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RU2008122048A - Аминопиримины в качестве ингибиторов киназ - Google Patents

Аминопиримины в качестве ингибиторов киназ Download PDF

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RU2008122048A
RU2008122048A RU2008122048/04A RU2008122048A RU2008122048A RU 2008122048 A RU2008122048 A RU 2008122048A RU 2008122048/04 A RU2008122048/04 A RU 2008122048/04A RU 2008122048 A RU2008122048 A RU 2008122048A RU 2008122048 A RU2008122048 A RU 2008122048A
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Хэйли БИНЧ (US)
Хэйли Бинч
Майкл МОРТИМОР (GB)
Майкл МОРТИМОР
Дамьен ФРАЙСС (GB)
Дамьен ФРАЙСС
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Элистер РЕЗЕРФОРД
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Abstract

1. Соединение формулы I: ! ! или его фармацевтически приемлемая соль, ! где R2 представляет собой C1-3-алкил или циклопропил; ! R9 представляет собой галоген, C1-3-алкил, -O-(C1-3-алкил), -S-(C1-3-алкил) или CF3 и ! p равно 1-2. ! 2. Соединение по п.1, в котором R2 представляет собой метил. ! 3. Соединение по п.2, в котором p равно 1. ! 4. Соединение по п.2, в котором R9 является заместителем в орто-положении. ! 5. Соединение по п.3, в котором R9 является заместителем в орто-положении. ! 6. Соединение по п.5, где R9 представляет собой F, Cl или CF3. ! 7. Соединение по п.1, выбранное из следующих: ! ! 8. Композиция, включающая соединение по любому из пп.1-7 и фармацевтически приемлемый носитель, вспомогательное вещество или разбавитель. ! 9. Способ ингибирования активности Аврора-протеинкиназы в биологическом образце, включающий контактирование указанного биологического образца с соединением по любому из пп.1-7. ! 10. Способ лечения пролиферативного расстройства у пациента, включающий стадию введения указанному пациенту соединения по любому из пп.1-7. ! 11. Способ по п.10, где указанное пролиферативное расстройство выбрано из меланомы, миеломы, лейкемии, лимфомы, нейробластомы, или рака, выбранного из рака толстой кишки, груди, желудка, яичников, шейки матки, легкого, центральной нервной системы (ЦНС), почки, простаты, мочевого пузыря, поджелудочной железы, мозга (глиомы), головы и шеи, почек, печени, меланомы, саркомы, или рака щитовидной железы у пациента, нуждающегося в лечении, где указанный способ включает введение указанному пациенту соединения по любому из пп.1-7. ! 12. Способ лечения рака у пациента, нуждающегося в лечении, включающий последовательное или совместное введение соедин

Claims (15)

1. Соединение формулы I:
Figure 00000001
или его фармацевтически приемлемая соль,
где R2 представляет собой C1-3-алкил или циклопропил;
R9 представляет собой галоген, C1-3-алкил, -O-(C1-3-алкил), -S-(C1-3-алкил) или CF3 и
p равно 1-2.
2. Соединение по п.1, в котором R2 представляет собой метил.
3. Соединение по п.2, в котором p равно 1.
4. Соединение по п.2, в котором R9 является заместителем в орто-положении.
5. Соединение по п.3, в котором R9 является заместителем в орто-положении.
6. Соединение по п.5, где R9 представляет собой F, Cl или CF3.
7. Соединение по п.1, выбранное из следующих:
Figure 00000002
Figure 00000003
Figure 00000004
Figure 00000005
8. Композиция, включающая соединение по любому из пп.1-7 и фармацевтически приемлемый носитель, вспомогательное вещество или разбавитель.
9. Способ ингибирования активности Аврора-протеинкиназы в биологическом образце, включающий контактирование указанного биологического образца с соединением по любому из пп.1-7.
10. Способ лечения пролиферативного расстройства у пациента, включающий стадию введения указанному пациенту соединения по любому из пп.1-7.
11. Способ по п.10, где указанное пролиферативное расстройство выбрано из меланомы, миеломы, лейкемии, лимфомы, нейробластомы, или рака, выбранного из рака толстой кишки, груди, желудка, яичников, шейки матки, легкого, центральной нервной системы (ЦНС), почки, простаты, мочевого пузыря, поджелудочной железы, мозга (глиомы), головы и шеи, почек, печени, меланомы, саркомы, или рака щитовидной железы у пациента, нуждающегося в лечении, где указанный способ включает введение указанному пациенту соединения по любому из пп.1-7.
