ATE371656T1 - Heteroaryl-pyrimidinderivate als jak-inhibitoren - Google Patents

Heteroaryl-pyrimidinderivate als jak-inhibitoren

Info

Publication number
ATE371656T1
ATE371656T1 AT03786582T AT03786582T ATE371656T1 AT E371656 T1 ATE371656 T1 AT E371656T1 AT 03786582 T AT03786582 T AT 03786582T AT 03786582 T AT03786582 T AT 03786582T AT E371656 T1 ATE371656 T1 AT E371656T1
Authority
AT
Austria
Prior art keywords
heteroaryl
pyrimidine derivatives
jak inhibitors
pharmaceutically acceptable
provides
Prior art date
Application number
AT03786582T
Other languages
English (en)
Inventor
Randy Bethiel
Mark Ledeboer
Original Assignee
Vertex Pharma
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 Pharma filed Critical Vertex Pharma
Application granted granted Critical
Publication of ATE371656T1 publication Critical patent/ATE371656T1/de

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    • 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
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Tropical Medicine & Parasitology (AREA)
AT03786582T 2002-11-04 2003-11-04 Heteroaryl-pyrimidinderivate als jak-inhibitoren ATE371656T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US42357902P 2002-11-04 2002-11-04

Publications (1)

Publication Number Publication Date
ATE371656T1 true ATE371656T1 (de) 2007-09-15

Family

ID=32312681

Family Applications (1)

Application Number Title Priority Date Filing Date
AT03786582T ATE371656T1 (de) 2002-11-04 2003-11-04 Heteroaryl-pyrimidinderivate als jak-inhibitoren

Country Status (9)

Country Link
US (1) US7259161B2 (de)
EP (1) EP1562938B1 (de)
JP (2) JP4688498B2 (de)
AT (1) ATE371656T1 (de)
AU (1) AU2003295396B2 (de)
CA (1) CA2506773A1 (de)
DE (1) DE60316013T2 (de)
ES (1) ES2289349T3 (de)
WO (1) WO2004041814A1 (de)

