In one aspect, the invention relates to substituted 1-phenyl-3-(piperidin-4-yl)urea analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the DCN1-UBC12 interaction inhibitors of DCN1-mediated cullin-RING ligase activity, methods of making same, pharmaceutical compositions comprising same, methods of treating disorders using the disclosed compounds and compositions, methods of treating disorders associated with a DCN1-UBC12 interaction dysfunction, methods of treating disorders associated with a DCN1-mediated cullin-RING ligase activity dysfunction, methods of male contraception comprising the disclosed compounds and compositions, and kits comprising the disclosed compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

In one aspect, the invention relates to substituted 1-phenyl-3-(piperidin-4-yl)urea analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the DCN1-UBC12 interaction inhibitors of DCN1-mediated cullin-RING ligase activity, methods of making same, pharmaceutical compositions comprising same, methods of treating disorders using the disclosed compounds and compositions, methods of treating disorders associated with a DCN1-UBC12 interaction dysfunction, methods of treating disorders associated with a DCN1-mediated cullin-RING ligase activity dysfunction, methods of male contraception comprising the disclosed compounds and compositions, and kits comprising the disclosed compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

The invention provides compositions and methods for long term release of Gonadotropin-releasing hormone (GnRH) antagonists and uses thereof. Specifically, the invention provides polymer compositions and methods for controlled release of GnRH antagonists.

The invention provides compositions and methods for long term release of Gonadotropin-releasing hormone (GnRH) antagonists and uses thereof. Specifically, the invention provides polymer compositions and methods for controlled release of GnRH antagonists.

The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I. ##STR00001##

Novel compounds of Formula I

##STR00001##

and their use in therapeutic treatments.

The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula I:

##STR00001##

wherein W, X, Y, Z, R.sup.1, R.sup.2, R.sup.5, and R.sup.8 are as described herein.

The invention provides compositions and methods for long term release of Gonadotropin-releasing hormone (GnRH) antagonists, and uses thereof. Specifically, the invention provides polymer compositions and methods for controlled release of GnRH antagonists.

The invention provides compositions and methods for long term release of Gonadotropin-releasing hormone (GnRH) antagonists, and uses thereof. Specifically, the invention provides polymer compositions and methods for controlled release of GnRH antagonists.

The present invention provides for compounds of formula (I) wherein R.sup.1, R.sup.2, R.sup.6, Y.sup.1, Y.sup.3, A.sup.1, A.sup.2, A.sup.3 and A.sup.4 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I). ##STR00001##