Boehringer Ingelheim International Gmbh

Centrexion Therapeutics Corporation

Florian Paul Christian Binder

Martin Thomas Fleck

Jens Willwacher

Doris Riether

Achim Sauer

Janet Rachel Nicholson

Henri Doods

Stephan Georg Mueller

Georg Dahmann

Annekatrin Charlotte Heimann

Joerg P Hehn

Thorsten K Oost

Uta Friederike Lessel

Henri Doobs

Thomas Martin Fleck

Stephan George Mueller

This invention relates to novel (Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.

(cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles

The present disclosure provides certain 3H,4H-thieno[2,3-d]pyrimidin-4-one derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

3H,4H-thieno[2,3-d]pyrimidin-4-one derivatives as TRPA1 inhibitors

The present disclosure provides certain tetrazole derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

Tetrazole derivatives as TRPA1 inhibitors

The present disclosure provides certain 3H,4H,5H,6H,7H-pyrimido[4,5-b][1,4]oxazine-4,6-dione derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

3H,4H,5H,6H,7H-pyrimido[4,5-b][1,4]oxazine-4,6-dione derivatives as TRPA1 inhibitors

The present disclosure provides certain substituted 1,2,4-oxadiazole derivatives of the below formula (I) that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

Substituted 1,2,4-oxadiazoles as TRPA1 inhibitors

The present disclosure provides certain uracil derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing said compounds.

Uracil derivatives as TRPA1 inhibitors

(Cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles

The present disclosure provides certain tetrazole derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing the same.

This invention relates to thienopyrimidinones and their use as inhibitors of TRPA1 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of fibrotic diseases, inflammatory and auto-immune diseases and CNS-related diseases.

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Maselheim, Germany

Florian Paul Christian Binder