C07J71/00

6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal FXR modulators

The invention relates to compounds of formula (I) and related methods, wherein R.sup.1, R.sup.2, Y, R.sup.4 and R.sup.5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids with pharmacological activity. The invention futher provides intermediated in the systhesis of obeticholic acid and its analogues. The invention also provides methods related to the synthesizing of these intermediates and methods of preparing obeticholic acid and obeticholic acid analogues from the compound of the invention. ##STR00001##

NOVEL SALTS AND POLYMORPHS OF SCY-078
20190153024 · 2019-05-23 · ·

SCY-078 is a glucan synthase inhibitor with antimicrobial activity. Novel salts and polymorph forms of SCY-078 are disclosed herein. The disclosure also relates to pharmaceutical compositions, methods of use, and methods of preparing the novel salts and polymorphs of SCY-078.

Steroid 6.7.Beta.-Epoxides as Chemical Intermediates

The invention relates to a process for preparing a compound of general formula (Ia):

##STR00001##

wherein R.sup.2, Y, R.sup.4 and R.sup.5 are as defined herein. The invention also relates to certain compounds per se. The compounds are intermediates in the synthesis of synthetic bile acids.

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.

C4-MODIFIED OLEANOLIC ACID DERIVATIVES FOR INHIBITION OF IL-17 AND OTHER USES

Disclosed herein are C4 modified oleanolic acid derivatives of the formula: Formula (X) or Formula (XII), as well as analogs thereof, wherein the variables are defined herein. In addition, disclosed herein are pharmaceutical compositions of these derivatives or analogs, methods for their manufacture, and methods for their use, including for the prevention and treatment of diseases or disorders associated with overproduction of IL-17.

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NANOEMULSIONS AND METHODS FOR CANCER THERAPY

An oxysterol or oxysterol-like compound is provided, which finds use in treating and/or targeting cancer.

Isoxazolidine derivatives

Anti-inflammatory and antiallergic compounds of the glucocorticosteroid series, according to formula (I) according to formula (I) defined herein are useful for treating diseases of the respiratory tract characterized by airway obstruction.

Cortistatin analogues and syntheses and uses thereof

Compounds of Formula (A), (B), (C), (D), (E), (A), (B), (C), (D), (E), (G1), and (G2) are useful as therapeutics for treating a wide variety of conditions in a host such as a human, e.g., including but not limited to, conditions associated with angiogenesis and/or which are mediated by CDK8 and/or CDK19 kinase activity. Also provided are methods of modulating the -catenin pathway, methods of modulating STAT1 activity, methods of modulating the TGF/BMP pathway, methods of modulating HIF-1-alpha activity in a cell, and methods of increasing BIM expression to induce apoptosis, using an effective amount of a compound of Formula (A), (B), (C), (D), (E), (A), (B), (C), (D), (E), (G1), or (G2).

Processes and compositions obtained from the Solanum genus of plants

Pure saponins and processes for making such saponins are described herein. In addition, cosmetic compositions, such as skin care compositions, comprising such saponins and methods for improving skin health and appearance with such skincare compositions are also described herein.

Terpenoid derivatives

It is intended to provide a novel terpenoid derivative that exhibits anti-inflammatory action and a cytoprotective action by activating the Keap1/Nrf2/ARE signaling pathway. The present invention provides terpenoid derivative A represented by the following formula (I): ##STR00001##