ES2183866T3 - Derivados de beta-aril y beta-heteroaril-alfa-cianoacrilamidas sustituido como inhibidors de la tirosina quinasa. - Google Patents

Derivados de beta-aril y beta-heteroaril-alfa-cianoacrilamidas sustituido como inhibidors de la tirosina quinasa.

Info

Publication number
ES2183866T3
ES2183866T3 ES95910542T ES95910542T ES2183866T3 ES 2183866 T3 ES2183866 T3 ES 2183866T3 ES 95910542 T ES95910542 T ES 95910542T ES 95910542 T ES95910542 T ES 95910542T ES 2183866 T3 ES2183866 T3 ES 2183866T3
Authority
ES
Spain
Prior art keywords
beta
alkyl
pct
hydrogen
inhibidors
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.)
Expired - Lifetime
Application number
ES95910542T
Other languages
English (en)
Inventor
Franco Buzzetti
Angelo Crugnola
Antonio Longo
Gabriella Maria Brasca
Dario Ballinari
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.)
Pfizer Italia SRL
Original Assignee
Pharmacia Italia SpA
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 Pharmacia Italia SpA filed Critical Pharmacia Italia SpA
Application granted granted Critical
Publication of ES2183866T3 publication Critical patent/ES2183866T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic 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
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/01Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
    • C07C255/32Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
    • C07C255/41Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by carboxyl groups, other than cyano groups
    • 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
    • C07D209/12Radicals substituted by oxygen atoms
    • 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
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 to ring carbon atoms
    • C07D215/20Oxygen atoms
    • C07D215/24Oxygen atoms attached in position 8
    • C07D215/26Alcohols; Ethers thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/14Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/14Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
    • C07D217/16Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00Systems containing two condensed rings
    • C07C2602/02Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (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)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

LA PRESENTE INVENCION SE REFIERE A NUEVOS COMPUESTOS DE LA FORMULA (I) EN LA QUE A ES UN ANILLO BICICLICO SELECCIONADO DEL NAFTALENO, TETRAHIDRONAFTALENO, QUINOLINA, ISOQUINOLINA E INDOL; B ES UN ANILLO DE BENCENO SUSTITUIDO POR R{SUP,2} O UN ANILLO DE PIRIDINA O DE TIFENO NO SUSTITUIDO; R ES HIDROGENO, ALQUILO C{SUB,1}-C{SUB,6}, HALOGENO, NITRO, CIANO O UN GRUPO NR{SUP,3}R{SUP,4}, EN DONDE CADA UNO DE ENTRE R{SUP,3} Y R{SUP,4} ES, INDEPENDIENTEMENTE, HIDROGENO O ALQUILO C{SUB,1}-C{SUB,6}; R{SUP,1} ES HIDROGENO, ALQUILO C{SUB,1}-C{SUB,6} O ALCANOILO C{SUB,1}-C{SUB,6}; R{SUP,2} ES HIDROGENO, ALQUILO C{SUB,1}C{SUB,6}, HALOGENO, NITRO, CIANO, CARBOXI, HIDROGENO, ALCOXI C{SUB,1}-C{SUB,6}, ALCANOILOXI C{SUB,1}-C{SUB,6} O UN GRUPO NR{SUP,3}R{SUP,4}, EN DONDE R{SUP,3} Y R{SUP,4} SON COMO SE HA DEFINIDO ARRIBA; N ES CERO O UN ENTERO DE 1 A 2; X ES CERO O UN ENTERO DE 1 A 5; A Y LAS SALES FARMACEUTICAMENTE ACEPTABLES DE LOS MISMOS. LOS COMPUESTOS DE LA INVENCION SON UTILES COMO INHIBIDORES DE LA QUINASA DE TIROSINA.
ES95910542T 1994-03-28 1995-03-02 Derivados de beta-aril y beta-heteroaril-alfa-cianoacrilamidas sustituido como inhibidors de la tirosina quinasa. Expired - Lifetime ES2183866T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB9406137A GB9406137D0 (en) 1994-03-28 1994-03-28 N-substituted beta-aryl- and betaheteroaryl-alpha-cyanoacrylamide derivatives and process for their preparation

Publications (1)

Publication Number Publication Date
ES2183866T3 true ES2183866T3 (es) 2003-04-01

Family

ID=10752648

Family Applications (1)

Application Number Title Priority Date Filing Date
ES95910542T Expired - Lifetime ES2183866T3 (es) 1994-03-28 1995-03-02 Derivados de beta-aril y beta-heteroaril-alfa-cianoacrilamidas sustituido como inhibidors de la tirosina quinasa.

