Small molecules for inhibiting male fertility

A method of providing contraception, comprising administering an effective amount of a compound having one of the following formulas:

• and tautomers, and pharmaceutically-acceptable salts thereof,
• wherein:
• R1 is —CH2R5,
• R2 is H, C1-8 alkyl, C1-8 haloalkyl, C2-8 alkenyl, C2-8 alkynyl, aryl, arylalkyl, alkylaryl, C(X)R6 or C(X)XR6,
• R3 is —NHR7, —C(X)NHR7, —NHC(X)R7, —NHC(X)XR7, —R8, or C(X)R8;
• R4 is OR7 or —C(X)OR7,
• R5 is H, F, C1-8 alkyl, C1-8 haloalkyl, C2-8 alkenyl, C2-8 alkynyl, aryl, arylalkyl, alkylaryl, —XC(X)XR6, C(X)XR6, or C(X)R6,
• R6 and R7 are H, C1-8 alkyl, C1-8 haloalkyl, C2-8 alkenyl, C2-8 alkynyl, aryl, arylalkyl, or alkylaryl;
• R8 is
• X is O, S, or NR7,
• Y is O, S, NR7, or C(R7)2,
• Zj refers to j number of Z substituents, which substituents can be present at any carbon atom on the benzene ring, wherein j is 0, 1 or 2, each Z is, individually, a substituent species selected from the group consisting of C1-8 alkyl, C1-8 substituted alkyl, C2-8 alkenyl, C2-8 substituted alkenyl, C3-8 cycloalkyl, C3-8 substituted cycloalkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, arylalkyl, substituted arylalkyl, halo, —OR7, —N(R7)2, —CF3, —CN, —NO2, —C2R7, —SR7, —N3, —C(═O)N(R7)2, —NR7C(═O)R7, —C(═O)R7, —C(═O)OR7, —OC(═O)R7, —O(CR6R7)rC(═O)R7—, —O(CR6R7)rNR7C(═O)R7, —O(CR6R7)rNR7SO2R7, —OC(═O)NR6R7, —NR7C(═O)OR7, —SO2R7, —SO2NR6R7, and —NR7SO2R7,
• r is an integer from 1 to 6, and
• n is 0, 1, 2, or 3,
• the term “substituted” as applied to alkyl, aryl, cycloalkyl and the like refers to the substituents described above, starting with halo and ending with —NR7SO2R7;
• and tautomers, and pharmaceutically-acceptable salts thereof,
• wherein the compounds can exist as single stereoisomers or as mixtures of stereoisomers.