Patent ID: 6015805
Filing Date: 2000-01-18
Classification: A61K,A61P,C07J

Abstract:
A hormonal or antihormonal steroid compound of structure II, ##STR11## wherein R.sup.1 is (R.sup.2 R.sup.3 N(O).sub.r)--, where r is 0 or 1 and R.sup.2 and R.sup.3 are each independently H, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl, any of which may be optionally substituted; or ##STR12## Y is --(CH.sub.2).sub.m -- where m is an integer of 0 to 5, or Y is --CH.sub.2).sub.n --Z--(CH.sub.2).sub.p -- where n is an integer of 0 to 2, p is an integer of 0 to 2, and Z is a heteroatom (optionally substituted) and where the CH.sub.2 groups may be optionally substituted; orR.sup.1 is N-imidazolyl-, N-pyrrolyl-, halo-, HO--, CF.sub.3 SO.sub.2 O--, C.sub.1-6 alkyl O--, C.sub.1-6 alkyl S--, C.sub.1-6 alkyl S(O)--, C.sub.1-6 alkyl S(O.sub.2)--, C.sub.1-6 alkyl CO--, C.sub.1-6 alkyl CH(OH)--, NC--, HCC--, C.sub.6 H.sub.5 CC--, 2'-furyl, 3'-turyl-, (2'-thiophenyl, 3'-thiophenyl-, 2'-pyridyl, 3'-pyridyl, 4'-pyridyl-, 2'-thiazolyl-, 2'-N-methylimidazolyl-, 5'-pyrimidinyl-, C.sub.6 H.sub.5 --, H.sub.2 C.dbd.CH--, C.sub.1-6 alkyl or MeC(.dbd.CH.sub.2)--; andR.sup.12 is H or halo; orR.sup.1 and R.sup.12 combine to form a ring ##STR13## where W is CH.sub.2, CH, NH, N, O, or S, and R.sup.4 is H or C.sub.1-6 alkyl; andX is O or NOR.sup.5, where R.sup.5 is H or C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.2 -6 alkenyl, C.sub.2-6 alkynyl, C.sub.6-12 aryl, or heteroaryl, any of which may be optionally substituted; orX is (H, H), (H, OH), (H, OSi(C.sub.1-6 alkyl).sub.3), or (H, OCOR.sup.5), where R.sup.5 is C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.6-12 aryl, aralkyl, aralkenyl, aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl or heteroaralkynyl, any of which may be optionally substituted; or ##STR14## where Y is --(CH.sub.2).sub.m -- where m is an integer of 0 to 3, or Y is --(CH.sub.2).sub.n --Z--(CH.sub.2).sub.p -- where n is an integer of 0 to 2, p is an integer of 0 to 2 and Z is a heteroatom (optionally substituted) or Z is a carbon atom substituted with one or two C.sub.1-6 alkyl groups;R.sup.6 is H, C.sub.1-6 alkyl, or halogen; andR.sup.8 is H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, or C.sub.2-6 alkynyl, C.sub.3-8 cycloalkyl, C.sub.6-12 aryl, aralkyl, aralkenyl, aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl or heteroaralkynyl, any of which may be optionally substituted, and pharmaceutically acceptable salts thereof.