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US 2014/0005164 A1Published application
Wnt pathway antagonists
AssigneeSiena Biotech S.P.A.
InventorsMaurizio Varrone, Massimiliano Travagli, Giacomo Minetto, Lucia Cesari, Simone Galeazzi, Andrea Caricasole, Antonio Chiumiento, Massimiliano Salerno
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Abstract
The present invention relates to novel compounds of formula (I): as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.
Claims20
Compounds of formula I
- wherein, as valence and stability permit:
- any carbon-bound hydrogen atom may be substituted with a fluorine atom;
- X1 is CR2 or N;
- X2 is CR3 or N;
- -Y-Q is
- Q is C1-C6 linear branched or cylic alkyl, alkylcarbonyl, oxalkyl, dioxalkyl, alkylaminocarbonyl, oxalkylamminocarbonyl group wherein any methylene group may be substituted with an oxo group;
- a C5-C10 aryl or heteroaryl group optionally substituted with 1, 2 or 3 groups selected from the list of C1-C6 linear branched or cyclic alkyl, oxalkyl, alkylamino, alkylaminocarbonyl, oxalkylamino, oxalkyloxy, azalkyloxy, halogen, cyano, or a C5-C6 aryl or heteroaryl group optionally substituted with halogen, C1-C3 alkyl, C1-C3 oxalkyl;
- R1 is H;
- F;
- Cl;
- Br;
- OH;
- CN;
- linear branched or cyclic C1-C6 alkyl, alkenyl, alkynyl, oxalkyl, oxalkenyl, oxalkynil, azalkenyl, azalkynyl, alkyloxy, alkenyloxy, oxalkyloxy, dioxalkyloxy, oxazalkyloxy, azalkyloxy, dialkylamino, oxalkylamino, azalkylamino, group optionally substituted with one or more F or CN;
- C5-C6 aryl- or heteroarylmethylammino or C5-C6 aryl- or heterorylmethyloxy group where the aryl or heteroaryl moiety may optionally be substituted with one or more C1-C3 alkyl, C1-C3 alkoxy, halogen or CN groups;
- R2 is H or Cl;
- R3 is H, Cl or F;
- R4 is H or Cl;
- R5 is a C1-C3 linear, branched or cylic alkyl group;
- Rx is H;
- a linear, branched or cyclic C1-C3 alkyl group;
- n may be nil, 1, 2 or 3;
- Ry is—independently from one another when n=2 or more—F;
- a linear, branched or cyclic C1-C3 alkyl group;
- or Ry, together with the carbon atom to which it is attached, forms an oxo group.
- X3 is either N, O or S;
- tautomers, optical isomers and pharmaceutically acceptable salts thereof;
- with the exception of
25 more elements
Dependencies are inferred from the claim text.