EA202192575A1 - Соединения dbait в сочетании с ингибиторами киназ для лечения рака - Google Patents

Соединения dbait в сочетании с ингибиторами киназ для лечения рака

Info

Publication number
EA202192575A1
EA202192575A1 EA202192575A EA202192575A EA202192575A1 EA 202192575 A1 EA202192575 A1 EA 202192575A1 EA 202192575 A EA202192575 A EA 202192575A EA 202192575 A EA202192575 A EA 202192575A EA 202192575 A1 EA202192575 A1 EA 202192575A1
Authority
EA
Eurasian Patent Office
Prior art keywords
dbait
combination
compounds
kinase inhibitors
cancer treatment
Prior art date
Application number
EA202192575A
Other languages
English (en)
Inventor
Франсуаза Боно
Жиль Фавр
Оливье Кальвейрак
Original Assignee
Онксео
Инсерм (Энститю Насьональ Де Ля Сантэ Э Де Ля Решерш Медикаль)
Юниверсите Поль Сабатье Тулуз Iii
Энститю Клодиус Рего
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 Онксео, Инсерм (Энститю Насьональ Де Ля Сантэ Э Де Ля Решерш Медикаль), Юниверсите Поль Сабатье Тулуз Iii, Энститю Клодиус Рего filed Critical Онксео
Publication of EA202192575A1 publication Critical patent/EA202192575A1/ru

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/554—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/661—Phosphorus acids or esters thereof not having P—C bonds, e.g. fosfosal, dichlorvos, malathion or mevinphos
    • A61K31/6615—Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/543—Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • A61K47/544—Phospholipids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • 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
    • C12N15/111—General methods applicable to biologically active non-coding nucleic acids
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/10—Type of nucleic acid
    • C12N2310/13—Decoys
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/31—Chemical structure of the backbone
    • C12N2310/315—Phosphorothioates
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2310/00—Structure or type of the nucleic acid
    • C12N2310/30—Chemical structure
    • C12N2310/35—Nature of the modification
    • C12N2310/351—Conjugate
    • C12N2310/3515—Lipophilic moiety, e.g. cholesterol
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N2320/00—Applications; Uses
    • C12N2320/30—Special therapeutic applications
    • C12N2320/31—Combination therapy

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Genetics & Genomics (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Biotechnology (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Microbiology (AREA)
  • Plant Pathology (AREA)
  • Physics & Mathematics (AREA)
  • Biochemistry (AREA)
  • Botany (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Изобретение относится к комбинации соединения Dbait с ингибитором протеинкиназы для лечения рака.
EA202192575A 2019-03-21 2020-03-19 Соединения dbait в сочетании с ингибиторами киназ для лечения рака EA202192575A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP19305349 2019-03-21
PCT/EP2020/057555 WO2020188015A1 (en) 2019-03-21 2020-03-19 A dbait molecule in combination with kinase inhibitor for the treatment of cancer

Publications (1)

Publication Number Publication Date
EA202192575A1 true EA202192575A1 (ru) 2022-01-14

Family

ID=66103004

Family Applications (1)

Application Number Title Priority Date Filing Date
EA202192575A EA202192575A1 (ru) 2019-03-21 2020-03-19 Соединения dbait в сочетании с ингибиторами киназ для лечения рака

Country Status (12)

Country Link
US (1) US20220143049A1 (ru)
EP (1) EP3942045A1 (ru)
JP (1) JP2022526713A (ru)
KR (1) KR20210142154A (ru)
CN (1) CN114364798A (ru)
AU (1) AU2020242287A1 (ru)
BR (1) BR112021018168B1 (ru)
CA (1) CA3129665A1 (ru)
EA (1) EA202192575A1 (ru)
IL (1) IL284856A (ru)
MX (1) MX2021009863A (ru)
WO (1) WO2020188015A1 (ru)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019175132A1 (en) * 2018-03-13 2019-09-19 Onxeo A dbait molecule against acquired resistance in the treatment of cancer
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
KR102657354B1 (ko) * 2021-06-08 2024-04-15 한국과학기술원 Syk 저해제를 포함하는 대장암 예방 또는 치료용 병용투여 조성물
WO2023129667A1 (en) 2021-12-30 2023-07-06 Biomea Fusion, Inc. Pyrazine compounds as inhibitors of flt3

