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US 2009/0156593 A1Published application
Spirocyclic Azaindole Derivatives
AssigneeGrüNenthal GmbH
InventorsSaskia Zemolka, Stefan Schunk, Ellen Bergrath, Babette-Yvonne Kogel, Werner Englberger, Klaus Linz, Hans Schick
Life of this patent
Estimating the term…
Abstract
The invention relates to substituted azaindole derivatives, to methods for the production thereof, to medicaments containing said compounds and to the use of substituted azaindole derivatives for producing medicaments.
Claims18
Spirocyclic azaindole derivatives of the Formula I,
- wherein
- A denotes N or CR7-10, wherein at least once and at most twice A denotes N
- W denotes NR4
- X denotes NR17, O or S
- R1 and R2 independently of one another denote H;
- C1-5-alkyl, in each case saturated or unsaturated, branched or unbranched, monosubstituted or polysubstituted or unsubstituted;
- C3-8-cycloalkyl, in each case monosubstituted or polysubstituted or unsubstituted;
- or denote aryl, C3-8-cycloalkyl or heteroaryl bonded via C1-3-alkyl, in each case monosubstituted or polysubstituted or unsubstituted;
- or the radicals R1 and R2 together denote CH2CH2OCH2CH2, CH2CH2NR10CH2CH2 or (CH2)3-6,
- wherein R10 denotes H;
- C1-5-alkyl, in each case saturated or unsaturated, branched or unbranched, monosubstituted or polysubstituted or unsubstituted;
- C3-8-cycloalkyl, in each case monosubstituted or polysubstituted or unsubstituted;
- aryl or heteroaryl, in each case monosubstituted or polysubstituted or unsubstituted;
- or aryl, C3-8-cycloalkyl or heteroaryl bonded via C1-3-alkyl, in each case monosubstituted or polysubstituted or unsubstituted;
- C(O)phenyl, C(O)heteroaryl, C(O)C1-5-alkyl, in each case substituted or unsubstituted;
- R3 denotes C1-8-alkyl, in each case saturated or unsaturated, branched or unbranched, monosubstituted or polysubstituted or unsubstituted;
- C3-8-cycloalkyl, in each case monosubstituted or polysubstituted or unsubstituted;
- aryl or heteroaryl, in each case unsubstituted or monosubstituted or polysubstituted;
- aryl, heteroaryl or C3-8-cycloalkyl bonded via a C1-3-alkyl group, in each case unsubstituted or monosubstituted or polysubstituted;
- R4 denotes H;
- C1-5-alkyl, saturated or unsaturated, branched or unbranched, unsubstituted or monosubstituted or polysubstituted;
- aryl or heteroaryl, in each case substituted or unsubstituted;
- aryl, heteroaryl or cycloalkyl bonded via a C1-3-alkyl group, in each case monosubstituted or polysubstituted or unsubstituted;
- COR12;
- SO2R12,
- wherein R12 denotes H;
- C1-5-alkyl, in each case saturated or unsaturated, branched or unbranched, monosubstituted or polysubstituted or unsubstituted;
- C3-8-cycloalkyl, in each case saturated or unsaturated, monosubstituted or polysubstituted or unsubstituted;
- aryl or heteroaryl, in each case monosubstituted or polysubstituted or unsubstituted;
- or aryl, C3-8-cycloalkyl or heteroaryl bonded via C1-3-alkyl, in each case monosubstituted or polysubstituted or unsubstituted;
- OR13;
- NR14R15;
- R5 denotes ═O;
- H;
- COOR13, CONR13, OR13;
- C1-5-alkyl, saturated or unsaturated, branched or unbranched, unsubstituted or monosubstituted or polysubstituted;
- C3-8-cycloalkyl, saturated or unsaturated, unsubstituted or monosubstituted or polysubstituted;
- aryl or heteroaryl, unsubstituted or monosubstituted or polysubstituted;
- or aryl, C3-8-cycloalkyl or heteroaryl bonded via C1-3-alkyl, unsubstituted or monosubstituted or polysubstituted;
- R6 denotes H;
- F, Cl, NO2, CF3, OR3, SR13, SO2R13, SO2OR13, CN, COOR13, NR14R15;
- C1-5-alkyl, saturated or unsaturated, branched or unbranched, unsubstituted or monosubstituted or polysubstituted;
- C3-8-cycloalkyl, saturated or unsaturated, unsubstituted or monosubstituted or polysubstituted;
- aryl or heteroaryl, unsubstituted or monosubstituted or polysubstituted;
- or aryl, C3-8-cycloalkyl or heteroaryl bonded via C1-3-alkyl, unsubstituted or monosubstituted or polysubstituted;
- or R5 and R6 together denote (CH2)n where n=2, 3, 4, 5 or 6, wherein individual hydrogen atoms can also be replaced by F, Cl, Br, I, NO2, CF3, OR13, CN or C1-5-alkyl;
- R7, R8, R9 and R10 independently of one another denote
- H, F, Cl, Br, I, NO2, CF3, OR13, SR13, SO2R13, SO2OR13, CN, COOR13, NR14R15;
- C1-5-alkyl, C3-8-cycloalkyl, unsubstituted or monosubstituted or polysubstituted;
- aryl or heteroaryl, unsubstituted or monosubstituted or polysubstituted;
- or aryl, C3-8-cycloalkyl or heteroaryl bonded via C1-3-alkyl, unsubstituted or monosubstituted or polysubstituted;
- wherein R13 denotes H;
- C1-5-alkyl, in each case saturated or unsaturated, branched or unbranched, unsubstituted or monosubstituted or polysubstituted;
- C3-8-cycloalkyl, in each case saturated or unsaturated, unsubstituted or monosubstituted or polysubstituted;
- aryl or heteroaryl, unsubstituted or monosubstituted or polysubstituted;
- or aryl, C3-8-cycloalkyl or heteroaryl bonded via C1-3-alkyl, unsubstituted or monosubstituted or polysubstituted;
- R14 and R15 independently of one another denote H;
- C1-5-alkyl, in each case saturated or unsaturated, branched or unbranched, unsubstituted or monosubstituted or polysubstituted;
- or C3-8-cycloalkyl, in each case saturated or unsaturated, unsubstituted or monosubstituted or polysubstituted;
- aryl or heteroaryl, unsubstituted or monosubstituted or polysubstituted;
- or aryl, C3-8-cycloalkyl or heteroaryl bonded via
- C1-3-alkyl, unsubstituted or monosubstituted or polysubstituted;
- or R14 and R15 together denote CH2CH2OCH2CH2, CH2CH2NR16CH2CH2 or (CH2)3-6,
- wherein R16 denotes H;
- C1-5-alkyl, saturated or unsaturated, branched or unbranched, unsubstituted or monosubstituted or polysubstituted;
- R17 denotes H;
- C1-8-alkyl, saturated or unsaturated, branched or unbranched;
- COR12 or SO2R12
- in the form of the racemate;
- in the form of the enantiomers, diastereomers, mixtures of the enantiomers or diastereomers, or of an individual enantiomer or diastereomer;
- in the form of the bases and/or salts of physiologically compatible acids.
68 more elements
Dependencies are inferred from the claim text.