12. Способ лечения рака у пациента, нуждающегося в лечении, включающий последовательное или совместное введение соединения по любому из пп.1-7 или его фармацевтически приемлемой соли, и другого терапевтического агента.
13. Способ по п.12, где указанный терапевтический агент выбран из таксанов, ингибиторов bcr-abl, ингибиторов EGFR, повреждающих ДНК агентов и антиметаболитов.
14. Способ по п.12, где указанный терапевтический агент выбран из паклитаксела, гливека, дасатиниба, нилотиниба, тарсева, ирессы, цисплатина, оксалиплатина, карбоплатина, антрациклинов, AraC и 5-FU.
15. Способ по п.12, где указанный терапевтический агент выбран из камптотецина, доксорубицина, идарубицина, цисплатина, таксола, таксотера, винкристина, тарсева, ингибитора MEK, U0126, ингибитора KSP, вориностата, гливека, дасатиниба и нилотиниба.
RU2008122048/04A 2005-11-03 2006-11-03 Аминопиримидины в качестве ингибиторов киназ RU2427578C2 (ru)

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Families Citing this family (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6660731B2 (en) 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
EP1317450B1 (en) 2000-09-15 2006-11-22 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
SE0104140D0 (sv) * 2001-12-07 2001-12-07 Astrazeneca Ab Novel Compounds
WO2004072029A2 (en) 2003-02-06 2004-08-26 Vertex Pharmaceuticals Incorporated Pyrazolopyridazines useful as inhibitors of protein kinases
BRPI0607455A2 (pt) * 2005-02-16 2009-09-01 Astrazeneca Ab composto, processo para a preparação do mesmo, uso de um composto, e composição farmacêutica
JP2008540622A (ja) * 2005-05-16 2008-11-20 アストラゼネカ アクチボラグ 化合物
CN101340909B (zh) * 2005-10-18 2012-01-11 詹森药业有限公司 抑制flt3激酶的方法
EP1945631B8 (en) * 2005-10-28 2013-01-02 AstraZeneca AB 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer
SG166827A1 (en) * 2005-11-03 2010-12-29 Vertex Pharma Aminopyrimidines useful as kinase inhibitors
CN101360740A (zh) * 2005-11-16 2009-02-04 沃泰克斯药物股份有限公司 可用作激酶抑制剂的氨基嘧啶
US8697716B2 (en) 2006-04-20 2014-04-15 Janssen Pharmaceutica Nv Method of inhibiting C-KIT kinase
CA2650057C (en) * 2006-04-20 2014-07-29 Janssen Pharmaceutica N.V. Phenyl- or pyridinyl-amide as inhibitors of c-fms kinase
MX2009004807A (es) 2006-11-02 2009-06-15 Vertex Pharma Aminopiridinas y aminopirimidinas utiles como inhibidores de proteina cinasa.
DE602007007985D1 (de) 2006-12-19 2010-09-02 Vertex Pharma Als inhibitoren von proteinkinasen geeignete aminopyrimidine
MX2009009591A (es) * 2007-03-09 2009-11-10 Vertex Pharma Aminopirimidinas utiles como inhibidores de proteinas cinasas.
MX2009009592A (es) 2007-03-09 2009-11-10 Vertex Pharma Aminopiridinas utiles como inhibidores de proteinas cinasas.
CN101663295B (zh) 2007-03-09 2014-11-05 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的氨基嘧啶类化合物
CN101679386A (zh) 2007-04-13 2010-03-24 沃泰克斯药物股份有限公司 可用作激酶抑制剂的氨基嘧啶类化合物
WO2008129255A1 (en) * 2007-04-18 2008-10-30 Astrazeneca Ab 5-aminopyrazol-3-yl-3h-imidazo [4,5-b] pyridine derivatives and their use for the treatment of cancer
WO2008137621A1 (en) * 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
EP2152694A2 (en) 2007-05-02 2010-02-17 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
MX2009011811A (es) * 2007-05-02 2010-01-14 Vertex Pharma Aminopirimidinas utiles como inhibidores de cinasa.
