Indolylmaleimide derivatives
OwnerRainer Albert, Nigel Cooke +7inventors
InventorsRainer Albert, Nigel Cooke, Sylvain Cottens, Claus Ehrhardt, Jean-Pierre Evenou, Richard Sedrani, Peter Von Matt, Jurgen Wagner, Gerhard Zenke
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Abstract
Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.
Claims4
1-11. (canceled)
A method for preventing or treating disorders or diseases mediated by lymphocytes and or PKC in a subject in need of such treatment, which method comprises administering to said subject an effective amount of a compound of formula I:
- wherein
- Ra is H;
- C1-4alkyl;
- or C1-4alkyl substituted by OH, NH2, NHC1-4alkyl or N(C1-4alkyl)2;
- Rb is H or C1-4alkyl;
- R is a radical of formula (b) or (c),
- wherein
- each of R4 and R7 is OH;
- SH;
- NR16R17 wherein each of R16 and R17, independently, is H or C1-4alkyl 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 and —NR19R20 wherein each of R19 and R20 independently is H,
- C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl, aryl-C1-4alkyl or C, 4alkyl optionally substituted on the terminal carbon atom by OH;
- each of R5and R6, independently, is H, halogen, C1-4alkyl, CF3, OH, SH, NH2, C1-4alkoxy, C1-4alkylthio, NHC1-4alkyl, N(C1-4alkyl)2 or CN;
- and
- ring A is optionally substituted,
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.