SG11202003035SA - Use of p38 inhibitors to reduce expression of dux4 - Google Patents

Use of p38 inhibitors to reduce expression of dux4

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Publication number
SG11202003035SA
SG11202003035SA SG11202003035SA SG11202003035SA SG11202003035SA SG 11202003035S A SG11202003035S A SG 11202003035SA SG 11202003035S A SG11202003035S A SG 11202003035SA SG 11202003035S A SG11202003035S A SG 11202003035SA SG 11202003035S A SG11202003035S A SG 11202003035SA
Authority
SG
Singapore
Prior art keywords
dux4
inhibitors
reduce expression
expression
reduce
Prior art date
Application number
SG11202003035SA
Inventor
Angela Marie Cacace
Soto Luis Gustavo Alejandro Rojas
Lorin A Thompson
Owen Brendan Wallace
Lucienne Ronco
Ning Shen
Alan Scott Robertson
Aaron Nakwon Chang
Original Assignee
Fulcrum Therapeutics Inc
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 Fulcrum Therapeutics Inc filed Critical Fulcrum Therapeutics Inc
Publication of SG11202003035SA publication Critical patent/SG11202003035SA/en

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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
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SG11202003035SA 2017-10-05 2018-10-05 Use of p38 inhibitors to reduce expression of dux4 SG11202003035SA (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762568754P 2017-10-05 2017-10-05
US201762568673P 2017-10-05 2017-10-05
US201862682563P 2018-06-08 2018-06-08
US201862682565P 2018-06-08 2018-06-08
PCT/US2018/054638 WO2019071144A1 (en) 2017-10-05 2018-10-05 Use of p38 inhibitors to reduce expression of dux4

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SG11202003035SA true SG11202003035SA (en) 2020-04-29

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EP (3) EP3692144A1 (en)
JP (5) JP2021501130A (en)
KR (2) KR20200066655A (en)
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Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019071147A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce dux4 and downstream gene expression for the treatment of fshd
US20210038653A1 (en) * 2018-02-02 2021-02-11 Fred Hutchinson Cancer Research Center Methods for treating facioscapulohumeral muscular dystrophy
TW202112368A (en) 2019-06-13 2021-04-01 荷蘭商法西歐知識產權股份有限公司 Inhibitor combinations for treatment of diseases related to dux4 expression
WO2021105474A1 (en) 2019-11-29 2021-06-03 Facio Intellectual Property B.V. New compounds for treatment of diseases related to dux4 expression
WO2021105481A1 (en) 2019-11-29 2021-06-03 Facio Intellectual Property B.V. Novel compounds for treatment of diseases related to dux4 expression
CN111004802A (en) * 2019-12-31 2020-04-14 深圳市疾病预防控制中心（深圳市卫生检验中心、深圳市预防医学研究所） shRNA recombinant vector construction method for specifically inhibiting expression of p38MAPK gene and application thereof
WO2022056266A2 (en) 2020-09-11 2022-03-17 Arrowhead Pharmaceuticals, Inc. Rnai agents for inhibiting expression of dux4, compositions thereof, and methods of use
US20240342148A1 (en) * 2021-07-27 2024-10-17 Fulcrum Therapeutics, Inc. Methods of treating facioscapulohumeral muscular dystrophy with losmapimod
WO2024145662A1 (en) * 2022-12-30 2024-07-04 Altay Therapeutics, Inc. 2-substituted thiazole and benzothiazole compositions and methods as dux4 inhibitors

Family Cites Families (451)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5593992A (en) 1993-07-16 1997-01-14 Smithkline Beecham Corporation Compounds
US5670527A (en) 1993-07-16 1997-09-23 Smithkline Beecham Corporation Pyridyl imidazole compounds and compositions
US6369068B1 (en) 1995-06-07 2002-04-09 Smithkline Beecham Corporation Amino substituted pyrimidine containing compounds
IL118544A (en) 1995-06-07 2001-08-08 Smithkline Beecham Corp Imidazole derivatives, process for their preparation and pharmaceutical compositions comprising them
JP2001508395A (en) 1996-01-11 2001-06-26 スミスクライン・ビーチャム・コーポレイション New cycloalkyl-substituted imidazole
ZA97175B (en) 1996-01-11 1997-11-04 Smithkline Beecham Corp Novel substituted imidazole compounds.
AP9700912A0 (en) 1996-01-11 1997-01-31 Smithkline Beecham Corp Novel cycloalkyl substituted imidazoles
WO1997032583A1 (en) 1996-03-08 1997-09-12 Smithkline Beecham Corporation Use of csaidtm compounds as inhibitors of angiogenesis
JP2000510327A (en) 1996-03-12 2000-08-15 スミスクライン・ビーチャム・コーポレイション Methods for identifying pharmaceutically active compounds
WO1997033883A1 (en) 1996-03-13 1997-09-18 Smithkline Beecham Corporation Novel pyrimidine compounds useful in treating cytokine mediated diseases
US6235760B1 (en) 1996-03-25 2001-05-22 Smithkline Beecham Corporation Treatment for CNS injuries
US6096739A (en) 1996-03-25 2000-08-01 Smithkline Beecham Corporation Treatment for CNS injuries
WO1998007425A1 (en) 1996-08-21 1998-02-26 Smithkline Beecham Corporation Imidazole compounds, compositions and use
US6096753A (en) 1996-12-05 2000-08-01 Amgen Inc. Substituted pyrimidinone and pyridone compounds and methods of use
US6147080A (en) 1996-12-18 2000-11-14 Vertex Pharmaceuticals Incorporated Inhibitors of p38
WO1998028292A1 (en) 1996-12-23 1998-07-02 Smithkline Beecham Corporation Novel piperidine containing compounds
US5965583A (en) 1997-04-24 1999-10-12 Ortho-Mcneil Pharmaceutical, Inc. Substituted imidazoles useful in the treatment of inflammatory disease
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
AU7966198A (en) 1997-06-13 1998-12-30 Smithkline Beecham Corporation Novel pyrazole and pyrazoline substituted compounds
US6610695B1 (en) 1997-06-19 2003-08-26 Smithkline Beecham Corporation Aryloxy substituted pyrimidine imidazole compounds
US6093742A (en) 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
AR016294A1 (en) 1997-07-02 2001-07-04 Smithkline Beecham Corp IMIDAZOL SUBSTITUTE COMPOSITE, PHARMACEUTICAL COMPOSITION CONTAINING IT, ITS USE IN THE MANUFACTURE OF A MEDICINAL PRODUCT AND PROCEDURE FOR SUPREPARATION
TW517055B (en) 1997-07-02 2003-01-11 Smithkline Beecham Corp Novel substituted imidazole compounds
GB9721437D0 (en) 1997-10-10 1997-12-10 Glaxo Group Ltd Heteroaromatic compounds and their use in medicine
CN1279682A (en) 1997-10-20 2001-01-10 霍夫曼-拉罗奇有限公司 bicyclic kinase inhibitors
US6162613A (en) 1998-02-18 2000-12-19 Vertex Pharmaceuticals, Inc. Methods for designing inhibitors of serine/threonine-kinases and tyrosine kinases
EP1075467B1 (en) 1998-05-05 2005-03-30 F. Hoffmann-La Roche Ag Pyrazole derivatives as p-38 map kinase inhibitors
US6316466B1 (en) 1998-05-05 2001-11-13 Syntex (U.S.A.) Llc Pyrazole derivatives P-38 MAP kinase inhibitors
MY132496A (en) 1998-05-11 2007-10-31 Vertex Pharma Inhibitors of p38
US6867209B1 (en) 1998-05-22 2005-03-15 Scios, Inc. Indole-type derivatives as inhibitors of p38 kinase
NZ508790A (en) 1998-05-22 2003-10-31 Scios Inc Heterocyclic compounds and methods to treat cardiac failure and other disorders
US6448257B1 (en) 1998-05-22 2002-09-10 Scios, Inc. Compounds and methods to treat cardiac failure and other disorders
US6589954B1 (en) 1998-05-22 2003-07-08 Scios, Inc. Compounds and methods to treat cardiac failure and other disorders
US6340685B1 (en) 1998-05-22 2002-01-22 Scios, Inc. Compounds and methods to treat cardiac failure and other disorders
JP2002516322A (en) 1998-05-22 2002-06-04 スミスクライン・ビーチャム・コーポレイション New 2-alkyl-substituted imidazole compounds
JP2002517486A (en) 1998-06-12 2002-06-18 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 p38
EP1112070B1 (en) 1998-08-20 2004-05-12 Smithkline Beecham Corporation Novel substituted triazole compounds
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
JP2002526482A (en) 1998-09-18 2002-08-20 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 p38
EP1119254A4 (en) 1998-10-07 2004-05-12 Smithkline Beecham Corp Novel treatment for stroke management
DE69914357T2 (en) 1998-11-04 2004-11-11 Smithkline Beecham Corp. PYRIDIN-4-YL OR PYRIMIDIN-4-YL SUBSTITUTED PYRAZINE
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
AU765473B2 (en) 1999-04-23 2003-09-18 Takeda Pharmaceutical Company Limited 5-pyridyl-1,3-azole compounds, process for producing the same and use thereof
ATE376547T1 (en) 1999-05-21 2007-11-15 Scios Inc INDOLE-TYPE DERIVATIVES AS P38 KINASE INHIBITORS
ATE312823T1 (en) 1999-07-09 2005-12-15 Boehringer Ingelheim Pharma METHOD FOR PRODUCING HETEROARYL-SUBSTITUTED UREA COMPOUNDS
US6541477B2 (en) 1999-08-27 2003-04-01 Scios, Inc. Inhibitors of p38-a kinase
KR20020032591A (en) 1999-09-17 2002-05-03 스튜어트 알. 수터, 스티븐 베네티아너, 피터 존 기딩스 Use of CSAIDs in Rhinovirus Infection
JP3961830B2 (en) 1999-10-21 2007-08-22 エフ．ホフマン−ラ ロシュ アーゲー Heteroalkylamino-substituted bicyclic nitrogen heterocycles as inhibitors of p38 protein kinase
TR200201058T2 (en) 1999-10-21 2002-07-22 F.Hoffmann-La Roche Ag Bicyclic, nitrogenous heterocycles substituted with alkylamino as P38 protein kinase inhibitors
WO2001038312A1 (en) 1999-11-23 2001-05-31 Smithkline Beecham Corporation 3,4-DIHYDRO-(1H)QUINAZOLIN-2-ONE COMPOUNDS AS CSBP/p38 KINASE INHIBITORS
ES2241675T3 (en) 1999-11-23 2005-11-01 Smithkline Beecham Corporation 3,4-DIHIDRO- (1H) QUINAZOLIN-2-ONA COMPOUNDS AS CSPB / P38 QUINASA INHIBITORS.
