Small molecule that mimics the binding of anti-EPPIN antibodies to EPPIN to provide male contraception, wherein the small molecule has one of the following formulas: and tautomers, and pharmaceutically-acceptable salts thereof, wherein: R 1 is -CH 2 R 5 , R 2 is H, C 1-8 alkyl, C 1-8 haloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, arylalkyl, alkylaryl, C(X)R 6 or C(X)XR 6 , R 3 is -NHR 7 , -C(X)NHR 7 , -NHC(X)R 7 , -NHC(X)XR 7 , -R 8 , or -C(X)R 8 ; R 4 is OR 7 or -C(X)OR 7 , R 5 is H, F, C 1-8 alkyl, C 1-8 haloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, arylalkyl, alkylaryl, -XC(X)XR 6 , C(X)XR 6 , or C(X)R 6 , R 6 and R 7 are H, C 1-8 alkyl, C 1-8 haloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, arylalkyl, or alkylaryl; R 8 is X is O, S, or NR 7 , Y is O, S, NR 7 , or C(R 7 ) 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 C 1-8 alkyl, C 1-8 substituted alkyl, C 2-8 alkenyl, C- 2-8 substituted alkenyl, heterocyclyl, substituted heterocyclyl, C 3-8 cycloalkyl, C 3-8 substituted cycloalkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, arylalkyl, substituted arylalkyl, halo, -OR 7 , -N(R 7 ) 2 , -CF 3 , -CN, -NO 2 , -C 2 R 7 , -SR 7 , -N 3 , -C(=O)N(R 7 ) 2 ,-NR 7 C(=O)R 7 , -C(=O)R 7 , -C(=O)OR 7 , -OC(=O)R 7 , -O(CR 6 R 7 ) r C(=O)R 7 -,-O(CR 6 R 7 ) r NR 7 C(=O)R 7 , -O(CR 6 R 7 ) r NR 7 SO 2 R 7 , -OC(=O)NR 6 R 7 ,-NR 7 C(=O)OR 7 , -SO 2 R 7 ,-SO 2 NR 6 R 7 , and -NR 7 SO 2 R 7 , 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 refers to the substituents described above, starting with halo and ending with -NR 7 SO 2 R 7 ; and tautomers, and pharmaceutically-acceptable salts thereof, wherein the compounds can exist as single stereoisomers or as mixtures of stereoisomers,-optionally wherein haloalkyl is mono-fluoromethyl, R 5 is F, -XC(X)XR 6 , or C(X)XR 6 , or one or more C=X moieties are carbonyl (C=O). R 1 is -CH 2 R 5 , R 2 is H, C 1-8 alkyl, C 1-8 haloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, arylalkyl, alkylaryl, C(X)R 6 or C(X)XR 6 , R 3 is -NHR 7 , -C(X)NHR 7 , -NHC(X)R 7 , -NHC(X)XR 7 , -R 8 , or -C(X)R 8 ; R 4 is OR 7 or -C(X)OR 7 , R 5 is H, F, C 1-8 alkyl, C 1-8 haloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, arylalkyl, alkylaryl, -XC(X)XR 6 , C(X)XR 6 , or C(X)R 6 , R 6 and R 7 are H, C 1-8 alkyl, C 1-8 haloalkyl, C 2-8 alkenyl, C 2-8 alkynyl, aryl, arylalkyl, or alkylaryl; R 8 is X is O, S, or NR 7 , Y is O, S, NR 7 , or C(R 7 ) 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 C 1-8 alkyl, C 1-8 substituted alkyl, C 2-8 alkenyl, C- 2-8 substituted alkenyl, heterocyclyl, substituted heterocyclyl, C 3-8 cycloalkyl, C 3-8 substituted cycloalkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, arylalkyl, substituted arylalkyl, halo, -OR 7 , -N(R 7 ) 2 , -CF 3 , -CN, -NO 2 , -C 2 R 7 , -SR 7 , -N 3 , -C(=O)N(R 7 ) 2 ,-NR 7 C(=O)R 7 , -C(=O)R 7 , -C(=O)OR 7 , -OC(=O)R 7 , -O(CR 6 R 7 ) r C(=O)R 7 -,-O(CR 6 R 7 ) r NR 7 C(=O)R 7 , -O(CR 6 R 7 ) r NR 7 SO 2 R 7 , -OC(=O)NR 6 R 7 ,-NR 7 C(=O)OR 7 , -SO 2 R 7 ,-SO 2 NR 6 R 7 , and -NR 7 SO 2 R 7 , 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 refers to the substituents described above, starting with halo and ending with -NR 7 SO 2 R 7 ; and tautomers, and pharmaceutically-acceptable salts thereof, wherein the compounds can exist as single stereoisomers or as mixtures of stereoisomers,-optionally wherein haloalkyl is mono-fluoromethyl, R 5 is F, -XC(X)XR 6 , or C(X)XR 6 , or one or more C=X moieties are carbonyl (C=O). <EOS>