CN103169708B - 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 - Google Patents

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 Download PDF

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CN103169708B
CN103169708B CN201310060555.0A CN201310060555A CN103169708B CN 103169708 B CN103169708 B CN 103169708B CN 201310060555 A CN201310060555 A CN 201310060555A CN 103169708 B CN103169708 B CN 103169708B
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CN103169708A (zh
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R·辛格
A·阿加德
D·G·帕颜
J·克罗格
H·凯姆
C·赛尔维恩
H·李
S·伯汉米迪帕提
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Rigel Pharmaceuticals Inc
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CN201310060555.0A 2002-07-29 2003-07-29 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 Expired - Lifetime CN103169708B (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US39967302P 2002-07-29 2002-07-29
US60/399,673 2002-07-29
US44394903P 2003-01-31 2003-01-31
US60/443,949 2003-01-31
US45233903P 2003-03-06 2003-03-06
US60/452,339 2003-03-06
US10/631,029 2003-07-29
US10/631,029 US7517886B2 (en) 2002-07-29 2003-07-29 Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
CNA038211203A CN1678321A (zh) 2002-07-29 2003-07-29 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

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CNA038211203A Division CN1678321A (zh) 2002-07-29 2003-07-29 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

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CN103169708A CN103169708A (zh) 2013-06-26
CN103169708B true CN103169708B (zh) 2018-02-02

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CNA038211203A Pending CN1678321A (zh) 2002-07-29 2003-07-29 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

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Publication number Priority date Publication date Assignee Title
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
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
WO2004048343A1 (en) * 2002-11-28 2004-06-10 Schering Aktiengesellschaft Chk-, pdk- and akt-inhibitory pyrimidines, their production and use as pharmaceutical agents
UA80767C2 (en) * 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
CL2004000303A1 (es) * 2003-02-20 2005-04-08 Tibotec Pharm Ltd Compuestos derivados de pirimidinas y triazinas; proceso de preparacion; composicion farmaceutica; y su uso para inhibir la replicacion del vih.
WO2005012262A1 (en) * 2003-07-30 2005-02-10 Cyclacel Limited 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
US7122542B2 (en) 2003-07-30 2006-10-17 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
DK1663242T3 (da) * 2003-08-07 2011-08-01 Rigel Pharmaceuticals Inc 2,4-Pyrimidindiamin-forbindelser og anvendelse som antiproliferative midler
JP4607879B2 (ja) * 2003-08-15 2011-01-05 ノバルティス アーゲー 新生物疾患、炎症および免疫障害の処置に有用な２，４−ピリミジンジアミン
NZ551027A (en) 2004-04-08 2011-01-28 Targegen Inc Benzotriazine inhibitors of kinases
JP4812763B2 (ja) 2004-05-18 2011-11-09 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 シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途
JP5275628B2 (ja) 2004-08-25 2013-08-28 ターゲジェン インコーポレーティッド 複素環式化合物および使用方法
US20060058525A1 (en) * 2004-09-01 2006-03-16 Rajinder Singh Synthesis of 2,4-pyrimidinediamine compounds
CA2581454A1 (en) 2004-09-23 2006-03-30 Reddy Us Therapeutics, Inc. Novel pyrimidine compounds, process for their preparation and compositions containing them
GB2420559B (en) 2004-11-15 2008-08-06 Rigel Pharmaceuticals Inc Stereoisomerically enriched 3-aminocarbonyl bicycloheptene pyrimidinediamine compounds and their uses
ATE540035T1 (de) 2004-11-24 2012-01-15 Rigel Pharmaceuticals Inc Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen
MY169441A (en) * 2004-12-08 2019-04-11 Janssen Pharmaceutica Nv 2,4, (4,6) pyrimidine derivatives
US7713975B1 (en) 2005-01-12 2010-05-11 Alcon, Inc. 3,6-substituted imidazol[1,2-b]pyridazine analogs for treating allergic and inflammatory diseases
US7799778B1 (en) 2005-01-12 2010-09-21 Alcon, Inc. 5-substituted 2-aminopyridine analogs for treating allergic and inflammatory diseases
US7449458B2 (en) 2005-01-19 2008-11-11 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
KR20070097590A (ko) 2005-01-25 2007-10-04 에픽스 델라웨어, 인코포레이티드 치환된 아릴아민 화합물 및 5―ｈｔ6 조절제로서의 이의용도
US8227455B2 (en) 2005-04-18 2012-07-24 Rigel Pharmaceuticals, Inc. Methods of treating cell proliferative disorders
US20060270694A1 (en) * 2005-05-03 2006-11-30 Rigel Pharmaceuticals, Inc. JAK kinase inhibitors and their uses
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
US7576053B2 (en) 2005-06-13 2009-08-18 Rigel Pharmaceuticals, Inc. Methods and compositions for treating degenerative bone disorders
EP1890703B1 (en) * 2005-06-14 2016-05-11 Taigen Biotechnology Pyrimidine compounds as chemokine receptors inhibitors
PT1734251E (pt) * 2005-06-17 2007-03-30 Magneti Marelli Powertrain Spa Injector de combustível
US20070032514A1 (en) * 2005-07-01 2007-02-08 Zahn Stephan K 2,4-diamino-pyrimidines as aurora inhibitors
WO2007009681A1 (en) * 2005-07-15 2007-01-25 Glaxo Group Limited 1 , 1-DIOXID0-2 , 3-DIHYDRO-l , 2-BENZISOTHIAZ0L-6-YL-1H-INDAZOL-4-YL-2 , 4-PYRIMIDINEDI AMINE DERIVATIVES
WO2007028445A1 (en) * 2005-07-15 2007-03-15 Glaxo Group Limited 6-indolyl-4-yl-amino-5-halogeno-2-pyrimidinyl-amino derivatives
US8133900B2 (en) * 2005-11-01 2012-03-13 Targegen, Inc. Use of bi-aryl meta-pyrimidine inhibitors of kinases
MY167260A (en) * 2005-11-01 2018-08-14 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
US8604042B2 (en) 2005-11-01 2013-12-10 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
WO2007111720A2 (en) * 2005-12-06 2007-10-04 Rigel Pharmaceuticals, Inc. Formulation of insoluble small molecule therapeutics in lipid-based carriers
US7713987B2 (en) * 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
WO2007085540A1 (en) * 2006-01-27 2007-08-02 Glaxo Group Limited 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives
CA2642211C (en) 2006-02-17 2012-01-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
US8962643B2 (en) 2006-02-24 2015-02-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US8623887B2 (en) 2006-05-15 2014-01-07 Boehringer Ingelheim International Gmbh Compounds
CA2673125C (en) 2006-10-19 2015-04-21 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
JP5512274B2 (ja) 2006-10-23 2014-06-04 セファロン、インク． ＡＬＫ阻害剤およびｃ−ＭＥＴ阻害剤としての２，４−ジアミノピリミジンの縮合二環式誘導体
US8163902B2 (en) 2006-11-21 2012-04-24 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
WO2008118822A1 (en) 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US7834024B2 (en) * 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
MX2009011199A (es) * 2007-04-16 2010-03-17 Hutchison Medipharma Entpr Ltd Derivados de pirimidina.
