AU2002232439A1 - Benzimidazole derivatives useful as tie-2 and/or vegfr-2 inhibitors - Google Patents

Benzimidazole derivatives useful as tie-2 and/or vegfr-2 inhibitors

Info

Publication number
AU2002232439A1
AU2002232439A1 AU2002232439A AU3243902A AU2002232439A1 AU 2002232439 A1 AU2002232439 A1 AU 2002232439A1 AU 2002232439 A AU2002232439 A AU 2002232439A AU 3243902 A AU3243902 A AU 3243902A AU 2002232439 A1 AU2002232439 A1 AU 2002232439A1
Authority
AU
Australia
Prior art keywords
vegfr
tie
inhibitors
benzimidazole derivatives
derivatives useful
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.)
Abandoned
Application number
AU2002232439A
Other languages
English (en)
Inventor
Mui Cheung
Philip Anthony Harris
Masaichi Hasegawa
Satoru Ida
Kazuya Kano
Naohiko Nishigaki
Hideyuki Sato
James Marvin Veal
Yoshiaki Washio
Rob I. West
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.)
Glaxo Group Ltd
Original Assignee
Glaxo Group Ltd
GlaxoSmithKline KK
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 Glaxo Group Ltd, GlaxoSmithKline KK filed Critical Glaxo Group Ltd
Publication of AU2002232439A1 publication Critical patent/AU2002232439A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30Nitrogen atoms not forming part of a nitro radical
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/30Nitrogen atoms not forming part of a nitro radical
    • C07D235/32Benzimidazole-2-carbamic acids, unsubstituted or substituted; Esters thereof; Thio-analogues thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62Benzothiazoles
    • C07D277/68Benzothiazoles 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 in position 2
    • C07D277/82Nitrogen atoms
    • 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
    • C07D401/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero 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
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02Heterocyclic 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 two hetero rings
    • C07D417/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
AU2002232439A 2000-11-29 2001-11-28 Benzimidazole derivatives useful as tie-2 and/or vegfr-2 inhibitors Abandoned AU2002232439A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US25386800P 2000-11-29 2000-11-29
US60/253,868 2000-11-29
US31093901P 2001-08-08 2001-08-08
US60/310,939 2001-08-08
PCT/US2001/044553 WO2002044156A2 (en) 2000-11-29 2001-11-28 Benzimidazole derivatives useful as tie-2 and/or vegfr-2 inhibitors

Publications (1)

Publication Number Publication Date
AU2002232439A1 true AU2002232439A1 (en) 2002-06-11

Family

ID=26943640

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2002232439A Abandoned AU2002232439A1 (en) 2000-11-29 2001-11-28 Benzimidazole derivatives useful as tie-2 and/or vegfr-2 inhibitors

Country Status (5)

Country Link
US (2) US7238813B2 (enExample)
EP (1) EP1341771A2 (enExample)
JP (1) JP2004517080A (enExample)
AU (1) AU2002232439A1 (enExample)
WO (1) WO2002044156A2 (enExample)

Families Citing this family (114)