CN101687863B (zh) * 2007-05-04 2012-09-12 阿斯利康(瑞典)有限公司 氨基-噻唑基-嘧啶衍生物及其治疗癌症的用途
UA99459C2 (en) * 2007-05-04 2012-08-27 Астразенека Аб 9-(pyrazol-3-yl)- 9h-purine-2-amine and 3-(pyraz0l-3-yl)-3h-imidazo[4,5-b]pyridin-5-amine derivatives and their use for the treatment of cancer
AU2008257044A1 (en) * 2007-05-24 2008-12-04 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
US20090029992A1 (en) * 2007-06-11 2009-01-29 Agoston Gregory E Substituted pyrazole compounds
CA2694499A1 (en) * 2007-07-31 2009-02-05 Vertex Pharmaceuticals Incorporated Process for preparing 5-fluoro-1h-pyrazolo [3, 4-b] pyridin-3-amine and derivatives thereof
AU2008287339A1 (en) * 2007-08-15 2009-02-19 Vertex Pharmaceuticals Incorporated 4-(9-(3, 3-difluorocyclopentyl) -5, 7, 7-trimethyl-6-oxo-6, 7, 8, 9-tetrahydro-5H-pyrimido [4, 5-b][1, 4] diazepin-2-ylamino)-3-methoxybenzamide Derivatives as Inhibitors of the Human Protein Kinases PLK1 to PLK4 for the Treatment of Proliferative Diseases
AU2008305294B2 (en) 2007-09-21 2012-11-29 Array Biopharma Inc. Pyridin-2 -yl-amino-1, 2, 4 -thiadiazole derivatives as glucokinase activators for the treatment of diabetes mellitus
WO2009086012A1 (en) * 2007-12-20 2009-07-09 Curis, Inc. Aurora inhibitors containing a zinc binding moiety
US20110033461A1 (en) * 2008-03-12 2011-02-10 Vladimir Ratushny Combination Therapy for the Treatment of Cancer
US8324199B2 (en) * 2008-03-13 2012-12-04 Bristol-Myers Squibb Company Pyridazine derivatives as factor xia inhibitors
CN104694570B (zh) * 2008-03-17 2019-07-16 斯克里普斯研究所 用于产生诱导的多能干细胞的组合化学遗传方法
TW201006830A (en) * 2008-06-11 2010-02-16 Astrazeneca Ab Chemical compounds
NZ603495A (en) * 2008-09-05 2014-05-30 Celgene Avilomics Res Inc Algorithm for designing irreversible inhibitors
MX2011003447A (es) * 2008-09-30 2011-07-29 Astrazeneca Ab Inhibidores heterociclicos de jak quinasa.
AU2009330727B2 (en) 2008-12-22 2016-07-28 Millennium Pharmaceuticals, Inc. Combination of Aurora kinase inhibitors and anti-CD20 antibodies
KR20120016676A (ko) * 2009-06-09 2012-02-24 아브락시스 바이오사이언스, 엘엘씨 우레이도페닐치환 트리아진 유도체와 이들의 치료적 용도
MX339811B (es) 2009-09-16 2016-06-08 Celgene Avilomics Res Inc * Conjugados e inhibidores de cinasa de proteina.
US20110269244A1 (en) 2009-12-30 2011-11-03 Petter Russell C Ligand-directed covalent modification of protein
CA2803446C (en) 2010-07-02 2019-06-04 University Health Network Use of plk4 antagonists for treating pten mutant diseases
SG10201505951VA (en) * 2010-07-30 2015-08-28 Oncotherapy Science Inc Quinoline derivatives and melk inhibitors containing the same
US9382229B2 (en) 2011-02-15 2016-07-05 The Johns Hopkins University Compounds and methods of use thereof for treating neurodegenerative disorders
EP2736895B1 (en) 2011-07-27 2016-01-06 Astrazeneca AB 2-(2,4,5-substituted-anilino) pyrimidine derivatives as egfr modulators useful for treating cancer
CN104024248A (zh) 2011-08-25 2014-09-03 霍夫曼-拉罗奇有限公司 丝氨酸/苏氨酸pak1抑制剂
JP2014525418A (ja) * 2011-09-05 2014-09-29 浙江海正薬業股▲ふん▼有限公司 タンパク質キナーゼ阻害活性を有する４−置換−（３−置換−１ｈ−ピラゾール−５−アミノ）−ピリミジン誘導体及びその使用
MX2014006479A (es) 2011-11-30 2015-01-22 Univ Emory Inhibidores antivirales de la janus cinasa utiles en el tratamiento o prevencion de infecciones retrovirales y otras infecciones virales.
