EP 2104664 A1 20090930 - TETRAHYDROBENZOISOXAZOLE - AND TETRAHYDROINDAZOLE DERIVATIVES AS MODULATORS OF THE MITOTIC MOTOR PROTEIN
Title (en)
TETRAHYDROBENZOISOXAZOLE - AND TETRAHYDROINDAZOLE DERIVATIVES AS MODULATORS OF THE MITOTIC MOTOR PROTEIN
Title (de)
TETRAHYDROBENZOISOXAZOLE- UND TETRAHYDROINDAZOLE-DERIVATE ALS MODULATOREN DER MITOTISCHE MOTOR-PROTEIN
Title (fr)
TÉTRAHYDROBENZO-ISOXAZOLE ET DÉRIVÉ DE TÉTRAHYDRO-INDAZOLE COMME MODULATEURS DE LA PROTÉINE MOTEUR MITOTIQUE
Publication
Application
Priority
- EP 2007010122 W 20071122
- DE 102006060598 A 20061221
Abstract (en)
[origin: DE102006060598A1] Tetrahydrobenzoisoxazole compounds (I) and their derivatives, solvates, tautomers, salts and/or stereoisomers, are new. Tetrahydrobenzoisoxazole compounds of formula (I) and their derivatives, solvates, tautomers, salts and/or stereoisomers, are new. A 1>, A 2>N, O or S; X 1>-X 3>single bond, NR 3>-NR 3>, NR 3>, O, S, piperazine unit of formula (a), piperidine unit of formula (b) or cyclohexane unit of formula (c); Y 1>C=O, SO, SO 2, (CR 1> 2) n or 2,4-dimethyl-4,5-dihydro-oxazole; Cy : H or carbocyclic or heterocyclic, optionally saturated or aromatic residue (optionally substituted by alkyl, hal, CN, OH, OR, OCF 3, CF 3, COOR or (CR 1> 2) n-Y 1>-X 1>-(CR 1> 2) n-Q); Q : H, (cyclo)alkyl or (hetero)aryl; R, R 1>-R 3>H, alkyl, hal, alkoxy, OH, alkenyl, alkoxyalkyl, hydroxyalkyl, (CH 2) n-Q, (CH 2) n-Cy or (CH 2) nNR 2; hal : F, Br or Cl; n : 0-8; m : 1 or 2; and p : 0-2. Independent claims are included for: (1) the preparation of (I); and (2) a mixture containing one or more phenyl compound of formula (V) or its analog and/or metabolite. Y 2>, Z 2>O or N; R 9>, R 1> 0>H, OH, halo, O(1-10C alkyl), OCF 3, NO 2 or NH 2; R 8>, R 1> 1>-C(=NH)(NH 2), -C(=NOH)(NH 2), 4,5-dihydro-1H-imidazole-2-yl, 1-methyl-4,5-dihydro-1H-imidazole-2-yl, 1H-tetrazole-5-yl or -(=NOH)(NH 2), at the meta- or para position; and s : 2-6. [Image] [Image] ACTIVITY : Cytostatic. MECHANISM OF ACTION : Mitotic motor protein Eg5 modulator.
IPC 8 full level
C07D 231/54 (2006.01); A61K 31/416 (2006.01); A61K 31/423 (2006.01); A61K 31/454 (2006.01); A61K 31/5377 (2006.01); A61P 35/00 (2006.01); C07D 261/20 (2006.01); C07D 413/04 (2006.01); C07D 413/06 (2006.01); C07D 413/12 (2006.01); C07D 413/14 (2006.01)
CPC (source: EP US)
A61P 35/00 (2017.12 - EP); A61P 35/02 (2017.12 - EP); C07D 231/56 (2013.01 - EP US); C07D 261/20 (2013.01 - EP US); C07D 333/72 (2013.01 - EP US); C07D 413/04 (2013.01 - EP US); C07D 413/06 (2013.01 - EP US); C07D 413/12 (2013.01 - EP US); C07D 413/14 (2013.01 - EP US)
Citation (search report)
See references of WO 2008080455A1
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC MT NL PL PT RO SE SI SK TR
DOCDB simple family (publication)
DE 102006060598 A1 20080626; AU 2007341749 A1 20080710; CA 2673428 A1 20080710; EP 2104664 A1 20090930; JP 2010513335 A 20100430; US 2010022530 A1 20100128; WO 2008080455 A1 20080710
DOCDB simple family (application)
DE 102006060598 A 20061221; AU 2007341749 A 20071122; CA 2673428 A 20071122; EP 07856223 A 20071122; EP 2007010122 W 20071122; JP 2009541799 A 20071122; US 52045107 A 20071122