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Polymorph of acid 4-[2-[4-[1-2-ethoxyethyl)-1h-benzimidazole-2-il]-1-piper idinyl]ethyl]-dollar G (A), dollar G (A)-dimethyl-benzeneacetic

A technology of polymorph and crystal system, applied in 4-[2-[1-(2-ethoxyethyl)-1H-benzodiimazol-2-yl]-1-piperidinyl Field of polymorphs of ]ethyl]-α,α-dimethylphenylacetic acid

Inactive Publication Date: 2005-06-15
FAES FARMA SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The patent also relates to the method of preparing bilastine and the application of the preparation to treat allergic reactions in mammals, but does not include or imply the existence of polymorphic forms of the compound.

Method used

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  • Polymorph of acid 4-[2-[4-[1-2-ethoxyethyl)-1h-benzimidazole-2-il]-1-piper idinyl]ethyl]-dollar G (A), dollar G (A)-dimethyl-benzeneacetic
  • Polymorph of acid 4-[2-[4-[1-2-ethoxyethyl)-1h-benzimidazole-2-il]-1-piper idinyl]ethyl]-dollar G (A), dollar G (A)-dimethyl-benzeneacetic
  • Polymorph of acid 4-[2-[4-[1-2-ethoxyethyl)-1h-benzimidazole-2-il]-1-piper idinyl]ethyl]-dollar G (A), dollar G (A)-dimethyl-benzeneacetic

Examples

Experimental program
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Effect test

Embodiment 1

[0070] Preparation of bilastine polymorph 1

[0071] Dissolve bilastine (US Pat. No. 5,877,187) in isopropanol and heat to reflux for about 15-20 minutes under nitrogen atmosphere while stirring. The solution was cooled to 50°C over 6 hours and stirring was stopped. The solution was cooled to room temperature and stirred for another 3 hours, filtered and washed with cold isopropanol. The solid residue was dried in a vacuum cabinet at 35-40°C until constant weight.

Embodiment 2

[0073] Preparation of bilastine polymorph 1

[0074] A suspension of bilastine (US Pat. No. 5,877,187) in n-butanol was heated and refluxed for 3 hours with stirring under a nitrogen atmosphere. Cool the solution while stirring, filter off the solid residue, and dry the solid residue in a vacuum cabinet at 35-40°C until constant weight.

Embodiment 3

[0076] Preparation of bilastine polymorph 1

[0077] The mixture of bilastine polymorphs 2 and 3 was treated with hot acetone for several hours. The mixture was cooled to room temperature, the solid residue was filtered off and dried to constant weight.

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Abstract

The invention relates to polymorph 1 of acid 4-[2-[4-[1-(2-ethoxyethyl)-1H-benzimidazole-2-il]-1-piperidinyl]ethyl-alpha, alpha-dimethyl-benzeneacetic having formula (I), preparation methods thereof, pharmaceutical formulations containing polymoph 1 and the use of polymorph 1 for the treatment of allergic reactions and pathological processes mediated by histamine in mammals such as humans.

Description

field of invention [0001] The present invention relates to a kind of new 4-[2-[1-(2-ethoxyethyl)-1H-benzodiimazol-2-yl]-1-piperidinyl]ethyl of formula (I) base]-[alpha],[alpha]-dimethylphenylacetic acid (referred to herein as "bilastin") as a polymorphic form. [0002] [0003] Concerned herein are polymorphs of formula 1, processes for their preparation, pharmaceutical formulations containing polymorph 1 and use of polymorph 1 for the treatment of allergic reactions and histamine-mediated method of pathological process. Background of the invention [0004] US Patent No. 5,877,187 rights to bilastine, a formulation with antihistamine properties but no sedative or cardiovascular effects. The patent also relates to the method for preparing bilastine and the application of using the preparation to treat allergic reactions in mammals, but does not include or imply the possibility of the existence of polymorphs of the compound. [0005] In order to prepare bilastine-contain...

Claims

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Application Information

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IPC IPC(8): A61K31/445A61K31/454A61P37/00A61P37/08A61P43/00C07DC07D211/62C07D235/14C07D401/04
CPCA61K31/445C07D401/04A61P37/00A61P37/08A61P43/00
Inventor A·奥哈莱斯维内罗M·博尔德利马丁G·卡纳尔莫里H·布兰科富恩特M·L·卢塞罗德巴勃罗V·鲁维罗罗约R·莫斯克拉佩斯塔纳
Owner FAES FARMA SA
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