JP5611826B2 - タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン - Google Patents

タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン Download PDF

Info

Publication number
JP5611826B2
JP5611826B2 JP2010524122A JP2010524122A JP5611826B2 JP 5611826 B2 JP5611826 B2 JP 5611826B2 JP 2010524122 A JP2010524122 A JP 2010524122A JP 2010524122 A JP2010524122 A JP 2010524122A JP 5611826 B2 JP5611826 B2 JP 5611826B2
Authority
JP
Japan
Prior art keywords
formula
phenyl
triazol
pyrimidin
procedure
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2010524122A
Other languages
English (en)
Japanese (ja)
Other versions
JP2010538076A (ja
JP2010538076A5 (OSRAM
Inventor
カメネッカ，セオドア，マーク
チャン，ロン
ソン，シンイ
ログラッソ，フィリップ
キャメロン，マイケル，ダーリン
ダケット，デリク，アール
Original Assignee
ザ スクリプス リサーチ インスティテュート
ザ スクリプス リサーチ インスティテュート
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 ザ スクリプス リサーチ インスティテュート, ザ スクリプス リサーチ インスティテュート filed Critical ザ スクリプス リサーチ インスティテュート
Publication of JP2010538076A publication Critical patent/JP2010538076A/ja
Publication of JP2010538076A5 publication Critical patent/JP2010538076A5/ja
Application granted granted Critical
Publication of JP5611826B2 publication Critical patent/JP5611826B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/113—Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Psychology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2010524122A 2007-09-04 2008-09-03 タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン Expired - Fee Related JP5611826B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US96984907P 2007-09-04 2007-09-04
US60/969,849 2007-09-04
PCT/US2008/075151 WO2009032861A1 (en) 2007-09-04 2008-09-03 Substituted pyrimidinyl-amines as protein kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2014177846A Division JP5937648B2 (ja) 2007-09-04 2014-09-02 タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン

Publications (3)

Publication Number Publication Date
JP2010538076A JP2010538076A (ja) 2010-12-09
JP2010538076A5 JP2010538076A5 (OSRAM) 2011-10-13
JP5611826B2 true JP5611826B2 (ja) 2014-10-22

Family

ID=40429327

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2010524122A Expired - Fee Related JP5611826B2 (ja) 2007-09-04 2008-09-03 タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン
JP2014177846A Expired - Fee Related JP5937648B2 (ja) 2007-09-04 2014-09-02 タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2014177846A Expired - Fee Related JP5937648B2 (ja) 2007-09-04 2014-09-02 タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン

Country Status (7)

Country Link
US (3) US8530480B2 (OSRAM)
EP (1) EP2200436B1 (OSRAM)
JP (2) JP5611826B2 (OSRAM)
CA (1) CA2698511C (OSRAM)
ES (1) ES2535166T3 (OSRAM)
PT (1) PT2200436E (OSRAM)
WO (1) WO2009032861A1 (OSRAM)