KR20140103972A (ko) 2011-12-22 2014-08-27 에프. 호프만-라 로슈 아게 세린/트레오닌 키나아제 억제제로서의 2,4-다이아민-피리미딘 유도체
SG11201405761WA (en) 2012-03-16 2014-10-30 Axikin Pharmaceuticals Inc 3,5-diaminopyrazole kinase inhibitors
RS61664B1 (sr) 2012-04-24 2021-04-29 Vertex Pharma Inhibitori dna-pk
WO2013173506A2 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
EP2852388A4 (en) 2012-05-23 2016-01-13 Univ Johns Hopkins COMPOUNDS AND METHOD FOR USE THEREOF FOR THE TREATMENT OF NEURODEEGENERATIVE DISEASES
CA2880896C (en) 2012-06-26 2021-11-16 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
BR112015010109A2 (pt) 2012-11-05 2017-07-11 Nant Holdings Ip Llc derivados de indol-5-ol substituídos e suas aplicações terapêuticas
HUE057527T2 (hu) 2013-03-12 2022-05-28 Vertex Pharma DNS-PK inhibitorok
RU2015143657A (ru) 2013-03-15 2017-04-27 Нэнтбайосайенс, Инк. Замещенные производные индол-5-ола и их терапевтические применения
US11491154B2 (en) 2013-04-08 2022-11-08 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds
CA2949048A1 (en) * 2013-05-22 2014-11-27 The Regents Of The University Of California Aurora kinase inhibitors
NZ631142A (en) 2013-09-18 2016-03-31 Axikin Pharmaceuticals Inc Pharmaceutically acceptable salts of 3,5-diaminopyrazole kinase inhibitors
HRP20181841T1 (hr) 2013-10-17 2019-01-11 Vertex Pharmaceuticals Incorporated Sukristali (s)-n-metil-8-(1-((2′-metil-[4,5′-bipirimidin]-6-il)amino)propan-2-il)kinolin-4-karboksamida i njegovih deuteriranih derivata kao inhibitora dna-pk
EP3076963A4 (en) 2013-12-06 2017-09-13 Millennium Pharmaceuticals, Inc. Combination of aurora kinase inhibitors and anti-cd30 antibodies
EA032473B1 (ru) 2014-12-23 2019-05-31 Аксикин Фармасьютикалз, Инк. 3,5-диаминопиразоловые ингибиторы киназы
US10118904B2 (en) 2015-06-05 2018-11-06 Vertex Pharmaceuticals Incorporated Triazoles for the treatment of Demyelinating Diseases
EP3324976A4 (en) 2015-07-21 2019-03-27 Millennium Pharmaceuticals, Inc. ADMINISTRATION OF KINASE AURORA INHIBITOR AND CHEMOTHERAPEUTIC AGENTS
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
JP2019529475A (ja) 2016-09-27 2019-10-17 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ｄｎａ損傷剤とｄｎａ−ｐｋ阻害剤との組合せ物を使用する、がんを処置するための方法
CN110062754B (zh) * 2016-12-14 2024-01-02 英特维特国际股份有限公司 作为选择性Janus激酶抑制剂的氨基吡唑类化合物
US11440898B2 (en) 2016-12-28 2022-09-13 Minoryx Therapeutics S.L. Isoquinoline compounds, methods for their preparation, and therapeutic uses thereof in conditions associated with the alteration of the activity of beta galactosidase
CN106841420A (zh) * 2016-12-30 2017-06-13 广州中大南沙科技创新产业园有限公司 一种LC‑MS/MS测定大鼠血浆中Ly‑7u浓度的方法
WO2019195658A1 (en) 2018-04-05 2019-10-10 Dana-Farber Cancer Institute, Inc. Sting levels as a biomarker for cancer immunotherapy
KR20210144844A (ko) 2019-03-29 2021-11-30 아스트라제네카 아베 비-소세포 폐암의 치료에 사용하기 위한 오시머티닙
CN110132795A (zh) * 2019-05-20 2019-08-16 华核（天津）新技术开发有限公司 放射性去污效率测试方法
WO2021041532A1 (en) 2019-08-26 2021-03-04 Dana-Farber Cancer Institute, Inc. Use of heparin to promote type 1 interferon signaling
WO2021178485A1 (en) * 2020-03-06 2021-09-10 National Health Research Institutes Pyrimidine compounds and their pharmaceutical uses
US11643394B2 (en) 2020-04-30 2023-05-09 Icahn School Of Medicine At Mount Sinai Krüppel-like factor 15 (KLF15) small molecule agonists in kidney disease
