JP2014533695A5 - - Google Patents

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JP2014533695A5
JP2014533695A5 JP2014542506A JP2014542506A JP2014533695A5 JP 2014533695 A5 JP2014533695 A5 JP 2014533695A5 JP 2014542506 A JP2014542506 A JP 2014542506A JP 2014542506 A JP2014542506 A JP 2014542506A JP 2014533695 A5 JP2014533695 A5 JP 2014533695A5
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optionally substituted
ring
hydrogen
alkyl
heteroaryl
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JP2014542506A
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JP6106685B2 (ja
JP2014533695A (ja
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Priority claimed from PCT/US2012/065618 external-priority patent/WO2013074986A1/en
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Publication of JP2014533695A5 publication Critical patent/JP2014533695A5/ja
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JP2014542506A 2011-11-17 2012-11-16 C−jun−n−末端キナーゼ(jnk)の阻害剤 Expired - Fee Related JP6106685B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161561078P 2011-11-17 2011-11-17
US61/561,078 2011-11-17
PCT/US2012/065618 WO2013074986A1 (en) 2011-11-17 2012-11-16 Inhibitors of c-jun-n-terminal kinase (jnk)

Related Child Applications (1)

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JP2017042266A Division JP6262383B2 (ja) 2011-11-17 2017-03-06 C−jun−n−末端キナーゼ(jnk)の阻害剤

Publications (3)

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JP2014533695A JP2014533695A (ja) 2014-12-15
JP2014533695A5 true JP2014533695A5 (enExample) 2016-04-07
JP6106685B2 JP6106685B2 (ja) 2017-04-05

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JP2014542506A Expired - Fee Related JP6106685B2 (ja) 2011-11-17 2012-11-16 C−jun−n−末端キナーゼ(jnk)の阻害剤
JP2017042266A Expired - Fee Related JP6262383B2 (ja) 2011-11-17 2017-03-06 C−jun−n−末端キナーゼ(jnk)の阻害剤

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JP2017042266A Expired - Fee Related JP6262383B2 (ja) 2011-11-17 2017-03-06 C−jun−n−末端キナーゼ(jnk)の阻害剤

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US (4) US9382239B2 (enExample)
EP (2) EP3569598A1 (enExample)
JP (2) JP6106685B2 (enExample)
AU (1) AU2012340200B2 (enExample)
CA (1) CA2856291C (enExample)
WO (1) WO2013074986A1 (enExample)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010144909A1 (en) 2009-06-12 2010-12-16 Novartis Ag Fused heterocyclic compounds and their uses
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
CA2856291C (en) 2011-11-17 2020-08-11 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
WO2013142817A2 (en) 2012-03-23 2013-09-26 Dennis Brown Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
US9168257B2 (en) * 2013-05-22 2015-10-27 Children's Hospital Medical Center Combination therapy for MDS
US10047070B2 (en) 2013-10-18 2018-08-14 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
EP3057954A2 (en) * 2013-10-18 2016-08-24 Syros Pharmaceuticals, Inc. Heteromaromatic compounds useful for the treatment of proliferative diseases
AU2014337122B2 (en) * 2013-10-18 2019-01-03 Dana-Farber Cancer Institute, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
JP6879740B2 (ja) 2013-12-13 2021-06-02 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド リンパ形質細胞性リンパ腫を処置する方法
US9908872B2 (en) 2013-12-13 2018-03-06 Dana-Farber Cancer Institute, Inc. Methods to treat lymphoplasmacytic lymphoma
LT3126352T (lt) * 2014-04-04 2019-01-10 Syros Pharmaceuticals, Inc. Nuo ciklino priklausomos kinazės 7 (cdk7) inhibitoriai
US10336760B2 (en) 2014-04-05 2019-07-02 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2016014542A1 (en) 2014-07-21 2016-01-28 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
EP3172213B1 (en) 2014-07-21 2021-09-22 Dana-Farber Cancer Institute, Inc. Macrocyclic kinase inhibitors and uses thereof
AU2015300782B2 (en) 2014-08-08 2020-04-16 Dana-Farber Cancer Institute, Inc. Uses of salt-inducible kinase (SIK) inhibitors
JP6788583B2 (ja) 2014-10-22 2020-11-25 ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド 増殖性疾患を処置するためのチアゾリル含有化合物
EP3236959B1 (en) 2014-12-23 2025-09-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
EP3302448B1 (en) * 2015-06-04 2023-10-25 Aurigene Oncology Limited Substituted heterocyclyl derivatives as cdk inhibitors
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
EP3313530B1 (en) * 2015-06-26 2022-10-05 Dana Farber Cancer Institute, Inc. 4,6-pyrimidinylene derivatives and uses thereof
HK1254469A1 (zh) * 2015-06-26 2019-07-19 Dana Farber Cancer Institute, Inc. 稠合双环嘧啶衍生物及其用途
EP4019515A1 (en) 2015-09-09 2022-06-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
EP3445365A4 (en) * 2016-04-22 2019-10-16 Dana-Farber Cancer Institute, Inc. EZH2 INHIBITORS AND USES THEREOF
CN109311858B (zh) 2016-05-26 2021-12-03 里科瑞尔姆Ip控股有限责任公司 Egfr抑制剂化合物
US10954242B2 (en) 2016-07-05 2021-03-23 The Broad Institute, Inc. Bicyclic urea kinase inhibitors and uses thereof
WO2018029336A1 (en) 2016-08-12 2018-02-15 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for determining whether a subject was administered with an activator of the ppar beta/delta pathway.