Family Cites Families (637)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2229515T3 (es) 1997-07-01 2005-04-16 Warner-Lambert Company Llc Derivados 4-bromo o 4-yodo del acido fenilamino benzhidroxamico y su uso como inhibidores de la mek.
US5932580A (en) 1997-12-01 1999-08-03 Yissum Research And Development Company Of The Hebrew University Of Jerusalem PDGF receptor kinase inhibitory compounds their preparation and compositions
AU3653099A (en) 1998-04-17 1999-11-08 Parker Hughes Institute Btk inhibitors and methods for their identification and use
SK16352000A3 (sk) 1998-05-04 2002-07-02 Zentaris Ag Indolové deriváty, spôsob ich výroby, ich použitie na liečivá obsahujúce tieto zlúčeniny
ID30439A (id) 1999-01-13 2001-12-06 Warner Lambert Co Benzoheterosiklus dan penggunaannya sebagai penghambat mek
CA2348236A1 (en) 1999-01-13 2000-07-20 Stephen Douglas Barrett 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors
AU2482800A (en) 1999-01-13 2000-08-01 Warner-Lambert Company Sulphohydroxamic acids and sulphohydroxamates and their use as mek inhibitors
CA2349832A1 (en) 1999-01-13 2000-07-20 Warner-Lambert Company Benzenesulfonamide derivatives and their use as mek inhibitors
CA2362380A1 (en) 1999-03-19 2000-09-28 Bristol-Meyers Squibb Pharma Company Amino-thio-acrylonitriles as mek inhibitors
GB9910577D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
EP1184376B1 (en) 1999-06-09 2005-02-02 Yamanouchi Pharmaceutical Co. Ltd. Novel heterocyclic carboxamide derivatives
GB9918035D0 (en) 1999-07-30 1999-09-29 Novartis Ag Organic compounds
DE60014130T2 (de) 1999-10-06 2006-03-09 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Heterocyclische verbindungen verwendbar als tyrosinkinase inhibitoren
UA74803C2 (ru) 1999-11-11 2006-02-15 Осі Фармасьютікалз, Інк. Стойкий полиморф гидрохлорида n-(3-этинилфенил)-6,7-бис(2-метоксиэтокси)-4-хиназолинамина, способ его получения (варианты) и фармацевтическое применение
HUP0203895A3 (en) 1999-12-24 2004-09-28 Aventis Pharma Ltd West Mallin Substituted azaindoles and pharmaceutical compositions containing them and their use
AU2968701A (en) 2000-01-24 2001-07-31 Genzyme Corporation Jak/stat pathway inhibitors and the uses thereof
HRP20020751B1 (hr) 2000-02-15 2011-01-31 Sugen Pirolom supstituirani 2-indolinoni kao inhibitori protein kinaze
US7087608B2 (en) 2000-03-03 2006-08-08 Robert Charles Atkins Use of PDGF receptor tyrosine kinase inhibitors for the treatment of diabetic nephropathy
JP2003527379A (ja) 2000-03-15 2003-09-16 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー Mex阻害物質としての5−アミド置換ジアリールアミン類
AR035851A1 (es) 2000-03-28 2004-07-21 Wyeth Corp 3-cianoquinolinas, 3-ciano-1,6-naftiridinas y 3-ciano-1,7-naftiridinas como inhibidoras de proteina quinasas
AR028261A1 (es) 2000-03-28 2003-04-30 Wyeth Corp Inhibidores triciclicos de la proteina quinasa
DE10017480A1 (de) 2000-04-07 2001-10-11 Transmit Technologietransfer Verwendung von Substanzen, die als MEK Inhibitor wirken, zur Herstellung eines Arneimittels gegen DNA- und RNA-Viren
JP2001302667A (ja) 2000-04-28 2001-10-31 Bayer Ag イミダゾピリミジン誘導体およびトリアゾロピリミジン誘導体
AU2002249261A1 (en) 2001-03-06 2002-09-19 Axxima Pharmaceuticals Ag Use of mek inhibitors for treating inflammation and virus induced hemorrhagic shock
EP1389209B1 (en) 2001-04-24 2009-04-08 Purdue Research Foundation Folate mimetics and folate-receptor binding conjugates thereof
TWI238824B (en) 2001-05-14 2005-09-01 Novartis Ag 4-amino-5-phenyl-7-cyclobutyl-pyrrolo[2,3-d]pyrimidine derivatives
JP2004530730A (ja) 2001-06-29 2004-10-07 アブ サイエンス 腫瘍の血管新生を治療するための強力で選択的かつ非毒性のc−kit阻害剤の使用法
JP2005503361A (ja) 2001-06-29 2005-02-03 アブ サイエンス 肥満細胞症治療のための強力で選択的かつ非毒性のc−kit阻害剤の使用
WO2003003006A2 (en) 2001-06-29 2003-01-09 Ab Science New potent, selective and non toxic c-kit inhibitors
DE60225590T2 (de) 2001-09-20 2008-09-25 Ab Science C-kithemmer zur behandlung von bakteriellen infektionen
US7015231B2 (en) 2001-09-27 2006-03-21 Smithkline Beecham Corporation Chemical compounds
US20030158195A1 (en) 2001-12-21 2003-08-21 Cywin Charles L. 1,6 naphthyridines useful as inhibitors of SYK kinase
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
SG2013013339A (en) 2002-03-13 2014-12-30 Array Biopharma Inc N3 alkylated benzimidazole derivatives as mek inhibitors
WO2003077855A2 (en) 2002-03-13 2003-09-25 Array Biopharma, Inc N3 alkylated benzimidazole derivatives as mek inhibitors
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
DK1487424T3 (da) 2002-03-15 2007-01-08 Novartis Ag 4-(4-Methylpiperazin-1-ylmethyl)-N-(4-methyl-3-(4-pyridin-3-yl)-pyrimidin-2-yl-amino)phenyl-benzamid til behandling af Ang II-medierede sygdomme
CN1665808A (zh) 2002-05-06 2005-09-07 沃泰克斯药物股份有限公司 噻二唑或噁二唑及其作为jak蛋白激酶抑制剂的用途
CA2487679A1 (en) 2002-05-30 2003-12-11 Vertex Pharmaceuticals Incorporated Inhibitors of jak and cdk2 protein kinases
GB0215823D0 (en) 2002-07-09 2002-08-14 Astrazeneca Ab Quinazoline derivatives
CA2493701A1 (en) 2002-07-25 2004-02-05 Pfizer Products Inc. Isothiazole derivatives useful as anticancer agents
MXPA05001277A (es) 2002-08-02 2005-10-06 Ab Science 2-(3-aminoaril)amino-4-aril-tiazoles y su uso como inhibidores del c-kit.
EP1562911B1 (en) 2002-11-01 2010-01-06 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of jak and other protein kinases
US7259161B2 (en) 2002-11-04 2007-08-21 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
US7348335B2 (en) 2002-11-05 2008-03-25 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of JAK and other protein kinases
US7098332B2 (en) 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
EP1604665B1 (en) 2003-03-10 2011-05-11 Eisai R&D Management Co., Ltd. C-kit kinase inhibitor
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
US7872014B2 (en) 2003-07-23 2011-01-18 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
KR20060054412A (ko) 2003-08-01 2006-05-22 와이어쓰 홀딩스 코포레이션 암 치료 및 억제용 표피 성장인자 수용체 키나제 억제제와세포독성제의 배합물 용도
ATE542801T1 (de) 2003-08-15 2012-02-15 Novartis Ag Zur behandlung von neoplastischen krankheiten, entzündlichen erkrankungen und erkrankungen des immunsystems geeignete 2,4-pyrimidindiamine
BRPI0413746A (pt) 2003-08-21 2006-10-24 Osi Pharm Inc composto ou um seu n-óxido ou seu sal farmaceuticamente aceitável, composição, e, método de tratamento de distúrbio hiperproliferativo
JP4795237B2 (ja) 2003-08-21 2011-10-19 オーエスアイ・フアーマシユーテイカルズ・エル・エル・シー N−置換ピラゾリル−アミジル−ベンズイミダゾリルc−Kit阻害剤
AP2006003552A0 (en) 2003-08-21 2006-04-30 Osi Pharm Inc N3 - substituted imidazopyridine C-kit inhibitors.
US7144907B2 (en) 2003-09-03 2006-12-05 Array Biopharma Inc. Heterocyclic inhibitors of MEK and methods of use thereof
US7538120B2 (en) 2003-09-03 2009-05-26 Array Biopharma Inc. Method of treating inflammatory diseases
DE10342794A1 (de) 2003-09-16 2005-04-21 Basf Ag Sekretion von Proteinen aus Hefen
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
JP4931419B2 (ja) 2003-09-19 2012-05-16 中外製薬株式会社 新規4−フェニルアミノ−ベンズアルドオキシム誘導体並びにそのmek阻害剤としての使用
EA200600495A1 (ru) 2003-09-23 2006-10-27 Новартис Аг Комбинация ингибитора vegf рецептора с химиотерапевтическим агентом
ES2372694T3 (es) 2003-10-15 2012-01-25 OSI Pharmaceuticals, LLC Inhibidores de tirosina cinasa de imidazo[1,5-a]pirazina.
EP1526177A1 (en) 2003-10-24 2005-04-27 Institut Curie Nucleic acids useful for triggering tumor cell lethality
US7476729B2 (en) * 2003-10-24 2009-01-13 Institut Curie Dbait and uses thereof
MY141220A (en) 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
KR101190912B1 (ko) 2003-11-19 2012-10-12 어레이 바이오파마 인크. Mek의 헤테로시클릭 억제제 및 그의 사용 방법
DE102004001607A1 (de) 2004-01-09 2005-08-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Arzneimittelkombinationen auf der Basis von Scopin- oder Tropensäureestern mit EGFR-Kinase-Hemmern
CN1934107A (zh) 2004-01-30 2007-03-21 Ab科学公司 作为酪氨酸激酶抑制剂的2-(3-取代芳基)氨基-4-芳基-噻唑
KR100799534B1 (ko) 2004-02-27 2008-01-31 에자이 알앤드디 매니지먼트 가부시키가이샤 신규 피리딘 유도체 및 피리미딘 유도체(1)
ES2364340T3 (es) 2004-03-30 2011-08-31 Vertex Pharmaceuticals Incorporated Azaindoles útiles como inhibidores de jak y otras proteína quinasas.
FR2868422B1 (fr) 2004-03-31 2006-07-14 Aventis Pharma Sa Nouveaux derives pyrrolo(2,3-b) pyridine, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
MXPA06011423A (es) 2004-04-02 2007-01-23 Osi Pharm Inc Inhibidores de proteina cinasa heterobiciclica sustituida en el anillo 6,6-biciclico.
WO2005123696A1 (en) 2004-06-15 2005-12-29 Astrazeneca Ab Substituted quinazolones as anti-cancer agents
TW200616974A (en) 2004-07-01 2006-06-01 Astrazeneca Ab Chemical compounds
JP5704785B2 (ja) 2004-07-19 2015-04-22 ザ・ジョンズ・ホプキンス・ユニバーシティ 免疫抑制のためのflt3阻害剤
MY144232A (en) 2004-07-26 2011-08-15 Chugai Pharmaceutical Co Ltd 5-substituted-2-phenylamino benzamides as mek inhibitors
WO2007040469A2 (en) 2005-09-15 2007-04-12 Kosak Ken M Chloroquine coupled compositions and methods for their synthesis
US20090118261A1 (en) 2004-08-31 2009-05-07 Astrazeneca Ab Quinazolinone derivatives and their use as b-raf inhibitors
AU2005278961A1 (en) 2004-09-01 2006-03-09 Astrazeneca Ab Quinazolinone derivatives and their use as B-Raf inhibitors
PT1791830E (pt) 2004-09-17 2011-04-04 Vertex Pharma Compostos de diaminotriazole úteis como inibidores de proteína-quinase
CA2583096A1 (en) 2004-10-15 2006-04-20 Astrazeneca Ab Quinoxalines as b raf inhibitors
EP1838675A1 (en) 2004-11-24 2007-10-03 Laboratoires Serono S.A. Novel 4-arylamino pyridone derivatives as mek inhibitors for the treatment of hyperproliferative disorders
RU2007123675A (ru) 2004-11-24 2008-12-27 Новартис АГ (CH) Комбинации ингибиторов jak
CA2589770A1 (en) 2004-12-01 2006-06-08 Osi Pharmaceuticals, Inc. N-substituted benzimidazolyl c-kit inhibitors and combinatorial benzimidazole library
ES2330872T3 (es) 2004-12-01 2009-12-16 Merck Serono Sa Derivados de (1,2,4)triazolo(4,3-a)piridina para el tratamiento de enfermedades hiperproliferativas.
TW200634003A (en) 2004-12-22 2006-10-01 Astrazeneca Ab Chemical compounds
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
WO2006079791A1 (en) 2005-01-25 2006-08-03 Astrazeneca Ab Chemical compounds
ES2426482T3 (es) 2005-01-27 2013-10-23 Kyowa Hakko Kirin Co., Ltd. Inhibidor de IGF-1R
DK2383268T3 (en) 2005-02-04 2015-09-14 Astrazeneca Ab PYRAZOLYLAMINOPYRIDINDERIVATER useful as kinase inhibitors
KR20070104936A (ko) 2005-02-16 2007-10-29 아스트라제네카 아베 화합물
KR101362621B1 (ko) 2005-02-16 2014-02-13 아스트라제네카 아베 화합물
BRPI0607062A2 (pt) 2005-02-28 2009-08-04 Japan Tobacco Inc composto de aminopiridina com atividade inibidora de syk, composição farmacêutica e agente terapêutico compreendendo os mesmos
AU2006229343A1 (en) 2005-03-28 2006-10-05 Kirin Pharma Kabushiki Kaisha Thienopyridine derivative, or quinoline derivative, or quinazoline derivative, having c-Met autophosphorylation inhibiting potency
MX2007012392A (es) 2005-04-04 2007-12-05 Ab Science Derivados de oxazol sustituidos y su uso como inhibidores de tirosina cinasa.
KR20080011199A (ko) 2005-04-19 2008-01-31 교와 핫꼬 고교 가부시끼가이샤 질소 함유 복소환 화합물
CA2608009A1 (en) 2005-05-16 2006-11-23 Astrazeneca Ab Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors
TWI441637B (zh) 2005-05-18 2014-06-21 Array Biopharma Inc Mek雜環抑制劑及其使用方法
US7541367B2 (en) 2005-05-31 2009-06-02 Janssen Pharmaceutica, N.V. 3-benzoimidazolyl-pyrazolopyridines useful in treating kinase disorders
WO2006133417A1 (en) 2005-06-07 2006-12-14 Valeant Pharmaceuticals International Phenylamino isothiazole carboxamidines as mek inhibitors
US20070021435A1 (en) 2005-06-10 2007-01-25 Gaul Michael D Aminopyrimidines as kinase modulators
TW200738638A (en) 2005-06-23 2007-10-16 Merck & Co Inc Tyrosine kinase inhibitors
RU2408584C2 (ru) 2005-06-23 2011-01-10 Мерк Шарп Энд Домэ Корп. Ингибиторы тирозинкиназы
TW200740820A (en) 2005-07-05 2007-11-01 Takeda Pharmaceuticals Co Fused heterocyclic derivatives and use thereof
EP1904065A2 (en) 2005-07-14 2008-04-02 AB Science Use of dual c-kit/fgfr3 inhibitors for treating multiple myeloma