JP4782239B2 (ja) 2007-04-18 2011-09-28 ファイザー・プロダクツ・インク 異常細胞増殖治療のためのスルホニルアミド誘導体
ATE521609T1 (de) * 2007-05-04 2011-09-15 Astrazeneca Ab Aminothiazolylpyrimidinderivate und ihre verwendung bei der behandlung von krebs
CA2693594A1 (en) 2007-07-17 2009-01-22 Rigel Pharmaceuticals, Inc. Cyclic amine substituted pyrimidinediamines as pkc inhibitors
RU2477282C2 (ru) * 2007-08-17 2013-03-10 Эл Джи Лайф Сайенсиз Лтд. Соединения индола в качестве ингибиторов клеточного некроза
US20090088371A1 (en) * 2007-08-28 2009-04-02 Rigel Pharmaceuticals, Inc. Combination therapy with syk kinase inhibitor
US20110028405A1 (en) 2007-12-20 2011-02-03 Richard John Harrison Sulfamides as zap-70 inhibitors
DK2252594T3 (en) 2008-01-22 2015-11-23 Dow Agrosciences Llc 4-amino-5-fluoro-pyrimidine derivatives as fungicides
HRP20170317T1 (hr) * 2008-02-15 2017-04-21 Rigel Pharmaceuticals, Inc. Spojevi pirimidin-2-amina i njihova uporaba kao inhibitora jak kinaza
EP2276747A1 (en) * 2008-03-11 2011-01-26 Cellzome Limited Sulfonamides as zap-70 inhibitors
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
KR20100132550A (ko) 2008-04-16 2010-12-17 포톨라 파마슈티컬스, 인코포레이티드 ｓｙｋ 또는 ＪＡＫ 키나제 억제제로서의 ２,６－디아미노-피리미딘－５－일－카르복스아미드
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
US7829574B2 (en) 2008-05-09 2010-11-09 Hutchison Medipharma Enterprises Limited Substituted quinazoline compounds and their use in treating angiogenesis-related diseases
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
PT2300013T (pt) 2008-05-21 2017-10-31 Ariad Pharma Inc Derivados de fósforo como inibidores de cinases
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
EP2361248B1 (en) 2008-06-27 2018-09-19 Celgene CAR LLC Heteroaryl compounds and uses thereof
US8426430B2 (en) 2008-06-30 2013-04-23 Hutchison Medipharma Enterprises Limited Quinazoline derivatives
US7737157B2 (en) 2008-08-29 2010-06-15 Hutchison Medipharma Enterprises Limited Pyrimidine compounds
CN101659659B (zh) * 2008-08-29 2013-01-02 和记黄埔医药（上海）有限公司 嘧啶衍生物及其医药用途
EP2161259A1 (de) 2008-09-03 2010-03-10 Bayer CropScience AG 4-Halogenalkylsubstituierte Diaminopyrimidine als Fungizide
CA2736258C (en) * 2008-09-23 2016-11-29 Rigel Pharmaceuticals, Inc. Tricyclic carbamate jak inhibitors
WO2010078369A2 (en) 2008-12-30 2010-07-08 Rigel Pharmaceuticals, Inc. Pyrimidinediamine kinase inhibitors
ES2635504T3 (es) 2009-01-21 2017-10-04 Rigel Pharmaceuticals, Inc. Derivados de N2-(3-piridilo o fenil)-N4-(4-piperidil)-2,4-pirimidinadiamina útiles en el tratamiento de enfermedades inflamatorias, toimmunitarias o proliferativas
HRP20151325T1 (hr) 2009-01-23 2016-01-01 Rigel Pharmaceuticals, Inc. Pripravci i postupci za inhibiciju jak puta
JP5918693B2 (ja) 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド Ｅｇｆｒ阻害剤及び疾患の治療方法
AR076550A1 (es) 2009-05-06 2011-06-22 Portola Pharm Inc Inhibidores de la janus tirosina kinasa (jak)
WO2010143733A1 (en) 2009-06-09 2010-12-16 Takeda Pharmaceutical Company Limited Novel fused cyclic compound and use thereof
CA2763717A1 (en) * 2009-06-10 2010-12-16 Cellzome Limited Pyrimidine derivatives as zap-70 inhibitors
UA108077C2 (xx) 2009-07-02 2015-03-25 Синтез динатрієвої солі n4-(2,2-диметил-4-$(дигідрофосфонокси)метил]-3-оксо-5-піридо$1,4]оксазин-6-іл)-5-фтор-n2-(3,4,5-триметоксифеніл)-2,4-піримідиндіаміну
CA2768368A1 (en) 2009-07-17 2011-01-20 Rigel Pharmaceuticals, Inc. Deuterated 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses
CA2768543C (en) * 2009-07-28 2017-06-20 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
ES2608670T3 (es) 2009-08-17 2017-04-12 Memorial Sloan-Kettering Cancer Center Derivados de 2-(pirimidin-5-il)-tiopirimidina como moduladores de Hsp70 y Hsc70 para el tratamiento de trastornos proliferativos
EP2501705B1 (en) 2009-11-20 2014-08-27 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses
CA2780759A1 (en) 2009-12-01 2011-06-09 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
US8618095B2 (en) 2010-04-13 2013-12-31 Rigel Pharmaceuticals, Inc. 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses
WO2011144742A1 (en) * 2010-05-21 2011-11-24 Chemilia Ab Novel pyrimidine derivatives
NZ604040A (en) 2010-06-03 2015-02-27 Pharmacyclics Inc The use of inhibitors of bruton’s tyrosine kinase (btk)
JP6035238B2 (ja) 2010-07-21 2016-11-30 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 プロテインキナーゼｃ阻害剤およびその使用
WO2012015972A1 (en) 2010-07-28 2012-02-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
NZ607845A (en) 2010-08-10 2015-03-27 Celgene Avilomics Res Inc Besylate salt of a btk inhibitor
WO2012061299A1 (en) 2010-11-01 2012-05-10 Avila Therapeutics, Inc. Heterocyclic compounds and uses thereof
US20130317029A1 (en) 2010-11-01 2013-11-28 Portola Pharmaceuticals, Inc. Oxypyrimidines as syk modulators
CA2816219C (en) 2010-11-01 2019-10-29 Portola Pharmaceuticals, Inc. Nicotinamides as syk modulators
EP2975027A1 (en) 2010-11-01 2016-01-20 Portola Pharmaceuticals, Inc. Nicotinamides as jak kinase modulators
EP2635285B1 (en) 2010-11-01 2017-05-03 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2012060847A1 (en) 2010-11-07 2012-05-10 Targegen, Inc. Compositions and methods for treating myelofibrosis
