Merck Sharp + Dohme Corp.

Msd K.k.

Kevin J Rodzinak

Mark E Layton

Philip E Sanderson

Antonella Converso

Jun Liang

Jiabing Wang

Essa H Hu

Yiwei Li

Mark E Fraley

Mark T Bilodeau

Yasuhiro Goto

Brian Andrew Stearns

Toshihiro Sakamoto

Jeannie M Arruda

Lida R Tehrani

Peter J Manley

Tony Siu

Yoshio Ogino

Kenneth L Arrington

Nicholas D P Cosford

Brian T Campbell

Vadim Y Dudkin

Michael J Kelly, Iii

Hidetomo Furuyama

Nobuhiko Kawanishi

Jacob M Hoffman

Takashi Mita

Akira Naya

Joseph E Pero

Michael A Rossi

Mildred L Kaufman

Alexander J Reif

Yu Onozaki

Michael J Rossi

Vadim Dudkin

Victoria Cofre

Donna J Armstrong

Michael J Iii Kelly

The present invention is directed to azacyanoquinolinone compounds of the general structural formula: (wherein Rand Rare defined herein) which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Substituted quinolinones as PDE9 inhibitors

The present invention is directed to oxycyanoquinolinone compounds which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Oxy-cyanoquinolinone PDE9 inhibitors

The present invention is directed to phenylcyanoquinolinone compounds which may be useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.

Phenyl-cyanoquinolinone PDE9 inhibitors

The present invention is directed to benzimidazolone derivatives which are positive allosteric modulators of the mGluR2 receptor, useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved, such as schizophrenia.

Positive allosteric modulators of MGLUR2

The compounds of Formula D are of the class of triazolo-pyrido-pyrazines which are inhibitors of AKT useful for the treatment of cancer 

Substituted [1,2,4]triazolo[4',3&#x2032;:1,6]pyrido[2,3-b]pyrazines of the formula D

The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.

Inhibitors of AKT activity

Inhibitors of akt activtiy

The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.

Inhibitors of Akt activity

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Schwenksville, PA, United States of America

Kevin J Rodzinak