US11254667B2 (en) 2016-08-17 2022-02-22 Children's Hospital Medical Center Substituted imidazo[1,2-A]pyridines as IRAK 1/4 and flt3 inhibitors
US11542261B2 (en) 2016-08-17 2023-01-03 Children's Hospital Medical Center Substituted Imidazo[1,2-a]-pyridines as IRAK 1/4 and FLT3 inhibitors
US11241435B2 (en) 2016-09-16 2022-02-08 The General Hospital Corporation Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis
US11547696B2 (en) 2016-10-28 2023-01-10 Children's Hospital Medical Center Methods and compositions for treatment of myelodysplastic syndromes and/or acute myeloid leukemias
CA3041563C (en) 2016-11-22 2023-10-31 Dana-Farber Cancer Institute, Inc. Pyrimidin-2-amine derivatives and pharmaceutical compositions thereof useful as inhibitors of cyclin-dependent kinase 12 (cdk12)
WO2018098367A1 (en) * 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Inhibitors of interleukin-1 receptor-associated kinases and uses thereof
US11285158B2 (en) 2017-02-28 2022-03-29 The General Hospital Corporation Uses of pyrimidopyrimidinones as SIK inhibitors
US12133896B2 (en) 2017-03-23 2024-11-05 Kaohsiung Medical University Methods for treating or alleviating a bone-loss related disease or condition by administering a nucleic acid encoding a discoidin domain receptor 1 (DDR1) protein
TWI676482B (zh) 2017-03-23 2019-11-11 高雄醫學大學 盤基蛋白結構域受體1的抑制劑及活化劑及其用途
EP3787629A4 (en) 2018-05-02 2022-01-05 Kinnate Biopharma Inc. CYCLINE-DEPENDENT KINASE INHIBITORS
JP7590185B2 (ja) 2018-06-25 2024-11-26 ダナ-ファーバー キャンサー インスティテュート, インコーポレイテッド Taireファミリーキナーゼインヒビターおよびそれらの使用
EP3813819A4 (en) * 2018-06-29 2022-08-17 Kinnate Biopharma Inc. CYCLIN-DEPENDENT KINASE INHIBITORS
AU2019362788A1 (en) * 2018-10-15 2021-04-15 Dana-Farber Cancer Institute, Inc. Transcriptional enhanced associate domain (TEAD) transcription factor inhibitors and uses thereof
CN109303782A (zh) * 2018-10-24 2019-02-05 厦门大学 Jnk-in-8在制备干性年龄相关性黄斑变性的神经保护剂中的应用
CA3115126A1 (en) * 2018-12-14 2020-06-18 Nathanael S. Gray Pyrazolopyridine inhibitors of c-jun-n-terminal kinases and uses thereof
AU2019413694B2 (en) 2018-12-28 2025-03-20 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 and uses thereof
IL293735A (en) * 2019-12-24 2022-08-01 Dana Farber Cancer Inst Inc Inhibitors of transcription factor enhanced transcription partner region and their uses
CN113603695B (zh) * 2021-08-05 2022-06-14 青岛恒宁生物科技有限公司 一种取代的嘧啶胺类化合物或其作为农药可接受的盐、组合物及其用途
WO2024105420A2 (en) 2022-11-15 2024-05-23 Természettudományi Kutatóközpont Cyclic designer scaffolds for the covalent targeting of proteins via michael addition

Family Cites Families (285)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB796524A (en) * 1956-03-21 1958-06-11 Hickson & Welch Ltd Improvements in or relating to optical whitening agents
US4231938A (en) 1979-06-15 1980-11-04 Merck & Co., Inc. Hypocholesteremic fermentation products and process of preparation
US4270537A (en) 1979-11-19 1981-06-02 Romaine Richard A Automatic hypodermic syringe
AU570021B2 (en) 1982-11-22 1988-03-03 Novartis Ag Analogs of mevalolactone
US4828991A (en) 1984-01-31 1989-05-09 Akzo N.V. Tumor specific monoclonal antibodies
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
CA1283827C (en) 1986-12-18 1991-05-07 Giorgio Cirelli Appliance for injection of liquid formulations
GB8704027D0 (en) 1987-02-20 1987-03-25 Owen Mumford Ltd Syringe needle combination
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US4940460A (en) 1987-06-19 1990-07-10 Bioject, Inc. Patient-fillable and non-invasive hypodermic injection device assembly
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US4782084A (en) 1987-06-29 1988-11-01 Merck & Co., Inc. HMG-COA reductase inhibitors
US4885314A (en) 1987-06-29 1989-12-05 Merck & Co., Inc. Novel HMG-CoA reductase inhibitors
US5339163A (en) 1988-03-16 1994-08-16 Canon Kabushiki Kaisha Automatic exposure control device using plural image plane detection areas
FR2638359A1 (fr) 1988-11-03 1990-05-04 Tino Dalto Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5420245A (en) 1990-04-18 1995-05-30 Board Of Regents, The University Of Texas Tetrapeptide-based inhibitors of farnesyl transferase
US5190521A (en) 1990-08-22 1993-03-02 Tecnol Medical Products, Inc. Apparatus and method for raising a skin wheal and anesthetizing skin
US5527288A (en) 1990-12-13 1996-06-18 Elan Medical Technologies Limited Intradermal drug delivery device and method for intradermal delivery of drugs
US5747469A (en) 1991-03-06 1998-05-05 Board Of Regents, The University Of Texas System Methods and compositions comprising DNA damaging agents and p53
GB9118204D0 (en) 1991-08-23 1991-10-09 Weston Terence E Needle-less injector
SE9102652D0 (sv) 1991-09-13 1991-09-13 Kabi Pharmacia Ab Injection needle arrangement
US5328483A (en) 1992-02-27 1994-07-12 Jacoby Richard M Intradermal injection device with medication and needle guard
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US5569189A (en) 1992-09-28 1996-10-29 Equidyne Systems, Inc. hypodermic jet injector
US5334144A (en) 1992-10-30 1994-08-02 Becton, Dickinson And Company Single use disposable needleless injector
EP0604181A1 (en) 1992-12-21 1994-06-29 Eli Lilly And Company Antitumor compositions and method of treatment
WO1994019357A1 (en) 1993-02-23 1994-09-01 Merrell Dow Pharmaceuticals Inc. Farnesyl:protein transferase inhibitors as anticancer agents
CA2118985A1 (en) 1993-04-02 1994-10-03 Dinesh V. Patel Heterocyclic inhibitors of farnesyl protein transferase
EP0698015A1 (en) 1993-05-14 1996-02-28 Genentech, Inc. Preparation of n-cyanodithioimino-carbonates and 3-mercapto-5-amino-1h-1,2,4-triazole
US5602098A (en) 1993-05-18 1997-02-11 University Of Pittsburgh Inhibition of farnesyltransferase
US5571902A (en) 1993-07-29 1996-11-05 Isis Pharmaceuticals, Inc. Synthesis of oligonucleotides