US8796255B2 (en) 2010-11-10 2014-08-05 Celgene Avilomics Research, Inc Mutant-selective EGFR inhibitors and uses thereof
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
EP2489663A1 (en) 2011-02-16 2012-08-22 Almirall, S.A. Compounds as syk kinase inhibitors
US8497279B2 (en) 2011-03-10 2013-07-30 Rigel Pharmaceuticals, Inc. Treatment for discoid lupus
EP2688883B1 (en) 2011-03-24 2016-05-18 Noviga Research AB Pyrimidine derivatives
US9249124B2 (en) 2011-03-30 2016-02-02 H. Lee Moffitt Cancer Center And Research Institute, Inc. Aurora kinase inhibitors and methods of making and using thereof
PE20140502A1 (es) 2011-04-22 2014-05-02 Signal Pharm Llc Pirimidinas sustituidas de diaminocarboxamida y diaminocarbonitrilo, composiciones de las mismas y metodos de tratamiento con las mismas
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
EP2736487B2 (en) 2011-07-28 2024-08-28 Rigel Pharmaceuticals, Inc. New (trimethoxyphenylamino)pyrimidinyl formulations
CN108707151B (zh) 2011-08-23 2022-06-03 阿萨纳生物科技有限责任公司 嘧啶并-哒嗪酮化合物及其用途
EP2770830A4 (en) 2011-10-28 2015-05-27 Celgene Avilomics Res Inc METHODS OF TREATING A DISEASE OR DISEASE ASSOCIATED WITH TYROSINE KINASE BTK (BRUTON'S TYROSINE KINASE)
US8877760B2 (en) 2011-11-23 2014-11-04 Portola Pharmaceuticals, Inc. Substituted pyrazine-2-carboxamide kinase inhibitors
MX356753B (es) 2012-03-15 2018-06-12 Celgene Avilomics Res Inc Formas solidas de un inhibidor de cinasa del receptor del factor de crecimiento epidermico.
PT2825042T (pt) 2012-03-15 2018-11-16 Celgene Car Llc Sais de um inibidor de cinases do recetor do fator de crescimento epidérmico
AU2013204563B2 (en) 2012-05-05 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
WO2013173506A2 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
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)
HUE033766T2 (en) 2012-06-15 2018-01-29 Commw Scient Ind Res Org Production of long chain polyunsaturated fatty acids in plant cells
WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
KR101446742B1 (ko) 2012-08-10 2014-10-01 한국화학연구원 Ｎ2,ｎ4-비스(4-(피페라진-1-일)페닐)피리미딘-2,4-디아민 유도체 또는 이의 약학적으로 허용가능한 염 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
WO2014043257A1 (en) 2012-09-12 2014-03-20 Rigel Pharmaceuticals, Inc. Treatment for vitiligo
EP2903970A4 (en) 2012-10-08 2016-11-30 Portola Pharm Inc SUBSTITUTED PYRIMIDINYL KINASE INHIBITORS
DE13847827T1 (de) 2012-10-19 2016-03-10 The University Of North Carolina At Chapel Hill Ionenleitende polymere und polymermischungen für alkalimetallionenbatterien
DK2915804T3 (da) * 2012-10-31 2019-06-03 Fujifilm Toyama Chemical Co Ltd Nyt aminderivat eller salt deraf som TNF-alpha-inhibitorer
EP2928891B1 (en) 2012-12-04 2019-02-20 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US9126950B2 (en) 2012-12-21 2015-09-08 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
EP2948150A1 (en) 2013-01-25 2015-12-02 Rigel Pharmaceuticals, Inc. Compounds and methods for treating inflammatory bowel diseases
WO2014124230A2 (en) 2013-02-08 2014-08-14 Celgene Avilomics Research, Inc. Erk inhibitors and uses thereof
US10130609B2 (en) 2013-03-13 2018-11-20 University Health Network Pyrazole derivatives and their uses thereof
EP2970275B1 (en) 2013-03-14 2018-05-09 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
CN105210227A (zh) 2013-04-01 2015-12-30 北卡罗来纳-查佩尔山大学 用于碱金属离子电池的离子导电含氟聚合物碳酸酯
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
KR102269032B1 (ko) 2013-04-19 2021-06-24 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
US9492471B2 (en) 2013-08-27 2016-11-15 Celgene Avilomics Research, Inc. Methods of treating a disease or disorder associated with Bruton'S Tyrosine Kinase
TWI667233B (zh) * 2013-12-19 2019-08-01 德商拜耳製藥公司 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途
US9415049B2 (en) 2013-12-20 2016-08-16 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
NZ715903A (en) 2014-01-30 2017-06-30 Signal Pharm Llc Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use
EP3143013B1 (en) 2014-05-13 2019-12-18 Memorial Sloan Kettering Cancer Center Hsp70 modulators and methods for making and using the same
ES2741785T3 (es) 2014-08-13 2020-02-12 Celgene Car Llc Formas y composiciones de un inhibidor de ERK
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
JP6903577B2 (ja) 2014-12-16 2021-07-14 シグナル ファーマシューティカルズ，エルエルシー 皮膚におけるｃ−Ｊｕｎ Ｎ末端キナーゼの阻害の測定方法
BR112017012795A2 (pt) 2014-12-16 2018-01-02 Signal Pharmaceuticals, Llc Formulações de 2-(terc-butilamino)-4-((1r,3r,4r)-3- hidroxi-4-metilciclo-hexilamino)-pirimidina-5- carboxamida
CA2975260C (en) 2015-01-29 2024-05-21 Signal Pharmaceuticals Llc Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide
US10227288B2 (en) 2015-02-03 2019-03-12 Blue Current, Inc. Functionalized fluoropolymers and electrolyte compositions
US9580423B2 (en) 2015-02-20 2017-02-28 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
JP6853234B2 (ja) * 2015-07-09 2021-03-31 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Ｍｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ Ｂｔｋ阻害剤としてのピリミジン誘導体及びその使用
MX2018001004A (es) 2015-07-24 2018-06-07 Celgene Corp Metodos de sintesis de clorhidrato de (1r,2r,5r)-5-amino-2-metilci clohexanol e intermedios utiles en este.
