ATE511503T1 - Aryl- und heteroarylharnstoff-chk1-inhibitoren zur verwendung als radiosensibilisatoren und chemosensibilisatoren - Google Patents

Aryl- und heteroarylharnstoff-chk1-inhibitoren zur verwendung als radiosensibilisatoren und chemosensibilisatoren

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Publication number
ATE511503T1
ATE511503T1 AT02728396T AT02728396T ATE511503T1 AT E511503 T1 ATE511503 T1 AT E511503T1 AT 02728396 T AT02728396 T AT 02728396T AT 02728396 T AT02728396 T AT 02728396T AT E511503 T1 ATE511503 T1 AT E511503T1
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Austria
Prior art keywords
aryl
chemosensitizers
radiosensitizers
chk1 inhibitors
heteroaryl
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AT02728396T
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English (en)
Inventor
Kathleen Keegan
Edward Kesicki
John Gaudino
Adam Wade Cook
Scott Cowen
Laurence Burgess
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Icos Corp
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Publication of ATE511503T1 publication Critical patent/ATE511503T1/de

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    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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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
    • A61K31/4965Non-condensed pyrazines
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Families Citing this family (116)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
ATE538794T1 (de) 1999-01-13 2012-01-15 Bayer Healthcare Llc Gamma carboxyarylsubstituierte diphenylharnstoffverbindungen als p38 kinasehemmer
UA76977C2 (en) * 2001-03-02 2006-10-16 Icos Corp Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers
US7838541B2 (en) 2002-02-11 2010-11-23 Bayer Healthcare, Llc Aryl ureas with angiogenesis inhibiting activity
US20060235035A1 (en) * 2002-04-09 2006-10-19 7Tm Pharma A/S Novel methoxybenzamibe compounds for use in mch receptor related disorders
US7202244B2 (en) 2002-05-29 2007-04-10 Millennium Pharmaceuticals, Inc. Chk-1 inhibitors
AU2003243921B2 (en) 2002-06-27 2009-05-07 Novo Nordisk A/S Aryl carbonyl derivatives as therapeutic agents
KR101124245B1 (ko) 2002-06-27 2012-07-02 노보 노르디스크 에이/에스 치료제로서 아릴 카르보닐 유도체
CA2493458A1 (en) 2002-07-24 2004-01-29 Ptc Therapeutics, Inc. Ureido substituted benzoic acid compounds, their use for nonsense suppression and the treatment of diseases caused by such mutations
US20040034038A1 (en) * 2002-08-13 2004-02-19 Goaquan Li Urea kinase inhibitors
US7056925B2 (en) * 2002-08-13 2006-06-06 Abbott Laboratories Urea kinase inhibitors
WO2004048319A1 (en) * 2002-11-25 2004-06-10 7Tm Pharma A/S Novel benzamide compounds for use in mch receptor related disorders
DK1585749T3 (da) 2003-01-09 2008-09-22 Pfizer Diazepinoindol-derivater som kinaseinhibitorer
NZ589793A (en) * 2003-02-21 2011-12-22 Resmed Ltd Nozzle configuration of nasal cushion for respiratory assistance mask
UY28213A1 (es) 2003-02-28 2004-09-30 Bayer Pharmaceuticals Corp Nuevos derivados de cianopiridina útiles en el tratamiento de cáncer y otros trastornos.
