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PT3691620T - Os inibidores da quinase p38 reduzem a expressão de dux4 e genes a jusante para o tratamento de fshd - Google Patents

Os inibidores da quinase p38 reduzem a expressão de dux4 e genes a jusante para o tratamento de fshd

Info

Publication number
PT3691620T
PT3691620T PT187928122T PT18792812T PT3691620T PT 3691620 T PT3691620 T PT 3691620T PT 187928122 T PT187928122 T PT 187928122T PT 18792812 T PT18792812 T PT 18792812T PT 3691620 T PT3691620 T PT 3691620T
Authority
PT
Portugal
Prior art keywords
fshd
treatment
gene expression
kinase inhibitors
downstream gene
Prior art date
Application number
PT187928122T
Other languages
English (en)
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 PT3691620T publication Critical patent/PT3691620T/pt

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    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5044—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics involving specific cell types
    • G01N33/5061—Muscle cells
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    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • 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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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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PT187928122T 2017-10-05 2018-10-05 Os inibidores da quinase p38 reduzem a expressão de dux4 e genes a jusante para o tratamento de fshd PT3691620T (pt)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201762568673P 2017-10-05 2017-10-05
US201762568754P 2017-10-05 2017-10-05
US201862682565P 2018-06-08 2018-06-08
US201862682563P 2018-06-08 2018-06-08

Publications (1)

Publication Number Publication Date
PT3691620T true PT3691620T (pt) 2022-10-06

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Application Number Title Priority Date Filing Date
PT187928122T PT3691620T (pt) 2017-10-05 2018-10-05 Os inibidores da quinase p38 reduzem a expressão de dux4 e genes a jusante para o tratamento de fshd

Country Status (28)

Country Link
US (5) US11479770B2 (pt)
EP (3) EP3691620B1 (pt)
JP (5) JP7012152B2 (pt)
KR (2) KR20200067170A (pt)
CN (4) CN114748622B (pt)
AU (3) AU2018346709A1 (pt)
BR (2) BR112020006169A2 (pt)
CA (4) CA3077499C (pt)
CL (3) CL2020000911A1 (pt)
CO (2) CO2020005351A2 (pt)
DK (1) DK3691620T3 (pt)
EC (1) ECSP20024210A (pt)
ES (1) ES2927715T3 (pt)
HR (1) HRP20221196T1 (pt)
HU (1) HUE060024T2 (pt)
IL (2) IL273589B (pt)
LT (1) LT3691620T (pt)
MX (2) MX2020003961A (pt)
NZ (1) NZ762856A (pt)
PH (2) PH12020550215B1 (pt)
PL (1) PL3691620T3 (pt)
PT (1) PT3691620T (pt)
RS (1) RS63581B1 (pt)
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Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7012152B2 (ja) 2017-10-05 2022-02-10 フルクラム セラピューティクス，インコーポレイテッド Ｆｓｈｄの治療のためにｄｕｘ４および下流遺伝子発現を低減するｐ３８キナーゼ阻害剤
EP3746082A4 (en) * 2018-02-02 2021-12-08 Fred Hutchinson Cancer Research Center METHOD OF TREATMENT OF FACIOUS CAPULOHUMERAL MUSCULAR DYSTROPHY
TW202112368A (zh) 2019-06-13 2021-04-01 荷蘭商法西歐知識產權股份有限公司 用於治療有關dux4表現之疾病的抑制劑組合
EP3772513A1 (en) * 2019-08-09 2021-02-10 C.N.C.C.S. S.c.a.r.l. Collezione Nazionale Dei Composti Chimici e Centro Screening Shp2 inhibitors
WO2021105474A1 (en) 2019-11-29 2021-06-03 Facio Intellectual Property B.V. New compounds for treatment of diseases related to dux4 expression
US20230271953A1 (en) * 2019-11-29 2023-08-31 Facio Intellectual Property B.V. Novel compounds for treatment of diseases related to DUX4 expression
CN111004802A (zh) * 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） 特异抑制p38MAPK基因表达的shRNA重组载体构建方法与应用
CA3172111A1 (en) 2020-03-19 2021-09-23 Barbora MALECOVA Compositions and methods of treating facioscapulohumeral muscular dystrophy
CN115768487A (zh) * 2020-04-17 2023-03-07 内华达研究与创新公司 用于面肩肱型肌营养不良症的crispr抑制
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
CN118265544A (zh) 2021-09-16 2024-06-28 艾维迪提生物科学公司 治疗面肩肱型肌营养不良的组合物和方法
CN120418231A (zh) * 2022-12-30 2025-08-01 阿勒泰治疗公司 2-取代噻唑和苯并噻唑组合物和作为dux4抑制剂的方法

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
US5670527A (en) 1993-07-16 1997-09-23 Smithkline Beecham Corporation Pyridyl imidazole compounds and compositions
US5593992A (en) 1993-07-16 1997-01-14 Smithkline Beecham Corporation Compounds
US5658903A (en) 1995-06-07 1997-08-19 Smithkline Beecham Corporation Imidazole compounds, compositions and use
US6369068B1 (en) 1995-06-07 2002-04-09 Smithkline Beecham Corporation Amino substituted pyrimidine containing compounds
EP0883402A4 (en) 1996-01-11 1999-08-11 Smithkline Beecham Corp NEW CYCLOALKYL-SUBSTITUTED IMIDAZOLES
AP9700912A0 (en) 1996-01-11 1997-01-31 Smithkline Beecham Corp Novel cycloalkyl substituted imidazoles
ZA97175B (en) 1996-01-11 1997-11-04 Smithkline Beecham Corp Novel substituted imidazole compounds.
WO1997032583A1 (en) 1996-03-08 1997-09-12 Smithkline Beecham Corporation Use of csaidtm compounds as inhibitors of angiogenesis
WO1997034137A2 (en) 1996-03-12 1997-09-18 Smithkline Beecham Corporation Methods of the identification of pharmaceutically active compounds
JP2000506532A (ja) 1996-03-13 2000-05-30 スミスクライン・ビーチャム・コーポレイション サイトカイン介在疾患の治療にて有用な新規ピリミジン化合物
EP0889888A4 (en) 1996-03-25 2003-01-08 Smithkline Beecham Corp NEW TREATMENT OF LESIONS IN THE CENTRAL NERVOUS SYSTEM
US6235760B1 (en) 1996-03-25 2001-05-22 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
JP2002504909A (ja) 1997-06-13 2002-02-12 スミスクライン・ビーチャム・コーポレイション 新規な置換ピラゾールおよびピラゾリン化合物
CA2294137A1 (en) 1997-06-19 1998-12-23 Smithkline Beecham Corporation Novel aryloxy substituted pyrimidine imidazole compounds
US6093742A (en) 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
TW517055B (en) 1997-07-02 2003-01-11 Smithkline Beecham Corp Novel substituted imidazole compounds
AR016294A1 (es) 1997-07-02 2001-07-04 Smithkline Beecham Corp Compuesto de imidazol sustituido, composicion farmaceutica que la contiene, su uso en la fabricacion de un medicamento y procedimiento para supreparacion
GB9721437D0 (en) 1997-10-10 1997-12-10 Glaxo Group Ltd Heteroaromatic compounds and their use in medicine
KR100378937B1 (ko) 1997-10-20 2003-05-09 에프. 호프만-라 로슈 아게 바이사이클릭 키나아제 억제제
US6162613A (en) 1998-02-18 2000-12-19 Vertex Pharmaceuticals, Inc. Methods for designing inhibitors of serine/threonine-kinases and tyrosine kinases
AU765030B2 (en) 1998-05-05 2003-09-04 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
US6340685B1 (en) 1998-05-22 2002-01-22 Scios, Inc. 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
HUP0102058A3 (en) 1998-05-22 2002-05-28 Smithkline Beecham Corp Novel 2-alkyl substituted imidazole compounds, process for their preparation, pharmaceutical compositions containing them and their use
US6589954B1 (en) 1998-05-22 2003-07-08 Scios, Inc. Compounds and methods to treat cardiac failure and other disorders
WO1999061426A1 (en) 1998-05-22 1999-12-02 Scios Inc. Heterocyclic compounds and methods to treat cardiac failure and other disorders
US6867209B1 (en) 1998-05-22 2005-03-15 Scios, Inc. Indole-type derivatives as inhibitors of p38 kinase
JP2002517486A (ja) 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 ｐ３８のインヒビター
ES2221426T3 (es) 1998-08-20 2004-12-16 Smithkline Beecham Corporation Nuevos compuestos de triazol sustituidos.
