QUINAZOLINONE AND BENZOXAZINE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS

摘要

This invention provides compounds which are agonists and antagonists of the progesterone receptor having general structure (I): wherein R<1> and R<2> are independently selected from H, COR<A>, or NR<B>COR<A>, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, or heterocyclic moieties; or R<1> and R<2> are fused to form: 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic rings; R<A> is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl groups; R<B> is H, C1 to C3 alkyl or substituted C1 to C3 alkyl; R<3> is H, OH, NH2, COR<C> or optionally substituted alkyl, alkenyl, or alkynyl; R<C> is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; R<4> is H, halogen, CN, NO2, or optionally substituted alkyl, alkynyl, alkoxy, amino or aminoalkyl; R<5> is an optionally substituted benzene or five or six membered ring with 1, 2, or 3 heteroatoms selected from O, S, SO, SO2 or NR<6>; R<6> is H or C1 to C3 alkyl; G1 is O, NR7, or CR7R8; G2 is CO, CS, or CR7R8; provided that when G1 is O, G2 is CR7R8, and G1 and G2 cannot both be CR7R8; R7 and R8 are H or an optionally substituted alkyl, aryl, or heterocyclic moiety; or pharmaceutically acceptable salt thereof, and methods using these compounds in mammals as agonists or antagonists of the progesterone receptor.