US7320986B2 (en) 2003-03-07 2008-01-22 Abbott Labortories Fused tri and tetra-cyclic pyrazole kinase inhibitors
GB2400101A (en) * 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
WO2004113274A2 (en) 2003-05-20 2004-12-29 Bayer Pharmaceuticals Corporation Diaryl ureas with kinase inhibiting activity
US7297709B2 (en) 2003-05-22 2007-11-20 Abbott Laboratories Indazole, benzisoxazole, and benzisothiazole kinase inhibitors
WO2005028474A2 (en) * 2003-05-29 2005-03-31 Millennium Pharmaceuticals, Inc. Pyrazoloquinoline derivatives as chk-1 inhibitors
RS52625B (sr) 2003-07-23 2013-06-28 Bayer Healthcare Llc Fluoro supstituisana omega-karboksiaril difenil urea za lečenje i prevenciju bolesti i stanja bolesti
EP1660474B1 (de) * 2003-08-15 2008-10-29 AstraZeneca AB Substituierte thiophene und deren verwendungen
US7338957B2 (en) * 2003-08-28 2008-03-04 Irm Llc Compounds and compositions as protein kinase inhibitors
EP1660504B1 (de) 2003-08-29 2008-10-29 Pfizer Inc. Als neue antiangiogene mittel geeignete thienopyridinphenylacetamide und derivate davon
CA2539320A1 (en) * 2003-09-17 2005-03-31 Icos Corporation Use of chk1 inhibitors to control cell proliferation
WO2005046683A1 (en) 2003-10-07 2005-05-26 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
US7163939B2 (en) * 2003-11-05 2007-01-16 Abbott Laboratories Macrocyclic kinase inhibitors
US20050096324A1 (en) * 2003-11-05 2005-05-05 Zhi-Fu Tao Macrocyclic kinase inhibitors
WO2005066145A1 (en) 2004-01-06 2005-07-21 Novo Nordisk A/S Heteroaryl-ureas and their use as glucokinase activators
WO2005072733A1 (en) * 2004-01-20 2005-08-11 Millennium Pharmaceuticals, Inc. Dyarylurea compounds as chk-1 inhibitors
ES2551293T3 (es) 2004-03-24 2015-11-17 Abbvie Inc. Inhibidores de quinasas de pirazol tricíclicos
US7625949B2 (en) 2004-04-23 2009-12-01 Roche Palo Alto Llc Methods for treating retroviral infections
US7166738B2 (en) 2004-04-23 2007-01-23 Roche Palo Alto Llc Non-nucleoside reverse transcriptase inhibitors
US20050276765A1 (en) * 2004-06-10 2005-12-15 Paul Nghiem Preventing skin damage
GB0512324D0 (en) * 2005-06-16 2005-07-27 Novartis Ag Organic compounds
BRPI0512593A (pt) * 2004-06-25 2008-03-25 Icos Corp composto ou um sal ou pró-droga ou solvato farmaceuticamente aceitável do mesmo, composição, e, métodos de inibir a quinase 1 de ponto de verificação em uma célula, de sensibilizar células em um indivìduo e de inibir a proliferação de célula aberrante
CN101010316A (zh) 2004-07-02 2007-08-01 艾科斯有限公司 用于抑制chk1的化合物
CN101115727A (zh) * 2004-08-19 2008-01-30 艾科斯有限公司 用于抑制chk1的化合物
DE102004055582A1 (de) 2004-11-18 2006-05-24 Bayer Cropscience Ag N-Heterocyclyl-phthalsäurediamide
CA2589271A1 (en) * 2004-12-07 2006-06-15 Locus Pharmaceuticals, Inc. Urea inhibitors of map kinases
EP1824843A2 (de) * 2004-12-07 2007-08-29 Locus Pharmaceuticals, Inc. Inhibitoren von proteinkinasen
US7576099B2 (en) 2005-02-28 2009-08-18 Renovis, Inc. Amide derivatives as ion-channel ligands and pharmaceutical compositions and methods of using the same
WO2006105262A1 (en) * 2005-03-29 2006-10-05 Icos Corporation HETEROARYL UREA DERIVATIVES USEFUL FOR INHIBITING CHKl
BRPI0617720A2 (pt) 2005-10-19 2011-08-02 Hoffmann La Roche compostos inibidores de nnrt de fenil-acetamida, usos dos referidos compostos e composição farmacêutica que os contém
US8014957B2 (en) 2005-12-15 2011-09-06 Fred Hutchinson Cancer Research Center Genes associated with progression and response in chronic myeloid leukemia and uses thereof
MEP3808A (xx) 2005-12-21 2010-02-10 Novartis Ag Derivati pirimidinil aril uree kao fgf inhibitori
JP2009522363A (ja) * 2006-01-04 2009-06-11 ローカス ファーマシューティカルズ、インク. プロテインキナーゼの阻害剤
JP2009541323A (ja) * 2006-06-22 2009-11-26 マリンクロット インコーポレイテッド 拡張された共役を有するピラジン誘導体およびその使用
EP1882475A1 (de) * 2006-07-26 2008-01-30 Novartis AG Methoden zur Behandlung von Erkrankungen, die durch den Fibroblastwachstumsfaktorrezeptor vermittelt werden