JP2003517471A (en) 1999-11-23 2003-05-27 スミスクライン・ビーチャム・コーポレイション 3,4-dihydro- (1H) -quinazolin-2-one and its use as CSBP / p38 kinase inhibitors
AU1782301A (en) 1999-11-23 2001-06-04 Smithkline Beecham Corporation 3,4-dihydro-(1h)quinazolin-2-one compounds as csbp/p39 kinase inhibitors
AU2735201A (en) 1999-12-28 2001-07-09 Pharmacopeia, Inc. Pyrimidine and triazine kinase inhibitors
US6906067B2 (en) 1999-12-28 2005-06-14 Bristol-Myers Squibb Company N-heterocyclic inhibitors of TNF-α expression
AU2001241927A1 (en) 2000-02-28 2001-09-12 Scios Inc. Inhibitors of p38-alpha kinase
AR030053A1 (en) 2000-03-02 2003-08-13 Smithkline Beecham Corp 1H-PIRIMIDO [4,5-D] PIRIMIDIN-2-ONAS AND SALTS, PHARMACEUTICAL COMPOSITIONS, USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT AND PROCEDURE FOR PRODUCERS
US6565880B2 (en) 2000-07-24 2003-05-20 Boehringer Ingelheim Pharmaceuticals, Inc. Oral dosage formulations of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea
PE20020506A1 (en) 2000-08-22 2002-07-09 Glaxo Group Ltd PIRAZOLE DERIVATIVES FUSED AS PROTEIN KINASE INHIBITORS
CN1275964C (en) 2000-08-31 2006-09-20 霍夫曼-拉罗奇有限公司 7-oxo pyridopyrimidines as inhibitors of a cellular proliferation
MXPA03001733A (en) 2000-08-31 2003-05-27 Hoffmann La Roche 7-oxo pyridopyrimidines.
WO2002032862A2 (en) 2000-10-19 2002-04-25 Smithkline Beecham Corporation Use of p38 inhibitors for the treatment of smoke inhalation
AU2002248269A1 (en) 2000-10-19 2002-08-12 Smithkline Beecham Corporation Use of p38 inhibitors for the treatment of inflammation-enhanced cough
EP1333833B1 (en) 2000-10-23 2011-08-24 GlaxoSmithKline LLC Novel trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compound for the treatment of CSBP/p38 kinase mediated diseases
JP2004522713A (en) 2000-11-17 2004-07-29 ブリストル−マイヤーズ　スクイブ　カンパニー Method for treating p38 kinase-related diseases and pyrrolotriazine compounds useful as kinase inhibitors
CA2429258A1 (en) 2000-11-20 2002-06-13 Scios Inc. Piperidine/piperazine-type inhibitors of p38 kinase
CA2429382A1 (en) 2000-11-20 2002-06-06 Scios Inc. Indole-type inhibitors of p38 kinase
CA2429605A1 (en) 2000-11-20 2002-05-30 Scios Inc. Indol derivative and their use as inhibitors of p38 kinase
US20020165286A1 (en) 2000-12-08 2002-11-07 Hanne Hedeman Dermal anti-inflammatory composition
WO2002058695A1 (en) 2000-12-20 2002-08-01 Merck & Co., Inc. (halo-benzo carbonyl)heterocyclo fused phenyl p38 kinase inhibiting agents
WO2002064594A2 (en) 2001-02-12 2002-08-22 F. Hoffmann-La Roche Ag 6-substituted pyrido-pyrimidines
EP1370253B8 (en) 2001-02-28 2008-11-26 Temple University of the Commonwealth System of Higher Education Use of alpha, beta unsaturated aryl sulfones for protecting cells and tissues from ionizing radiation toxicity
ES2251582T3 (en) 2001-03-09 2006-05-01 Pfizer Products Inc. BENCIMIDAZOL ANTI-INFLAMMATORY COMPOUNDS.
ATE323701T1 (en) 2001-03-09 2006-05-15 Pfizer Prod Inc TRIAZOLOPYRIDINES AS ANTI-INFLAMMATORY AGENTS
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
WO2002076954A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
AU2002303145A1 (en) 2001-03-23 2002-10-08 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
WO2002076984A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
WO2002076463A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
ATE304009T1 (en) 2001-04-04 2005-09-15 Pfizer Prod Inc NEW BENZOTRIAZOLES WITH ANTI-INFLAMMATORY EFFECT
US20040136949A1 (en) 2001-04-24 2004-07-15 Matthias Grell Combination therapy using anti-angiogenic agents and tnf alpha
WO2002090360A1 (en) 2001-05-10 2002-11-14 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
EP1392300A1 (en) 2001-05-11 2004-03-03 Vertex Pharmaceuticals Incorporated 2,5-disubstituted pyridine, pyrimidine, pyridazine and 1, 2, 4-triazine derivatives for use as p38 inhibitors
DE60221392T2 (en) 2001-05-24 2008-04-17 Eli Lilly And Co., Indianapolis NEW PYROL DERIVATIVES AS PHARMACEUTICAL AGENTS
ATE415162T1 (en) 2001-06-11 2008-12-15 Vertex Pharma ISOQUINOLINE INHIBITORS OF P38
US7196095B2 (en) 2001-06-25 2007-03-27 Merck & Co., Inc. (Pyrimidinyl) (phenyl) substituted fused heteroaryl p38 inhibiting and PKG kinase inhibiting compounds
JP4510442B2 (en) 2001-06-26 2010-07-21 ブリストル−マイヤーズ スクイブ カンパニー N-heterocyclic inhibitor of TNF-α expression
DE60219793T2 (en) 2001-07-11 2008-01-24 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Process for the treatment of cytokine-mediated diseases
CA2454913A1 (en) 2001-08-20 2003-02-27 Boehringer Ingelheim Pharmaceuticals, Inc. Parenteral formulations of 1-(5-tert-butyl-2-p-tolyl-2h-pryrazol-3-yl)-3-¬4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl|-urea and a cyclodextrin
AU2002331179B2 (en) 2001-08-30 2008-04-17 F. Hoffmann-La Roche Ag Aminopyrrole compounds as antiinflammatory agents
US20040235808A1 (en) 2001-09-21 2004-11-25 Jiabing Wang Androstanes as androgen receptor modulators
US7205275B2 (en) 2001-10-11 2007-04-17 Amgen Inc. Methods of treatment using specific binding agents of human angiopoietin-2
WO2003032894A2 (en) 2001-10-12 2003-04-24 Pfizer Products Inc. Method of monitoring neuroprotective treatment
GB0124928D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124938D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124936D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124932D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124933D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124939D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124931D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124941D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
JP2005511593A (en) 2001-11-08 2005-04-28 メルク　エンド　カムパニー　インコーポレーテッド Compositions and methods for treating osteoporosis
US20040009990A1 (en) 2001-11-09 2004-01-15 Higgins Linda S. Method to treat cystic fibrosis
US20050261836A1 (en) 2001-12-05 2005-11-24 Wuyi Meng Crystal structure of mitogen-activated protein kinase-activated protein kinase 2 and binding pockets thereof
US20030118575A1 (en) 2001-12-11 2003-06-26 Boehringer Ingelheim Pharmaceuticals, Inc. Method for administering BIRB 796 BS
AU2003206382B2 (en) 2002-01-03 2008-01-24 Smithkline Beecham Corporation Novel pharmaceutical dosage forms and method for producing same
US7605152B2 (en) 2002-01-15 2009-10-20 Merck & Co., Inc. 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators
DE10203749A1 (en) 2002-01-31 2003-08-14 Boehringer Ingelheim Pharma New anticholinergics, process for their preparation and their use as medicines
DE10203753A1 (en) 2002-01-31 2003-08-14 Boehringer Ingelheim Pharma New xanthene carboxylic acid esters, processes for their preparation and their use as medicines
