Lipophilic benzothiophenes used for treating endometriosis

Details Lipophilic benzothiophenes used for treating endometriosis Lipophilic benzothiophenes used for treating endometriosis

1997-10-03

1998-10-27

Schenkman, Leonard

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

514324, 514422, 514443, A61K 3158, A61K 31445

Patent

active

058278443

ABSTRACT:
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.

REFERENCES:
patent: 4133814 (1979-01-01), Jones et al.
patent: 4418068 (1983-11-01), Jones
Haudenschild, Christian C., "Pathobiology of Restenosis After Angioplasty", American Journal of Medicine, 94, 40-44 (1993).
Wilensky, Robert L. et al., "Methods and Devices for Local Devices for Local Drug Delivery in Coronary and Peripheral Arteries", Trends Cardiovasc Med, 3, 163-170 (1993).
Waller, Bruce F. et al., "Morphologic Observations Late After Coronary Balloon Angioplasty: Mechanisms of Acute Injury and Relationship to Restenosis.sup.1 ", Radiology, 174,961-967 (1990).

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