US9056136B2 (en) * 2006-10-06 2015-06-16 Natural Pharmacia International, Inc. Weakly basic 2-nitroimidazoles for the non-invasive detection of tissue hypoxia
UA95310C2 (ru) 2006-10-20 2011-07-25 Айкос Корпорейшен Композиция, содержащая ингибитор chk1 и циклодекстрин, для лечения рака
EP2086644A2 (de) * 2006-11-17 2009-08-12 Schering Corporation Kombination aus einem hemmer der dna-polymerase-alpha und einem hemmer der checkpointkinase zur behandlung von proliferativen erkrankungen
EP2409700A1 (de) 2007-05-08 2012-01-25 Schering Corporation Verfahren zur Behandlung mit intravenösen Formulierungen mit Temozolomid
EP2247953A2 (de) * 2008-02-04 2010-11-10 Dana-farber Cancer Institute, Inc. Chk1 unterdrückt eine apoptotische caspase-2-reaktion auf p53, bcl-2 und caspase-3 umgehende dna-schädigung
ES2378513T3 (es) 2008-08-06 2012-04-13 Pfizer Inc. Compuestos 2-heterociclilamino piracinas sustituidas en posición 6 como inhibidores de CHK-1
US8314108B2 (en) 2008-12-17 2012-11-20 Eli Lilly And Company 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2-carbonitrile, pharmaceutically acceptable salts thereof, or solvate of salts
EP2241557A1 (de) * 2009-04-02 2010-10-20 Æterna Zentaris GmbH Chinoxalin-Derivate und deren Anwendung zur Behandlung gutartiger und bösartiger Tumorerkrankungen
CN101857575A (zh) * 2009-04-07 2010-10-13 上海合全药业有限公司 2-氨基-5-甲基吡嗪的工业化制备方法
CN101560175B (zh) * 2009-05-08 2012-10-10 南京大学 一类硫脲类衍生物及其制备方法与用途
EP2448938B9 (de) 2009-06-29 2015-06-10 Incyte Corporation Pyrimidinone als pi3k-hemmer
EP2305643A1 (de) * 2009-10-02 2011-04-06 Ikerchem, S.L. Neue Histondeacetylase-Inhibitoren, die zugleich auf trisubstituierten 1H-Pyrrolen und aromatischen und heteroaromatischen Spacern basieren
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
AR079529A1 (es) * 2009-12-18 2012-02-01 Incyte Corp Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k
EP2558463A1 (de) 2010-04-14 2013-02-20 Incyte Corporation Kondensierte derivate als i3-hemmer
JP5585822B2 (ja) * 2010-05-11 2014-09-10 東レ・ファインケミカル株式会社 光学活性ニペコチン酸誘導体の製造方法
GB201008005D0 (en) 2010-05-13 2010-06-30 Sentinel Oncology Ltd Pharmaceutical compounds
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
US8716246B2 (en) 2011-01-03 2014-05-06 The Regents Of The University Of California Azuvirin peptides
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
KR102030609B1 (ko) 2011-09-02 2019-10-11 인사이트 홀딩스 코포레이션 Pi3k 억제제로서 헤테로시클릴아민
GB201119799D0 (en) 2011-11-16 2011-12-28 Sentinel Oncology Ltd Pharmaceutical compounds
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
CA2938626A1 (en) 2013-07-26 2015-01-29 John Rothman Compositions to improve the therapeutic benefit of bisantrene
GB201402277D0 (en) 2014-02-10 2014-03-26 Sentinel Oncology Ltd Pharmaceutical compounds
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
DK3831833T3 (da) 2015-02-27 2022-11-14 Incyte Holdings Corp Fremgangsmåder til fremstillingen af en pi3k-inhibitor
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
KR102768838B1 (ko) 2015-09-17 2025-02-14 시티 오브 호프 Pcna 억제제
DK3411036T3 (da) 2016-02-04 2022-01-17 Pharmaengine Inc 3,5-disubstituerede pyrazoler, der er nyttige som checkpoint-kinase 1 (chk1)-hæmmere, samt fremstilling og anvendelse deraf
CN106632093A (zh) * 2016-11-23 2017-05-10 山东友帮生化科技有限公司 一种2‑溴‑5,6‑二苯基吡嗪的制备方法
AU2018243667A1 (en) 2017-03-31 2019-10-17 Seagen Inc. Combinations of Chk1- and Wee1 - inhibitors
EP3461480A1 (de) 2017-09-27 2019-04-03 Onxeo Kombination von checkpoint-hemmern des dna-schädigungsantwort-zellzyklus und belinostat zur behandlung von krebs
CN119258070A (zh) 2018-06-01 2025-01-07 因赛特公司 治疗pi3k相关病症的给药方案
KR20210020866A (ko) 2018-06-12 2021-02-24 브이티브이 테라퓨틱스 엘엘씨 인슐린 또는 인슐린 유사체와 조합된 글루코키나제 활성제의 치료적 용도
EP3818044A1 (de) * 2018-07-03 2021-05-12 IFM Due, Inc. Verbindungen und zusammensetzungen zur behandlung von erkrankungen in zusammenhang mit sting-aktivität
GB201813060D0 (en) * 2018-08-10 2018-09-26 Artios Pharma Ltd Novel compounds
