JP2004528295A - キナーゼ阻害方法 - Google Patents

キナーゼ阻害方法 Download PDF

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Publication number
JP2004528295A
JP2004528295A JP2002560683A JP2002560683A JP2004528295A JP 2004528295 A JP2004528295 A JP 2004528295A JP 2002560683 A JP2002560683 A JP 2002560683A JP 2002560683 A JP2002560683 A JP 2002560683A JP 2004528295 A JP2004528295 A JP 2004528295A
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Prior art keywords
heterocycle
alkyl
halo
amino
arylamide
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JP2002560683A
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Japanese (ja)
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JP2004528295A5 (enExample
Inventor
バーンズ,クリストファー,ジョン
ウイルクス,アンドリュー,フレデリック
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サイトピア ピーティワイ リミテッド
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Priority claimed from AUPR2793A external-priority patent/AUPR279301A0/en
Priority claimed from AUPR2792A external-priority patent/AUPR279201A0/en
Application filed by サイトピア ピーティワイ リミテッド filed Critical サイトピア ピーティワイ リミテッド
Publication of JP2004528295A publication Critical patent/JP2004528295A/ja
Publication of JP2004528295A5 publication Critical patent/JP2004528295A5/ja
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
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    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
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    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
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    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/495Heterocyclic 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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JP2002560683A 2001-01-30 2002-01-30 キナーゼ阻害方法 Pending JP2004528295A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
AUPR2793A AUPR279301A0 (en) 2001-01-30 2001-01-30 Method of inhibiting jak
AUPR2792A AUPR279201A0 (en) 2001-01-30 2001-01-30 Jak inhibitors
PCT/AU2002/000089 WO2002060492A1 (en) 2001-01-30 2002-01-30 Methods of inhibiting kinases

Publications (2)

Publication Number Publication Date
JP2004528295A true JP2004528295A (ja) 2004-09-16
JP2004528295A5 JP2004528295A5 (enExample) 2005-12-22

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JP2002560683A Pending JP2004528295A (ja) 2001-01-30 2002-01-30 キナーゼ阻害方法

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US (2) US20040102455A1 (enExample)
EP (1) EP1363702A4 (enExample)
JP (1) JP2004528295A (enExample)
CA (1) CA2436487A1 (enExample)
WO (1) WO2002060492A1 (enExample)

Cited By (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006514685A (ja) * 2002-12-11 2006-05-11 サイトピア・リサーチ・ピーティーワイ・リミテッド ピラジン系チューブリン阻害剤
JP2009515888A (ja) * 2005-11-10 2009-04-16 シェーリング コーポレイション プロテインキナーゼインヒビターとしてのイミダゾピラジン
JP2010501003A (ja) * 2006-08-16 2010-01-14 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 ピラジン化合物、その使用及び調製方法
JP2010532772A (ja) * 2007-07-11 2010-10-14 バイエル・シェーリング・ファルマ・アクチェンゲゼルシャフト イミダゾ−、ピラゾロピラジン類およびイミダゾトリアジン類およびそれらの使用
KR20100116599A (ko) * 2008-02-01 2010-11-01 어키니언 파마슈티칼스 아베 피라진 유도체 및 단백질 키나아제 억제제로서의 이의 용도
JP2012510997A (ja) * 2008-12-08 2012-05-17 ギリアード コネチカット, インコーポレイテッド イミダゾピラジンSyk阻害剤
JP2012510998A (ja) * 2008-12-08 2012-05-17 ギリアード コネチカット, インコーポレイテッド イミダゾピラジンsyk阻害剤
JP2012524053A (ja) * 2009-04-16 2012-10-11 セントロ ナシオナル デ インベスティガシオネス オンコロヒカス(セエネイオ) キナーゼ阻害剤として使用するためのイミダゾピラジン類
JP2014074057A (ja) * 2007-06-08 2014-04-24 Abbvie Inc キナーゼ阻害薬としての5−ヘテロアリール置換インダゾール類