Families Citing this family (98)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080153863A1 (en) 2006-12-22 2008-06-26 Caterina Bissantz Spiropiperidine derivatives
HUE029188T2 (en) * 2007-03-12 2017-03-28 Ym Biosciences Australia Pty Phenylamino-pyrimidine compounds and their use
AU2013201306B2 (en) * 2007-03-12 2015-11-12 Glaxosmithkline Llc Phenyl Amino Pyrimidine Compounds and Uses Thereof
AU2016200866B2 (en) * 2007-03-12 2017-06-22 Glaxosmithkline Llc Phenyl amino pyrimidine compounds and uses thereof
US8507511B2 (en) * 2007-04-24 2013-08-13 Ingenium Pharmaceuticals Gmbh Inhibitors of protein kinases
ES2535166T3 (es) 2007-09-04 2015-05-06 The Scripps Research Institute Pirimidinil-aminas sustituidas como inhibidores de proteína-quinasas
ATE535515T1 (de) 2008-01-11 2011-12-15 Hoffmann La Roche Modulatoren für amyloid beta
RU2010137300A (ru) * 2008-02-22 2012-03-27 Ф. Хоффманн-Ля Рош Аг (Ch) Модуляторы бета-амилоида
CN102177151A (zh) 2008-10-09 2011-09-07 弗·哈夫曼-拉罗切有限公司 β-淀粉样蛋白的调节剂
MX2011004954A (es) 2008-11-10 2011-05-30 Hoffmann La Roche Moduladores heterociclicos de gamma-secretasa.
EP2488503A1 (en) * 2009-10-12 2012-08-22 Myrexis, Inc. Amino - pyrimidine compounds as inhibitors of tbkl and/or ikk epsilon
WO2011075560A1 (en) 2009-12-17 2011-06-23 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
MA33926B1 (fr) 2009-12-17 2013-01-02 Merck Sharp & Dohme Aminopyrimidines en tant qu'inhibiteurs de la syk
US8486967B2 (en) 2010-02-17 2013-07-16 Hoffmann-La Roche Inc. Heteroaryl substituted piperidines
ES2603032T3 (es) 2010-07-15 2017-02-23 Bayer Intellectual Property Gmbh Compuestos de 3-piridil-heteroarilcarboxamida como pesticidas
GB201012105D0 (en) 2010-07-19 2010-09-01 Domainex Ltd Novel pyrimidine compounds
WO2012018638A2 (en) 2010-07-26 2012-02-09 Biomatrica, Inc. Compositions for stabilizing dna, rna and proteins in blood and other biological samples during shipping and storage at ambient temperatures
EP2598661B1 (en) 2010-07-26 2017-09-27 Biomatrica, INC. Compositions for stabilizing dna, rna and proteins in saliva and other biological samples during shipping and storage at ambient temperatures
JP5953308B2 (ja) * 2010-10-22 2016-07-20 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 殺害虫剤としての新規ヘテロ環式化合物
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
JP6085866B2 (ja) 2011-02-28 2017-03-01 アレイ バイオファーマ、インコーポレイテッド セリン／トレオニンキナーゼインヒビター
CN103889962B (zh) 2011-04-01 2017-05-03 犹他大学研究基金会 作为受体酪氨酸激酶btk抑制剂的取代的n‑(3‑(嘧啶‑4‑基)苯基)丙烯酰胺类似物
CN103732067A (zh) * 2011-04-12 2014-04-16 美国阿尔茨海默病研究所公司 化合物，组合物及它们的治疗用途
ES2613103T3 (es) 2011-04-19 2017-05-22 Bayer Intellectual Property Gmbh 4-Aril-n-fenil-1,3,5-triacin-2-aminas sustituidas
EP2706852B1 (en) 2011-05-10 2018-08-22 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors
JP2014513687A (ja) 2011-05-10 2014-06-05 メルク・シャープ・アンド・ドーム・コーポレーション Ｓｙｋ阻害薬としてのピリジルアミノピリジン
EP2706853B1 (en) 2011-05-10 2017-06-14 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
TWI555737B (zh) 2011-05-24 2016-11-01 拜耳知識產權公司 含有硫醯亞胺基團之４－芳基－ｎ－苯基－１，３，５－三氮雜苯－２－胺
US20130019348A1 (en) * 2011-07-12 2013-01-17 Dow Agrosciences Llc Pesticidal compositions and processes related thereto
BR112014002675A2 (pt) 2011-08-04 2017-02-21 Array Biopharma Inc "quinazolina como inibidores de serina/treonina quinase, seus usos, e composição"
DE102011112978A1 (de) * 2011-09-09 2013-03-14 Merck Patent Gmbh Benzonitrilderivate
EP2755948B1 (en) 2011-09-16 2016-05-25 Bayer Intellectual Property GmbH Disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group
US9108926B2 (en) 2011-09-16 2015-08-18 Bayer Intellectual Property Gmbh Disubstituted 5-fluoro-pyrimidines
PL2820009T3 (pl) 2012-03-01 2018-09-28 Array Biopharma, Inc. Inhibitory kinaz serynowo/treoninowych
PE20190736A1 (es) 2012-06-13 2019-05-23 Incyte Holdings Corp Compuestos triciclicos sustituidos como inhibidores del receptor del factor de crecimiento de fibroblastos (fgfr)
US8809359B2 (en) 2012-06-29 2014-08-19 Ym Biosciences Australia Pty Ltd Phenyl amino pyrimidine bicyclic compounds and uses thereof
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
CA2882750A1 (en) 2012-08-27 2014-03-06 Jim Blake Serine/threonine kinase inhibitors for the treatment of hyperproliferative|diseases
