EP 1633738 A2 20060315 - NOVEL INDOLE DERIVATIVES, METHOD OF PREPARING SAME IN THE FORM OF MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND, IN PARTICULAR, KDR INHIBITORS
Title (en)
NOVEL INDOLE DERIVATIVES, METHOD OF PREPARING SAME IN THE FORM OF MEDICAMENTS, PHARMACEUTICAL COMPOSITIONS AND, IN PARTICULAR, KDR INHIBITORS
Title (de)
NEUE INDOLDERIVATE, VERFAHREN ZU DEREN HERSTELLUNG IN FORM VON MEDIKAMENTEN, PHARMAZEUTISCHE ZUSAMMENSETZUNGEN UND INSBESONDERE KDR-INHIBITOREN
Title (fr)
NOUVEAUX DERIVES DE L INDOLE, LEUR PREPARATION A TITRE DE ME DICAMENTS, COMPOSITIONS PHARMACEUTIQUES ET NOTAMMENT COMME INHIBITEURS DE KDR
Publication
Application
Priority
- FR 2004000979 W 20040422
- FR 0305088 A 20030425
Abstract (en)
[origin: FR2854159A1] 2-(Pyrazolyl or indazolyl)-indole derivatives (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. 2-(pyrazolyl or indazolyl)-indole derivatives of formula (I), in all possible racemic, enantiomeric or diasteroisomeric forms, their addition salts with (in)organic acids or inorganic bases are new. [Image] R 1>pyrazolyl or indazolyl, optionally substituted by one or more of halo, hydroxy, nitro, cyano, R 4>, OR4, SR 4>, COR 4>, OCOR 4>, COOR 4>, COOH (optionally as salt), NR 5>COR 4>, NR 5>COOR 4>, S(O) nR 4>, S(O) nOR 4>, NR5-SO 2R 4>, OS(O) nR 4>, NY 1>Y 2>, CONY 1>Y 2>, OCONY 1>Y 2>, NR5CONY 1>Y 2>, S(O) nNY 1>Y 2>or optionally substituted thienyl; R 2>, R 3>hydrogen, halo, hydroxy, nitro, cyano, R 4>, OR 4>, COR 4>, OCOR 4>, COOR 4>, COOH, NR 5>COR 4>, NR5COOR 4>, S(O) nR 4>, S(O) nOR 4>, NR 5>-SO 2R 4>, NY 1>Y 2>, CONY 1>Y 2>, NR 5>CONY 1>Y 2>, S(O) nNY 1>Y 2>or OCONY 1>Y 2>; or R 2>+ R 3>optionally substituted 4-6 membered ring optionally containing one or more heteroatoms O,N or S; n : 0-2; R 4>alkyl, alk-NY 1>Y 2>, alk-CONY 1>Y 2>, alkenyl, alkynyl, cycloalkyl, (hetero)aryl, (hetero)cycloalkylalkyl, heteroarylalkyl or aralkyl, all optionally substituted; R 5>hydrogen, alkyl, alkenyl, (hetero)cycloalkyl, (hetero)aryl, aralkyl, (hetero)cycloalkylalkyl, or heteroarylalkyl, all optionally substituted; Y 1>, Y 2>hydrogen, alkyl, alkenyl, (hetero)cycloalkyl, heterocycloalkylalkyl, (hetero)aryl, (hetero)aralkyl or (hetero)arylcarboxy, (all optionally substituted by one or more of halo, hydroxy, alkoxy, alkyl (optionally substituted by hydroxy or carboxy), cyano, nitro, trifluoromethyl, trifluoromethoxy, carboxy (optionally as salt or optionally substituted alkyl ester), Nalk-CO-alk, NHCO-alk, S(O) n-alk, NHS(O) n-alkyl, NHCO-NY 3>Y 4>, CONY 3>Y 4>, S(O) nNY 3>Y 4>, aryl, arylalkoxy, aryloxy, aryloxyalkyl, heteroaryl or heterocycloalkyl (both optionally substituted by one or more T 1>)); or NY 1>Y 2>optionally substituted ring; Y 3>, Y 4>hydrogen, aryl or alkyl (optionally substituted by one or more T 1>); T 1>halo, alkyl, carboxy (optionally as salt or ester) or amino (optionally substituted by 1 or 2 alkyl or by one phenyl (optionally substituted by a dioxol residue)); and alk : 1-6C alkyl. ACTIVITY : Cytostatic; Antiallergic; Antiasthmatic; Anticoagulant; Thrombolytic; Ophthalmological; Antipsoriatic; Antiasthmatic; Antirheumatic; Antidiabetic; Antiarteriosclerotic; Anorectic; Antiparkinsonian; Antidepressant; Neuroleptic; Nootropic; Neuroprotective; Analgesic; Immunomodulator; Antiangiogenic; Vulnerary; Osteopathic. No details of tests for these activities are given. MECHANISM OF ACTION : Inhibition of protein kinases, particularly vascular endothelial growth factor receptor 2 (KDR) and focal adhesion kinase (FAK), and insulin-like growth factor 1 receptor.
IPC 1-7
C07D 403/04; C07D 401/14; C07D 405/14; A61K 31/416; A61P 7/00; A61P 35/00
IPC 8 full level
A61P 9/00 (2006.01); A61P 35/00 (2006.01); C07D 401/14 (2006.01); C07D 403/04 (2006.01); C07D 405/14 (2006.01)
CPC (source: EP)
A61P 3/10 (2017.12); A61P 7/00 (2017.12); A61P 7/02 (2017.12); A61P 9/00 (2017.12); A61P 11/06 (2017.12); A61P 17/06 (2017.12); A61P 21/04 (2017.12); A61P 25/00 (2017.12); A61P 27/02 (2017.12); A61P 29/00 (2017.12); A61P 35/00 (2017.12); A61P 37/08 (2017.12); A61P 43/00 (2017.12); C07D 401/14 (2013.01); C07D 403/04 (2013.01); C07D 405/14 (2013.01)
Citation (search report)
See references of WO 2004096792A2
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IT LI LU MC NL PL PT RO SE SI SK TR
Designated extension state (EPC)
AL HR LT LV MK
DOCDB simple family (publication)
FR 2854159 A1 20041029; FR 2854159 B1 20080111; EP 1633738 A2 20060315; JP 2006524668 A 20061102; WO 2004096792 A2 20041111; WO 2004096792 A3 20050915
DOCDB simple family (application)
FR 0305088 A 20030425; EP 04742556 A 20040422; FR 2004000979 W 20040422; JP 2006505807 A 20040422