JP2014520767A (ja) * 2011-07-07 2014-08-25 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 がんの処置のための置換されたアザ複素環
US9382256B2 (en) 2013-07-30 2016-07-05 Gilead Connecticut, Inc. Formulation of Syk inhibitors
US9562056B2 (en) 2010-03-11 2017-02-07 Gilead Connecticut, Inc. Imidazopyridines Syk inhibitors
US9657023B2 (en) 2013-07-30 2017-05-23 Gilead Connecticut, Inc. Polymorph of Syk inhibitors
US9687492B2 (en) 2013-12-04 2017-06-27 Gilead Sciences, Inc. Methods for treating cancers
US9707236B2 (en) 2014-07-14 2017-07-18 Gilead Sciences, Inc. Combination methods for treating cancers
US9968601B2 (en) 2013-12-23 2018-05-15 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
US11339168B2 (en) 2019-02-22 2022-05-24 Kronos Bio, Inc. Crystalline forms of 6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine as Syk inhibitors

Families Citing this family (122)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2002364889A1 (en) * 2001-09-24 2003-06-10 University Of Aarhus Methods for diagnosis and treatment of diseases associated with altered expression of nrf2
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
IL164703A0 (en) 2002-04-19 2005-12-18 Cellular Genomics Inc ImidazoÄ1,2-AÜpyrazin-8-ylamines method of making and method of use thereof
US7122550B2 (en) 2002-05-23 2006-10-17 Cytopia Pty Ltd Protein kinase inhibitors
CA2486187C (en) 2002-05-23 2013-02-19 Cytopia Pty Ltd. Kinase inhibitors
US7015227B2 (en) 2002-06-21 2006-03-21 Cgi Pharmaceuticals, Inc. Certain amino-substituted monocycles as kinase modulators
GB0215775D0 (en) * 2002-07-06 2002-08-14 Astex Technology Ltd Pharmaceutical compounds
CN103169708B (zh) 2002-07-29 2018-02-02 里格尔药品股份有限公司 用2,4‑嘧啶二胺化合物治疗或者预防自体免疫性疾病的方法
MXPA05002572A (es) 2002-09-04 2005-09-08 Schering Corp Compuestos pirazolo[1,5-a]pirimidinas como inhibidores de cinasa depentes de ciclina.
US7205308B2 (en) 2002-09-04 2007-04-17 Schering Corporation Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
AU2003270489A1 (en) 2002-09-09 2004-03-29 Cellular Genomics, Inc. 6-ARYL-IMIDAZO(1,2-a)PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
JP2006503838A (ja) 2002-09-23 2006-02-02 シェーリング コーポレイション サイクリン依存性キナーゼインヒビターとしての新規イミダゾピラジン
ATE377600T1 (de) * 2002-09-23 2007-11-15 Schering Corp Imidazopyrazine als cdk-inhibitoren
EP1554271A1 (en) * 2002-10-15 2005-07-20 Rigel Pharmaceuticals, Inc. Substituted indoles and their use as hcv inhibitors
US7160885B2 (en) 2003-02-10 2007-01-09 Cgi Pharmaceuticals, Inc. Certain 6, 8-(heteroaryl or aryl) disubstituted imidazo[1,2-a]pyrazines as modulators of Hsp90 complex activity
AR043002A1 (es) * 2003-02-18 2005-07-13 Altana Pharma Ag Imidazopirazinas 6-substituidos
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
EP1608373A4 (en) 2003-03-19 2010-09-29 Exelixis Inc TIE-2 MODULATORS AND USE METHOD
WO2004084813A2 (en) 2003-03-21 2004-10-07 Smithkline Beecham Corporation Chemical compounds
CA2520323C (en) * 2003-04-09 2013-07-09 Exelixis, Inc. Tie-2 modulators and methods of use
WO2005014599A1 (en) * 2003-06-04 2005-02-17 Cellular Genomics, Inc. Imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of bruton’s tyrosine kinase by such compounds
US7393848B2 (en) 2003-06-30 2008-07-01 Cgi Pharmaceuticals, Inc. Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds
US7122542B2 (en) 2003-07-30 2006-10-17 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
US7259164B2 (en) 2003-08-11 2007-08-21 Cgi Pharmaceuticals, Inc. Certain substituted imidazo[1,2-a]pyrazines, as modulators of kinase activity
MXPA06003615A (es) * 2003-09-30 2006-06-05 Amgen Inc Ligandos del receptor vanilloide y su uso en tratamientos.