* 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
EP1158985B1 (en) 1999-01-13 2011-12-28 Bayer HealthCare LLC OMEGA-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS
AU9598601A (en) 2000-10-20 2002-04-29 Eisai Co Ltd Nitrogenous aromatic ring compounds
WO2003047579A1 (en) 2001-12-03 2003-06-12 Bayer Pharmaceuticals Corporation Aryl urea compounds in combination with other cytostatic or cytotoxic agents for treating human cancers
SI1478358T1 (sl) 2002-02-11 2013-09-30 Bayer Healthcare Llc Sorafenib tozilat za zdravljenje bolezni, značilnih po abnormalni angiogenezi
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
WO2003082272A1 (en) 2002-03-29 2003-10-09 Chiron Corporation Substituted benzazoles and use thereof as raf kinase inhibitors
DE60304718T2 (de) 2002-08-06 2007-04-26 Astrazeneca Ab Kondensierte pyridine und pyrimidine mit tie2 (tek) aktivität
US20060004029A1 (en) * 2002-08-30 2006-01-05 Akihiko Tsuruoka Nitrogen-containing aromatic derivatives
US7365209B2 (en) 2003-02-11 2008-04-29 Pharmacopeia, Inc. Nitrogen heterocycle biaryls for osteoporosis and other diseases
US7531553B2 (en) * 2003-03-21 2009-05-12 Amgen Inc. Heterocyclic compounds and methods of use
WO2004085433A2 (en) * 2003-03-28 2004-10-07 Pharmacia & Upjohn Company Llc Positive allosteric modulators of the nicotinic acetylcholine receptor
WO2004087153A2 (en) 2003-03-28 2004-10-14 Chiron Corporation Use of organic compounds for immunopotentiation
EP1636585B2 (en) 2003-05-20 2012-06-13 Bayer HealthCare LLC Diaryl ureas with kinase inhibiting activity
US6887798B2 (en) 2003-05-30 2005-05-03 International Business Machines Corporation STI stress modification by nitrogen plasma treatment for improving performance in small width devices
EP1653951B1 (en) 2003-07-11 2011-12-28 Merck Patent GmbH Benzimidazole derivatives as raf kinase inhibitors
EP1663978B1 (en) 2003-07-23 2007-11-28 Bayer Pharmaceuticals Corporation Fluoro substituted omega-carboxyaryl diphenyl urea for the treatment and prevention of diseases and conditions
DE10334663A1 (de) * 2003-07-30 2005-03-10 Merck Patent Gmbh Harnstoffderivate
DE10337942A1 (de) * 2003-08-18 2005-03-17 Merck Patent Gmbh Aminobenzimidazolderivate
DE10342503A1 (de) 2003-09-12 2005-04-14 Merck Patent Gmbh Benzyl-Benzimidazolylderivate
DE10344223A1 (de) * 2003-09-24 2005-04-21 Merck Patent Gmbh 1,3-Benzoxazolylderivate als Kinase-Inhibitoren
KR20060118472A (ko) 2003-10-16 2006-11-23 카이론 코포레이션 치환 벤자졸 및 raf 키나아제의 저해제로서 그것의 사용
DE10349587A1 (de) * 2003-10-24 2005-05-25 Merck Patent Gmbh Benzimidazolylderivate
US7683172B2 (en) 2003-11-11 2010-03-23 Eisai R&D Management Co., Ltd. Urea derivative and process for preparing the same
EP1684762A4 (en) * 2003-11-13 2009-06-17 Ambit Biosciences Corp UREA DERIVATIVES AS MODULATORS OF KINASE
DE10352979A1 (de) 2003-11-13 2005-06-09 Merck Patent Gmbh Pyridopyrimidinone
TW200530236A (en) 2004-02-23 2005-09-16 Chugai Pharmaceutical Co Ltd Heteroaryl phenylurea
US20070191444A1 (en) * 2004-02-26 2007-08-16 Hans-Peter Buchstaller Benzimidazolyl derivatives
US7459562B2 (en) 2004-04-23 2008-12-02 Bristol-Myers Squibb Company Monocyclic heterocycles as kinase inhibitors
TW200538453A (en) 2004-04-26 2005-12-01 Bristol Myers Squibb Co Bicyclic heterocycles as kinase inhibitors
EP2295426A1 (en) 2004-04-30 2011-03-16 Bayer HealthCare, LLC Substituted pyrazolyl urea derivatives useful in the treatment of cancer
US7432373B2 (en) 2004-06-28 2008-10-07 Bristol-Meyers Squibb Company Processes and intermediates useful for preparing fused heterocyclic kinase inhibitors
US7439246B2 (en) 2004-06-28 2008-10-21 Bristol-Myers Squibb Company Fused heterocyclic kinase inhibitors
US7173031B2 (en) 2004-06-28 2007-02-06 Bristol-Myers Squibb Company Pyrrolotriazine kinase inhibitors
US20090181092A1 (en) * 2004-07-16 2009-07-16 Spinal Restoration, Inc. Methods for Treating Joints and Discs with a Carrier Matrix and Cells
ATE428421T1 (de) 2004-09-17 2009-05-15 Eisai R&D Man Co Ltd Medizinische zusammensetzung mit verbesserter stabilität und reduzierten gelierungseigenschaften
EP1798216A4 (en) * 2004-09-28 2008-12-03 Sankyo Co INTERMEDIATE PRODUCT OF A 6-SUBSTITUTED 1-METHYL-1H-BENZIMIDAZOLE DERIVATIVE AND METHOD FOR THE PRODUCTION THEREOF
JP4789180B2 (ja) * 2004-09-28 2011-10-12 第一三共株式会社 6−置換−1−メチル−1−h−ベンズイミダゾール誘導体の製造方法及びその製造中間体
