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US 6,020,328 AGranted
20-keto-11.beta.-arylsteroids and their derivatives having agonist or antagonist hormonal properties
AssigneeResearch Triangle Institute
InventorsC. Edgar Cook, John A. Kepler, Ping-sheng Zhang, Yue-wei Lee, C. Ray Tallent
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Abstract
The invention is directed to 20-keto-11.beta.-arylsteroids of formula I: ##STR1## wherein R.sup.1, R.sup.6, R.sup.7, R.sup.9, R.sup.12 and X are as defined by the specification. The compounds exhibit progestational and antiprogestational activities.
Claims9
A hormonal or antihormonal steroid compound of structure I, ##STR17## wherein R.sup.1 is ##STR18## where q is 0 or 1, Y is --(CH.sub.2).sub.m -- where m is an integer of 0 to 5, optionally substituted;
- R.sup.12 is H or halo;
- ##STR19## where Y is --(CH.sub.2).sub.m -- where m is an integer of 0 through 3, R.sup.6 is H, CH.sub.3, or halogen;
- R.sup.7 is C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, or C.sub.2 -C.sub.4 alkynyl, any of which may be optionally substituted;
- or
- R.sup.7 is O--CO--R.sup.8 or O--R.sup.8 where R.sup.8 is C.sub.1 -C.sub.18 alkyl, C.sub.2 -C.sub.18 alkenyl, C.sub.2 -C18 alkynyl, C.sub.4 -C.sub.8 cycloalkyl, C.sub.6 -C.sub.12 aryl, aralkyl, aralkenyl, aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl or heteroaralkyl, any of which may be optionally substituted;
- and
- R.sup.9 is H, lower alkyl, alkenyl or alkynyl, halo, O--CO--R.sup.8 or O--R.sup.8 where R.sup.8 is as defined above, and pharmaceutically acceptable salts thereof.
4 more elements
Dependencies are inferred from the claim text.