BJERGARDE, KRISTEN,DODSON, MARK,MAUGER, JACQUES,NAIR, ANIL,PATEK, MARCEL,TABART, MICHEL
申请号：
PE0002962012
公开号：
PE11522012A1
申请日:
2007.11.09
申请国别(地区):
PE
年份:
2012
代理人:
摘要：
Refers to a compound of formula I, where r - L - IS II x1, X2, X3 and X4 are each cr 5 5 R IS h, F, is piridilo phenyl, substituted or unsubstituted with F, CL, sedan, c1-c6 alkyl, etc. L nh-co-nh or co NH r1 is h, X is o, NH R3 is H, alkyl of C1 - C6 R4A is H, c1-c4 alkyl r4b is H, alkyl C1 - C4 R5 is H, halogen.Preferred compounds are: trifluoroacetate (4 - [3 - [(2-fluorophenyl) Carbamoyl] amino} benzyl) amino] - 1H pyrazole-3-carboxamide trifluoroacetate 4 - [3 - ({{[2-fluoro-3 - (trifluoromethyl) phenyl] amino} Carbamoyl) benzyl] amino} - 1H pyrazole-3-carboxamide among others.These compounds are inhibitors of KDR (kinase insert Domain receptor (Tie2) and endothelial cell specific tyrosine kinase) useful in the treatment of cancerREFERIDA A UN COMPUESTO DE FORMULA I, DONDE Ar-L-A ES II X1, X2, X3 Y X4 SON CADA UNO CR5 R5 ES H, F A ES FENILO, PIRIDILO SUSTITUIDO O NO CON F, Cl, SF5, ALQUILO C1-C6, ENTRE OTROS L ES NH-CO-NH, O-CO-NH R1 ES H X ES O, NH R3 ES H, ALQUILO C1-C6 R4a ES H, ALQUILO C1-C4 R4b ES H, ALQUILO C1-C4 R5 ES H, HALOGENO. SON COMPUESTOS PREFERIDOS: TRIFLUOROACETATO DE 4-[(3-{[(2-FLUOROFENIL)CARBAMOIL]AMINO}BENCIL)AMINO]-1H-PIRAZOL-3-CARBOXAMIDA TRIFLUOROACETATO DE 4-{[3-({[2-FLUORO-3-(TRIFLUOROMETIL)FENIL]CARBAMOIL}AMINO)BENCIL]AMINO}-1H-PIRAZOL-3-CARBOXAMIDA ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DE KDR (RECEPTOR CON DOMINIO DE INSERCION QUINASA) Y TIE2 (TIROSINA QUINASA ESPECIFICO DE CELULAS ENDOTELIALES) UTILES EN EL TRATAMIENTO DE CANCER