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
WO2025049402A1 (en) * 2023-08-28 2025-03-06 Quanta Therapeutics, Inc. Kras modulators and uses thereof

Family Cites Families (119)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3133081A (en) * 1964-05-12 J-aminoindazole derivatives
US3935183A (en) * 1970-01-26 1976-01-27 Imperial Chemical Industries Limited Indazole-azo phenyl compounds
BE754242A (fr) 1970-07-15 1971-02-01 Geigy Ag J R Diamino-s-triazines et dinitro-s-triazines
US3998951A (en) * 1974-03-13 1976-12-21 Fmc Corporation Substituted 2-arylquinazolines as fungicides
DE2458965C3 (de) 1974-12-13 1979-10-11 Bayer Ag, 5090 Leverkusen 3-Amino-indazol-N-carbonsäure-Derivate, Verfahren zu ihrer Herstellung sowie sie enthaltende Arzneimittel
MA18829A1 (fr) 1979-05-18 1980-12-31 Ciba Geigy Ag Derives de la pyrimidine,procedes pour leur preparation,compositions pharmaceutiques contenant ces composes et leur utilisation therapeutique
DOP1981004033A (es) 1980-12-23 1990-12-29 Ciba Geigy Ag Procedimiento para proteger plantas de cultivo de la accion fitotoxica de herbicidas.
SE8102193L (sv) * 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och dess anvendning
SE8102194L (sv) 1981-04-06 1982-10-07 Pharmacia Ab Terapeutiskt aktiv organisk forening och farmaceutisk beredning innehallande denna
JPS58124773A (ja) * 1982-01-20 1983-07-25 Mitsui Toatsu Chem Inc ５−メチルチオピリミジン誘導体とその製造法と農園芸用殺菌剤
EP0136976A3 (de) 1983-08-23 1985-05-15 Ciba-Geigy Ag Verwendung von Phenylpyrimidinen als Pflanzenregulatoren
DE3725638A1 (de) 1987-08-03 1989-02-16 Bayer Ag Neue aryloxy (bzw. thio)aminopyrimidine
US5710158A (en) 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5597920A (en) 1992-04-30 1997-01-28 Neurogen Corporation Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes
JPH0665237A (ja) 1992-05-07 1994-03-08 Nissan Chem Ind Ltd 置換ピラゾール誘導体および農園芸用殺菌剤
ATE325113T1 (de) 1993-10-01 2006-06-15 Novartis Pharma Gmbh Pharmacologisch wirksame pyrimidinderivate und verfahren zu deren herstellung
AU700964B2 (en) 1994-11-10 1999-01-14 Cor Therapeutics, Inc. Pharmaceutical pyrazole compositions useful as inhibitors of protein kinases
IL117659A (en) * 1995-04-13 2000-12-06 Dainippon Pharmaceutical Co Substituted 2-phenyl pyrimidino amino acetamide derivative process for preparing the same and a pharmaceutical composition containing same
US5935966A (en) 1995-09-01 1999-08-10 Signal Pharmaceuticals, Inc. Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions
WO1997009325A1 (en) 1995-09-01 1997-03-13 Signal Pharmaceuticals, Inc. Pyrimidine carboxylates and related compounds and methods for treating inflammatory conditions
GB9523675D0 (en) 1995-11-20 1996-01-24 Celltech Therapeutics Ltd Chemical compounds
US6716575B2 (en) * 1995-12-18 2004-04-06 Sugen, Inc. Diagnosis and treatment of AUR1 and/or AUR2 related disorders
PT912559E (pt) 1996-07-13 2003-03-31 Glaxo Group Ltd Compostos heterociclicos fundidos como inibidores de proteina tirosina quinase
JPH10130150A (ja) 1996-09-05 1998-05-19 Dainippon Pharmaceut Co Ltd 酢酸アミド誘導体からなる医薬
GB9619284D0 (en) 1996-09-16 1996-10-30 Celltech Therapeutics Ltd Chemical compounds
US6251911B1 (en) 1996-10-02 2001-06-26 Novartis Ag Pyrimidine derivatives and processes for the preparation thereof
CA2268098A1 (en) 1996-10-11 1998-04-23 Warner-Lambert Company Aspartate ester inhibitors of interleukin-1.beta. converting enzyme
