Patent ID: 6043235
Filing Date: 2000-03-28
Classification: A61P,C07J

Abstract:
A hormonal or antihormonal steroid compound of structure I ##STR7## wherein s is an integer from 0 to 2;R.sup.1 is 4-(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 ##STR8## where q is 0 or 1 and Y is --(CH.sub.2).sub.m - where m is an integer of 0 to 5, orY 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 methylene groups in both cases may be optionally substituted; orR.sup.1 is 4-halo-, 4-HO--, 4-CF.sub.3 SO.sub.2 O--, 4-CH.sub.3 O--, 4-CH.sub.3 S--, 4-CH.sub.3 S(O)--, 4-CH.sub.3 S(O).sub.2 --, 4-CH.sub.3 CO--, 4-CH.sub.3 CH(OH)--, 4-N--C--, 4-HC.ident.--C--, 4-C.sub.6 H.sub.5 C.ident.C--, 4-H.sub.2 C.dbd.CH--, 4-C.sub.2 H.sub.5 --, 4-MeC(.dbd.CH.sub.2)--, 4-C.sub.6 H.sub.5, 4-(N-imidazolyl)-, 4-(N-pyrrolyl)-, 4-(2'-furyl), 4-(3'-furyl)-, 4-(2'-thiophenyl), 4-(3'-thiophenyl)-, 4-(2'-pyridyl), 4-(3'-pyridyl), 4-(4'-pyridyl)-, 4-(2'-thiazolyl)-, 4(2'-N-methylimidazolyl)-, or 4-(5'-pyrimidinyl)-;R.sup.14 is H or halo; orR.sup.1 and R.sup.14 combine to form a ring ##STR9## where W is CH, CH.sub.2, N, NH, O, or S, and R.sup.4 is H, CH.sub.3, or C.sub.2 H,;X 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 -.sub.6 alkynyl, C.sub.6-12 aryl, or heteroaryl, any of which may be optionally substituted; orX is (H,H), (H,OH) or X is (H,OSi(C.sub.1-6 -alkyl).sub.3) or X is (H,OCOR.sup.5), where R.sup.5 is C.sub.2-6 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 ##STR10## 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 lower alkyl groups;R.sup.6 is H, C.sub.1-6 alkyl, or halogen;R.sup.8 and R.sup.9 are individually H, C.sub.1-18 alkyl, C.sub.2-18 alkenyl, C.sub.2-18 alkynyl, C.sub.4-8 cycloalkyl, C.sub.6-12 aryl, aralkyl, aralkenyl or aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl or heteroaralkynyl, any of which may be optionally substituted; andR.sup.10 is H, C.sub.1-18 alkyl, C.sub.2-18 alkenyl, C.sub.2-18 alkynyl, C.sub.4-8 cycloalkyl, C.sub.6-12 aryl, aralkyl, aralkenyl or aralkynyl, heteroaryl, heteroaralkyl, heteroaralkenyl or heteroaralkynyl, any of which may be optionally substituted; andR.sup.11 and R.sup.12 are .dbd.CH.sub.2 orR.sup.11 and R.sup.12 are each H;pharmaceutically acceptable salts thereof.