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
EP1114039A1 (en) 1998-09-18 2001-07-11 Vertex Pharmaceuticals Incorporated INHIBITORS OF p38
WO2000019824A1 (en) 1998-10-07 2000-04-13 Smithkline Beecham Corporation Novel treatment for stroke management
WO2000025791A1 (en) 1998-11-04 2000-05-11 Smithkline Beecham Corporation Pyridin-4-yl or pyrimidin-4-yl substituted pyrazines
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
KR100449215B1 (ko) 1999-04-23 2004-09-18 다케다 야쿠힌 고교 가부시키가이샤 5-피리딜-1,3-아졸 화합물, 이의 제조 방법 및 이의 용도
JP2003500403A (ja) 1999-05-21 2003-01-07 サイオス，インコーポレーテッド ｐ３８キナーゼのインヒビターとしてのインドール型誘導体
ATE312823T1 (de) 1999-07-09 2005-12-15 Boehringer Ingelheim Pharma Verfahren zur herstellung heteroarylsubstituierter ureaverbindungen
US6541477B2 (en) 1999-08-27 2003-04-01 Scios, Inc. Inhibitors of p38-a kinase
CN1382044A (zh) 1999-09-17 2002-11-27 史密丝克莱恩比彻姆公司 细胞因子抑制性抗炎药在鼻病毒感染中的用途
ATE349447T1 (de) 1999-10-21 2007-01-15 Hoffmann La Roche Alkylamino-substituierte bicyclische heterocyclen als p38 protein kinase inhibitoren
AU776250B2 (en) 1999-10-21 2004-09-02 F. Hoffmann-La Roche Ag Heteroalkylamino-substituted bicyclic nitrogen heterocycles as inhibitors of P38 protein kinase
AU1782301A (en) 1999-11-23 2001-06-04 Smithkline Beecham Corporation 3,4-dihydro-(1h)quinazolin-2-one compounds as csbp/p39 kinase inhibitors
AU1783201A (en) 1999-11-23 2001-06-04 Smithkline Beecham Corporation 3,4-dihydro-(1h)quinazolin-2-one compounds as csbp/p38 kinase inhibitors
AU1626001A (en) 1999-11-23 2001-06-04 Smithkline Beecham Corporation 3,4-dihydro-(1h)-quinazolin-2-ones and their use as csbp/p38 kinase inhibitors
JP2003514899A (ja) 1999-11-23 2003-04-22 スミスクライン・ビーチャム・コーポレイション ＣＳＢＰ／ｐ３８キナーゼ阻害剤としての３，４‐ジヒドロ−（１Ｈ）−キナゾリン−２−オン化合物
US6906067B2 (en) 1999-12-28 2005-06-14 Bristol-Myers Squibb Company N-heterocyclic inhibitors of TNF-α expression
DE60043397D1 (de) 1999-12-28 2010-01-07 Pharmacopeia Inc Cytokine, insbesondere tnf-alpha, hemmer
AU2001241927A1 (en) 2000-02-28 2001-09-12 Scios Inc. Inhibitors of p38-alpha kinase
AR030053A1 (es) 2000-03-02 2003-08-13 Smithkline Beecham Corp 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas
CA2415131A1 (en) 2000-07-24 2002-01-31 Boehringer Ingelheim Pharmaceuticals, Inc. Improved 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 (es) 2000-08-22 2002-07-09 Glaxo Group Ltd Derivados de pirazol fusionados como inhibidores de la proteina cinasa
BR0113628A (pt) 2000-08-31 2003-07-01 Hoffmann La Roche 7-oxo-piridopirimidinas como inibidores de uma proliferação celular
ES2243568T3 (es) 2000-08-31 2005-12-01 F. Hoffmann-La Roche Ag 7-oxo-piridopirimidinas.
EP1337255A4 (en) 2000-10-19 2006-01-25 Smithkline Beecham Corp USE OF P38 INHIBITORS FOR THE TREATMENT OF INFLAMMATORY COUGH
EP1337250A2 (en) 2000-10-19 2003-08-27 SmithKline Beecham Corporation Use of p38 inhibitors for the treatment of smoke inhalation
BR0114829A (pt) 2000-10-23 2003-09-23 Smithkline Beecham Corp Novos compostos
GEP20063915B (en) 2000-11-17 2006-09-11 Bristol Myers Squibb Co PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS AND USE THEREOF FOR TREATING p38 KINASE-ASSOCIATED CONDITIONS
AU2002226911A1 (en) 2000-11-20 2002-06-03 Scios Inc. Indol derivative and their use as inhibitors of p38 kinase
JP2004533989A (ja) 2000-11-20 2004-11-11 サイオス インコーポレイテッド ｐ３８キナーゼのピペリジン／ピペラジン型阻害剤
US6890938B2 (en) 2000-11-20 2005-05-10 Scios, Inc. Indole-type inhibitors of p38 kinase
US20020165286A1 (en) 2000-12-08 2002-11-07 Hanne Hedeman Dermal anti-inflammatory composition
EP1345603A4 (en) 2000-12-20 2004-09-08 Merck & Co Inc (HALO-BENZO-CARBONYL) HETEROCYCLO-CONDENSED PHENYL-P38-KINASE INHIBITING AGENTS
WO2002064594A2 (en) 2001-02-12 2002-08-22 F. Hoffmann-La Roche Ag 6-substituted pyrido-pyrimidines
WO2002069892A2 (en) 2001-02-28 2002-09-12 Temple University Of The Commonwealth System Of Higher Education METHOD FOR PROTECTING CELLS AND TISSUES FROM IONIZING RADIATION TOXICITY WITH α, β UNSATURATED ARYL SULFONES
WO2002072576A1 (en) 2001-03-09 2002-09-19 Pfizer Products Inc. Benzimidazole anti-inflammatory compounds
HRP20030719A2 (en) 2001-03-09 2005-04-30 Pfizer Products Inc. Triazolopyridines as anri-inflammatory agents
WO2002076984A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
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
WO2002076396A2 (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
DE60205974T2 (de) 2001-04-04 2006-06-29 Pfizer Products Inc., Groton Neue Benzotriazole mit entzündungshemmender Wirkung
CZ20033119A3 (cs) 2001-04-24 2005-01-12 Merck Patent Gmbh Kombinovaná terapie za použití antiangiogenových činidel a TNF alfa
WO2002090360A1 (en) 2001-05-10 2002-11-14 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
US7271181B2 (en) 2001-05-11 2007-09-18 Vertex Pharmaceuticals Incorporated Inhibitors of p38
DK1397364T3 (da) 2001-05-24 2007-11-26 Lilly Co Eli Hidtil ukendte pyrrolderivater som farmaceutiske midler
JP2005500284A (ja) 2001-06-11 2005-01-06 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 Ｐ３８のイソキノリンインヒビター
US7196095B2 (en) 2001-06-25 2007-03-27 Merck & Co., Inc. (Pyrimidinyl) (phenyl) substituted fused heteroaryl p38 inhibiting and PKG kinase inhibiting compounds
WO2003002544A1 (en) 2001-06-26 2003-01-09 Bristol-Myers Squibb Company N-heterocyclic inhibitors of tnf-alpha expression
