JP2006518381A - プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール - Google Patents

プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール Download PDF

Info

Publication number
JP2006518381A
JP2006518381A JP2006503279A JP2006503279A JP2006518381A JP 2006518381 A JP2006518381 A JP 2006518381A JP 2006503279 A JP2006503279 A JP 2006503279A JP 2006503279 A JP2006503279 A JP 2006503279A JP 2006518381 A JP2006518381 A JP 2006518381A
Authority
JP
Japan
Prior art keywords
heteroatoms
ring
optionally substituted
membered
independently
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.)
Pending
Application number
JP2006503279A
Other languages
English (en)
Japanese (ja)
Other versions
JP2006518381A5 (https=
Inventor
アレックス アロノブ，
マイケル アール． ヘイル，
フランソワ マルタワ，
チン タン，
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of JP2006518381A publication Critical patent/JP2006518381A/ja
Publication of JP2006518381A5 publication Critical patent/JP2006518381A5/ja
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • 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
    • A61P31/12—Antivirals
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C07D401/14—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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
JP2006503279A 2003-02-07 2004-02-03 プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール Pending JP2006518381A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US44596203P 2003-02-07 2003-02-07
US46384703P 2003-04-18 2003-04-18
PCT/US2004/003026 WO2004072063A1 (en) 2003-02-07 2004-02-03 Heteroaryl substituted pyrolls useful as inhibitors of protein kinases

Publications (2)

Publication Number Publication Date
JP2006518381A true JP2006518381A (ja) 2006-08-10
JP2006518381A5 JP2006518381A5 (https=) 2007-03-22

Family

ID=32871966

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2006503279A Pending JP2006518381A (ja) 2003-02-07 2004-02-03 プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール

Country Status (6)

Country Link
US (1) US7407962B2 (https=)
EP (1) EP1611125A1 (https=)
JP (1) JP2006518381A (https=)
AU (1) AU2004212421B2 (https=)
CA (1) CA2515132C (https=)
WO (1) WO2004072063A1 (https=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012508223A (ja) * 2008-11-10 2012-04-05 ユニバーシティ オブ バーゼル トリアジン、ピリミジン、及びピリジン類似体、並びに、治療薬及び診断プローブとしてのそれらの使用
JP2014510068A (ja) * 2011-03-02 2014-04-24 リード ディスカバリー センター ゲーエムベーハー 薬学的活性化二置換トリアジン誘導体
JP2015530980A (ja) * 2012-08-02 2015-10-29 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性な置換ピロール類