WO2017070796A1 (en) * 2015-10-30 2017-05-04 Trillium Therapeutics Inc. Heterocycle derivatives and their use for the treatment of cns disorders
KR20230130747A (ko) * 2016-04-15 2023-09-12 에피자임, 인코포레이티드 Ehmt1 및 ehmt2 저해제로서의 아민-치환된 아릴 또는 헤테로아릴 화합물
DK3448859T3 (da) 2017-03-20 2019-09-23 Forma Therapeutics Inc Pyrrolopyrrolsammensætninger som pyruvatkinase- (pkr) aktivatorer
EP3612181A4 (en) 2017-04-21 2021-01-06 Epizyme, Inc. Combination therapies with ehmt2 inhibitors
US20190008868A1 (en) 2017-04-28 2019-01-10 Asana Biosciences, Llc Formulations, methods, kits, and dosage forms for treating atopic dermatitis and for improved stability of an active pharmaceutical ingredient
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
JP7311228B2 (ja) * 2017-06-30 2023-07-19 ベイジン タイド ファーマシューティカル カンパニー リミテッド Ｒｈｏ－関連プロテインキナーゼ阻害剤、それを含む医薬組成物並びにその調製方法及び使用
CN107417611A (zh) * 2017-07-25 2017-12-01 广州大学 一种3‑（4‑甲氧基苯基）‑6‑甲氧基‑4‑氯‑5,7‑二溴喹啉的合成方法
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
WO2020061378A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Treating sickle cell disease with a pyruvate kinase r activating compound
JP7450610B2 (ja) 2018-09-19 2024-03-15 ノヴォ・ノルディスク・ヘルス・ケア・アーゲー ピルビン酸キナーゼｒの活性化
CN111362928A (zh) * 2018-12-26 2020-07-03 上海喆邺生物科技有限公司 2,4-二氨基嘧啶衍生物
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
SG11202111552YA (en) 2019-05-08 2021-11-29 Aligos Therapeutics Inc MODULATORS OF THR-ß AND METHODS OF USE THEREOF
US20200377518A1 (en) 2019-05-29 2020-12-03 Rigel Pharmaceuticals, Inc. Method of preventing and treating thrombosis
WO2020257495A1 (en) * 2019-06-18 2020-12-24 Purdue Research Foundation Inhibitors of erythrocyte band 3 tyrosine phosphorylation and uses thereof
US11529350B2 (en) 2019-07-03 2022-12-20 Sumitomo Pharma Oncology, Inc. Tyrosine kinase non-receptor 1 (TNK1) inhibitors and uses thereof
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CA3147443A1 (en) 2019-08-08 2021-02-11 Rigel Pharmaceuticals, Inc. Compounds and method for treating cytokine release syndrome
ES2970382T3 (es) 2019-08-14 2024-05-28 Rigel Pharmaceuticals Inc Método para bloquear o mejorar el síndrome de liberación de citocinas
MX2022003254A (es) 2019-09-19 2022-04-18 Forma Therapeutics Inc Composiciones activadoras de piruvato cinasa r (pkr).
CN110746402B (zh) * 2019-09-21 2021-01-15 温州医科大学 一种2-n-芳基-4-n-芳基-5-氟嘧啶类化合物及其制备方法和应用
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
KR20220152293A (ko) 2020-03-12 2022-11-15 리겔 파마슈티칼스, 인크. Covid-19 관련 병태의 치료 방법
GB202007903D0 (en) * 2020-05-27 2020-07-08 Univ Edinburgh Method of producing macrophages
CN112920124B (zh) * 2021-01-29 2024-03-01 安徽医科大学 一种嘧啶-2,4-二胺类化合物及其制备方法与应用
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CN116041263A (zh) * 2023-01-03 2023-05-02 湖南吴赣药业有限公司 一种4-氨基-2,6-二氯嘧啶的合成方法
KR20240156074A (ko) * 2023-04-21 2024-10-29 (주)엠디바이오팜 Hpk1 및 mlk3 저해제 및 이를 함유하는 항암용 조성물

Family Cites Families (201)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3159547A (en) * 1963-06-28 1964-12-01 Abbott Lab Method of lowering blood pressure with 4-(2-amino-4-pyrimidylamino)-benzene-sulfonamide
US3320256A (en) * 1965-04-09 1967-05-16 Hoffmann La Roche Fluorinated imidazoo[1, 2-c]pyrimidines and pyrimido[1, 2-c]pyrimidines
EP0139613A1 (de) 1983-08-29 1985-05-02 Ciba-Geigy Ag N-(2-Nitrophenyl)-4-aminopyrimidin-Derivate, deren Herstellung und Verwendung
DE3618353A1 (de) 1986-05-31 1987-12-03 Hoechst Ag Schaedlingsbekaempfungsmittel auf der basis von aminopyrimidin-derivaten sowie neue aminopyrimidin-verbindungen
EP0285571B1 (de) * 1987-04-02 1992-02-05 Ciba-Geigy Ag Reaktivfarbstoffe, deren Herstellung und Verwendung
SU1499883A1 (ru) 1987-11-24 1991-10-23 Научно-исследовательский институт фармакологии АМН СССР Дихлоргидрат 2,4-бис-(п-трет-бутиланилино)-5-окси-6-метилпиримидина, обладающий анальгетической и противовоспалительной активностью
HU206337B (en) * 1988-12-29 1992-10-28 Mitsui Petrochemical Ind Process for producing pyrimidine derivatives and pharmaceutical compositions
IE63502B1 (en) * 1989-04-21 1995-05-03 Zeneca Ltd Aminopyrimidine derivatives useful for treating cardiovascular disorders
US4983608A (en) * 1989-09-05 1991-01-08 Hoechst-Roussell Pharmaceuticals, Inc. N-substituted-4-pyrimidinamines and pyrimidinediamines
US5179204A (en) * 1989-09-05 1993-01-12 Hoechst-Roussel Pharmaceuticals Incorporated N-substituted-4-pyrimidinamines and pyrimidinediamines
JPH03127790A (ja) 1989-10-11 1991-05-30 Morishita Pharmaceut Co Ltd Ｎ―（１ｈ―テトラゾール―５―イル）―２―アニリノ―５―ピリミジンカルボキシアミド類及びその合成中間体
TW224941B (enExample) 1989-11-08 1994-06-11 Yamanouchi Pharma Co Ltd
GB9012592D0 (en) 1990-06-06 1990-07-25 Smithkline Beecham Intercredit Compounds
DE4029650A1 (de) 1990-09-19 1992-03-26 Hoechst Ag 2-anilino-pyrimidine, verfahren zu ihrer herstellung, sie enthaltene mittel und ihre verwendung als fungizide
CA2074864A1 (en) 1991-07-30 1993-01-31 Carmen Almansa Tetralones with pharmacological activity
