Patent ID: 6794373
Filing Date: 2004-09-21
Classification: A61K,A61P

Abstract:
A method of contraception, which comprises administering to a female of child bearing age over a period of 28 consecutive days:a) a first phase of from 18 to 21 daily dosage units of a progestational agent equal in progestational activity to about 35 to about 150 &mgr;g levonorgestrel, and ethinyl estradiol at a daily dose range of from about 10 to about 35 &mgr;g; b) a second phase of from 1 to 7 daily dosage units of a daily dose of from about 2 to 50 mg of an antiprogestin of the formula: wherein:A is O, S, or NR4; B is a bond between A and C&boxH;O, or the moiety CR5R6; R4, R5, and R6 are independently selected from the group consisting of H, C1 to C6 alkyl, substituted C1 to C6 alkyl, C2 to C6 alkenyl, substituted C2 to C6 alkenyl, C2 to C6 alkynyl, substituted C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8cycloalkyl, aryl, substituted aryl, heterocyclic, and substituted heterocyclic; or R4 and R5 are fused to form a 5 to 7 membered ring; R1 is selected from the group consisting of H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C3 to C6 alkenyl, alkynyl, substituted alkynyl, and CORA; RA is selected from the group consisting of H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, and substituted C1 to C3 aminoalkyl; R2 is selected from the group consisting of H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, C1 to C6 aminoalkyl, and substituted C1 to C6 aminoalkyl; R3 is selected from the group consisting of (i) and (ii): (i) a substituted benzene ring having the substituents X, Y and Z and of the formula: X is selected from the group consisting of halogen, CN, C1 to C3 alkyl, substituted C1 to C3 alkyl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 thioalkoxy, substituted C1 to C3 thioalkoxy, C1 to C3 aminoalkyl, substituted C1 to C3 aminoalkyl, NO2, C1 to C3 perfluoroalkyl, 5 or 6 membered heterocyclic ring having in its backbone 1 to 3 heteroatoms, CORB, OCORB, and NRCCORB; RB is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; RC is H, C1 to C3 alkyl, or substituted C1 to C3 alkyl; Y and Z are independent substituents selected from the group consisting of H, halogen, CN, NO2, C1 to C3 alkoxy, C1 to C3 alkyl, and C1 to C3 thioalkoxy; and (ii) a five or six membered ring having it its backbone 1, 2, or 3 heteroatoms selected from the group consisting of O, S, SO, SO2 and NR7 and having one or two independent substituents selected from the group consisting of H, halogen, CN, NO2, C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aminoalkyl, CORD, and NRECORD; RD is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy, substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; RE is H, C1 to C3 alkyl, or substituted C1 to C3 alkyl; R7 is H or C to C3 alkyl; or a pharmaceutically acceptable salt thereof, and c) optionally, an orally and pharmaceutically acceptable placebo for each remaining day of the 28 consecutive days.