CA2792278C - 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses - Google Patents

2,4-pyrimidinediamine compounds and prodrugs thereof and their uses Download PDF

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Publication number
CA2792278C
CA2792278C CA2792278A CA2792278A CA2792278C CA 2792278 C CA2792278 C CA 2792278C CA 2792278 A CA2792278 A CA 2792278A CA 2792278 A CA2792278 A CA 2792278A CA 2792278 C CA2792278 C CA 2792278C
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CA
Canada
Prior art keywords
alkyl
fluoro
oxo
pyrimidinediamine
dihydro
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.)
Active
Application number
CA2792278A
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English (en)
French (fr)
Other versions
CA2792278A1 (en
Inventor
Jiaxin Yu
Jeffrey Clough
Rajinder Singh
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.)
Rigel Pharmaceuticals Inc
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Rigel Pharmaceuticals Inc
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Publication date
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Publication of CA2792278A1 publication Critical patent/CA2792278A1/en
Application granted granted Critical
Publication of CA2792278C publication Critical patent/CA2792278C/en
Active legal-status Critical Current
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • 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
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P37/08—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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA2792278A 2010-04-13 2011-04-13 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses Active CA2792278C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US32369910P 2010-04-13 2010-04-13
US61/323,699 2010-04-13
PCT/US2011/032291 WO2011130390A1 (en) 2010-04-13 2011-04-13 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses

Publications (2)

Publication Number Publication Date
CA2792278A1 CA2792278A1 (en) 2011-10-20
CA2792278C true CA2792278C (en) 2019-05-14

Family

ID=44583348

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2792278A Active CA2792278C (en) 2010-04-13 2011-04-13 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses

Country Status (6)

Country Link
US (1) US8618095B2 (https=)
EP (1) EP2558474B1 (https=)
JP (2) JP6067550B2 (https=)
CA (1) CA2792278C (https=)
ES (1) ES2562419T3 (https=)
WO (1) WO2011130390A1 (https=)

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US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
HRP20190186T4 (hr) 2011-07-28 2024-12-20 Rigel Pharmaceuticals, Inc. Nove formulacije (trimetoksifenilamino)pirimidinila
US9676870B2 (en) * 2011-08-04 2017-06-13 The Brigham And Women's Hospital, Inc. Methods of treating atherosclerosis and aneurysm
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
CN103958526B (zh) * 2012-06-20 2015-09-09 上海恒瑞医药有限公司 嘧啶二胺类衍生物、其制备方法及其在医药上的应用
CN102746337B (zh) * 2012-06-21 2014-12-17 成都苑东药业有限公司 一种2，4-嘧啶二胺类化合物及其制备方法
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
BR112015002493A8 (pt) * 2012-08-30 2019-07-30 Hoffmann La Roche composto, composição farmacêutica, processo para a preparação de uma composição farmacêutica, kit e uso de um composto”
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
EP2970138B1 (en) 2013-03-13 2019-01-16 Canadian Blood Services Pyrazole derivatives and their uses thereof
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
JP7118642B2 (ja) * 2014-08-08 2022-08-16 アリ リサーチ ソシエタ ア レスポンサビリタ リミタータ センプリフィカタ 炎症性およびアレルギー性病変の治療に用いるための脂肪酸とパルミトイルエタノールアミドの混合物
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
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
HRP20241288T1 (hr) 2018-05-04 2024-12-06 Incyte Corporation Čvrsti oblici fgfr inhibitora i postupci za njihovu proizvodnju
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
US11628162B2 (en) 2019-03-08 2023-04-18 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
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Ｆｇｆｒ阻害剤の誘導体
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN116670127A (zh) * 2021-03-30 2023-08-29 贝达药业股份有限公司 Egfr抑制剂及其组合物和用途
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
WO2022236255A2 (en) * 2021-05-03 2022-11-10 Nuvation Bio Inc. Heterocyclic compounds as kinase inhibitors
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11939331B2 (en) 2021-06-09 2024-03-26 Incyte Corporation Tricyclic heterocycles as FGFR inhibitors
JP2026505741A (ja) * 2023-01-19 2026-02-18 ハンジョウ イノゲート ファーマ カンパニー リミテッド キナーゼ阻害剤としての縮合三環式化合物
CN119431398A (zh) * 2023-07-31 2025-02-14 中国科学院上海有机化学研究所 R406及其衍生物协同trail的抗肿瘤应用