AU741203B2 (en) 1997-10-10 2001-11-22 Cytovia, Inc. Dipeptide apoptosis inhibitors and the use thereof
US6267952B1 (en) * 1998-01-09 2001-07-31 Geltex Pharmaceuticals, Inc. Lipase inhibiting polymers
JP2000026421A (ja) 1998-01-29 2000-01-25 Kumiai Chem Ind Co Ltd ジアリ―ルスルフィド誘導体及び有害生物防除剤
US6200977B1 (en) * 1998-02-17 2001-03-13 Tularik Inc. Pyrimidine derivatives
DE69925268T2 (de) 1998-03-16 2006-03-23 Cytovia, Inc., San Diego Dipeptid-Caspase-Inhibitoren und deren Verwendung
TR200003513T2 (tr) 1998-06-02 2001-06-21 Osi Pharmaceuticals, Inc. Pirolo[2,3d]Pirimidin kompozisyonları ve kullanımları
JP4533534B2 (ja) 1998-06-19 2010-09-01 ノバルティス バクシンズ アンド ダイアグノスティックス，インコーポレーテッド グリコーゲンシンターゼキナーゼ３のインヒビター
CA2339188A1 (en) * 1998-08-21 2000-03-02 Dupont Pharmaceuticals Company Isoxazolo¬4,5-d|pyrimidines as crf antagonists
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
DE69925141T2 (de) 1998-10-08 2006-04-27 Astrazeneca Ab Chinazolin derivate
GB9828640D0 (en) 1998-12-23 1999-02-17 Smithkline Beecham Plc Novel method and compounds
GB9828511D0 (en) 1998-12-24 1999-02-17 Zeneca Ltd Chemical compounds
BR9916896A (pt) 1999-01-13 2001-11-20 Warner Lambert Co Diaril aminas substituìdas com 1-heterociclo
DE60012721D1 (de) 1999-03-29 2004-09-09 Uutech Ltd Analoge des magensaft inhibierenden peptides und ihre verwendung für die behandlung von diabetes
AU766081B2 (en) 1999-03-30 2003-10-09 Novartis Ag Phthalazine derivatives for treating inflammatory diseases
AU781849C (en) 1999-06-17 2006-03-02 Synta Pharmaceuticals Corp. Inhibitors of IL-12 production
GB9914258D0 (en) 1999-06-18 1999-08-18 Celltech Therapeutics Ltd Chemical compounds
CZ2002534A3 (cs) 1999-08-13 2002-07-17 Vertex Pharmaceuticals Incorporated Inhibitory protein-kináz, farmaceutické prostředky, které je obsahují, a jejich pouľití
ATE396978T1 (de) 1999-10-07 2008-06-15 Amgen Inc Triazin-kinase-hemmer
HUP0203300A3 (en) 1999-11-30 2003-10-28 Pfizer Prod Inc 2,4-diaminopyrimidine compounds useful as immunosuppressants, pharmaceutical compositions containing them and their use
WO2001039777A1 (en) 1999-12-02 2001-06-07 Osi Pharmaceuticals, Inc. Compounds specific to adenosine a1 a2a, and a3 receptors and uses thereof
US6376489B1 (en) 1999-12-23 2002-04-23 Icos Corporation Cyclic AMP-specific phosphodiesterase inhibitors
MY125768A (en) 1999-12-15 2006-08-30 Bristol Myers Squibb Co N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl]-carboxamide inhibitors of cyclin dependent kinases
AU2735201A (en) 1999-12-28 2001-07-09 Pharmacopeia, Inc. Pyrimidine and triazine kinase inhibitors
US20020065270A1 (en) * 1999-12-28 2002-05-30 Moriarty Kevin Joseph N-heterocyclic inhibitors of TNF-alpha expression
CN1362953A (zh) * 2000-02-05 2002-08-07 沃泰克斯药物股份有限公司 用作erk抑制剂的吡唑组合物
AU2001237041B9 (en) 2000-02-17 2005-07-28 Amgen Inc. Kinase inhibitors
GB0004887D0 (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
ATE297946T1 (de) 2000-04-03 2005-07-15 Vertex Pharma Inhibitoren von serin proteasen, speziell der hepatitis-c-virus ns3-protease
CA2398446A1 (en) 2000-04-18 2001-10-25 Agouron Pharmaceuticals, Inc. Pyrazoles for inhibiting protein kinases
ES2305081T3 (es) * 2000-06-28 2008-11-01 Astrazeneca Ab Derivados de quinozolina sustituidos y su uso como inhibidores.
