PENTACYCLIC COMPOUNDS, INTERMEDIATES, PROCESSES, COMPOSITIONS, AND METHODS

摘要

The present invention relates to compounds of formulae (I) and (II) wherein X is -O-, -S-, or -NR5-; Y is -O-, -S-, -CH2-, -CH2CH2-, -CH=CH-, or -NR5-; B is -CH2- or -CO-; R1, R2, and R3 are each independently -H, -OH, -O(C1-C4 alkyl), -OCOC6H5, -OCO(C1-C6 alkyl), -OSO2(C4-C6 alkyl), -OSO2CF3, Cl, or F; n is 1 or 2; W is CH2 or C=O; R4 is 1-piperidinyl, 2-oxo-1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 2-oxo-1-pyrrolidinyl, 4morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; R5 is C1-C3 alkyl, -COC6H5, -CO(C1-C6 alkyl), -C(O)OC6H5, -C(O)O(C1-C6 alkyl), -SO2(C1-C6 alkyl), -SO2C6H5, or -SO2CF3; or a pharmaceutically acceptable salt thereof. Also provided by the present invention are intermediate compounds; processes for the preparation of compounds of formulae (I) and (II); and pharmaceutical methods and formulations employing the compounds of formulae (I) and (II).