AU2002316459A1 (en) 2001-07-11 2003-01-29 Boehringer Ingelheim Pharmaceuticals, Inc. Methods of treating 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
WO2003020715A1 (en) 2001-08-30 2003-03-13 F. Hoffmann-La Roche Ag Aminopyrrole compounds as antiinflammatory agents
CA2459943A1 (en) 2001-09-21 2003-04-03 Merck & Co., Inc. 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
GB0124931D0 (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
GB0124933D0 (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
GB0124928D0 (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
GB0124941D0 (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
JP2005511593A (ja) 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 骨粗鬆症を治療するための組成物及び方法
IL161667A0 (en) 2001-11-09 2004-09-27 Scios Inc Method and composition to treat cystic fibrosis
EP1461758A4 (en) 2001-12-05 2005-10-05 Vertex Pharma CRYSTAL STRUCTURE OF AN MITOGENIC ACTIVATED PROTEIN, KINASE-ACTIVATED PROTEIN, KINASE-2 AND BINDING POCKETS THEREFOR
AU2002366644A1 (en) 2001-12-11 2003-06-23 Boehringer Ingelheim Pharmaceuticals, Inc. Method for administering birb 796 bs
WO2003057197A1 (en) 2002-01-03 2003-07-17 Smithkline Beecham Corporation Novel pharmaceutical dosage forms and method for producing same
EP1467739A4 (en) 2002-01-15 2008-01-09 Merck & Co Inc 17-HYDROXY-4-AZA-ANDROSTAN-3-ONE AS ANDROGEN RECEPTOR MODULATORS
DE10203749A1 (de) 2002-01-31 2003-08-14 Boehringer Ingelheim Pharma Neue Anticholinergika, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
DE10203753A1 (de) 2002-01-31 2003-08-14 Boehringer Ingelheim Pharma Neue Xanthencarbonsäureester, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
DE10203741A1 (de) 2002-01-31 2003-08-14 Boehringer Ingelheim Pharma Neue Fluorencarbonsäureester, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
US20040023961A1 (en) 2002-02-11 2004-02-05 Bayer Corporation Aryl ureas with raf kinase and angiogenisis inhibiting activity
SI1474395T1 (sl) * 2002-02-12 2008-02-29 Smithkline Beecham Corp Nikotinamidni derivati, uporabni kot inhibitorji p38
DE60323946D1 (de) 2002-03-07 2008-11-20 Hoffmann La Roche Bicyclische pyridin- und pyrimidininhibitoren von p38-kinase
MXPA04008800A (es) 2002-03-13 2004-11-26 Merck & Co Inc Derivados de 4-azasteroides fluorados como moduladores del receptor de androgenos.
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
EP1492790A1 (en) 2002-04-03 2005-01-05 F. Hoffmann-La Roche Ag Imidazo fused compounds
KR20040101398A (ko) 2002-04-05 2004-12-02 베링거 잉겔하임 파르마 게엠베하 운트 코 카게 점액 과다분비의 치료방법
US20030225089A1 (en) 2002-04-10 2003-12-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and p38 kinase inhibitors
DE10216339A1 (de) 2002-04-13 2003-10-23 Boehringer Ingelheim Pharma Neue Ester hydroxy-substituierter Stickstoffheterocyclen, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
AU2003229689A1 (en) 2002-04-15 2003-10-27 Glaxo Group Limited A method of identifying a modudator for a serine/theronine kinase
JP4603268B2 (ja) 2002-04-19 2010-12-22 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー 新規化合物
ATE418546T1 (de) 2002-04-23 2009-01-15 Bristol Myers Squibb Co Als kinase inhibitoren geeignete arylketonpyrrolotriazin-verbindungen
US7388009B2 (en) 2002-04-23 2008-06-17 Bristol-Myers Squibb Company Heteroaryl-substituted pyrrolo-triazine compounds useful as kinase inhibitors
WO2003090912A1 (en) 2002-04-23 2003-11-06 Bristol-Myers Squibb Company Pyrrolo-triazine aniline compounds useful as kinase inhibitors
GB0209891D0 (en) 2002-04-30 2002-06-05 Glaxo Group Ltd Novel compounds
AU2003223754B2 (en) 2002-04-30 2007-08-16 Merck Sharp & Dohme Corp. 4-azasteroid derivatives as androgen receptor modulators
EP1511738A4 (en) 2002-05-17 2007-05-09 Scios Inc TREATMENT OF FIBROPROLIFERATIVE DISEASES USING TGF BETA INHIBITORS
TW200400034A (en) 2002-05-20 2004-01-01 Bristol Myers Squibb Co Pyrazolo-pyrimidine aniline compounds useful as kinase inhibitors
AU2003239508A1 (en) 2002-05-21 2003-12-12 Bristol-Myers Squibb Company Indole compounds useful as impdh inhibitors
EP1515727A4 (en) 2002-06-11 2009-04-08 Merck & Co Inc (HALO-BENZO CARBONYL) HETEROBICYCLIC P38 KINASE INHIBITION
AU2003245989A1 (en) 2002-07-09 2004-01-23 Boehringer Ingelheim Pharma Gmbh And Co. Kg Pharmaceutical compositions of anticholinergics and p38 kinase inhibitors in the treatment of respiratory diseases
AU2003256783A1 (en) 2002-07-25 2004-02-16 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
BR0313297A (pt) 2002-08-06 2005-06-21 Hoffmann La Roche 6-alcóxi-pirido-pirimidinas como inibidores de p-38 map cinase
AU2003257991A1 (en) 2002-08-08 2004-02-25 Boehringer Ingelheim Pharmaceuticals, Inc. Fluorinated phenyl-naphthalenyl-urea compounds as inhibitors of cytokines involved in inflammatory processes
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
JP2006500365A (ja) 2002-08-14 2006-01-05 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド ｐ３８ＭＡＰキナーゼインヒビターを用いた抗凝固及び線維素溶解療法
CA2497240A1 (en) 2002-08-29 2004-03-11 Andrew Asher Protter Methods of promoting osteogenesis
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
US7005523B2 (en) 2002-08-30 2006-02-28 Pfizer Inc. Cycloalkyl-[4-(trifluorophenyl)-oxazol-5yl]-triazolo-pyridines
US7012143B2 (en) 2002-08-30 2006-03-14 Dombroski Mark A Cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines
PA8579601A1 (es) 2002-08-30 2004-05-07 Pfizer Prod Inc Compuestos antiinflamatorios de di y trifloruro-triazolo-piridinas
WO2004020438A2 (en) 2002-08-30 2004-03-11 Pfizer Products Inc. Novel processes and intermediates for preparing triazolo-pyridines
WO2004022712A2 (en) 2002-09-03 2004-03-18 Scios Inc. INDOLE-TYPE DERIVATIVES AS INHIBITORS OF p38 KINASE
CA2497951A1 (en) 2002-09-05 2004-03-18 Scios Inc. Treatment of pain by inhibition of p38 map kinase
WO2004021979A2 (en) 2002-09-06 2004-03-18 Smithkline Beecham Corporation PYRROLO[2, 3-d]PYRIMIDINE-4-YL AND PURIN-6-YL UREA COMPOUNDS
US7115644B2 (en) 2002-09-13 2006-10-03 Boehringer Ingelheim Pharmaceuticals Inc. Heterocyclic compounds
ATE370139T1 (de) 2002-09-17 2007-09-15 Lilly Co Eli Pyrazolopyridin derivate als tgf beta hemmstoffe zur behandlung von krebs
KR20050053694A (ko) 2002-09-27 2005-06-08 얀센 파마슈티카 엔.브이. 3, 4-이치환된 피롤 및 염증 질환을 치료하기 위한 그의용도
US7041693B2 (en) 2002-10-04 2006-05-09 Bristol-Myers Squibb Company Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
JP2006505552A (ja) 2002-10-09 2006-02-16 サイオス インク． ｐ３８キナーゼ阻害剤としてのアザインドール系誘導体
US20050288299A1 (en) 2002-10-09 2005-12-29 Mavunkel Babu J Azaindole derivatives as inhibitors of p38 kinase
EP1581217A4 (en) 2002-11-01 2007-07-11 Merck & Co Inc CARBONYLAMINO-BENZIMIDAZOLE DERIVATIVES AS MODULATORS OF ANDROGENIC RECEPTORS
ATE427951T1 (de) 2002-11-18 2009-04-15 Hoffmann La Roche Diazinopyrimidine und ihre verwendung als proteinkinaseinhibitoren
DE10255040A1 (de) 2002-11-26 2004-06-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Carbaminsäureester mit anticholinerger Wirksamkeit
AU2003299652A1 (en) 2002-12-06 2004-06-30 Scios Inc. Methods for treating diabetes
US7105537B2 (en) 2003-01-28 2006-09-12 Bristol-Myers Squibb Company 2-substituted cyclic amines as calcium sensing receptor modulators
PL378121A1 (pl) 2003-02-05 2006-03-06 Bristol-Myers Squibb Company Sposób wytwarzania pirolotriazynowych inhibitorów kinazy
CA2755297A1 (en) 2003-02-10 2004-08-26 Vertex Pharmaceuticals Incorporated 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
JP2006517580A (ja) 2003-02-14 2006-07-27 ファイザー・プロダクツ・インク 抗炎症化合物としてのトリアゾロピリジン
CA2515939A1 (en) 2003-02-14 2004-09-02 Smithkline Beecham Corporation Novel compounds
AU2004215644B2 (en) 2003-02-27 2010-09-02 Palau Pharma, S.A. Pyrazolopyridine derivates
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
CA2517517C (en) 2003-03-03 2012-12-18 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
MXPA05010975A (es) 2003-04-16 2005-11-28 Hoffmann La Roche Derivados de (6-(fenoxi)-pirido[3,4-d]pirimidin-2-il)-amina como inhibidores de p38 cinasa para el tratamiento de condiciones inflamatorias como artritis reumatoide.
BRPI0409580A (pt) 2003-04-16 2006-04-18 Hoffmann La Roche compostos de quinazolina
RU2342365C2 (ru) 2003-05-01 2008-12-27 Бристол-Маерс Сквибб Компани Арилзамещенные пиразоламиды в качестве ингибиторов киназ
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
ATE384697T1 (de) 2003-06-04 2008-02-15 Pfizer 2-amino-pyridin-derivate als beta-2 adrenoreceptor agonisten
BRPI0411825B8 (pt) 2003-06-26 2021-05-25 Novartis Ag inibidores de p38 quinase a base de heterociclo de 5 elementos, seus processos de preparação e seus usos, bem como composição farmacêutica
US7696217B2 (en) 2003-06-30 2010-04-13 Merck Sharp & Dohme Corp. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
EP1660184A4 (en) 2003-06-30 2008-05-14 Merck & Co Inc 17-ACETAMIDO-4-AZASTEROIDE DERIVATIVES AS ANDROGEN RECEPTOR MODULATORS
US20060234931A1 (en) 2003-07-17 2006-10-19 Biggs William H Iii Treatment of diseases with kinase inhibitors
GB0317516D0 (en) 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as PDE4 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
JP2007507204A (ja) 2003-07-29 2007-03-29 ブリストル−マイヤーズ　スクイブ　カンパニー サイクリン依存性キナーゼモデュレーションのバイオマーカー
GB0318814D0 (en) 2003-08-11 2003-09-10 Smithkline Beecham Corp Novel compounds
NL1026826C2 (nl) 2003-08-13 2007-01-04 Pharmacia Corp Gesubstitueerde pyridinonen.
EP1658060A2 (en) 2003-08-22 2006-05-24 Boehringer Ingelheim Pharmaceuticals Inc. Methods of treating copd and pulmonary hypertension
WO2005023201A2 (en) 2003-09-09 2005-03-17 Medarex, Inc. Methods for treating rheumatoid arthritis
CA2537660A1 (en) 2003-09-10 2005-03-24 Merck & Co., Inc. 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators
MXPA06002853A (es) 2003-09-11 2006-06-14 Kemia Inc Inhibidores citoquina.
WO2005032481A2 (en) 2003-09-30 2005-04-14 Scios Inc. Quinazoline derivatives as medicaments
WO2005032551A1 (en) 2003-09-30 2005-04-14 Scios Inc. TREATMENT OF CARDIOVASCULAR DISEASE WITH INHIBITORS OF p38 KINASE
EP1675830A4 (en) 2003-09-30 2008-08-20 Scios Inc HETEROCYCLIC AMIDES AND SULFONAMIDES
US7419978B2 (en) 2003-10-22 2008-09-02 Bristol-Myers Squibb Company Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors
EP1685131B1 (en) 2003-11-13 2007-03-07 F. Hoffmann-La Roche AG Hydroxyalkyl substituted pyrido-7-pyrimidin-7-ones
EP1538201A1 (en) 2003-12-02 2005-06-08 F.Hoffmann-La Roche Ag Method for the recombinant production and purification of protein kinases
CA2547837A1 (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
MXPA06007023A (es) 2003-12-18 2006-08-31 Pfizer Prod Inc Metodos para tratar la inflamacion aguda en animales con inhibidores de p38 map cinasa.