JP5071374B2 (ja) 2005-07-14 2012-11-14 アステラス製薬株式会社 ヘテロ環ヤヌスキナーゼ3阻害剤
WO2007009681A1 (en) 2005-07-15 2007-01-25 Glaxo Group Limited 1 , 1-DIOXID0-2 , 3-DIHYDRO-l , 2-BENZISOTHIAZ0L-6-YL-1H-INDAZOL-4-YL-2 , 4-PYRIMIDINEDI AMINE DERIVATIVES
WO2007028445A1 (en) 2005-07-15 2007-03-15 Glaxo Group Limited 6-indolyl-4-yl-amino-5-halogeno-2-pyrimidinyl-amino derivatives
MX2008002114A (es) 2005-07-21 2008-04-17 Ardea Biosciences Inc Inhibidores de n-(arilamino)-sulfonamida de mek.
TWI377198B (en) 2005-08-24 2012-11-21 Eisai R&D Man Co Ltd Novel pyridine derivatives and pyrimidine derivatives (3)
CA2621503C (en) 2005-09-07 2014-05-20 Rigel Pharmaceuticals, Inc. Triazole derivatives useful as axl inhibitors
FR2891273B1 (fr) 2005-09-27 2007-11-23 Aventis Pharma Sa NOUVEAUX DERIVES BENZIMIDAZOLES ET BENZOTHIAZOLES, LEUR PREPARATION ET LEUR UTILISATION PHARMACEUTIQUE NOTAMMENT COMME INHIBITEURS DE CMet
BRPI0616575A2 (pt) 2005-09-27 2011-06-21 Irm Llc compostos e composições contendo diarilamina, seu uso como moduladores de receptores de c-kit bem como método para sua produção
NZ567140A (en) 2005-10-07 2011-09-30 Exelixis Inc Azetidines as MEK inhibitors for the treatment of proliferative diseases
JP2009511527A (ja) 2005-10-13 2009-03-19 グラクソ グループ リミテッド Syk阻害物質としてのピロロピリミジン誘導体
PT1963302E (pt) 2005-12-05 2013-04-09 Pfizer Prod Inc Polimorfos de um inibidor de c-met/hgfr
HUE028588T2 (hu) 2005-12-13 2016-12-28 Incyte Holdings Corp Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok
US20080299113A1 (en) 2005-12-19 2008-12-04 Arnold Lee D Combined treatment with and composition of 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitor and anti-cancer agents
WO2007071951A1 (en) 2005-12-21 2007-06-28 Astrazeneca Ab Tosylate salt of 6- (4-br0m0-2-chl0r0phenylamin0) -7-fluoro-n- (2-hydroxyethoxy) -3-methyl-3h-benzimi dazole- 5 - carboxamide , mek inhibitor useful in the treatment of cancer
CA2632929A1 (en) 2005-12-22 2007-06-28 Astrazeneca Ab Quinazoline derivatives, process for their preparation and their use as anti-cancer agents
NZ592968A (en) 2006-01-17 2012-08-31 Vertex Pharma Azaindoles substituted with either triazine or pyrimidine useful as inhibitors of janus kinases consisting of JAK1, JAK2, JAK3, and TYK2
FR2896503B1 (fr) 2006-01-23 2012-07-13 Aventis Pharma Sa Nouveaux derives soufres d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
FR2896504B1 (fr) 2006-01-23 2012-07-13 Aventis Pharma Sa Nouveaux derives d'uree cyclique, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
WO2007085540A1 (en) 2006-01-27 2007-08-02 Glaxo Group Limited 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives
GB0601962D0 (en) 2006-01-31 2006-03-15 Ucb Sa Therapeutic agents
TW200740776A (en) 2006-02-06 2007-11-01 Osi Pharm Inc N-phenylbenzotriazolyl c-kit inhibitors
KR20090007347A (ko) 2006-03-22 2009-01-16 버텍스 파마슈티칼스 인코포레이티드 증식성 장애의 치료를 위한 c-MET 단백질 키나제 억제제
JP2009532449A (ja) 2006-04-05 2009-09-10 アストラゼネカ アクチボラグ 抗癌活性のある置換キナゾリン
WO2007113558A2 (en) 2006-04-05 2007-10-11 Astrazeneca Ab Quinazolinone derivatives having b-raf inhibitory activity
JP2009532475A (ja) 2006-04-05 2009-09-10 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 ヤヌスキナーゼの阻害剤として有用なデアザプリン
US20090203718A1 (en) 2006-04-13 2009-08-13 Smithkline Beecham (Cork) Ltd. Cancer treatment method
AU2007237901B2 (en) 2006-04-18 2012-07-05 Ardea Biosciences, Inc. Pyridone sulfonamides and pyridone sulfamides as MEK inhibitors
JP2009534364A (ja) 2006-04-18 2009-09-24 アストラゼネカ アクチボラグ キナゾリン−4−オン誘導体、それらの製造方法およびそれらを含有する医薬組成物
EA200802050A1 (ru) 2006-04-19 2009-04-28 Лаборатуар Сероно Са Новые гетероарилзамещенные ариламинопиридиновые производные в качестве мек ингибиторов
JP5182088B2 (ja) 2006-04-19 2013-04-10 アステラス製薬株式会社 アゾールカルボキサミド誘導体
EP2397138B1 (en) 2006-04-20 2013-12-11 Janssen Pharmaceutica NV Aromatic amide derivatives as C-KIT kinase inhibitors
PL2026775T3 (pl) 2006-05-09 2015-12-31 Novaremed Ltd Zastosowanie inhibitorów kinazy tyrozynowej Syk w leczeniu komórkowych zaburzeń proliferacyjnych
CN104706637A (zh) 2006-05-18 2015-06-17 卫材R&D管理有限公司 针对甲状腺癌的抗肿瘤剂
WO2008005877A2 (en) 2006-06-30 2008-01-10 Board Of Regents, The University Of Texas System Inhibitors of c-kit and uses thereof
TW200813021A (en) 2006-07-10 2008-03-16 Merck & Co Inc Tyrosine kinase inhibitors
DE602007004638D1 (de) 2006-07-20 2010-03-18 Amgen Inc Benzoädüisoxazol-derivate als c-kit-tyrosinkinase-hemmer zur behandlung von erkrankungen im zusammenhang mit der überproduktion von histamin
WO2008016192A2 (en) 2006-08-04 2008-02-07 Takeda Pharmaceutical Company Limited Fused heterocyclic derivative and use thereof
WO2008020203A1 (en) 2006-08-17 2008-02-21 Astrazeneca Ab Pyridinylquinaz0linamine derivatives and their use as b-raf inhibitors
CN101500548A (zh) 2006-08-18 2009-08-05 弗·哈夫曼-拉罗切有限公司 用于体内递送多核苷酸的多缀合物
ATE535520T1 (de) 2006-08-23 2011-12-15 Eisai R&D Man Co Ltd Salz eines phenoxypyridinderivats oder kristall davon und verfahren zu dessen herstellung
CL2007002617A1 (es) 2006-09-11 2008-05-16 Sanofi Aventis Compuestos derivados de pirrolo[2,3-b]pirazin-6-ilo; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar inflamacion de las articulaciones, artritis reumatoide, tumores, linfoma de las celulas del manto.
EP2529621B1 (en) 2006-09-22 2016-10-05 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
US8097630B2 (en) 2006-10-10 2012-01-17 Rigel Pharmaceuticals, Inc. Pinane-substituted pyrimidinediamine derivatives useful as Axl inhibitors
CN101558068A (zh) 2006-10-16 2009-10-14 诺瓦提斯公司 用作蛋白激酶抑制剂的苯乙酰胺类
JPWO2008047831A1 (ja) 2006-10-17 2010-02-25 協和発酵キリン株式会社 Jak阻害剤
TW200829566A (en) 2006-12-08 2008-07-16 Astrazeneca Ab Chemical compounds
WO2008076415A1 (en) 2006-12-14 2008-06-26 Exelixis, Inc. Methods of using mek inhibitors
WO2008076143A1 (en) 2006-12-18 2008-06-26 Osi Pharmaceuticals, Inc. Combination of igfr inhibitor and anti-cancer agent
US7737149B2 (en) 2006-12-21 2010-06-15 Astrazeneca Ab N-[5-[2-(3,5-dimethoxyphenyl)ethyl]-2H-pyrazol-3-yl]-4-(3,5-dimethylpiperazin-1-yl)benzamide and salts thereof
WO2008080134A2 (en) 2006-12-22 2008-07-03 Rigel Pharmaceuticals, Inc. 4-amin0-2- (hetero) arylamino-5- (hetero) arylthiazoles useful as axl inhibitors
CN101679408B (zh) 2006-12-22 2016-04-27 Astex治疗学有限公司 作为fgfr抑制剂的双环杂环化合物
CA2710230C (en) 2006-12-29 2016-02-23 Rigel Pharmaceuticals, Inc. Bridged bicyclic aryl and bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
CA2710051C (en) 2006-12-29 2017-05-16 Rigel Pharmaceuticals, Inc. Substituted triazoles useful as axl inhibitors
RS53281B (sr) 2006-12-29 2014-08-29 Rigel Pharmaceuticals Inc. Policiklični heteroaril supstituisani triazoli koji su korisni kao axl inhibitori
ES2406930T3 (es) 2006-12-29 2013-06-10 Rigel Pharmaceuticals, Inc. Triazoles sustituidos con arilo bicíclico y heteroarilo bicíclico útiles como inhibidores de AXL
CN101622248B (zh) 2006-12-29 2013-04-17 里格尔制药公司 用作axl抑制剂的n3-杂芳基取代的三唑和n5-杂芳基取代的三唑
EP1944369A1 (en) 2007-01-12 2008-07-16 The Centre National de la Recherche Scientifique Dbait and its standalone uses thereof
ES2547303T3 (es) 2007-01-19 2015-10-05 Ardea Biosciences, Inc. Inhibidores de MEK
EP2114983B8 (en) 2007-02-07 2015-02-18 The Regents of the University of Colorado, A Body Corporate Axl tyrosine kinase inhibitors and methods of making and using the same
AU2008217931A1 (en) 2007-02-23 2008-08-28 Eisai R & D Management Co., Ltd. Pyridine or pyrimidine derivative having excellent cell growth inhibition effect and excellent anti-tumor effect on cell strain having amplification of HGFR gene
JPWO2008111441A1 (ja) 2007-03-05 2010-06-24 協和発酵キリン株式会社 医薬組成物
HUE029188T2 (en) 2007-03-12 2017-03-28 Ym Biosciences Australia Pty Phenylamino-pyrimidine compounds and their use
KR20090129488A (ko) 2007-03-22 2009-12-16 버텍스 파마슈티칼스 인코포레이티드 야누스 키나아제의 억제제로서 유용한 n-헤테로사이클릭 화합물
EP2139487B1 (en) 2007-03-28 2015-11-11 Pharmacyclics LLC Inhibitors of bruton's tyrosine kinase
AU2008240188A1 (en) 2007-04-13 2008-10-23 Supergen, Inc. Axl kinase inhibitors useful for the treatment of cancer or hyperproliferative disorders
UA99459C2 (en) 2007-05-04 2012-08-27 Астразенека Аб 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
GB0714384D0 (en) 2007-07-23 2007-09-05 Ucb Pharma Sa theraputic agents
CN103479604B (zh) 2007-07-30 2016-08-10 阿迪生物科学公司 作为mek抑制剂的包括多晶型物的n-(芳氨基)磺酰胺衍生物和组合物、其使用方法和制备方法
CA2694646C (en) 2007-07-30 2017-09-05 Ardea Biosciences, Inc. Combinations of mek inhibitors and raf kinase inhibitors and uses thereof
PA8792501A1 (es) 2007-08-09 2009-04-23 Sanofi Aventis Nuevos derivados de 6-triazolopiridacina-sulfanil benzotiazol y bencimidazol,su procedimiento de preparación,su aplicación como medicamentos,composiciones farmacéuticas y nueva utilización principalmente como inhibidores de met.
ES2452965T3 (es) 2007-09-05 2014-04-03 Rigel Pharmaceuticals, Inc. Sal de xinafoato de N4-[(2,2-difluoro-4H-benzo[1,4]oxazin-3-ona)-6-il]-5-fluoro-N2-[3-(metilaminocarbonilmetilenoxi)fenil]-2,4-pirimidindiamina
JP5587193B2 (ja) 2007-10-23 2014-09-10 エフ.ホフマン−ラ ロシュ アーゲー 新規なキナーゼ阻害剤
SI2206707T1 (sl) 2007-10-24 2014-11-28 Astellas Pharma Inc. Azolkarboksamidna spojina ali njena sol
CA2704052C (en) 2007-10-26 2015-04-21 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors
SI2215094T1 (sl) 2007-11-15 2016-05-31 Ym Biosciences Australia Pty Ltd N vsebujoče heterociklične spojine
US20110039856A1 (en) 2007-11-29 2011-02-17 Pfizer Inc. Polymorphs of a c-met/hgfr inhibitor
WO2009093008A1 (en) 2008-01-21 2009-07-30 Ucb Pharma S.A. Thieno-pyridine derivatives as mek inhibitors
GB0801416D0 (en) 2008-01-25 2008-03-05 Piramed Ltd Pharmaceutical compounds
US8436171B2 (en) 2008-02-01 2013-05-07 Akinion Pharmaceuticals Ab Amino substituted pyrazines as inhibitors or protein kinases
ES2420846T3 (es) 2008-02-05 2013-08-27 F. Hoffmann-La Roche Ag Nuevas piridinonas y piridazinonas
EP2252612B1 (en) 2008-02-22 2012-03-28 Irm Llc Heterocyclic compounds and compositions as c-kit and pdgfr kinase inhibitors
AR072657A1 (es) 2008-02-29 2010-09-15 Genentech Inc Compuestos inhibidores de raf y metodos para su uso
CA2716947A1 (en) 2008-02-29 2009-09-11 Array Biopharma Inc. Imidazo [4,5-b] pyridine derivatives used as raf inhibitors
US20110003859A1 (en) 2008-02-29 2011-01-06 Array Biopharma Inc. N- (6-aminopyridin-3-yl) -3- (sulfonamido) benzamide derivatives as b-raf inhibitors for the treatment of cancer
WO2009111278A2 (en) 2008-02-29 2009-09-11 Array Biopharma Inc. Raf inhibitor compounds and methods of use thereof
MY165582A (en) 2008-03-11 2018-04-05 Incyte Holdings Corp Azetidine and cyclobutane derivatives as jak inhibitors
US8822500B2 (en) 2008-03-19 2014-09-02 Chembridge Corporation Tyrosine kinase inhibitors
US8815906B2 (en) 2008-03-19 2014-08-26 Chembridge Corporation Tyrosine kinase inhibitors
US8575123B2 (en) 2008-04-11 2013-11-05 Tekmira Pharmaceuticals Corporation Site-specific delivery of nucleic acids by combining targeting ligands with endosomolytic components
CN102131771A (zh) 2008-04-14 2011-07-20 阿迪生物科学公司 组合物及其制备和使用方法
CA2723205C (en) 2008-04-16 2017-03-14 Portola Pharmaceuticals, Inc. 2,6-diamino-pyrimidin-5-yl-carboxamides as syk or jak kinase inhibitors
JP5746015B2 (ja) 2008-04-16 2015-07-08 マックス プランク ゲゼルシャフト ツゥアー フェデルゥン デル ヴィッセンシャフテン エー フォー Axlキナーゼ阻害剤としてのキノリン誘導体
KR20100132550A (ko) 2008-04-16 2010-12-17 포톨라 파마슈티컬스, 인코포레이티드 syk 또는 JAK 키나제 억제제로서의 2,6-디아미노-피리미딘-5-일-카르복스아미드
BRPI0910668A2 (pt) 2008-04-22 2019-09-24 Portola Pharmaceutiacals Inc inibidores de proteína quinases
CA2722326A1 (en) 2008-04-24 2009-10-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
SI2300455T1 (sl) 2008-05-21 2017-12-29 Incyte Holdings Corporation Soli 2-fluoro-n-metil-4-(7-(kinolin-6-il-metil)-imidazo(1,2-b)1,2,4) triazin-2-il)benzamid in postopki v zvezi z njihovo pripravo
JP2011523646A (ja) 2008-05-21 2011-08-18 アリアド・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害剤としてのリン誘導体
CA2728063A1 (en) 2008-06-19 2009-12-23 Astrazeneca Ab Pyrazole compounds 436