US5728536A (en) 1993-07-29 1998-03-17 St. Jude Children's Research Hospital Jak kinases and regulation of Cytokine signal transduction
US5521184A (en) * 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
TW287160B (enExample) * 1992-12-10 1996-10-01 Hoffmann La Roche
HUT74464A (en) * 1993-10-12 1996-12-30 Du Pont Merck Pharma 1n-alkyl-n-arylpyrimidinamines and derivatives thereof, and pharmaceutical compositions containing them
IL112290A (en) 1994-01-12 1999-01-26 Novartis Ag Transformed aryl and the troiryl pyrimidines and herbicides containing them
CA2150609C (en) * 1994-06-01 1998-12-08 Mikiro Yanaka Pyrimidine derivatives and pharmaceutical composition
US5733932A (en) * 1995-01-06 1998-03-31 The Picower Institute For Medical Research Compounds and methods of use to derivatize neighboring lysine residues in proteins under physiological conditions
GB9516121D0 (en) * 1995-08-05 1995-10-04 Pfizer Ltd Organometallic addition to ketones
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
TW440563B (en) * 1996-05-23 2001-06-16 Hoffmann La Roche Aryl pyrimidine derivatives and a pharmaceutical composition thereof
GB9619284D0 (en) * 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
US6004985A (en) * 1996-10-09 1999-12-21 Berlex Laboratories, Inc. Thio acid derived monocylic N-heterocyclics as anticoagulants
DE19710435A1 (de) * 1997-03-13 1998-09-17 Hoechst Ag Verwendung von Pyrimidinderivaten zur Prävention von Krebs allein oder in Kombination mit anderen therapeutischen Maßnahmen
GB9705361D0 (en) 1997-03-14 1997-04-30 Celltech Therapeutics Ltd Chemical compounds
US6022884A (en) * 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
GB9723859D0 (en) 1997-11-12 1998-01-07 Zeneca Ltd Compound,composition and use
DE19750701A1 (de) * 1997-11-15 1999-05-20 Dystar Textilfarben Gmbh & Co Verfahren zur Umsetzung von fluorsubstituierten Heterocyclen mit Aminen in Gegenwart von Phasentransfer-Katalysatoren
JP4135318B2 (ja) 1997-12-15 2008-08-20 アステラス製薬株式会社 新規なピリミジン−５−カルボキサミド誘導体
ATE261730T1 (de) 1997-12-31 2004-04-15 Univ Kansas Wasserlösliche medikamentenvorstufen tertiärer amine enthaltender medikamente und verfahren zu ihrer herstellung
CA2321153A1 (en) * 1998-02-17 1999-08-19 Timothy D. Cushing Anti-viral pyrimidine derivatives
ES2244178T3 (es) * 1998-03-09 2005-12-01 Vertex Pharmaceuticals Incorporated Derivados de 1,2-diazepan como inhibidores de la enzima convertidora de interleuquina-1 beta.
EP1064289A1 (en) 1998-03-18 2001-01-03 Ariad Pharmaceuticals, Inc. Heterocyclic signal transduction inhibitors, compositions containing them
DK0945443T3 (da) 1998-03-27 2003-06-02 Janssen Pharmaceutica Nv HIV-hæmmende pyrimidinderivater
BRPI9909191B8 (pt) * 1998-03-27 2021-07-06 Janssen Pharmaceutica Nv derivados de pirimidina inibidores do hiv, seu uso e composição farmacêutica que os compreende
GB9806739D0 (en) 1998-03-28 1998-05-27 Univ Newcastle Ventures Ltd Cyclin dependent kinase inhibitors
AU3213799A (en) * 1998-04-01 1999-10-18 Du Pont Pharmaceuticals Company Integrin antagonists
KR20010025087A (ko) 1998-05-22 2001-03-26 스튜어트 알. 수터 신규한 2-알킬 치환된 이미다졸 화합물
US6093743A (en) * 1998-06-23 2000-07-25 Medinox Inc. Therapeutic methods employing disulfide derivatives of dithiocarbamates and compositions useful therefor
AU4851599A (en) 1998-06-30 2000-01-17 Parker Hughes Institute Method for inhibiting c-jun expression using jak-3 inhibitors
KR20010089171A (ko) 1998-08-21 2001-09-29 추후제출 퀴나졸린 유도체
AU5438299A (en) 1998-08-29 2000-03-21 Astrazeneca Ab Pyrimidine compounds
DE19851421A1 (de) 1998-11-07 2000-05-11 Boehringer Ingelheim Pharma Neue Pyrimidine, deren Herstellung und Verwendung
AU762523C (en) 1998-11-10 2004-02-12 Janssen Pharmaceutica N.V. HIV replication inhibiting pyrimidines
US6127376A (en) * 1998-12-04 2000-10-03 Berlex Laboratories, Inc. Aryl and heterocyclyl substituted pyrimidine derivatives as anti-coagulants
GB9828511D0 (en) * 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
US6080747A (en) 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
EE200100502A (et) 1999-03-26 2002-12-16 Astrazeneca Ab Ühendid
WO2000059893A1 (en) 1999-04-06 2000-10-12 Krenitsky Pharmaceuticals Inc. Neurotrophic thio substituted pyrimidines
DE19917785A1 (de) 1999-04-20 2000-10-26 Bayer Ag 2,4-Diamino-pyrimidin-Derivate
WO2000076980A1 (en) 1999-06-10 2000-12-21 Yamanouchi Pharmaceutical Co., Ltd. Novel nitrogen-contaiing heterocyclic derivatives or salts thereof
GB9914258D0 (en) * 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
GB9918035D0 (en) 1999-07-30 1999-09-29 Novartis Ag Organic compounds
KR100820605B1 (ko) 1999-09-24 2008-04-08 얀센 파마슈티카 엔.브이. 항바이러스 조성물
DE19945982A1 (de) 1999-09-24 2001-03-29 Knoll Ag Geschwindigkeitsbestimmte Partikel
CZ20021086A3 (cs) 1999-09-30 2002-10-16 Neurogen Corporation Alkylendiaminem substituované heterocykly
AU1026901A (en) 1999-10-29 2001-05-08 Syngenta Participations Ag Novel herbicides
AU4903201A (en) 1999-11-30 2001-07-03 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
