JPH05506857A - Egfレセプタチロシンキナーゼを阻害するスチリル―置換単環式および二環式複素アリール化合物 - Google Patents

Egfレセプタチロシンキナーゼを阻害するスチリル―置換単環式および二環式複素アリール化合物

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Publication number
JPH05506857A
JPH05506857A JP91508820A JP50882091A JPH05506857A JP H05506857 A JPH05506857 A JP H05506857A JP 91508820 A JP91508820 A JP 91508820A JP 50882091 A JP50882091 A JP 50882091A JP H05506857 A JPH05506857 A JP H05506857A
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JP
Japan
Prior art keywords
compound
ring
alkyl
group
independently
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.)
Pending
Application number
JP91508820A
Other languages
English (en)
Japanese (ja)
Inventor
スパーダ アルフレッド ピー
ポール イー パーソンズ
レヴィツキ アレクサンダー
ギロン ハイム
ガジト アヴィヴ
Original Assignee
ローヌ―プーラン ローラー インターナショナル (ホウルディングス)インコーポレイテッド
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.)
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Application filed by ローヌ―プーラン ローラー インターナショナル (ホウルディングス)インコーポレイテッド filed Critical ローヌ―プーラン ローラー インターナショナル (ホウルディングス)インコーポレイテッド
Publication of JPH05506857A publication Critical patent/JPH05506857A/ja
Pending legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • 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
    • C07D213/89Heterocyclic 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 with hetero atoms directly attached to the ring nitrogen atom
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D213/54Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/57Nitriles

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP91508820A 1990-04-16 1991-04-16 Egfレセプタチロシンキナーゼを阻害するスチリル―置換単環式および二環式複素アリール化合物 Pending JPH05506857A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US50994290A 1990-04-16 1990-04-16
PCT/US1991/002603 WO1991016051A1 (fr) 1990-04-16 1991-04-16 Composes heteroaryles monocycliques et bicycliques a substitution styrile qui inhibent la kinase de tyrosine du recepteur egf

Publications (1)

Publication Number Publication Date
JPH05506857A true JPH05506857A (ja) 1993-10-07

Family

ID=24028743

Family Applications (1)

Application Number Title Priority Date Filing Date
JP91508820A Pending JPH05506857A (ja) 1990-04-16 1991-04-16 Egfレセプタチロシンキナーゼを阻害するスチリル―置換単環式および二環式複素アリール化合物

Country Status (6)

Country Link
EP (1) EP0525109A4 (fr)
JP (1) JPH05506857A (fr)
AU (1) AU658567B2 (fr)
CA (1) CA2080581A1 (fr)
IL (1) IL97872A (fr)
WO (1) WO1991016051A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005095341A1 (fr) * 2004-03-30 2005-10-13 Kyowa Hakko Kogyo Co., Ltd. Composé hétérocyclique contenant de l'azote
WO2006106778A1 (fr) * 2005-03-30 2006-10-12 Kabushiki Kaisha Yakult Honsha Inhibiteurs de bcrp/abcg2
JP2012531399A (ja) * 2009-06-23 2012-12-10 セントレ・ナショナル・デ・ラ・レシェルシェ・サイエンティフィーク ガンの処置の為にインドールの誘導体を使用する方法

