Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Mochida Pharmaceutical Co., Ltd.

Scynexis, Inc.

Other

Mochida Pharmacuetical Co., Ltd.

James M Balkovec

Frances A Bouffard

Donald W Graham

James Francis Dropinski

Sherman Tim Waddell

Milton L Hammond

Xin Gu

Milana M Maletic

Bruno Tse

Susan D Aster

Amjad Ali

Cameron James Smith

Gina M Santorelli

Aaron H Leeman

William J Greenlee

Samuel Chackalamannil

Mark L Greenlee

Liangqin Guo

Robert E Schwartz

Robert A Zambias

Yi-Heng Chen

Gool F Patel

Christopher Francis Thompson

David J Mathre

Nancy J Kevin

Ting Zhang

Steven L Colletti

Phieng Siliphaivanh

Mitree M Ponpipom

Derun Li

Tin-Yau Chan

Dongfang Meng

Jiayi Xu

Yuping Zhu

Regina M Black

Steven H Olson

Yili Chen

Tomokazu Hirabayashi

John Qiang Tan

Weiming Fan

Michael Robert Peel

Nazia Quraishi

Ahmed Mamai

Jan S Tkacz

Akinlolu A Adefarati

Mika Sekioka

Rolf Thieringer

Edward C Sherer

Gayle E Taylor

Hiroshi Nagasue

Louis-Charles Campeau

Richard Beresis

Kouki Ogawa

Mallory F Loewe

Hao Liu

Regina C Black

Gregory P Rouen

Roland A Bouffard, Legal Representative

Sarah Dimick Gray

Keqaing Li

Steven S Mundt

Anne Hermanowski-Vosatka

William John Greenlee

Mika Katsuno

Tin Yan Chan

Frances Aileen Bouffard

Sarah M Dimick Gray

The present invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula I, and methods for using compounds of Formula I for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes.

Factor IXa inhibitors

The present invention provides a compound of Formula (I) wherein

The present invention provides a compound of Formula (I) where A is a heterocycle ring system and B is a heterocycle ring system or aryl ring system, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes.

Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-&#x3b2;-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.

Antifungal agents

2,5-Diaryl-1,2,4-triazole derivatives of structural formula I are selective inhibitors of the 11&#x3b2;-hydroxysteroid dehydrogenase Type 1 enzyme (11&#x3b2;-HSD-1). The compounds are useful for the treatment of diabetes, hyperglycemia, obesity, insulin resistance, atherosclerosis, dyslipidemia, hyperlipidemia, hypertension, and Metabolic Syndrome. Also disclosed are novel compounds of structural formula II which are inhibitors of 11&#x3b2;-HSD-1.

Diaryltriazoles as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1

Triazole derivatives of structural formula I are selective inhibitors of the 11&#x3b2;-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.

Triazole derivatives as inhibitors of 11-&#x3b2; hydroxysteroid dehydrogenase-1

Triazole derivatives as inhibitors of 11-&#x3b2;-hydroxysteroid dehydrogenase-1

Sulfonyl derivatives of structural formula I are selective inhibitors of the 11&#x3b2;-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome or Syndrome X, and other symptoms associated with NIDDM.

Sulfonyl compounds as inhibitors of 11-beta-hydroxysteroid dehydrogenase-1

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.

The present invention encompasses compounds of Formula (I) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included. 

17-carbamoyloxy cortisol derivatives as selective glucocorticoid receptor modulators

The present invention provides a method for the treatment or prevention of conditions which can be ameliorated by Smo antagonism, which method comprises administration to a patient in need thereof of an effective amount of a compound of formula I or a composition comprising a compound of formula I: or a pharmaceutically acceptable salt or solvate thereof; wherein:

Triazole derivatives which are SMO antagonists

The present invention encompasses compounds of Formula (I) and Formula (II) or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included. 

Selective spirocyclic glucocorticoid receptor modulators

The present invention encompasses compounds of Formula I: or pharmaceutically acceptable salts or hydrates thereof, which are useful as selective glucocorticoid receptor ligands for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.

1H-benzo[F]indazol-5-YL derivatives as selective glucocorticoid receptor modulators

Compounds having Formula (I), including pharmaceutically acceptable salts and prodrugs thereof: are selective inhibitors of the 11&#x3b2;-HSD1 enzyme. They inhibit the 11&#x3b2;-HSD1-mediated conversion of cortisone and other 11-keto-glucocorticoids to cortisol and other 11&#x3b2;-hydroxy-glucocorticoids. The 11&#x3b2;-HSD1 inhibitors therefore decrease the amount of cortisol in target tissues, thereby modulating the effects of cortisol. Modulation of cortisol may be effective in controlling non-insulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM or with excess cortisol in the body 

11-&#x3b2;-hydroxysteroid dehydrogenase 1 inhibitors useful for the treatment of diabetes, obesity and dyslipidemia

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North Plainfield, NJ, United States of America

James M Balkovec