WO2006040056A1 (en) * 2004-10-13 2006-04-20 Merck Patent Gmbh Heterocyclic substituted bisarylurea derivatives as kinase inhibitors
EP1799679B1 (de) * 2004-10-13 2008-01-23 Merck Patent GmbH Als kinaseinhibitoren geeignete derivate des n,n'-diphenylharnstoffs
GB0423554D0 (en) * 2004-10-22 2004-11-24 Cancer Rec Tech Ltd Therapeutic compounds
DE102004054216A1 (de) 2004-11-10 2006-05-11 Merck Patent Gmbh Substituierte 4-Amino-pyridopyrimidinone
EP1674466A1 (en) * 2004-12-27 2006-06-28 4Sc Ag 2,5- and 2,6-disubstituted benzazole analogues useful as protein kinase inhibitors
US7576090B2 (en) 2004-12-27 2009-08-18 4Sc Ag Benzazole analogues and uses thereof
JP4989476B2 (ja) 2005-08-02 2012-08-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 血管新生阻害物質の効果を検定する方法
US7202513B1 (en) 2005-09-29 2007-04-10 International Business Machines Corporation Stress engineering using dual pad nitride with selective SOI device architecture
US8986650B2 (en) 2005-10-07 2015-03-24 Guerbet Complex folate-NOTA-Ga68
US8926945B2 (en) 2005-10-07 2015-01-06 Guerbet Compounds comprising a biological target recognizing part, coupled to a signal part capable of complexing gallium
CA2649288C (en) 2006-04-19 2015-11-24 Novartis Ag 6-o-substituted benzoxazole and benzothiazole compounds and methods of inhibiting csf-1r signaling
AU2007245495A1 (en) 2006-04-26 2007-11-08 Astex Therapeutics Limited Imidazo[4, 5-b]pyridin-2-one and oxazolo[4, 5-b]pyridin-2-one compounds and analogs thereof as cancer therapeutic compounds
EP2258700A1 (en) 2006-05-09 2010-12-08 Pfizer Products Inc. Cycloalkylamino acid derivatives and pharmaceutical compositions thereof
CN104706637A (zh) 2006-05-18 2015-06-17 卫材R&D管理有限公司 针对甲状腺癌的抗肿瘤剂
WO2008026748A1 (en) 2006-08-28 2008-03-06 Eisai R & D Management Co., Ltd. Antitumor agent for undifferentiated gastric cancer
US20080076770A1 (en) * 2006-09-25 2008-03-27 Arete Therapeutics, Inc. Soluble epoxide hydrolase inhibitors
CN101516838A (zh) * 2006-09-28 2009-08-26 亚瑞特医疗公司 可溶性环氧化物水解酶抑制剂
CA2676796C (en) 2007-01-29 2016-02-23 Eisai R & D Management Co., Ltd. Composition for treatment of undifferentiated gastric cancer
CL2008001626A1 (es) * 2007-06-05 2009-06-05 Takeda Pharmaceuticals Co Compuestos derivados de heterociclos fusionados, agente farmaceutico que los comprende y su uso en la profilaxis y tratamiento del cancer.
US8431608B2 (en) 2007-08-17 2013-04-30 Icagen Inc. Heterocycles as potassium channel modulators
ES2400604T3 (es) * 2007-08-17 2013-04-11 Icagen, Inc. Heterociclos como moduladores del canal de potasio
EP2181987B9 (en) 2007-08-23 2014-09-03 Takeda Pharmaceutical Company Limited 2-Carbonylaminobenzothiazoles and their use for the prophylaxis and treatment of cancer
JP5350247B2 (ja) * 2007-08-29 2013-11-27 武田薬品工業株式会社 複素環化合物およびその用途
US8952035B2 (en) 2007-11-09 2015-02-10 Eisai R&D Management Co., Ltd. Combination of anti-angiogenic substance and anti-tumor platinum complex
NZ586418A (en) 2007-12-19 2012-09-28 Cancer Rec Tech Ltd Pyrido[2,3-b]pyrazine-8-substituted compounds and their use
EP2277881A4 (en) 2008-04-18 2011-09-07 Shionogi & Co HETEROCYCLIC COMPOUND HAVING INHIBITORY ACTIVITY ON P13K
GB0807609D0 (en) * 2008-04-25 2008-06-04 Cancer Rec Tech Ltd Therapeutic compounds and their use
WO2009136663A1 (en) * 2008-05-08 2009-11-12 Takeda Pharmaceutical Company Limited Fused heterocyclic derivatives and use thereof
EP2307456B1 (en) 2008-06-27 2014-10-15 Amgen Inc. Ang-2 inhibition to treat multiple sclerosis
US8697874B2 (en) 2008-12-01 2014-04-15 Takeda Pharmaceutical Company Limited Heterocyclic compound and use thereof
JO3101B1 (ar) * 2008-12-02 2017-09-20 Takeda Pharmaceuticals Co مشتقات بنزوثيازول كعوامل مضادة للسرطان
FR2942227B1 (fr) 2009-02-13 2011-04-15 Guerbet Sa Utilisation de tampons pour la complexation de radionucleides
WO2010126922A1 (en) * 2009-04-30 2010-11-04 Glaxosmithkline Llc Benzimidazolecarboxamides as inhibitors of fak
MY162940A (en) 2009-08-19 2017-07-31 Eisai R&D Man Co Ltd Quinoline derivative-containing pharmaceutical composition
JP5760010B2 (ja) 2010-02-01 2015-08-05 キャンサー・リサーチ・テクノロジー・リミテッド 1−(5−tert−ブチル−2−フェニル−2H−ピラゾール−3−イル)−3−[2−フルオロ−4−(1−メチル−2−オキソ−2,3−ジヒドロ−1H−イミダゾ[4,5−B]ピリジン−7−イルオキシ)−フェニル]−尿素および関連化合物ならびに治療におけるそれらの使用
