Estrane-based and androstane-based aminosteroid derivatives are described herein. More specifically, the following piperazinyl-steroid compounds of Formula I, Formula II, Formula III, and Formula IV are described. The compounds display cytotoxicity on a variety of cancer cell lines. A process for producing the compounds and their use in the manufacture of pharmaceutical formulations and/or combinations is also disclosed.

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Provided herein is a compound of Formula (I)

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or a pharmaceutically acceptable salt thereof, wherein ring D and the substituents are defined herein. Also provided are pharmaceutical compositions comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and methods of using the compound of Formula (I) in the treatment of CNS-related disorders.

Provided herein is a compound of Formula (I-I)

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or a pharmaceutically acceptable salt thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I-I), and methods of using the compounds, e.g., in the treatment of CNS-related disorders.

The present invention provides a compound having the structure:

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for use in combination with an anti-tuberculosis drug for treating a subject infected with M. tuberculosis.

The invention provides a novel, general, and facile strategy for the creation of small molecules with high structural and stereochemical complexity. Aspects of the methods include ring system distortion reactions that are systematically applied to rapidly convert readily available natural products to structurally complex compounds with diverse molecular architectures. Through evaluation of chemical properties including fraction of sp.sup.3 carbons, ClogP, and the number of stereogenic centers, these compounds are shown to be significantly more complex and diverse than those in standard screening collections. This approach is demonstrated with natural products (gibberellic acid, adrenosterone, and quinine) from three different structural classes, and methods are described for the application of this strategy to any suitable natural product.

Novel homo-aza-steroidal esters with alkylating bis(2-chloroethyl)aminophenoxy propanoic acid and substituted derivatives, processes for their preparation, pharmaceutical compositions containing them and use thereof in the treatment of cancer.

Novel chemical agents are described herein. More specifically, a novel inhibitor of 17?-HSD7 for decreasing estradiol concentrations while restoring dihydrotestosterone (DHT) concentrations in breast cancer cells is disclosed herein. In a particular embodiment, the inhibitor of 17?-HSD7 has the following structure: (Formula I) A process for producing the novel inhibitors of 17?-HSD7 and their use in the manufacture of pharmaceutical formulations and/or combinations is also disclosed.

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The present application discloses derivatives of steroids, pharmaceutically acceptable salts, stereoisomers or tautomers thereof, and processes for preparation thereof. The compounds and compositions described herein can be used in therapy.

The invention a novel, general, and facile strategy for the creation of small molecules with high structural and stereochemical complexity. Aspects of the methods include ring system distortion reactions that are systematically applied to rapidly convert readily available natural products to structurally complex compounds with diverse molecular architectures. Through evaluation of chemical properties including fraction of sp.sup.3 carbons, ClogP, and the number of stereogenic centers, these compounds are shown to be significantly more complex and diverse than those in standard screening collections. This approach is demonstrated with natural products (gibberellic acid, adrenosterone, and quinine) from three different structural classes, and methods are described for the application of this strategy to any suitable natural product.

Disclosed herein are novel sialyltransferase inhibitors, and compositions and methods for treating diseases and/or conditions associated with the activation of sialyltransferase, such as a cancer, an immune disease or an inflammatory disease.