Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I:

##STR00001##

wherein R.sub.1 to R.sub.5 and X.sub.1 to X.sub.5 are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed.

Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I:

##STR00001##

wherein R.sub.1 to R.sub.5 and X.sub.1 to X.sub.5 are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed.

The present disclosure relates to HIF-2? inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2? scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

The present disclosure relates to HIF-2? inhibitors and methods of making and using them for treating cancer. Certain compounds were potent in HIF-2? scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and led to tumor size reduction and regression in 786-O xenograft bearing mice in vivo.

A quinone derivative is represented by general formula (1), (2), or (3). In general formulae (1), (2), and (3), R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.21, R.sup.22, R.sup.23, and R.sup.24 each represent, independently of one another, a hydrogen atom, a cyano group, a halogen atom, an optionally substituted alkyl group having a carbon number of 1-6, or an optionally substituted alkoxy group having a carbon number of 1-6. R.sup.5, R.sup.6, R.sup.15, R.sup.16, R.sup.25, and R.sup.26 each represent, independently of one another, an optionally substituted alkyl group having a carbon number of 1-6, an optionally substituted alkoxy group having a carbon number of 1-6, an optionally substituted aryl group having a carbon number of 6-14, an optionally substituted aralkyl group having a carbon number of 7-12, or an optionally substituted cycloalkyl group having a carbon number of 3-10. ##STR00001##

A quinone derivative is represented by general formula (1), (2), or (3). In general formulae (1), (2), and (3), R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.21, R.sup.22, R.sup.23, and R.sup.24 each represent, independently of one another, a hydrogen atom, a cyano group, a halogen atom, an optionally substituted alkyl group having a carbon number of 1-6, or an optionally substituted alkoxy group having a carbon number of 1-6. R.sup.5, R.sup.6, R.sup.15, R.sup.16, R.sup.25, and R.sup.26 each represent, independently of one another, an optionally substituted alkyl group having a carbon number of 1-6, an optionally substituted alkoxy group having a carbon number of 1-6, an optionally substituted aryl group having a carbon number of 6-14, an optionally substituted aralkyl group having a carbon number of 7-12, or an optionally substituted cycloalkyl group having a carbon number of 3-10. ##STR00001##

Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein R.sub.1 to R.sub.5 and X.sub.1 to X.sub.5 are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed. ##STR00001##

Disclosed are compounds which are nuclear receptor modulators that can act as antagonists to the androgen receptor, for example, a compound of Formula I: wherein R.sub.1 to R.sub.5 and X.sub.1 to X.sub.5 are as described herein, as well as pharmaceutically acceptable salts, solvates, and stereoisomers thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment for cancers, including prostate cancers, other nuclear receptor mediated cancers, and other conditions, are also disclosed. ##STR00001##

Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor positive allosteric modulators (PAMS), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.

Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor positive allosteric modulators (PAMS), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.