US8759535B2 (en) 2010-02-18 2014-06-24 High Point Pharmaceuticals, Llc Substituted fused imidazole derivatives, pharmaceutical compositions, and methods of use thereof
DK2536285T3 (en) 2010-02-18 2018-07-16 Vtv Therapeutics Llc Substituted fused imidazole derivatives, pharmaceutical compositions and methods for their use
CN102958523B (zh) 2010-06-25 2014-11-19 卫材R&D管理有限公司 使用具有激酶抑制作用的组合的抗肿瘤剂
CN103270023B (zh) 2010-09-03 2016-11-02 福马Tm有限责任公司 作为用于治疗疾病诸如癌症的nampt 抑制剂的4-{[(吡啶-3-基-甲基)氨基羰基]氨基}苯-砜衍生物
FR2968999B1 (fr) 2010-12-20 2013-01-04 Guerbet Sa Nanoemulsion de chelate pour irm
CN103402519B (zh) 2011-04-18 2015-11-25 卫材R&D管理有限公司 肿瘤治疗剂
JP6038128B2 (ja) 2011-06-03 2016-12-07 エーザイ・アール・アンド・ディー・マネジメント株式会社 レンバチニブ化合物に対する甲状腺癌対象及び腎臓癌対象の反応性を予測及び評価するためのバイオマーカー
FR2980364B1 (fr) 2011-09-26 2018-08-31 Guerbet Nanoemulsions et leur utilisation comme agents de contraste
KR20150098605A (ko) 2012-12-21 2015-08-28 에자이 알앤드디 매니지먼트 가부시키가이샤 퀴놀린 유도체의 비정질 형태 및 그의 제조방법
FR3001154B1 (fr) 2013-01-23 2015-06-26 Guerbet Sa Magneto-emulsion vectorisee
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
NZ714049A (en) 2013-05-14 2020-05-29 Eisai R&D Man Co Ltd Biomarkers for predicting and assessing responsiveness of endometrial cancer subjects to lenvatinib compounds
HK1223307A1 (zh) * 2013-05-30 2017-07-28 Kala Pharmaceuticals, Inc. 新型化合物和其用途
GB201320732D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Methods of chemical synthesis
GB201320729D0 (en) 2013-11-25 2014-01-08 Cancer Rec Tech Ltd Therapeutic compounds and their use
PT3524595T (pt) 2014-08-28 2022-09-19 Eisai R&D Man Co Ltd Derivado de quinolina altamente puro e método para produção do mesmo
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
WO2016089648A1 (en) 2014-12-01 2016-06-09 Vtv Therapeutics Llc Bach 1 inhibitors in combination with nrf2 activators and pharmaceutical compositions thereof
LT3263106T (lt) 2015-02-25 2024-01-10 Eisai R&D Management Co., Ltd. Chinolino darinių kartumo sumažinimo būdas
KR102662228B1 (ko) 2015-03-04 2024-05-02 머크 샤프 앤드 돔 코포레이션 암을 치료하기 위한 pd-1 길항제 및 vegfr/fgfr/ret 티로신 키나제 억제제의 조합
MX373231B (es) 2015-06-16 2020-05-08 Eisai R&D Man Co Ltd Agente anticancerigeno.
US12220398B2 (en) 2015-08-20 2025-02-11 Eisai R&D Management Co., Ltd. Tumor therapeutic agent
EP3383852A4 (en) * 2015-11-30 2019-08-28 Children's Medical Center Corporation COMPOUNDS FOR THE TREATMENT OF PROLIFERATIVE DISEASES
AU2017329090B9 (en) 2016-09-19 2019-09-05 Novartis Ag Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor
US12303505B2 (en) 2017-02-08 2025-05-20 Eisai R&D Management Co., Ltd. Tumor-treating pharmaceutical composition
CA3057969A1 (en) 2017-05-02 2018-11-08 Novartis Ag Combination therapy
RU2019134940A (ru) 2017-05-16 2021-06-16 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Лечение гепатоцеллюлярной карциномы
CN107954939B (zh) * 2017-12-07 2019-09-17 福建医科大学 一种微波辐射下n,n-二甲基氨基硫代甲酰氯衍生物催化合成苯并咪唑衍生物的方法
EP3876939A4 (en) 2018-11-07 2022-08-10 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
US12522583B2 (en) 2018-11-07 2026-01-13 Dana-Farber Cancer Institute, Inc. Benzimidazole derivatives and aza-benzimidazole derivatives as Janus kinase 2 inhibitors and uses thereof
EP3877371A4 (en) 2018-11-07 2022-07-27 Dana-Farber Cancer Institute, Inc. IMIDAZOPYRIDINE DERIVATIVES AND AZA-IMIDAZOPYRIDINE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND USES THEREOF
WO2020201773A1 (en) * 2019-04-05 2020-10-08 Storm Therapeutics Ltd Mettl3 inhibitory compounds
EP3969449B1 (en) 2019-05-13 2025-02-12 Novartis AG New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
US11691963B2 (en) 2020-05-06 2023-07-04 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors
CN116348114B (zh) * 2020-10-19 2025-09-16 高丽大学校产学协力团 硫代苯并咪唑衍生物或其药学上可接受的盐及其用途
US12043632B2 (en) 2020-12-23 2024-07-23 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors
US12162881B2 (en) 2021-11-09 2024-12-10 Ajax Therapeutics, Inc. Forms and compositions of inhibitors of JAK2
WO2023086319A1 (en) 2021-11-09 2023-05-19 Ajax Therapeutics, Inc. 6-he tero aryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
TW202346485A (zh) 2022-03-28 2023-12-01 瑞士商杭斯曼高級材料公司 基於2-羥基萘-3-羧酸的分散偶氮染料
CN115724837B (zh) * 2022-10-26 2024-07-23 中国人民解放军海军军医大学 一种抑制程序性细胞坏死的苯并噻唑衍生物及其应用
CN117820253A (zh) * 2023-09-19 2024-04-05 西北农林科技大学 3,6-二取代苯并噻唑类化合物及其合成与应用

