Benzoimidazol-2-yl pyrimidine modulators of the histamine H4 receptor

Patent metadata

Field	Value
Publication number	US-9434715-B2
Application number	US-201615047359-A
Country	US
Kind code	B2
Filing date	Feb 18, 2016
Priority date	Mar 6, 2013
Publication date	Sep 6, 2016
Grant date	Sep 6, 2016

Abstract

Benzoimidazol-2-yl pyrimidines, purification methods for the same, and pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H 4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritus.

First claim

What is claimed is:

1. A method of obtaining a purified pharmaceutically acceptable salt of a [5-(4,6-dimethyl-1H-benzoimidazol-2-yl)-4-methyl-pyrimidin-2-yl]-[3-(1-methyl-piperidin-4-yl)-propyl]-amine, comprising:
forming a hemitartrate salt of the compound of formula (2):

in water to yield an aqueous hemitartrate salt solution;
seeding said aqueous solution with crystal seeds of the tetrahydrate of said hemitartrate to obtain a seeded aqueous solution; and
crystallizing out of said seeded aqueous solution the solid tetrahydrate hemitartrate of formula (3):

2. A method according to claim 1 , wherein said solid tetrahydrate hemitartrate of formula (3) is substantially free from at least impurities I1 and I3 of formulae:

3. A method according to claim 1 , wherein said forming a hemitartrate salt comprises reacting compound of formula (2) with L-(+)-tartaric acid in water, and said crystallizing comprises cooling said seeded aqueous solution to about 5° C.

Assignees

• Janssen Pharmaceutica Nv

Inventors

• Conza Matteo
• Hickey Magali B
• Horns Stefan
• Lochner Susanne

Classifications

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P5/16

  for decreasing, blocking or antagonising the activity of the thyroid hormones · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P43/00

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

• A61P3/06

  Antihyperlipidemics · CPC title