Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1997-10-03
1998-09-22
Robinson, Allen J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514324, 514422, A61K 3140, A61K 3158, A61K 31445
Patent
active
058114157
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.
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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 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).
Cullinan George Joseph
Kauffman Raymond Francis
Boone David E.
Eli Lilly and Company
Robinson Allen J.
Sales James J.
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