SUBSTITUTED DIBENZO-AZEPINE DERIVATIVES

THE PRESENT INVENTION RELATES TO COMPOUNDS OF THE GENERAL FORMULA (FORMULA I)WHEREINR1 IS -(CHR')q-ARYL OR -(CHR')q-HETEROARYL, WHICH ARE UNSUBSTITUTED OR MONO, DI- OR TRI-SUBSTITUTED BY LOWER ALKYL, LOWER ALKOXY, CF3 OR HALOGEN, OR IS LOWER ALKYL, LOWER ALKNEYL, -(CH2)n-Si(CH3)3 -(CH2)n-O...

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Hauptverfasser: ALEXANDER FLOHR, WOLFGANG WOSTL, JENS-UWE PETERS, GUIDO GALLEY, ROLAND JAKOD-ROETNE, ERIC ARGIRIOS KITAS
Format: Patent
Sprache:eng
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Zusammenfassung:THE PRESENT INVENTION RELATES TO COMPOUNDS OF THE GENERAL FORMULA (FORMULA I)WHEREINR1 IS -(CHR')q-ARYL OR -(CHR')q-HETEROARYL, WHICH ARE UNSUBSTITUTED OR MONO, DI- OR TRI-SUBSTITUTED BY LOWER ALKYL, LOWER ALKOXY, CF3 OR HALOGEN, OR IS LOWER ALKYL, LOWER ALKNEYL, -(CH2)n-Si(CH3)3 -(CH2)n-O-LOWER ALKYL, -(CH2)n-S-LOWER ALKYL, -(CH2)q-CYCLOALKYL, -(CH2)n-[CH(OH)]m-(CF2)p-CHqF(3-q), OR IS -(CH2)n-CR2-CF3, WHEREIN THE TWO R RADICALS FORM TOGETHER WITH THE CARBON ATOM A CYCLOALKYL RING; R' IS HYDROGEN OR LOWER ALKYL; n IS 1, 2 OR 3;m IS 0 OR 1;p IS 0, 1, 2, 3, 4, 5 OR 6;q IS 0, 1, 2 OR 3;R2 IS HYDROGEN OR LOWER ALKYL;R3 IS HYDROGEN, LOWER ALKYL, -CH2CF2CF3, CH2CF3, (CH2)2CF3, CF3, CHF2, CF3, CHF2, CH2F, OR IS ARYL, OPTIONALLY MONO, DI OR TRI-SUBSTITUTED BY HALOGEN, OR IS -(CH2)nNR5R6, WHEREIN R5 AND R6 ARE INDEPENDENTLY FROM EACH OTHER HYDROGEN OR LOWER ALKYL; R4 IS ONE OF THE FOLLOWING GROUPSWHEREIN@R7 IS HYDROGEN, LOWER ALKYL, -(CH2)n-CF3 OR -(CH2)n-CYCLOALKYL;R8 IS HYDROGEN, LOWER ALKYL, -C(O)-PHENYL, -C(O)-LOWER ALKYL, -C(O)O-(CH2)n-CYCLOALKYL, -C(O)O-(CH2)n-LOWER ALKYL, -C(CH2)n-LOWER ALKYL OR -C(O)NH-(CH2)n-CYCLOALKYL; R9 IS HYDROGEN, LOWER ALKYL, -(CH2)n-CYCLOALKYL OR -(CH2)n-CF3; AND TO PHARMACEUTICALLY SUITABLE ACID ADDITION SALTS, OPTIONALLY PURE ENANTIOMERS, RACEMATES OR DIASTEREOMERIC MIXTURES THEREOF FOR THE TREATMENT OF ALZHEIMER'S DISEASE..