CZ303875B6 (cs) 1999-12-10 2013-06-05 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidinová sloucenina a farmaceutická kompozice s jejím obsahem
US20020065270A1 (en) 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
DE60043397D1 (de) * 1999-12-28 2010-01-07 Pharmacopeia Inc Cytokine, insbesondere tnf-alpha, hemmer
US6362172B2 (en) 2000-01-20 2002-03-26 Bristol-Myers Squibb Company Water soluble prodrugs of azole compounds
AU2001237041B9 (en) 2000-02-17 2005-07-28 Amgen Inc. Kinase inhibitors
GB0004886D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004887D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
GB0004888D0 (en) * 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US6525051B2 (en) * 2000-03-27 2003-02-25 Schering Aktiengesellschaft N-heterocyclic derivatives as NOS inhibitors
JP5230050B2 (ja) 2000-05-08 2013-07-10 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ Ｈｉｖ複製阻害剤
US7034019B2 (en) 2000-05-08 2006-04-25 Janssen Pharmaceutica N.V. Prodrugs of HIV replication inhibiting pyrimidines
EA006153B1 (ru) 2000-06-26 2005-10-27 Пфайзер Продактс Инк. СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИММУНОДЕПРЕССАНТОВ
GB0016877D0 (en) 2000-07-11 2000-08-30 Astrazeneca Ab Chemical compounds
JP5220978B2 (ja) 2000-08-18 2013-06-26 スリーエム イノベイティブ プロパティズ カンパニー フルオロアルキル（メタ）アクリレートコポリマーコーティング組成物
AU2001296871A1 (en) 2000-09-15 2002-03-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
CN1592645A (zh) * 2000-09-18 2005-03-09 拜奥根Idec公司 使用b细胞耗尽/免疫调节抗体组合治疗自身免疫病的联合疗法
WO2002043735A1 (en) 2000-11-29 2002-06-06 Parker Hughes Institute Inhibitors of thrombin induced platelet aggregation
US20020137755A1 (en) 2000-12-04 2002-09-26 Bilodeau Mark T. Tyrosine kinase inhibitors
EP1343782B1 (en) 2000-12-21 2009-05-06 SmithKline Beecham Corporation Pyrimidineamines as angiogenesis modulators
HUP0400639A3 (en) 2000-12-21 2010-03-29 Vertex Pharma Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them
WO2002060492A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
WO2002064096A2 (en) 2001-02-16 2002-08-22 Tularik Inc. Methods of using pyrimidine-based antiviral agents
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
ATE416175T1 (de) 2001-02-20 2008-12-15 Astrazeneca Ab 2-arylaminopyrimidine zur behandlung von mit gsk3 in zusammenhang stehenden erkrankungen
GB2373186A (en) 2001-02-23 2002-09-18 Astrazeneca Ab Pharmaceutical combinations of a CCR3 antagonist and a compound which is usefulreatment of asthma, allergic disease or inflammation
HUP0303258A3 (en) 2001-02-23 2004-06-28 Merck & Co Inc N-substituted nonaryl-heterocyclic nmda/nr2b antagonists and pharmaceutical compositions containing them
CA2439263C (en) * 2001-03-02 2012-10-23 Frank Becker Three hybrid assay system
IL159120A0 (en) 2001-05-29 2004-05-12 Schering Ag Cdk inhibiting pyrimidines, production thereof and their use as medicaments
MXPA03010961A (es) 2001-05-31 2004-02-27 Vertex Pharma Compuestos de tiazol utiles como inhibidores de proteinas cinasas.
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
JP4523271B2 (ja) 2001-06-01 2010-08-11 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 プロテインキナーゼのインヒビターとして有用なチアゾール化合物
EP1399440B1 (en) 2001-06-15 2009-06-03 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl)benzisoxazoles as protein kinase inhibitors
HUP0402352A2 (hu) 2001-06-19 2005-02-28 Bristol-Myers Squibb Co. Foszfodiészteráz (PDE) 7 inhibitorként alkalmazható pirimidinszármazékok és ezeket tartalmazó gyógyszerkészítmények
US6878697B2 (en) 2001-06-21 2005-04-12 Ariad Pharmaceuticals, Inc. Phenylamino-pyrimidines and uses thereof
GB0115393D0 (en) 2001-06-23 2001-08-15 Aventis Pharma Ltd Chemical compounds
MXPA03011998A (es) 2001-06-23 2005-07-01 Aventis Pharma Inc Pirrolopirimidinas como inhibidores de protein cinasa.
JP4510442B2 (ja) * 2001-06-26 2010-07-21 ブリストル−マイヤーズ スクイブ カンパニー ＴＮＦ−α発現のＮ−ヘテロ環インヒビター
JO3429B1 (ar) 2001-08-13 2019-10-20 Janssen Pharmaceutica Nv مشتقات برميدينات مثبطة فيروس الايدز
US7115617B2 (en) 2001-08-22 2006-10-03 Amgen Inc. Amino-substituted pyrimidinyl derivatives and methods of use
US6939874B2 (en) * 2001-08-22 2005-09-06 Amgen Inc. Substituted pyrimidinyl derivatives and methods of use
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
WO2003026666A1 (en) 2001-09-26 2003-04-03 Bayer Pharmaceuticals Corporation 2-phenylamino-4- (5-pyrazolylamino)-pyrimidine derivatives as kinase inhibitors, in particular, as src kinase inhibitors
WO2003040141A1 (en) 2001-09-28 2003-05-15 Bayer Pharmaceuticals Corporation Oxazolyl-phenyl-2,4-diamino-pyrimidine compounds and methods for treating hyperproliferative disorders
WO2003032994A2 (de) 2001-10-17 2003-04-24 Boehringer Ingelheim Pharma Gmbh & Co. Kg 5-substituierte 4-amino-2-phenylamino-pyrimidinderivate und ihre verwendung als beta-amyloid modulatoren
ES2314106T3 (es) 2001-10-17 2009-03-16 BOEHRINGER INGELHEIM PHARMA GMBH & CO.KG Derivados de pirimidina, agentes farmaceuticos que contiene dichos compuestos, uso y metodo para su obtencion.
