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Co-crystals and pharmaceutical compositions comprising the same

A technology of co-crystals and compositions, applied in the field of co-crystals and pharmaceutical compositions containing the co-crystals, can solve problems such as uncertain prospects for anti-HCV vaccines

Inactive Publication Date: 2010-09-15
VERTEX PHARMA INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Additionally, the prospects for an effective anti-HCV vaccine remain uncertain

Method used

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  • Co-crystals and pharmaceutical compositions comprising the same
  • Co-crystals and pharmaceutical compositions comprising the same
  • Co-crystals and pharmaceutical compositions comprising the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0055] Example 1. Prepared by ball milling

[0056] Mix VX-950 and an equimolar equivalent of the co-crystal former (e.g., 2,4-dihydroxybenzoic acid or 3-methoxy-4-hydroxybenzoic acid) with a solvent (e.g., butanone or ethyl acetate) . The components can then be milled at a frequency of 15 Hz for 10 minutes using a Wig-L-Bug instrument, such as a Retsch MM200 (GlenMills Inc, Clifton, NJ). After milling, the raw material is dried, for example in a vacuum oven at 75° C. for 2 hours, to obtain the co-crystal of the present invention.

Embodiment 2

[0057] Example 2. Preparation by melting method

[0058] Mix VX-950 and equimolar equivalents of the co-crystal former (e.g., 2,4-dihydroxybenzoic acid or 3-methoxy-4-hydroxybenzoic acid), e.g., by vortexing for 5 min, with or without solvent . The mixture is then placed in a reaction block (eg RR 98072 from Radley Discovery Technologies), closed and heated to endotherm. The mixture was maintained at the endothermic temperature for 30 minutes, the lid was then removed to cool the resulting mixture at ambient conditions, and the solvent (if used) removed to obtain the co-crystal of the present invention.

Embodiment 3

[0059] Example 3. Preparation by solvent-evaporation method

[0060] 2,4-Dihydroxybenzoic acid : 200 mg VX-950 and 80 mg 2,4-dihydroxybenzoic acid (Sigma Chemicals Co., St. Louis, MO, USA) were charged into a 20 mL glass vial. 100 μL of dichloromethane and 100 μL of acetonitrile were then added to the vial. The vial containing the mixture was capped and the mixture was stirred using a magnetic stir bar at 600 rpm for 16 hours at room temperature. The crystalline solid was isolated and the superficial liquid was removed by filter paper to yield a co-crystal of VX-950 and 2,4-dihydroxybenzoic acid.

[0061] 3-methoxy-4-hydroxybenzoic acid : 200 mg of VX-950 and 80 mg of 3-methoxy-4-hydroxybenzoic acid (Sigma Chemicals Co., St. Louis, MO, USA) were charged into a 20 mL glass vial. 100 μL of dichloromethane and 100 μL of acetonitrile were then added to the vial. The vial containing the mixture was capped and the mixture was stirred using a magnetic stir bar at 600 rpm for 7...

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PUM

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Abstract

The invention relates to co-crystals and compositions each comprising VX-950 and a co-crystal former selected from the group consisting of 3-methoxy-4-hydroxybenzoic acid, 2,4-dihydroxybenzoic acid, and 2,5-dihydroxybenzoic acid. Also within the scope of this invention are methods of making and using the same.

Description

[0001] cross reference [0002] This application claims priority to US Application No. 60 / 969,023, filed August 30, 2007, the entire contents of which are incorporated herein by reference. Background of the invention [0003] Hepatitis C virus ("HCV") is a compelling human medical problem. HCV is considered to be the causative factor of most non-A non-B hepatitis, with an estimated global human prevalence of 3% [A.Alberti et al., "Natural History of Hepatitis C," J.Hepatology, 31(Suppl.1 ), pp. 17-24 (1999)]. Nearly four million individuals are infected in the United States alone [M.J. Alter et al., "The Epidemiology of Viral Hepatitis in the United States", Gastroenterol. Clin. North Am., 23, pp. 437-455 (1994); M.J. Alter " Hepatitis C Virus Infection in the United States," J. Hepatology, 31 (Suppl. 1), pp. 88-91 (1999)]. [0004] After first exposure to HCV, only about 20% of infected individuals develop acute clinical hepatitis, while others appear to clear the infecti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D403/12A61K31/454A61P1/16
CPCC07D403/12A61P1/16A61P31/12A61P31/14
Inventor 张越刚P·R·康内利S·约翰斯顿
Owner VERTEX PHARMA INC
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