# US 7,612,095 B2 · Polymorph of 4-[2-[4-[1-(2-ethoxyethyl)-1H-benzimidazole-2-yl]-1-piperidinyl]ethyl]-αα-dimethyl-benzeneacetic acid

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- Number: US 7,612,095 B2
- Document ID: US7612095B2
- Status: Granted
- Kind: B2
- Application number: 10/511,822
- Filed: 2002-04-19
- Published: 2005-09-15
- Granted: 2009-11-03
- Earliest claimed: 2002-04-19
- Assignees: Faes Farma, S.A.
- Inventors: Aurelio Orjales Venero; Maravillas Bordell Martin; Gonzalo Canal Mori; Haydee Blanco Fuente; Maria Luisa Lucero De Pablo; Victor Rubio Royo; Ramon Mosquera Pestaña
- Web page: https://patentgrep.com/patent/US7612095B2

## CPC

- C07D 401/04: directly linked by a ring-member-to-ring-member bond
- A61K 31/445: Non condensed piperidines, e.g. piperocaine
- A61P 37/00: Drugs for immunological or allergic disorders
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## 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.

## Claims

### Claim 1

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.

### Claim 2 (depends on 1)

A process for preparing the crystalline form 1 of bilastine according to claim 1, wherein said process comprises:
a) combining bilastine with a solvent selected from the group consisting of isopropylic alcohol, n-butanol and acetone to form a mixture and heating the mixture to a reflux temperature of said solvent;
b) letting the mixture cool to room temperature;
c) filtering off solid residue from said cooled mixture; and
d) drying said solid residue to a constant weight.

### Claim 3 (depends on 1)

A process for preparing the crystalline form 1 of bilastine according to claim 1, wherein said process comprises:
a) combining crystalline form 2 of bilastine, or crystalline form 3 of bilastine, or a mixture thereof with a solvent selected from the group consisting of isopropylic alcohol, n-butanol and acetone to form a mixture and heating the bilastine/solvent mixture to a reflux temperature of the solvent;
b) letting the mixture cool to room temperature;
c) filtering off solid residue from said cooled mixture; and
d) drying said solid residue to a constant weight.

### Claim 4 (depends on 1)

A solid antihistiminic pharmaceutical composition comprising the crystalline form 1 of bilastine according to claim 1 as an active ingredient together with at least one excipient.

### Claim 5 (depends on 4)

A process for treating allergic diseases in a patient in need thereof, wherein the process comprises administering to said patient a pharmaceutical composition according to claim 4.

### Claim 6 (depends on 4)

A process for treating allergic diseases in a patient in need thereof, wherein the process comprises administering to said patient an effective amount of crystalline form 1 of bilastine in a solid pharmaceutical composition according to claim 4.