GB0811304D0 (en) 2008-06-19 2008-07-30 Ucb Pharma Sa Therapeutic agents
PE20110063A1 (es) 2008-06-20 2011-02-16 Genentech Inc DERIVADOS DE [1, 2, 4]TRIAZOLO[1, 5-a]PIRIDINA COMO INHIBIDORES DE JAK
AU2009259853A1 (en) 2008-06-20 2009-12-23 Genentech, Inc. Triazolopyridine JAK inhibitor compounds and methods
PE20100851A1 (es) 2008-06-24 2011-01-31 Hoffmann La Roche PIRIDIN-2-ONAS Y PIRIDAZIN-3-ONAS SUSTITUIDAS COMO INHIBIDORES DE Btk
CA2730231C (en) 2008-07-09 2016-10-18 Rigel Pharmaceuticals, Inc. Polycyclic heteroaryl substituted triazoles useful as axl inhibitors
CA2730251C (en) 2008-07-09 2016-08-09 Rigel Pharmaceuticals, Inc. Bridged bicyclic heteroaryl substituted triazoles useful as axl inhibitors
CN102159214A (zh) 2008-07-16 2011-08-17 药品循环公司 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂
TW201008938A (en) 2008-07-18 2010-03-01 Sanofi Aventis Novel triazolo[4,3-a]pyridine derivatives, process for the preparation thereof, use thereof as medicaments, pharmaceutical compositions and novel use, in particular as MET inhibitors
US20110257171A1 (en) 2008-07-18 2011-10-20 Sanofi-Aventis Novel imidazo[1,2-a]pyridine derivatives, method for the preparation thereof, use thereof as medicaments, pharmaceutical compositions and novel use in particular as met inhibitors
FR2933982A1 (fr) 2008-07-18 2010-01-22 Sanofi Aventis Nouveaux derives imidazo°1,2-a!pyrimidine, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de met
AU2009279940B2 (en) 2008-08-04 2014-01-16 Merck Patent Gmbh Novel phenylamino isonicotinamide compounds
UY32049A (es) 2008-08-14 2010-03-26 Takeda Pharmaceutical Inhibidores de cmet
SI2350075T1 (sl) 2008-09-22 2014-06-30 Array Biopharma, Inc. Substituirane imidazo (1,2b)piridazinske spojine kot Trk kinazni inhibitorji
CN102264736B (zh) 2008-10-22 2013-08-14 阵列生物制药公司 作为TRK激酶抑制剂的取代的吡唑并[1,5-a]嘧啶化合物
BRPI0914404A2 (pt) 2008-10-31 2019-03-06 Genentech Inc "compostos, composição farmacêutica e método para tratar ou atenuar a gravidade de uma doença ou condição responsiva à inibição da atividade jak quinase em um paciente"
WO2010056875A1 (en) 2008-11-12 2010-05-20 Cgi Pharmaceuticals, Inc. Pyridazinones and their use as btk inhibitors
MX2011005250A (es) 2008-11-19 2011-07-29 Vertex Pharma Inhibidores de triazolotiadiazol de cinasa de proteina c-met.
PE20120121A1 (es) 2008-12-08 2012-02-20 Gilead Connecticut Inc Derivados de imidazopirazina como inhibidores de syk
EA020461B1 (ru) 2008-12-08 2014-11-28 Джилид Коннектикут, Инк. ИМИДАЗОПИРАЗИНОВЫЕ ИНГИБИТОРЫ Syk
ITMI20082336A1 (it) 2008-12-29 2010-06-30 Univ Parma Composti inibitori irreversibili di egfr con attivita' antiproliferativa
CA2749403A1 (en) 2009-01-13 2010-09-02 Glaxo Group Limited Pyrimidinecarboxamide derivatives as inhibitors of syk kinase
WO2010083283A2 (en) 2009-01-15 2010-07-22 Incyte Corporation Processes for preparing jak inhibitors and related intermediate compounds
BRPI1007046B1 (pt) 2009-01-16 2019-07-16 Rigel Pharmaceuticals, Inc. Inibidores axl para uso em terapia de combinação para evitar, tratar ou controlar o câncer metastático.
US8765727B2 (en) 2009-01-23 2014-07-01 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
FR2941951B1 (fr) 2009-02-06 2011-04-01 Sanofi Aventis Derives de 6-(6-nh-substitue-triazolopyridazine-sulfanyl) benzothiazoles et benzimidazoles : preparation, application comme medicaments et utilisation comme inhibiteurs de met.
FR2941952B1 (fr) 2009-02-06 2011-04-01 Sanofi Aventis Derives de 6-(6-substitue-triazolopyridazine-sulfanyl) 5-fluoro-benzothiazoles et 5-fluoro-benzimidazoles : preparation, application comme medicaments et utilisation comme inhibiteurs de met.
SG172857A1 (en) 2009-02-09 2011-08-29 Supergen Inc Pyrrolopyrimidinyl axl kinase inhibitors
US8673919B2 (en) 2009-03-27 2014-03-18 Ardea Biosciences, Inc. Dihydropyridin sulfonamides and dihydropyridin sulfamides as MEK inhibitors
EP2421612A1 (en) 2009-04-21 2012-02-29 Novartis AG Heterocyclic compounds as mek inhibitors
US8765754B2 (en) 2009-04-29 2014-07-01 Locus Pharmaceuticals, Inc. Pyrrolotriazine compounds
KR101705158B1 (ko) 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Egfr 억제제 및 질환 치료방법
BRPI1012108B8 (pt) 2009-05-22 2021-05-25 Incyte Corp composto 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octa no- ou heptano-nitrila, sua composição, seus usos e processo para preparar um sal de ácido fosfórico
ES2668775T3 (es) 2009-06-10 2018-05-22 Chugai Seiyaku Kabushiki Kaisha Compuestos tetracíclicos
TW201103904A (en) 2009-06-11 2011-02-01 Hoffmann La Roche Janus kinase inhibitor compounds and methods
CA2765534C (en) 2009-06-15 2018-09-18 Rigel Pharmaceuticals, Inc. Small molecule inhibitors of spleen tyrosine kinase (syk)
CN102134218A (zh) 2009-06-15 2011-07-27 凯美隆(北京)药业技术有限公司 6-芳氨基吡啶酮磺酰胺和6-芳氨基吡嗪酮磺酰胺mek抑制剂
TWI462920B (zh) 2009-06-26 2014-12-01 葛萊伯格有限公司 用於治療退化性及發炎疾病之新穎化合物
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
CN102574847A (zh) 2009-07-30 2012-07-11 Irm责任有限公司 作为syk激酶抑制剂的化合物和组合物
TW201105669A (en) 2009-07-30 2011-02-16 Irm Llc Compounds and compositions as Syk kinase inhibitors
US20120157452A1 (en) 2009-08-28 2012-06-21 Genentech, Inc. 1h-pyrazolo[3,4-b] pyridine compounds for inhibiting raf kinase
WO2011025965A1 (en) 2009-08-28 2011-03-03 Genentech, Inc. Raf inhibitor compounds and methods of use thereof
CN102858754A (zh) 2009-08-28 2013-01-02 阵列生物制药公司 Raf抑制剂化合物及其使用方法
SG178853A1 (en) 2009-08-28 2012-04-27 Array Biopharma Inc Raf inhibitor compounds and methods of use thereof
TWI557127B (zh) 2009-09-04 2016-11-11 百健Ma公司 布魯頓氏酪胺酸激酶抑制劑
WO2011029043A1 (en) 2009-09-04 2011-03-10 Biogen Idec Ma Inc. Heteroaryl btk inhibitors
US9238571B2 (en) 2009-09-30 2016-01-19 Merck Sharp & Dohme Limited Formulations for c-Met kinase inhibitors
CA2814617C (en) 2009-10-13 2017-12-19 Allostem Therapeutics Llc Novel mek inhibitors, useful in the treatment of diseases
HUE060206T2 (hu) 2009-10-16 2023-02-28 Novartis Ag MEK gátlót és B-Raf gátlót tartalmazó kombináció
BR112012010519A2 (pt) 2009-11-04 2017-12-05 Novartis Ag derivados de sulfonamida heterocíclicos
AU2010331927B2 (en) 2009-12-17 2013-10-10 Merck Canada Inc. Aminopyrimidines as Syk inhibitors
EP2512246B1 (en) 2009-12-17 2015-09-30 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
JP2013515737A (ja) 2009-12-23 2013-05-09 アークル インコーポレイテッド 精製されたピロロキノリニル−ピロリジン−2,5−ジオン組成物ならびにその調製方法および使用方法
EP2516434B1 (en) 2009-12-23 2015-05-27 Takeda Pharmaceutical Company Limited Fused heteroaromatic pyrrolidinones as syk inhibitors
EP2338888A1 (en) 2009-12-24 2011-06-29 Almirall, S.A. Imidazopyridine derivatives as JAK inhibitors
EP2937345B1 (en) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
CN102812022B (zh) 2010-01-12 2016-02-03 Ab科学有限公司 噻唑和噁唑激酶抑制剂
CA2786245A1 (en) 2010-01-29 2011-08-04 Boehringer Ingelheim International Gmbh Substituted naphthyridines and their use as syk kinase inhibitors
JP5938352B2 (ja) 2010-03-11 2016-06-22 ギリアード コネチカット, インコーポレイテッド イミダゾピリジンsyk阻害剤
US8481541B2 (en) 2010-03-22 2013-07-09 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
EP2550266B1 (en) 2010-03-24 2018-05-09 Amitech Therapeutics Solutions, Inc. Heterocyclic compounds useful for kinase inhibition
WO2011121223A1 (fr) 2010-03-30 2011-10-06 Sanofi-Aventis Derives de 6-(alkyl- ou cycloalkyl-triazolopyridazine-sulfanyl) benzothiazoles: preparation, application comme medicaments et utilisation comme inhibiteurs de met
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
CA2796967C (en) 2010-05-04 2015-12-01 Pfizer Inc. Heterocyclic derivatives as alk inhibitors
US20130072495A1 (en) 2010-05-14 2013-03-21 OSI Pharmaceuticals, LLC Fused bicyclic kinase inhibitors
MX2012013194A (es) 2010-05-20 2013-01-22 Hoffmann La Roche Derivados pirrolopirazinas como inhibidores de cinasas tirocina-cinasa del baso (syk) y cinasa de janus (jak).
EP2571880A1 (en) 2010-05-20 2013-03-27 F.Hoffmann-La Roche Ag Pyrrolo [2, 3 - b]pyrazine - 7 - carboxamide derivatives and their use as jak and syk inhibitors
JP2013527195A (ja) 2010-05-27 2013-06-27 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 c−Metプロテインキナーゼのアミノピラゾールトリアゾロチアジアゾールインヒビター
US8669256B2 (en) 2010-05-28 2014-03-11 Merck Sharp & Dohme B.V. Substituted thieno[2,3-b]pyrazine compounds as modulators of B-Raf kinase activity
US8940725B2 (en) 2010-05-31 2015-01-27 Ono Pharmaceutical Co., Ltd. Purinone derivative
MX380504B (es) 2010-06-03 2025-03-12 Pharmacyclics Llc El uso de inhibidores de la tirosina quinasa de bruton (btk).
TR201807294T4 (tr) 2010-06-22 2018-06-21 Centre Nat Rech Scient Nükleik asit konjugatları için endosomolitik ajanlar ile optimize edilmiş in vivo aktarım sistemi.
JP5744021B2 (ja) 2010-06-30 2015-07-01 富士フイルム株式会社 新規なニコチンアミド誘導体またはその塩
WO2012005299A1 (ja) 2010-07-07 2012-01-12 日本新薬株式会社 Rosチロシンキナーゼ阻害剤
SG187064A1 (en) 2010-07-14 2013-02-28 Zhejiang Beta Pharma Inc NOVEL FUSED HETEROCYCLIC DERIVATIVES USEFUL AS c-MET TYROSINE KINASE INHIBITORS
EP2594566A4 (en) 2010-07-16 2014-10-01 Kyowa Hakko Kirin Co Ltd AROMATIC HETEROCYCLIC NITROGEN CYCLE DERIVATIVE
WO2012008564A1 (ja) 2010-07-16 2012-01-19 協和発酵キリン株式会社 含窒素芳香族複素環誘導体
AR085183A1 (es) 2010-07-30 2013-09-18 Lilly Co Eli Compuesto 6-(1-metil-1h-pirazol-4-il)-3-(2-metil-2h-indazol-5-iltio)-[1,2,4]triazol[4,3-b]piridazina, composicion farmaceutica que lo comprende y uso para preparar un medicamento util para tratar cancer
UY33539A (es) 2010-08-02 2012-02-29 Astrazeneca Ab Compuestos químicos alk
PH12013500246A1 (en) 2010-08-10 2019-10-11 Celgene Avilomics Res Inc Besylate salt of a btk inhibitor
EP2606886B1 (en) 2010-08-20 2020-01-08 Chugai Seiyaku Kabushiki Kaisha Composition comprising tetracyclic compound
SG187956A1 (en) 2010-08-27 2013-03-28 Merck Patent Gmbh Furopyridine derivatives
CA2809331C (en) 2010-08-27 2018-09-25 Merck Patent Gmbh Triazolopyrazine derivatives
EP2423208A1 (en) 2010-08-28 2012-02-29 Lead Discovery Center GmbH Pharmaceutically active compounds as Axl inhibitors
UY33597A (es) 2010-09-09 2012-04-30 Irm Llc Compuestos y composiciones como inhibidores de la trk
US8664244B2 (en) 2010-09-12 2014-03-04 Advenchen Pharmaceuticals, LLC Compounds as c-Met kinase inhibitors
JO3062B1 (ar) 2010-10-05 2017-03-15 Lilly Co Eli R)-(e)-2-(4-(2-(5-(1-(3، 5-داي كلورو بيريدين-4-يل)إيثوكسي)-1h-إندازول-3-يل)?ينيل)-1h-بيرازول-1-يل)إيثانول بلوري
EA025030B1 (ru) 2010-10-08 2016-11-30 Икскавери Холдинг Кампани, Ллс Соединение {5-[(1r)-1-(2,6-дихлор-3-фторфенил)этокси]-6-аминопиридазин-3-ил}-n-(1-метил-6-оксо-1,6-дигидропиридин-3-ил)карбоксамид в качестве киназного ингибитора
AU2011323484B2 (en) 2010-11-01 2016-10-06 Portola Pharmaceuticals, Inc. Benzamides and nicotinamides as Syk modulators
CN102020651B (zh) 2010-11-02 2012-07-18 北京赛林泰医药技术有限公司 6-芳基氨基吡啶酮甲酰胺mek抑制剂
CN102532141A (zh) 2010-12-08 2012-07-04 中国科学院上海药物研究所 [1,2,4]三唑并[4,3-b][1,2,4]三嗪类化合物、其制备方法和用途
US20130004481A1 (en) 2011-01-12 2013-01-03 Boehringer Ingelheim International Gmbh Anticancer therapy
BR112013021638A2 (pt) 2011-02-25 2016-08-02 Irm Llc "compostos inibidores de trk, seu uso e composições que os compreendem"
US20140005188A1 (en) 2011-03-11 2014-01-02 Glaxo Group Limited Pyrido[3,4-b]pyrazine derivatives as syk inhibitors
GB201104153D0 (en) 2011-03-11 2011-04-27 Glaxo Group Ltd Novel compounds
KR20140020972A (ko) 2011-03-28 2014-02-19 에프. 호프만-라 로슈 아게 티아졸로피리미딘 화합물
EP2694486B1 (en) 2011-04-01 2018-01-10 University of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk inhibitors
EP3628665B1 (en) 2011-04-01 2022-11-02 University of Utah Research Foundation Substituted n-phenylpyrimidin-2-amine analogs as inhibitors of the axl kinase
EP2694509B1 (en) 2011-04-05 2016-05-18 Pfizer Limited Pyrrolo[2,3-d]pyrimidine derivatives as inhibitors of tropomyosin-related kinases
WO2012151137A1 (en) 2011-05-04 2012-11-08 Merck Sharp & Dohme Corp. Amino-pyridine-containing spleen tyrosine kinase (syk) inhibitors
WO2012154518A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors
