Unlock instant, AI-driven research and patent intelligence for your innovation.

Co-crystals of benzimidazole compounds

A technology of co-crystals and compounds, applied in the field of co-crystals of benzimidazole compounds, can solve the problems of hindering the pharmaceutically acceptable means of compounds and low solubility of benzimidazole compounds

Inactive Publication Date: 2018-07-17
法斯法尔玛有限公司
View PDF11 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] with selective H 1 The aforementioned benzimidazole compounds with antihistamine activity have low solubility in water, which hampers the development of pharmaceutically acceptable means of administering said compounds in liquid form

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Co-crystals of benzimidazole compounds
  • Co-crystals of benzimidazole compounds
  • Co-crystals of benzimidazole compounds

Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment approach

[0066] In one embodiment, the co-crystal comprises bilastine and glutaric acid. In a specific embodiment, the molar ratio of bilastine: glutaric acid is 1:1. In a specific embodiment, the molar ratio of bilastine:glutaric acid is 2:1. In another specific embodiment, said co-crystal of bilastine and glutaric acid comprises water molecules, ie it is a hydrate. In one embodiment, the molar ratio of bilastine: glutaric acid: water in the hydrate is between 2:1:3 and 2:1:1.

[0067] In a specific embodiment, the present invention discloses a co-crystal crystalline form known as GL(I) having a bilastine:glutaric acid molar ratio of 2:1, the X-ray powder diffraction pattern of which shows The characteristic peaks at the reflection angles [2θ°]±0.2° disclosed in Table 1.1 are shown.

[0068] In a specific embodiment, the present invention discloses a 2:1 molar ratio of bilastine:glutaric acid in a co-crystalline crystalline form known as GL(IV) having an X-ray powder diffraction pa...

Embodiment 1

[0136] Example 1. Bilastine / glutaric acid co-crystal

Embodiment 11

[0137] Example 1.1. Crystalline form GL(I)_bilastine / glutaric acid 2:1 co-crystal

[0138] The crystalline form known as GL(I) was obtained by wet milling a bilastine:glutaric acid (1:2) mixture in water.

[0139] This crystalline form was also obtained by slurrying bilastine (120 mg) and glutaric acid in water (15 mL) in a stoichiometric ratio of 1:1 or 1:2. After stirring for 15 hours, the resulting solid suspended in water was isolated by filtration, washed with water and dried in vacuo. This crystalline form was also seeded with GL(I) in a suspension consisting of BLN(I) (1000 mg, 2.157 mmol) and glutaric acid (570.0 mg, 4.314 mmol) in water (10 mL) at room temperature. get. After stirring at room temperature for 18 hours, the resulting solid suspended in water was isolated by filtration, washed with water (2 x 1 mL) and dried under vacuum within 18 hours to afford 974 mg of GL(I) as a white solid (81% yield) .

[0140] By XPRD (see Figure 1.1.a )), 1 H-NMR (see ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to a cocrystal comprising a) at least bilastine and, b) at least a cocrystal forming compound selected from the group consisting of glutaric acid, adipic acid, sorbic acid, succinic acid, benzoic acid, 4-aminobenzoic acid, L-malic acid, resorcinol, methyl 4-hydroxy benzoate and N-(4- hydroxyphenyl)acetamide and mixtures thereof, or a solvate thereof. The invention further relates to methods for obtaining said cocrystals and to their use in the treatment and / or prevention of conditions mediated by H1 histamine receptor, such as allergic disorders or diseases. The inventionalso relates to a method for increase the aqueous solubility of the above compounds of formula (I).

Description

technical field [0001] The present invention relates to co-crystals of benzimidazole compounds, methods for obtaining them and their use in pharmaceutical compositions, especially their use in antihistamines and antiallergic compositions. The present invention also relates to a method of increasing the water solubility of benzimidazole compounds. Background technique [0002] It has long been known that histamine plays a very important role in allergic-type diseases such as allergic rhinitis, conjunctivitis, rhinoconjunctivitis, dermatitis, urticaria and asthma. acting on H 1 - Antihistamine compounds at the receptor's histamine level are useful in the treatment of such conditions. [0003] Documents EP 0818454 A1 and EP 0580541 A1 disclose the selective H 1 Benzimidazole compounds with antihistamine activity and no proarrhythmic effects. Patent application EP14382576.8 also discloses H 1 Benzimidazole compounds with antihistamine activity and lack of activity on the ce...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/04A61K31/445A61P37/08
CPCA61P11/02A61P11/06A61P17/00A61P17/04A61P27/02A61P37/08C07D401/04C07B2200/13C07C39/10C07C55/10C07C55/12C07C55/14C07C57/10C07C59/245C07C63/06C07C69/88C07C229/60C07C235/34
Inventor 贡萨洛·埃尔南德斯·埃雷罗维克托·卢比奥·拉约内夫塔利·加西亚·多明格斯贡萨洛·纳尔·莫里尼古拉斯·泰松卡米·西蒙尼斯·冈萨雷斯约尔迪·德米尔文纽
Owner 法斯法尔玛有限公司
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com