Country Status (21)

Country Link
US (1) US5652250A (es)
EP (1) EP0700388B1 (es)
JP (1) JPH08511562A (es)
KR (1) KR960702442A (es)
CN (1) CN1125942A (es)
AT (1) ATE224371T1 (es)
AU (1) AU685599B2 (es)
DE (1) DE69528229T2 (es)
ES (1) ES2183866T3 (es)
FI (1) FI955661A (es)
GB (1) GB9406137D0 (es)
HU (1) HUT73811A (es)
IL (1) IL113044A0 (es)
MX (1) MX9504895A (es)
MY (1) MY130160A (es)
NO (1) NO954692D0 (es)
NZ (1) NZ281630A (es)
PL (1) PL311745A1 (es)
TW (1) TW347386B (es)
WO (1) WO1995026341A1 (es)
ZA (1) ZA952423B (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9613021D0 (en) * 1996-06-21 1996-08-28 Pharmacia Spa Bicyclic 4-aralkylaminopyrimidine derivatives as tyrosine kinase inhibitors
WO1997049653A2 (en) * 1996-06-24 1997-12-31 Irori Solid phase tyrphostin library linked to matrices with memories
EP1060160A2 (en) 1998-02-27 2000-12-20 THE UNITED STATES GOVERNMENT as represented by THE DEPARTMENT OF HEALTH AND HUMAN SERVICES Disubstituted lavendustin a analogs and pharmaceutical compositions comprising the analogs
HUP0000920A3 (en) * 2000-02-28 2002-03-28 Sanofi Synthelabo Pde4 inhibitor isoquinolinylidene derivatives, process for their preparation and medicaments containing them
DK1272457T3 (da) 2000-04-13 2007-01-08 Hsc Res Dev Lp Forbindelser til modulation af celleproliferation
EP1752446A3 (en) * 2000-04-13 2007-03-21 HSC Research and Development Limited Partnership Compounds for modulating cell proliferation
EP1453500A1 (en) * 2001-10-11 2004-09-08 The Hospital For Sick Children Styryl acrylonitrile compounds and their use to promote myelopoiesis
US7745468B2 (en) * 2003-12-11 2010-06-29 Board of Regents, University of Texas Systems The Compounds for treatment of cell proliferative diseases
CA2560584A1 (en) 2004-03-26 2005-10-06 Hsc Research And Development Limited Partnership Novel compounds for modulating cell proliferation
WO2008005954A2 (en) * 2006-06-30 2008-01-10 The Board Of Regents Of The University Of Texas System Tryphostin-analogs for the treatment of cell proliferative diseases
UA103492C2 (ru) 2008-07-08 2013-10-25 Борд Оф Риджентс, Дзе Юниверсити Оф Техас Систем Ингибиторы пролиферации и активации переносчика сигнала и активатора транскрипции (stats)
WO2011060440A2 (en) 2009-11-16 2011-05-19 The Regents Of The University Of California Kinase inhibitors
CN103459371A (zh) * 2011-04-02 2013-12-18 中国人民解放军军事医学科学院毒物药物研究所 芳基丙烯酰胺化合物及其用于制备免疫抑制剂的用途
AU2012255759B2 (en) * 2011-05-17 2017-08-10 Principia Biopharma, Inc. Kinase inhibitors
EP2797886A2 (fr) * 2011-12-30 2014-11-05 Ecole Nationale Superieure de Chimie de Clermont Ferrand Composes anti-douleur
EP3055310B1 (en) * 2013-10-10 2021-03-31 The Regents of The University of Michigan Deubiquitinase inhibitors and methods for use of the same
CN108276366B (zh) * 2018-01-08 2021-09-03 四川大学 一种丙烯酰胺类衍生物及其制备方法与应用

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9000950D0 (en) * 1990-01-16 1990-03-14 Erba Carlo Spa New arylvinylamide derivatives and process for their preparation
GB9000939D0 (en) * 1990-01-16 1990-03-14 Erba Carlo Spa Improvement in the total synthesis of erbstatin analogs
GB9004483D0 (en) * 1990-02-28 1990-04-25 Erba Carlo Spa New aryl-and heteroarylethenylene derivatives and process for their preparation
US5196446A (en) * 1990-04-16 1993-03-23 Yissum Research Development Company Of The Hebrew University Of Jerusalem Certain indole 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
GB9115160D0 (en) * 1991-07-12 1991-08-28 Erba Carlo Spa Methylen-oxindole derivatives and process for their preparation
CA2080554A1 (en) * 1991-10-15 1993-04-16 Mitsubishi Chemical Corporation Styrene derivatives
GB9204945D0 (en) * 1992-03-06 1992-04-22 Erba Carlo Spa 3-aryl-glycidic ester derivatives and process for their preparation
GB9226855D0 (en) * 1992-12-23 1993-02-17 Erba Carlo Spa Vinylene-azaindole derivatives and process for their preparation

Also Published As

Publication number Publication date
HU9503714D0 (en) 1996-02-28
NZ281630A (en) 1998-02-26
HUT73811A (en) 1996-09-30
DE69528229D1 (en) 2002-10-24
MX9504895A (es) 1998-03-31
NO954692L (no) 1995-11-20
WO1995026341A1 (en) 1995-10-05
FI955661A0 (fi) 1995-11-24
PL311745A1 (en) 1996-03-18
CN1125942A (zh) 1996-07-03
AU1849895A (en) 1995-10-17
MY130160A (en) 2007-06-29
US5652250A (en) 1997-07-29
EP0700388B1 (en) 2002-09-18
TW347386B (en) 1998-12-11
EP0700388A1 (en) 1996-03-13
AU685599B2 (en) 1998-01-22
ATE224371T1 (de) 2002-10-15
JPH08511562A (ja) 1996-12-03
KR960702442A (ko) 1996-04-27
ZA952423B (en) 1995-12-19
IL113044A0 (en) 1995-06-29
NO954692D0 (no) 1995-11-20
GB9406137D0 (en) 1994-05-18
FI955661A (fi) 1996-01-19
DE69528229T2 (de) 2003-08-14

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