C07J73/005

Enzyme compositions, steroid derivatives, enzyme inhibitors, and methods of making same for pharmaceutical applications

The present disclosure provides for a synthetic strategy to incorporate a C12α-hydroxy group from the methylene (—CH2-) in a steroid backbone, combining synthetic chemistry and enzymology techniques to develop a selective inhibitor for cytochrome P450 8B1, and developing a selective P450 8B1 inhibitor, which can be used as a tool to study P450 8B1 and treat health issues.

Steroidal piperidone derivative, synthesis method, and use thereof

A steroidal piperidone derivative, a synthesis method, and a use thereof are provided. The steroidal piperidone derivative has a chemical structure shown in general formula (1) or general formula (2), where R is any one selected from the group consisting of alkyl, phenyl, substituted phenyl, and a heterocycle. In the synthesis method of the steroidal piperidone derivative, dehydroepiandrosterone (DHEA) is used as a basic raw material to prepare the steroidal piperidone derivative of the present disclosure through a series of reactions. A product prepared by the synthesis method has a high yield and is easily separated, and thus the synthesis method is the optimal method for preparing the steroidal piperidone derivative of the present disclosure. The present steroidal piperidone derivative exhibits prominent toxic activity against sucking pests, such as aphids, spider mites, rice planthoppers, and B. tabaci, and can be used for the control of a plant pest. ##STR00001##

pH DEPENDENT PHOTOACOUSTIC COMPOUNDS AND APPLICATIONS THEREOF
20210309645 · 2021-10-07 ·

In one aspect, photoacoustic compounds are described herein. A photoacoustic compound, for example, comprises two multicyclic ring moieties coupled by a rotationally restricted linkage, wherein the photoacoustic compound exhibits at least one of a pH dependent absorption spectrum, pH dependent emission spectrum and pH dependent photoacoustic spectrum. In being pH dependent, the absorption, emission and/or photoacoustic spectra of the photoacoustic compound can vary in response to environmental pH changes. Accordingly, the photoacoustic compound can provide differing photoacoustic responses based on the local pH environment.

Azasteroids for treatment of tuberculosis

The present invention provides a compound having the structure: ##STR00001##
for use in combination with an anti-tuberculosis drug for treating a subject infected with M. tuberculosis.

HYDROXYSTEROID COMPOUNDS, THEIR INTERMEDIATES, PROCESS OF PREPARATION, COMPOSITION AND USES THEREOF
20210024572 · 2021-01-28 ·

The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds.

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Sialyltransferase inhibitors and uses thereof
10889611 · 2021-01-12 · ·

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.

COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS

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

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Complex and structurally diverse compounds

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.

ENZYME COMPOSITIONS, STEROID DERIVATIVES, ENZYME INHIBITORS, AND METHODS OF MAKING SAME FOR PHARMACEUTICAL APPLICATIONS
20200172567 · 2020-06-04 ·

The present disclosure provides for a synthetic strategy to incorporate a C12-hydroxy group from the methylene (CH2-) in a steroid backbone, combining synthetic chemistry and enzymology techniques to develop a selective inhibitor for cytochrome P450 8B1, and developing a selective P450 8B1 inhibitor, which can be used as a tool to study P450 8B1 and treat health issues.

Hydroxysteroid compounds, their intermediates, process of preparation, composition and uses thereof

The present invention relates to novel steroidal compounds of formula (I), process for preparation of the same and composition comprising these compounds. ##STR00001##