JP2004517080A - Ｔｉｅ−２および／またはｖｅｇｆｒ−２の阻害剤として有用なベンゾイミダゾール誘導体 - Google Patents

Ｔｉｅ−２および／またはｖｅｇｆｒ−２の阻害剤として有用なベンゾイミダゾール誘導体 Download PDF

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JP2004517080A
JP2004517080A JP2002546526A JP2002546526A JP2004517080A JP 2004517080 A JP2004517080 A JP 2004517080A JP 2002546526 A JP2002546526 A JP 2002546526A JP 2002546526 A JP2002546526 A JP 2002546526A JP 2004517080 A JP2004517080 A JP 2004517080A
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Prior art keywords
aminocarbonylamino
benzimidazol
phenoxy
phenyl
methyl
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Pending
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JP2002546526A
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Japanese (ja)
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JP2004517080A5 (enExample
Inventor
チュン，ムーイ
ハリス，フィリップ，アンソニー
雅一 長谷川
覚 井田
一也 鹿野
直彦 西垣
秀行 佐藤
ヴィール，ジェームス，マーヴィン
嘉明 鷲尾
ウェスト，ロブ，アイ．
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Glaxo Group Ltd
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Glaxo Group Ltd
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Publication of JP2004517080A publication Critical patent/JP2004517080A/ja
Publication of JP2004517080A5 publication Critical patent/JP2004517080A5/ja
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic 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
    • C07D231/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic 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
    • C07D233/56—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; 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
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; 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
    • C07D235/30—Nitrogen atoms not forming part of a nitro radical
    • C07D235/32—Benzimidazole-2-carbamic acids, unsubstituted or substituted; Esters thereof; Thio-analogues thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles 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
    • C07D277/82—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/12—Heterocyclic 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
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (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)
JP2002546526A 2000-11-29 2001-11-28 Ｔｉｅ−２および／またはｖｅｇｆｒ−２の阻害剤として有用なベンゾイミダゾール誘導体 Pending JP2004517080A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US25386800P 2000-11-29 2000-11-29
US31093901P 2001-08-08 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 (2)

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JP2004517080A true JP2004517080A (ja) 2004-06-10
JP2004517080A5 JP2004517080A5 (enExample) 2005-05-26

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Country Status (5)

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

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006035685A1 (ja) * 2004-09-28 2006-04-06 Sankyo Company, Limited 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
JP2006124375A (ja) * 2004-09-28 2006-05-18 Sankyo Co Ltd 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
JP2008515943A (ja) * 2004-10-13 2008-05-15 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフトング キナーゼ阻害剤としての複素環式置換ビスアリール尿素誘導体
JP2008525361A (ja) * 2004-12-27 2008-07-17 ４エスツェー アクチェンゲゼルシャフト プロテインキナーゼ阻害剤として有用な２，５及び２，６−二置換ベンザゾール類似体
WO2010064611A1 (ja) * 2008-12-01 2010-06-10 武田薬品工業株式会社 複素環化合物およびその用途
JP2010527909A (ja) * 2007-06-05 2010-08-19 武田薬品工業株式会社 キナーゼ阻害剤としての二環式複素環化合物
JP2010536796A (ja) * 2007-08-17 2010-12-02 アイカジェン， インコーポレイテッド カリウムチャネル調節物質としての複素環
JP2012510467A (ja) * 2008-12-02 2012-05-10 武田薬品工業株式会社 抗癌剤としてのベンゾチアゾール誘導体
JP2016520617A (ja) * 2013-05-30 2016-07-14 カラ ファーマシューティカルズ インコーポレイテッド 新規の化合物及びその使用
JP2022528562A (ja) * 2019-04-05 2022-06-14 ストーム・セラピューティクス・リミテッド Ｍｅｔｔｌ３阻害化合物

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US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
EP2298311B1 (en) 1999-01-13 2012-05-09 Bayer HealthCare LLC w-Carboxy aryl substituted diphenyl ureas as p38 kinase inhibitors
KR100600550B1 (ko) 2000-10-20 2006-07-13 에자이 가부시키가이샤 질소 함유 방향환 유도체
EP2305255B1 (en) † 2001-12-03 2012-08-22 Bayer HealthCare LLC Aryl urea compounds in combination with other cytostatic or cytotoxic agents for treating human cancers
DK1478358T3 (da) 2002-02-11 2013-10-07 Bayer Healthcare Llc Sorafenibtosylat til behandling af sygdomme kendetegnet ved unormal angiogenese
MXPA04009541A (es) 2002-03-29 2005-01-25 Chiron Corp Benzazoles sustituidos y uso de los mismos como inhibidores de cinasa raf.
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
ATE323702T1 (de) 2002-08-06 2006-05-15 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
JP2006521345A (ja) * 2003-03-28 2006-09-21 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー ニコチン性アセチルコリン受容体の正のアロステリック調節剤
WO2004087153A2 (en) 2003-03-28 2004-10-14 Chiron Corporation Use of organic compounds for immunopotentiation
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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
WO2005004864A1 (en) * 2003-07-11 2005-01-20 Merck Patent Gmbh Benzimidazole derivatives as raf kinase inhibitors
PL1663978T3 (pl) 2003-07-23 2008-04-30 Bayer Healthcare Llc Fluoropodstawiony omega-karboksyarylodifenylomocznik do leczenia i profilaktyki chorób i stanów
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
EP1682126B1 (en) 2003-10-16 2009-07-01 Novartis Vaccines and Diagnostics, Inc. Substituted benzazoles and use thereof as inhibitors of raf kinase
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JP4303726B2 (ja) 2003-11-11 2009-07-29 エーザイ・アール・アンド・ディー・マネジメント株式会社 ウレア誘導体およびその製造方法
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TW200530236A (en) 2004-02-23 2005-09-16 Chugai Pharmaceutical Co Ltd Heteroaryl phenylurea
JP2007523929A (ja) * 2004-02-26 2007-08-23 メルク　パテント　ゲゼルシャフト　ミット　ベシュレンクテル　ハフトング ベンズイミダゾリル誘導体
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JP5065034B2 (ja) * 2004-10-13 2012-10-31 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング キナーゼ阻害剤として適しているｎ，ｎ’−ジフェニル尿素誘導体
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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
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