ES2330090T3 (es) 2001-11-28 2009-12-04 Btg International Limited Agentes profilacticos o remedios para la enfermedad de alzheimer o unhibidores de la fibrosis de las proteinas amiloides que contiene compuestos de heteroarilo que contiene nitrogeno.
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
SE0104140D0 (sv) 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
AU2002367172A1 (en) 2001-12-21 2003-07-15 Bayer Pharmaceuticals Corporation 2,4-diamino-pyrimidine derivative compounds as inhibitors of prolylpeptidase, inducers of apoptosis and cancer treatment agents
US6924290B2 (en) 2002-01-23 2005-08-02 Bayer Pharmaceuticals Corporation Rho-kinase inhibitors
TWI329105B (en) * 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
US6998391B2 (en) 2002-02-07 2006-02-14 Supergen.Inc. Method for treating diseases associated with abnormal kinase activity
WO2003066601A1 (en) 2002-02-08 2003-08-14 Smithkline Beecham Corporation Pyrimidine compounds
ATE365165T1 (de) 2002-03-01 2007-07-15 Smithkline Beecham Corp Diaminopyrimidine und deren verwendung als angiogenesehemmer
EP1483260A1 (de) * 2002-03-11 2004-12-08 Schering Aktiengesellschaft Cdk inhibitorische 2-heteroaryl-pyrimidine, deren herstellung und verwendung als arzneimittel
US7288547B2 (en) * 2002-03-11 2007-10-30 Schering Ag CDK-inhibitory 2-heteroaryl-pyrimidines, their production and use as pharmaceutical agents
GB0206215D0 (en) * 2002-03-15 2002-05-01 Novartis Ag Organic compounds
NZ535365A (en) 2002-03-20 2006-07-28 Bristol Myers Squibb Co Phosphate prodrugs of fluorooxindoles
WO2003095448A1 (en) 2002-05-06 2003-11-20 Bayer Pharmaceuticals Corporation Pyridinyl amino pyrimidine derivatives useful for treating hyper-proliferative disorders
CA2485429A1 (en) 2002-05-06 2004-07-15 Vertex Pharmaceuticals Incorporated Thiadiazoles or oxadiazoles and their use as inhibitors of jak protein kinase
WO2004039359A2 (en) 2002-05-06 2004-05-13 Bayer Pharmaceuticals Corporation Use of pyrimidine derivates for the manifacture of a medicament for the treatment of hyper-proliferative disorders
AR039540A1 (es) 2002-05-13 2005-02-23 Tibotec Pharm Ltd Compuestos microbicidas con contenido de pirimidina o triazina
KR20050013562A (ko) 2002-05-30 2005-02-04 버텍스 파마슈티칼스 인코포레이티드 Ｊａｋ 및 ｃｄｋ2 프로테인 키나아제의 억제제
IL165286A0 (en) 2002-06-17 2005-12-18 Smithkline Beecham Corp Chemical process
AU2003244098A1 (en) * 2002-06-28 2004-01-19 Yamanouchi Pharmaceutical Co., Ltd. Diaminopyrimidinecarboxa mide derivative
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
AU2003249539A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc Cyclic compounds containing zinc binding groups as matrix metalloproteinase inhibitors
RU2005106871A (ru) 2002-08-14 2005-10-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибиторы протеинкиназ и их применение
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
GB0226582D0 (en) 2002-11-14 2002-12-18 Cyclacel Ltd Anti-viral compounds
GB0226583D0 (en) 2002-11-14 2002-12-18 Cyclacel Ltd Compounds
EP1572649A2 (en) 2002-11-21 2005-09-14 Pfizer Products Inc. 3-amino-piperidine derivatives and processes for their preparation
CA2507392A1 (en) 2002-11-26 2004-06-10 Pfizer Products Inc. Method of treatment of transplant rejection
WO2004048343A1 (en) 2002-11-28 2004-06-10 Schering Aktiengesellschaft Chk-, pdk- and akt-inhibitory pyrimidines, their production and use as pharmaceutical agents
WO2004050068A1 (en) 2002-11-29 2004-06-17 Janssen Pharmaceutica N.V. Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base
JPWO2004054617A1 (ja) 2002-12-13 2006-04-20 協和醗酵工業株式会社 中枢疾患の予防および／または治療剤
US7226919B2 (en) 2002-12-18 2007-06-05 Vertex Pharmaceuticals Inc. Compositions useful as inhibitors of protein kinases
US7098332B2 (en) * 2002-12-20 2006-08-29 Hoffmann-La Roche Inc. 5,8-Dihydro-6H-pyrido[2,3-d]pyrimidin-7-ones
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
EA011164B1 (ru) 2003-02-07 2009-02-27 Янссен Фармацевтика Н. В. Производные пиримидина для профилактики вич-инфекции
DE602004021472D1 (en) 2003-02-20 2009-07-23 Smithkline Beecham Corp Pyrimiidinverbindungen
CL2004000303A1 (es) 2003-02-20 2005-04-08 Tibotec Pharm Ltd Compuestos derivados de pirimidinas y triazinas; proceso de preparacion; composicion farmaceutica; y su uso para inhibir la replicacion del vih.
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
ES2290743T3 (es) 2003-04-30 2008-02-16 The Institutes For Pharmaceutical Discovery, Llc Heteroarilos sustituidos como inhibidores de las proteina-tirosina fosfatasas.
