C07D211/18

Compositions and uses thereof

The disclosure is directed to compounds of the formula (1A), (I)(V) and others disclosed herein and uses of such compounds.

Cycloalkylurea derivative

The present invention relates to a medicament for treating or preventing a disease related to orexin receptor, especially orexin type 2 receptor, comprising a new compound having a urea structure or a pharmaceutically acceptable salt thereof as an active ingredient. In more detail, the present invention relates to a medicament for treating or preventing narcolepsy, idiopathic hypersomnia, hypersomnia, sleep apnea syndrome, etc.

CYCLIC PEPTIDE COMPOUND HAVING KRAS INHIBITORY ACTION

The present inventors found cyclic peptide compounds that interact with Ras, and non-natural amino acids useful for the production of the cyclic peptide compounds. The inventors also found that the cyclic peptide compounds inhibit the binding between Ras and SOS. In addition, the inventors found specific non-natural amino acids contained in the cyclic peptide compounds and methods for production thereof.

Amido Compounds And Their Use As Pharmaceuticals

The present invention relates to inhibitors of 11- hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11- hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Amido Compounds And Their Use As Pharmaceuticals

The present invention relates to inhibitors of 11- hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11- hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Amido compounds and their use as pharmaceuticals

The present invention relates to inhibitors of 11- hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11- hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Amido compounds and their use as pharmaceuticals

The present invention relates to inhibitors of 11- hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11- hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

CYCLOALKYLUREA DERIVATIVE

The present invention relates to a medicament for treating or preventing a disease related to orexin receptor, especially orexin type 2 receptor, comprising a new compound having a urea structure or a pharmaceutically acceptable salt thereof as an active ingredient. In more detail, the present invention relates to a medicament for treating or preventing narcolepsy, idiopathic hypersomnia, hypersomnia, sleep apnea syndrome, etc.

QUATERNARY HETEROATOM CONTAINING COMPOUNDS

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II):

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comprising treating a compound of Formula (I):

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with a transition metal catalyst and under alkylation conditions as valence and stability permit.

SYNTHETIC PROCESS
20170107208 · 2017-04-20 ·

The present invention relates to a process for preparing substituted piperidine compounds and especially chiral substituted piperidine compounds. The process involves reacting a substituted pyridinium ion with an amine as defined herein, in the presence of a hydrogen donor, a catalysts and a suitable solvent.