04-14 宇部興産株式会社 4-Aralkylaminopyrimidine derivatives and antibacterial agents
UA92150C2 (en) 2004-06-04 2010-10-11 Арена Фармасьютикалз, Инк. Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
ES2359007T3 (en) 2004-09-17 2011-05-17 Vertex Pharmaceuticals Incorporated DIAMINOTRIAZOL COMPOUNDS USEFUL AS INHIBITORS OF KINASE PROTEINS.
WO2006044505A2 (en) 2004-10-13 2006-04-27 Ptc Therapeutics, Inc. Compounds for nonsense suppression, and methods for their use
GT200500284A (en) 2004-10-15 2006-03-27 Aventis Pharma Inc PYRIMIDINS AS ANTAGONISTS OF PROSTAGLANDINA D2 RECEPTOR
JP2008516939A (en) 2004-10-15 2008-05-22 アストラゼネカ アクチボラグ Chemical compound
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
EP1831181A2 (en) 2004-12-14 2007-09-12 Vertex Pharmaceuticals Incorporated Pyrimidine inhibitors of erk protein kinase and uses thereof
EP1833820A1 (en) 2004-12-23 2007-09-19 Vertex Pharmaceuticals Incorporated Selective inhibitors of erk protein kinase and uses therof
JP4734346B2 (en) 2005-02-04 2011-07-27 セノミックス インコーポレイテッド Compounds containing linked heteroaryl moieties, and novel umami flavor modifiers, tastants and taste enhancers for edible compositions
CN101184395A (en) 2005-04-06 2008-05-21 Irm责任有限公司 Diarylamine-containing compounds and compositions, and their use as modulators of steroid hormone nuclear receptors
AR053358A1 (en) 2005-04-15 2007-05-02 Cancer Rec Tech Ltd DNA INHIBITORS - PK
JP2008542219A (en) * 2005-05-25 2008-11-27 インゲニウム ファーマシューティカルズ ジーエムビーエイチ Pain treatment
WO2006138418A2 (en) 2005-06-14 2006-12-28 President And Fellows Of Harvard College Improvement of cognitive performance with sirtuin activators
JP2007008045A (en) 2005-06-30 2007-01-18 Mitsui Chemicals Inc Optical recording medium and 1h-quinoxaline-2-on derivative
US7874452B2 (en) 2005-07-22 2011-01-25 Berkeley Law & Technology Group, Llp Cup cover
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
JP5249771B2 (en) 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 Aminopyrimidines useful as kinase inhibitors
ATE508126T1 (en) 2005-11-16 2011-05-15 Vertex Pharma AMINOPYRIMIDINES SUITABLE 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 Kinase inhibitors and methods of their use
PE20071025A1 (en) 2006-01-31 2007-10-17 Mitsubishi Tanabe Pharma Corp TRISUSTITUTED AMINE COMPOUND
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
MX2009000310A (en) 2006-07-14 2009-01-26 Novartis Ag Pyrimidine derivatives as alk-5 inhibitors.