GB0311274D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
GB0311276D0 (en) 2003-05-16 2003-06-18 Astrazeneca Ab Chemical compounds
WO2005007621A2 (en) 2003-05-30 2005-01-27 Rigel Pharmaceuticals, Inc. Ubiquitin ligase inhibitors
EP1651636A1 (en) 2003-07-10 2006-05-03 Neurogen Corporation Substituted heterocyclic diarylamine analogues
CN100549014C (zh) 2003-07-16 2009-10-14 詹森药业有限公司 作为糖原合酶激酶3抑制剂的三唑并嘧啶衍生物
CA2531333A1 (en) 2003-07-16 2005-02-10 Janssen Pharmaceutica N.V. Triazolopyrimidine derivatives as glycogen synthase kinase 3 inhibitors
WO2005009980A1 (en) 2003-07-22 2005-02-03 Neurogen Corporation Substituted pyridin-2-ylamine analogues
US7442698B2 (en) * 2003-07-24 2008-10-28 Amgen Inc. Substituted heterocyclic compounds and methods of use
WO2005012262A1 (en) 2003-07-30 2005-02-10 Cyclacel Limited 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors
US7122542B2 (en) 2003-07-30 2006-10-17 Rigel Pharmaceuticals, Inc. Methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds
DK1663242T3 (da) * 2003-08-07 2011-08-01 Rigel Pharmaceuticals Inc 2,4-Pyrimidindiamin-forbindelser og anvendelse som antiproliferative midler
JP4607879B2 (ja) 2003-08-15 2011-01-05 ノバルティス アーゲー 新生物疾患、炎症および免疫障害の処置に有用な２，４−ピリミジンジアミン
WO2005028467A1 (en) 2003-09-15 2005-03-31 Anadys Pharmaceuticals, Inc. Antibacterial 3,5-diaminopiperidine-substitute aromatic and heteroaromatic compounds
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
CA2538413A1 (en) 2003-09-18 2005-03-24 Novartis Ag 2,4-di (phenylamino) pyrimidines useful in the treatment of proliferative disorders
WO2005027848A2 (en) 2003-09-19 2005-03-31 Barnes-Jewish Hospital Methods for screening osteogenic compounds targeting syk kinase and/or vav3 and uses of syk modulators and/or vav modulators
KR20060121878A (ko) 2003-09-25 2006-11-29 얀센 파마슈티카 엔.브이. Ｈｉｖ를 저해하는 퓨린 유도체
DE10349423A1 (de) 2003-10-16 2005-06-16 Schering Ag Sulfoximinsubstituierte Parimidine als CDK- und/oder VEGF-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
BRPI0416935A (pt) 2003-11-28 2007-01-16 Novartis Ag derivados de diaril ureia no tratamento de doenças dependentes de quìnase de proteìna
MY141255A (en) 2003-12-11 2010-03-31 Memory Pharm Corp Phosphodiesterase 4 inhibitors, including n-substituted diarylamine analogs
US7511137B2 (en) * 2003-12-19 2009-03-31 Rigel Pharmaceuticals, Inc. Stereoisomers and stereoisomeric mixtures of 1-(2,4-pyrimidinediamino)-2-cyclopentanecarboxamide synthetic intermediates
GB2432834A (en) 2004-01-12 2007-06-06 Cytopia Res Pty Ltd Selective Kinase Inhibitors
GB0402653D0 (en) 2004-02-06 2004-03-10 Cyclacel Ltd Compounds
PL1713806T3 (pl) 2004-02-14 2013-09-30 Irm Llc Związki i kompozycje jako inhibitory kinaz białkowych
US7607424B2 (en) * 2004-02-17 2009-10-27 Planet Eclipse Limited Electro-magnetically operated rotating projectile loader
US7745625B2 (en) 2004-03-15 2010-06-29 Bristol-Myers Squibb Company Prodrugs of piperazine and substituted piperidine antiviral agents
WO2005107760A1 (en) 2004-04-30 2005-11-17 Irm Llc Compounds and compositions as inducers of keratinocyte differentiation
JP4812763B2 (ja) 2004-05-18 2011-11-09 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 シクロアルキル置換ピリミジンジアミン化合物およびそれらの用途
GB0419161D0 (en) 2004-08-27 2004-09-29 Novartis Ag Organic compounds
US20060047135A1 (en) 2004-08-30 2006-03-02 Chadwick Scott T Process for preparing chloromethyl di-tert-butylphosphate
US20060058525A1 (en) * 2004-09-01 2006-03-16 Rajinder Singh Synthesis of 2,4-pyrimidinediamine compounds
JP2008514571A (ja) 2004-09-29 2008-05-08 バイエル・シエーリング・ファーマ アクチエンゲゼルシャフト 細胞周期−キナーゼまたはレセプター−チロシン−キナーゼインヒビターとしての置換２−置換アニリノピリミジン類、それらの製造および薬剤としての使用
US7585883B2 (en) 2004-10-29 2009-09-08 Rigel Pharmaceuticals, Inc. Substituted pyridines and their uses
ATE540035T1 (de) * 2004-11-24 2012-01-15 Rigel Pharmaceuticals Inc Spiro-2,4-pyrimidindiamin-verbindungen und ihre verwendungen
US7442716B2 (en) 2004-12-17 2008-10-28 Merck Frosst Canada Ltd. 2-(phenyl or heterocyclic)-1H-phenantrho[9,10-d]imidazoles as mPGES-1 inhibitors
US8211929B2 (en) 2004-12-30 2012-07-03 Exelixis, Inc. Pyrimidine derivatives as kinase modulators and method of use
US7449458B2 (en) 2005-01-19 2008-11-11 Rigel Pharmaceuticals, Inc. Prodrugs of 2,4-pyrimidinediamine compounds and their uses
US20060270694A1 (en) * 2005-05-03 2006-11-30 Rigel Pharmaceuticals, Inc. JAK kinase inhibitors and their uses
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
US7576053B2 (en) * 2005-06-13 2009-08-18 Rigel Pharmaceuticals, Inc. Methods and compositions for treating degenerative bone disorders
MX2008000574A (es) 2005-07-11 2008-03-14 Sanofi Aventis Nuevos derivados de 2,4-dianilinopirimidinas, la preparacion de los mismos, su uso como medicamentos, composiciones farmaceuticas y, en particular, como inhibidores ikk.
PT1913009E (pt) 2005-07-28 2010-06-25 Intervet Int Bv Novos (tio)carbamatos de benzimidazole com actividade antiparasitária e sua síntese
US20090114877A1 (en) 2005-09-13 2009-05-07 Eisai R&D Management Co., Ltd. Composition Containing Stability-Improved Chloromethyl Phosphate Derivatve and Process for Producing Same
EP1951261A4 (en) * 2005-10-31 2009-06-24 Rigel Pharmaceuticals Inc PREPARATIONS AND METHODS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
MY167260A (en) 2005-11-01 2018-08-14 Targegen Inc Bi-aryl meta-pyrimidine inhibitors of kinases
US7713987B2 (en) * 2005-12-06 2010-05-11 Rigel Pharmaceuticals, Inc. Pyrimidine-2,4-diamines and their uses
TW200736232A (en) 2006-01-26 2007-10-01 Astrazeneca Ab Pyrimidine derivatives
WO2007085540A1 (en) 2006-01-27 2007-08-02 Glaxo Group Limited 1h-indaz0l-4-yl-2 , 4-pyrimidinediamine derivatives
CA2642211C (en) * 2006-02-17 2012-01-24 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds for treating or preventing autoimmune diseases
US8962643B2 (en) * 2006-02-24 2015-02-24 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
US7776855B2 (en) 2006-07-27 2010-08-17 Janssen Pharmaceutica N.V. Antimicrobial oxazolidinone prodrugs

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CA2492325C (en) 2012-09-18
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