Trillium Therapeutics Inc.

Neuraxon, Inc.

Astrazeneca Ab

Peter Dove

Abdelmalik Slassi

Jailall Ramnauth

Shawn Maddaford

Subhash Annedi

Suman Rakhit

Sarah Silverman

Louise G Edwards

Methvin Benjamin Isaac

Tao Xin

Paul Renton

Tomislav Stefanac

Joanne Patman

John S Andrews

Subhash C Annedi

A novel class of fluorinated derivatives of Formula I have been prepared and found to be useful in the treatment of cancers and other disorders related mediated by Bromodomain-Containing Proteins. 

Fluorinated imidazo[4,5-C]quinoline derivatives as inhibitors of bromodomain containing proteins

A novel class of fluorinated derivatives of Formula (I) have been prepared and found to be useful in the treatment of cancers and other disorders related mediated by Bromodomain-Containing Proteins. 

The present application relates to novel fluorinated epoxyketone-based compounds, compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions mediated by proteasome inhibition, in particular, the present application includes compounds of Formula I, and compositions and uses thereof. 

Fluorinated epoxyketone-based compounds and uses thereof as proteasome inhibitors

The present invention features benzoxazines, benzothiazines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. Exemplary compounds are of the formula: The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.

Benzoxazines, benzothiazines, and related compounds having NOS inhibitory activity

The present invention features quinolones, tetrahydroquinolines, and related compounds that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.

Quinolone and tetrahydroquinolone and related compounds having NOS inhibitory activity

The present invention features benzothiazines that inhibit nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms, and that have the formula: The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions.

The present invention is directed to compounds of formula I: Wherein Rto R, X and Z are further defined in the description. The invention also relates to processes for the preparation of the compounds and to intermediates used in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.

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Toronto, Canada

Peter Dove