KR100872204B1 (ko) * 2003-10-15 2008-12-09 오에스아이 파마슈티컬스, 인코포레이티드 이미다조피라진 티로신 키나제 억제제
US20050288295A1 (en) * 2003-11-11 2005-12-29 Currie Kevin S Certain imidazo[1,2-a]pyrazin-8-ylamines, method of making, and method of use thereof
JP4808628B2 (ja) * 2003-12-03 2011-11-02 ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド アゾール系キナーゼ阻害剤
ATE497949T1 (de) * 2003-12-03 2011-02-15 Ym Biosciences Australia Pty Tubulininhibitoren
WO2005058876A1 (en) * 2003-12-16 2005-06-30 Gpc Biotech Ag Pyrazine derivatives as effective compounds against infectious diseases
WO2005085252A1 (en) * 2004-03-04 2005-09-15 Biofocus Discovery Limited Imidazo ‘1,2-a’ pyrazine compounds which interact with protein kinases
DE602005014964D1 (de) 2004-04-02 2009-07-30 Osi Pharm Inc Mit einem 6,6-bicyclischen ring substituierte heterobicyclische proteinkinaseinhibitoren
ATE458730T1 (de) 2004-04-13 2010-03-15 Icagen Inc Polycyclische pyrazine als kaliumionenkanal- modulatoren
CA2586334A1 (en) * 2004-11-16 2006-06-08 Neurochem (International) Limited Compounds for the treatment of cns and amyloid associated diseases
KR20070085433A (ko) * 2004-11-24 2007-08-27 노파르티스 아게 Jak 저해제들과 bcr-abl, flt-3, fak 또는raf 키나제 저해제들 중 하나 이상의 조합물
GB0428082D0 (en) * 2004-12-22 2005-01-26 Welcome Trust The Ltd Therapeutic 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.
WO2007024294A2 (en) 2005-05-03 2007-03-01 Cgi Pharmaceuticals, Inc. Certain substituted ureas, as modulators of kinase activity
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
RU2485106C2 (ru) 2005-06-08 2013-06-20 Райджел Фамэсьютикэлз, Инк. Соединения, проявляющие активность в отношении jak-киназы (варианты), способ лечения заболеваний, опосредованных jak-киназой, способ ингибирования активности jak-киназы (варианты), фармацевтическая композиция на основе указанных соединений
JP2009507032A (ja) 2005-09-02 2009-02-19 アボット・ラボラトリーズ 新規なイミダゾ系複素環
US20070149506A1 (en) 2005-09-22 2007-06-28 Arvanitis Argyrios G Azepine inhibitors of Janus kinases
KR101391900B1 (ko) 2005-12-13 2014-05-02 인사이트 코포레이션 야누스 키나아제 억제제로서의 헤테로아릴 치환된 피롤로[2,3-b]피리딘 및 피롤로[2,3-b]피리미딘
US8575164B2 (en) * 2005-12-19 2013-11-05 OSI Pharmaceuticals, LLC Combination cancer therapy
US8962643B2 (en) 2006-02-24 2015-02-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
AR060336A1 (es) 2006-03-31 2008-06-11 Schering Corp Derivados de indazolilpirazinilo inhibidores de proteinquinasas, composiciones farmaceuticas que los contienen y usos como agentes anticancer,entre otros.
US7893058B2 (en) * 2006-05-15 2011-02-22 Janssen Pharmaceutica Nv Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
BRPI0712531A2 (pt) * 2006-05-31 2012-12-25 Galapagos Nv composto de triazolopirazina éteis para o tratamento de doenÇas degenarativas e inflamatàrias
US20090175852A1 (en) 2006-06-06 2009-07-09 Schering Corporation Imidazopyrazines as protein kinase inhibitors
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
HUE029188T2 (en) 2007-03-12 2017-03-28 Ym Biosciences Australia Pty Phenylamino-pyrimidine compounds and their use
US8148369B2 (en) 2007-05-10 2012-04-03 Janssen Pharmaceutica Nv Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases
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.