US20060058296A1 (en) 2003-12-24 2006-03-16 Scios, Inc. Treatment of osteolytic lesions associated with multiple myeloma by inhibition of p38 map kinase
US20060052390A1 (en) 2003-12-24 2006-03-09 Scios, Inc. Treatment of multiple myeloma by p38 MAP kinase and proteasome inhibition
BRPI0417213A (pt) 2003-12-24 2007-02-06 Scios Inc tratamento de gliomas malìgnos com inibidores de tgf-beta
US20060079461A1 (en) 2003-12-24 2006-04-13 Scios, Inc. Treatment of multiple myeloma by inhibition of p38 MAP kinase
GB0402138D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
GB0402140D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
GB0402137D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
CA2554878A1 (en) 2004-01-30 2005-08-18 Merck Patent Gmbh Bisarylurea derivatives
GB0402143D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
TWI332003B (en) 2004-01-30 2010-10-21 Lilly Co Eli Kinase inhibitors
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
WO2005085248A1 (en) 2004-02-27 2005-09-15 F.Hoffmann-La Roche Ag Heteroaryl-fused pyrazolo derivatives
AU2005219518A1 (en) 2004-02-27 2005-09-15 F. Hoffmann-La Roche Ag Indazole derivatives and pharmaceutical compositions containing them
EP1574501A1 (en) 2004-03-11 2005-09-14 Pfizer Limited Quinolinone derivatives, pharmaceutical compositions containing them and their use
AU2005227192A1 (en) 2004-03-11 2005-10-06 Kythera Biopharmaceuticals, Inc. Compositions and methods for preventing and treating skin and hair conditions
EP1577292A1 (en) 2004-03-17 2005-09-21 Pfizer Limited Phenylaminoethanol derivatives as beta2 receptor agonists
EP1577291A1 (en) 2004-03-17 2005-09-21 Pfizer Limited Phenylethanolamine derivatives as beta-2 agonists
CA2564564A1 (en) 2004-04-28 2005-11-10 Merck & Co., Inc. Fluorinated 4-azasteroids as androgen receptor modulators
CA2566677A1 (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
EP1609789A1 (en) 2004-06-23 2005-12-28 Eli Lilly And Company Ureido-pyrazole derivatives and their use as kinase inhibitors
ATE400567T1 (de) 2004-06-23 2008-07-15 Lilly Co Eli Kinaseinhibitoren
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
PE20060421A1 (es) 2004-08-12 2006-06-01 Bristol Myers Squibb Co Procedimiento para preparar un compuesto de pirrolotriazina anilina como inhibidores de cinasa
JP4084836B2 (ja) 2004-08-12 2008-04-30 ファイザー・インク ｐ３８ＭＡＰキナーゼインヒビターとしてのトリアゾロピリジニルスルファニル誘導体
CN101005841A (zh) 2004-08-25 2007-07-25 默克公司 雄激素受体调节剂
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
PE20060493A1 (es) 2004-10-05 2006-09-03 Smithkline Beecham Corp Compuestos derivados de bifenil (di o tri) carboxamidas como inhibidores de serina/treonina quinasa p38
US8003657B2 (en) 2004-10-13 2011-08-23 Merck Patent Gmbh Heterocyclic substituted bisarylurea derivatives
ES2400689T3 (es) 2004-10-18 2013-04-11 Amgen, Inc Compuestos de tiadiazol y métodos de uso
CN101052398A (zh) 2004-10-29 2007-10-10 默克公司 作为雄激素受体调节剂的n－(吡啶－3－基)－2－苯基丁酰胺
WO2006048266A2 (en) 2004-11-04 2006-05-11 Roche Diagnostics Gmbh Gene expression profiling of leukemias with mll gene rearrangements
US20060258582A1 (en) 2004-11-04 2006-11-16 Scios, Inc. Method of treating myelodysplastic syndromes
WO2006051373A1 (en) 2004-11-12 2006-05-18 Pfizer Limited Compounds for the treatment of diseases
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
CN101056842A (zh) 2004-11-16 2007-10-17 默克公司 治疗中风的(2r)－2－丙基辛酸前药
WO2006058023A2 (en) 2004-11-23 2006-06-01 Merck & Co., Inc. 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
US20060154939A1 (en) 2004-12-24 2006-07-13 Boehringer Ingelheim International Gmbh Medicaments for the Treatment or Prevention of Fibrotic Diseases
PE20061155A1 (es) 2004-12-24 2006-12-16 Boehringer Ingelheim Int Derivados de indolinona como agentes para el tratamiento o la prevencion de enfermedades fibroticas
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
CN101080404B (zh) 2004-12-28 2011-06-08 Aska制药株式会社 嘧啶基异噁唑衍生物
US20060178388A1 (en) 2005-02-04 2006-08-10 Wrobleski Stephen T Phenyl-substituted pyrimidine compounds useful as kinase inhibitors
WO2006089798A1 (en) 2005-02-28 2006-08-31 Merckle Gmbh 2-sulfinyl- and 2-sulfonyl-substituted imidazole derivatives and their use as cytokine inhibitors
US7759337B2 (en) 2005-03-03 2010-07-20 Amgen Inc. Phthalazine compounds and methods of use
TWI389690B (zh) 2005-03-25 2013-03-21 Glaxo Group Ltd 新穎化合物（一）
US7423042B2 (en) 2005-03-25 2008-09-09 Glaxo Group Limited Compounds
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
US20060264431A1 (en) 2005-05-11 2006-11-23 Array Biopharma Inc. P38 inhibitors and methods of use thereof
EP1885181A2 (en) 2005-05-23 2008-02-13 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
JP2009503078A (ja) 2005-08-02 2009-01-29 メルク エンド カムパニー インコーポレーテッド アンドロゲン受容体モジュレーターとしてのｎ−（ピリジン−４−イル）−２−フェニルブタンアミド
CA2618614A1 (en) 2005-08-12 2007-02-22 Merck & Co., Inc. Heterobicyclic compounds useful as p38 kinase inhibiting agents
AU2006283476A1 (en) 2005-08-22 2007-03-01 Amgen Inc. Bis-aryl urea compounds for the treatment of protein kinase-mediated diseaes
JP2009506007A (ja) 2005-08-25 2009-02-12 エフ．ホフマン−ラ ロシュ アーゲー ｐ３８ＭＡＰキナーゼ阻害剤及びその使用方法
KR20080031460A (ko) 2005-08-25 2008-04-08 에프. 호프만-라 로슈 아게 Ｐ38 ｍａｐ 키나아제 저해제 및 이의 사용 방법
EP1919470A1 (en) 2005-08-25 2008-05-14 F.Hoffmann-La Roche Ag FUSED PYRAZOLE AS p38 MAP KINASE INHIBITORS
RU2008110941A (ru) 2005-08-25 2009-09-27 Ф.Хоффманн-Ля Рош Аг (Ch) ИНГИБИТОРЫ КИНАЗЫ p38 МАР И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
MX2008002590A (es) 2005-08-25 2008-03-18 Hoffmann La Roche Inhibidores de la p38-map-cinasa y metodos para el uso de los mismos.
