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EP1381598A4 - NEW INHIBITORS OF TYROSINE KINASE - Google Patents

NEW INHIBITORS OF TYROSINE KINASE

Info

Publication number
EP1381598A4
EP1381598A4 EP02723631A EP02723631A EP1381598A4 EP 1381598 A4 EP1381598 A4 EP 1381598A4 EP 02723631 A EP02723631 A EP 02723631A EP 02723631 A EP02723631 A EP 02723631A EP 1381598 A4 EP1381598 A4 EP 1381598A4
Authority
EP
European Patent Office
Prior art keywords
tyrosine kinase
kinase inhibitors
novel tyrosine
novel
inhibitors
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP02723631A
Other languages
German (de)
English (en)
French (fr)
Other versions
EP1381598A1 (en
Inventor
Mark D Wittman
Neelakantan Balasubramanian
Upender Velaparthi
Kurt Zimmermann
Mark G Saulnier
Peiying Liu
Xiaopeng Sang
David B Frennesson
Karen M Stoffan
James G Tarrant
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of EP1381598A1 publication Critical patent/EP1381598A1/en
Publication of EP1381598A4 publication Critical patent/EP1381598A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D233/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/081,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
EP02723631A 2001-03-28 2002-03-26 NEW INHIBITORS OF TYROSINE KINASE Withdrawn EP1381598A4 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US27932701P 2001-03-28 2001-03-28
US279327P 2001-03-28
PCT/US2002/009402 WO2002079192A1 (en) 2001-03-28 2002-03-26 Novel tyrosine kinase inhibitors

Publications (2)

Publication Number Publication Date
EP1381598A1 EP1381598A1 (en) 2004-01-21
EP1381598A4 true EP1381598A4 (en) 2008-03-19

Family

ID=23068491

Family Applications (1)

Application Number Title Priority Date Filing Date
EP02723631A Withdrawn EP1381598A4 (en) 2001-03-28 2002-03-26 NEW INHIBITORS OF TYROSINE KINASE

Country Status (25)