DE10203741A1 (en) 2002-01-31 2003-08-14 Boehringer Ingelheim Pharma New fluorene carboxylic acid esters, process for their preparation and their use as medicaments
US20040023961A1 (en) 2002-02-11 2004-02-05 Bayer Corporation Aryl ureas with raf kinase and angiogenisis inhibiting activity
ATE485275T1 (en) 2002-02-12 2010-11-15 Glaxosmithkline Llc NICOTINAMIDES AND THEIR USE AS P38 INHIBITORS
ATE410429T1 (en) 2002-03-07 2008-10-15 Hoffmann La Roche BICYCLIC PYRIDINE AND PYRIMIDINE INHIBITORS OF P38 KINASE
AU2003218235B2 (en) 2002-03-13 2008-05-15 Merck Sharp & Dohme Corp. Fluorinated 4-azasteroid derivatives as androgen receptor modulators
WO2003079986A2 (en) 2002-03-18 2003-10-02 Bristol-Myers Squibb Company Uracil derivatives as inhibitors of tnf-alpha converting enzyme (tace) and matrix metalloproteinases
US6900208B2 (en) 2002-03-28 2005-05-31 Bristol Myers Squibb Company Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders
RU2310657C2 (en) 2002-04-03 2007-11-20 Ф.Хоффманн-Ля Рош Аг Imidazo-condensed compounds and pharmaceutical composition containing thereof
BR0309009A (en) 2002-04-05 2005-03-22 Boehringer Ingelheim Pharma Method for the treatment of mucus hypersecretion
US20030225089A1 (en) 2002-04-10 2003-12-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and p38 kinase inhibitors
DE10216339A1 (en) 2002-04-13 2003-10-23 Boehringer Ingelheim Pharma New diarylacetic acid quaternized tropanyl esters, are anticholinergic agents useful e.g. for treating asthma, chronic obstructive pulmonary disease, arrhythmia or menstrual disorders
WO2003087394A1 (en) 2002-04-15 2003-10-23 Glaxo Group Limited A method of identifying a modudator for a serine/theronine kinase
BR0309053A (en) 2002-04-19 2005-02-22 Smithkline Beecham Corp Compounds
EP1503996B1 (en) 2002-04-23 2008-12-24 Bristol-Myers Squibb Company Aryl ketone pyrrolo-triazine compounds useful as kinase inhibitors
DK1497019T3 (en) 2002-04-23 2015-08-03 Bristol Myers Squibb Co PYRROLO-TRIAZINANILINE COMPOSITIONS USED AS KINase INHIBITORS
US7388009B2 (en) 2002-04-23 2008-06-17 Bristol-Myers Squibb Company Heteroaryl-substituted pyrrolo-triazine compounds useful as kinase inhibitors
US20050131005A1 (en) 2002-04-30 2005-06-16 Jiabing Wang 4-azasteroid derivatives as androgen receptor modulators
GB0209891D0 (en) 2002-04-30 2002-06-05 Glaxo Group Ltd Novel compounds
AU2003229305A1 (en) 2002-05-17 2003-12-02 Scios, Inc. TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-Beta INHIBITORS
TW200400034A (en) 2002-05-20 2004-01-01 Bristol Myers Squibb Co Pyrazolo-pyrimidine aniline compounds useful as kinase inhibitors
US7008958B2 (en) 2002-05-21 2006-03-07 Bristol-Myers Squibb Company 2-substituted 5-oxazolyl indole compounds useful as IMPDH inhibitors and pharmaceutical compositions comprising same
JP4245561B2 (en) 2002-06-11 2009-03-25 メルク エンド カムパニー インコーポレーテッド (Halo-benzocarbonyl) heterobicyclic P38 kinase inhibitors
DE60310730T2 (en) 2002-07-09 2007-05-16 Boehringer Ingelheim Pharma Gmbh & Co. Kg PHARMACEUTICAL COMPOSITIONS OF ANTICHOLINERGICA AND P38 KINASE INHIBITORS FOR THE TREATMENT OF RESPIRATORY DISEASES
EP1575506A4 (en) 2002-07-25 2008-04-23 Scios Inc Methods for improvement of lung function using tgf-beta inhibitors
GB0217757D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Novel compounds
JP4252534B2 (en) 2002-08-06 2009-04-08 エフ．ホフマン−ラ ロシュ アーゲー 6-Alkoxy-pyrido-pyrimidines as p-38 MAP kinase inhibitors
US6872726B2 (en) 2002-08-08 2005-03-29 Boehringer Ingelheim Pharmaceuticals Inc. Fluorinated di-aryl urea compounds
AU2003256297A1 (en) 2002-08-09 2004-02-25 Eli Lilly And Company Benzimidazoles and benzothiazoles as inhibitors of map kinase
US20040110755A1 (en) 2002-08-13 2004-06-10 Boehringer Ingelheim Pharmaceuticals, Inc. Combination therapy with p38 MAP kinase inhibitors and their pharmaceutical compositions
CA2496445A1 (en) 2002-08-14 2004-02-26 Boehringer Ingelheim Pharmaceuticals, Inc. Anticoagulant and fibrinolytic therapy using p38 map kinase inhibitors
EP1539121A4 (en) 2002-08-29 2008-08-13 Scios Inc Methods of promoting osteogenesis
PA8579601A1 (en) 2002-08-30 2004-05-07 Pfizer Prod Inc ANTIINFLAMMATORY COMPOUNDS OF DI AND TRIFLORURO-TRIAZOLO-PIRIDINAS
US7005523B2 (en) 2002-08-30 2006-02-28 Pfizer Inc. Cycloalkyl-[4-(trifluorophenyl)-oxazol-5yl]-triazolo-pyridines
US20040092547A1 (en) 2002-08-30 2004-05-13 Pfizer Inc Alkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines
US7037923B2 (en) 2002-08-30 2006-05-02 Pfizer, Inc. Alkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines
AU2003253188A1 (en) 2002-08-30 2004-03-19 Pfizer Products Inc. Novel processes and intermediates for preparing triazolo-pyridines
US7012143B2 (en) 2002-08-30 2006-03-14 Dombroski Mark A Cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines
AU2003268464A1 (en) 2002-09-03 2004-03-29 Scios Inc. INDOLE-TYPE DERIVATIVES AS INHIBITORS OF p38 KINASE
JP2006503025A (en) 2002-09-05 2006-01-26 サイオス インク． Pain treatment by inhibiting p38MAP kinase
US20050288503A1 (en) 2002-09-06 2005-12-29 Adams Jerry L Novel compounds
US7115644B2 (en) 2002-09-13 2006-10-03 Boehringer Ingelheim Pharmaceuticals Inc. Heterocyclic compounds
WO2004026871A1 (en) 2002-09-17 2004-04-01 Eli Lilly And Company Novel pyrazolopyridine derivatves as pharmaceutical agents
WO2004029040A1 (en) 2002-09-27 2004-04-08 Janssen Pharmaceutica N.V. 3,4-disubstituted pyrroles and their for use in treating inflammatory diseases
WO2004033632A2 (en) 2002-10-04 2004-04-22 Bristol-Myers Squibb Company Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme (tace)
US20050288299A1 (en) 2002-10-09 2005-12-29 Mavunkel Babu J Azaindole derivatives as inhibitors of p38 kinase
EP1560582A4 (en) 2002-10-09 2008-03-12 Scios Inc AZAINDOLE DERIVATIVES AS INHIBITORS OF p38 KINASE
WO2004041277A1 (en) 2002-11-01 2004-05-21 Merck & Co., Inc. Carbonylamino-benzimidazole derivatives as androgen receptor modulators
EP1565475B1 (en) 2002-11-18 2009-04-08 F. Hoffmann-La Roche Ag Diazinopyrimidines and their use as protein kinase inhibitors
DE10255040A1 (en) 2002-11-26 2004-06-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg New carbamic acid esters with anticholinergic activity
AU2003299652A1 (en) 2002-12-06 2004-06-30 Scios Inc. Methods for treating diabetes
WO2004069793A2 (en) 2003-01-28 2004-08-19 Bristol-Myers Squibb Company Novel 2-substituted cyclic amines as calcium sensing receptor modulators
CN1771234A (en) 2003-02-05 2006-05-10 布里斯托尔-迈尔斯斯奎布公司 Process for preparing pyrrolotriazine kinase inhibitors
MXPA05008450A (en) 2003-02-10 2005-10-18 Vertex Pharma Processes for the preparation of n-heteroaryl-n-aryl-amines by reacting an n-aryl carbamic acid ester with a halo-heteroaryl and analogous processes.