KR20080049758A (ko) 2005-09-01 2008-06-04 아스텔라스세이야쿠 가부시키가이샤 통증 치료용으로 사용되는 피리다지논 유도체
GEP20104880B (en) 2005-09-21 2010-01-11 Pfizer Ltd Carboxamide derivatives as muscarinic receptor antagonists
WO2007038444A2 (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 (es) 2005-10-28 2007-06-15 Lilly Co Eli Inhibidores de cinasa
AR056582A1 (es) 2005-10-28 2007-10-10 Lilly Co Eli COMPUESTOS DE PIRAZOLIL UREA CON ACTIVIDAD INHIBITORIA DE CINASA P38 Y FORMULACIoN FARMACÉUTICA QUE LO COMPRENDE
WO2007056016A2 (en) 2005-11-02 2007-05-18 Kemia, Inc. Bisamide cytokine inhibitors
CA2624625A1 (en) 2005-11-04 2007-05-10 Pfizer Limited Tetrahydronaphthyridine derivative
WO2007054896A1 (en) 2005-11-08 2007-05-18 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 (es) 2005-11-15 2007-08-09 Glaxo Group Ltd Sal tosilato de 8-(2,6-difluorofenil)-4-(4-fluoro-2-metilfenil)-2-{[2-hidroxi-1-(hidroximetil)etil]amino}pirido[2,3-]pirimidin-7(8h)-ona
NL2000323C2 (nl) 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.
WO2007075896A2 (en) 2005-12-22 2007-07-05 Kemia, Inc. Heterocyclic cytokine inhibitors
ES2389062T3 (es) 2006-01-18 2012-10-22 Amgen, Inc Compuestos de tiazol como inhibidores de proteína cinasa B (PKB)
AU2007210073B2 (en) 2006-01-31 2011-10-06 Array Biopharma Inc. Kinase inhibitors and methods of use thereof
WO2007091152A1 (en) 2006-02-09 2007-08-16 Pfizer Limited Triazolopyridine compounds
CA2640665A1 (en) 2006-02-10 2007-08-16 Pfizer Products Inc. Pyridinone pyrazole urea and pyrimidinone pyrazole urea derivatives
GB0603684D0 (en) 2006-02-23 2006-04-05 Novartis Ag Organic compounds
AU2007223901A1 (en) 2006-03-07 2007-09-13 Vertex Pharmaceuticals Incorporated Use of VX-702 for treating rheumatoid arthritis
JP2009535295A (ja) 2006-03-07 2009-10-01 ブリストル−マイヤーズ スクイブ カンパニー キナーゼ阻害剤として有用なピロロトリアジンアニリンプロドラッグ化合物
BRPI0708956A2 (pt) 2006-03-20 2011-06-28 Pfizer Ltd derivado de amina
US8026233B2 (en) 2006-03-29 2011-09-27 Array Biopharma Inc. P38 inhibitors and methods of use thereof
CA2649000A1 (en) 2006-04-12 2007-10-18 Merck Patent Gesellschaft Mit Beschraenkter Haftung N-oxides of heterocyclic substituted bisarylureas for treating kinase-mediated diseases
CA2649543A1 (en) 2006-04-21 2007-11-01 Amgen Inc. Thieno-[2,3-d]pyrimidine and thieno-pyridazine compounds and methods of use
WO2007146712A2 (en) 2006-06-09 2007-12-21 Kemia, Inc. Therapy using cytokine inhibitors
EP2034838A4 (en) 2006-06-16 2012-01-04 Glaxo Group Ltd NOVEL CONNECTIONS
GB0612026D0 (en) 2006-06-16 2006-07-26 Smithkline Beecham Corp New use
US20090318424A1 (en) 2006-06-16 2009-12-24 Mauro Corsi Novel compounds
JP2009542817A (ja) 2006-06-16 2009-12-03 グラクソ グループ リミテッド 新規化合物
JPWO2008001929A1 (ja) 2006-06-28 2009-12-03 あすか製薬株式会社 炎症性腸疾患の処置剤
US8207203B2 (en) 2006-06-28 2012-06-26 Aska Pharmaceutical Co., Ltd. Pyridylisoxazole derivatives
US7935709B2 (en) 2006-07-17 2011-05-03 Amgen Inc. 2-quinazolinone compounds and methods of use
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
US20090247624A1 (en) 2006-07-28 2009-10-01 Onconova Therapeutics Inc. Formulations of radioprotective alpha beta unsaturated aryl sulfones
PE20080906A1 (es) 2006-08-17 2008-07-05 Kemia Inc Derivados heteroarilo como inhibidores de citocina
WO2008024391A1 (en) 2006-08-22 2008-02-28 Scios Inc. Pharmaceutical formulations of an indole-type derivative and related methods of use
BRPI0719270A2 (pt) 2006-10-04 2014-03-11 Pfizer Ltd Derivados de sulfonamida como agonistas adrenérgicos e antagonistas muscarínicos
EP2086973B1 (en) 2006-10-11 2012-01-25 Amgen Inc., Imidazo- and triazolo-pyridine compounds and methods of use therof
JP2010506914A (ja) 2006-10-18 2010-03-04 メルク エンド カムパニー インコーポレーテッド アンドロゲン受容体モジュレーターとしての２−ヒドロキシ−２−フェニル／チオフェニルプロピオンアミド
EP2086641A2 (en) 2006-10-26 2009-08-12 Boehringer Ingelheim International GmbH Egfr kinase inhibitor combinations for the 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
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
AR064307A1 (es) 2006-12-13 2009-03-25 Gilead Sciences Inc Monofosfatos utiles para el tratamiento de la inflamacion pulmonar y broncoconstriccion, formulaciones aerosolicas que los contienen, y metodo de preparacion.
