Takeda Pharmaceutical Company Limited

Maria Hopkins

Holger Monenschein

Huikai Sun

Holly Reichard

Shota Kikuchi

Stephen A Hitchcock

Todd Macklin

Jason W Brown

Kristin Schleicher

Betty Lam

Mark E Adams

Benjamin Jones

Thomas Nixey

Andre A Kiryanov

Sean Timothy Murphy

Jon Kuehler

Jason Green

Steve Hitchcock

Hukai Sun

Holdger Monenschein

Disclosed are compounds of Formula 1 and pharmaceutically acceptable salts thereof, wherein L, R, R, R, R, R, X, X, X, X, X, and Z are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with GPR6.

Piperidinyl- and piperazinyl-substituted heteroaromatic carboxamides as modulators of GPR6

The present invention provides compounds of formula I: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.

Substituted pyrido[3,4-b]pyrazines as GPR6 modulators

Tetrahydropyridopyrazines as modulators of GPR6

The present invention provides 5-HT3 receptor antagonists of Formula (I): which are useful for the treatment of diseases treatable by inhibition of 5-HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

5-HT3 receptor antagonists

Disclosed is a compound of Formula 1, and a pharmaceutically acceptable salt thereof. This disclosure also relates to materials and methods for preparing the compound of Formula 1, to pharmaceutical compositions which contain it, and to its use for treating diseases, disorders, and conditions associated with GPR6.

Tetrahydropyridopyrazine modulators of GPR6

Pyrazines as modulators of GPR6

The present invention provides compounds of Formula (I): that are GPR6 modulators and are therefore useful for the treatment of diseases treatable by modulation of GPR6, in particular treating Parkinson disease, levodopa induced dyskinesias, Huntington's disease, other dyskinesias, akinesias, and motor disorders involving dysfunction of the striatum, schizophrenia and drug addiction. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Quinoxaline derivatives as GPR6 modulators

This present invention provides compounds of formula II: which are useful as modulators of GPR6, pharmaceutical compositions thereof, methods for treatment of conditions associated with GPR6, processes for making the compounds and intermediates thereof.

The present invention provides compounds of the formula: that are 5HT3 receptor antagonists and are therefore useful for the treatment of diseases treatable by inhibition of 5HT3 receptor such as emesis, pain, drug addiction, neurodegenerative and psychiatric disorders, and GI disorders. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

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San Diego, CA, United States of America

Maria Hopkins