JP2002509536A - 2−(4−ブロモ又は4−ヨードフェニルアミノ)安息香酸誘導体及びmek阻害物質としてのそれらの使用 - Google Patents

2−(4−ブロモ又は4−ヨードフェニルアミノ)安息香酸誘導体及びmek阻害物質としてのそれらの使用

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Publication number
JP2002509536A
JP2002509536A JP50722799A JP50722799A JP2002509536A JP 2002509536 A JP2002509536 A JP 2002509536A JP 50722799 A JP50722799 A JP 50722799A JP 50722799 A JP50722799 A JP 50722799A JP 2002509536 A JP2002509536 A JP 2002509536A
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Prior art keywords
iodo
methylphenylamino
benzamide
fluoro
bromo
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Withdrawn
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JP50722799A
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English (en)
Japanese (ja)
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JP2002509536A5 (https=
Inventor
バーレット,スティーブン・ダグラス
ブリッジス,アレクサンダー・ジェームズ
コーディ,ドナ・レイノルズ
ドハーティ,アンネット・マリアン
ダッドレー,デイビッド・トーマス
サルティエル,アラン・ロバート
シュローダー,メル・コンラッド
テクル,ハイル
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Warner Lambert Co LLC
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Warner Lambert Co LLC
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Publication of JP2002509536A publication Critical patent/JP2002509536A/ja
Publication of JP2002509536A5 publication Critical patent/JP2002509536A5/ja
Withdrawn legal-status Critical Current

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/36Radicals substituted by singly-bound nitrogen atoms
    • C07D213/40Acylated substituent nitrogen atom
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/68Compounds containing amino and hydroxy groups bound to the same carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings and hydroxy groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/52Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C07C229/54Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring
    • C07C229/56Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in ortho-position
    • C07C229/58Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton with amino and carboxyl groups bound to carbon atoms of the same non-condensed six-membered aromatic ring with amino and carboxyl groups bound in ortho-position having the nitrogen atom of at least one of the amino groups further bound to a carbon atom of a six-membered aromatic ring, e.g. N-phenyl-anthranilic acids
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/30Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
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    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/32Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to an acyclic carbon atom of a hydrocarbon radical substituted by oxygen atoms
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/36Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C243/00Compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
    • C07C243/24Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids
    • C07C243/38Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to carbon atoms of six-membered aromatic rings
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    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/37Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C07C311/38Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton
    • C07C311/44Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring having sulfur atoms of sulfonamide groups and amino groups bound to carbon atoms of six-membered rings of the same carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D257/00Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
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    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07D295/22Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
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    • C07D295/32Nitrogen atoms acylated with carboxylic or carbonic acids, or their nitrogen or sulfur analogues
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    • C07D333/06Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/20Radicals substituted by singly bound hetero atoms other than halogen by nitrogen atoms

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  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Neurology (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Emergency Medicine (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP50722799A 1997-07-01 1998-06-24 2−(4−ブロモ又は4−ヨードフェニルアミノ)安息香酸誘導体及びmek阻害物質としてのそれらの使用 Withdrawn JP2002509536A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US5143397P 1997-07-01 1997-07-01
US60/051,433 1997-07-01
PCT/US1998/013105 WO1999001421A1 (en) 1997-07-01 1998-06-24 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as mek inhibitors

Publications (2)

Publication Number Publication Date
JP2002509536A true JP2002509536A (ja) 2002-03-26
JP2002509536A5 JP2002509536A5 (https=) 2005-12-22

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JP50722799A Withdrawn JP2002509536A (ja) 1997-07-01 1998-06-24 2−(4−ブロモ又は4−ヨードフェニルアミノ)安息香酸誘導体及びmek阻害物質としてのそれらの使用

Country Status (17)

Country Link
EP (1) EP0993437B1 (https=)
JP (1) JP2002509536A (https=)
KR (1) KR20010014360A (https=)
AR (1) AR016119A1 (https=)
AT (1) ATE344791T1 (https=)
AU (1) AU756586C (https=)
BR (1) BR9810385A (https=)
CA (1) CA2290509A1 (https=)
DE (1) DE69836378T2 (https=)
ES (1) ES2274572T3 (https=)
HR (1) HRP980369A2 (https=)
NZ (1) NZ501277A (https=)
PE (1) PE98099A1 (https=)
TW (1) TWI221831B (https=)
UY (1) UY25075A1 (https=)
WO (1) WO1999001421A1 (https=)
ZA (1) ZA985726B (https=)

Cited By (11)

