Salts of aza-bicyclic di-aryl ethers and methods to make them or their precursors

Patent metadata

Field	Value
Publication number	US-2018009801-A1
Application number	US-201715712279-A
Country	US
Kind code	A1
Filing date	Sep 22, 2017
Priority date	Jul 15, 2011
Publication date	Jan 11, 2018
Grant date	—

Abstract

The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments.

First claim

We claim:

1 . A salt of (R)-3-(6-(4-methylphenyI)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane wherein said salt is the fumarate, maleate, chloride, phosphate, succinate, or malonate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane.

2 . The salt according to claim 1 , wherein the salt is the mono-fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane in crystalline form.

3 . The salt according to claim 2 , wherein the salt is characterized by an XRPD pattern substantially the same as the XRPD pattern shown in FIG. 1 .

4 . The salt according to claim 1 , wherein the salt is the mono-fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane in crystalline form, wherein the mean particle size of the crystals is at least 15 μm.

5 . The salt according to claim 2 , wherein the salt is the mono-fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane in crystalline form, and wherein the salt is in substantially pure form.

6 . The salt according to claim 2 , wherein the salt is the mono-fumarate salt of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane in crystalline form, and wherein the salt has a purity greater than 90 weight %.

7 . A method for the prevention, treatment, and/or delay of progression of a disease or condition, in which nAChR α7 activation plays a role or is implicated, in a subject in need of such treatment, which comprises administering to such subject a therapeutically effective amount of a salt as defined in claim 1 .

8 . A method for the prevention, treatment, and/or delay of progression of psychiatric or neurodegenerative disorders in a subject in need of such treatment, which comprises administering to such subject a therapeutically effective amount of a salt as defined in claim 1 .

Assignees

• Novartis Ag

Inventors

• Marterer Wolfgang
• Prashad Mahavir
• Villhauer Edwin Bernard
• Waykole Liladhar Murlidhar
• Vivelo James Anthony
• Sutter Bertrand
• Bianchi Jean-Claude
• Wu Raeann
• Har Denis
• Karpinski Piotr H
• Pignone Massimo
• Stingelin Doris
• Buerger Eckart

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P9/12

  Antihypertensives · CPC title

• A61P9/06

  Antiarrhythmics · CPC title

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P25/28

  for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia · CPC title