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US 2008/0187582 A1Published application
Pharmaceutical Composition Comprising an Indolylmaleimide Derivative
OwnerPatrice Guitard, Marie-Christine Wolfinventors
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Abstract
The application relates to solid pharmaceutical compositions suitable for oral administration comprising a water sensitive drug, preferably an indolylmaleimide derivative, process for their production and use of the pharmaceutical compositions.
Claims28
A solid pharmaceutical composition suitable for oral administration comprising an indolylmaleimide derivative of formula I
- wherein
- Ra is H;
- C1-4alkyl;
- or C1-4alkyl substituted by OH, NH2, NHC1-4alkyl or N(di-C1-4alkyl)2;
- Rb is H;
- or C1-4alkyl;
- R is a radical of formula (a), (b), (c), (d), (e) or (f)
- wherein
- each of R1, R4, R7, R8, R11 and R14 is OH;
- SH;
- a heterocyclic residue;
- NR16R17 wherein each of R16 and R17, independently, is H or C1-4alkyl or R16 and R17 form together with the nitrogen atom to which they are bound a heterocyclic residue;
- or a radical of formula α
- —X—Rc—Y (α)
- wherein X is a direct bond, O, S or NR18 wherein R18 is H or C1-4alkyl,
- Rc is C1-4alkylene or C1-4alkylene wherein one CH2 is replaced by CRxRy wherein one of Rx and Ry is H and the other is CH3, each of Rx and Ry is CH3 or Rx and Ry form together —CH2—CH2—, and
- Y is bound to the terminal carbon atom and is selected from OH, a heterocyclic residue and —NR19R20 wherein each of R19 and R20 independently is H, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl, aryl-C1-4alkyl or C1-4alkyl optionally substituted on the terminal carbon atom by OH, or R19 and R20 form together with the nitrogen atom to which they are bound a heterocyclic residue;
- each of R2, R3, R5, R6, R9, R10, R12, R13, R15 and R′15, independently, is H, halogen, C1-4alkyl, CF3, OH, SH, NH2, C1-4alkoxy, C1-4alkylthio, NHC1-4alkyl, N(di-C1-4alkyl)2 or CN;
- either E is —N═ and G is —CH═ or E is —CH═ and G is —N═;
- and
- in free form or in pharmaceutically acceptable salt.
18 more elements
(canceled)
Dependencies are inferred from the claim text.