WO1995008542A1 (en) 1993-09-22 1995-03-30 Kyowa Hakko Kogyo Co., Ltd. Farnesyltransferase inhibitor
US5721236A (en) 1993-10-15 1998-02-24 Schering Corporation Tricyclic carbamate compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
IL111235A (en) 1993-10-15 2001-03-19 Schering Plough Corp Medicinal preparations for inhibiting protein G activity and for the treatment of malignant diseases, containing tricyclic compounds, some such new compounds and a process for the preparation of some of them
US5661152A (en) 1993-10-15 1997-08-26 Schering Corporation Tricyclic sulfonamide compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US5719148A (en) 1993-10-15 1998-02-17 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
IL111257A0 (en) 1993-10-15 1994-12-29 Schering Corp Tricyclic sulfonamide compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
ATE210652T1 (de) 1993-10-15 2001-12-15 Schering Corp Tricyclische carbamat-derivate zur inhibierung der g-protein funktion und für die behandlung von proliferativen erkrankungen
AU682906B2 (en) 1993-10-25 1997-10-23 Parke, Davis & Company Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase
CA2152822A1 (en) 1993-11-04 1995-05-11 William R. Baker Cyclobutane derivatives as inhibitors of squalene synthetase and protein farnesyltransferase
US5783593A (en) 1993-11-04 1998-07-21 Abbott Laboratories Inhibitors of squalene synthetase and protein farnesyltransferase
EP0730605A1 (en) 1993-11-05 1996-09-11 Warner-Lambert Company Substituted di- and tripeptide inhibitors of protein:farnesyl transferase
US5484799A (en) 1993-12-09 1996-01-16 Abbott Laboratories Antifungal dorrigocin derivatives
WO1995024176A1 (en) 1994-03-07 1995-09-14 Bioject, Inc. Ampule filling device
US5466220A (en) 1994-03-08 1995-11-14 Bioject, Inc. Drug vial mixing and transfer device
FI963597L (fi) 1994-03-15 1996-11-14 Eisai Co Ltd Isoprenyylitransferaasi-inhibiittoreita
US6312699B1 (en) 1994-03-28 2001-11-06 Uab Research Foundation Ligands added to adenovirus fiber
HUT72440A (en) 1994-03-31 1996-04-29 Bristol Myers Squibb Co Imidazole-containing inhibitors of farnesyl protein transferase and pharmaceutical compositions containing them
US5523430A (en) 1994-04-14 1996-06-04 Bristol-Myers Squibb Company Protein farnesyl transferase inhibitors
US5510510A (en) 1994-05-10 1996-04-23 Bristol-Meyers Squibb Company Inhibitors of farnesyl protein transferase
US5563255A (en) 1994-05-31 1996-10-08 Isis Pharmaceuticals, Inc. Antisense oligonucleotide modulation of raf gene expression
TW365602B (en) 1994-06-10 1999-08-01 Rhone Poulenc Rorer Sa New farnesyl transferase inhibitors, their preparation and the pharmaceutical compositions which contain them
US5571792A (en) 1994-06-30 1996-11-05 Warner-Lambert Company Histidine and homohistidine derivatives as inhibitors of protein farnesyltransferase
WO1996005168A1 (en) 1994-08-11 1996-02-22 Banyu Pharmaceutical Co., Ltd. Substituted amide derivative
CA2155448A1 (en) 1994-08-11 1996-02-12 Katerina Leftheris Inhibitors of farnesyl protein transferase
EP0805154A1 (en) 1994-08-12 1997-11-05 Banyu Pharmaceutical Co., Ltd. N,n-disubstituted amic acid derivative
DE4429506B4 (de) 1994-08-19 2007-09-13 Degussa Gmbh Verfahren zur Extraktion natürlicher Carotinoid-Farbstoffe
WO1996017861A1 (en) 1994-12-09 1996-06-13 Warner-Lambert Company Substituted tetra- and pentapeptide inhibitors of protein:farnesyl transferase
US5599302A (en) 1995-01-09 1997-02-04 Medi-Ject Corporation Medical injection system and method, gas spring thereof and launching device using gas spring
WO1996021456A1 (en) 1995-01-12 1996-07-18 University Of Pittsburgh Inhibitors of prenyl transferases
FR2729390A1 (fr) 1995-01-18 1996-07-19 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2730491B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2730492B1 (fr) 1995-02-09 1997-03-14 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
US5684013A (en) 1995-03-24 1997-11-04 Schering Corporation Tricyclic compounds useful for inhibition of g-protein function and for treatment of proliferative diseases
US5700806A (en) 1995-03-24 1997-12-23 Schering Corporation Tricyclic amide and urea compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
IL117580A0 (en) 1995-03-29 1996-07-23 Merck & Co Inc Inhibitors of farnesyl-protein transferase and pharmaceutical compositions containing them
EP0820452B1 (en) 1995-04-07 2003-06-04 Schering Corporation Carbonyl-piperazinyl and piperidinil compounds which inhibit farnesyl protein transferase
US5891872A (en) 1995-04-07 1999-04-06 Schering Corporation Tricyclic compounds
IL117798A (en) 1995-04-07 2001-11-25 Schering Plough Corp Tricyclic compounds useful for inhibiting the function of protein - G and for the treatment of malignant diseases, and pharmaceutical preparations containing them
US5712280A (en) 1995-04-07 1998-01-27 Schering Corporation Tricyclic compounds useful for inhibition of G-protein function and for treatment of proliferative diseases
US5831115A (en) 1995-04-21 1998-11-03 Abbott Laboratories Inhibitors of squalene synthase and protein farnesyltransferase
IL118101A0 (en) 1995-05-03 1996-09-12 Abbott Lab Inhibitors of farnesyltransferase
US5730723A (en) 1995-10-10 1998-03-24 Visionary Medical Products Corporation, Inc. Gas pressured needle-less injection device and method
US5919780A (en) 1995-06-16 1999-07-06 Warner Lambert Company Tricyclic inhibitors of protein farnesyltransferase
FR2736641B1 (fr) 1995-07-10 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
FR2736638B1 (fr) 1995-07-12 1997-08-22 Rhone Poulenc Rorer Sa Nouveaux inhibiteurs de farnesyl transferase, leur preparation et les compositions pharmaceutiques qui les contiennent
CH690163A5 (fr) 1995-07-28 2000-05-31 Symphar Sa Dérivés gem-diphosphonates substitués utiles en tant qu'agents anti-cancers.
