Novel n-substituted-pyrrolidines as inhibitors of mdm2-p-53 interactions

A compound of the formula

• wherein
• X is selected from the group consisting of H, F, Cl, Br, I, cyano, nitro, ethynyl, cyclopropyl, methyl, ethyl, isopropyl, vinyl and methoxy,
• Y is one to four group(s) independently selected from the group consisting of H, F, Cl, Br, I, CN, OH, nitro, lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aryl, heteroaryl, heterocycle, COOR′, OCOR′, CONR′R″, NR′COR″, NR″SO2R′, SO2NR′R″ and NR′R″ wherein
• R′ and R″ are independently selected from H, lower alkyl, substituted lower alkyl, lower cycloalkyl, substituted lower cycloalkyl, lower alkenyl, substituted lower alkenyl, lower cycloalkenyl, substituted lower cycloalkenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, or substituted heterocycle
• and in the case of R′ and R″ may independently link to form a cyclic structure selected from substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle,
• one of R1 and R2 is selected from the group consisting of lower alkyl,
• substituted lower alkyl, lower alkenyl, substituted lower alkenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, substituted heterocycle, cycloalkyl, substituted cycloalkyl, cycloalkenyl, and substituted cycloalkenyl and the other is hydrogen
• one of R3 and R4 is selected from the group consisting of lower alkyl, substituted lower alkyl, lower alkenyl, substituted lower alkenyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycle, substituted heterocycle, cycloalkyl, substituted cycloalkyl, cycloalkenyl, and substituted cycloalkenyl and the other is hydrogen,
• R5 is selected from the group consisting of lower alkyl, substituted lower alkyl, —CH2(CH2)n—CHOH—R′, —CH2(CH2)n—CHOH—CH2—(CH2)n—NR′R″, CH2(CH2)n—CO(CH2)nNR′R″, CO(CH2)n—R′, —CO(CH2)n—NR′—(CH2)n—CHOH—R′, —CO(CH2)n—NR′R″, (CH2)n—NR′SO2R″, —COCH2(CH2)n—COOH, (CH2)n—COOR′, (CH2)n—CONR′R″, —CO(CH2)n—OR′, —COCH2(CH2)n—SR′, —COCH2(CH2)n—SOR′, —COCH2(CH2)n—SO2R′, —COCH2(CH2)n—COR′, —COCH2(CH2)n—SO3H, —COCH2(CH2)n—SONR′R″, —COCH2(CH2)n—SO2NR′R″, —COCH2(CH2CH2O)m—(CH2)n—R′, —COCH2(CH2CH2O)m—(CH2)n—OH, —COCH2(CH2CH2O)m—(CH2)n—OR′, —COCH2(CH2CH2O)m—(CH2)n—NR′R″, —COCH2(CH2CH2O)m—(CH2)n—NR′COR″, —COCH2(CH2CH2O)m—(CH2)n—NR′SO2R″, —COCH2(CH2CH2O)m—(CH2)n—COOH, —COCH2(CH2CH2O)m—(CH2)n—COOR′, —COCH2(CH2CH2O)m—(CH2)n—CONR′R″, —COCH2(CH2CH2O)m—(CH2)n—SO2R′, —COCH2(CH2CH2O)m—(CH2)n—COR′, —COCH2(CH2CH2O)m—(CH2)n—SONR′R″, —COCH2(CH2CH2O)m—(CH2)n—SO2NR′R″, —COCH2(CH2)p—(CH2CH2O)m—(CH2)n—R′, —COCH2(CH2)p— (CH2CH2O)m—(CH2)n—OH, —COCH2(CH2)p—(CH2CH2O)m—(CH2)n—OR′, —COCH2(CH2)p—(CH2CH2O)m—(CH2)n—NR′R″, —COCH2(CH2)p—(CH2CH2O)m—(CH2)n—NR′COR′, —COCH2(CH2)p—(CH2CH2O)m—(CH2)n—NR′SO2R″, —COCH2(CH2)p—(CH2CH2O)m—(CH2)n—COOH, —COCH2(CH2)p—(CH2CH2O)m—(CH2)n—COOR′, —COCH2(CH2)p—(CH2CH2O)m—(CH2)n—CONR′R″, —COCH2(CH2)p—(CH2CH2O)m—(CH2)n—SO2R′, —COCH2(CH2)p—(CH2CH2O)m—(CH2)n—COR′, —COCH2(CH2)p—(CH2CH2O)m—(CH2)n—SONR′R″, —COCH2(CH2)p—(CH2CH2O)m—(CH2)n—SO2NR′R″, —COCH2—COR′, —COCH2—SOR′ and —COCH2SO2R′ wherein R′ and R″ are as above,
• m, n, and p are independently 0 to 6,
• and the pharmaceutically acceptable salts and esters thereof.