WO2008157208A2 (en) 2007-06-13 2008-12-24 Incyte Corporation Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
GB0716292D0 (en) * 2007-08-21 2007-09-26 Biofocus Dpi Ltd Imidazopyrazine compounds
JP2011510018A (ja) * 2008-01-18 2011-03-31 オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド 癌治療のためのイミダゾピラジノール誘導体
US20090221612A1 (en) 2008-02-13 2009-09-03 Mitchell Scott A Certain substituted amides, method of making, and method of use thereof
HRP20170317T1 (hr) * 2008-02-15 2017-04-21 Rigel Pharmaceuticals, Inc. Spojevi pirimidin-2-amina i njihova uporaba kao inhibitora jak kinaza
MX2010010012A (es) 2008-03-11 2010-10-20 Incyte Corp Derivados de azetidina y ciclobutano como inhibidores de jak.
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
PT2323993E (pt) 2008-04-16 2015-10-12 Portola Pharm Inc 2,6-diamino-pirimidina-5-il-carboxamidas como inibidores de quinasses syk ou jak
US8258144B2 (en) 2008-04-22 2012-09-04 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
EP2286224A4 (en) * 2008-05-05 2012-04-25 Univ Winthrop Hospital METHOD FOR IMPROVING THE CARDIOVASCULAR RISK PROFILE OF COX-INHIBITORS
EP2283020B8 (en) * 2008-05-19 2012-12-12 OSI Pharmaceuticals, LLC Substituted imidazopyr-and imidazotri-azines
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
GB0822981D0 (en) * 2008-12-17 2009-01-21 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
EP2421837A1 (en) 2009-04-20 2012-02-29 OSI Pharmaceuticals, LLC Preparation of c-pyrazine-methylamines
JP2012526138A (ja) * 2009-05-07 2012-10-25 オーエスアイ・ファーマシューティカルズ,エルエルシー 副腎皮質癌を治療するためのosi−906の使用
DK2432472T3 (da) 2009-05-22 2019-11-18 Incyte Holdings Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octan- eller heptan-nitril som jak-inhibitorer
TW201100429A (en) 2009-05-22 2011-01-01 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
ES2435491T3 (es) 2009-10-09 2013-12-19 Incyte Corporation Derivados de hidroxilo, ceto y glucurónido de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo
EP2496231A1 (en) * 2009-11-05 2012-09-12 Lexicon Pharmaceuticals, Inc. Tryptophan hydroxylase inhibitors for the treatment of cancer
PH12012501361A1 (en) * 2009-12-31 2012-10-22 Centro Nac De Investigaciones Oncologicas Cnio Tricyclic compounds for use as kinase inhibitors
AU2010338365B2 (en) * 2009-12-31 2014-01-30 Novartis Ag Pyrazine derivatives and their use in the treatment of neurological disorders
EP2526102B1 (en) 2010-01-22 2017-03-08 Fundación Centro Nacional de Investigaciones Oncológicas Carlos III Inhibitors of PI3 kinase
PH12015502575A1 (en) 2010-03-10 2017-04-24 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors
US20130131057A1 (en) * 2010-05-13 2013-05-23 Centro Nacional De Investigaciones Oncologicas (Cnio New bicyclic compounds as pi3-k and mtor inhibitors
EP3087972A1 (en) 2010-05-21 2016-11-02 Incyte Holdings Corporation Topical formulation for a jak inhibitor
EP2441755A1 (en) * 2010-09-30 2012-04-18 Almirall, S.A. Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
EP2444084A1 (en) * 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
EP2975027A1 (en) 2010-11-01 2016-01-20 Portola Pharmaceuticals, Inc. Nicotinamides as jak kinase modulators
CA2818545C (en) 2010-11-19 2019-04-16 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
CN103415515B (zh) 2010-11-19 2015-08-26 因塞特公司 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物