IL153670A0 (en) 2000-07-21 2003-07-06 Schering Corp Novel peptides as ns3-serine protease inhibitors of hepatitis c virus
NZ523656A (en) 2000-08-31 2004-11-26 Pfizer Prod Inc Pyrazole derivatives and their use as protein kinase inhibitors
US6660731B2 (en) * 2000-09-15 2003-12-09 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US6613776B2 (en) * 2000-09-15 2003-09-02 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
NZ525016A (en) * 2000-09-15 2004-10-29 Vertex Pharma Isoxazoles and their use as inhibitors of ERK
US6610677B2 (en) 2000-09-15 2003-08-26 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
EP1317450B1 (en) 2000-09-15 2006-11-22 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
US7473691B2 (en) * 2000-09-15 2009-01-06 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
BR0114020A (pt) 2000-09-20 2003-07-22 Merck Patent Gmbh 4-amino-quinazolinas
US6641579B1 (en) 2000-09-29 2003-11-04 Spectrasonics Imaging, Inc. Apparatus and method for ablating cardiac tissue
US6716851B2 (en) 2000-12-12 2004-04-06 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof
DE10061863A1 (de) 2000-12-12 2002-06-13 Basf Ag Verfahren zur Herstellung von Triethylendiamin (TEDA)
WO2002047690A1 (en) 2000-12-12 2002-06-20 Cytovia, Inc. Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof
CA2432222C (en) * 2000-12-21 2008-07-29 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
MY130778A (en) * 2001-02-09 2007-07-31 Vertex Pharma Heterocyclic inhibitiors of erk2 and uses thereof
US6759983B2 (en) * 2001-03-28 2004-07-06 Strategic Analysis, Inc. Method and device for precise geolocation of low-power, broadband, amplitude-modulated signals
DE60223790D1 (de) * 2001-03-29 2008-01-10 Vertex Pharma Hemmer von c-jun-terminal kinase (jnk) und andere protein kinase
AU2002338642A1 (en) * 2001-04-13 2002-10-28 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
US20030096813A1 (en) * 2001-04-20 2003-05-22 Jingrong Cao Compositions useful as inhibitors of GSK-3
WO2002092573A2 (en) 2001-05-16 2002-11-21 Vertex Pharmaceuticals Incorporated Heterocyclic substituted pyrazoles as inhibitors of src and other protein kinases
CA2450769A1 (en) * 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors
JP4342937B2 (ja) 2001-07-03 2009-10-14 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 ＳｒｃおよびＬｃｋタンパク質キナーゼの阻害剤としてのイソキサゾールピリミジン
US6698980B2 (en) 2001-07-30 2004-03-02 Stewart Mining Products Inc. Rock stabilizing apparatus and method
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
US6569499B2 (en) * 2001-10-02 2003-05-27 Xerox Corporation Apparatus and method for coating photoreceptor substrates
MXPA04005510A (es) 2001-12-07 2006-02-24 Vertex Pharma Compuestos basados en pirimidina utiles como inhibidores de gsk-3.
