A61K31/4747

Compounds inhibiting eukaryotic elongation factor 2 kinase activity
10106552 · 2018-10-23 · ·

Eukaryotic elongation factor 2 kinase inhibitors of the formula ##STR00001##
where R.sub.1, R.sub.2, R.sub.3a, R.sub.3b, R.sub.4a, R.sub.4b, R.sub.5a, R.sub.5b, R.sub.6a, R.sub.6b, R.sub.7 and x are as defined in the specification, pharmaceutical compositions and formulations including compounds of the foregoing formula, and methods of preventing, ameliorating or treating indications, conditions, disorders or syndromes associated with elongation factor 2 phosphorylation.

Compounds inhibiting eukaryotic elongation factor 2 kinase activity
10106552 · 2018-10-23 · ·

Eukaryotic elongation factor 2 kinase inhibitors of the formula ##STR00001##
where R.sub.1, R.sub.2, R.sub.3a, R.sub.3b, R.sub.4a, R.sub.4b, R.sub.5a, R.sub.5b, R.sub.6a, R.sub.6b, R.sub.7 and x are as defined in the specification, pharmaceutical compositions and formulations including compounds of the foregoing formula, and methods of preventing, ameliorating or treating indications, conditions, disorders or syndromes associated with elongation factor 2 phosphorylation.

PHARMACEUTICAL COMPOSITIONS

This invention relates to the use of low doses of (+)--dihydrotetrabenazine for the treatment of movement disorders, such as Tourette's syndrome.

PHARMACEUTICAL COMPOSITIONS

This invention relates to the use of low doses of (+)--dihydrotetrabenazine for the treatment of movement disorders, such as Tourette's syndrome.

OSMOTIC DOSAGE FORMS COMPRISING DEUTETRABENAZINE AND METHODS OF USE THEREOF

Provided herein are osmotic dosage forms containing deutetrabenazine for use in the treatment of, e.g., hyperkinetic movement disorders. When orally administered to a subject on a once-daily basis, the dosage forms provide a favorable pharmacokinetic profile for the active agent indicating treatment efficacy over an extended period of time.

PHARMACOLOGICALLY ACTIVE COMPOUNDS

The present invention relates to compounds of formula II

##STR00001##

wherein X, Y, R.sub.2, R.sub.3, R.sub.4 and Ar are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

PHARMACOLOGICALLY ACTIVE COMPOUNDS

The present invention relates to compounds of formula II

##STR00001##

wherein X, Y, R.sub.2, R.sub.3, R.sub.4 and Ar are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

Pharmacologically active compounds

The present invention relates to compounds of formula II ##STR00001##
wherein X, Y, R.sub.2, R.sub.3, R.sub.4 and Ar are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

Pharmacologically active compounds

The present invention relates to compounds of formula II ##STR00001##
wherein X, Y, R.sub.2, R.sub.3, R.sub.4 and Ar are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

Spiro-quinazolinone derivatives and their use as positive allosteric modulators of mGluR4

The present invention relates to novel spiro-quinazolinone derivatives as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 4 (mGluR4) and/or altering glutamate level or glutamatergic signalling.