CN111377874A (zh) * 2018-12-28 2020-07-07 南京艾德凯腾生物医药有限责任公司 一种制备赛乐西帕中间体的方法
EP3904352A4 (de) * 2018-12-28 2022-09-07 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Substituierte arylverbindung sowie herstellungsverfahren dafür und verwendung davon
CN111377873B (zh) * 2018-12-28 2023-03-28 四川科伦博泰生物医药股份有限公司 氨基嘧啶化合物及其制备方法和用途
CN112457306A (zh) 2019-09-06 2021-03-09 上海瑛派药业有限公司 3,5-二取代吡唑化合物作为激酶抑制剂及其应用
ES3014705T3 (en) 2019-11-29 2025-04-24 Novaonco Js Therapeutics Co Ltd Diazaindole derivative and use thereof as chk1 inhibitor
WO2021119236A1 (en) 2019-12-10 2021-06-17 Seagen Inc. Preparation of a chk1 inhibitor compound
WO2021167840A1 (en) 2020-02-18 2021-08-26 Vtv Therapeutics Llc Sulfoxide and sulfone glucokinase activators and methods of use thereof
EP4161640A4 (de) 2020-06-08 2024-01-17 vTv Therapeutics LLC Salze oder cokristalle von {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido)-thiazol-5-ylsulfanyl}-essigsäure und verwendungen davon
GB202107924D0 (en) 2021-06-03 2021-07-21 Sentinel Oncology Ltd A pharmaceutical salt
GB202107932D0 (en) 2021-06-03 2021-07-21 Sentinel Oncology Ltd Preparation of a CHK1 Inhibitor Compound
CN115353512B (zh) * 2021-07-30 2025-07-08 上海翊石医药科技有限公司 一种杂环脲类化合物及其制备方法和用途
CN113717115A (zh) * 2021-08-27 2021-11-30 湖北石河医药科技有限公司 一种赛乐西帕中间体的制备方法及其在制备赛乐西帕中的应用
KR20240158305A (ko) * 2022-03-07 2024-11-04 시티 오브 호프 Pcna 억제제 및 이의 용도
WO2024229406A1 (en) 2023-05-04 2024-11-07 Revolution Medicines, Inc. Combination therapy for a ras related disease or disorder
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
TW202530228A (zh) 2023-10-12 2025-08-01 美商銳新醫藥公司 Ras抑制劑
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025217307A1 (en) 2024-04-09 2025-10-16 Revolution Medicines, Inc. Methods for predicting response to a ras(on) inhibitor and combination therapies
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ras抑制劑
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2762743A (en) * 1953-03-11 1956-09-11 Merck & Co Inc 1-phenyl-3(3-as-triazinyl) urea compositions for the treatment of coccidiosis and method for preparing the same
US4609659A (en) * 1985-01-16 1986-09-02 Merck & Co., Inc. 2,6-disubstituted derivatives of 3-nitropyrazines useful as adjuncts to radiation therapy
US5215738A (en) * 1985-05-03 1993-06-01 Sri International Benzamide and nicotinamide radiosensitizers
US5041653A (en) * 1985-05-03 1991-08-20 Sri International Substituted benzamide radiosensitizers
SU1624949A1 (ru) 1987-12-15 1996-02-27 И.И. Красильников м,N-БУТИРИЛАМИНОБЕНЗАМИД, ОБЛАДАЮЩИЙ РАДИОСЕНСИБИЛИЗИРУЮЩЕЙ АКТИВНОСТЬЮ
SU1621447A1 (ru) 1989-06-29 1996-02-27 О.В. Арапов м,-(N-ТРИФТОРАЦЕТИЛАМИНО)БЕНЗАМИД, ОБЛАДАЮЩИЙ РАДИОСЕНСИБИЛИЗИРУЮЩЕЙ АКТИВНОСТЬЮ
US5212738A (en) * 1991-04-12 1993-05-18 Martin Marietta Magnesia Specialties Inc. Scanning laser measurement system
HU221816B1 (hu) 1991-10-11 2003-01-28 Bristol-Myers Squibb Pharma Company Gyűrűs karbonil vegyületek, és ezeket tartalmazó gyógyászati készítmények
WO1994026715A1 (en) * 1993-05-11 1994-11-24 Smithkline Beecham Plc Amidine derivatives as gastric acid secretion inhibitors
US5547966A (en) * 1993-10-07 1996-08-20 Bristol-Myers Squibb Company Aryl urea and related compounds
GB9420999D0 (en) * 1994-10-18 1994-12-07 Smithkline Beecham Plc Novel compounds
US6033582A (en) * 1996-01-22 2000-03-07 Etex Corporation Surface modification of medical implants
US6051218A (en) * 1996-02-02 2000-04-18 The Regents Of The University Of California Tumor radiosensitization using gene therapy
US6093742A (en) * 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
WO1999011621A2 (en) * 1997-09-03 1999-03-11 American Home Products Corporation Thiourea for increasing hdl-cholesterol levels, which are useful as anti-atherosclerotic agents
US6218109B1 (en) * 1997-09-05 2001-04-17 Baylor College Of Medicine Mammalian checkpoint genes and proteins
TR200001645T2 (tr) * 1997-12-11 2000-12-21 Janssen Pharmaceutica N.V. Retinoyik asit taklidi anilürler.
