Disclosed are novel compounds of specific chemical structures having inhibitory activity on c-Myc/Max/DNA complex formation or pharmaceutically acceptable salts thereof.

The invention provides certain bicyclic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X.sup.1, X.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT. ##STR00001##

The invention provides certain bicyclic heterocyclic compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein X.sup.1, X.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT. ##STR00001##

A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: ##STR00001##
wherein X is N, C(OH), or CH;
Y is H or OH;
each of Z.sup.1-Z.sup.5 is independently H or halogen;
R.sup.4 is H, OH, NH.sub.2, NHR.sup.8, NR.sup.8R.sup.9 or R.sup.8;
R.sup.5, R.sup.6, and R.sup.7 is each independently H, halogen, OR.sup.8, R.sup.8, NHR.sup.8, NR.sup.8R.sup.9, CO.sub.2R.sup.8, CONR.sup.8R.sup.9, SO.sub.2NR.sup.8R.sup.9, or R.sup.5 and R.sup.6 together with the carbon atoms to which R.sup.5 and R.sup.6 are attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; and
R.sup.8 and R.sup.9 is each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or R.sup.8 and R.sup.9 together with the nitrogen to which R.sup.8 and R.sup.9 are attached form an optionally-substituted heterocycle.

A method of inhibiting drug-resistant HIV-1 integrase in a subject comprising administering to a subject in need thereof a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or ester thereof, having a structure of: ##STR00001##
wherein X is N, C(OH), or CH;
Y is H or OH;
each of Z.sup.1-Z.sup.5 is independently H or halogen;
R.sup.4 is H, OH, NH.sub.2, NHR.sup.8, NR.sup.8R.sup.9 or R.sup.8;
R.sup.5, R.sup.6, and R.sup.7 is each independently H, halogen, OR.sup.8, R.sup.8, NHR.sup.8, NR.sup.8R.sup.9, CO.sub.2R.sup.8, CONR.sup.8R.sup.9, SO.sub.2NR.sup.8R.sup.9, or R.sup.5 and R.sup.6 together with the carbon atoms to which R.sup.5 and R.sup.6 are attached form an optionally-substituted carbocycle or optionally-substituted heterocycle; and
R.sup.8 and R.sup.9 is each independently H, optionally-substituted alkyl, optionally-substituted alkenyl, optionally-substituted alkynyl, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted cycloalkylene, optionally-substituted heterocycle, optionally-substituted amide, optionally-substituted ester, or R.sup.8 and R.sup.9 together with the nitrogen to which R.sup.8 and R.sup.9 are attached form an optionally-substituted heterocycle.

Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (II):

##STR00001##

The present methods include administering to a subject an effective amount of one or more compounds of Formula (II). In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.

Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (I):

##STR00001##

The present methods include administering to a subject an effective amount of one or more compounds of Formula (I). In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.

The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of USP30, and the treatment of USP30-mediated disorders.

Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.

Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.