DE69627195T2 (de) 1995-11-01 2004-01-29 Novartis Ag Purinderivate und verfahren zu ihrer herstellung
DK0873123T3 (da) 1995-11-06 2003-08-04 Univ Pittsburgh Inhibitorer af protein-isoprenyltransferaser
WO1997018813A1 (en) 1995-11-22 1997-05-29 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
SK283335B6 (sk) 1995-12-08 2003-06-03 Janssen Pharmaceutica N. V. (Imidazol-5-yl)metyl-2-chinolinónové deriváty, spôsob a medziprodukty na ich prípravu, ich použitie a farmaceutické kompozície na ich báze
MY119007A (en) 1995-12-22 2005-03-31 Schering Corp Tricyclic amides useful for inhibition of g-protein function and for treatment of proliferative diseases.
US5893397A (en) 1996-01-12 1999-04-13 Bioject Inc. Medication vial/syringe liquid-transfer apparatus
AU1529997A (en) 1996-01-16 1997-08-11 Warner-Lambert Company Substituted histidine inhibitors of protein farnesyltransferase
US6673927B2 (en) 1996-02-16 2004-01-06 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Farnesyl transferase inhibitors
EP0944388A4 (en) 1996-04-03 2001-08-16 Merck & Co Inc INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
GB9607549D0 (en) 1996-04-11 1996-06-12 Weston Medical Ltd Spring-powered dispensing device
IL126833A0 (en) 1996-05-22 1999-08-17 Warner Lambert Co Inhibitors of protein farnesyl transferase
EP0918771A4 (en) 1996-07-15 2001-02-07 Bristol Myers Squibb Co THIADIOXOBENZODIAZEPINES FOR USE AS FARNESYL PROTEIN TRANSFERASE INHIBITORS
US5866702A (en) 1996-08-02 1999-02-02 Cv Therapeutics, Incorporation Purine inhibitors of cyclin dependent kinase 2
EP1003374A4 (en) 1996-12-30 2000-05-31 Merck & Co Inc INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
EP0951285A1 (en) 1996-12-30 1999-10-27 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5993412A (en) 1997-05-19 1999-11-30 Bioject, Inc. Injection apparatus
IT1298087B1 (it) 1998-01-08 1999-12-20 Fiderm S R L Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni
US6214852B1 (en) 1998-10-21 2001-04-10 Bristol-Myers Squibb Company N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
WO2000044777A1 (en) 1999-01-29 2000-08-03 Imclone Systems Incorporated Antibodies specific to kdr and uses thereof
GB9903762D0 (en) 1999-02-18 1999-04-14 Novartis Ag Organic compounds
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
EP1187633A4 (en) 1999-04-08 2005-05-11 Arch Dev Corp USE OF ANTI-VEGF ANTIBODIES TO ENHANCE RADIATION IN ANTICANCER THERAPY
BR0011571A (pt) 1999-06-24 2002-03-05 Smithkline Beecham Corp Antagonistas do receptor de limpeza de macrófago
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
CO5190714A1 (es) 1999-07-20 2002-08-29 Smithkline Beecham Corp Inhibidores del transporte de fosfato
IL148718A0 (en) 1999-09-17 2002-09-12 Abbott Gmbh & Co Kg Pyrazolopyrimidines as therapeutic agents
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
WO2001060157A2 (en) 2000-02-18 2001-08-23 The Procter & Gamble Company Antibacterial agents and compositions
US20090124690A1 (en) 2000-04-03 2009-05-14 Alberte Randall S Generation of Combinatorial Synthetic Libraries and Screening for Novel Proadhesins and Nonadhesins
KR100904157B1 (ko) 2000-08-10 2009-06-23 파마시아 이탈리아 에스.피.에이. 키나제 억제제로서 활성인 비사이클로-피라졸, 이의제조방법 및 이를 포함하는 약제학적 조성물
ATE426603T1 (de) 2000-10-31 2009-04-15 Aventis Pharma Inc Acyl- und sulfonylderivative 6,9- disubstitutierter 2-(trans-1,4-diaminocyclohexyl)-purine und ihre verwendung als antiproliferative mittel
US7429599B2 (en) * 2000-12-06 2008-09-30 Signal Pharmaceuticals, Llc Methods for treating or preventing an inflammatory or metabolic condition or inhibiting JNK
HUP0400639A3 (en) 2000-12-21 2010-03-29 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them
FR2818642B1 (fr) 2000-12-26 2005-07-15 Hoechst Marion Roussel Inc Nouveaux derives de la purine, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilistion
MXPA03008560A (es) 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
EP1373257B9 (en) * 2001-03-29 2008-10-15 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
EP1401469A2 (en) * 2001-04-09 2004-03-31 Lorantis Limited Therapeutic use and identification of modulators of a hedgehog signalling pathway or one of its target pathways
US6881737B2 (en) 2001-04-11 2005-04-19 Amgen Inc. Substituted triazinyl acrylamide derivatives and methods of use