Families Citing this family (84)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1317450B1 (en) * 2000-09-15 2006-11-22 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
JP2007512275A (ja) * 2003-11-24 2007-05-17 エフ．ホフマン−ラ　ロシュ　アーゲー ピラゾリルおよびイミダゾリルピリミジン
EP1730134A1 (en) 2004-03-26 2006-12-13 Vertex Pharmaceuticals Incorporated Pyridine inhibitors of erk2 and uses thereof
CA2596830A1 (en) * 2005-02-03 2006-09-14 Vertex Pharmaceuticals Incorporated Pyrrolopyrimidines useful as inhibitors of protein kinase
WO2006127587A1 (en) * 2005-05-20 2006-11-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
EP2258358A3 (en) 2005-08-26 2011-09-07 Braincells, Inc. Neurogenesis with acetylcholinesterase inhibitor
EP1928437A2 (en) 2005-08-26 2008-06-11 Braincells, Inc. Neurogenesis by muscarinic receptor modulation
EP2270014A1 (en) 2005-09-22 2011-01-05 Incyte Corporation Azepine inhibitors of janus kinases
UY29827A1 (es) * 2005-10-03 2007-05-31 Astrazeneca Ab 2-amina-pirimidina-4-(2-metil-1-(tetrahidro-2h-piran-4-il)-1-imidazol-5-y1) sustituidas y sus derivados, composiciones farmacéuticas que las contienen, procesos para su preparación y aplicaciones
CN101321531A (zh) * 2005-10-03 2008-12-10 阿斯利康(瑞典)有限公司 嘧啶衍生物在制备用于预防和/或治疗阿尔茨海默病的药物中的用途
EP1940389A2 (en) 2005-10-21 2008-07-09 Braincells, Inc. Modulation of neurogenesis by pde inhibition
US20070112017A1 (en) 2005-10-31 2007-05-17 Braincells, Inc. Gaba receptor mediated modulation of neurogenesis
EP2455382B1 (en) 2005-12-13 2016-10-26 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
US20070155746A1 (en) * 2005-12-23 2007-07-05 Kalypsys, Inc. Novel substituted pyridinyloxy and pyrimidinyloxy amides useful as inhibitors of protein kinases
US20100216734A1 (en) 2006-03-08 2010-08-26 Braincells, Inc. Modulation of neurogenesis by nootropic agents
WO2007111275A1 (ja) * 2006-03-24 2007-10-04 The University Of Tokyo シグナル伝達阻害方法、それに用いるシグナル伝達阻害剤およびその用途
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
AR060635A1 (es) * 2006-04-27 2008-07-02 Banyu Pharma Co Ltd Derivados de 1,2-dihidro-3h-pirazolo[3,4-d]pirimidin-3-ona, composiciones farmaceuticas que los comprenden y su uso en el tratamiento del cancer
WO2007134077A2 (en) 2006-05-09 2007-11-22 Braincells, Inc. 5 ht receptor mediated neurogenesis
AU2007249399A1 (en) 2006-05-09 2007-11-22 Braincells, Inc. Neurogenesis by modulating angiotensin
EP2068872A1 (en) 2006-09-08 2009-06-17 Braincells, Inc. Combinations containing a 4-acylaminopyridine derivative
US20100184806A1 (en) 2006-09-19 2010-07-22 Braincells, Inc. Modulation of neurogenesis by ppar agents
WO2008041118A2 (en) 2006-10-04 2008-04-10 Pfizer Products Inc. Pyrido[4,3-d]pyrimidin-4(3h)-one derivatives as calcium receptor antagonists
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
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.
EP3070090B1 (en) 2007-06-13 2018-12-12 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
WO2009064835A1 (en) 2007-11-16 2009-05-22 Incyte Corporation 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
US8158616B2 (en) 2008-03-11 2012-04-17 Incyte Corporation Azetidine and cyclobutane derivatives as JAK inhibitors
WO2009132202A2 (en) 2008-04-24 2009-10-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
US8765727B2 (en) 2009-01-23 2014-07-01 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
WO2010099217A1 (en) 2009-02-25 2010-09-02 Braincells, Inc. Modulation of neurogenesis using d-cycloserine combinations
JP2012524063A (ja) 2009-04-15 2012-10-11 アストラゼネカ・アクチエボラーグ アルツハイマー病などのグリコーゲンシンターゼキナーゼ３関連障害の治療に有用なイミダゾール置換ピリミジン
JP5775070B2 (ja) 2009-05-22 2015-09-09 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ ヤヌスキナーゼ阻害剤としてのピラゾール−４−イル−ピロロ［２，３−ｄ］ピリミジンおよびピロール−３−イル−ピロロ［２，３−ｄ］ピリミジンのＮ−（ヘテロ）アリール−ピロリジン誘導体
SG176111A1 (en) 2009-05-22 2011-12-29 Incyte Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
KR101921850B1 (ko) 2009-10-09 2018-11-23 인사이트 홀딩스 코포레이션 3-（4-（7Ｈ-피롤로〔2,3-ｄ〕피리미딘-4-일）-1Ｈ-피라졸-1-일）-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체
PT3354652T (pt) 2010-03-10 2020-07-20 Incyte Holdings Corp Derivados de piperidin-4-ilazetidina como inibidores de jak1