CA2672719A1 (en) 2006-12-19 2008-06-26 F. Hoffmann-La Roche Ag Pyrazolo [3, 4 -d] pyrimidine p38 map kinase inhibitors
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
AU2008215659B2 (en) 2007-02-16 2012-11-01 Aska Pharmaceutical Co., Ltd. Pharmaceutical composition comprising microparticle oily suspension
US20100015218A1 (en) 2007-02-16 2010-01-21 Vasant Jadhav Compositions and methods for potentiated activity of biologically active molecules
WO2008104473A2 (en) 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag Pyrazolopyriidine derivatives and their use as kinase inhibitors
KR101120227B1 (ko) 2007-03-16 2012-03-20 화이자 리미티드 5-［3-（3-하이드록시페녹시）아제티딘-1-일］-5-메틸-2,2-다이페닐-헥산아마이드의 염산염
US7846944B2 (en) 2007-05-07 2010-12-07 Amgen Inc. Pyrazolo-pyridinone compounds and methods of use thereof
AU2008248296B2 (en) 2007-05-07 2011-12-01 Amgen Inc. Pyrazolo-pyridinone and pyrazolo-pyrazinone compounds as P38 modulators, process for their preparation, and their pharmaceutical use
CA2692713A1 (en) 2007-07-17 2009-01-22 Amgen Inc. Heterocyclic modulators of pkb
AU2008276512A1 (en) 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole 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
US8202899B2 (en) 2007-07-25 2012-06-19 Array Biopharma Inc. Pyrazole urea derivatives used as kinase inhibitors
EP2200969A2 (en) 2007-09-14 2010-06-30 Pfizer Limited Novel compounds active as muscarinic receptor antagonists
WO2009038784A1 (en) 2007-09-21 2009-03-26 Amgen Inc. Triazole fused heteroaryl compounds as p38 kinase inhibitors
AP2010005267A0 (en) 2007-11-30 2010-06-30 Pfizer Ltd Novel glucocorticoid receptor agonists
WO2009074518A1 (en) 2007-12-12 2009-06-18 Glaxo Group Limited Combinations of prolinamide p2x7 modulators with further therapeutic agents
GB0724258D0 (en) 2007-12-12 2008-01-30 Glaxo Group Ltd Novel combinations
WO2009078992A1 (en) 2007-12-17 2009-06-25 Amgen Inc. Linear tricyclic compounds as p38 kinase inhibitors
WO2009094556A2 (en) 2008-01-25 2009-07-30 Bristol-Myers Squibb Pharma Company Identification of predictive markers of response to dasatinib in human colon cancer
JP2011512209A (ja) 2008-02-20 2011-04-21 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 粉末吸入器
WO2009117156A1 (en) 2008-03-21 2009-09-24 Amgen Inc. Pyrazolo-pyrazinone compounds and methods of use thereof
JP2009263234A (ja) 2008-04-21 2009-11-12 Ranbaxy Lab Ltd ホスホジエステラーゼタイプｉｖ阻害剤の組成物
AR072008A1 (es) 2008-06-13 2010-07-28 Merck & Co Inc Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38
JP2011525183A (ja) 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 キナーゼ阻害剤として有用なイミダゾピリジンおよびイミダゾピラジン化合物
EP2307411B1 (en) 2008-06-20 2014-01-01 Bristol-Myers Squibb Company Triazolopyridine compounds useful as kinase inhibitors
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
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
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
PE20110312A1 (es) 2008-07-15 2011-06-25 Pfizer Ltd Compuestos piperidinicos de esteres del acido bifenil-2-ilcarbamico como antagonistas del receptor muscarinico m3
WO2010025201A1 (en) 2008-08-29 2010-03-04 Amgen Inc. Pyridazino- pyridinone compounds for the treatment of protein kinase mediated diseases.
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
WO2010038428A1 (ja) 2008-09-30 2010-04-08 武田薬品工業株式会社 タキサン系抗がん剤の置き換え薬
EP2206534A1 (de) 2008-10-09 2010-07-14 c-a-i-r biosciences GmbH Dibenzocycloheptanonderivate und pharmazeutische Mittel, welche diese Verbindungen enthalten
WO2010042646A1 (en) 2008-10-10 2010-04-15 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
US20120129820A1 (en) 2009-02-09 2012-05-24 Boehringer Ingelheim International Gmbh New pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
EP2396302A2 (en) 2009-02-13 2011-12-21 Vertex Pharmceuticals Incorporated Processes for producing phenyl-6-(1-(phenyl)ureido)nicotinamides)
CA2752544A1 (en) 2009-02-13 2010-08-19 Vertex Pharmaceuticals Incorporated Solid forms of 2-(2, 4-difluorophenyl)-6-(1-(2,6-difluorophenyl)ureido)nicotinamide
GB0902648D0 (en) 2009-02-17 2009-04-01 Argenta Discovery Ltd Pharmaceutical compounds and compositions
CA2752693A1 (en) 2009-02-17 2010-08-26 Chiesi Farmaceutici S.P.A. Triazolopyridine derivatives as p38 map kinase inhibitors
WO2010120963A1 (en) 2009-04-16 2010-10-21 Bristol-Myers Squibb Company Tablet formulation for p38 inhibitor and method
WO2010129208A1 (en) 2009-05-05 2010-11-11 Merck Sharp & Dohme Corp. P38 kinase inhibiting agents
EP2470534A4 (en) 2009-08-24 2013-02-27 Merck Sharp & Dohme JAK INHIBITION FOR BLOCKING TOXICITY ASSOCIATED WITH RNA INTERFERENCE
EP3011970A3 (en) 2009-10-22 2016-06-08 F. Hoffmann-La Roche AG 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
EP2549867A4 (en) 2010-03-24 2013-08-14 Onconova Therapeutics Inc COMPOSITIONS AND METHODS FOR PREVENTING AND TREATING WOUNDS
EA023535B9 (ru) 2010-03-26 2016-11-30 Онконова Терапьютикс, Инк. Композиция водного радиопротекторного фармацевтического раствора и способ предотвращения, снижения или исключения эффектов ионизирующей радиации
GB201009731D0 (en) 2010-06-10 2010-07-21 Pulmagen Therapeutics Inflamma Kinase inhibitors
PE20130376A1 (es) 2010-06-28 2013-03-30 Merck Patent Gmbh [1,8]naftiridinas sustituidas por 2,4-diarilo como inhibidores de quinasas para uso contra el cancer
ES2535656T3 (es) 2010-07-05 2015-05-13 Merck Patent Gmbh Derivados de bipiridilo útiles para el tratamiento de enfermedades inducidas por quinasas
WO2012031057A1 (en) 2010-09-01 2012-03-08 Bristol-Myers Squibb Company Bms- 582949 for the treatment of resistant rheumatic disease
WO2012074933A1 (en) 2010-11-29 2012-06-07 Genentech, Inc. Methods for detecting neurodegenerative diseases or disorders
TWI410425B (zh) 2010-12-03 2013-10-01 Lilly Co Eli 唑并［５，４－ｂ］吡啶－５－基化合物
ES2542647T3 (es) 2011-03-09 2015-08-07 Merck Patent Gmbh Derivados de pirido[2,3 b]pirazina y sus usos terapéuticos
CN103842362B (zh) 2011-05-09 2017-05-24 爱普制药有限责任公司 用于治疗阿尔茨海默氏病的组合物和方法
MX346559B (es) 2011-06-10 2017-03-24 Chiesi Farm Spa Compuestos con actividad antagonista de los receptores muscarinicos y actividad agonista del receptor beta2 adrenergico.
