Pyrrolidine derivatives pharmaceutically active as inhibitors of bax.

2001 
Pyrrolidine derivatives according to formula I (See formula) as well as its geometrical isomers, its optically active forms as enantiomers, diastereomers and its racemate forms, as well as pharmaceutically acceptable salts thereof, wherein X is selected from the group It is consisting of O, S, CR6R7; A is selected from the group consisting of - (C = O) -, - (C = O) -O-, - (C = NH) -, - (C = O) -NH-, - (C = S) NH-, -SO2-, -SO2NH-, -CH2-; B is either an amido group of the formula - (C = O) -NR8R9 or represents a heterocyclic residue having the formula (See formula) wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; m is an integer selected from 0, 1, 2 or 3; Y, Z and E form together with the 2 carbons to which they are attached a ring 5-6miembros aryl or heteroaryl; R1 is selected from the group comprising or consisting of C1-C6 alkyl unsubstituted or substituted C2-C6 unsubstituted or substituted C2-C6 unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl unsubstituted or substituted cycloalkyl, 3-8 membered saturated or unsaturated unsubstituted or substituted, acyl, C1-C6 alkyl unsubstituted or substituted aryl, heteroaryl C1-C6 alkyl unsubstituted or substituted and may be said cycloalkyl or aryl or heteroaryl groups fused 1-2 cycloalkyl or aryl or heteroaryl; R2, R3, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy; R6 and R7 are independently selected from the group comprising or consisting of hydrogen, C1-C6 alkyl unsubstituted or substituted C2-C6 unsubstituted or substituted C2-C6 unsubstituted or substituted, alkoxy unsubstituted or substituted, I thioalkoxy without unsubstituted or substituted, halogen, cyano, nitro, acyl, alkoxycarbonyl, aminocarbonyl, C 3-8-membered saturated or unsaturated unsubstituted or substituted which can contain 1 to 3 heteroatoms selected from N, O, S, unsubstituted or substituted aryl heteroaryl unsubstituted or substituted, C1-C6 unsubstituted or substituted aryl, C1-C6 alkyl unsubstituted or substituted heteroaryl; R8, R9 and R10 are independently selected from the group comprising or consisting of hydrogen, C1-C6 unsubstituted or substituted alkyl, C2-C6 unsubstituted or substituted C2-C6 unsubstituted or substituted 3-8 membered cycloalkyl saturated or unsaturated unsubstituted or substituted which may contain 1 to 3 heteroatoms selected from N, O, S, aryl unsubstituted or substituted heteroaryl, unsubstituted or substituted; or each pair R6, R7 and / or R8, R9 could form together with the nitrogen atom to which they are attached a heterocyclic ring or unsaturated 3 to 8 membered saturated unsubstituted or substituted which may contain 1-2 additional heteroatoms selected from N, O and S, and which is optionally fused with an aryl, heteroaryl or cycloalkyl of 3 to 8 membered saturated or unsaturated.
    • Correction
    • Source
    • Cite
    • Save
    • Machine Reading By IdeaReader
    0
    References
    0
    Citations
    NaN
    KQI
    []
    Baidu
    map