RS54824B1 (sr) 2010-05-21 2016-10-31 Incyte Holdings Corp Topikalna formulacija za inhibiciju jak-a
DK2597084T3 (en) 2010-07-08 2016-08-15 Kaken Pharma Co Ltd N-HYDROXYFORMAMIDE DERIVATIVE AND MEDICINAL CONTAINING SAME
WO2012068440A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
CA2827673C (en) 2011-02-18 2020-10-27 Novartis Pharma Ag Mtor/jak inhibitor combination therapy
EP2681193B1 (en) 2011-03-02 2016-01-06 Lead Discovery Center GmbH Pharmaceutically active disubstituted pyridine derivatives
CN103476759B (zh) 2011-04-19 2016-03-16 拜耳知识产权有限责任公司 取代的4-芳基-n-苯基-1,3,5-三嗪-2-胺
TW201636330A (zh) 2011-05-24 2016-10-16 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
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
EP2741747A1 (en) 2011-08-10 2014-06-18 Novartis Pharma AG JAK P13K/mTOR COMBINATION THERAPY
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
WO2013037896A1 (en) 2011-09-16 2013-03-21 Bayer Intellectual Property Gmbh Disubstituted 5-fluoro-pyrimidines
EP2755948B1 (en) 2011-09-16 2016-05-25 Bayer Intellectual Property GmbH Disubstituted 5-fluoro pyrimidine derivatives containing a sulfoximine group
JP6378171B2 (ja) 2012-04-24 2018-08-22 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ｄｎａ−ｐｋ阻害剤
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
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
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
CN113384546A (zh) 2012-11-15 2021-09-14 因赛特公司 鲁索利替尼的缓释剂型
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
WO2014138168A1 (en) 2013-03-06 2014-09-12 Incyte Corporation Processes and intermediates for making a jak inhibitor
SI3527563T1 (sl) 2013-03-12 2022-01-31 Vertex Pharmaceuticals Incorporated Inhibitorji DNA-PK
WO2014154723A1 (en) * 2013-03-29 2014-10-02 F. Hoffmann-La Roche Ag Novel pyrrole derivatives for the treatment of cancer
SG10201801069QA (en) 2013-08-07 2018-03-28 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
RU2675270C2 (ru) 2013-10-17 2018-12-18 Вертекс Фармасьютикалз Инкорпорейтед Сокристаллы и содержащие их фармацевтические композиции
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
WO2016059011A1 (en) 2014-10-16 2016-04-21 Bayer Pharma Aktiengesellschaft Fluorinated benzofuranyl-pyrimidine derivatives containing a sulfone group
EP3273963A1 (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 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
CN107428707A (zh) 2015-03-24 2017-12-01 拜耳制药股份公司 4‑(4‑氟‑2‑甲氧基苯基)‑n‑{3‑[(s‑甲基亚磺酰亚胺基)甲基]苯基}‑1,3,5‑三嗪‑2‑胺用于治疗多发性骨髓瘤的用途
US10717749B2 (en) 2015-09-29 2020-07-21 Bayer Pharma Aktiengesellschaft 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
CN107513067A (zh) 2016-06-16 2017-12-26 北京赛林泰医药技术有限公司 含有取代环戊基的吡咯并嘧啶化合物
RU2758669C2 (ru) 2016-09-27 2021-11-01 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с применением сочетания днк-поражающих агентов и ингибиторов днк-пк
CA3057891A1 (en) 2017-03-28 2018-10-04 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
EP3601253B1 (en) 2017-03-28 2021-09-15 Bayer Aktiengesellschaft Novel ptefb inhibiting macrocyclic compounds
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
EA202091830A1 (ru) 2018-01-30 2020-12-29 Инсайт Корпорейшн Способы и промежуточные соединения для получения ингибитора jak
MA51820A (fr) 2018-02-13 2021-05-19 Bayer Ag Utilisation de 5-fluoro-4-(4-fluoro-2-méthoxyphényl)-n-(4-[(s-méthylsulfonimidoyl)méthyl]pyridin-2-yl)pyridin-2-amine pour traiter un lymphome diffus à grandes cellules b
MD3773593T2 (ro) 2018-03-30 2024-10-31 Incyte Corp Tratament hidradenitei supurative utilizând inhibitori ai JAK
US12213970B2 (en) 2018-10-29 2025-02-04 Boehringer Ingelheim International Gmbh Pyridinyl sulfonamide derivatives, pharmaceutical compositions and uses thereof
CN115038443A (zh) 2019-11-22 2022-09-09 因西特公司 包含alk2抑制剂和jak2抑制剂的组合疗法
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN113288899B (zh) * 2021-05-17 2022-10-11 浙江工业大学 一种杂环硫醇类化合物在制备抗肿瘤药物中的应用
WO2026024674A1 (en) 2024-07-22 2026-01-29 Genesis Therapeutics, Inc. Methods of treating skp2-associated cancers