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US6573256B2 (en) 1996-12-30 2003-06-03 Bone Care International, Inc. Method of inhibiting angiogenesis using active vitamin D analogues
FR2785284B1 (fr) 1998-11-02 2000-12-01 Galderma Res & Dev Analogues de la vitamine d
US6358939B1 (en) 1999-12-21 2002-03-19 Northern Lights Pharmaceuticals, Llc Use of biologically active vitamin D compounds for the prevention and treatment of inflammatory bowel disease
US6924400B2 (en) 2001-12-10 2005-08-02 Galderma Research & Development, Snc Triaromatic vitamin D analogues
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
HRP20050089B1 (hr) 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
EP1635773A2 (en) 2003-06-06 2006-03-22 Merck & Co., Inc. (a New Jersey corp.) Combination therapy for the treatment of hypertension
WO2005012294A1 (en) 2003-07-30 2005-02-10 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
ATE506953T1 (de) 2003-08-07 2011-05-15 Rigel Pharmaceuticals Inc 2,4-pyrimidindiamin-verbindungen und verwendungen als antiproliferative mittel
US20070092888A1 (en) 2003-09-23 2007-04-26 Cornelius Diamond Diagnostic markers of hypertension and methods of use thereof
SI1814878T1 (sl) * 2004-11-24 2012-06-29 Rigel Pharmaceuticals Inc Spojine spiro-2,4-pirimidindiamina in njihova uporaba
AU2006206458B2 (en) 2005-01-19 2012-10-25 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
US8227455B2 (en) 2005-04-18 2012-07-24 Rigel Pharmaceuticals, Inc. Methods of treating cell proliferative disorders
US7713987B2 (en) 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
ATE540041T1 (de) 2006-11-21 2012-01-15 Rigel Pharmaceuticals Inc Prodrug-salze von 2,4-pyrimidindiaminverbindungen und anwendungen davon
US7834024B2 (en) * 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
WO2009003136A1 (en) 2007-06-26 2008-12-31 Rigel Pharmaceuticals, Inc. Substituted pyrimidine-2, 4 -diamines for treating cell proliferative disorders
NZ603525A (en) * 2008-06-27 2015-02-27 Celgene Avilomics Res Inc Pyrimidine based compound and uses thereof
ES2542884T3 (es) * 2008-09-23 2015-08-12 Rigel Pharmaceuticals, Inc. Inhibidores de JAK de carbamato tricíclico
JP5815411B2 (ja) * 2008-12-30 2015-11-17 ライジェル ファーマシューティカルズ， インコーポレイテッド ピリミジンジアミンキナーゼ阻害剤
JP5681723B2 (ja) * 2009-11-20 2015-03-11 ライジェル ファーマシューティカルズ， インコーポレイテッド ２，４−ピリミジンジアミン化合物およびそのプロドラッグならびにそれらの使用
CA2792278C (en) * 2010-04-13 2019-05-14 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses

Also Published As

Publication number Publication date
JP6067550B2 (ja) 2017-01-25
EP2558474A1 (en) 2013-02-20
EP2558474B1 (en) 2015-11-25
JP2013523891A (ja) 2013-06-17
US20110251177A1 (en) 2011-10-13
JP2016041700A (ja) 2016-03-31
CA2792278A1 (en) 2011-10-20
ES2562419T3 (es) 2016-03-04
WO2011130390A1 (en) 2011-10-20
US8618095B2 (en) 2013-12-31

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