US7205322B2 (en) 2003-02-12 2007-04-17 Bristol-Myers Squibb Company Thiazolidine compounds as calcium sensing receptor modulators
DE602004001676T2 (en) 2003-02-14 2007-08-30 Pfizer Products Inc., Groton Triazolo-pyridines as anti-inflammatory compounds
MXPA05008612A (en) 2003-02-14 2005-12-05 Smithkline Beecham Corp Novel compounds.
TWI325865B (en) 2003-02-27 2010-06-11 Palau Pharma Sa Pyrazolopyridine derivatives
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
MXPA05009459A (en) 2003-03-03 2006-05-17 Array Biopharma Inc P38 inhibitors and methods of use thereof.
US7030112B2 (en) 2003-03-25 2006-04-18 Bristol-Myers Squibb Company Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders
GB0308186D0 (en) 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
GB0308201D0 (en) 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
GB0308185D0 (en) 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
ES2279361T3 (en) 2003-04-16 2007-08-16 F. Hoffmann-La Roche Ag DERIVATIVES OF (6- (FENOXI) -PIRIDO-3,4-DIPIRIMIDIN-2-IL) -AMINE AS INHIBITORS OF P38 KINASA FOR THE TREATMENT OF INFLAMMATORY STATES SUCH AS REUMATOID ARTHRITIS.
MXPA05011103A (en) 2003-04-16 2005-12-12 Hoffmann La Roche Quinazoline compounds useful as p38 kinase inhibitors.
PT1618092E (en) 2003-05-01 2010-11-22 Bristol Myers Squibb Co Aryl-substituted pyrazole-amide compounds useful as kinase inhibitors
GB0320244D0 (en) 2003-05-06 2003-10-01 Aventis Pharma Inc Pyrazoles as inhibitors of tumour necrosis factor
WO2004100874A2 (en) 2003-05-07 2004-11-25 Merck & Co., Inc. Androgen receptor modulators and methods of use thereof
MXPA05013059A (en) 2003-06-04 2006-03-02 Pfizer 2-amino-pyridine derivatives as beta-2 adrenoreceptor agonists.
ATE517872T1 (en) 2003-06-26 2011-08-15 Novartis Ag FIVE-MEMBER HETEROCYCLE-BASED P38 KINASE INHIBITORS
CN1816370A (en) 2003-06-30 2006-08-09 麦克公司 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
CA2530182A1 (en) 2003-06-30 2005-01-20 Merck & Co., Inc. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
WO2005009367A2 (en) 2003-07-17 2005-02-03 Ambit Biosciences Corporation Treatment of diseases with kinase inhibitors
GB0317482D0 (en) 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
US7153870B2 (en) 2003-07-25 2006-12-26 Pfizer Inc. Nicotinamide derivatives useful as PDE4 inhibitors
GB0317484D0 (en) 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
US20050020587A1 (en) 2003-07-25 2005-01-27 Pfizer Inc Nicotinamide derivatives useful as PDE4 inhibitors
GB0317516D0 (en) 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as PDE4 inhibitors
CA2533803A1 (en) 2003-07-29 2005-02-10 Bristol-Myers Squibb Company Biomarkers of cyclin-dependent kinase modulation
GB0318814D0 (en) 2003-08-11 2003-09-10 Smithkline Beecham Corp Novel compounds
CL2004002050A1 (en) 2003-08-13 2005-06-03 Pharmacia Corp Sa Organizada B COMPOUNDS DERIVED FROM REPLACED PIRIDINONES; ITS USE IN THE TREATMENT OF AFFECTIONS CAUSED OR EXACTED BY ACTIVITY P38 MAP KINASA AND / OR NON-REGULATED TNF, SUCH AS INFLAMMATIONS, TUMORS, AIDS AND OTHERS.
CN1838958A (en) 2003-08-22 2006-09-27 贝林格尔·英格海姆药物公司 Methods of treating COPD and pulmonary hypertension
US20050053600A1 (en) 2003-09-09 2005-03-10 Lane Thomas E. Methods for treating rheumatoid arthritis
EP1663228A4 (en) 2003-09-10 2010-10-06 Merck Sharp & Dohme 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators
SG146624A1 (en) 2003-09-11 2008-10-30 Kemia Inc Cytokine inhibitors
CA2540828A1 (en) 2003-09-30 2005-04-14 Scios Inc. Heterocyclic amides and sulfonamides
WO2005032551A1 (en) 2003-09-30 2005-04-14 Scios Inc. TREATMENT OF CARDIOVASCULAR DISEASE WITH INHIBITORS OF p38 KINASE
US7232824B2 (en) 2003-09-30 2007-06-19 Scios, Inc. Quinazoline derivatives as medicaments
US7419978B2 (en) 2003-10-22 2008-09-02 Bristol-Myers Squibb Company Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors
ES2281843T3 (en) 2003-11-13 2007-10-01 F. Hoffmann-La Roche Ag PIRIDO-7-PIRIMIDIN-7-WAVES REPLACED WITH HYDROXIALQUIL.
EP1538201A1 (en) 2003-12-02 2005-06-08 F.Hoffmann-La Roche Ag Method for the recombinant production and purification of protein kinases
WO2005063715A1 (en) 2003-12-18 2005-07-14 Boehringer Ingelheim Pharmaceuticals, Inc. Polymorph of birb 796, a p38map kinase inhibitor
GB0329275D0 (en) 2003-12-18 2004-01-21 Merck Sharp & Dohme Therapeutic treatment
AU2004305318A1 (en) 2003-12-18 2005-07-07 Pfizer Products Inc. Methods of treating acute inflammation in animals with p38 MAP kinase inhibitors
US20060052390A1 (en) 2003-12-24 2006-03-09 Scios, Inc. Treatment of multiple myeloma by p38 MAP kinase and proteasome inhibition
US20060058296A1 (en) 2003-12-24 2006-03-16 Scios, Inc. Treatment of osteolytic lesions associated with multiple myeloma by inhibition of p38 map kinase
US20060079461A1 (en) 2003-12-24 2006-04-13 Scios, Inc. Treatment of multiple myeloma by inhibition of p38 MAP kinase
CN1921864A (en) 2003-12-24 2007-02-28 西奥斯公司 Treatment of malignant gliomas with TGF-beta inhibitors
GB0402140D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
GB0402138D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
BRPI0507198A (en) 2004-01-30 2007-06-26 Merck Patent Gmbh bisarylurea derivatives
TWI332003B (en) 2004-01-30 2010-10-21 Lilly Co Eli Kinase inhibitors
GB0402137D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
GB0402143D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
US7863310B2 (en) 2004-02-03 2011-01-04 Eli Lilly And Company Kinase inhibitors
US7652146B2 (en) 2004-02-06 2010-01-26 Bristol-Myers Squibb Company Process for preparing 2-aminothiazole-5-carboxamides useful as kinase inhibitors
TWI338004B (en) 2004-02-06 2011-03-01 Bristol Myers Squibb Co Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors
CA2557398A1 (en) 2004-02-26 2005-09-09 Hans-Peter Buchstaller Benzimidazolyl derivatives as kinase inhibitors
RU2006134021A (en) 2004-02-27 2008-04-10 Ф.Хоффманн-Ля Рош Аг (Ch) Heteroaryl-Condensed Pyrazole Derivatives
KR20060114022A (en) 2004-02-27 2006-11-03 에프. 호프만-라 로슈 아게 Indazole derivatives and pharmaceutical compositions containing them
AU2005227192A1 (en) 2004-03-11 2005-10-06 Kythera Biopharmaceuticals, Inc. Compositions and methods for preventing and treating skin and hair conditions
EP1574501A1 (en) 2004-03-11 2005-09-14 Pfizer Limited Quinolinone derivatives, pharmaceutical compositions containing them and their use
EP1577291A1 (en) 2004-03-17 2005-09-21 Pfizer Limited Phenylethanolamine derivatives as beta-2 agonists
EP1577292A1 (en) 2004-03-17 2005-09-21 Pfizer Limited Phenylaminoethanol derivatives as beta2 receptor agonists
EP1742631A4 (en) 2004-04-28 2009-11-11 Merck & Co Inc Fluorinated 4-azasteroids as androgen receptor modulators
WO2005110455A2 (en) 2004-05-13 2005-11-24 Intermune, Inc. Combination therapy for treating hepatitis virus infection
UA87854C2 (en) 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