US7863282B2 (en) 2003-03-14 2011-01-04 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
EP1485376B1 (en) * 2002-03-15 2007-06-27 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
WO2003077921A1 (en) 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
US7179826B2 (en) * 2002-03-15 2007-02-20 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
US20040009981A1 (en) * 2002-03-15 2004-01-15 David Bebbington Compositions useful as inhibitors of protein kinases
US20030207873A1 (en) * 2002-04-10 2003-11-06 Edmund Harrington Inhibitors of Src and other protein kinases
AU2003237121A1 (en) 2002-04-26 2003-11-10 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
MY141867A (en) * 2002-06-20 2010-07-16 Vertex Pharma Substituted pyrimidines useful as protein kinase inhibitors
CA2491895C (en) * 2002-07-09 2011-01-18 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
CN101037438A (zh) 2002-08-02 2007-09-19 沃泰克斯药物股份有限公司 用作gsk－3的抑制剂的吡唑组合物
AU2003286711A1 (en) 2002-10-25 2004-05-13 Vertex Pharmaceuticals Incorporated Indazolinone compositions useful as kinase inhibitors
JP2004224944A (ja) * 2003-01-24 2004-08-12 Kuraray Plast Co Ltd 高周波接着性に優れた熱可塑性樹脂組成物
JP2007510626A (ja) 2003-10-17 2007-04-26 アストラゼネカ アクチボラグ 癌の治療に使用の４−（ピラゾール−３−イルアミノ）ピリミジン誘導体
MY141220A (en) * 2003-11-17 2010-03-31 Astrazeneca Ab Pyrazole derivatives as inhibitors of receptor tyrosine kinases
GB0402653D0 (en) * 2004-02-06 2004-03-10 Cyclacel Ltd Compounds
ZA200801172B (en) 2005-07-28 2009-04-29 Vertex Pharma Caspase inhibitor prodrugs
EP1917259B1 (en) 2005-08-18 2012-01-25 Vertex Pharmaceuticals Incorporated Pyrazine kinase inhibitors
WO2007023382A2 (en) 2005-08-25 2007-03-01 Pfizer Inc. Pyrimidine amino pyrazole compounds, potent kinase inhibitors
NZ567241A (en) * 2005-09-30 2010-08-27 Miikana Therapeutics Inc Substituted pyrazole compounds
SG166827A1 (en) * 2005-11-03 2010-12-29 Vertex Pharma Aminopyrimidines useful as kinase inhibitors
CN101360740A (zh) 2005-11-16 2009-02-04 沃泰克斯药物股份有限公司 可用作激酶抑制剂的氨基嘧啶
MX2009004807A (es) 2006-11-02 2009-06-15 Vertex Pharma Aminopiridinas y aminopirimidinas utiles como inhibidores de proteina cinasa.
DE602007007985D1 (de) 2006-12-19 2010-09-02 Vertex Pharma Als inhibitoren von proteinkinasen geeignete aminopyrimidine
MX2009007006A (es) * 2006-12-29 2009-07-09 Tibotec Pharm Ltd Pirimidinas 5,6-sustituidas inhibidoras del virus de inmunodeficiencia humana.
CN101663295B (zh) 2007-03-09 2014-11-05 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的氨基嘧啶类化合物
MX2009009591A (es) 2007-03-09 2009-11-10 Vertex Pharma Aminopirimidinas utiles como inhibidores de proteinas cinasas.
MX2009009592A (es) 2007-03-09 2009-11-10 Vertex Pharma Aminopiridinas utiles como inhibidores de proteinas cinasas.
CN101675041A (zh) 2007-03-20 2010-03-17 沃泰克斯药物股份有限公司 用作激酶抑制剂的氨基嘧啶类化合物
EP2148931A2 (en) 2007-04-17 2010-02-03 Vertex Pharmaceuticals Incorporated Drug discovery methods for aurora kinase inhibitors
MX2009011811A (es) 2007-05-02 2010-01-14 Vertex Pharma Aminopirimidinas utiles como inhibidores de cinasa.
EP2152694A2 (en) 2007-05-02 2010-02-17 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
WO2008137621A1 (en) 2007-05-02 2008-11-13 Vertex Pharmaceuticals Incorporated Aminopyrimidines useful as kinase inhibitors
AU2008257044A1 (en) 2007-05-24 2008-12-04 Vertex Pharmaceuticals Incorporated Thiazoles and pyrazoles useful as kinase inhibitors
HRP20151137T1 (hr) 2009-03-20 2015-11-20 Vertex Pharmaceuticals Incorporated Postupak za dobivanje modulatora transmembranskog regulatora vodljivosti cistiäśne fibroze

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