Myriad Genetics, Inc.

Molecumetics Ltd.

Sepracor, Inc.

Merial Limited

Boehringer Ingelheim Animal Health USA Inc.

Scynexis, Inc.

Avista Pharma Solutions, Inc.

Cyprian Okwara Ogbu

Michael S Kahn

Hwa-Ok Kim

Masakatsu Eguchi

Patrick Douglas Boatman, Jr

Qun Kevin Fang

Kerry Leigh Spear

Charles Q Meng

Loic Patrick Le Hir De Fallois

Hyoung Ik Lee

Michele L R Heffernan

Seth C Hopkins

Alan Long

Robert J Foglesong

John E Tulinsky

Greg Pacofsky

Keqiang Li

Mustapha Soukri

Michael K McMillan

Maher N Qabar

Jessymol Mathew

Jason Daniel Speake

Joe B Perales

Andrew Scribner

Joseph Alexander Moore, Iii

David Renwick Houck

Michael Robert Peel

James Michael Dorsey

Bharathi Pandi

Jeffrey A Adams

Mark A Blaskovich

The present invention provides cyclic depsipeptide compounds of formula (I) and compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.

Anthelmintic depsipeptide compounds

The present disclosure describes a synthetic process and novel intermediates related to spirocyclic azetidenyl-isobenzofuran derivatives having an isothiazoline moiety, which are useful as antiparasitics.

Synthetic process and intermediates

Disclosed herein are compounds of general formula (I): wherein A, B, Rand Rare as defined in the specification, and their use as pharmaceuticals.

Macrocycles

The present invention provides novel inhibitors of the enzyme D-amino acid oxidase. The compounds of the invention are useful for treating or preventing diseases and/or condition, wherein modulation of D-serine levels, and/or its oxidative products, is effective in ameliorating symptoms. The invention further provides methods of enhancing learning, memory and/or cognition. For example, the invention provides methods for treating or preventing loss of memory and/or cognition associated with neurodegenerative diseases, such as Alzheimer's disease. The invention further provides methods for preventing loss of neuronal function characteristic of neurodegenerative diseases. In addition, methods are provided for the treatment or prevention of neuropsychiatric diseases (e.g., schizophrenia) and for the treatment or prevention of pain and ataxia.

Inhibitors of D-amino acid oxidase

This invention provides fused heterocycles having the formula: in which Ris a member selected from the group consisting of H, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from the group consisting of H substituted or unsubstituted alkenyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from the group consisting of H, C-Csubstituted or unsubstituted alkyl, substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl. Ris a member selected from OH and OX, in which Xis positive ion which is a member selected from organic positive ions and inorganic positive ions. Substituted or unsubstituted arylalkyl and substituted or unsubstituted heteroarylalkyl moieties have the formula: in which Ar is a member selected from the group consisting of substituted or unsubstituted aryl and substituted or unsubstituted heteroaryl. The index n is an integer from 1 to 4.

Fused heterocycles

There are disclosed &#x3b2;-sheet mimetics and methods relating to the same for imparting or stabilizing the &#x3b2;-sheet structure of a peptide, protein or molecule. In one aspect, &#x3b2;-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the &#x3b2;-sheet mimetic is a thrombin inhibitor.

&#x3b2;-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins

Compounds having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein A, A', B, X, Y, R, R, Rand Rare as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing such compounds, are tryptase antagonists.

&#x3b2;-sheet mimetics and composition and methods relating thereto

There are disclosed &bgr;-sheet mimetics and methods relating to the same for imparting or stabilizing the &bgr;-sheet structure of a peptide, protein or molecule. In one aspect, &bgr;-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the &bgr;-sheet mimetic is a thrombin inhibitor.

&bgr;-sheet mimetics and use thereof as inhibitors of biologically active peptides or proteins

&bgr;-sheet mimetics and methods relating to the same are disclosed. The &bgr;-sheet mimetics have utility as protease and kinase inhibitors, as well as inhibitors of transcription factors and protein-protein binding interactions. Methods of the invention include administration of a &bgr;-sheet mimetic, or use of the same for the manufacture of a medicament for treatment of a variety of conditions associated with the targeted protease, kinase, transcription factor and/or protein-protein binding interaction.

&bgr;-sheet mimetics and methods relating to the use thereof

.beta.-sheet mimetics and methods relating to the same are disclosed. The .beta.-sheet mimetics have utility as protease and kinase inhibitors, as well as inhibitors of transcription factors and protein-protein binding interactions. Methods of the invention include administration of a .beta.-sheet mimetic, or use of the same for the manufacture of a medicament for treatment of a variety of conditions associated with the targeted protease, kinase, transcription factor and/or protein-protein binding interaction.

Methods for regulating transcription factors

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Durham, NC, United States of America

Cyprian Okwara Ogbu