SI1761520T1 (en) 2004-06-23 2008-10-31 Lilly Co Eli Kinase inhibitors
EP1609789A1 (en) 2004-06-23 2005-12-28 Eli Lilly And Company Ureido-pyrazole derivatives and their use as kinase inhibitors
US7253167B2 (en) 2004-06-30 2007-08-07 Bristol-Myers Squibb Company Tricyclic-heteroaryl compounds useful as kinase inhibitors
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
TW200618803A (en) 2004-08-12 2006-06-16 Bristol Myers Squibb Co Process for preparing pyrrolotriazine aniline compounds useful as kinase inhibitors
GEP20104973B (en) 2004-08-12 2010-04-26 Pfizer Triazolopyridinylsulfanyl derivatives as p38 map kinase inhibitors
AU2005280334A1 (en) 2004-08-25 2006-03-09 Merck Sharp & Dohme Corp. Androgen receptor modulators
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
PE20060493A1 (en) 2004-10-05 2006-09-03 Smithkline Beecham Corp COMPOUNDS DERIVED FROM BIPHENYL (DI OR TRI) CARBOXAMIDES AS SERINE / THREONINE KINASE P38 INHIBITORS
CA2584185C (en) 2004-10-13 2014-07-15 Frank Stieber Heterocyclic substituted bisarylurea derivates as kinase inhibitors
CA2583217C (en) 2004-10-18 2011-05-31 Amgen Inc. 1,3,4-thiadiazole compounds as protein kinase inhibitors
CA2585276A1 (en) 2004-10-29 2006-06-08 Merck & Co., Inc. N-(pyridin-3-yl)-2-phenylbutanamides as androgen receptor modulators
WO2006055302A2 (en) 2004-11-04 2006-05-26 Scios Inc. Method of treating myelodysplastic syndromes
WO2006048266A2 (en) 2004-11-04 2006-05-11 Roche Diagnostics Gmbh Gene expression profiling of leukemias with mll gene rearrangements
GB0425057D0 (en) 2004-11-12 2004-12-15 Pfizer Ltd L-tartrate salt of N-1-adamantyl-2-{3-[(2R)-2-hydroxy-2-[4-hydroxy-3-(hydroxymethyl)phenyl]eth yl}amino)propyl]phenyl}acetamide
WO2006051373A1 (en) 2004-11-12 2006-05-18 Pfizer Limited Compounds for the treatment of diseases
WO2006055381A2 (en) 2004-11-16 2006-05-26 Merck & Co., Inc. Prodrugs of (2r)-2-propyloctanoic acid for treatment of stroke
US20080139614A1 (en) 2004-11-23 2008-06-12 Seabrook Guy R Treatment Of Stroke With Histamine H3 Inverse Agonists Or Histamine H3 Antagonists
US20060111416A1 (en) 2004-11-24 2006-05-25 Lane Charlotte A L Octahydropyrrolo[3,4-C]pyrrole derivatives
US20070224662A1 (en) 2004-12-17 2007-09-27 Jun Luo Post-translational modification of proteins in cell-free expression systems
PE20061155A1 (en) 2004-12-24 2006-12-16 Boehringer Ingelheim Int INDOLINONE DERIVATIVES AS AGENTS FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES
US20060154939A1 (en) 2004-12-24 2006-07-13 Boehringer Ingelheim International Gmbh Medicaments for the Treatment or Prevention of Fibrotic Diseases
PE20060777A1 (en) 2004-12-24 2006-10-06 Boehringer Ingelheim Int INDOLINONE DERIVATIVES FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES
ATE538118T1 (en) 2004-12-28 2012-01-15 Aska Pharm Co Ltd PYRIMIDINYLISOXAZOLE DERIVATIVE
US20060178388A1 (en) 2005-02-04 2006-08-10 Wrobleski Stephen T Phenyl-substituted pyrimidine compounds useful as kinase inhibitors
ATE469893T1 (en) 2005-02-28 2010-06-15 Merckle Gmbh 2-SULFINYL AND 2-SULFONYL SUBSTITUTED IMIDAZOLE DERIVATIVES AND THEIR USE AS CYTOKIN INHIBITORS
US7759337B2 (en) 2005-03-03 2010-07-20 Amgen Inc. Phthalazine compounds and methods of use
JP2008535822A (en) 2005-03-25 2008-09-04 グラクソ グループ リミテッド New compounds
AR053346A1 (en) 2005-03-25 2007-05-02 Glaxo Group Ltd COMPOSITE DERIVED FROM 8H -PIRIDO (2,3-D) PIRIMIDIN -7 ONA 2,4,8- TRISUSTITUTED PHARMACEUTICAL COMPOSITION AND USE TO PREPARE A COMPOSITION FOR TREATMENT AND PROFILXIS OF A DISEASE MEDIATED BY KINASE CSBP / RK / P38
TW200724142A (en) 2005-03-25 2007-07-01 Glaxo Group Ltd Novel compounds
US20060235020A1 (en) 2005-04-18 2006-10-19 Soojin Kim Process for preparing salts of 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide and novel stable forms produced therein
TW200716561A (en) 2005-05-11 2007-05-01 Array Biopharma Inc P38 inhibitors and methods of use thereof
WO2006127678A2 (en) 2005-05-23 2006-11-30 Smithkline Beecham Corporation Inhibition of p38 mark for treatment of obesity
GB0512429D0 (en) 2005-06-17 2005-07-27 Smithkline Beecham Corp Novel compound
US20070032506A1 (en) 2005-07-02 2007-02-08 Peter Giannousis Crystalline forms of (2r-trans)-6-chloro-5[[4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-n,n, 1-trimethyl-alpha-oxo-1h-indole-3-acetamide monohydrochloride
US7473784B2 (en) 2005-08-01 2009-01-06 Bristol-Myers Squibb Company Benzothiazole and azabenzothiazole compounds useful as kinase inhibitors
US20090088458A1 (en) 2005-08-02 2009-04-02 Meissner Robert S N-(Pyridin-4-Yl)-2-Phenylbutanamides as Androgen Receptor Modulators
JP5113751B2 (en) 2005-08-12 2013-01-09 メルク・シャープ・エンド・ドーム・コーポレイション Bicyclic heterocyclic compounds useful as p38 kinase inhibitors
EP1928843A1 (en) 2005-08-22 2008-06-11 Amgen, Inc Bis-aryl urea compounds for the treatment of protein kinase-mediated diseaes
CN101243088B (en) 2005-08-25 2011-06-29 霍夫曼-拉罗奇有限公司 P38 map kinase inhibitors and methods for using the same
EP1919877A1 (en) 2005-08-25 2008-05-14 F.Hoffmann-La Roche Ag P38 map kinase inhibitors and methods for using the same
JP2009506006A (en) 2005-08-25 2009-02-12 エフ．ホフマン−ラ ロシュ アーゲー p38 MAP kinase inhibitor and method of using the same
CA2620104A1 (en) 2005-08-25 2007-03-01 F. Hoffman-La Roche Ag Fused pyrazole as p38 map kinase inhibitors
BRPI0615272A2 (en) 2005-08-25 2009-08-04 Hoffmann La Roche p38 map kinase inhibitors and methods for their use
EP1919919A1 (en) 2005-09-01 2008-05-14 Astellas Pharma Inc. Pyridazinone derivatives used for the treatment of pain
SI1928821T1 (en) 2005-09-21 2009-04-30 Pfizer Ltd Carboxamide derivatives as muscarinic receptor antagonists
CA2623063A1 (en) 2005-09-26 2007-04-05 Merck & Co., Inc. N-(4-oxo-3,4-dihydroquinazolin-2-yl)butanamides as androgen receptor modulators
WO2007045989A1 (en) 2005-10-20 2007-04-26 Pfizer Limited Pyridyl derivatives useful as h3 ligands
DOP2006000233A (en) 2005-10-28 2007-06-15 Lilly Co Eli KINASE INHIBITORS
AR056582A1 (en) 2005-10-28 2007-10-10 Lilly Co Eli PIRAZOLIL UREA COMPOUNDS WITH INHIBITORY ACTIVITY OF CINASA P38 AND PHARMACEUTICAL FORMULATION THAT INCLUDES IT
WO2007056016A2 (en) 2005-11-02 2007-05-18 Kemia, Inc. Bisamide cytokine inhibitors
EP1945639A1 (en) 2005-11-04 2008-07-23 Pfizer Limited Tetrahydronaphthyridine derivative
AU2006313430B2 (en) 2005-11-08 2012-09-06 Ranbaxy Laboratories Limited Process for (3R,5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4- [(4-hydroxy methyl phenyl amino) carbonyl]-pyrrol-1-yl]-3, 5-dihydroxy-heptanoic acid hemi calcium salt
PE20070823A1 (en) 2005-11-15 2007-08-09 Glaxo Group Ltd SALT 8- (2,6-DIFLUOROPHENYL) -4- (4-FLUORO-2-METHYLPHENYL) -2 - {[2-HYDROXY-1- (HYDROXIMETHYL) ETHYL] AMINO} PYRID [2,3-] PYRIMIDIN SALT -7 (8H) -ONA
NL2000323C2 (en) 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine derivatives.