Country Link
EP (1) EP1381598A4 (ru)
JP (1) JP2004534010A (ru)
KR (1) KR20030083016A (ru)
CN (1) CN1514833A (ru)
AR (1) AR035804A1 (ru)
BG (1) BG108206A (ru)
BR (1) BR0208373A (ru)
CA (1) CA2442428A1 (ru)
CZ (1) CZ20032615A3 (ru)
EE (1) EE200300475A (ru)
GE (1) GEP20053660B (ru)
HR (1) HRP20030844A2 (ru)
HU (1) HUP0400323A2 (ru)
IL (1) IL158041A0 (ru)
IS (1) IS6968A (ru)
MX (1) MXPA03008690A (ru)
NO (1) NO20034308L (ru)
PE (1) PE20021015A1 (ru)
PL (1) PL373300A1 (ru)
RU (1) RU2003131693A (ru)
SK (1) SK12002003A3 (ru)
UY (1) UY27234A1 (ru)
WO (1) WO2002079192A1 (ru)
YU (1) YU84603A (ru)
ZA (1) ZA200307466B (ru)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7081454B2 (en) * 2001-03-28 2006-07-25 Bristol-Myers Squibb Co. Tyrosine kinase inhibitors
US7265260B2 (en) 2002-03-01 2007-09-04 Bristol-Myers Squibb Company Transgenic non-human mammals expressing constitutively activated tyrosine kinase receptors
US6921821B2 (en) * 2002-06-12 2005-07-26 Abbott Laboratories Antagonists of melanin concentrating hormone receptor
WO2004050033A2 (en) * 2002-12-02 2004-06-17 Arqule, Inc. Method of treating cancers
EP1581539A4 (en) * 2003-01-03 2007-09-19 Bristol Myers Squibb Co NEW TYROSINE KINASE HEMMER
EP1590339A4 (en) * 2003-01-28 2007-07-25 Smithkline Beecham Corp CHEMICAL COMPOUNDS
US7312215B2 (en) 2003-07-29 2007-12-25 Bristol-Myers Squibb Company Benzimidazole C-2 heterocycles as kinase inhibitors
WO2005020921A2 (en) 2003-08-29 2005-03-10 Exelixis, Inc. C-kit modulators and methods of use
US20050075358A1 (en) * 2003-10-06 2005-04-07 Carboni Joan M. Methods for treating IGF1R-inhibitor induced hyperglycemia
DE102004010207A1 (de) 2004-03-02 2005-09-15 Aventis Pharma S.A. Neue 4-Benzimidazol-2-yl-pyridazin-3-on-Derivate
MY143225A (en) 2004-04-02 2011-03-31 Osi Pharm Inc 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors
AU2005316540A1 (en) * 2004-12-16 2006-06-22 Vertex Pharmaceuticals Incorporated Pyrid-2-ones useful as inhibitors of Tec family protein kinases for the treatment of inflammatory, proliferative and immunologically-mediated diseases
US7393667B2 (en) 2005-05-31 2008-07-01 Bristol-Myers Squibb Company Stereoselective reduction process for the preparation of pyrrolotriazine compounds
US8093401B2 (en) 2005-08-04 2012-01-10 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
US8088928B2 (en) 2005-08-04 2012-01-03 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
PL1910384T3 (pl) 2005-08-04 2013-03-29 Sirtris Pharmaceuticals Inc Pochodne imidazo[2,1-b]tiazolu jako związki modulujące sirtuinę
US7855289B2 (en) 2005-08-04 2010-12-21 Sirtris Pharmaceuticals, Inc. Sirtuin modulating compounds
WO2007027729A1 (en) 2005-08-29 2007-03-08 Vertex Pharmaceuticals Incorporated 3, 5-disubstituted pyrid-2-ones useful as inhibitors of tec family of non-receptor tyrosine kinases
JP5112317B2 (ja) * 2005-08-29 2013-01-09 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 非受容体型チロシンキナーゼのtecファミリーの阻害剤として有用な3,5−二置換ピリド−2−オン
US7691885B2 (en) 2005-08-29 2010-04-06 Vertex Pharmaceuticals Incorporated Pyridones useful as inhibitors of kinases
WO2007026720A1 (ja) * 2005-08-31 2007-03-08 Taisho Pharmaceutical Co., Ltd. 縮環ピラゾール誘導体
US8575164B2 (en) 2005-12-19 2013-11-05 OSI Pharmaceuticals, LLC Combination cancer therapy
WO2007145203A1 (ja) * 2006-06-13 2007-12-21 Daiichi Fine Chemical Co., Ltd. 光学活性2-アミノ-1-(4-フルオロフェニル)エタノール
US8063225B2 (en) 2006-08-14 2011-11-22 Chembridge Corporation Tricyclic compound derivatives useful in the treatment of neoplastic diseases, inflammatory disorders and immunomodulatory disorders
WO2008022747A1 (en) * 2006-08-21 2008-02-28 F. Hoffmann-La Roche Ag Tricyclic lactam derivatives, their manufacture and use as pharmaceutical agents
WO2008025526A1 (en) * 2006-08-31 2008-03-06 F. Hoffmann-La Roche Ag Indole derivatives, their manufacture and use as pharmaceutical agents
EP2559771A3 (en) 2007-05-17 2013-06-12 Bristol-Myers Squibb Company Biomarkers and methods for determining sensitivity to insulin growth factor-1 receptor modulators
CL2008001822A1 (es) 2007-06-20 2009-03-13 Sirtris Pharmaceuticals Inc Compuestos derivados de tiazolo[5,4-b]piridina; composicion farmaceutica que comprende a dichos compuestos; y uso del compuesto en el tratamiento de la resistencia a la insulina, sindrome metabolico, diabetes, entre otras.
WO2009000489A1 (en) * 2007-06-25 2008-12-31 F. Hoffmann-La Roche Ag Benzimidazole amido derivatives as kinase inhibitors
EP2065380A1 (en) * 2007-08-22 2009-06-03 F.Hoffmann-La Roche Ag Pyridoneamide derivatives as focal adhesion kinase (FAK) inhibitors and their use for the treatment of cancer
US7816540B2 (en) * 2007-12-21 2010-10-19 Hoffmann-La Roche Inc. Carboxyl- or hydroxyl-substituted benzimidazole derivatives
PL2294065T3 (pl) * 2008-01-22 2014-11-28 Vernalis R&D Ltd Pochodne indolilo-pirydonu wykazujące działanie hamujące aktywność kinazy 1 punktu kontrolnego
EP2283020B8 (en) 2008-05-19 2012-12-12 OSI Pharmaceuticals, LLC Substituted imidazopyr-and imidazotri-azines
MY160006A (en) 2008-12-19 2017-02-15 Sirtris Pharmaceuticals Inc Thiazolopyridine sirtuin modulating compounds
DE102010001064A1 (de) * 2009-03-18 2010-09-23 Bayer Schering Pharma Aktiengesellschaft Substituierte 2-Acetamido-5-Aryl-1,2,4-triazolone und deren Verwendung
JP2012524119A (ja) 2009-04-20 2012-10-11 オーエスアイ・ファーマシューティカルズ,エルエルシー C−ピラジン−メチルアミンの調製
ES2453097T3 (es) * 2009-05-27 2014-04-04 Abbvie Inc. Inhibidores de pirimidina de actividad quinasa
EP2494070A2 (en) 2009-10-30 2012-09-05 Bristol-Myers Squibb Company Methods for treating cancer in patients having igf-1r inhibitor resistance
PL2624696T3 (pl) * 2010-10-06 2017-07-31 Glaxosmithkline Llc Pochodne benzimidazolu jako inhibitory kinazy PI3
US8772304B2 (en) * 2010-11-01 2014-07-08 Boehringer Ingelheim International Gmbh Benzimidazole inhibitors of leukotriene production
US20140309229A1 (en) 2011-10-13 2014-10-16 Bristol-Myers Squibb Company Methods for selecting and treating cancer in patients with igf-1r/ir inhibitors
JP6461118B2 (ja) * 2013-06-21 2019-01-30 ゼニス・エピジェネティクス・リミテッドZenith Epigenetics Ltd. ブロモドメイン阻害剤としての新規の置換された二環式化合物
ES2806135T3 (es) 2013-06-21 2021-02-16 Zenith Epigenetics Ltd Nuevos inhibidores de bromodominios bicíclicos
US9855271B2 (en) 2013-07-31 2018-01-02 Zenith Epigenetics Ltd. Quinazolinones as bromodomain inhibitors
CN103936719A (zh) * 2014-05-14 2014-07-23 中国药科大学 苯并咪唑类衍生物制备方法及用途
CN108064274A (zh) 2014-07-30 2018-05-22 耶达研究及发展有限公司 用于培养多能干细胞的培养基
US10710992B2 (en) 2014-12-01 2020-07-14 Zenith Epigenetics Ltd. Substituted pyridinones as bromodomain inhibitors
WO2016092375A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Corp. Substituted heterocycles as bromodomain inhibitors
CN107406438B (zh) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
EP3283475B1 (en) * 2015-04-16 2019-10-16 Merck Patent GmbH 3-(1h-benzimidazol-2-yl)-1h-pyridin-2-one derivatives
EP3914698A1 (en) 2019-01-23 2021-12-01 Yeda Research and Development Co. Ltd Culture media for pluripotent stem cells
CN117069696B (zh) * 2023-08-17 2024-04-26 中国药科大学 一种双靶点小分子抑制剂及其制备方法和应用

