Merck Sharp + Dohme Corp.

June J Kim

Michael R Wood

Harold G Selnick

Scott D Kuduk

Christopher D Cox

Thomas S Reger

Carol A McVean

Kathy Schirripa

Justin T Sheen

Philip Jones

Ian M Bell

Christopher J Dinsmore

David James Witter

Craig A Stump

Shawn J Stachel

Douglas C Beshore

Joon Jung

John W Butcher

Vadim Y Dudkin

Thomas G Steele

Melody McWherter

Alexey A Rivkin

Sean P Ahearn

Justin T Steen

John T Hendrix

Raksha Archarya

Carol Mcvean

Justin Steen

Thomas Steele

John Hendrix

The present invention is directed to substituted azetidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). 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.

1,3 substituted azetidine PDE10 inhibitors

The present invention is directed to substituted triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). 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.

Triazolyl PDE10 inhibitors

The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.

Azaindoles as Janus kinase inhibitors

The present invention is directed to novel non-amidic linkers with branched termini derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.

Non-amidic linkers with branched termini as CGRP receptor antagonists

Compounds of Formula (I): (where variables R, R, R, R, R, A, and Z are as defined herein) which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. 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 CGRP receptors are involved. 

3- and 6-quinolines with N-attached heterocyclic CGRP receptor antagonists

The present invention is directed to novel branched 3- and 6-substituted quinoline derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.

Branched 3- and 6-substituted quinolines as CGRP receptors antagonists

Compounds of formula I: (wherein variables A, m, n, J, R, R, R, E, E, E, Rand Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

CGRP receptor antagonists with tertiary amide, sulfonamide, carbamate and urea end groups

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Collegeville, PA, United States of America

June J Kim