The present invention provides bivalent inhibitors of BET bromodomains, such as compounds of Formulae (I), (II), (III), (IV), (V) and (VI). Some bromdomain-containing proteins (e.g., BRD4) have a tandem bromodomain primary structure comprising more than one bromodomain binding site (e.g., BRD4 comprises BD1 and BD2). Bivalent inhibitors of BET bromodomains provided herein can target bromodomains through advantageous multivalent interactions, and can therefore can be to treat diseases comprising the inventive compounds, as well as methods of using the inventive compounds.

The present invention provides bivalent inhibitors of BET bromodomains, such as compounds of Formulae (I), (II), (III), (IV), (V) and (VI). Some bromdomain-containing proteins (e.g., BRD4) have a tandem bromodomain primary structure comprising more than one bromodomain binding site (e.g., BRD4 comprises BD1 and BD2). Bivalent inhibitors of BET bromodomains provided herein can target bromodomains through advantageous multivalent interactions, and can therefore can be to treat diseases comprising the inventive compounds, as well as methods of using the inventive compounds.

The present invention generally relates to a pharmaceutical dosage form and controlled release of biologically active agents, diagnostic agents, reagents, cosmetic agents, and agricultural/insecticide agents. In one embodiment, the dosage form has a substrate that forms a compartment, wherein the substrate includes at least a first piece and a second piece, wherein the first piece operably links to the second piece. The dosage form contains a drug content that is loaded into the compartment. The dosage form also has a releaser operably linked to the substrate which upon contact with water or body fluid is capable of separating the first and second piece to open the compartment and release the drug content.

The present invention provides for compounds of formula (I). wherein R.sup.x, R.sup.y, R.sup.x1, L.sup.1, G.sup.1, 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 comprised of one or more compounds of formula (I). ##STR00001##

The present invention provides for compounds of formula (I)

##STR00001##

wherein R1, R2, R6, Y1, Y2, Y3, A1, A2, A3, and A4 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).

The present invention provides for compounds of formula (I)

##STR00001##

wherein A.sup.1, A.sup.2, A.sup.3, A.sup.4, X.sup.1, X.sup.2, Y.sup.1, L.sup.1, G.sup.1, R.sup.x, and R.sup.y have any of the values defined thereof 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).

The present invention provides for compounds of formula (I) ##STR00001##
wherein Y.sup.1, Y.sup.2, R.sup.1, R.sup.2, R.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 for the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

This invention relates to an immunogen comprising a gonadotropin releasing hormone (GnRH) peptide sequence, a kisspeptin peptide sequence and a stimulant of raising an immune response, such an immunogen for use in a method to regulate the release of hormones in a vertebrate including modulation of reproductive hormones, to reduce fertility in a vertebrate and to treat hormone-dependent diseases including hormone-dependent tumours including prostate tumours, breast, ovary and endometrial tumours, benign hyperplasia including benign prostatic hyperplasia and uterine fibroids, endometriosis, polycystic ovarian disease, infertility, sexual dysfunction and any disorder that would benefit from an increased or decreased GnRH-dependent activity and a vaccine formulation comprising the immunogen. The invention also relates to the use of the immunogen in the preparation of a medicament for use in a method to regulate the release of hormones in a vertebrate.

This invention relates to an immunogen comprising a gonadotropin releasing hormone (GnRH) peptide sequence, a kisspeptin peptide sequence and a stimulant of raising an immune response, such an immunogen for use in a method to regulate the release of hormones in a vertebrate including modulation of reproductive hormones, to reduce fertility in a vertebrate and to treat hormone-dependent diseases including hormone-dependent tumours including prostate tumours, breast, ovary and endometrial tumours, benign hyperplasia including benign prostatic hyperplasia and uterine fibroids, endometriosis, polycystic ovarian disease, infertility, sexual dysfunction and any disorder that would benefit from an increased or decreased GnRH-dependent activity and a vaccine formulation comprising the immunogen. The invention also relates to the use of the immunogen in the preparation of a medicament for use in a method to regulate the release of hormones in a vertebrate.

The present disclosure relates to compositions and methods for inhibiting inflammation and reducing the risk of spreading sexually transmitted diseases using an alginic acid-based antimicrobial compound. Such compositions provide dual protection by (1) attacking and inactivating viruses and other microbes and (2) blocking the host response that viruses trigger to invade host cells. Such compositions can also be part of an acid buffering contraceptive.