JP4523271B2 (ja) 2001-06-01 2010-08-11 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼのインヒビターとして有用なチアゾール化合物
US6825190B2 (en) 2001-06-15 2004-11-30 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof
CA2453381A1 (en) 2001-07-10 2003-01-23 Massachusetts Institute Of Technology Methods for ex vivo propagation of somatic stem cells
US6939874B2 (en) 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
WO2003026665A1 (en) * 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4-(5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, src kinase inhibitors
WO2003051847A1 (en) 2001-12-19 2003-06-26 Smithkline Beecham P.L.C. (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors
FR2836915B1 (fr) 2002-03-11 2008-01-11 Aventis Pharma Sa Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant
AU2003231231A1 (en) 2002-05-06 2003-11-11 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
EP1506176B1 (en) 2002-05-17 2013-04-24 Pfizer Italia S.r.l. Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
WO2004005283A1 (en) 2002-07-09 2004-01-15 Vertex Pharmaceuticals Incorporated Imidazoles, oxazoles and thiazoles with protein kinase inhibiting activities
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
GB0217757D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Novel compounds
DE10239042A1 (de) 2002-08-21 2004-03-04 Schering Ag Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel
EP1537116B1 (en) 2002-09-04 2010-06-02 Schering Corporation Pyrazolopyrimidines suitable for the treatment of cancer diseases
CN1701073B (zh) 2002-09-04 2011-06-22 先灵公司 作为细胞周期蛋白依赖激酶抑制剂的吡唑并[1,5-a]嘧啶
US7205308B2 (en) 2002-09-04 2007-04-17 Schering Corporation Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
US7119200B2 (en) 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
CN100376580C (zh) 2002-09-04 2008-03-26 先灵公司 作为细胞周期蛋白依赖性激酶抑制剂的吡唑并嘧啶
GB0222514D0 (en) 2002-09-27 2002-11-06 Novartis Ag Organic compounds
WO2004032869A2 (en) 2002-10-08 2004-04-22 The Government Of The Usa As Represented By The Secretary Of The Dept. Of Health And Human Services Identification of anti-hiv compounds inhibiting virus assembly and binding of nucleocapsid protein to nucleic acid
US20050250837A1 (en) 2002-10-18 2005-11-10 D Mello Santosh R Use of C-Raf inhibitors for the treatment of neurodegenerative diseases
AU2003278088A1 (en) 2002-10-28 2004-05-25 Bayer Healthcare Ag Heteroaryloxy-substituted phenylaminopyrimidines as rho-kinase inhibitors
UA81790C2 (uk) 2002-12-19 2008-02-11 Фармация Италия С.П.А. Заміщені піролопіразольні похідні як інгібітори кінази
FR2850022B1 (fr) * 2003-01-22 2006-09-08 Centre Nat Rech Scient Nouvelle utilisation de la mifepristone et de ses derives comme modulateurs de la voie de signalisation des proteines hedgehog et ses applications
ATE479667T1 (de) 2003-02-06 2010-09-15 Bristol Myers Squibb Co Als kinaseinhibitoren geeignete verbindungen auf thiazolylbasis
EP1597256A1 (en) 2003-02-21 2005-11-23 Pfizer Inc. N-heterocyclyl-substituted amino-thiazole derivatives as protein kinase inhibitors
EP1599482A4 (en) 2003-02-28 2008-10-01 Teijin Pharma Ltd PYRAZOLO1,5-A PYRIMIDINE DERIVATIVES
GB0304665D0 (en) 2003-02-28 2003-04-02 Teijin Ltd Compounds
GB0305142D0 (en) 2003-03-06 2003-04-09 Eisai London Res Lab Ltd Synthesis
GB0305559D0 (en) 2003-03-11 2003-04-16 Teijin Ltd Compounds
DE602004014117D1 (de) 2003-03-25 2008-07-10 Vertex Pharma Thiazole zur verwendung als inhibitoren von protein-kinasen
EP1608652A1 (en) 2003-03-31 2005-12-28 Vernalis (Cambridge) Limited Pyrazolopyrimidine compounds and their use in medicine
US7244763B2 (en) 2003-04-17 2007-07-17 Warner Lambert Company Llc Compounds that modulate PPAR activity and methods of preparation
US20050008640A1 (en) 2003-04-23 2005-01-13 Wendy Waegell Method of treating transplant rejection
US20040235892A1 (en) 2003-05-22 2004-11-25 Yujia Dai Indazole and benzisoxazole kinase inhibitors
CN1826324B (zh) 2003-05-22 2011-12-07 雅培制药有限公司 吲唑、苯并异*唑和苯并异噻唑激酶抑制剂
SE0301906D0 (sv) 2003-06-26 2003-06-26 Astrazeneca Ab New compounds
NZ544756A (en) 2003-07-22 2009-09-25 Astex Therapeutics Ltd 3,4-Disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators
US7442698B2 (en) 2003-07-24 2008-10-28 Amgen Inc. Substituted heterocyclic compounds and methods of use
