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US 2008/0076784 A1Published application
Bicyclic, Nitrogen-Containing Heterocycles and Aromatase Inhibitors
OwnerPeter Herold, Robert Mah +3inventors
InventorsPeter Herold, Robert Mah, Vincenzo Tschinke, Christoph Schumacher, Michael Quirmbach
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Abstract
The application relates to novel heterocyclic compounds of the general formula (I) (I*) in which R, R1, R2, X, Y, Z and n have the meanings defined in the description, to a process for their preparation and to the use of these compounds as medicaments, in particular as aromatase inhibitors.
Claims17
Compound of the general formula
- in which,
- X is C;
- Y is C or N;
- Z is C;
- R
- a) is hydrogen;
- or
- b) is C1-C8-alkyl, C1-C8-alkoxy, halogen or trifluoromethyl;
- R1 is aryl-C0-C4-alkyl or unsaturated heterocyclyl-C0-C4-alkyl, which radicals are unsubstituted or substituted by 1-4 C1-C8-alkoxy, C1-C8-alkoxycarbonyl, C1-C8-alkyl, C0-C8-alkylcarbonyl, C1-C8-alkylsulfonyl, aryl-C0-C4-alkoxycarbonyl, aryl, cyano, halogen, heterocyclyl, oxo, trifluoromethoxy, trifluoromethyl or tri-C1-C4-alkylsilyl;
- R2
- a) is hydrogen;
- or
- b) is C1-C8-alkyl, C3-C8-cycloalkyl, halogen, carboxy-C1-C4-alkyl, C1-C4-alkoxycarbonyl-C1-C4-alkyl, C0-C4-alkylcarbonyl, aryl-C0-C4-alkyl or unsaturated heterocyclyl-C1-C4-alkyl, which radicals are unsubstituted or substituted by 1-4 C1-C8-alkoxy, C1-C8-alkoxycarbonyl, C1-C8-alkyl, C0-C8-alkylcarbonyl, C1-C8-alkylsulfonyl, aryl-C0-C4-alkoxycarbonyl, aryl, cyano, halogen, heterocyclyl, oxo, trifluoromethoxy, trifluoromethyl or tri-C1-C4-alkylsilyl;
- n is a number 0, 1 or 2;
- whereby the term heterocyclyl stands for a saturated, partially saturated or unsaturated, 4-8-membered monocyclic ring system, for a saturated, partially saturated or unsaturated, 7-12-membered bicyclic ring system and also for a saturated, partially saturated or unsaturated, 7-12-membered tricyclic ring system, in each case comprising an N, O or S atom in at least one ring;
- * designates an asymmetric carbon atom
- and its salt, prodrug or compound in which one or more atoms are replaced by their stable, nonradioactive isotopes, in particular pharmaceutically usable salt,
- where, if X, Y and Z are C, R1 is not an unsubstituted or alkoxy-substituted benzyl radical;
- and excluding the compounds 5,6,7,8-tetrahydro-8-(4-pyridinyl)-isoquinoline and 5,6,7,8-tetrahydro-8-(4-pyridinyl)-isoquinoline.
16 more elements
8-9. (canceled)
Dependencies are inferred from the claim text.