4-PHENYL-5-OXO-1,4,5,6,7,8-HEXAHYDROCHINOLINE DERIVATIVES AS MEDICINES FOR INFERTILITY TREATMENT

摘要

1. The derivative of 2-methyl-4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline of the formula 1,! ! in which R1 represents (1-6C) alkyl, (2-6C) alkenyl or (2-6C) alkynyl; ! R2 is halogen; ! R3 is SO2NR5R6 or (1-4C) alkoxy optionally substituted with one or more fluorine atoms; ! X represents O or NR7; ! R4 is R8- (2-8C) alkyl, R8- (3-8C) alkenyl, R8- (3-8C) alkynyl or R8- (2-4C) alkoxy- (2-4C) alkyl; ! Z represents CN or NO2; ! R5 and R6 are independently H or (1-4C) alkyl; or ! R5 together with R6 and N to which they are attached form a 3-8 membered saturated ring, optionally containing an additional heteroatom selected from O and S; ! R8 is OH, (1-4C) alkoxy, NH2; NR9C (O) R11, NR9SO2R11 or C (O) NR9R10; ! R7 and R9 independently represent H or (1-4C) alkyl; ! R10 is (1-4C) alkyl, (1-4C) alkoxy (1-4C) alkyl, or phenyl (1-4C) alkyl or (2-5C) heteroaryl (1-4C) alkyl, both optionally substituted a (hetero) aromatic ring with one or more substituents selected from OH, NH2, halogen, NO2, CF3, CN, (1-4C) alkyl, (1-4C) alkoxy, and (di) (1-4C) alkylamino; ! R11 is (1-4C) alkyl, (2-4C) alkenyl, (2-4C) alkynyl, (1-4C) alkoxy (1-4C) alkyl, (3-6C) cycloalkyl, (1-4C) alkoxy , (di) (1-4C) alkylamino, or phenyl or (2-5C) heteroaryl, both optionally substituted on the (hetero) aromatic ring by one or more substituents selected from OH, NH2, halogen, NO2, CF3, CN, (1-4C) alkyl, (1-4C) alkoxy, and (di) (1-4C) alkylamino; or a pharmaceutically acceptable salt thereof. ! 2. The 2-methyl-4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivative of claim 1, wherein X is O.! 3. The 2-methyl-4-phenyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline derivative according to claim 1 or 2, wherein R1 is (1-6C) alkyl. ! 4. Derivative