PL2675451T3 (pl) 2011-02-18 2016-05-31 Novartis Pharma Ag Terapia skojarzona z inhibitorem mTOR/JAK
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
EP2706852B1 (en) 2011-05-10 2018-08-22 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
WO2013023119A1 (en) 2011-08-10 2013-02-14 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
US8877760B2 (en) 2011-11-23 2014-11-04 Portola Pharmaceuticals, Inc. Substituted pyrazine-2-carboxamide kinase inhibitors
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
WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
EP2903970A4 (en) 2012-10-08 2016-11-30 Portola Pharm Inc SUBSTITUTED PYRIMIDINYL KINASE INHIBITORS
SG10201705989YA (en) 2012-10-15 2017-08-30 Epizyme Inc Substituted benzene compounds
US20150299125A1 (en) * 2012-11-07 2015-10-22 Merck Sharp & Dohme Corp. Prodrug bipyridylaminopyridines as syk inhibitors
EP3949953A1 (en) 2012-11-15 2022-02-09 Incyte Holdings Corporation Sustained-release dosage forms of ruxolitinib
WO2014106606A1 (en) * 2013-01-05 2014-07-10 F. Hoffmann-La Roche Ag Nove phenyl/pyridine series substitued by hydroxyethylamino for the treatment of cancer
CA2897651C (en) 2013-01-10 2021-09-21 Pulmokine, Inc. Non-selective kinase inhibitors
BR112015021458B1 (pt) 2013-03-06 2022-06-07 Incyte Holdings Corporation "processos e intermediários para preparar {1-{1-[3-flúor2-(trifluormetil)isonicotinoil] piperidin-4-il}-3-[4-(7hpirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrila, útil no tratamento de doenças relacionadas com a atividade de janus quinases
WO2015021153A1 (en) 2013-08-07 2015-02-12 Incyte Corporation Sustained release dosage forms for a jak1 inhibitor
CA2926793C (en) 2013-10-11 2022-11-22 Lawrence S. ZISMAN Spray-dry formulations for treating pulmonary arterial hypertension
US9290505B2 (en) 2013-12-23 2016-03-22 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
WO2015157955A1 (en) * 2014-04-17 2015-10-22 Abbvie Inc. Heterocyclic btk inhibit ors
US9856263B2 (en) 2014-04-28 2018-01-02 Pfizer Inc. Heteroaromatic compounds and their use as dopamine D1 ligands
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
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
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
CN110087653A (zh) 2016-10-27 2019-08-02 普尔莫凯恩股份有限公司 用于治疗肺高血压的组合疗法
CN115028640A (zh) 2017-08-25 2022-09-09 吉利德科学公司 Syk抑制剂的多晶型物
TW201924683A (zh) 2017-12-08 2019-07-01 美商英塞特公司 用於治療骨髓增生性贅瘤的低劑量組合療法
DK3746429T3 (da) 2018-01-30 2022-05-02 Incyte Corp Fremgangsmåder til fremstilling af (1-(3-fluor-2-(trifluormethyl)isonicotinyl)piperidin-4-on)
CN112423759A (zh) 2018-03-30 2021-02-26 因赛特公司 使用jak抑制剂治疗化脓性汗腺炎
US20220177978A1 (en) 2019-04-02 2022-06-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
EP3955920A1 (en) 2019-04-16 2022-02-23 Institut National de la Santé et de la Recherche Médicale (INSERM) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
TW202214634A (zh) * 2020-06-09 2022-04-16 大陸商賽諾哈勃藥業(成都)有限公司 雜環化合物及其衍生物
EP4526469A1 (en) 2022-05-16 2025-03-26 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stems cells induced by chronic inflammation
CN119630668A (zh) * 2022-07-25 2025-03-14 细胞基因公司 取代的咪唑并吡嗪化合物作为irak3结合剂

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1345449A (en) * 1971-05-14 1974-01-30 Science Union & Cie Pyridylpiperazines and process for their preparation
