US 7,612,095 B2Granted

Polymorph of 4-[2-[4-[1-(2-ethoxyethyl)-1H-benzimidazole-2-yl]-1-piperidinyl]ethyl]-αα-dimethyl-benzeneacetic acid

AssigneeFaes Farma, S.A.

InventorsAurelio Orjales Venero, Maravillas Bordell Martin, Gonzalo Canal Mori, Haydee Blanco Fuente, Maria Luisa Lucero De Pablo, Victor Rubio Royo, Ramon Mosquera Pestaña

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Abstract

Crystalline form 1 of 4-[2-[4-[1-(2-ethoxyethyl)-1H-benzimidazole-2-yl]-1 -piperidinyl]ethyl]-αα-dimethyl-benzen⊖eacetic acid Crystalline form 1 of 4-[2-[4-[1-(2-ethoxyethyl)-1H-benzimidazole-2-yl]-1 -piperidinyl]ethyl]-αα-dimethyl-benzen⊖eacetic acid of formula (I) is described, procedures for its preparation, pharmaceutical formulae containing crystalline form 1 and the use of crystalline form 1 to treat allergic reactions and pathological processes mediated by histamine in mammals such as man.

Claims6

Dependent claims

A crystalline form 1 of bilastine having, upon X-ray crystallography analysis, crystal parameters of substantially the following:

Crystallographic system
Monoclinic
Spatial group
P2 (1)/c
Crystal size
0.56 × 0.45 × 0.24 mm
Cell dimension
a = 23.38 (5) A angstrom
α = 90°
b = 8.829 (17) A
β = 90°
c = 12.59 (2) A
Y = 90°
Volume
2600 A3
Z, calculated density
4, 1.184 mg/m3,
an infrared spectrum in potassium bromide with the following bands:
Wavenumber (cm−1)
3057
2929
2883
2857
2797
1666
1481
1431
1346
1326
1288
1020
973
945
829
and an infrared spectrum in potassium bromide which is substantially identical to that shown in FIG. 1.

32 more elements

Dependencies are inferred from the claim text.

Facts

Application: 10/511,822Filed 19 Apr 2002
Published: US 2005/0203141 A115 Sep 2005
Granted: 3 Nov 2009
Term ends: Not estimatedThe source records don’t support an estimate.

Classification8 codes

C07D 401/04
Containing two hetero rings: directly linked by a ring-member-to-ring-member bond
A61K 31/445
Non condensed pyridines; Hydrogenated derivatives thereof: non condensed piperidines, e.g. piperocaine
A61P 37/00
Drugs for immunological or allergic disorders
A61P 37/08
Drugs for immunological or allergic disorders: antiallergic agents

Family

US 2005/0203141 A1Pre-grant publication · published 15 Sep 2005
US 7,612,095 B2This patent

From the US filing history. Foreign family members aren’t listed.

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