AU2012253885A1 (en) 2011-05-10 2013-10-31 Merck Sharp & Dohme Corp. Aminopyrimidines as Syk inhibitors
CA2834062A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Pyridyl aminopyridines as syk inhibitors
NZ618795A (en) 2011-05-13 2015-07-31 Array Biopharma Inc Pyrrolidinyl urea, pyrrolidinyl thiourea and pyrrolidinyl guanidine compounds as trka kinase inhibitors
EP2527440A1 (en) * 2011-05-27 2012-11-28 Institut Curie Cancer treatment by combining DNA molecules mimicking double strand breaks with hyperthermia
WO2012167423A1 (en) 2011-06-08 2012-12-13 Hutchison Medipharma Limited Substituted pyridopyrazines as novel syk inhibitors
CN102816162B (zh) 2011-06-10 2016-04-27 中国科学院广州生物医药与健康研究院 嘧啶并嘧啶酮类化合物及其药用组合物和应用
US9073947B2 (en) 2011-06-10 2015-07-07 Merck Patent Gmbh Compositions and methods for the production of pyrimidine and pyridine compounds with BTK inhibitory activity
CN102393896B (zh) 2011-07-11 2014-08-27 成都西谷曙光数字技术有限公司 一种简单精确的射频定位系统和方法
US9102673B2 (en) 2011-07-12 2015-08-11 Merck Sharp & Dohme Corp. Substituted pyrrolo[3,2-c]pyridines as TrkA kinase inhibitors
CN103889987B (zh) 2011-07-19 2016-09-14 默沙东有限责任公司 作为btk抑制剂的选择的咪唑并吡嗪类
WO2013010869A1 (en) 2011-07-19 2013-01-24 Msd Oss B.V. 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides btk-inhibitors
EP2548877A1 (en) 2011-07-19 2013-01-23 MSD Oss B.V. 4-(5-Membered fused pyridinyl)benzamides as BTK-inhibitors
CA2842841C (en) 2011-07-27 2016-04-19 Nanjing Allgen Pharma Co. Ltd. Spirocyclic molecules as protein kinase inhibitors
ES2573831T3 (es) 2011-07-27 2016-06-10 Ab Science Derivados de oxazol y tiazol como inhibidores selectivos de la proteína quinasa (C-kit)
US9199981B2 (en) 2011-09-01 2015-12-01 Novartis Ag Compounds and compositions as C-kit kinase inhibitors
CA2845785A1 (en) 2011-09-01 2013-03-07 Irm Llc Compounds and compositions as c-kit kinase inhibitors
US8569283B2 (en) 2011-09-01 2013-10-29 Valentina Molteni Compounds and compositions as c-Kit kinase inhibitors
CN103930424A (zh) 2011-09-01 2014-07-16 Irm责任有限公司 作为c-Kit激酶抑制剂的化合物和组合物
AU2012308238B2 (en) 2011-09-14 2017-05-25 Neupharma, Inc. Certain chemical entities, compositions, and methods
WO2013047813A1 (ja) 2011-09-30 2013-04-04 大鵬薬品工業株式会社 1,2,4-トリアジン-6-カルボキサミド誘導体
US8987456B2 (en) 2011-10-05 2015-03-24 Merck Sharp & Dohme Corp. 3-pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors
EP2763976B1 (en) 2011-10-05 2016-05-18 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
WO2013052391A1 (en) 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. PHENYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
UA111382C2 (uk) 2011-10-10 2016-04-25 Оріон Корпорейшн Інгібітори протеїнкінази
US20140303191A1 (en) 2011-10-19 2014-10-09 Pharmacyclics, Inc. Use of inhibitors of bruton's tyrosine kinase (btk)
EP2773645A1 (en) 2011-11-01 2014-09-10 F.Hoffmann-La Roche Ag Imidazopyridazine compounds
UA111756C2 (uk) 2011-11-03 2016-06-10 Ф. Хоффманн-Ля Рош Аг Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона
TW201326171A (zh) 2011-11-03 2013-07-01 Genentech Inc 烷基化哌□化合物
US8669251B2 (en) 2011-11-03 2014-03-11 Genentech, Inc. 8-fluorophthalazin-1(2H)-one compounds
EA023521B1 (ru) 2011-11-14 2016-06-30 Сефалон, Инк. ПРОИЗВОДНЫЕ УРАЦИЛА В КАЧЕСТВЕ ИНГИБИТОРОВ AXL И c-MET КИНАЗЫ
BR112014012727B1 (pt) 2011-11-29 2022-10-25 Ono Pharmaceutical Co., Ltd Cloridrato de 6-amino-9-[(3r)-1-(2-butinoil)-3-pirrolidinil]-7-(4-fenoxifenil)-7,9-di-hidro-8h-puri- 8-ona e composição farmacêutica
KR20140105508A (ko) 2011-12-12 2014-09-01 닥터 레디스 레보러터리즈 리미티드 트로포미오신 수용체 키나제(Trk) 억제제인 치환된 피라졸로[1,5-a]피리딘
JP6075736B2 (ja) 2011-12-21 2017-02-08 ジエンス ヘンルイ メデイシンカンパニー リミテッドJiangsu Hengrui Medicine Co.,Ltd. ピロール−6員ヘテロアリール環誘導体、その合成法およびその医薬用途
DK2799431T3 (en) 2011-12-28 2018-03-26 Fujifilm Corp Hitherto unknown nicotinamide derivatives or salts thereof
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
KR20140108594A (ko) 2012-01-10 2014-09-11 에프. 호프만-라 로슈 아게 피리다진 아미드 화합물 및 syk 저해제로서의 이의 용도
JP6109193B2 (ja) 2012-01-10 2017-04-05 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト チエノピリミジン化合物
CN103204844A (zh) 2012-01-17 2013-07-17 上海艾力斯医药科技有限公司 氨基杂芳基化合物及其制备方法与应用
CN103204825B (zh) 2012-01-17 2015-03-04 上海科州药物研发有限公司 作为蛋白激酶抑制剂的苯并噻唑化合物及其制备方法和用途
AU2013210403B2 (en) 2012-01-19 2016-01-14 Taiho Pharmaceutical Co., Ltd. 3,5-disubstituted alkynylbenzene compound and salt thereof
CA2863517C (en) 2012-01-20 2019-11-05 Genosco Substituted pyrimidine compounds and their use as syk inhibitors
SG11201404505PA (en) 2012-01-31 2014-10-30 Daiichi Sankyo Co Ltd Pyridone derivative
US8501724B1 (en) 2012-01-31 2013-08-06 Pharmacyclics, Inc. Purinone compounds as kinase inhibitors
WO2013124869A2 (en) 2012-02-21 2013-08-29 Amrita Vishwa Vidyapeetham University The art, method,manner process and system of fibrous bio-degradable polymeric wafers for the local delivery of therapeutic agents in combinations
US9073944B2 (en) 2012-02-21 2015-07-07 Merck Patent Gmbh Cyclic diaminopyrimidine derivatives
JP6479476B2 (ja) 2012-02-21 2019-03-06 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 SykチロシンキナーゼインヒビターおよびGCN2セリンキナーゼインヒビターとしての8−置換2−アミノー[1,2,4]トリアゾロ[1,5−A]ピラジン類
ES2606638T3 (es) 2012-02-21 2017-03-24 Merck Patent Gmbh Derivados de furopiridina
UA114501C2 (uk) 2012-02-28 2017-06-26 Астеллас Фарма Інк. Азотовмісна ароматична гетероциклічна сполука
MA37405A1 (fr) 2012-03-14 2016-03-31 Lupin Ltd Composés hétérocyclyle
ES2880109T3 (es) 2012-03-15 2021-11-23 Celgene Car Llc Formas sólidas de un inhibidor de la cinasa del receptor del factor de crecimiento epidérmico
WO2013142382A1 (en) 2012-03-22 2013-09-26 Genosco Substituted pyridopyrimidine compounds and their use as flt3 inhibitors
WO2013148603A1 (en) 2012-03-27 2013-10-03 Takeda Pharmaceutical Company Limited Cinnoline derivatives as as btk inhibitors
EP2830626B1 (en) 2012-03-30 2019-01-02 Novartis AG Fgfr inhibitor for use in the treatment of hypophosphatemic disorders
MX371119B (es) 2012-04-03 2020-01-17 Novartis Ag Productos de combinacion con los inhibidores de cinasa de tirosina y su uso.
WO2013152135A1 (en) 2012-04-04 2013-10-10 Dawei Zhang Substituted quinolines as bruton's tyrosine kinases inhibitors
WO2013157540A1 (ja) 2012-04-17 2013-10-24 富士フイルム株式会社 含窒素複素環化合物またはその塩
WO2013158859A1 (en) 2012-04-18 2013-10-24 Cell Signaling Technology, Inc. Egfr and ros1 in cancer
ES2605388T3 (es) 2012-04-26 2017-03-14 Ono Pharmaceutical Co., Ltd. Compuesto inhibidor de Trk
CN106008511B (zh) 2012-05-14 2018-08-14 华东理工大学 蝶啶酮衍生物及其作为egfr、blk、flt3抑制剂的应用
WO2013176970A1 (en) 2012-05-22 2013-11-28 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
GB201209613D0 (en) 2012-05-30 2012-07-11 Astex Therapeutics Ltd New compounds
WO2013180183A1 (ja) 2012-05-30 2013-12-05 日本新薬株式会社 芳香族複素環誘導体及び医薬
TWI585088B (zh) 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并[1,2-b]嗒衍生物
AR091273A1 (es) 2012-06-08 2015-01-21 Biogen Idec Inc Inhibidores de pirimidinil tirosina quinasa
CA2876689C (en) 2012-06-13 2022-04-26 Incyte Corporation Substituted tricyclic compounds as fgfr inhibitors
JP6092376B2 (ja) 2012-06-14 2017-03-08 イーライ リリー アンド カンパニー Jak1およびjak2の阻害剤
WO2013192125A1 (en) 2012-06-20 2013-12-27 Merck Sharp & Dohme Corp. Pyrazolyl derivatives as syk inhibitors
EP2863913B1 (en) 2012-06-20 2018-09-12 Merck Sharp & Dohme Corp. Imidazolyl analogs as syk inhibitors
WO2013192088A1 (en) 2012-06-22 2013-12-27 Merck Sharp & Dohme Corp. SUBSTITUTED DIAZINE AND TRIAZINE SPLEEN TYROSINE KINASE (Syk) INHIBITORS
US9376418B2 (en) 2012-06-22 2016-06-28 Merck Sharp & Dohme Corp. Substituted pyridine spleen tyrosine kinase (SYK) inhibitors
TWI520962B (zh) 2012-06-29 2016-02-11 貝達藥業股份有限公司 As the c-Met tyrosine kinase inhibitors novel fused pyridine derivatives
CA2782774A1 (en) 2012-07-06 2014-01-06 Pharmascience Inc. Protein kinase inhibitors
WO2014009319A1 (en) 2012-07-11 2014-01-16 Boehringer Ingelheim International Gmbh Indolinone derivatives anticancer compounds
CA2881279C (en) 2012-08-07 2020-07-07 Merck Patent Gmbh Pyridopyrimidine derivatives as protein kinase inhibitors
CN104603124B (zh) 2012-08-10 2018-04-17 勃林格殷格翰国际有限公司 用作布鲁顿酪氨酸激酶(btk)抑制剂的杂芳族化合物
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
US9315500B2 (en) 2012-08-13 2016-04-19 Novartis Ag Bicyclic heteroaryl cycloalkyldiamine derivatives
EP2884982B1 (en) 2012-08-20 2017-09-20 Merck Sharp & Dohme Corp. SUBSTITUTED PHENYL SPLEEN TYROSINE KINASE (Syk) INHIBITORS
CN104507945B (zh) 2012-08-21 2018-03-23 霍夫曼-拉罗奇有限公司 作为syk抑制剂的吡咯并[2,3‑b]吡嗪
CN103122000B (zh) 2012-09-03 2013-12-25 中美冠科生物技术(太仓)有限公司 用作抗肿瘤药物的高选择性的c-Met激酶抑制剂
SMT201900344T1 (it) 2012-09-10 2019-07-11 Principia Biopharma Inc Composti di pirazolopirimidina come inibitori di chinasi
US9533989B2 (en) 2012-09-18 2017-01-03 Ziarco Pharma Ltd. Substituted pyrimidine-5-carboxamides as spleen tyrosine kinase inhibitors
PL2902029T3 (pl) 2012-09-25 2019-01-31 Chugai Seiyaku Kabushiki Kaisha Inhibitor RET
US9469654B2 (en) 2012-09-27 2016-10-18 Portola Pharmaceuticals, Inc. Bicyclic oxa-lactam kinase inhibitors
WO2014048065A1 (en) 2012-09-28 2014-04-03 Merck Sharp & Dohme Corp. Triazolyl derivatives as syk inhibitors
JP6313772B2 (ja) 2012-10-04 2018-04-18 ユニヴァーシティー オブ ユタ リサーチ ファウンデーション チロシン受容体キナーゼbtk阻害剤である置換n−(3−(ピリミジン−4−イル)フェニル)アクリルアミド類似体
KR102194611B1 (ko) 2012-10-04 2020-12-23 유니버시티 오브 유타 리서치 파운데이션 티로신 수용체 키나아제 btk 억제제로서 치환된 n-(3-(피리미딘-4-일)페닐)아크릴아미드 유사체
MX2015004801A (es) 2012-10-19 2015-08-14 Hoffmann La Roche Inhibidores de la syk.
BR112015004427A2 (pt) 2012-10-26 2017-07-04 Hoffmann La Roche compostos , métodos para o tratamento de um estado inflamatório , da artrite reumatóide , da asma , de um distúrbio imunológico e de um distúrbio imune e composição farmacêutica
US20150291554A1 (en) 2012-11-02 2015-10-15 Pfizer Inc. Bruton's Tyrosine Kinase Inhibitors
CN102977014B (zh) 2012-11-05 2015-01-07 沈阳药科大学 新的喹啉类化合物及其用途
US20150284381A1 (en) 2012-11-07 2015-10-08 Merck Sharp & Dohme Corp. Amino-pyridine-containing spleen tyrosine kinase (syk) inhibitors
WO2014078328A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-bicyclic aryl,n'-pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
US9828360B2 (en) 2012-11-13 2017-11-28 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
US9822118B2 (en) 2012-11-13 2017-11-21 Array Biopharma Inc. Bicyclic heteroaryl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
WO2014078331A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(arylalkyl)-n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078417A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrazolyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078372A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. Pyrrolidinyl urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
WO2014078325A1 (en) 2012-11-13 2014-05-22 Array Biopharma Inc. N-(monocyclic aryl),n'-pyrazolyl-urea, thiourea, guanidine and cyanoguanidine compounds as trka kinase inhibitors
ME02990B (me) 2012-11-13 2018-10-20 Array Biopharma Inc Jedinjenja n-pirolidinil, n'-pirazolil- uree, tiouree, guanidina i cijanoguanidina kао inhibitori trka kinaze
US9981959B2 (en) 2012-11-13 2018-05-29 Array Biopharma Inc. Thiazolyl and oxazolyl urea, thiourea, guanidine and cyanoguanidine compounds as TrkA kinase inhibitors
KR20150084923A (ko) 2012-11-15 2015-07-22 파마시클릭스, 인코포레이티드 키나제 억제제로서의 피롤로피리미딘 화합물
CN103848810A (zh) 2012-11-30 2014-06-11 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
WO2014086032A1 (en) 2012-12-07 2014-06-12 Hutchison Medipharma Limited Substituted pyridopyrazines as syk inhibitors
EP2931281B1 (en) 2012-12-12 2018-01-17 Merck Sharp & Dohme Corp. Amino-pyrimidine-containing spleen tyrosine kinase inhibitors
EP2934525B1 (en) 2012-12-21 2019-05-08 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyridines as spleen tyrosine kinase inhibitors
US9422267B2 (en) 2012-12-26 2016-08-23 Medivation Technologies, Inc. Fused pyrimidine compounds and use thereof