US4876256A (en) * 1988-04-29 1989-10-24 Merck & Co., Inc. Alkylpiperazinylpyridines as hypoglycemic agents
US5494908A (en) * 1992-11-23 1996-02-27 Hoechst-Roussel Pharmaceutical Incorporated Substituted 3-(aminoalkylamino)-1,2-benzisoxazoles and related compounds
US5679683A (en) * 1994-01-25 1997-10-21 Warner-Lambert Company Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
US6231833B1 (en) * 1999-08-05 2001-05-15 Pfizer Inc 2,7-substituted octahydro-1H-pyrido[1,2-A]pyrazine derivatives as ligands for serotonin receptors
JPH09132529A (ja) * 1995-11-09 1997-05-20 Ono Pharmaceut Co Ltd 一酸化窒素合成酵素阻害剤
US5958919A (en) * 1996-09-20 1999-09-28 Washington University Treatment of presymptomatic alzheimer's disease to prevent neuronal degeneration
WO1999045009A1 (en) * 1998-03-04 1999-09-10 Bristol-Myers Squibb Company Heterocyclo-substituted imidazopyrazine protein tyrosine kinase inhibitors
RS50087B (sr) * 1998-06-19 2009-01-22 Pfizer Products Inc., Pirolo (2,3-d) pirimidin jedinjenja
EP0982030A3 (en) * 1998-08-17 2000-05-10 Pfizer Products Inc. 2,7-substituted octahydro-pyrrolo 1,2-a]pyrazine derivatives as 5ht 1a ligands
JP2002528506A (ja) * 1998-11-04 2002-09-03 スミスクライン・ビーチャム・コーポレイション ピリジン−4−イルまたはピリミジン−4−イル置換ピラジン
EP1165085B1 (en) * 1999-03-30 2006-06-14 Novartis AG Phthalazine derivatives for treating inflammatory diseases
ATE309241T1 (de) * 1999-09-10 2005-11-15 Merck & Co Inc Tyrosin kinase inhibitoren
ATE384704T1 (de) * 1999-12-17 2008-02-15 Novartis Vaccines & Diagnostic Pyrazin-basierte hemmer der glycogen-synthase- kinase 3
US6335342B1 (en) * 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
IL154267A0 (en) * 2000-08-08 2003-09-17 Ortho Mcneil Pharm Inc Neuroprotective 2-pyridinamine compositions and related methods
JP2004513953A (ja) * 2000-10-24 2004-05-13 メルク エンド カムパニー インコーポレーテッド ジベンズオキサゼピンαVインテグリン受容体アンタゴニスト
EP1399440B1 (en) * 2001-06-15 2009-06-03 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl)benzisoxazoles as protein kinase inhibitors

Cited By (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4777065B2 (ja) * 2002-12-11 2011-09-21 ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド ピラジン系チューブリン阻害剤
JP2006514685A (ja) * 2002-12-11 2006-05-11 サイトピア・リサーチ・ピーティーワイ・リミテッド ピラジン系チューブリン阻害剤
JP2009515888A (ja) * 2005-11-10 2009-04-16 シェーリング コーポレイション プロテインキナーゼインヒビターとしてのイミダゾピラジン
JP2010501003A (ja) * 2006-08-16 2010-01-14 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 ピラジン化合物、その使用及び調製方法
JP2014074057A (ja) * 2007-06-08 2014-04-24 Abbvie Inc キナーゼ阻害薬としての5−ヘテロアリール置換インダゾール類
JP2010532772A (ja) * 2007-07-11 2010-10-14 バイエル・シェーリング・ファルマ・アクチェンゲゼルシャフト イミダゾ−、ピラゾロピラジン類およびイミダゾトリアジン類およびそれらの使用
KR20100116599A (ko) * 2008-02-01 2010-11-01 어키니언 파마슈티칼스 아베 피라진 유도체 및 단백질 키나아제 억제제로서의 이의 용도
JP2011510948A (ja) * 2008-02-01 2011-04-07 アチニオン・ファーマスーティカルズ・アクチエボラーグ 新規化合物、その使用及び製造
KR101599082B1 (ko) * 2008-02-01 2016-03-02 어키니언 파마슈티칼스 아베 피라진 유도체 및 단백질 키나아제 억제제로서의 이의 용도
JP2014148522A (ja) * 2008-02-01 2014-08-21 Akinion Pharmaceuticals Ab 新規化合物、その使用及び製造
US8765761B2 (en) 2008-12-08 2014-07-01 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-{4-[2-methyl-1-(morpholin-4-yl)propan-2-yl]phenyl}imidazo[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a syk inhibitor
JP2012510998A (ja) * 2008-12-08 2012-05-17 ギリアード コネチカット, インコーポレイテッド イミダゾピラジンsyk阻害剤