PE20080403A1 (en) * 2006-07-14 2008-04-25 Amgen Inc FUSED HETEROCYCLIC DERIVATIVES AND METHODS OF USE
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 (en) 2006-09-07 2008-03-26 Bayer Schering Pharma Aktiengesellschaft N-(1-hetaryl-piperidin-4-yl)-(het)arylamide as EP2 receptor modulators
US7875603B2 (en) 2006-09-21 2011-01-25 Nova Southeastern University Specific inhibitors for vascular endothelial growth factor receptors
WO2008042639A1 (en) * 2006-10-02 2008-04-10 Irm Llc Compounds and compositions as protein kinase inhibitors
DE102006050512A1 (en) 2006-10-26 2008-04-30 Bayer Healthcare Ag New substituted dihydropyrazole- and dihydrotriazole derivatives are hypoxia-inducible transcription factor-prolyl-4-hydroxylase inhibitors useful to treat/prevent e.g. cardiovascular diseases, heart-circulation diseases and anemia
JP2010509231A (en) 2006-11-02 2010-03-25 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 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
MX2009006690A (en) 2006-12-19 2009-07-31 Vertex Pharma 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
EP2114900B1 (en) 2007-01-31 2018-10-10 YM BioSciences Australia Pty Ltd Thiopyrimidine-based compounds and uses thereof
WO2008106202A1 (en) 2007-02-27 2008-09-04 Housey Gerard M Theramutein modulators
EP2134709A1 (en) 2007-03-09 2009-12-23 Vertex Pharmaceuticals, Inc. Aminopyridines useful as inhibitors of protein kinases
ES2435997T3 (en) 2007-03-09 2013-12-26 Vertex Pharmaceuticals, Inc. Aminopyrimidines useful as protein kinase inhibitors
CA2680029A1 (en) 2007-03-09 2008-09-18 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as inhibitors of protein kinases
JP2010522194A (en) 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 Aminopyrimidines useful as kinase inhibitors
DE102007015169A1 (en) 2007-03-27 2008-10-02 Universität des Saarlandes Campus Saarbrücken 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-dependent diseases
MX2009011059A (en) 2007-04-13 2009-11-26 Vertex Pharma Aminopyrimidines useful as kinase inhibitors.
US7910587B2 (en) 2007-04-26 2011-03-22 Enanta Pharmaceuticals, Inc. Quinoxalinyl dipeptide hepatitis C virus inhibitors
AU2008247594A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2008247592A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
AU2008247595A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
WO2008141065A1 (en) 2007-05-10 2008-11-20 Smithkline Beecham Corporation Quinoxaline derivatives as p13 kinase inhibitors
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
TWI443090B (en) 2007-05-25 2014-07-01 Abbvie Deutschland 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
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 (en) 2007-07-19 2009-03-02 COMPOUNDS DERIVED FROM DIBENZOTIFENILAMINO-CROMEN-4-ACTIVE WAVES REPLACED AND ITS ISOMERS AND APPLICATIONS
MX2010001240A (en) 2007-08-01 2010-04-30 Kumiai Chemical Industry Co Oxopyrazine derivative and herbicide.
EP2190466A4 (en) 2007-08-10 2011-12-21 Burnham Inst Medical Research Tissue-nonspecific alkaline phosphatase (tnap) activators and uses thereof
DE102007044032A1 (en) 2007-09-14 2009-03-19 Bayer Healthcare Ag New substituted heteroaryl compounds are hypoxia-inducible factor prolyl-4-hydroxylase inhibitors useful to treat and/or prevent e.g. circulatory heart diseases, heart failure, anemia, chronic kidney diseases and renal failure
JP5681855B2 (en) 2007-10-12 2015-03-11 アストラゼネカ エービー Protein kinase inhibitors
KR20100088150A (en) 2007-11-06 2010-08-06 이 아이 듀폰 디 네모아 앤드 캄파니 Fungicidal heterocyclic amines
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 (en) 2008-03-05 2014-03-19 默克专利有限公司 Quinoxalinone derivatives as insulin secretion stimulators, methods for obtaining them and use thereof for the treatment of diabetes
US8268834B2 (en) 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
JPWO2009147990A1 (en) 2008-06-02 2011-10-27 Ｍｓｄ株式会社 New isoxazole derivatives
MX2010013577A (en) 2008-06-16 2010-12-21 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
MX2011000839A (en) 2008-07-23 2011-04-05 Vertex Pharma Pyrazolopyridine kinase inhibitors.