EP2903972B1 (en) * 2012-10-04 2019-12-04 University of Utah Research Foundation Substituted n-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase btk 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
CN105102434A (zh) 2012-10-18 2015-11-25 拜耳药业股份公司 含砜基团的4-(邻)-氟苯基-5-氟嘧啶-2-基胺
HK1209414A1 (en) 2012-10-18 2016-04-01 Bayer Pharma Aktiengesellschaft 5-fluoro-n-(pyridin-2-yl)pyridin-2-amine derivatives containing a sulfone group
TW201418243A (zh) 2012-11-15 2014-05-16 Bayer Pharma AG 含有磺醯亞胺基團之ｎ－（吡啶－２－基）嘧啶－４－胺衍生物
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
EP3249054A1 (en) 2012-12-20 2017-11-29 Biomatrica, INC. Formulations and methods for stabilizing pcr reagents
GB201303109D0 (en) * 2013-02-21 2013-04-10 Domainex Ltd Novel pyrimidine compounds
KR102269032B1 (ko) 2013-04-19 2021-06-24 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
EP3007556B1 (en) 2013-06-13 2020-05-20 Biomatrica, INC. Cell stabilization
EP3942931A1 (en) 2014-06-10 2022-01-26 Biomatrica, INC. Stabilization of thrombocytes at ambient temperatures
TW202134236A (zh) 2014-06-12 2021-09-16 美商西爾拉癌症醫學公司 N-(氰基甲基)-4-(2-(4-𠰌啉基苯基胺基)嘧啶-4-基)苯甲醯胺
CA2964683A1 (en) 2014-10-16 2016-04-21 Bayer Pharma Aktiengesellschaft Fluorinated benzofuranyl-pyrimidine derivatives containing a sulfone group
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
ES2895769T3 (es) 2015-02-20 2022-02-22 Incyte Corp Heterociclos bicíclicos como inhibidores de FGFR
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016150903A1 (en) 2015-03-24 2016-09-29 Bayer Pharma Aktiengesellschaft Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating lymphomas
WO2016150902A1 (en) 2015-03-24 2016-09-29 Bayer Pharma Aktiengesellschaft Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating gastric cancers
EP3274338A1 (en) 2015-03-24 2018-01-31 Bayer Pharma Aktiengesellschaft Use of 4-(4-fluoro-2-methoxyphenyl)-n-{3-[(s-methylsulfonimidoyl)methyl]phenyl}-1,3,5-triazin-2-amine for treating multiple myeloma
EP3319968A1 (en) 2015-07-06 2018-05-16 Rodin Therapeutics, Inc. Heterobicyclic n-aminophenyl-amides as inhibitors of histone deacetylase
ES2899906T3 (es) 2015-07-06 2022-03-15 Alkermes Inc Inhibidores bicíclicos de histona desacetilasa
CA2999931A1 (en) 2015-09-29 2017-04-06 Bayer Pharma Aktiengesellschaft Novel macrocyclic sulfondiimine compounds
JP6888000B2 (ja) 2015-10-08 2021-06-16 バイエル ファーマ アクチエンゲゼルシャフト 新規な修飾された大環状化合物
WO2017060322A2 (en) 2015-10-10 2017-04-13 Bayer Pharma Aktiengesellschaft Ptefb-inhibitor-adc
MY196174A (en) 2015-10-12 2023-03-20 Chong Kun Dang Pharmaceutical Corp Oxadiazole Amine Derivative Compounds as Histone Deacetylase 6 Inhibitor, and the Pharmaceutical Composition Comprising the Same
KR20250047404A (ko) 2015-12-08 2025-04-03 바이오매트리카 인코포레이티드 적혈구 침강 속도의 감소
JP6740452B2 (ja) 2016-07-26 2020-08-12 深▲セン▼市塔吉瑞生物医▲薬▼有限公司Ｓｈｅｎｚｈｅｎ ＴａｒｇｅｔＲｘ，Ｉｎｃ． プロテインチロシンキナーゼの活性を阻害するためのアミノピリミジン系化合物
US20190231751A1 (en) * 2016-09-12 2019-08-01 Imago Pharmaceuticals, Inc. Treatment of fibrotic disorders with jun n-terminal kinase inhibitors
ES2875562T3 (es) 2017-01-11 2021-11-10 Alkermes Inc Inhibidores bicíclicos de histona desacetilasa
US20190381125A1 (en) * 2017-02-15 2019-12-19 University Of Massachusetts Methods of Treating Angiogenesis-Related Disorders Using JNK3 Inhibitors
GB201702947D0 (en) 2017-02-23 2017-04-12 Domainex Ltd Novel compounds
EP3601236A1 (en) 2017-03-28 2020-02-05 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
ES2900199T3 (es) 2017-03-28 2022-03-16 Bayer Ag Novedosos compuestos macrocíclicos inhibidores de PTEFB
GB201705263D0 (en) * 2017-03-31 2017-05-17 Probiodrug Ag Novel inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
US11225475B2 (en) 2017-08-07 2022-01-18 Alkermes, Inc. Substituted pyridines as inhibitors of histone deacetylase
CA3078579A1 (en) * 2017-10-17 2019-04-25 Merck Patent Gmbh Pyrimidine tbk/ikk.epsilon. inhibitor compounds and uses thereof
RU2020115295A (ru) 2017-10-17 2021-11-18 Мерк Патент Гмбх ПИРИМИДИНОВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ ΤΒΚ/ΙΚΚε И ИХ ПРИМЕНЕНИЕ
EP3732285A1 (en) 2017-12-28 2020-11-04 Tract Pharmaceuticals, Inc. Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
US11701347B2 (en) 2018-02-13 2023-07-18 Bayer Aktiengesellschaft Use of 5-fluoro-4-(4-fluoro-2-methoxyphenyl)-N-{4-[(S-methylsulfonimidoyl)methyl]pyridin-2-yl}pyridin-2-amine for treating diffuse large B-cell lymphoma