BRPI0413005A (pt) 2003-07-29 2006-09-26 Irm Llc compostos e composições como inibidores da proteìna cinase
BR122019017579B8 (pt) 2003-08-15 2021-07-27 Novartis Ag 2,4-pirimidinadiaminas, seus usos, combinação e composição farmacêutica
US20050130974A1 (en) 2003-10-17 2005-06-16 Rigel Pharmaceuticals, Inc. Benzothiazole compositions and their use as ubiquitin ligase inhibitors
WO2005037797A1 (en) 2003-10-21 2005-04-28 Pharmacia Corporation Substituted pyrazole urea compounds for the treatment of inflammation
CA2545711A1 (en) 2003-11-13 2005-06-02 Ambit Biosciences Corporation Urea derivatives as kinase modulators
DE10357510A1 (de) 2003-12-09 2005-07-07 Bayer Healthcare Ag Heteroarylsubstituierte Benzole
BRPI0418031A (pt) 2003-12-22 2007-04-17 Gilead Sciences Inc inibidores de quinase fosfonato-substituìdos
CN1960995B (zh) 2004-04-02 2010-12-08 诺瓦提斯公司 作为葡糖激酶活化剂、可用于治疗ⅱ型糖尿病的磺酰胺-噻唑并吡啶衍生物
DE102004017438A1 (de) 2004-04-08 2005-11-03 Bayer Healthcare Ag Hetaryloxy-substituierte Phenylaminopyrimidine
DE102004020570A1 (de) 2004-04-27 2005-11-24 Bayer Healthcare Ag Substituierte Phenylaminopyrimidine
GB0411791D0 (en) * 2004-05-26 2004-06-30 Cyclacel Ltd Compounds
FR2871158A1 (fr) 2004-06-04 2005-12-09 Aventis Pharma Sa Indazoles substitues, compositions les contenant, procede de fabrication et utilisation
CN1960988B (zh) 2004-06-10 2012-01-25 Irm责任有限公司 作为蛋白激酶抑制剂的化合物和组合物
DE102004028862A1 (de) 2004-06-15 2005-12-29 Merck Patent Gmbh 3-Aminoindazole
EP1789399A1 (en) 2004-08-31 2007-05-30 AstraZeneca AB Quinazolinone derivatives and their use as b-raf inhibitors
US20060100226A1 (en) * 2004-09-10 2006-05-11 Sikorski James A 2-Thiopyrimidinones as therapeutic agents
WO2006034341A2 (en) 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Pyridazine derivatives for inhibiting human stearoyl-coa-desaturase
MX2007004480A (es) 2004-10-15 2007-05-08 Astrazeneca Ab Quinoxalinas como inhibidores b raf.
US7632854B2 (en) 2004-11-17 2009-12-15 Pfizer Italia S.R.L. Aminoindazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
AU2005322855B2 (en) 2004-12-30 2012-09-20 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
CN101106990B (zh) 2005-01-26 2010-12-08 Irm责任有限公司 用作蛋白激酶抑制剂的化合物和组合物
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
US20090156582A1 (en) 2005-02-09 2009-06-18 Tetsuya Tsukamoto Pyrazole Compound
US7511077B2 (en) 2005-02-09 2009-03-31 Neuromed Pharmaceuticals Ltd. Diamine calcium channel blockers
WO2006124731A2 (en) 2005-05-12 2006-11-23 Irm Llc Compounds and compositions as protein kinase inhibitors
AU2006247322A1 (en) 2005-05-16 2006-11-23 Irm Llc Pyrrolopyridine derivatives as protein kinase inhibitors
PL2395004T3 (pl) 2005-06-22 2016-08-31 Plexxikon Inc Pochodne pirolo[2,3-b]pirydyny jako inhibitory kinazy białkowej
AU2006283592A1 (en) 2005-08-22 2007-03-01 Amgen Inc. Pyrazolopyridine and pyrazolopyrimidine compounds useful as kinase enzymes modulators
US7880004B2 (en) 2005-09-15 2011-02-01 Bristol-Myers Squibb Company Met kinase inhibitors
GT200600429A (es) 2005-09-30 2007-04-30 Compuestos organicos
AU2006295645B2 (en) 2005-09-30 2011-09-29 Msd K.K. 2-heteroaryl-substituted indole derivative
GB0520955D0 (en) 2005-10-14 2005-11-23 Cyclacel Ltd Compound
US8247556B2 (en) 2005-10-21 2012-08-21 Amgen Inc. Method for preparing 6-substituted-7-aza-indoles
MEP0808A (xx) 2005-12-21 2010-02-10 Pfizer Prod Inc Karbonilamino pirolopirayoli, snažni inhibitori kinaza
JP5200939B2 (ja) 2005-12-23 2013-06-05 アリアド・ファーマシューティカルズ・インコーポレイテッド 二環式ヘテロアリール化合物
WO2007129195A2 (en) 2006-05-04 2007-11-15 Pfizer Products Inc. 4-pyrimidine-5-amino-pyrazole compounds
KR20090019796A (ko) 2006-05-22 2009-02-25 쉐링 코포레이션 CDK 억제제로서의 피라졸로[1,5-a]피리미딘
JP2009538352A (ja) 2006-05-26 2009-11-05 アストラゼネカ アクチボラグ 細胞増殖を阻害するための薬剤としての2−カルボシクロアミノ−4−イミダゾリルピリミジン類
EA018573B1 (ru) 2006-09-22 2013-09-30 Фармасайкликс, Инк. Ингибиторы тирозинкиназы брутона
EP2089394B1 (en) 2006-10-11 2011-06-29 Nerviano Medical Sciences S.r.l. Substituted pyrrolo-pyrazole derivatives as kinase inhibitors
WO2008049856A2 (en) 2006-10-25 2008-05-02 Ingenium Pharmaceuticals Gmbh Methods of treating pain using cdk inhibitors
WO2008054827A2 (en) 2006-11-03 2008-05-08 Pharmacyclics, Inc. Bruton's tyrosine kinase activity probe and method of using
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
JP5179509B2 (ja) * 2006-12-08 2013-04-10 エフ.ホフマン−ラ ロシュ アーゲー 置換ピリミジン類及びjnkモジュレーターとしてのこれらの使用
ES2509820T3 (es) 2006-12-20 2014-10-20 Nerviano Medical Sciences S.R.L. Derivados de indazol como inhibidores de la cinasa para el tratamiento del cáncer
US7872018B2 (en) 2006-12-21 2011-01-18 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
US20090016990A1 (en) 2007-01-24 2009-01-15 Alberte Randall S Antimicrobial Compositions
JP5161245B2 (ja) 2007-02-07 2013-03-13 ファイザー・インク PKC阻害剤としての3−アミノ−ピロロ[3,4−c]ピラゾール−5(1H,4H,6H)カルボアルデヒド誘導体
JP5577104B2 (ja) * 2007-03-14 2014-08-20 エクセリクシス パテント カンパニー エルエルシー ヘッジホッグ経路の阻害剤
WO2008124393A1 (en) 2007-04-04 2008-10-16 Irm Llc Benzothiazole derivatives and their use as protein kinase inhibitors
CA2683695C (en) 2007-04-12 2013-06-18 Pfizer Inc. 3-amido-pyrrolo[3,4-c]pyrazole-5(1h,4h,6h) carbaldehyde derivatives
WO2008144253A1 (en) 2007-05-14 2008-11-27 Irm Llc Protein kinase inhibitors and methods for using thereof
EP2152079A4 (en) * 2007-06-04 2011-03-09 Avila Therapeutics Inc HETEROCYCLIC COMPOUNDS AND USES THEREOF
WO2008151304A1 (en) 2007-06-05 2008-12-11 Emory University Selective inhibitors for cyclin-dependent kinases
US20100240656A1 (en) 2007-07-12 2010-09-23 Oryzon Genomics, S.A. Compounds as hsp90 inhibitors
ES2401557T3 (es) 2007-08-02 2013-04-22 Amgen, Inc Moduladores de Pl3 cinasas y métodos de uso
US20090054392A1 (en) 2007-08-20 2009-02-26 Wyeth Naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analogs and their use as agonists of the wnt-beta-catenin cellular messaging system
WO2009032694A1 (en) 2007-08-28 2009-03-12 Dana Farber Cancer Institute Amino substituted pyrimidine, pyrollopyridine and pyrazolopyrimidine derivatives useful as kinase inhibitors and in treating proliferative disorders and diseases associated with angiogenesis
WO2009028655A1 (ja) 2007-08-30 2009-03-05 Takeda Pharmaceutical Company Limited 複素環化合物およびその用途
GB0719366D0 (en) 2007-10-03 2007-11-14 Smithkline Beecham Corp Compounds
WO2009122180A1 (en) 2008-04-02 2009-10-08 Medical Research Council Pyrimidine derivatives capable of inhibiting one or more kinases
GB0806419D0 (en) 2008-04-09 2008-05-14 Ineos Fluor Holdings Ltd Process
US20100197688A1 (en) 2008-05-29 2010-08-05 Nantermet Philippe G Epha4 rtk inhibitors for treatment of neurological and neurodegenerative disorders and cancer
EP2300481B1 (en) 2008-05-30 2015-09-30 Merck Sharp & Dohme Corp. Novel substituted azabenzoxazoles
TWI490214B (zh) 2008-05-30 2015-07-01 艾德克 上野股份有限公司 苯或噻吩衍生物及該等作為vap-1抑制劑之用途
WO2009152027A1 (en) 2008-06-12 2009-12-17 Merck & Co., Inc. 5,7-dihydro-6h-pyrrolo[2,3-d]pyrimidin-6-one derivatives for mark inhibition
WO2009155527A2 (en) 2008-06-19 2009-12-23 Progenics Pharmaceuticals, Inc. Phosphatidylinositol 3 kinase inhibitors
EP2311842A3 (en) 2008-06-24 2011-07-13 Takeda Pharmaceutical Company Limited PI3K/M TOR inhibitors
JP2010030970A (ja) 2008-07-31 2010-02-12 Bayer Cropscience Ag 殺虫性ベンゼンジカルボキサミド誘導体
WO2010017047A1 (en) 2008-08-05 2010-02-11 Merck & Co., Inc. Therapeutic compounds
MY156789A (en) 2008-09-05 2016-03-31 Celgene Avilomics Res Inc Algorithm for designing irreversible inhibitors
US8394818B2 (en) 2008-10-17 2013-03-12 Dana-Farber Cancer Institute, Inc. Soluble mTOR complexes and modulators thereof
CN101723936B (zh) 2008-10-27 2014-01-15 上海睿星基因技术有限公司 激酶抑制剂及其在药学中的用途
KR20110120286A (ko) 2009-02-12 2011-11-03 아스텔라스세이야쿠 가부시키가이샤 헤테로환 유도체
DK3366686T3 (da) 2009-03-20 2020-11-23 Metabasis Therapeutics Inc Inhibitorer af diacylglycerol-o-acyltransferase 1 (dgat-1) og anvendelser deraf
WO2010120386A1 (en) 2009-04-17 2010-10-21 Nektar Therapeutics Oligomer-protein tyrosine kinase inhibitor conjugates
JPWO2010125799A1 (ja) 2009-04-27 2012-10-25 塩野義製薬株式会社 Pi3k阻害活性を有するウレア誘導体
JP5918693B2 (ja) 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド Egfr阻害剤及び疾患の治療方法
WO2010138652A1 (en) 2009-05-27 2010-12-02 Ptc Therapeutics, Inc. Methods for treating kaposi sarcoma
WO2010138695A1 (en) 2009-05-27 2010-12-02 Ptc Therapeutics, Inc. Methods for treating neurofibromatosis
WO2010138659A1 (en) 2009-05-27 2010-12-02 Ptc Therapeutics, Inc. Methods for treating brain tumors
MX373926B (es) 2009-05-27 2020-07-10 Ptc Therapeutics Inc Metodos para tratar cancer y estados no neoplasicos.