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994000469A1 (en) 1992-06-26 1994-01-06 Immunex Corporation Novel tyrosine kinase
US5477860A (en) * 1992-11-05 1995-12-26 Synectics Medical, Inc. Catheter for measuring respiration and respiratory effort
GB9226581D0 (en) * 1992-12-21 1993-02-17 Merck Sharp & Dohme Therapeutic agents
JPH10506011A (ja) * 1994-09-22 1998-06-16 ヘルシンキ、ユニバーシティ、ライセンシング、リミテッド、オサケ、ユキチュア レセプターチロシンキナーゼ、tieのプロモーター
DK0986382T3 (da) 1997-05-23 2008-10-20 Bayer Pharmaceuticals Corp RAF-kinasehæmmere
DE69826695T2 (de) 1997-05-23 2006-02-02 Bayer Pharmaceuticals Corp., West Haven Arylharnstoffderivate zur behandlung von inflammatorischen oder immunomodulatorischen erkrankungen
US6030831A (en) * 1997-09-19 2000-02-29 Genetech, Inc. Tie ligand homologues
ATE315394T1 (de) * 1997-11-10 2006-02-15 Bristol Myers Squibb Co Benzothiazole als protein tyrosin-kinase inhibitoren
CN1213022C (zh) 1997-12-22 2005-08-03 拜尔有限公司 用对称和不对称的取代二苯脲抑制raf激酶
IL136768A0 (en) 1997-12-22 2001-06-14 Bayer Ag INHIBITION OF p38 KINASE ACTIVITY USING ARYL AND HETEROARYL SUBSTITUTED HETEROCYCLIC UREAS
ATE529109T1 (de) 1997-12-22 2011-11-15 Bayer Healthcare Llc Hemmung der p38 kinase aktivität durch substituierte heterocyclische harnstoffe
DE69831013T2 (de) 1997-12-22 2006-04-20 Bayer Pharmaceuticals Corp., West Haven Inhibierung der raf-kinase durch substituierte heterocyclische harnstoffverbindungen
WO1999032463A1 (en) 1997-12-22 1999-07-01 Bayer Corporation INHIBITION OF p38 KINASE USING SYMMETRICAL AND UNSYMMETRICAL DIPHENYL UREAS
PT1056725E (pt) 1997-12-22 2006-09-29 Bayer Pharmaceuticals Corp Inibicao da raf-quinase usando ureias heterociclicas substituidas com arilo e heteroarilo
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents

Also Published As

Publication number Publication date
US7238813B2 (en) 2007-07-03
WO2002044156A2 (en) 2002-06-06
EP1341771A2 (en) 2003-09-10
US20040082583A1 (en) 2004-04-29
US20070249600A1 (en) 2007-10-25
JP2004517080A (ja) 2004-06-10
WO2002044156A3 (en) 2002-10-17

Similar Documents

Publication Publication Date Title
AU2002232439A1 (en) Benzimidazole derivatives useful as tie-2 and/or vegfr-2 inhibitors
IL153246A0 (en) Substituted quinazoline derivatives and their use as inhibitors
IL152078A0 (en) 8-quinolinxanthine and 8-isoquinolinxanthine derivatives as pde 5 inhibitors
AU2002224038A1 (en) Benzimidazole derivatives
SI1686119T1 (sl) Derivati pirimidin-5-ona kot inhibitorji ldl-pla2
AU2001244355A1 (en) Heterobiarylsulphonamides and their use as pde 7 inhibitors
AU3034300A (en) Substituted benzimidazoles and their use as parp inhibitors
AU2403802A (en) Benzimidazole derivatives
AU2001288249A1 (en) Biosensors and methods for their use
HUP0301773A3 (en) Apomorphine derivatives and methods for their use
PL356427A1 (en) Indol-3-yl derivatives and their use as integrin inhibitors
AU2003232848A1 (en) Phenylaminopyrimidines and their use as rho-kinase inhibitors
AU2003215756A1 (en) Benzimidazoles and their use as mitogen-activated- and rho-kinase inhibitors
AU2002216649A1 (en) Benzoxazole lpaat- beta inhibitors and uses thereof
PL349769A1 (en) New amidinobenzylamine derivatives and their use as thrombin inhibitors
EP1390363A4 (en) SUBSTITUTED AZOLIC ACID DERIVATIVES, WHICH APPRECIATE AS AGENTS AGAINST DIABETES AND OBESITAS, AND METHODS
AU2001276027A1 (en) Heteroaryl-beta-alanine derivatives as alpha 4 integrin inhibitors
AU5693101A (en) New thiochromane derivatives and their use as thrombin inhibitors
ITMI991483A0 (it) Derivati tassanici e procedimenti per la loro preparazione
AU2001277561A1 (en) Biphenyl derivatives and the use thereof as integrin inhibitors
AU2001266124A1 (en) 2-aminothiazoline derivatives and their use as no-synthase inhibitors
AU2001291877A1 (en) N-alkoxyalkyl-substituted benzimidazoles and the use thereof as an agent againstparasitic protozoans
AU2002332178A1 (en) Benzimidazole derivatives
AU2001235364A1 (en) Tetrahydronaphtalene derivatives and their use
AU2001282268A1 (en) Phenantridine derivatives and their use as anti-telomerase agent