DK2940014T3 (en) 2012-12-28 2018-12-10 Crystalgenomics Inc 2,3-DIHYDRO-ISOINDOL-1-ON DERIVATIVE AS BTK KINase INHIBITORS AND PHARMACEUTICAL COMPOSITION INCLUDING THE SAME
ES2827233T3 (es) 2013-01-18 2021-05-20 Guangzhou Maxinovel Pharmaceuticals Co Ltd Compuesto heterocíclico de cinco y seis miembros, y método de preparación, composición farmacéutica y uso del mismo
US9481682B2 (en) 2013-01-23 2016-11-01 Merck Sharp & Dohme Corp. Substituted benzamides and substituted pyridinecarboxamides as Btk inhibitors
WO2014113942A1 (en) 2013-01-23 2014-07-31 Merck Sharp & Dohme Corp. Btk inhibitors
WO2014113932A1 (en) 2013-01-23 2014-07-31 Merck Sharp & Dohme Corp. Btk inhibitors
JP6248948B2 (ja) 2013-02-08 2017-12-20 日産化学工業株式会社 3環性ピロロピリジン化合物及びjak阻害剤
MX362181B (es) 2013-02-19 2019-01-08 Ono Pharmaceutical Co Compuesto inhibidor de cinasa del receptor de tropomiosina (trk).
AR094812A1 (es) 2013-02-20 2015-08-26 Eisai R&D Man Co Ltd Derivado de piridina monocíclico como inhibidor del fgfr
US9708326B2 (en) 2013-02-25 2017-07-18 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
JO3377B1 (ar) 2013-03-11 2019-03-13 Takeda Pharmaceuticals Co مشتقات بيريدينيل وبيريدينيل مندمج
KR20150132118A (ko) 2013-03-11 2015-11-25 이그니타, 인코포레이티드 퀴나졸린 유도체의 고체 상태 형태 및 braf 저해제로서의 그의 용도
US9963452B2 (en) 2013-03-14 2018-05-08 Augusta Pharmaceuticals Inc. Methods, compounds, and compositions for inhibition of ROS
WO2014151620A1 (en) 2013-03-14 2014-09-25 Boehringer Ingelheim International Gmbh 5-thiazolecarboxamide dervatives and their use as btk inhibitors
WO2014152114A1 (en) 2013-03-15 2014-09-25 Boehringer Ingelheim International Gmbh Heteroaromatic compounds as btk inhibitors
EP2976338B1 (en) 2013-03-19 2018-01-03 Merck Sharp & Dohme Corp. N-(2-cyano heterocyclyl)pyrazolo pyridones as janus kinase inhibitors
EP2981264B1 (en) 2013-04-02 2018-04-25 F.Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
TWI628176B (zh) 2013-04-04 2018-07-01 奧利安公司 蛋白質激酶抑制劑
US10072298B2 (en) * 2013-04-17 2018-09-11 Life Technologies Corporation Gene fusions and gene variants associated with cancer
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
WO2014176216A1 (en) 2013-04-26 2014-10-30 Merck Sharp & Dohme Corp. Thiazole-substituted aminopyrimidines as spleen tyrosine kinase inhibitors
EP2988744A4 (en) 2013-04-26 2016-11-02 Merck Sharp & Dohme THIAZOLSUBSTITUTED AMINOHETEROARYLE AS MILZTYROSINKINASE INHIBITOR
WO2014180182A1 (zh) 2013-05-10 2014-11-13 江苏豪森药业股份有限公司 [1,2,4]三唑并[4,3-a]吡啶类衍生物,其制备方法或其在医药上的应用
CR20190156A (es) 2013-05-17 2019-05-16 Incyte Corp Derivados de bipirazol como inhibidores jak
EP2999702A4 (en) 2013-05-21 2017-01-11 Jiangsu Medolution Ltd. Substituted pyrazolopyrimidines as kinases inhibitors
EP3004111A1 (en) 2013-05-29 2016-04-13 Cephalon, Inc. Pyrrolotriazines as alk inhibitors
AR096654A1 (es) 2013-06-20 2016-01-27 Ab Science Derivados de benzimidazol como inhibidores selectivos de proteína quinasa
WO2014204263A1 (en) 2013-06-20 2014-12-24 The Asan Foundation Substituted pyridinone compounds as mek inhibitors
EP3483167A1 (en) 2013-06-26 2019-05-15 AbbVie Inc. Primary carboxamides as btk inhibitors
WO2014206343A1 (en) 2013-06-28 2014-12-31 Beigene, Ltd. Fused tricyclic urea compounds as raf kinase and/or raf kinase dimer inhibitors
EP3016953A4 (en) 2013-07-02 2017-03-01 Pharmacyclics, LLC Purinone compounds as kinase inhibitors
TWI649308B (zh) 2013-07-24 2019-02-01 小野藥品工業股份有限公司 喹啉衍生物
EP3628749A1 (en) 2013-07-30 2020-04-01 Blueprint Medicines Corporation Ntrk2 fusions
EA031601B1 (ru) 2013-07-31 2019-01-31 Джилид Сайэнс, Инк. Ингибиторы syk
JP6612751B2 (ja) 2013-07-31 2019-11-27 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 Btkの阻害剤としてのピリジン、ピリミジン及びピラジンならびにその使用
EP3027623A4 (en) 2013-08-02 2017-03-01 Ignyta, Inc. METHODS OF TREATING VARIOUS CANCERS USING AN AXL/cMET INHIBITOR ALONE OR IN COMBINATION WITH OTHER AGENTS
MX360498B (es) 2013-08-12 2018-11-05 Taiho Pharmaceutical Co Ltd Compuesto novedoso de pirimidina fusionada o sal del mismo.
US9227969B2 (en) 2013-08-14 2016-01-05 Novartis Ag Compounds and compositions as inhibitors of MEK
US20160361314A1 (en) 2013-08-28 2016-12-15 Novartis Ag Combination of an alk inhibitor and a cdk inhibitor for the treatment of cell proliferative diseases
RU2650512C2 (ru) 2013-09-18 2018-04-16 Бейджин Ханми Фармасьютикал Ко., Лтд. Соединение, ингибирующее активности киназ ВТК и/или JAK3
WO2015039334A1 (en) 2013-09-22 2015-03-26 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
WO2015039333A1 (en) 2013-09-22 2015-03-26 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
RU2677884C2 (ru) 2013-09-30 2019-01-22 Гуанчжоу Иннокэа Фарма Тек Ко., Лтд. Замещенные никотинимидные ингибиторы втк, их получение и применение в терапии раковых, воспалительных и аутоиммунных заболеваний
CN105764896A (zh) 2013-09-30 2016-07-13 药品循环有限责任公司 布鲁顿氏酪氨酸激酶的抑制剂
WO2015056683A1 (ja) 2013-10-16 2015-04-23 富士フイルム株式会社 含窒素複素環化合物の塩またはその結晶、医薬組成物およびflt3阻害剤
SG11201602566XA (en) 2013-10-21 2016-05-30 Genosco Substituted pyrimidine compounds and their use as syk inhibitors
US10329270B2 (en) 2013-10-21 2019-06-25 Merck Patent Gmbh Heteroaryl compounds as BTK inhibitors and uses thereof
EP3061747B1 (en) 2013-10-25 2021-04-07 Shanghai Hengrui Pharmaceutical Co. Ltd. Pyridic ketone derivatives, method of preparing same, and pharmaceutical application thereof
CN105683188B (zh) 2013-10-25 2018-02-09 诺华股份有限公司 作为fgfr4抑制剂的稠环二环吡啶基衍生物
EP3067356B1 (en) 2013-11-08 2018-07-04 ONO Pharmaceutical Co., Ltd. Pyrrolo pyrimidine derivative
EP3078659B1 (en) 2013-12-02 2017-11-15 Jenkem Technology Co., Ltd. (Beijing) 3-furyl-2-cyano-2-acrylamide derivative, preparation method therefor, pharmaceutical composition and use thereof
AU2014360446A1 (en) 2013-12-05 2016-06-09 Pharmacyclics, Llc Inhibitors of Bruton's tyrosine kinase
US9067914B1 (en) 2013-12-10 2015-06-30 Genzyme Corporation Tropomyosin-related kinase (TRK) inhibitors
EP3083559B1 (en) 2013-12-20 2021-03-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9670196B2 (en) 2013-12-20 2017-06-06 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as Spleen Tyrosine Kinase inhibitors
WO2015094997A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
US9834554B2 (en) 2013-12-20 2017-12-05 Merck Sharp & Dohme Corp. BTK inhibitors
US9637486B2 (en) 2013-12-20 2017-05-02 Merck Sharp & Dohme Corp. Btk inhibitors
TWI662037B (zh) 2013-12-23 2019-06-11 美商基利科學股份有限公司 脾酪胺酸激酶抑制劑
PL3087070T3 (pl) 2013-12-26 2018-03-30 Ignyta, Inc. Pochodne pirazolo[1,5-a]pirydyny i sposoby ich zastosowania
JP6486954B2 (ja) 2014-01-29 2019-03-20 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 Btk阻害剤としてのピラゾール化合物
SG11201605417QA (en) 2014-02-03 2016-08-30 Cadila Healthcare Ltd Heterocyclic compounds
HUE049437T2 (hu) 2014-02-04 2020-09-28 Astellas Pharma Inc Hatóanyagként heterociklusos diamino-karboxamid vegyületet tartalmazó gyógyászati készítmény
US9783539B2 (en) 2014-02-27 2017-10-10 Jiangsu Ascentage Biomed Development Inc. Indoloquinolone compounds as anaplastic lymphoma kinase (ALK) inhibitors
WO2015138273A1 (en) 2014-03-13 2015-09-17 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
ES2738416T3 (es) 2014-03-19 2020-01-22 Boehringer Ingelheim Int Inhibidores heteroarílicos de SYK
MX2016012460A (es) 2014-03-24 2017-05-04 Ab Science Derivados de oxazol sustituidos por diazaespiroalcanona como inhibidores de torosina quinasa de bazo.
WO2015143654A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015143653A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
WO2015143652A1 (en) 2014-03-26 2015-10-01 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS,COMPOSITIONS AND METHODS THEREOF
EP3129376B1 (en) 2014-03-27 2018-12-26 Janssen Pharmaceutica NV Substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrazine derivatives and 5,6,7,8-tetrahydro-4h-pyrazolo[1,5-a][1,4]diazepine derivatives as ros1 inhibitors
US10342795B2 (en) 2014-03-27 2019-07-09 Janssen Pharmaceutica Nv Substituted 4,5,6,7-tetrahydro-pyrazolo[1,5-a]pyrimidine derivatives and 2,3-dihydro-1H-imidazo[1,2-b]pyrazole derivatives as ROS1 inhibitors
US20170137426A1 (en) 2014-03-28 2017-05-18 Changzhou Jiekai Pharmatech Co., Ltd. Heterocyclic compounds as axl inhibitors
CN105017256A (zh) 2014-04-29 2015-11-04 浙江导明医药科技有限公司 多氟化合物作为布鲁顿酪氨酸激酶抑制剂
CN105085474B (zh) 2014-05-07 2018-05-18 北京赛林泰医药技术有限公司 鲁顿酪氨酸激酶抑制剂
JP6561984B2 (ja) 2014-05-14 2019-08-21 日産化学株式会社 3環性化合物及びjak阻害剤
CN106459013B (zh) 2014-05-15 2019-10-25 阵列生物制药公司 作为trka激酶抑制剂的化合物及其用途
CN105294654B (zh) 2014-05-30 2018-01-09 北京浦润奥生物科技有限责任公司 Alk激酶抑制剂及其制备方法和应用
US10053458B2 (en) 2014-06-17 2018-08-21 Korea Research Institute Of Chemical Technology Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient
WO2015200341A1 (en) 2014-06-23 2015-12-30 Dr. Reddy's Laboratories Ltd. Substituted imidazo[1,2-a]pyridine compounds useful for the treatment of pain
TWI723572B (zh) 2014-07-07 2021-04-01 日商第一三共股份有限公司 具有四氫吡喃基甲基之吡啶酮衍生物及其用途
TW201617074A (zh) 2014-07-14 2016-05-16 吉李德科學股份有限公司 Syk(脾酪胺酸激酶)抑制劑
CA2959602A1 (en) 2014-08-01 2016-02-04 Pharmacyclics Llc Inhibitors of bruton's tyrosine kinase
WO2016021629A1 (ja) 2014-08-06 2016-02-11 塩野義製薬株式会社 TrkA阻害活性を有する複素環および炭素環誘導体
NO2721710T3 (ru) 2014-08-21 2018-03-31
KR101710127B1 (ko) 2014-08-29 2017-02-27 한화제약주식회사 야누스인산화효소 억제제로서의 치환된 N-(피롤리딘-3-일)-7H-피롤로[2,3-d]피리미딘-4-아민
WO2016036796A1 (en) 2014-09-03 2016-03-10 Genzyme Corporation Cyclic urea compounds as tropomyosin-related kinase (trk) inhibitors
CN105524068B (zh) 2014-09-30 2017-11-24 上海海雁医药科技有限公司 氮杂双环衍生物、其制法与医药上的用途
ES2756748T3 (es) 2014-10-03 2020-04-27 Novartis Ag Uso de derivados de piridilo bicíclicos de anillo fusionado como inhibidores de fgfr4
CN107001362A (zh) 2014-10-06 2017-08-01 默克专利有限公司 用作btk抑制剂的杂芳基化合物及其用途
EP3205650B1 (en) 2014-10-11 2021-08-04 Shanghai Hansoh Biomedical Co., Ltd. Egfr inhibitor, and preparation and application thereof
CN107108555B (zh) 2014-10-24 2020-12-01 百时美施贵宝公司 三环阻转异构体化合物
CN107148421A (zh) 2014-10-30 2017-09-08 桑多斯股份公司 活性丙烯酰胺类化合物
CN111170998B (zh) 2014-11-05 2023-04-11 益方生物科技(上海)股份有限公司 嘧啶或吡啶类化合物、其制备方法和医药用途
US9862712B2 (en) 2014-11-20 2018-01-09 Council Of Scientific & Industrial Research Benzimidazole based EGFR inhibitors
CN105601573B (zh) 2014-11-24 2021-07-02 中国科学院上海药物研究所 2-氨基嘧啶类化合物及其药物组合物和应用
WO2016091849A2 (en) 2014-12-11 2016-06-16 Bayer Pharma Aktiengesellschaft Use of pan fgfr inhibitors and method of identifying patients with cancer eligible for treatment with a pan fgfr inhibitor
WO2016097918A1 (en) 2014-12-18 2016-06-23 Pfizer Inc. Pyrimidine and triazine derivatives and their use as axl inhibitors
WO2016104617A1 (ja) 2014-12-25 2016-06-30 小野薬品工業株式会社 キノリン誘導体
WO2016106627A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Btk inhibitors
WO2016106628A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Btk inhibitors
WO2016106626A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Imidazopyrazine analogs with 3-tertiary carbon substitutions as btk inhibitors
WO2016106623A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Benzamide imidazopyrazine btk inhibitors
WO2016106624A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Tertiary alcohol imidazopyrazine btk inhibitors
WO2016106652A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Biarylether imidazopyrazine btk inhibitors
WO2016106629A1 (en) 2014-12-31 2016-07-07 Merck Sharp & Dohme Corp. Btk inhibitors
CN104530063B (zh) 2015-01-13 2017-01-18 北京赛特明强医药科技有限公司 喹唑啉并杂环类化合物及其制备方法和作为用于治疗癌症的表皮生长因子受体抑制剂的应用
CN105837576B (zh) 2015-01-14 2019-03-26 湖北生物医药产业技术研究院有限公司 Btk抑制剂
ES2962330T3 (es) 2015-01-20 2024-03-18 Wuxi Fortune Pharmaceutical Co Ltd Inhibidor de jak
EP3247692B1 (en) 2015-01-23 2022-09-07 GVK Biosciences Private Limited Inhibitors of trka kinase
WO2016123706A1 (en) 2015-02-03 2016-08-11 Trillium Therapeutics Inc. Novel fluorinated derivatives as egfr inhibitors useful for treating cancers
WO2016125186A1 (en) 2015-02-03 2016-08-11 Council Of Scientific & Industrial Research Novel flavone based egfr inhibitors and process for preparation thereof
