Merck + Co., Inc.

Orphagen Pharmaceuticals

Merck Sharp + Dohme Corp.

Auspex Pharmaceuticals, Inc.

Scynexis, Inc.

Auspex Pharmaceutical, Inc.

Bruno Tse

James M Balkovec

Xiaolin Li

Sepehr Sarshar

Robert E Babine

Scott Thacher

Mark L Greenlee

Yuan Cheng

Dongfang Meng

Alan D Adams

James Francis Dropinski

Frances A Bouffard

A Brian Jones

Weiming Fan

Michael Robert Peel

Ahmed Mamai

Shaei Y Huang

Clare E Gutteridge

Hao Liu

Borcherng Hong

Keqaing Li

Ahren I Green

Frances Aileen Bouffard

Methods for modulating (inhibiting or stimulating) retinoid-related orphan receptor &#x3b3; (ROR&#x3b3;) activity. This modulation has numerous effects, including inhibition of T-17 cell function and/or T-17 cell activity, and inhibition of re-stimulation of T-17 cells, which are beneficial to treatment of inflammation and autoimmune disorders. Stimulation of ROR&#x3b3; results in stimulation of T-17 cell function and/or activity which is beneficial for immune-enhancing compositions (e.g., vaccines).

Modulators of retinoid-related orphan receptor gamma

The present invention relates to novel enfumafungin derivatives of formula I and pharmaceutically acceptable salts thereof, their synthesis, and their use as inhibitors of (1,3)-&#x3b2;-D-glucan synthase. The present compounds and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the present compounds and pharmaceutically acceptable salts thereof, are useful for treating or preventing antifungal infections and associated diseases and conditions.

Antifungal agents

The present invention is directed to compounds having the structure wherein R, R, R, R, Rand m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals 

Therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders

The present invention is directed to compounds having the structure (I) wherein R, R, R, R, Rand m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals. 

The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol. 

Therapeutic compounds for treating dyslipidemic conditions

Sordarin derivatives prepared from C-11-hydroxysordarin are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.

Antifungal agents of sordarin derivatives

Sordarin derivatives

Sordarin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.

4-Cyano-4-deformylsordaricin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.

4-cyano-4-deformylsordaricin derivatives

There are disclosed novel antifungal macrolides of the formula ##STR1## compositions containing said compounds, methods of using said compounds and a method for synthesizing the compounds.

Antifungal macrolides and their synthesis

Growing community of inventors

San Diego, CA, United States of America

Bruno Tse