Patent ID: 6583130
Filing Date: 2003-06-24
Classification: C07J

Abstract:
A C13-substituted estra-1,3,5(10)-trien-3-yl sulfamate of general formula I, whereinR1 represents COR3, COOR4, CONR5R6, SO2R4, SO2NR5R6, R2 represents hydrogen, C1-C10 alkyl, C1-C10 alkoxyalkyl, C3-C10 cycloalkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, aryl(C1-C3)alkyl, or C1-C3 alkylaryl, COR3; COOR4; CONR5R6; SO2R4; SO2NR5R6, R3 represents H or R4, R4 represents C1-C17 alkyl, C1-C17 haloalkyl, C2-C17 alkenyl, C2-C17 alkynyl, C3-C10 cycloalkyl, aryl, aryl(C1-C3)alkyl, C1-C3 alkylaryl, R5, R6 independently represent hydrogen, C1-C5 alkyl, C1-C5 haloalkyl, aryl, aryl(C1-C3)alkyl, C1-C3 alkylaryl, or, together with the nitrogen atom to which they are bound, form a polymethyleneimino residue having 2-6 C atoms or a morpholino residue, R7, R9 independently represent H, OH, halogen, C1-C5 alkoxy or C1-C5 haloalkoxy, R8 represents H, OH, C1-C5 alkyl, C1-C5 haloalkyl, C2-C5 alkenyl, C2-C5 alkynyl, or halogen, R10, R11 represent hydrogen, or R10 and R11 together represent a CH2 group, R12, R13, R14 independently represent H, OH, C1-C5 alkoxy, or C1-C5 haloalkoxy, or R12 represents halogen, or R13 and R14 together represent oxygen, or together represent a &boxH;CXY group wherein X and Y independently represent hydrogen, halogen or a C1-C5 alkyl group, or R13, R14 independently represent C1-C5 alkyl, C2-C5 alkenyl, or C2-C5 alkynyl, R15 represents ethyl, R8, R9, R10, R12, R13, R15 independently are in &agr; or &bgr; position, and up to 2 additional double bonds may be present in rings B and C, their physiologically tolerable salts or esters.