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* Cited by examiner, † Cited by third party
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US5602130A (en) * 1987-03-20 1997-02-11 Allergan Disubstituted acetylenes bearing heteroaromatic and heterobicyclic groups having retinoid like activity
US5264578A (en) * 1987-03-20 1993-11-23 Allergan, Inc. Disubstituted acetylenes bearing heterobicyclic groups and heteroaromatic or phenyl groups having retinoid like activity
US5183827A (en) * 1989-09-19 1993-02-02 Allergan, Inc. Acetylenes disubstituted with a heteroaromatic group and a 2-substituted chromanyl, thiochromanyl or 1,2,3,4-tetrahydroquinolinyl group having retinoid-like activity
US5272156A (en) * 1989-09-19 1993-12-21 Allergan, Inc. Acetylenes disubstituted with a heteroaromatic group and a 2-substituted 1,2,3,4-tetrahydroquinolinyl group having retinoid-like activity
US5264456A (en) * 1989-12-29 1993-11-23 Allergan, Inc. Acetylenes disubstituted with a furyl group and a substituted phenyl group having retinoid like activity
US5302606A (en) * 1990-04-16 1994-04-12 Rhone-Poulenc Rorer Pharmaceuticals Inc. Styryl-substituted pyridyl compounds which inhibit EGF receptor tyrosine kinase
JPH05507072A (ja) * 1990-04-16 1993-10-14 イッスム リサーチ ディヴェロプメント カンパニー オブ ザ ヒーブルー ユニヴァーシティ オブ エルサレム Egfレセプタチロシンキナーゼを阻害する複素環式エテンジイル化合物
ES2108120T3 (es) * 1991-05-10 1997-12-16 Rhone Poulenc Rorer Int Compuestos bis arilicos y heteroarilicos mono- y biciclicos que inhiben tirosina quinasa receptora de egf y/o pdgf.
US5324840A (en) 1992-06-11 1994-06-28 Allergan, Inc. Method of treatment with compounds having retinoid-like activity and reduced skin toxicity and lacking teratogenic effects
US6172115B1 (en) 1993-02-11 2001-01-09 Allergan Sales, Inc. Method for preventing onset of restenosis after angioplasty employing an RXR-specific retinoid
US5455265A (en) 1993-02-11 1995-10-03 Allergan, Inc. Method of treatment with compounds having selective agonist-like activity on RXR retinoid receptors
US5475022A (en) * 1993-10-18 1995-12-12 Allergan, Inc. Phenyl or heteroaryl and tetrahydronaphthyl substituted diene compounds having retinoid like biological activity
US5426118A (en) * 1993-12-30 1995-06-20 Allergan, Inc. [4-(1,2-epoxycyclohexanyl)but-3-en-1-ynyl]aromatic and heteroaromatic acids and derivatives having retinoid-like biological activity
US5498755A (en) * 1994-08-23 1996-03-12 Chandraratna; Roshantha A. Disubstituted aryl and heteroaryl imines having retinoid-like biological activity
US5618943A (en) * 1994-12-29 1997-04-08 Allergan Acetylenes disubstituted with a 5 OXO substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity
US5556996A (en) * 1994-12-29 1996-09-17 Allergan Oxiranyls disubstituted with a phenyl group and a substituted chromanyl or tetrahydroquinolinyl group having retinoid like activity
US5534641A (en) * 1994-12-29 1996-07-09 Allergan Acetylenes disubstituted with 2-tetrahydropyranoxyaryl and aryl or heteroaryl groups having retinoid-like biological activity
US5618931A (en) * 1994-12-29 1997-04-08 Allergan Acetylenes disubstituted with a 5 substituted dihydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity
US5514825A (en) * 1994-12-29 1996-05-07 Allergan, Inc. Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity
US5599967A (en) * 1994-12-29 1997-02-04 Allergan Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl of heteroaryl group having retinoid-like biological activity
US5543534A (en) * 1994-12-29 1996-08-06 Allergan Acetylenes disubstituted with a 5 substituted tetrahydronaphthyl group and with an aryl or heteroaryl groups having retinoid-like biological activity
US5489584A (en) * 1994-12-29 1996-02-06 Allergan, Inc. Acetylenes disubstituted with a 5-amino or substituted 5-amino substituted tetrahydronaphthyl group and with an aryl or heteroaryl group having retinoid-like biological activity
US6025388A (en) * 1995-04-26 2000-02-15 Allergan Sales, Inc. Method for inhibiting gene expression promoted by AP1 protein with RARβ selective retinoids and method for treatment of diseases and conditions with such retinoids
US5616712A (en) * 1995-05-16 1997-04-01 Allergan Acetylenes disubstituted with a phenyl or heteroaryl group and a 2-thio-1,2,3,4-tetrahdroquinolinyl, 2-alkylthio-3,4-dihydroquinolinyl or 2-alkoxy-3,4-dihydroquinolinyl group having retinoid-like biological activity
US5675033A (en) * 1995-06-06 1997-10-07 Allergan 2,4-pentadienoic acid derivatives having retinoid-like biological activity
US5710164A (en) * 1995-06-06 1998-01-20 American Home Products Corporation Diheterocyclic styryl nitriles
AU7598596A (en) * 1995-11-01 1997-05-22 Allergan, Inc. Sulfides, sulfoxides and sulfones disubstituted with a tetrahydronaphthalenyl, chromanyl, thiochromanyl or tetrahydroquinolinyl and substituted phenyl or heteroaryl group, having retinoid-like biological activity
US5675024A (en) * 1995-11-22 1997-10-07 Allergan Aryl or heteroaryl amides of tetrahydronaphthalene, chroman, thiochroman and 1,2,3,4,-tetrahydroquinoline carboxylic acids, having an electron withdrawing substituent in the aromatic or heteroaromatic moiety, having retinoid-like biological activity
US5663357A (en) * 1995-11-22 1997-09-02 Allergan Substituted heteroarylamides having retinoid-like biological activity
US5688957A (en) * 1995-12-29 1997-11-18 Allergan (3"-thioxacyclohex-1"-enyl)!-but-3'-ene-1'-ynyl!aryl and (3"-thioxacyclohex-1"-enyl)!-but-3'-ene-1'-ynyl!heteroaryl carboxylic acids and esters having retinoid-like biological activity
US5965606A (en) 1995-12-29 1999-10-12 Allergan Sales, Inc. Methods of treatment with compounds having RAR.sub.α receptor specific or selective activity
US5723666A (en) * 1996-06-21 1998-03-03 Allergan Oxime substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity
US5763635A (en) * 1996-06-21 1998-06-09 Allergan Tetrahydronaphthalene derivatives substituted in the 8 position with alkyhidene groups having retinoid and/or retinoid antagonist-like biological activity
US5808124A (en) * 1996-06-21 1998-09-15 Allergan O- or S-substituted dihydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity
US5741896A (en) * 1996-06-21 1998-04-21 Allergan O- or S- substituted tetrahydronaphthalene derivatives having retinoid and/or retinoid antagonist-like biological activity
US5739338A (en) * 1996-11-05 1998-04-14 Allergan N-aryl substituted tetrahydroquinolines having retinoid agonist, retinoid antagonist or retinoid inverse agonist type biological activity
PE20011178A1 (es) 2000-04-07 2001-11-19 Takeda Chemical Industries Ltd Compuestos heterociclicos y su produccion
MXPA02010759A (es) 2000-05-02 2004-07-30 Sugen Inc Derivados del acido (2-oxindol-3-ilidenil) acetico y su uso como inhibidores de la proteina quinasa.
US6313107B1 (en) 2000-08-29 2001-11-06 Allergan Sales, Inc. Methods of providing and using compounds having activity as inhibitors of cytochrome P450RAI
US6369261B1 (en) 2000-08-29 2002-04-09 Allergan Sales, Inc. Compounds having activity as inhibitors of cytochrome P450RAI
US6387951B1 (en) 2000-08-29 2002-05-14 Allergan Sales, Inc. Compounds having activity as inhibitors of cytochrome P450RAI
EP1638600A4 (fr) 2003-06-09 2008-06-11 Samuel Waksal Procedes d'inhibition de tyrosine-kinases receptrices au moyen d'un antagoniste extracellulaire et d'un antagoniste intracellulaire
AU2005224267B2 (en) 2004-03-19 2011-07-21 Imclone Llc Human anti-epidermal growth factor receptor antibody
KR101246504B1 (ko) 2005-06-17 2013-03-26 임클론 엘엘씨 항-PDGFRα 항체
WO2007025044A2 (fr) 2005-08-24 2007-03-01 Bristol-Myers Squibb Company Marqueurs biologiques et procedes permettant de determiner la receptivite aux modulateurs du recepteur du facteur de croissance epidermique (egfr)
US8703808B2 (en) 2009-06-23 2014-04-22 Centre National De La Recherche Scientifique Use of derivatives of indoles for the treatment of cancer
US20120220594A1 (en) 2009-10-30 2012-08-30 Bristol-Meyers Squibb Company Methods for treating cancer in patients having igf-1r inhibitor resistance
GB201106870D0 (en) 2011-04-26 2011-06-01 Univ Belfast Marker
WO2013056069A1 (fr) 2011-10-13 2013-04-18 Bristol-Myers Squibb Company Procédés de sélection et de traitement du cancer chez des patients au moyen d'inhibiteurs de l'igf-1r/ir
GB201407695D0 (en) * 2014-05-01 2014-06-18 Univ Montfort Compounds
WO2018078143A1 (fr) 2016-10-28 2018-05-03 MAX-PLANCK-Gesellschaft zur Förderung der Wissenschaften e.V. Moyens et procédés pour déterminer l'efficacité d'inhibiteurs anti-egfr dans une thérapie du cancer colorectal (crc)