SI3788047T1 (sl) 2018-05-04 2024-11-29 Incyte Corporation Trdne oblike inhibitorja fgfr in postopki priprave le-teh
SG11202010882XA (en) 2018-05-04 2020-11-27 Incyte Corp Salts of an fgfr inhibitor
WO2020068846A1 (en) * 2018-09-25 2020-04-02 Heterocyclic Compound Heterocyclic compound
MX2021003516A (es) * 2018-09-25 2021-05-27 Cardurion Pharmaceuticals Llc Compuesto de aminopirimidina.
CN113473860A (zh) * 2018-12-21 2021-10-01 拜耳公司 作为新的抗真菌剂的1，3，4-噁二唑及其衍生物
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US20220348590A1 (en) * 2019-09-13 2022-11-03 The Board Institute, Inc. Cyclooxygenase-2 inhibitors and uses thereof
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11607416B2 (en) 2019-10-14 2023-03-21 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2021113462A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7587113B2 (ja) * 2020-09-29 2024-11-20 日亜化学工業株式会社 異方性磁性粉末の製造方法および異方性磁性粉末
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4876252A (en) 1986-01-13 1989-10-24 American Cyanamid Company 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines
US4788195A (en) * 1986-01-13 1988-11-29 American Cyanamid Company 4,5,6-substituted-N-(substituted-phenyl)-2-pyrimidinamines
ES2087056T3 (es) * 1986-01-13 1996-07-16 American Cyanamid Co 2-pirimidinaminas sustituidas en las posiciones 4, 5 y 6.
US5521184A (en) * 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
TW225528B (OSRAM) 1992-04-03 1994-06-21 Ciba Geigy Ag
ATE325113T1 (de) * 1993-10-01 2006-06-15 Novartis Pharma Gmbh Pharmacologisch wirksame pyrimidinderivate und verfahren zu deren herstellung
GB9523675D0 (en) * 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
GB9619284D0 (en) * 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
GB9924862D0 (en) * 1999-10-20 1999-12-22 Celltech Therapeutics Ltd Chemical compounds
GB0004887D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US7129242B2 (en) * 2000-12-06 2006-10-31 Signal Pharmaceuticals, Llc Anilinopyrimidine derivatives as JNK pathway inhibitors and compositions and methods related thereto
CA2441733A1 (en) * 2001-03-29 2002-10-10 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
CA2446939C (en) * 2001-05-16 2005-08-02 Matthias Stein-Gerlach Pyridylpyrimidine derivatives as effective compounds against prion diseases
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
EP2172460A1 (en) 2002-11-01 2010-04-07 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
AU2003286895A1 (en) * 2002-11-05 2004-06-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of jak and other protein kinases
GB0308466D0 (en) * 2003-04-11 2003-05-21 Novartis Ag Organic compounds
WO2005012262A1 (en) 2003-07-30 2005-02-10 Cyclacel Limited 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
CA2578122A1 (en) 2004-08-27 2006-03-02 Gpc Biotech Ag Pyrimidine derivatives
MX2007004488A (es) * 2004-10-13 2007-09-11 Wyeth Corp Analogos de anilino-pirimidina n-bencenosulfonilo sustituidos.
CA2635888A1 (en) 2006-01-04 2007-07-19 Locus Pharmaceuticals, Inc. Inhibitors of protein kinases
EP1979329A2 (en) * 2006-01-30 2008-10-15 Exelixis, Inc. 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as jak-2 modulators and methods of use
WO2008075151A2 (en) 2006-12-18 2008-06-26 Fundamo (Proprietary) Limited Transaction system and method
WO2008079933A2 (en) * 2006-12-22 2008-07-03 Novartis Ag Heteroaryl-heteroaryl compounds as cdk inhibitors for the treatment of cancer, inflammation and viral infections
AT504205B1 (de) * 2007-01-02 2008-04-15 Hoermann Richard Dr Einrichtung zur entkeimung eines fluids
AU2008208801A1 (en) * 2007-01-23 2008-07-31 Palau Pharma, S. A. Purine derivatives
HUE029188T2 (en) * 2007-03-12 2017-03-28 Ym Biosciences Australia Pty Phenylamino-pyrimidine compounds and their use
WO2008124085A2 (en) * 2007-04-03 2008-10-16 Exelixis, Inc. Methods of using combinations of mek and jak-2 inhibitors
WO2009017838A2 (en) * 2007-08-01 2009-02-05 Exelixis, Inc. Combinations of jak-2 inhibitors and other agents
ES2535166T3 (es) 2007-09-04 2015-05-06 The Scripps Research Institute Pirimidinil-aminas sustituidas como inhibidores de proteína-quinasas
HRP20170317T1 (hr) * 2008-02-15 2017-04-21 Rigel Pharmaceuticals, Inc. Spojevi pirimidin-2-amina i njihova uporaba kao inhibitora jak kinaza
RU2010137300A (ru) * 2008-02-22 2012-03-27 Ф. Хоффманн-Ля Рош Аг (Ch) Модуляторы бета-амилоида