EP3111937B1 (en) 2011-07-08 2020-06-17 Helmholtz-Zentrum für Infektionsforschung GmbH Medicament for treatment of liver cancer
EA026297B1 (ru) 2011-11-11 2017-03-31 Эли Лилли Энд Компани Комбинированная терапия рака яичников
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
KR20140103925A (ko) 2011-12-09 2014-08-27 키에시 파르마슈티시 엣스. 피. 에이. 4-히드록시-1,2,3,4-테트라히드로나프탈렌-1-일 우레아 및 호흡기 질환의 치료에서의 이들의 용도
SG10201604656YA (en) 2011-12-09 2016-07-28 Chiesi Farma Spa Kinase inhibitors
DK2788349T3 (en) 2011-12-09 2017-01-30 Chiesi Farm Spa kinase inhibitors
WO2013106643A2 (en) 2012-01-12 2013-07-18 Yale University Compounds & methods for the enhanced degradation of targeted proteins & other polypeptides by an e3 ubiquitin ligase
AU2013226163B2 (en) 2012-03-01 2017-06-08 Array Biopharma Inc. Crystalline forms of 1- (3 -tert-butyl- 1 - p-tolyl- 1H- pyrazol- 5 -yl) -3- (5-fluoro-2- (1- ( 2 - hydroxyethyl) - indazol- 5 -yloxy) benzyl) urea hydrochloride
BR112014023107B1 (pt) 2012-03-20 2021-08-10 Novartis Ag Usos de derivados de pirazol, e composição farmacêutica
WO2013174780A1 (en) 2012-05-22 2013-11-28 F. Hoffmann-La Roche Ag Substituted dipyridylamines and uses thereof
CA2876139A1 (en) * 2012-06-07 2013-12-12 President And Fellows Of Harvard College Nanotherapeutics for drug targeting
JP2015522612A (ja) * 2012-07-17 2015-08-06 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ 急性冠症候群の治療におけるニコチンアミド誘導体
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
WO2014033449A1 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
WO2014033446A1 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
GB201215357D0 (en) 2012-08-29 2012-10-10 Respivert Ltd Compounds
EP2890695A2 (en) 2012-08-29 2015-07-08 Respivert Limited Kinase inhibitors
US9155747B2 (en) 2012-09-13 2015-10-13 Chiesi Farmaceutici S.P.A. Isoxazolidine derivatives
WO2014076484A1 (en) 2012-11-16 2014-05-22 Respivert Limited Kinase inhibitors
CN104968346B (zh) 2012-11-30 2017-06-27 弗·哈夫曼-拉罗切有限公司 酪氨酸蛋白激酶抑制剂
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
JP6433922B2 (ja) 2013-02-27 2018-12-05 アレイ バイオファーマ、インコーポレイテッド インダゾール誘導体の調製に使用するための中間体およびその調製方法
US20160016934A1 (en) 2013-03-14 2016-01-21 Respivert Limited Kinase inhibitors
GB201305714D0 (en) 2013-03-28 2013-05-15 Ucl Business Plc Method
HK1221175A1 (zh) * 2013-04-01 2017-05-26 Pulmatrix Operating Company, Inc. 噻托溴铵乾粉
KR102283876B1 (ko) 2013-04-02 2021-07-29 옥슬러 액퀴지션즈 리미티드 키나제 저해제로서 유용한 우레아 유도체
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
RU2015151834A (ru) 2013-06-06 2017-06-08 КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. Ингибиторы киназы
WO2014195402A1 (en) 2013-06-06 2014-12-11 Chiesi Farmaceutici S.P.A. Kinase inhibitors
KR20160016973A (ko) 2013-06-06 2016-02-15 키에시 파르마슈티시 엣스. 피. 에이. P38 - map 키나아제 억제제로서 [1, 2, 4] 트리아졸로 [4, 3 - a] 피리딘의 유도체
KR20160030206A (ko) 2013-07-10 2016-03-16 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 사구체 질환을 치료하는데 사용하기 위한 로스마피모드
WO2015006753A2 (en) 2013-07-12 2015-01-15 The Regents Of The University Of California Therapies for diseases caused by arthropod-borne parasites
US9814728B2 (en) 2013-09-20 2017-11-14 Saint Louis University Inhibition of DUX4 expression using bromodomain and extra-terminal domain protein inhibitors (BETi)
JP6730701B2 (ja) * 2013-11-14 2020-07-29 学校法人同志社 細胞増殖促進または細胞障害抑制による角膜内皮治療薬
CN113717162A (zh) 2013-12-20 2021-11-30 奥苏拉收购有限公司 用作激酶抑制剂的脲衍生物
MX2016008110A (es) 2013-12-20 2016-08-19 Hoffmann La Roche Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos.
JP6630280B2 (ja) 2014-02-14 2020-01-15 レスピバート・リミテツド 抗炎症化合物としての芳香族複素環化合物
GEAP201814248A (en) 2014-02-19 2018-04-10 H Lundbeck As 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease
CN107073121A (zh) 2014-06-13 2017-08-18 基因泰克公司 治疗及预防癌症药物抗性的方法
CN106659788A (zh) 2014-06-13 2017-05-10 基因泰克公司 治疗和预防癌症耐药性的方法
WO2016007616A1 (en) 2014-07-09 2016-01-14 Eip Pharma, Llc Methods for treating neurologic disorders
MA40775A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivé d'acide 4-(4-(4-phényluréido-naphtalén -1-yl) oxy-pyridin-2-yl) amino-benzoïque utilisé en tant qu'inhibiteur de la kinase p38
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
ES2918975T3 (es) * 2015-02-06 2022-07-21 Association Inst De Myologie Tratamiento de la distrofia facioescapulohumeral
TWI703138B (zh) 2015-02-12 2020-09-01 義大利商吉斯藥品公司 具有蕈毒鹼受體拮抗劑及β２腎上腺素受體促效劑活性之化合物
EP3268373B1 (en) 2015-03-09 2022-04-27 F. Hoffmann-La Roche AG Tricyclic dlk inhibitors and uses thereof
US12370180B2 (en) * 2015-03-24 2025-07-29 The Trustees Of The University Of Pennsylvania P38 map kinase inhibitors for treating Friedreich's ataxia
JP2016193870A (ja) 2015-04-01 2016-11-17 国立大学法人広島大学 慢性骨髄性白血病治療剤
US9968604B2 (en) 2015-04-16 2018-05-15 Chiesi Farmaceutici S.P.A. Chromene derivatives as phoshoinositide 3-kinases inhibitors
JP6515182B2 (ja) * 2015-05-20 2019-05-15 大日本住友製薬株式会社 Ｗｔ１抗原ペプチドおよび免疫調節剤の併用
CA3254279A1 (en) * 2015-06-03 2025-03-18 Triastek, Inc. PHARMACEUTICAL FORMS AND RELATED USES
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
RU2722149C1 (ru) 2015-09-14 2020-05-27 Пфайзер Инк. Новые производные имидазо[4,5-c] хинолинов и имидазо[4,5-c][1,5] нафтиридинов в качестве ингибиторов LRRK2
EP3368040B1 (en) 2015-10-26 2022-08-17 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
WO2017093208A1 (en) 2015-12-03 2017-06-08 Chiesi Farmaceutici S.P.A. Compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity
WO2017108736A1 (en) 2015-12-23 2017-06-29 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
US10980787B2 (en) 2015-12-24 2021-04-20 The Doshisha Drug for treating or preventing disorder caused by TGF-B signals, and application thereof
CN109310768A (zh) 2015-12-29 2019-02-05 得克萨斯大学体系董事会 用于治疗癌症的p38 mapk的抑制
AU2017213796A1 (en) 2016-02-01 2018-09-20 President And Fellows Of Harvard College Small molecules for mouse satellite cell proliferation
EP3411375B1 (en) 2016-02-04 2020-08-05 Chiesi Farmaceutici S.p.A. Pyrazole derivatives as phosphoinositide 3-kinases inhibitors
EP3468604B1 (en) 2016-06-08 2021-01-20 Support-Venture GmbH Pharmaceutical combinations for treating 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
EP3582781A4 (en) 2017-02-15 2020-12-09 The University of Melbourne A method of treatment
JP7012152B2 (ja) * 2017-10-05 2022-02-10 フルクラム セラピューティクス，インコーポレイテッド Ｆｓｈｄの治療のためにｄｕｘ４および下流遺伝子発現を低減するｐ３８キナーゼ阻害剤
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
AU2019384547B2 (en) 2018-11-20 2025-10-30 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
TWI845638B (zh) 2019-03-15 2024-06-21 美商弗爾康醫療公司 Ｅｅｄ及ｐｒｃ２調節劑之巨環唑并吡啶衍生物
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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