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CH651034A5 (de) * 1982-05-12 1985-08-30 Hoffmann La Roche Chroman-, thiochroman- oder 1,2,3,4-tetrahydrochinolinderivate und ihre verwendung als arzneimittel-wirkstoffe.
CA1234388A (fr) * 1982-09-27 1988-03-22 Pieter T. Haken Composes fongicides contenant des derives de l'ethene
US4826984A (en) * 1984-04-09 1989-05-02 The Board Of Regents For The Oklahoma Agricultural And Mechanical College Acting For And On Behalf Of Oklahoma State University Heteroarotinoid compounds as anticancer agents

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005095341A1 (fr) * 2004-03-30 2005-10-13 Kyowa Hakko Kogyo Co., Ltd. Composé hétérocyclique contenant de l'azote
WO2006106778A1 (fr) * 2005-03-30 2006-10-12 Kabushiki Kaisha Yakult Honsha Inhibiteurs de bcrp/abcg2
EA014555B1 (ru) * 2005-03-30 2010-12-30 Кабусики Кайся Якулт Хонса Ингибитор bcrp/abcg2
US8697742B2 (en) 2005-03-30 2014-04-15 Kabushiki Kaisha Yakult Honsha BCRP/ABCG2 inhibitor
JP2012531399A (ja) * 2009-06-23 2012-12-10 セントレ・ナショナル・デ・ラ・レシェルシェ・サイエンティフィーク ガンの処置の為にインドールの誘導体を使用する方法

Also Published As

Publication number Publication date
AU7797991A (en) 1991-11-11
WO1991016051A1 (fr) 1991-10-31
CA2080581A1 (fr) 1991-10-17
EP0525109A4 (en) 1993-06-30
EP0525109A1 (fr) 1993-02-03
IL97872A (en) 1996-07-23
AU658567B2 (en) 1995-04-27
IL97872A0 (en) 1992-06-21

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