Also Published As

Publication number Publication date
JP2015007102A (ja) 2015-01-15
CA2698511A1 (en) 2009-03-12
ES2535166T3 (es) 2015-05-06
EP2200436B1 (en) 2015-01-21
JP5937648B2 (ja) 2016-06-22
EP2200436A4 (en) 2011-12-28
JP2010538076A (ja) 2010-12-09
US9018205B2 (en) 2015-04-28
WO2009032861A1 (en) 2009-03-12
CA2698511C (en) 2016-10-11
US20150232429A1 (en) 2015-08-20
PT2200436E (pt) 2015-04-29
US20130231336A1 (en) 2013-09-05
US8530480B2 (en) 2013-09-10
US20100298312A1 (en) 2010-11-25
EP2200436A1 (en) 2010-06-30

Similar Documents

Publication Publication Date Title
JP5937648B2 (ja) タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン
US11098061B2 (en) MK2 inhibitors and uses thereof
US11390618B2 (en) Inhibitors of cyclin-dependent kinases
US11186554B2 (en) Non-fused tricyclic compounds
TWI535442B (zh) A nitrogen-containing heterocyclic compound having an action of inhibiting the production of canine erythritine
EP2984088B1 (en) Quinazolines and azaquinazolines as dual inhibitors of ras/raf/mek/erk and pi3k/akt/pten/mtor pathways
US8324231B2 (en) Pyrimidinones as casein kinase II (CK2) modulators
KR20140041583A (ko) Ｌｒｒｋ2 키나제 활성의 억제제
TWI469975B (zh) ５－羥基嘧啶－４－羧醯胺衍生物
TW202028188A (zh) 新穎胺基-嘧啶酮基-哌啶基衍生物、其製備之方法及包含其之醫藥組合物
KR20240093844A (ko) Gpr39 단백질의 길항제
US20250333405A1 (en) Antagonists of gpr39 protein
EP3057950A1 (en) Phenyl linked quinolinyl modulators of ror-gamma-t
EA049416B1 (ru) Ингибиторы аутофагии на основе гетероариламинопиримидинамида и способы их применения
HK1215810B (en) Quinazolines and azaquinazolines as dual inhibitors of ras/raf/mek/erk and pi3k/akt/pten/mtor pathways
HK1133012B (en) Pyrimidinones as casein kinase ii (ck2) modulators
HK1181753A1 (en) Pyrimidine compounds as inhibitors of protein kinases ikk epsilon and/or tbk-1, processes for their preparation, and pharmaceutical compositions containing them

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20110826

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20110826

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120727

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20130711

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20130723

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20131015

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20131022

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20140318

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140612

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20140708

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20140710

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20140805

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20140903

R150 Certificate of patent or registration of utility model

Ref document number: 5611826

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees