Merck Patent Gmbh

Eli Lilly and Company

Sepracor, Inc.

Nuada, LLC

Robert J Foglesong

Thomas E Richardson

Daniel Jon Sall

Gerald Floyd Smith

Ho-Shen Lin

Minsheng Zhang

Richard Waltz Harper

Henry Yu

Kumiko Takeuchi

Jefferson Ray McCowan

Michael Lyle Denney

Mary George Johnson

Nickolay Y Chirgadze

Michael P Lynch

Alan David Palkowitz

Matthew Joseph Fisher

Michael Enrico Richett

Jolie Anne Bastian

Andreas Goutopoulos

Valentine Joseph Klimkowski

Kerry Leigh Spear

Michele L R Heffernan

Seth C Hopkins

Jennifer Marie Tinsley

Lizbeth Celeste DeSelm

Mustapha Soukri

Qun Kevin Fang

Shawn Christopher Miller

Cyprian Okwara Ogbu

Brian H Heasley

Todd Jonathan Kohn

James Michael Dorsey

Pandi Bharathi

Matthew G Jenks

Michael Robert Wiley

Nicholas J Bach

Brian Lewis Hodous

Nadia Brugger

Susan Marie Royalty

Theresa L Johnson

David Middlemiss

Justin Potnick

Amanda E Sutton

Jeffrey Thomas Mullaney

Mark A Varney

Jan Jozef Scicinski

James Ford Burns

Steven W Jones

Gunnar Erik Jagdmann, Jr

Thomas Francis Nelson Haxell

Kellee Griffin Ring

Tatyana Dyakonov

Novel benzamide derivatives of formula (I) wherein W, W, Rto Rand X have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.

Benzamide derivatives as modulators of the follicle stimulating hormone

Novel dihydropyrazole derivatives of formula (I) wherein L, R, R, R, R, R, R, X, X, X, X, Y, m and n have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.

Dihydropyrazoles

The present invention relates to novel spiro-quinazolinone derivatives as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 4 (mGluR4) and/or altering glutamate level or glutamatergic signalling.

Spiro-quinazolinone derivatives and their use as positive allosteric modulators of mGluR4

Novel dihydropyrazole derivatives of formula (I) 

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 novel inhibitors of the enzyme D-amino acid oxidase as well as pharmaceutical compositions including the compounds of the invention. The invention also provides methods for the treatment and prevention of neurological disorders, such as neuropsychiatric and neurodegenerative diseases, as well as pain, ataxia and convulsion. The compounds of the invention have the general structure: wherein A is NH or S. Q is a member selected from CRand N. X and Y are members independently selected from O, S, CR, N and NH. R, Rand Rare members independently selected from H and F, provided that at least one member selected from R, Rand Ris F. Ris a member selected from OXand OH, wherein Xis a positive ion, which is a member selected from inorganic positive ions and organic positive ions.

Fluoro-substituted inhibitors of D-amino acid oxidase

The present invention relates to a series of novel compounds having the formula (I) wherein: X is NRor O; n is 1 or 2; A is a bicyclic carbocycle and R1 and R2 are as described herein. The compounds are useful as DPP-IV inhibitors, such as for the treatment of diabetes. 

Peptidase inhibitors

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

The invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts, as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.

Antithrombotic agents

This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula I, and the use of defined compounds of formula I as thrombin inhibitors.

Thrombin inhibitors

This application relates to novel compounds of formula (I) (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical formulations comprising the novel compounds of formula (I), and the use of the compounds of formula (I) as thrombin inhibitors.

This application relates to the use as thrombin inhibitors, coagulation inhibitors and thromboembolic disorder agents of diamines of formula I as defined herein. It also provides novel compounds of formula I, processes and intermediates for their preparation, and pharmaceutical formulations comprising the novel compounds of formula I.

Antithrombotic diamines

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Durham, NC, United States of America

Robert J Foglesong