abstract |
The present invention relates to 16-hydroxy-11- (substituted phenyl) -estra-4,9-diene derivative of formula (I) or a pharmaceutically acceptable salt or solvate thereof, a preparation method thereof, a pharmaceutical preparation and medical treatment containing the same, In particular it relates to the use thereof in the treatment or prevention of glycocorticoid dependent diseases or symptoms.n n n Formula In n n n n n n n Wheren n n R 1 is C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkoxy, triflate, pyridyl or phenyl, wherein the phenyl moiety is optionally selected from cyano, halogen and C 1-4 alkyl Substituted with one or more substituents;n n n R 2 is hydrogen, C 1-6 alkyl, 1-oxo-C 1-6 alkyl or carboxy-1-oxo-C 1-6 alkyl;n n n R 3 is hydrogen, halogen or, C 1-6 alkoxy and by at least one substituent selected from halogen, optionally substituted C 1-6 alkyl;n n n R 4 is hydrogen, C 1-6 alkyl, 1-oxo-C 1-6 alkyl or carboxy-1-oxo-C 1-6 alkyl;n n n X is (H, OH), O or NOH. |