abstract |
1. A solid pharmaceutical composition for oral administration containing an indolyl maleimide derivative of the formula I! ! where! Ra is H, C1-C4 alkyl or C1-C4 alkyl substituted with OH, NH2, NH- (C1-C4) alkyl or N- (di (C1-C4) alkyl) 2,! Rb means H or C1-C4 alkyl,! R means a radical of the formula (a), (b), (c), (d), (e) or (f)! ! ! where! each R1, R4, R7, R8, R11 and R14 is OH, SH, a heterocyclic residue, NR16R17, where each R16 and R17 independently is H or C1-C4 alkyl, or R16 and R17 together with the nitrogen atom to which they are attached form heterocyclic radical, or radical of formula α! ! where X is a single bond, O, S or NR18, where R18 is H or C1-C4 alkyl,! Rc is C1-C4 alkylene or C1-C4 alkylene, in which one CH2 group is replaced by a CRxRy group, with one Rx and Ry being H and the other being CH3, each Rx and Ry is CH3, or Rx and Ry together form a -CH2- group CH2-, and! Y is bonded to the terminal carbon atom and is selected from the group consisting of OH, a heterocyclic residue, and —NR19R20, where each R19 and R20 independently means H, C3-C6 cycloalkyl, C3-C6 cycloalkyl (C1-C4) alkyl, aryl (C1-C4) alkyl or C1-C4 alkyl optionally substituted at the terminal carbon atom with an OH group, or R19 and R20 together with the nitrogen atom to which they are attached form a heterocyclic radical,! each R2, R3, R5, R6, R9, R10, R12, R13, R15 and R'15 independently means H, halogen, C1-C4 alkyl, CF3, OH, SH, NH2, C1-C4 alkoxy, C1-C4 alkylthio, NH - (C1-C4) alkyl, N- (di (C1-C4) alkyl) 2 or CN,! or E means -N = and G means -CH = or E means -CH = and G means -N =, a! cycle A is optionally substituted,! in free form or in the form of a pharmaceutically acceptable salt. ! 2. The composition according to claim 1, containing 20-70 wt.% Derived indolylmaleimide calculated on the total m |