Families Citing this family (86)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1317450B1 (de) * 2000-09-15 2006-11-22 Vertex Pharmaceuticals Incorporated Pyrazolverbindungen als protein-kinasehemmer
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
ES2445208T3 (es) 2002-07-29 2014-02-28 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para uso en métodos para tratar o prevenir enfermedades autoinmunitarias
BRPI0413018B8 (pt) * 2003-07-30 2021-05-25 Rigel Pharmaceuticals Inc composto, e, uso de um composto
RU2007107177A (ru) * 2004-07-28 2008-09-10 Айрм Ллк (Bm) Соединения и композиции, как модуляторы ядерных рецепторов стероидных гормонов
WO2006047492A2 (en) 2004-10-22 2006-05-04 Amgen Inc. Substituted nitrogen-containing heterocycles as vanilloid receptor ligands and their uses as medicament
EP1814878B1 (de) * 2004-11-24 2012-01-04 Rigel Pharmaceuticals, Inc. Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen
KR101484499B1 (ko) 2005-02-14 2015-01-20 존슨 앤드 존슨 비젼 케어, 인코포레이티드 안과용 렌즈의 제조방법, 안과용 장치 및 콘택트 렌즈
EP1883302A4 (de) * 2005-05-03 2009-05-20 Rigel Pharmaceuticals Inc Jak-kinase-hemmer und deren verwendung
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2006133426A2 (en) 2005-06-08 2006-12-14 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
US8133900B2 (en) 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
CN103626742B (zh) 2005-11-01 2017-04-26 塔格根公司 激酶的联-芳基间-嘧啶抑制剂
US8518964B2 (en) * 2005-11-22 2013-08-27 Merck Sharp & Dohme Corp. Tricyclic compounds useful as inhibitors of kinases
EP2455382B1 (de) 2005-12-13 2016-10-26 Incyte Holdings Corporation Heteroarylsubstituierte Pyrrolo[2,3-b]pyridine sowie Pyrrolo[2,3-b]pyrimidine als Januskinaseinhibitoren
KR20080110998A (ko) * 2006-01-30 2008-12-22 엑셀리시스, 인코포레이티드 Ｊａｋ­２ 조절자로서 ４­아릴­２­아미노­피리미딘 또는 4­아릴­２­아미노알킬­피리미딘 및 이들을 포함하는 약제학적 조성물
US9052529B2 (en) 2006-02-10 2015-06-09 Johnson & Johnson Vision Care, Inc. Comfortable ophthalmic device and methods of its production
CA2642229C (en) 2006-02-24 2015-05-12 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
CA2650140A1 (en) 2006-04-14 2007-10-25 Mriganka Sur Identifying and modulating molecular pathways that mediate nervous system plasticity
EP2089369B1 (de) 2006-10-19 2011-02-02 Rigel Pharmaceuticals, Inc. 2,4-pyridimediamon-derivate als hemmer von jak-kinasen zur behandlung von autoimmunerkrankungen
EP2121692B1 (de) 2006-12-22 2013-04-10 Incyte Corporation Substituierte heterozyklen als inhibitoren von janus-kinase
HRP20151386T1 (hr) 2007-03-12 2016-02-26 Ym Biosciences Australia Pty Ltd Fenil aminopirimidinski spojevi i njihova primjena
JP5676249B2 (ja) 2007-04-20 2015-02-25 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのアミノピリジン誘導体
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 (de) 2007-06-13 2018-12-12 Incyte Holdings Corporation Verwendung der salze des janus-kinasehemmers (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropannitril
US20090048282A1 (en) * 2007-08-14 2009-02-19 Wyeth Pyrimidine sulfonamide analogs and their use as agonists of the wnt-beta-catenin cellular messaging system
US8530480B2 (en) * 2007-09-04 2013-09-10 The Scripps Research Institute Substituted pyrimidinyl-amines as protein kinase inhibitors
US8309566B2 (en) 2008-02-15 2012-11-13 Rigel Pharmaceuticals, Inc. Pyrimidine-2-amine compounds and their use as inhibitors of JAK kinases
US8158616B2 (en) 2008-03-11 2012-04-17 Incyte Corporation Azetidine and cyclobutane derivatives as JAK inhibitors
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
MX2010011463A (es) 2008-04-16 2011-06-03 Portola Pharm Inc 2,6-diamino-pirimidin-5-il-carboxamidas como inhibidores de syk o jak quinasas.
NZ588830A (en) 2008-04-22 2012-11-30 Portola Pharm Inc Inhibitors of protein kinases
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
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
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
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
US9133123B2 (en) 2010-04-23 2015-09-15 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
RS54824B1 (sr) 2010-05-21 2016-10-31 Incyte Holdings Corp Topikalna formulacija za inhibiciju jak-a
US9102625B2 (en) 2010-11-01 2015-08-11 Portola Pharmaceuticals, Inc. Nicotinamides as JAK kinase modulators
CA2816957A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
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
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
EP2741747A1 (de) 2011-08-10 2014-06-18 Novartis Pharma AG Jak-/p13k-mtor-kombinationstherapie
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
EP2763976B1 (de) 2011-10-05 2016-05-18 Merck Sharp & Dohme Corp. 2-pyridyl-carboxamid-haltige milztyrosinkinase-hemmer
WO2013052391A1 (en) * 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. PHENYL CARBOXAMIDE-CONTAINING SPLEEN TYROSINE KINASE (Syk) INHIBITORS
CA3094793A1 (en) 2011-11-23 2013-05-30 Portola Pharmaceuticals, Inc. Pyrazine kinase inhibitors
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
US8809359B2 (en) 2012-06-29 2014-08-19 Ym Biosciences Australia Pty Ltd Phenyl amino pyrimidine bicyclic compounds and uses thereof
WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
US9676756B2 (en) 2012-10-08 2017-06-13 Portola Pharmaceuticals, Inc. Substituted pyrimidinyl kinase inhibitors
CN113384546A (zh) 2012-11-15 2021-09-14 因赛特公司 鲁索利替尼的缓释剂型
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
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
TWI729644B (zh) 2014-06-12 2021-06-01 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
TWI704151B (zh) * 2014-12-22 2020-09-11 美商美國禮來大藥廠 Ｅｒｋ抑制劑
GB201509893D0 (en) * 2015-06-08 2015-07-22 Ucb Biopharma Sprl Therapeutic agents
WO2018041989A1 (en) 2016-09-02 2018-03-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosing and treating refractory celiac disease type 2
RU2758669C2 (ru) 2016-09-27 2021-11-01 Вертекс Фармасьютикалз Инкорпорейтед Способ лечения рака с применением сочетания днк-поражающих агентов и ингибиторов днк-пк
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
WO2019161224A1 (en) * 2018-02-15 2019-08-22 GiraFpharma LLC Heterocyclic compounds as kinase inhibitors
MD3773593T2 (ro) 2018-03-30 2024-10-31 Incyte Corp Tratament hidradenitei supurative utilizând inhibitori ai JAK
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
JP2022527972A (ja) 2019-04-02 2022-06-07 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル 前悪性病変を有する患者において癌を予測及び予防する方法
US20220202820A1 (en) 2019-04-16 2022-06-30 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
US20220281859A1 (en) * 2019-08-14 2022-09-08 Nuvation Bio Inc. Heterocyclic compounds as kinase inhibitors
EP4013743A1 (de) * 2019-08-14 2022-06-22 Nuvation Bio Inc. Heterocyclische verbindungen als kinasehemmer
EP4054579A1 (de) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Verfahren zur behandlung von krebsarten, die resistenz gegen kinase-inhibitoren erworben haben
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN115677611B (zh) * 2021-07-22 2024-07-09 成都硕德药业有限公司 2H-苯并[b][1,4]恶嗪-3(4H）-酮衍生物
CN116947846B (zh) * 2022-04-15 2026-02-27 成都硕德药业有限公司 一种并环衍生物及其制备方法和用途
EP4526469A1 (de) 2022-05-16 2025-03-26 Institut National de la Santé et de la Recherche Médicale Verfahren zur beurteilung der erschöpfung von hämatopoetischen stammzellen durch chronische entzündung
CN117645604A (zh) * 2022-09-05 2024-03-05 浙江同源康医药股份有限公司 用作cdk4激酶抑制剂的化合物及其应用

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
JP4064671B2 (ja) * 2000-02-25 2008-03-19 エフ．ホフマン−ラ ロシュ アーゲー アデノシン受容体モジュレーター
AU2001295026B2 (en) * 2000-09-06 2008-04-03 Novartis Vaccines And Diagnostics, Inc. Inhibitors of glycogen synthase kinase 3
EP1373257B9 (de) * 2001-03-29 2008-10-15 Vertex Pharmaceuticals Incorporated Hemmer von c-jun-terminal kinase (jnk) und andere protein kinase
WO2002083668A1 (en) 2001-04-10 2002-10-24 Vertex Pharmaceuticals Incorporated Isoxaxole derivatives as inhibitors of src and other protein kinases
US6825190B2 (en) 2001-06-15 2004-11-30 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors and uses thereof

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