CA2976790C (en) 2015-02-20 2024-02-27 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2016161572A1 (en) 2015-04-08 2016-10-13 Merck Sharp & Dohme Corp. TrkA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
WO2016161571A1 (en) 2015-04-08 2016-10-13 Merck Sharp & Dohme Corp. Indazole and azaindazole btk inhibitors
WO2016161570A1 (en) 2015-04-08 2016-10-13 Merck Sharp & Dohme Corp. Azacarbazole btk inhibitors
KR102499359B1 (ko) 2015-04-14 2023-02-10 주식회사 큐리언트 Tam rtk 억제제로서 퀴놀린 유도체들
EP3290418B1 (en) 2015-04-29 2019-05-15 Wuxi Fortune Pharmaceutical Co., Ltd Janus kinase (jak) inhibitors
ES2924698T3 (es) 2015-05-28 2022-10-10 Theravance Biopharma R&D Ip Llc Proceso e intermedios para la preparación de compuestos de naftiridina como inhibidores de quinasa JAK
DK3305788T3 (da) 2015-05-29 2020-09-28 Wuxi Fortune Pharmaceutical Co Ltd Janus-kinase-hæmmer
BR112017025986A2 (pt) 2015-06-02 2018-08-14 Pharmacyclics Llc inibidores de tirosina quinase de bruton.
EP3912979B1 (en) 2015-06-03 2026-03-25 Principia Biopharma Inc. Tyrosine kinase inhibitors
WO2016192074A1 (en) 2015-06-04 2016-12-08 Merck Sharp & Dohme Corp. Btk inhibitors
US20180305350A1 (en) 2015-06-24 2018-10-25 Principia Biopharma Inc. Tyrosine kinase inhibitors
BR112017026173A2 (pt) 2015-07-07 2018-08-14 Japan Tobacco, Inc. Método para produção de derivado de 7h-pirrolo [2,3-d]pirimidina e intermediário do mesmo
US10640495B2 (en) 2015-07-07 2020-05-05 Shionogi & Co., Ltd. Heterocycle derivatives having TrkA inhibitory activity
JP6853234B2 (ja) 2015-07-09 2021-03-31 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 Btk阻害剤としてのピリミジン誘導体及びその使用
US10329277B2 (en) 2015-07-16 2019-06-25 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(3-methyl-2-OXO-2,3-dihydro-1h-benzo[d]imidazol-1-yl)pyrimidin-2-yl)amino)phenyl)acrylamide hydrochloride as an inhibitor of epidermal growth factor receptor activity
CA2992586A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
WO2017015363A1 (en) 2015-07-20 2017-01-26 Dana-Farber Cancer Institute, Inc. Novel pyrimidines as egfr inhibitors and methods of treating disorders
WO2017013237A1 (en) * 2015-07-23 2017-01-26 Institut Curie Use of a combination of dbait molecule and parp inhibitors to treat cancer
WO2017016463A1 (zh) 2015-07-24 2017-02-02 上海海雁医药科技有限公司 Egfr抑制剂及其药学上可接受的盐和多晶型物及其应用
KR101766194B1 (ko) 2015-08-07 2017-08-10 한국과학기술연구원 RET 키나아제 저해제인 신규 3-(이속사졸-3-일)-피라졸로[3,4-d]피리미딘-4-아민 화합물
CN106467541B (zh) 2015-08-18 2019-04-05 暨南大学 取代喹诺酮类衍生物或其药学上可接受的盐或立体异构体及其药用组合物和应用
CN107406431B (zh) 2015-08-20 2020-06-26 上海昂睿医药技术有限公司 吲哚类衍生物及其制备方法和其在医药上的用途
MA41559A (fr) 2015-09-08 2017-12-26 Taiho Pharmaceutical Co Ltd Composé de pyrimidine condensé ou un sel de celui-ci
US10611766B2 (en) 2015-09-16 2020-04-07 Loxo Oncology Inc. Pyrazolopyrimidine derivatives as BTK inhibitors for the treatment of cancer
EP3144307A1 (en) 2015-09-18 2017-03-22 AB Science Novel oxazole derivatives that inhibit syk
CN106554347B (zh) 2015-09-25 2020-10-30 浙江博生医药有限公司 Egfr激酶抑制剂及其制备方法和应用
WO2017059280A1 (en) 2015-10-02 2017-04-06 The University Of North Carolina At Chapel Hill Novel pan-tam inhibitors and mer/axl dual inhibitors
US10358446B2 (en) 2015-10-14 2019-07-23 Zibo Biopolar Changsheng Pharmaceutical Co., Ltd. Bruton's tyrosine kinase inhibitors
EP3365335B1 (en) 2015-10-23 2024-02-14 Array Biopharma, Inc. 2-aryl- and 2-heteroaryl-substituted 2-pyridazin-3(2h)-one compounds as inhibitors of fgfr tyrosine kinases
TWI710560B (zh) 2015-11-03 2020-11-21 美商施萬生物製藥研發Ip有限責任公司 用於治療呼吸疾病之jak激酶抑制劑化合物
CN106699743B (zh) 2015-11-05 2020-06-12 湖北生物医药产业技术研究院有限公司 嘧啶类衍生物及其用途
WO2017077507A1 (en) 2015-11-06 2017-05-11 Acerta Pharma B.V. Imidazopyrazine inhibitors of bruton's tyrosine kinase
SG10201912607SA (en) 2015-11-19 2020-02-27 Blueprint Medicines Corp Compounds and compositions useful for treating disorders related to ntrk
CA3003283A1 (en) 2015-11-24 2017-06-01 Theravance Biopharma R&D Ip, Llc Prodrugs of a jak inhibitor compound for treatment of gastrointestinal inflammatory disease
US10159662B2 (en) 2015-12-11 2018-12-25 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Azetidine derivative, preparation method therefor, and use thereof
HRP20211845T1 (hr) 2015-12-16 2022-03-04 Boehringer Ingelheim International Gmbh Derivati bipirazolila korisni za liječenje autoimunih bolesti
CN106928231B (zh) 2015-12-31 2021-06-01 合肥中科普瑞昇生物医药科技有限公司 一类新型的egfr野生型和突变型的激酶抑制剂
CA3008312A1 (en) 2016-01-06 2017-07-13 Trillium Therapeutics Inc. Novel fluorinated quinazoline derivatives as egfr inhibitors
MX382436B (es) 2016-01-11 2025-03-13 Merck Patent Gmbh Derivados de quinolin-2-ona.
US10570118B2 (en) 2016-01-13 2020-02-25 Boehringer Ingelheim International Gmbh Isoquinolones as BTK inhibitors
AU2017208998B2 (en) 2016-01-21 2021-07-15 Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences Bruton's tyrosine kinase inhibitors
WO2017129116A1 (zh) 2016-01-26 2017-08-03 杭州华东医药集团新药研究院有限公司 吡咯嘧啶五元氮杂环衍生物及其应用
CN107021963A (zh) 2016-01-29 2017-08-08 北京诺诚健华医药科技有限公司 吡唑稠环类衍生物、其制备方法及其在治疗癌症、炎症和免疫性疾病上的应用
WO2017135399A1 (ja) 2016-02-04 2017-08-10 塩野義製薬株式会社 TrkA阻害活性を有する含窒素複素環および炭素環誘導体
BR112018015369A2 (pt) 2016-02-19 2018-12-18 Jiangsu Hengrui Medicine Co., Ltd. composição farmacêutica contendo inibidor de jak cinase ou sal farmaceuticamente aceitável do mesmo
DK3269370T3 (da) 2016-02-23 2020-04-06 Taiho Pharmaceutical Co Ltd Hidtil ukendt kondenseret pyrimidinforbindelse eller salt deraf
KR20220127360A (ko) * 2016-03-01 2022-09-19 옹쎄오 Dbait 분자의 전신 투여에 의한 암 치료법
CN107151249B (zh) 2016-03-04 2020-08-14 华东理工大学 作为flt3抑制剂的蝶啶酮衍生物及应用
AR107912A1 (es) 2016-03-17 2018-06-28 Blueprint Medicines Corp Inhibidores de ret
CN107286077B (zh) 2016-04-01 2021-04-02 合肥中科普瑞昇生物医药科技有限公司 一种选择性的c-kit激酶抑制剂
CN109562181A (zh) 2016-04-29 2019-04-02 X-化学有限公司 共价btk抑制剂及其用途
CN109311858B (zh) 2016-05-26 2021-12-03 里科瑞尔姆Ip控股有限责任公司 Egfr抑制剂化合物
CN107759600A (zh) 2016-06-16 2018-03-06 正大天晴药业集团股份有限公司 作为jak抑制剂的吡咯并嘧啶化合物的结晶
WO2018001251A1 (zh) 2016-06-27 2018-01-04 杭州雷索药业有限公司 苯并呋喃吡唑胺类蛋白激酶抑制剂
US10640512B2 (en) 2016-06-30 2020-05-05 Hangzhou Sanyintai Pharmaceutical Technology Co., Ltd. Imidazopyrazinamine phenyl derivative and use thereof
WO2018002958A1 (en) 2016-06-30 2018-01-04 Sun Pharma Advanced Research Company Limited Novel hydrazide containing compounds as btk inhibitors
EP3481831B1 (en) 2016-07-07 2023-09-06 Daewoong Pharmaceutical Co., Ltd. 4-aminopyrazolo[3,4-d]pyrimidinylazabicyclo derivatives and pharmaceutical composition comprising the same
CN107619388A (zh) 2016-07-13 2018-01-23 南京天印健华医药科技有限公司 作为fgfr抑制剂的杂环化合物
WO2018017983A1 (en) 2016-07-22 2018-01-25 Blueprint Medicines Corporation Compounds useful for treating disorders related to ret
US10035789B2 (en) 2016-07-27 2018-07-31 Blueprint Medicines Corporation Compounds useful for treating disorders related to RET
CN107698593A (zh) 2016-08-09 2018-02-16 南京天印健华医药科技有限公司 作为fgfr抑制剂的杂环化合物
AU2017312970B2 (en) 2016-08-16 2021-08-12 Merck Patent Gmbh 2-oxo-imidazopyridines as reversible BTK inhibitors and uses thereof
SG11201901251SA (en) 2016-08-29 2019-03-28 Univ Michigan Regents Aminopyrimidines as alk inhibitors
TW201822764A (zh) 2016-09-14 2018-07-01 美商基利科學股份有限公司 Syk抑制劑
EP3512519A1 (en) 2016-09-14 2019-07-24 Gilead Sciences, Inc. Syk inhibitors
CN107840842A (zh) 2016-09-19 2018-03-27 北京天诚医药科技有限公司 炔代杂环化合物、其制备方法及其在医药学上的应用
CN107840846B (zh) 2016-09-19 2020-11-24 郑州泰基鸿诺医药股份有限公司 一种含嘧啶环的化合物、egfr抑制剂及其应用
JP2018052878A (ja) 2016-09-29 2018-04-05 第一三共株式会社 ピリジン化合物
TWI752098B (zh) 2016-10-10 2022-01-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
WO2018079759A1 (ja) 2016-10-31 2018-05-03 塩野義製薬株式会社 TrkA阻害活性を有する縮合複素環および縮合炭素環誘導体
KR102686957B1 (ko) 2016-11-08 2024-07-22 주식회사 대웅제약 신규한 피롤로피리미딘 유도체 및 이를 포함하는 약학적 조성물
ES3006132T3 (en) 2016-11-15 2025-03-17 Hangzhou Healzen Therapeutics Co Ltd Selective bruton's tyrosine kinase inhibitor and use thereof
AU2017363161B2 (en) 2016-11-18 2020-05-28 The Regents Of The University Of Michigan 5,6-dihydro-11H-indolo[2,3-b]quinolin-11-ones as ALK inhibitors
CN108101905A (zh) 2016-11-24 2018-06-01 中国科学院上海药物研究所 嘧啶并[5,4-b]吲嗪或嘧啶并[5,4-b]吡呤化合物、其制备方法及用途
WO2018108083A1 (zh) 2016-12-12 2018-06-21 杭州英创医药科技有限公司 作为Syk抑制剂和/或Syk-HDAC双重抑制剂的杂环化合物
WO2018108064A1 (zh) 2016-12-13 2018-06-21 南京明德新药研发股份有限公司 作为第四代egfr激酶抑制剂的螺环芳基磷氧化合物
US11117883B2 (en) 2016-12-15 2021-09-14 Ariad Pharmaceuticals, Inc. Benzimidazole compounds as c-Kit inhibitors
WO2018112136A1 (en) 2016-12-15 2018-06-21 Ariad Pharmaceuticals, Inc. Aminothiazole compounds as c-kit inhibitors
CN108250200A (zh) 2016-12-28 2018-07-06 中国科学院上海药物研究所 一种具有Axl抑制活性的化合物及其制备和应用
CN110139865B (zh) 2016-12-29 2022-02-18 石药集团中奇制药技术(石家庄)有限公司 Fgfr抑制剂
JP7053665B2 (ja) 2016-12-30 2022-04-12 南京明徳新薬研発有限公司 Egfr阻害としてのキナゾリン系化合物
CN108276410B (zh) 2017-01-06 2021-12-10 首药控股(北京)股份有限公司 一种间变性淋巴瘤激酶抑制剂及其制备方法和用途
CN115844877B (zh) 2017-01-10 2024-07-23 浙江嘉驰医药开发有限公司 拉索昔芬调节膜结合雌激素信号的应用及治疗癌症的方法
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
JP6888101B2 (ja) 2017-01-18 2021-06-16 アレイ バイオファーマ インコーポレイテッド RETキナーゼ阻害剤としての置換ピラゾロ[1,5−a]ピラジン化合物
CN106831787B (zh) 2017-01-20 2018-10-23 成都倍特药业有限公司 用作布鲁顿酪氨酸激酶抑制剂的化合物及其制备方法和应用
US11608334B2 (en) 2017-02-08 2023-03-21 The National Institutes of Pharmaceutical R&D Co., Ltd. Pyrrolo-aromatic heterocyclic compound, preparation method therefor, and medical use thereof
WO2018153293A1 (zh) 2017-02-27 2018-08-30 北京赛特明强医药科技有限公司 二噁烷并喹唑啉与二噁烷并喹啉类化合物及其制备方法与应用
US10464923B2 (en) 2017-02-27 2019-11-05 Merck Patent Gmbh Crystalline forms of 1-(4-{[6-amino-5-(4-phenoxy-phenyl)-pyrimidin-4-ylamino]-methyl}-piperidin-1-yl)-propenone
JP6876833B2 (ja) 2017-02-27 2021-05-26 ▲貝▼▲達▼▲薬▼▲業▼股▲フン▼有限公司Betta Pharmaceuticals Co., Ltd. Fgfr阻害剤およびその使用
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
US11554118B2 (en) 2017-03-22 2023-01-17 Xibin Liao Bruton's tyrosine kinase inhibitors
WO2018187355A1 (en) 2017-04-03 2018-10-11 Health Research Inc. Met kinase inhibitors and uses therefor
CN108721298A (zh) 2017-04-19 2018-11-02 华东理工大学 作为布鲁顿酪氨酸激酶抑制剂的嘧啶并杂环化合物及其应用
CN108727382B (zh) 2017-04-19 2022-07-19 华东理工大学 作为btk抑制剂的杂环化合物及其应用
CN107043366B (zh) 2017-04-25 2020-05-26 中国药科大学 4-氨基嘧啶类化合物、其制备方法及医药用途
AU2018257203B2 (en) 2017-04-27 2022-05-26 Mochida Pharmaceutical Co., Ltd. Novel tetrahydronaphthyl urea derivatives
AR111495A1 (es) 2017-05-01 2019-07-17 Theravance Biopharma R&D Ip Llc Compuestos de imidazo-piperidina fusionada como inhibidores de jak
WO2018208132A1 (en) 2017-05-12 2018-11-15 Korea Research Institute Of Chemical Technology Pyrazolopyrimidine derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating cancer, autoimmune disease and brain disease containing the same as an active ingredient
JP7256757B2 (ja) 2017-05-22 2023-04-12 エフ. ホフマン-ラ ロシュ アーゲー 処置用化合物及び組成物、並びにその使用方法
WO2018215390A1 (en) 2017-05-22 2018-11-29 F. Hoffmann-La Roche Ag Therapeutic compounds and compositions, and methods of use thereof
CN107176954B (zh) 2017-06-02 2019-01-11 无锡双良生物科技有限公司 一种egfr抑制剂的药用盐及其晶型、制备方法和应用
WO2018228475A1 (zh) 2017-06-14 2018-12-20 正大天晴药业集团股份有限公司 Syk抑制剂及其使用方法
CN109111446B (zh) 2017-06-22 2021-11-30 上海度德医药科技有限公司 一种具有药物活性的杂芳基化合物
EP3645526B1 (en) 2017-06-27 2024-09-04 Janssen Pharmaceutica NV New quinolinone compounds
JP2020526499A (ja) 2017-07-05 2020-08-31 シーエス ファーマテック リミテッド Egfrチロシンキナーゼの臨床上重要な突然変異体の選択的阻害剤
WO2019034009A1 (en) 2017-08-12 2019-02-21 Beigene, Ltd. BTK INHIBITOR WITH ENHANCED DOUBLE SELECTIVITY
WO2019034075A1 (zh) 2017-08-15 2019-02-21 南京明德新药研发股份有限公司 Fgfr和egfr抑制剂
CN111247150B (zh) 2017-08-15 2022-11-08 石药集团中奇制药技术(石家庄)有限公司 Fgfr抑制剂及其医药用途
EP3670500A4 (en) 2017-08-18 2020-12-16 Beijing Hanmi Pharmaceutical Co., Ltd. CHEMICAL COMPOUND, PHARMACEUTICAL COMPOSITION OF IT, CORRESPONDING USE AND APPLICATION
CN109400610A (zh) 2017-08-18 2019-03-01 浙江海正药业股份有限公司 吡咯并三嗪类衍生物、其制备方法及其在医药上的用途
US11384076B2 (en) 2017-08-18 2022-07-12 Universität Regensburg Synthesis, pharmacology and use of new and selective FMS-like tyrosine kinase 3 (FLT3) FLT3 inhibitors