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002064586A2 (en) * 2001-02-09 2002-08-22 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of erk2 and uses thereof
WO2003016275A1 (fr) * 2001-08-10 2003-02-27 Shionogi & Co., Ltd. Agent antiviral
WO2003093290A2 (en) * 2002-05-06 2003-11-13 Genelabs Technologies, Inc. Nucleoside derivatives for treating hepatitis c virus infection

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002064586A2 (en) * 2001-02-09 2002-08-22 Vertex Pharmaceuticals Incorporated Heterocyclic inhibitors of erk2 and uses thereof
WO2003016275A1 (fr) * 2001-08-10 2003-02-27 Shionogi & Co., Ltd. Agent antiviral
WO2003093290A2 (en) * 2002-05-06 2003-11-13 Genelabs Technologies, Inc. Nucleoside derivatives for treating hepatitis c virus infection

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012508223A (ja) * 2008-11-10 2012-04-05 ユニバーシティ オブ バーゼル トリアジン、ピリミジン、及びピリジン類似体、並びに、治療薬及び診断プローブとしてのそれらの使用
JP2014510068A (ja) * 2011-03-02 2014-04-24 リード ディスカバリー センター ゲーエムベーハー 薬学的活性化二置換トリアジン誘導体
JP2015530980A (ja) * 2012-08-02 2015-10-29 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤として活性な置換ピロール類

Also Published As

Publication number Publication date
US7407962B2 (en) 2008-08-05
CA2515132A1 (en) 2004-08-26
AU2004212421A1 (en) 2004-08-26
US20040214928A1 (en) 2004-10-28
WO2004072063A1 (en) 2004-08-26
EP1611125A1 (en) 2006-01-04
AU2004212421B2 (en) 2009-08-20
CA2515132C (en) 2012-01-03

Similar Documents

Publication Publication Date Title
JP2006518381A (ja) プロテインキナーゼのインヒビターとして有用なヘテロアリール置換ピロール
US7244735B2 (en) Heterocyclic protein kinase inhibitors and uses thereof
JP4173738B2 (ja) Ｅｒｋ２の複素環式インヒビターおよびその使用
US7345054B2 (en) Heterocyclic inhibitors of ERK2 and uses thereof
JP4889489B2 (ja) プロテインキナーゼのインヒビターとして有用なアミノトリアゾール化合物
EP1392684B1 (en) Thiazole compounds useful as inhibitors of protein kinases
JP4808154B2 (ja) プロテインキナーゼインヒビターとして有用な組成物
US20030225073A1 (en) Compositions useful as inhibitors of protein kinases
US8653088B2 (en) Compositions useful as inhibitors of protein kinases
JP2004529140A (ja) Ｃ−ｊｕｎｎ末端キナーゼ（ｊｎｋ）および他のタンパク質キナーゼのインヒビター
EP1423380A1 (en) Pyrazole-derived kinase inhibitors and uses thereof
AU2002255521A1 (en) Heterocyclic inhibitors of ERK2 and uses thereof
MXPA01010100A (en) Pyrazole compositions useful as inhibitors of erk
HK1109567A (en) Triazoles useful as inhibitors of protein kinases
AU2006202623A1 (en) Heterocyclic Inhibitors of Erk2 and Uses Thereof

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20070201

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20070201

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20100617

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20101112