WO2007075896A2 (en) 2005-12-22 2007-07-05 Kemia, Inc. Heterocyclic cytokine inhibitors
ES2389062T3 (en) 2006-01-18 2012-10-22 Amgen, Inc Thiazole compounds as protein kinase B inhibitors (PKB)
CN101415685B (en) 2006-01-31 2011-08-24 阿雷生物药品公司 Kinase inhibitors and methods of use thereof
WO2007091152A1 (en) 2006-02-09 2007-08-16 Pfizer Limited Triazolopyridine compounds
EP1987022A1 (en) 2006-02-10 2008-11-05 Pfizer Products Inc. Pyridinone pyrazole urea and pyrimidinone pyrazole urea derivatives
GB0603684D0 (en) 2006-02-23 2006-04-05 Novartis Ag Organic compounds
KR20080100484A (en) 2006-03-07 2008-11-18 버텍스 파마슈티칼스 인코포레이티드 Use of vx-702 for treating rheumatoid arthritis
BRPI0708644A2 (en) 2006-03-07 2011-06-07 Bristol-Myers Squibb Company pyrrolotriazine aniline prodrug compounds useful as kinase inhibitors
AU2007228511A1 (en) 2006-03-20 2007-09-27 Pfizer Limited Amine derivatives
EP2029581A1 (en) 2006-03-29 2009-03-04 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
JP2009533362A (en) 2006-04-12 2009-09-17 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 N-oxides of heterocyclic substituted bisarylureas for treating kinase mediated diseases
WO2007124181A2 (en) 2006-04-21 2007-11-01 Amgen Inc. Thieno-[2,3-d]pyrimidine and thieno-pyridazine compounds and methods of use
AU2007257959A1 (en) 2006-06-09 2007-12-21 Kemia, Inc. Therapy using cytokine inhibitors
GB0612026D0 (en) 2006-06-16 2006-07-26 Smithkline Beecham Corp New use
JP2009542816A (en) 2006-06-16 2009-12-03 グラクソ グループ リミテッド New compounds
US20090318424A1 (en) 2006-06-16 2009-12-24 Mauro Corsi Novel compounds
JP2009542817A (en) 2006-06-16 2009-12-03 グラクソ グループ リミテッド New compounds
EP2036905B1 (en) 2006-06-28 2012-12-12 ASKA Pharmaceutical Co., Ltd. Pyridylisoxazole derivative
EP2044957A4 (en) 2006-06-28 2011-01-05 Aska Pharm Co Ltd Treatment agent for inflammatory bowel disease
WO2008011032A1 (en) 2006-07-17 2008-01-24 Amgen Inc. Quinazoline and pyridopyrimidine derivatives as p38 kinase inhibitors
WO2008013823A2 (en) 2006-07-26 2008-01-31 Scios Inc. Co-crystals of (2r-trans)-6-chloro-5-[[4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-n,n,1-trimethyl-alpha-oxo-1h-indole-3-acetamide
CA2659222C (en) 2006-07-28 2012-01-31 Onconova Therapeutics, Inc. Formulations of radioprotective .alpha., .beta. unsaturated aryl sulfones
PE20080906A1 (en) 2006-08-17 2008-07-05 Kemia Inc HETEROARYL DERIVATIVES AS CYTOKINE INHIBITORS
WO2008024391A1 (en) 2006-08-22 2008-02-28 Scios Inc. Pharmaceutical formulations of an indole-type derivative and related methods of use
BRPI0719270A2 (en) 2006-10-04 2014-03-11 Pfizer Ltd SULFONAMIDE DERIVATIVES AS ADRENERGIC AGONISTS AND MUSCARINE ANTAGONISTS
ES2377821T3 (en) 2006-10-11 2012-04-02 Amgen Inc. Imidazo- and triazolo-pyridine compounds and methods of use thereof.
WO2008048540A2 (en) 2006-10-18 2008-04-24 Merck & Co., Inc. 2-hydroxy-2-phenyl/thiophenyl propionamides as androgen receptor modulators
US20100099651A1 (en) 2006-10-26 2010-04-22 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
US7943617B2 (en) 2006-11-27 2011-05-17 Bristol-Myers Squibb Company Heterobicyclic compounds useful as kinase inhibitors
WO2008071665A1 (en) 2006-12-12 2008-06-19 Smithkline Beecham Corporation A nicotinamide derivative useful as p38 kinase inhibitor
WO2008071664A1 (en) 2006-12-12 2008-06-19 Smithkline Beecham Corporation Nicotinamide derivative used as a p38 kinase inhibitor
CA2670730A1 (en) 2006-12-13 2008-06-26 Gilead Sciences, Inc. Monophosphates as mutual prodrugs of anti-inflammatory signal transduction modulators (aistm's) and beta-agonists for the treatment of pulmonary inflammation and bronchoconstriction
CA2672256C (en) 2006-12-13 2011-08-30 Pfizer Products Inc. Processes for the preparation of 3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2h)-yl)-n,4-dimethylbenzamide
JP2010513370A (en) 2006-12-19 2010-04-30 エフ．ホフマン−ラ ロシュ アーゲー Pyrazolo [3,4-d] pyrimidine p38 MAP kinase inhibitor
WO2008079857A1 (en) 2006-12-20 2008-07-03 Bristol-Myers Squibb Company Crystalline forms of aryl-substituted pyrazole-amide compounds
WO2008089034A2 (en) 2007-01-11 2008-07-24 Kemia, Inc. Cytokine inhibitors
WO2008098096A1 (en) 2007-02-08 2008-08-14 Boehringer Ingelheim International Gmbh Anti-cytokine heterocyclic compounds
AU2008219165A1 (en) 2007-02-16 2008-08-28 Merck Sharp & Dohme Corp. Compositions and methods for potentiated activity of biologicaly active molecules
EP2123255B1 (en) 2007-02-16 2013-05-15 ASKA Pharmaceutical Co., Ltd. Pharmaceutical composition containing fine particle oil-based suspension
WO2008104473A2 (en) 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag Pyrazolopyriidine derivatives and their use as kinase inhibitors
ES2364727T3 (en) 2007-03-16 2011-09-13 Pfizer Limited CHLORHYDRATE SALT OF 5- [3- (3-HYDROXYPHENOXY) AZETIDIN-1-IL] -5-METHYL-2,2-DIFENYLHEXANAMIDE.
WO2008137176A1 (en) 2007-05-07 2008-11-13 Amgen Inc. Pyrazolo-pyridinone compounds, process for their preparation, and their pharmaceutical use
CA2685597C (en) 2007-05-07 2012-10-02 Amgen Inc. Pyrazolo-pyridinone and pyrazolo-pyrazinone compounds as p38 modulators, process for their preparation, and their pharmaceutical use
AU2008276512A1 (en) 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of PKB
AU2008276521B2 (en) 2007-07-17 2011-11-03 Amgen Inc. Heterocyclic modulators of PKB
US7943658B2 (en) 2007-07-23 2011-05-17 Bristol-Myers Squibb Company Indole indane amide compounds useful as CB2 agonists and method
WO2009015000A1 (en) 2007-07-25 2009-01-29 Array Biopharma Inc. Pyrazole urea derivatives used as kinase inhibitors
CA2699463A1 (en) 2007-09-14 2009-03-19 Pfizer Limited Novel compounds active as muscarinic receptor antagonists
US8314131B2 (en) 2007-09-21 2012-11-20 Amgen Inc. Triazole fused heteroaryl compounds and methods of use thereof
CN101878221B (en) 2007-11-30 2014-04-02 辉瑞有限公司 Novel glucocorticoid receptor agonists
GB0724258D0 (en) 2007-12-12 2008-01-30 Glaxo Group Ltd Novel combinations
WO2009074518A1 (en) 2007-12-12 2009-06-18 Glaxo Group Limited Combinations of prolinamide p2x7 modulators with further therapeutic agents
WO2009078992A1 (en) 2007-12-17 2009-06-25 Amgen Inc. Linear tricyclic compounds as p38 kinase inhibitors
EP2235537A2 (en) 2008-01-25 2010-10-06 Bristol-Myers Squibb Pharma Company Identification of predictive markers of response to dasatinib in human colon cancer
CA2716124A1 (en) 2008-02-20 2009-08-27 Boehringer Ingelheim International Gmbh Powder inhalers
US8367671B2 (en) 2008-03-21 2013-02-05 Amgen Inc. Pyrazolo[3.4-B]pyrazine compounds as p38 modulators and methods of use as anti-inflamatory agents
JP2009263234A (en) 2008-04-21 2009-11-12 Ranbaxy Lab Ltd Composition of phosphodiesterase inhibitor of type iv
AR072008A1 (en) 2008-06-13 2010-07-28 Merck & Co Inc HETEROBICICLIC COMPOUNDS AS QUINASA P38 INHIBITION AGENTS
JP2011525184A (en) 2008-06-20 2011-09-15 ブリストル−マイヤーズ スクイブ カンパニー Triazolopyridine compounds useful as kinase inhibitors
US8338604B2 (en) 2008-06-20 2012-12-25 Bristol-Myers Squibb Company Imidazopyridine and imidazopyrazine compounds useful as kinase inhibitors
WO2009158450A1 (en) 2008-06-25 2009-12-30 Bristol-Myers Squibb Company Crystalline forms of ((((4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbonyl)(propyl)carbamoyl)oxy)methyl (4-(phosphonooxy)phenyl)acetate, preparation and use thereof
WO2009158446A2 (en) 2008-06-25 2009-12-30 Bristol-Myers Squibb Company Crystalline forms of ((((4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbonyl)(propyl)carbamoyl)oxy)methyl (4-(phosphonooxy)phenyl)acetate, method of preparation and use thereof
US8263623B2 (en) 2008-07-11 2012-09-11 Pfizer Inc. Triazol derivatives useful for the treatment of diseases
WO2010007561A1 (en) 2008-07-15 2010-01-21 Pfizer Limited Novel compounds active as muscarinic receptor antagonists
WO2010007552A1 (en) 2008-07-15 2010-01-21 Pfizer Limited Novel compounds active as muscarinic receptor antagonists
WO2010025202A1 (en) 2008-08-29 2010-03-04 Amgen Inc. PYRIDO[3,2-d]PYRIDAZINE-2(1H)-ONE COMPOUNDS AS P38 MODULATORS AND METHODS OF USE THEREOF
ES2387474T3 (en) 2008-08-29 2012-09-24 Amgen, Inc Pyridazine-pyridinone compounds for the treatment of protein kinase mediated diseases
WO2010038428A1 (en) 2008-09-30 2010-04-08 武田薬品工業株式会社 Alternative agent to taxane anti-cancer agent
EP2206534A1 (en) 2008-10-09 2010-07-14 c-a-i-r biosciences GmbH Dibenzocycloheptanone derivatives und pharmaceutical agents containing these compounds
US8772481B2 (en) 2008-10-10 2014-07-08 Amgen Inc. Aza- and diaza-phthalazine compounds as P38 map kinase modulators and methods of use thereof
US8497269B2 (en) 2008-10-10 2013-07-30 Amgen Inc. Phthalazine compounds as p38 map kinase modulators and methods of use thereof
US20110263647A1 (en) 2009-01-15 2011-10-27 Amgen Inc. Fluoroisoquinoline substituted thiazole compounds and methods of use
EP2393492A1 (en) 2009-02-09 2011-12-14 Boehringer Ingelheim International GmbH New pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
JP2012518003A (en) 2009-02-13 2012-08-09 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 Solid form of 2- (2,4-difluorophenyl) -6- (1- (2,6-difluorophenyl) ureido) nicotinamide
EP2396302A2 (en) 2009-02-13 2011-12-21 Vertex Pharmceuticals Incorporated Processes for producing phenyl-6-(1-(phenyl)ureido)nicotinamides)
GB0902648D0 (en) 2009-02-17 2009-04-01 Argenta Discovery Ltd Pharmaceutical compounds and compositions
PE20120655A1 (en) 2009-02-17 2012-06-07 Chiesi Farma Spa TRIAZOLOPYRIDINE DERIVATIVES AS INHIBITORS OF PROTEIN KINES ACTIVATED BY MITOGEN P38 (MAP)
WO2010120963A1 (en) 2009-04-16 2010-10-21 Bristol-Myers Squibb Company Tablet formulation for p38 inhibitor and method
CN102574838B (en) 2009-05-05 2014-07-02 默沙东公司 Pyrrole and [2,3-C] pyridine derivative using as P38 kinase inhibiting agents
EP2470534A4 (en) 2009-08-24 2013-02-27 Merck Sharp & Dohme Jak inhibition blocks rna interference associated toxicities
CN104043126A (en) 2009-10-22 2014-09-17 霍夫曼-拉罗奇有限公司 Modulation of axon degeneration
US20110117055A1 (en) 2009-11-19 2011-05-19 Macdonald James E Methods of Treating Hepatitis C Virus with Oxoacetamide Compounds
WO2011083387A1 (en) 2010-01-07 2011-07-14 Pfizer Limited Hydrochloride salt of biphenyl-2-yl-carbamic acid 1-{9-[(3-fluoro-4-hydroxy-benzoyl)-methyl-amino]-nonyl}-piperidin-4-yl ester
EA022360B1 (en) 2010-03-24 2015-12-30 Онконова Терапьютикс, Инк. Compositions and methods for prevention and treatment of wounds
US9060967B2 (en) 2010-03-26 2015-06-23 Onconova Therapeutics, Inc Stable aqueous formulation of (E)-4-carboxystyryl-4-chlorobenzyl sulfone
GB201009731D0 (en) 2010-06-10 2010-07-21 Pulmagen Therapeutics Inflamma Kinase inhibitors
SG186855A1 (en) 2010-06-28 2013-02-28 Merck Patent Gmbh 2,4- diaryl - substituted [1,8] naphthyridines as kinase inhibitors for use against cancer
JP5886842B2 (en) 2010-07-05 2016-03-16 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 Bipyridyl derivatives useful for the treatment of kinase-induced diseases
WO2012031057A1 (en) 2010-09-01 2012-03-08 Bristol-Myers Squibb Company Bms- 582949 for the treatment of resistant rheumatic disease
RU2013129860A (en) 2010-11-29 2015-01-10 Дженентек, Инк. METHODS FOR IDENTIFICATION OF NEURODEGENERATIVE DISEASES OR DISORDERS
AR083868A1 (en) 2010-12-03 2013-03-27 Lilly Co Eli OXAZOL COMPOUNDS [5,4-B] PIRIDIN-5-ILO
AU2012224979B2 (en) 2011-03-09 2017-01-19 Merck Patent Gmbh Pyrido [2, 3 - b] pyrazine derivatives and their therapeutical uses
DK3081568T3 (en) 2011-05-09 2020-02-24 Eip Pharma Llc COMPOSITIONS AND PROCEDURES FOR TREATING ALZHEIMER'S DISEASE
CN103562198B (en) 2011-06-10 2016-08-24 奇斯药制品公司 There is muscarinic receptor antagonist and the compound of beta 2-adrenergic receptor agonists activity
EP2729146B1 (en) 2011-07-08 2017-03-08 Helmholtz-Zentrum für Infektionsforschung GmbH Medicament for treatment of liver cancer
SG11201401795XA (en) 2011-11-11 2014-09-26 Lilly Co Eli Combination therapy for ovarian cancer
WO2013086002A1 (en) 2011-12-05 2013-06-13 Cellworks Research India Private Limited Compositions, process of preparation of said compositions and method of treating cancer
WO2013083606A1 (en) 2011-12-09 2013-06-13 Chiesi Farmaceutici S.P.A. Kinase inhibitors
ES2612259T3 (en) 2011-12-09 2017-05-16 Chiesi Farmaceutici S.P.A. Kinase inhibitors
US9458154B2 (en) 2011-12-09 2016-10-04 Chiesi Farmaceutici S.P.A. Kinase inhibitors
CN117736134A (en) 2012-01-12 2024-03-22 耶鲁大学 Compounds and methods for enhancing degradation of target proteins and other polypeptides by E3 ubiquitin ligases
UA113302C2 (en) 2012-03-01 2017-01-10 CRYSTAL POLYMORPH 1- (3-TRET-BUTYL-1-P-TOLYL-1H-PYRAZOL-5-IL) -3- (5-FLUOR-2- (1- (2-HYDROXYETHYL) -1H-INDAZOL-5- ILOXES) BENZYL) UREA HYDROCHLORIDE
ES2605942T3 (en) 2012-03-20 2017-03-17 Mereo Biopharma 1 Limited Use of a pyrazole derivative in the treatment of acute exacerbations of chronic obstructive pulmonary disease