WO2010048149A2 (en) 2008-10-20 2010-04-29 Kalypsys, Inc. Heterocyclic modulators of gpr119 for treatment of disease
WO2010059658A1 (en) 2008-11-20 2010-05-27 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
KR101755216B1 (en) 2008-12-19 2017-07-07 버텍스 파마슈티칼스 인코포레이티드 Pyrazine derivatives useful as inhibitors of ATR kinase
US8592415B2 (en) 2009-02-11 2013-11-26 Reaction Biology Corp. Selective kinase inhibitors
JP2010111702A (en) 2009-02-16 2010-05-20 Tetsuya Nishio Heterocyclic compound, method for producing the same and use thereof
AR077468A1 (en) 2009-07-09 2011-08-31 Array Biopharma Inc PIRAZOLO COMPOUNDS (1,5-A) PYRIMIDINE SUBSTITUTED AS TRK-QUINASA INHIBITORS
US8906914B2 (en) 2009-08-18 2014-12-09 Janssen Pharmaceutica Nv Ethylene diamine modulators of fatty acid hydrolase
AR077999A1 (en) 2009-09-02 2011-10-05 Vifor Int Ag ANTIGONISTS OF PYRIMIDIN AND TRIAZIN-HEPCIDINE
US9062076B2 (en) 2009-10-22 2015-06-23 Fibrotech Therapeutics Pty Ltd Fused ring analogues of anti-fibrotic agents
ES2360333B1 (en) 2009-10-29 2012-05-04 Consejo Superior De Investigaciones Cientificas (Csic) (70%) DERIVATIVES OF BIS (ARALQUIL) AMINO AND AROMATICS SYSTEMS OF SIX MEMBERS AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE PATHOLOGIES, INCLUDING ALZHEIMER'S DISEASE
WO2011052756A1 (en) 2009-10-30 2011-05-05 持田製薬株式会社 Novel 3-hydroxy-5-arylisoxazole derivative
MX2012007474A (en) 2009-12-25 2012-08-01 Mochida Pharm Co Ltd Novel 3-hydroxy-5-arylisothiazole derivative.
UY33213A (en) 2010-02-18 2011-09-30 Almirall Sa PIRAZOL DERIVATIVES AS JAK INHIBITORS
BR112012022868A2 (en) 2010-03-16 2018-06-05 Merck Patent Gmbh morpholinylquinazolines
TWI516264B (en) 2010-05-06 2016-01-11 臺北醫學大學 Aroylquinoline compounds
JP2011246389A (en) 2010-05-26 2011-12-08 Oncotherapy Science Ltd Condensed-ring pyrazole derivative having ttk inhibiting action
DE102010025786A1 (en) 2010-07-01 2012-01-05 Merck Patent Gmbh Pyrazolochinoline
DE102010035744A1 (en) 2010-08-28 2012-03-01 Merck Patent Gmbh Imidazolonylchinoline
WO2012129562A2 (en) 2011-03-24 2012-09-27 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
JP6002223B2 (en) 2011-08-26 2016-10-05 ニューファーマ， インコーポレイテッド Specific chemical entities, compositions and methods
CN104080455B (en) 2011-09-14 2018-07-31 润新生物公司 Certain chemical entities, composition and method
US9249110B2 (en) 2011-09-21 2016-02-02 Neupharma, Inc. Substituted quinoxalines as B-raf kinase inhibitors
WO2013049701A1 (en) 2011-09-30 2013-04-04 Neupharma, Inc. Certain chemical entities, compositions, and methods
DE102011118830A1 (en) 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
EP2806874B1 (en) 2012-01-25 2017-11-15 Neupharma, Inc. Quinoxaline-oxy-phenyl derivatives as kinase inhibitors
BR112014026703B1 (en) 2012-04-24 2022-10-25 Vertex Pharmaceuticals Incorporated DNA-PK INHIBITORS AND THEIR USES, PHARMACEUTICAL COMPOSITION AND THEIR USES, AND METHOD OF SENSITIZING A CELL
EP2916838B1 (en) 2012-11-12 2019-03-13 Neupharma, Inc. Certain chemical entities, compositions, and methods
PT3527563T (en) 2013-03-12 2021-12-09 Vertex Pharma Dna-pk inhibitors
ES2705342T3 (en) 2013-10-17 2019-03-22 Vertex Pharma Co-crystals of (S) -N-methyl-8- (1 - ((2'-methyl- [4,5'-bipirimidin] -6-yl) amino) propan-2-yl) quinoline-4-carboxamide and deuterated derivatives thereof as DNA-PK inhibitors

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