[9,10-dimethoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11bH-pyrido-[2,1-a]isoquinolin-2-yl]methanol and compounds, compositions and methods relating thereto

Patent metadata

Field	Value
Publication number	US-9714246-B2
Application number	US-201615017480-A
Country	US
Kind code	B2
Filing date	Feb 5, 2016
Priority date	Feb 6, 2015
Publication date	Jul 25, 2017
Grant date	Jul 25, 2017

Abstract

Compounds having a structure of formula (I), including stereoisomers and pharmaceutically acceptable salts and solvates thereof:

wherein R 1 is as defined herein. Such compounds are inhibitors of the vesicular monoamine transporter 2 (VMAT2) and have utility for treating, for example, hyperkinetic disorders. Also disclosed are compositions containing these compounds in combination with a pharmaceutically acceptable carrier or diluent, as well as methods relating to the use in a subject in need thereof.

First claim

We claim the following:

1. [(2R,3S,11bR)-9,10-dimethoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H, 11bH-pyrido-[2,1-a]isoquinolin-2-yl]methanol, or a pharmaceutically acceptable salt or solvate thereof.

2. [(2R,3S,11bR)-9,10-dimethoxy-3-(2-methylpropyl)-1H,2H,3H,4H,6H,7H,11bH-pyrido[2,1-a]isoquinolin-2-yl]methanol HCl.

3. A pharmaceutical composition comprising a compound of claim 1 in combination with a pharmaceutically acceptable excipient and/or diluent.

4. A pharmaceutical composition comprising a compound of claim 2 in combination with a pharmaceutically acceptable excipient and/or diluent.

Assignees

• Neurocrine Biosciences Inc

Inventors

• Ashweek Neil
• Harriott Nicole

Classifications

• A61P25/14

  for treating abnormal movements, e.g. chorea, dyskinesia · CPC title

• C07D471/04 Primary

  Ortho-condensed systems · CPC title

• C07D455/04 Primary

  containing a quinolizine ring system condensed with only one six-membered carbocyclic ring, e.g. julolidine · CPC title

• C07D519/00

  Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00 · CPC title

• A61K31/4745

  condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines (yohimbine derivatives, vinblastine A61K31/475; ergoline derivatives A61K31/48) · CPC title