US9796718B2 (en) 2008-12-08 2017-10-24 Gilead Connecticut, Inc. 6-(benzo[d]thiazol-5-yl)-n-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine
US10093684B2 (en) 2008-12-08 2018-10-09 Gilead Connecticut, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
JP2017101090A (ja) * 2008-12-08 2017-06-08 ギリアード コネチカット, インコーポレイテッド イミダゾピラジンSyk阻害剤
US8962835B2 (en) 2008-12-08 2015-02-24 Gilead Connecticut, Inc. Imidazopyrazine Syk inhibitors
US9120811B2 (en) 2008-12-08 2015-09-01 Gilead Connecticut, Inc. 6-(1H-indazol-6-YL)-N-(4-morpholinophenyl)imidazo[1,4-A]pyrazin-8-amine for treating leukemia or lymphoma
JP2015205935A (ja) * 2008-12-08 2015-11-19 ギリアード コネチカット, インコーポレイテッド イミダゾピラジンSyk阻害剤
US9212191B2 (en) 2008-12-08 2015-12-15 Gilead Connecticut, Inc. 6-(2,3-dihydro-1H-pyrido-[2,3-b][1,4]oxazin-7-yl)-N-(4-morpholinophenyl)imidazo[1,2-a] pyrazin-8-amine as a spleen tyrosine kinase inhibitor
US8748607B2 (en) 2008-12-08 2014-06-10 Gilead Connecticut, Inc. Imidazopyrizine syk inhibitors
JP2012510997A (ja) * 2008-12-08 2012-05-17 ギリアード コネチカット, インコーポレイテッド イミダゾピラジンSyk阻害剤
US9567348B2 (en) 2008-12-08 2017-02-14 Gilead Connecticut, Inc. Substituted pyrazolo[1,5-a]pyrimidines as Syk inhibitors
JP2012524053A (ja) * 2009-04-16 2012-10-11 セントロ ナシオナル デ インベスティガシオネス オンコロヒカス(セエネイオ) キナーゼ阻害剤として使用するためのイミダゾピラジン類
US9562056B2 (en) 2010-03-11 2017-02-07 Gilead Connecticut, Inc. Imidazopyridines Syk inhibitors
US10842803B2 (en) 2010-03-11 2020-11-24 Kronos Bio, Inc. Imidazopyridines Syk inhibitors
US10092583B2 (en) 2010-03-11 2018-10-09 Gilead Connecticut, Inc. Imidazopyridines Syk inhibitors
JP2014520767A (ja) * 2011-07-07 2014-08-25 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 がんの処置のための置換されたアザ複素環
US9382256B2 (en) 2013-07-30 2016-07-05 Gilead Connecticut, Inc. Formulation of Syk inhibitors
US9918939B2 (en) 2013-07-30 2018-03-20 Gilead Connecticut, Inc. Formulation of Syk inhibitors
US9949932B2 (en) 2013-07-30 2018-04-24 Gilead Connecticut, Inc. Formulation of syk inhibitors
US9657023B2 (en) 2013-07-30 2017-05-23 Gilead Connecticut, Inc. Polymorph of Syk inhibitors
US10266539B2 (en) 2013-07-30 2019-04-23 Gilead Connecticut, Inc. Polymorph of Syk inhibitors
US9687492B2 (en) 2013-12-04 2017-06-27 Gilead Sciences, Inc. Methods for treating cancers
US9974792B2 (en) 2013-12-04 2018-05-22 Gilead Sciences, Inc. Methods for treating cancers
US10342794B2 (en) 2013-12-23 2019-07-09 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
US10828299B2 (en) 2013-12-23 2020-11-10 Kronos Bio, Inc. Crystalline monomesylate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine
US9968601B2 (en) 2013-12-23 2018-05-15 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
US11517570B2 (en) 2013-12-23 2022-12-06 Kronos Bio, Inc. Crystalline succinate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine
US12263163B2 (en) 2013-12-23 2025-04-01 Kronos Bio, Inc. Crystalline succinate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine as a Syk inhibitor
US9707236B2 (en) 2014-07-14 2017-07-18 Gilead Sciences, Inc. Combination methods for treating cancers
US10080756B2 (en) 2014-07-14 2018-09-25 Gilead Sciences, Inc. Combination methods for treating cancers
US11339168B2 (en) 2019-02-22 2022-05-24 Kronos Bio, Inc. Crystalline forms of 6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine as Syk inhibitors

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