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6162804A (en) * 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
WO2001000610A1 (de) * 1999-06-23 2001-01-04 Aventis Pharma Deutschland Gmbh Substituierte benzimidazole
WO2004031401A2 (en) * 2002-10-02 2004-04-15 Bristol-Myers Squibb Company Novel tyrosine kinases inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6162804A (en) * 1997-09-26 2000-12-19 Merck & Co., Inc. Tyrosine kinase inhibitors
WO2001000610A1 (de) * 1999-06-23 2001-01-04 Aventis Pharma Deutschland Gmbh Substituierte benzimidazole
WO2004031401A2 (en) * 2002-10-02 2004-04-15 Bristol-Myers Squibb Company Novel tyrosine kinases inhibitors

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
KATZ B A ET AL: "A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site", JOURNAL OF MOLECULAR BIOLOGY, LONDON, GB, vol. 307, no. 5, 13 April 2001 (2001-04-13), pages 1451 - 1486, XP004466071, ISSN: 0022-2836 *
See also references of WO02079192A1 *

Also Published As

Publication number Publication date
CN1514833A (zh) 2004-07-21
HUP0400323A2 (hu) 2005-11-28
CA2442428A1 (en) 2002-10-10
JP2004534010A (ja) 2004-11-11
BG108206A (bg) 2004-11-30
NO20034308D0 (no) 2003-09-26
SK12002003A3 (en) 2004-10-05
GEP20053660B (en) 2005-11-10
HRP20030844A2 (en) 2005-08-31
CZ20032615A3 (en) 2004-03-17
PL373300A1 (en) 2005-08-22
IL158041A0 (en) 2004-03-28
EP1381598A1 (en) 2004-01-21
MXPA03008690A (es) 2003-12-12
ZA200307466B (en) 2005-01-13
KR20030083016A (ko) 2003-10-23
AR035804A1 (es) 2004-07-14
PE20021015A1 (es) 2002-11-10
EE200300475A (et) 2004-02-16
WO2002079192A1 (en) 2002-10-10
RU2003131693A (ru) 2005-05-10
YU84603A (sh) 2006-03-03
BR0208373A (pt) 2005-02-22
NO20034308L (no) 2003-11-26
IS6968A (is) 2003-09-26
UY27234A1 (es) 2002-10-31

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