Merck Sharp + Dohme Corp.

Carl A Baxter

Edward Cleator

Faye Sheen

Shane W Krska

Gavin William Stewart

Nobuyoshi Yasuda

Guy R Humphrey

Peter Emmanuel Maligres

Yong-Li Zhong

Lushi Tan

Gregory L Beutner

Jeremy Peter Scott

Qinghao Chen

Jeffrey T Kuethe

Neil A Strotman

Timothy James Wright

Debra J Wallace

Andrew Gibb

Edward Cleartor

Timothy Wright

The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.

Process for the preparation of an orexin receptor antagonist

This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.

Process for making M1 receptor positive allosteric modulators

A first aspect of the present invention describes a compound selected from group consisting of: wherein R is either H, C(O)R, or C(O)NHCH(X)COOH; provided that X is a C-Calkyl, or a C-Ccycloalkyl and Ris a Calkyl or aryl; These compounds are used to make Compound A 

Methods and intermediates for preparing macrolactams

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London, United Kingdom

Carl A Baxter