Lipophilic benzothiophenes
AssigneeEli Lilly and Company
InventorsGeorge Joseph Cullinan, Raymond Francis Kauffman
Life of this patent
Estimating the term…
Loading patent…
AssigneeEli Lilly and Company
InventorsGeorge Joseph Cullinan, Raymond Francis Kauffman
Estimating the term…
The invention provides novel benzothiophenes of the formula (I): ##STR1## wherein R.sub.1 is N-pyrrolidinyl or N-piperidinyl; R.sub.2 and R.sub.3 are independently hydrogen,--CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), --CO--(C.sub.10 -C.sub.22 alkynyl),or --CO--(CH.sub.2).sub.n COR.sub.4 ; provided R.sub.2 and R.sub.3 are not both dodecanoyl, and one of R.sub.2 or R.sub.3 is not hydrogen R.sub.4 is -3-cholesteryl or --O(CH.sub.2).sub.2 (OR.sub.5)CH.sub.2 OR.sub.6 ; R.sub.5 and R.sub.6 are independently hydrogen, --CO--(C.sub.10 -C.sub.22 alkyl), --CO--(C.sub.10 -C.sub.22 branched alkyl), --CO--(C.sub.10 -C.sub.22 alkenyl), --CO--(C.sub.10 -C.sub.22 polyalkenyl), or --CO--(C.sub.10 -C.sub.22 alkynyl); provided one of R.sub.5 or R.sub.6 is not hydrogen; n is 0-4; and pharmaceutically acceptable salts and solvates thereof. The present invention further provides pharmaceutical compositions containing compounds of formula I, and the use of such compounds.
A method for inhibiting estrogen-dependent cancer comprising administering to a human in need thereof a compound of formula (I):
Dependencies are inferred from the claim text.