| 摘要 |
Oxo substituted quinoline, isoquinoline and phthalazine derivatives are new. The oxo substituted quinoline, isoquinoline and phthalazine derivatives are compounds of formula (I) and their stereoisomers and acid addition and base salts: [Image] R 1>-CO-R 1>1>; CN; -CO-OR 1>2>; -CO-NR 1>2>R 1>3>; -SO x-R 1>2>; -SO 2-NR 1>2>R 1>3>; -or A-NR 1>4>-CO-NR 1>5>R 1>6>; R 2>-CH(R 2>1>)(R 2>2>; or -CH 2CH(R 2>3>)(R 2>4>; R 3>H; halo; or 1-10C alkyl; R 4>H; or 1-10C alkyl; R 5>: R 6>-CH 2-N(R 6>1>)R 6>2>; W-X-Y : : R 1>1>and R 1>2>saturated, unsaturated, cyclic or/and (hetero)aromatic organic group; R 1>3>H; or 1-10C alkyl; A : 1-4C alkylene optionally mono-substituted with 1-6C alkyl; CO; O; or -SO x-; R 1>4>and R 1>5>H; or 1-10C alkyl; R 1>6>1-10C alkyl; 3-10C cycloalkyl; 7-20C cycloalkylalkyl; or 7-20C aralkyl, phenyl or heterocyclyl each optionally substituted with alkyl or aryl (substitution is in the ring in the case of aralkyl); x : 0-2; R 2>1>H; 1-10C alkyl; or optionally substituted phenyl; R 2>2>phenyl or naphthyl each optionally substituted; R 2>3>and R 2>4>optionally substituted phenyl; G : -C=C-; -C=N-; -N=C-; O; or S; Z : direct bond; O; S; CH-R 5>2>; CHR 5>2>-CH-R 5>3>; -CC-; or -CR 5>2>=CR 5>3>or C=R 5>2>R 5>3>each with the E or Z configuration; R 5>1>amino optionally mono-substituted with alkyl; or alkyl or 3-7C cycloalkyl each optionally substituted with halo, OH or alkoxy; L : CH 2; or NH; Q : CO; or -SO x-; R 5>2>and R 5>3>H; or alkyl; R 6>1>H; or alkyl; R 6>2>alkyl; or aralkyl or 7-20C heteroaralkyl each optionally substituted; n (not listed in above definitions) : 1 or 2. An independent claim is also included for the preparation of compounds (I). ACTIVITY : Gynecological; Cytostatic. MECHANISM OF ACTION : Gonadotrophin-releasing hormone (GnRH) antagonist. |