Also Published As

Publication number Publication date
CN114364798A (zh) 2022-04-15
WO2020188015A1 (en) 2020-09-24
IL284856A (en) 2021-08-31
JP2022526713A (ja) 2022-05-26
MX2021009863A (es) 2021-11-12
EP3942045A1 (en) 2022-01-26
BR112021018168B1 (pt) 2023-11-28
AU2020242287A1 (en) 2021-09-02
KR20210142154A (ko) 2021-11-24
CA3129665A1 (en) 2020-09-24
BR112021018168A2 (ru) 2021-11-16
US20220143049A1 (en) 2022-05-12

Similar Documents

Publication Publication Date Title
IL292643A (en) Ras inhibitors
IL292644A (en) Ras inhibitors
IL292642A (en) Ras inhibitors
LT3986897T (lt) Egfr inhibitorius, skirtas vėžiui gydyti
CY1124483T1 (el) Συνθεσεις και μεθοδοι για την αναστολη της δραστικοτητας της αργινασης
IL290527A (en) Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
EP4125884A4 (en) COMBINATIONS OF EIF4A INHIBITORS
IL284199A (en) Csf1r inhibitors for use in treating cancer
EA202092590A1 (ru) Пиридазиноны в качестве ингибиторов parp7
EA202193015A1 (ru) Ингибиторы cdk
EA201691421A1 (ru) Гетероарилы и их применение
EA201891024A1 (ru) Соединения-ингибиторы tank-связывающей киназы
EA201792205A1 (ru) Гетероциклические соединения как ингибиторы lsd1
SA519410093B1 (ar) مركبات بيريميدو بيريميدينون مفيدة كمثبطات دبليو إى إى-1 كيناز
EA201591509A1 (ru) Ингибиторы cdc7
ZA202202245B (en) Quinoline derivatives as protein kinase inhibitors
EA201692470A1 (ru) Фармацевтические комбинации
EP4003986A4 (en) Inhibitor compounds
DK3956322T3 (da) Jak1-selektiv kinaseinhibitor
MX2019014845A (es) Compuestos de aminotiazol como inhibidores de la proteina quinasa.
JOP20210036A1 (ar) مثبطات او- جليكوبروتين-2-أسيتاميدو-2-ديوكسي-3-دي-جلوكوبيرانوسيداز
EA201790484A1 (ru) Производные тетрагидрохинолина в качестве ингибиторов бромодомена
EA201590744A1 (ru) Лечение рака tor киназными ингибиторами
MX388409B (es) Composiciones y metodos para tratar canceres.
MX2021009863A (es) Una molecula dbait en combinacion con inhibidor de quinasa para el tratamiento del cancer.