US8703726B2 (en) 2009-05-27 2014-04-22 Ptc Therapeutics, Inc. Methods for treating prostate conditions
US20120202801A1 (en) 2009-05-27 2012-08-09 Liangxian Cao Methods for treating breast cancer
WO2010144416A1 (en) 2009-06-08 2010-12-16 Gaeta Federico C A SUBSTITUTED PYRAZOLO [1,5-a] PYRIDINE COMPOUNDS HAVING MULTI-TARGET ACTIVITY
WO2010144909A1 (en) 2009-06-12 2010-12-16 Novartis Ag Fused heterocyclic compounds and their uses
FR2948367A1 (fr) * 2009-07-24 2011-01-28 Centre Nat Rech Scient Derives d'acyl-guanidines modulateurs de la voie de signalisation des proteines hedgehog
IN2012DN02534A (enExample) 2009-09-16 2015-08-28 Avila Therapeutics Inc
US8586584B2 (en) 2009-10-14 2013-11-19 Bristol-Myers Squibb Company Compounds for the treatment of hepatitis C
WO2011079231A1 (en) 2009-12-23 2011-06-30 Gatekeeper Pharmaceutical, Inc. Compounds that modulate egfr activity and methods for treating or preventing conditions therewith
US9180127B2 (en) 2009-12-29 2015-11-10 Dana-Farber Cancer Institute, Inc. Type II Raf kinase inhibitors
CN103080093A (zh) 2010-03-16 2013-05-01 达纳-法伯癌症研究所公司 吲唑化合物及其应用
US8981083B2 (en) 2010-05-14 2015-03-17 Dana Farber Cancer Institute, Inc. Compositions and methods for treating neoplasia, inflammatory disease and other disorders
CA2817785A1 (en) 2010-11-19 2012-05-24 Toby Blench Pyrazolopyridines and pyrazolopyridines and their use as tyk2 inhibitors
US8546443B2 (en) 2010-12-21 2013-10-01 Boehringer Ingelheim International Gmbh Benzylic oxindole pyrimidines
CN103781780B (zh) 2011-07-28 2015-11-25 赛尔佐姆有限公司 作为jak抑制剂的杂环基嘧啶类似物
WO2013040436A2 (en) 2011-09-16 2013-03-21 The Regents Of The University Of Michgian Esx-mediated transcription modulators and related methods
CA2856291C (en) 2011-11-17 2020-08-11 Dana-Farber Cancer Institute, Inc. Inhibitors of c-jun-n-terminal kinase (jnk)
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
US9879003B2 (en) 2012-04-11 2018-01-30 Dana-Farber Cancer Institute, Inc. Host targeted inhibitors of dengue virus and other viruses
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
CN103319483B (zh) 2012-10-19 2016-08-03 药源药物化学(上海)有限公司 一种利拉列汀重要中间体的制备方法
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
TWI621618B (zh) 2013-03-13 2018-04-21 比利時商健生藥品公司 經取代2-氮雜雙環類及其作為食慾素受體調控劑之用途
US9938279B2 (en) 2013-04-09 2018-04-10 Energenesis Biomedical Co., Ltd Method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK)
BR112016001457A2 (pt) 2013-07-25 2017-08-29 Dana Farber Cancer Inst Inc Inibidores de fatores de transcrição e usos dos mesmos
US10047070B2 (en) 2013-10-18 2018-08-14 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7)
AU2014337122B2 (en) 2013-10-18 2019-01-03 Dana-Farber Cancer Institute, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
KR20160111036A (ko) 2014-01-31 2016-09-23 다나-파버 캔서 인스티튜트 인크. 디아제판 유도체 및 그의 용도
WO2015117087A1 (en) 2014-01-31 2015-08-06 Dana-Farber Cancer Institute, Inc. Uses of diazepane derivatives
MX2016009974A (es) 2014-01-31 2016-10-31 Dana Farber Cancer Inst Inc Derivados de diaminopirimidina bencensulfona y sus usos.
US20160347750A1 (en) 2014-01-31 2016-12-01 Dana-Farber Cancer Institute, Inc. Dihydropteridinone derivatives and uses thereof
LT3126352T (lt) 2014-04-04 2019-01-10 Syros Pharmaceuticals, Inc. Nuo ciklino priklausomos kinazės 7 (cdk7) inhibitoriai
US10336760B2 (en) 2014-04-05 2019-07-02 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
CN104829610B (zh) 2014-06-20 2017-03-15 中国科学院合肥物质科学研究院 一种新型布鲁顿酪氨酸激酶抑制剂
EP3172213B1 (en) 2014-07-21 2021-09-22 Dana-Farber Cancer Institute, Inc. Macrocyclic kinase inhibitors and uses thereof
WO2016014542A1 (en) 2014-07-21 2016-01-28 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
AU2015300782B2 (en) 2014-08-08 2020-04-16 Dana-Farber Cancer Institute, Inc. Uses of salt-inducible kinase (SIK) inhibitors
WO2016058544A1 (en) 2014-10-16 2016-04-21 Syros Pharmaceuticals, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
EP3236959B1 (en) 2014-12-23 2025-09-24 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
CA2978170C (en) 2015-03-09 2024-02-27 Aurigene Discovery Technologies Limited Pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives as cdk inhibitors
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
US10702527B2 (en) 2015-06-12 2020-07-07 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
WO2017037576A1 (en) 2015-08-28 2017-03-09 Novartis Ag Pharmaceutical combinations comprising (a) the cyclin dependent kinase 4/6 (cdk4/6) inhibitor lee011 (=ribociclib), and (b) the epidermal growth factor receptor (egfr) inhibitor erlotinib, for the treatment or prevention of cancer
EP4019515A1 (en) 2015-09-09 2022-06-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases

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