JP6267193B2 (en) 2012-05-22 2018-01-24 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Substituted dipyridylamines and their use
EP2858630A4 (en) * 2012-06-07 2016-02-24 Harvard College Nanotherapeutics for drug targeting
CA2879222A1 (en) * 2012-07-17 2014-01-23 Glaxosmithkline Llc Nicotinamide derivate in the treatment of acute coronary syndrome
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
US20150225373A1 (en) 2012-08-29 2015-08-13 Respivert Limited Kinase inhibitors
US9783556B2 (en) 2012-08-29 2017-10-10 Respivert Limited Kinase inhibitors
EP2890460B1 (en) 2012-08-29 2017-02-22 Respivert Limited Kinase inhibitors
GB201215357D0 (en) 2012-08-29 2012-10-10 Respivert Ltd Compounds
US9155747B2 (en) 2012-09-13 2015-10-13 Chiesi Farmaceutici S.P.A. Isoxazolidine derivatives
US9732063B2 (en) 2012-11-16 2017-08-15 Respivert Limited Kinase inhibitors
JP6042995B2 (en) 2012-11-30 2016-12-14 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Breton tyrosine kinase inhibitor
US9370527B2 (en) 2012-12-28 2016-06-21 The Regents Of The University Of Michigan Amelioration of intestinal fibrosis and treatment of Crohn's disease
EP2961744B1 (en) 2013-02-27 2017-06-28 Array Biopharma, Inc. Intermediates for use in the preparation of indazole derivatives and processes for the preparation thereof
EP2970190A1 (en) 2013-03-14 2016-01-20 Respivert Limited Kinase inhibitors
GB201305714D0 (en) 2013-03-28 2013-05-15 Ucl Business Plc Method
CA2907566C (en) * 2013-04-01 2023-08-22 Pulmatrix, Inc. Tiotropium dry powders
TWI641592B (en) 2013-04-02 2018-11-21 英商瑞斯比維特有限公司 Kinase inhibitors
WO2014181213A1 (en) 2013-05-10 2014-11-13 Pfizer Inc. Crystalline form of (sa)-(-)-3-(3-bromo-4-((2,4-difluorobenzyl)oxy)-6-methyl-2-oxopyridin-1 (2h)-yl)-n,4-dimethylbenzamide
US9359354B2 (en) 2013-06-06 2016-06-07 Chiesi Farmaceutici S.P.A. Kinase inhibitors
KR20160016973A (en) 2013-06-06 2016-02-15 키에시 파르마슈티시 엣스. 피. 에이. Derivatives of [1, 2, 4] triazolo [4, 3 - a] pyridine as p38 - map kinase inhibitors
RU2015151886A (en) 2013-06-06 2017-06-08 КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. KINAZ INHIBITORS
US9707219B2 (en) 2013-07-10 2017-07-18 Glaxosmithkline Intellectual Property (No.2) Limited Losmapimod for use in treating glomerular disease
US9918989B2 (en) 2013-07-12 2018-03-20 The Regents Of The University Of California Combination therapies for malaria
US9814728B2 (en) * 2013-09-20 2017-11-14 Saint Louis University Inhibition of DUX4 expression using bromodomain and extra-terminal domain protein inhibitors (BETi)
EP3069732B1 (en) * 2013-11-14 2023-07-12 The Doshisha Drug for treating corneal endothelium by promoting cell proliferation or inhibiting cell damage
AU2014369449B2 (en) 2013-12-20 2018-07-05 Oxular Acquisitions Limited Urea derivatives useful as kinase inhibitors
MX2016008110A (en) 2013-12-20 2016-08-19 Hoffmann La Roche Pyrazole derivatives and uses thereof as inhibitors of dlk.
KR102413704B1 (en) 2014-02-14 2022-06-24 레스피버트 리미티드 Aromatic heterocyclic compounds as antiinflammatory compounds
AU2015220873A1 (en) 2014-02-19 2016-08-11 H. Lundbeck A/S 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as BACE1 inhibitors for treatment of Alzheimer's disease
US20230190750A1 (en) 2014-06-13 2023-06-22 Genentech, Inc. Methods of treating and preventing cancer drug resistance
WO2015191996A1 (en) 2014-06-13 2015-12-17 Genentech, Inc. Methods of treating and preventing cancer drug resistance
CN114010641A (en) 2014-07-09 2022-02-08 爱普制药有限责任公司 Methods for treating neurological disorders
MA40774A (en) 2014-10-01 2017-08-08 Respivert Ltd DIARYLEUREA DERIVATIVES AS KINASE P38 INHIBITORS
EP3201189A1 (en) 2014-10-01 2017-08-09 Respivert Limited N-phenyl-3-quinazolin-6-yl-benzamide derivatives as p38 kinase inhibitors
WO2016049677A1 (en) 2014-10-03 2016-04-07 The Walter And Eliza Hall Institute Of Medical Research Method of treating cancer
WO2016066687A1 (en) * 2014-10-30 2016-05-06 Glaxosmithkline Intellectual Property (No.2) Limited Losmapimod for treating copd
WO2016114655A1 (en) * 2015-01-12 2016-07-21 Ry Pharma B.V. Treating neuromuscular or neurologic disease through reducing gabaergic and/or glycinergic inhibitory neurotransmitter overstimulation
US10538763B2 (en) * 2015-01-16 2020-01-21 Ionis Pharmaceuticals, Inc. Compounds and methods for modulation of DUX4
EP3253874B1 (en) * 2015-02-06 2022-03-23 Association Institut de Myologie Treatment of facioscapulohumeral dystrophy
TWI703138B (en) 2015-02-12 2020-09-01 義大利商吉斯藥品公司 Compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity
JP6701225B2 (en) 2015-03-09 2020-05-27 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Tricyclic DLK inhibitors and uses thereof
WO2016154329A2 (en) * 2015-03-24 2016-09-29 The Trustees Of The University Of Pennsylvania P38 map kinase inhibitors for treating friedreich's ataxia
JP2016193870A (en) 2015-04-01 2016-11-17 国立大学法人広島大学 Therapeutic agent for chronic myelogenous leukemia
US9968604B2 (en) 2015-04-16 2018-05-15 Chiesi Farmaceutici S.P.A. Chromene derivatives as phoshoinositide 3-kinases inhibitors
CN107921106B (en) * 2015-05-20 2023-09-08 住友制药株式会社 Combined use of WT1 antigen peptide and immunomodulator
KR20180014778A (en) * 2015-06-03 2018-02-09 트리아스텍 인코포레이티드 Formulations and uses thereof
WO2016198698A2 (en) 2015-06-12 2016-12-15 Cnic Fundación Centro Nacional De Investigaciones Cardiovasculares Carlos Iii P38 inhibitors for the treatment and prophylaxis of liver cancer
CN108137586B (en) 2015-09-14 2021-04-13 辉瑞大药厂 Novel imidazo [4,5-c ] quinoline and imidazo [4,5-c ] [1,5] naphthyridine derivatives as LRRK2 inhibitors
WO2017075013A1 (en) 2015-10-26 2017-05-04 Eip Pharma, Llc Methods and compositions for recovery from stroke
US9427439B1 (en) 2015-10-26 2016-08-30 Eip Pharma, Llc Methods and compositions for recovery from stroke
EP3383867B1 (en) 2015-12-03 2021-04-14 Chiesi Farmaceutici S.p.A. Compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity
EP3394058B1 (en) 2015-12-23 2020-10-14 Chiesi Farmaceutici S.p.A. N-[3-(3-{4-[[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl} -ureido)-phenyl]-methanesulfonamide derivatives and their use as p38 mapk inhibitors
WO2017110093A1 (en) 2015-12-24 2017-06-29 学校法人同志社 DRUG FOR TREATING OR PREVENTING DISORDER CAUSED BY TGF-β SIGNALS, AND APPLICATION THEREOF
US20190125735A1 (en) 2015-12-29 2019-05-02 Board Of Regents, The University Of Texas System Inhibition of p38 mapk for the treatment of cancer
AU2017213796A1 (en) * 2016-02-01 2018-09-20 President And Fellows Of Harvard College Small molecules for mouse satellite cell proliferation
WO2017134053A1 (en) 2016-02-04 2017-08-10 Chiesi Farmaceutici S.P.A. Pyrazole derivatives as phosphoinositide 3-kinases inhibitors
PE20190376A1 (en) 2016-06-08 2019-03-08 Support Venture Gmbh PHARMACEUTICAL COMBINATIONS FOR THE TREATMENT OF CANCER
GB201611712D0 (en) 2016-07-02 2016-08-17 Hvivo Services Ltd Methods and compounds for the treatment or prevention of severe or persistent influenza
US11123349B2 (en) 2017-02-15 2021-09-21 The University Of Melbourne Method of treatment
WO2019071147A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce dux4 and downstream gene expression for the treatment of fshd
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
US20200297696A1 (en) 2017-11-21 2020-09-24 Saint Louis University P38 inhibitors for the treatment of fshd
US20220017908A1 (en) 2018-11-20 2022-01-20 Fulcrum Therapeutics, Inc. Compositions and methods for increasing fetal hemoglobin and treating sickle cell disease
US20220079951A1 (en) * 2018-12-20 2022-03-17 Saint Louis University Bet inhibitors for modulating dux4 expression in fshd
CN114144230B (en) 2019-03-15 2024-04-23 弗尔康医疗公司 Macrocyclic azolopyridine derivatives as EED and PRC2 modulators
WO2022056266A2 (en) * 2020-09-11 2022-03-17 Arrowhead Pharmaceuticals, Inc. Rnai agents for inhibiting expression of dux4, compositions thereof, and methods of use

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