DE69839735D1 (de) 1997-12-15 2008-08-28 Astellas Pharma Inc Pyrimidin-5-carboxamid-derivate
IL136737A0 (en) 1997-12-22 2001-06-14 Bayer Ag Inhibition of p38 kinase using symmetrical and unsymmetrical diphenyl ureas
EP1449834A3 (de) 1997-12-22 2004-12-22 Bayer Corporation Hemmung der RAF-Kinase unter Verwendung von symmetrisch und unsymmetrisch substituierten Harnstoffen
CA2300197A1 (en) * 1997-12-23 1999-07-01 Warner-Lambert Company Thiourea and benzamide compounds, compositions and methods of treating or preventing inflammatory diseases and atherosclerosis
US6383744B1 (en) 1998-07-10 2002-05-07 Incyte Genomics, Inc. Human checkpoint kinase
EP1115707B1 (de) * 1998-09-25 2003-11-12 AstraZeneca AB Benzamid-derivate und ihre verwendung als cytokine inhibitoren
GB9823873D0 (en) * 1998-10-30 1998-12-30 Pharmacia & Upjohn Spa 2-ureido-thiazole derivatives,process for their preparation,and their use as antitumour agents
FR2787322B1 (fr) 1998-12-18 2002-10-18 Galderma Res & Dev Emulsion huile-dans-eau comprenant un agent actif micronise et un systeme emulsionnant approprie
EP1165531A1 (de) * 1999-03-19 2002-01-02 Du Pont Pharmaceuticals Company N-adamant-1-yl-[4-chlorbenzothiazol-2-yl]harnstoff zur verwendung in der behandlung von entzündung und als antikrebs radiosensibilisierendes mittel
UA71971C2 (en) 1999-06-04 2005-01-17 Agoron Pharmaceuticals Inc Diaminothiazoles, composition based thereon, a method for modulation of protein kinases activity, a method for the treatment of diseases mediated by protein kinases
US6958333B1 (en) 1999-07-26 2005-10-25 Banyu Pharmaceutical Co., Ltd. Biarylurea derivatives
US6670167B1 (en) 1999-11-01 2003-12-30 Agouron Pharmaceuticals, Inc. Catalytic domain of the human effector cell cycle checkpoint protein kinase materials and methods for identification of inhibitors thereof
EP1268472B1 (de) 2000-02-07 2004-10-13 Bristol-Myers Squibb Company 3-aminopyrazole als inhibitoren von cyclinabhängigen kinasen
US6211164B1 (en) * 2000-03-10 2001-04-03 Abbott Laboratories Antisense oligonucleotides of the human chk1 gene and uses thereof
UA76977C2 (en) * 2001-03-02 2006-10-16 Icos Corp Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers

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EA014954B1 (ru) 2011-04-29
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PL364564A1 (en) 2004-12-13
SI1379510T1 (sl) 2011-10-28
PL212707B1 (pl) 2012-11-30
RS52077B (sr) 2012-06-30
CA2439709A1 (en) 2002-09-12
EP1379510A1 (de) 2004-01-14
CN100374425C (zh) 2008-03-12
PT1379510E (pt) 2011-07-15
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