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JP2006513154A (ja) * 2002-10-21 2006-04-20 ラモト アット テル アヴィヴ ユニヴァーシティ リミテッド カリウムチャネルおよび/または皮質ニューロン活性モジュレーターとしての、n−フェニルアントラニル酸および2−ベンズイミダゾロンの誘導体
JP2008517024A (ja) * 2004-10-20 2008-05-22 アプライド リサーチ システムズ エーアールエス ホールディング ナームロゼ フェンノートシャップ 3−アリルアミノピペリジン誘導体
WO2010068738A1 (en) 2008-12-10 2010-06-17 Dana-Farber Cancer Institute, Inc. Mek mutations conferring resistance to mek inhibitors
WO2011106298A1 (en) 2010-02-25 2011-09-01 Dana-Farber Cancer Institute, Inc. Braf mutations conferring resistance to braf inhibitors
US8278357B2 (en) 2002-10-21 2012-10-02 Ramot At Tel-Aviv University Ltd. Derivatives of N-phenylanthranilic acid and 2-benzimidazolone as potassium channel and/or neuron activity modulators
JP5091663B2 (ja) * 2005-03-16 2012-12-05 富山化学工業株式会社 新規なアントラニル酸誘導体またはその塩
WO2013169858A1 (en) 2012-05-08 2013-11-14 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy
US8765815B2 (en) 2007-09-20 2014-07-01 Ramot At Tel-Aviv University Ltd. N-phenyl anthranilic acid derivatives and uses thereof
JP2015533175A (ja) * 2012-10-12 2015-11-19 エグゼリクシス, インコーポレイテッド 癌の処置に使用するための化合物の製造方法
JP2016530317A (ja) * 2013-09-11 2016-09-29 ジ・アドミニストレーターズ・オブ・ザ・チューレーン・エデュケーショナル・ファンド 新規アントラニルアミドとその使用
US11078540B2 (en) 2010-03-09 2021-08-03 Dana-Farber Cancer Institute, Inc. Methods of diagnosing and treating cancer in patients having or developing resistance to a first cancer therapy

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US6506798B1 (en) 1997-07-01 2003-01-14 Warner-Lambert Company 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors
US6846799B1 (en) 1998-08-18 2005-01-25 The Regents Of The University Of California Preventing airway mucus production by administration of EGF-R antagonists
US7354894B2 (en) 1998-08-18 2008-04-08 The Regents Of The University Of California Preventing airway mucus production by administration of EGF-R antagonists
AU2180500A (en) * 1998-12-15 2000-07-03 Warner-Lambert Company Use of a mek inhibitor for preventing transplant rejection
AU2203800A (en) * 1999-01-07 2000-07-24 Warner-Lambert Company Antiviral method using mek inhibitors
HUP0105092A3 (en) * 1999-01-13 2003-12-29 Warner Lambert Co 1-heterocycle substituted diarylamines and medicaments containing them
CA2348236A1 (en) * 1999-01-13 2000-07-20 Stephen Douglas Barrett 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors
HRP20010603A2 (en) * 1999-02-24 2002-08-31 Hoffmann La Roche Phenyl-and pyridinyl derivatives
GB9910580D0 (en) 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
GB9910579D0 (en) * 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
JP2003504400A (ja) * 1999-07-16 2003-02-04 ワーナー−ランバート・カンパニー Mek阻害剤を用いた慢性痛の治療方法
EP1202732A2 (en) * 1999-07-16 2002-05-08 Warner-Lambert Company Llc Method for treating chronic pain using mek inhibitors
JP2003504401A (ja) * 1999-07-16 2003-02-04 ワーナー−ランバート・カンパニー Mek阻害剤を用いる慢性疼痛の治療方法
US7345051B2 (en) 2000-01-31 2008-03-18 Genaera Corporation Mucin synthesis inhibitors
ES2282235T3 (es) 2000-01-31 2007-10-16 Genaera Corporation Inhibidores de la sintesis de la mucina.
GB0002740D0 (en) * 2000-02-07 2000-03-29 Novartis Ag Organic compounds
BR0109188A (pt) * 2000-03-15 2003-03-18 Warner Lambert Co Diarilaminas 5-amida substituìdas como inibidores de mex
EP1339702A1 (en) 2000-03-15 2003-09-03 Warner-Lambert Company 5-amide substituted diarylamines as mek inhibitors
DE10017480A1 (de) * 2000-04-07 2001-10-11 Transmit Technologietransfer Verwendung von Substanzen, die als MEK Inhibitor wirken, zur Herstellung eines Arneimittels gegen DNA- und RNA-Viren
US6964982B2 (en) 2000-04-20 2005-11-15 Neurotech Co., Ltd. Compounds, compositions and methods for preventing neurodegeneration in acute and chronic injuries in the central nervous system
DZ3401A1 (fr) 2000-07-19 2002-01-24 Warner Lambert Co Esters oxygenes d'acides 4-iodophenylamino benzhydroxamiques
KR20030059115A (ko) * 2000-08-25 2003-07-07 워너-램버트 캄파니 엘엘씨 N-아릴-안트라닐산 및 그의 유도체의 제조 방법
EP1337524A1 (en) 2000-11-02 2003-08-27 AstraZeneca AB Substituted quinolines as antitumor agents
EP1337513A1 (en) 2000-11-02 2003-08-27 AstraZeneca AB 4-substituted quinolines as antitumor agents
IL149462A0 (en) * 2001-05-09 2002-11-10 Warner Lambert Co Method of treating or inhibiting neutrophil chemotaxis by administering a mek inhibitor
DOP2003000556A (es) * 2002-01-23 2003-10-31 Warner Lambert Co Esteres hidroxamato de acido n-(4-fenil-sustituido)-antranilico.
EP1467968A1 (en) 2002-01-23 2004-10-20 Warner-Lambert Company LLC N-(4-substituted phenyl)-anthranilic acid hydroxamate esters
US7235537B2 (en) 2002-03-13 2007-06-26 Array Biopharma, Inc. N3 alkylated benzimidazole derivatives as MEK inhibitors
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