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Claims for Patent: 6,939,971

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Claims for Patent: 6,939,971

Title: Benzimidazole compound crystal
Abstract:A novel crystal of (R)-2-[[[3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl]methyl]sulfinyl]-1 H-benzimidazole or a salt thereof of the present invention is useful for an excellent antiulcer agent.
Inventor(s): Fujishima; Akira (Sanda, JP), Aoki; Isao (Kawanishi, JP), Kamiyama; Keiji (Ibaraki, JP)
Assignee: Takeda Pharmaceutical Company, Ltd. (Osaka, JP)
Application Number:10/655,114
Patent Claims: 1. A method of treating Zollinger-Ellison syndrome in a mammal in need thereof which comprises administering to said mammal an effective amount of a crystalline compound of (R)-2-(((3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl)methyl)sulfinyl)-1 H-benzimidazole or a salt thereof and a pharmaceutically acceptable excipient, carrier or diluent.

2. The method of claim 1 wherein said crystalline compound is (R)-2-(((3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl)methyl)sulfinyl)-1 H-benzimidazole.

3. The method of claim 2 wherein said crystalline compound has an X-ray powder diffraction analysis pattern with characteristic peaks at interplanar spacings (d) of 11.68, 6.77, 5.84, 5.73, 4.43, 4.09, 3.94, 3.89, 3.69, 3.41 and 3.11 Angstrom.

4. The method of claim 1 wherein said crystalline compound is (R)-2-(((3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl)methyl)sulfinyl)-1 H-benzimidazole 1.5 hydrate and has an X-ray powder diffraction analysis pattern with characteristic peaks at interplanar spacings (d) of 13.22, 9.60, 8.87, 8.05, 6.61, 5.92, 5.65, 5.02, 4.49, 3.50 and 3.00 Angstrom.

5. A method of treating reflux esophagitis in a mammal in need thereof which comprises administering to said mammal an effective amount of a crystalline compound of (R)-2-(((3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl)methyl)sulfinyl)-1 H-benzimidazole or a salt thereof and a pharmaceutically acceptable excipient, carrier or diluent.

6. The method of claim 5 wherein said crystalline compound is (R)-2-(((3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl)methyl)sulfinyl)-1 H-benzimidazole.

7. The method of claim 6 wherein said crystalline compound has an X-ray powder diffraction analysis pattern with characteristic peaks at interplanar spacings (d) of 11.68, 6.77, 5.84, 5.73, 4.43, 4.09, 3.94, 3.89, 3.69, 3.41 and 3.11 Angstrom.

8. The method of claim 5 wherein said crystalline compound is (R)-2-(((3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl)methyl)sulfinyl)-1 H-benzimidazole 1.5 hydrate and has an X-ray powder diffraction analysis pattern with characteristic peaks at interplanar spacings (d) of 13.22, 9.60, 8.87, 8.05, 6.61, 5.92, 5.65, 5.02, 4.49, 3.50 and 3.00 Angstrom.

9. A method of eradicating Helicobacter pylori in a mammal in need thereof which comprises administering to said mammal an effective amount of a crystalline compound of (R)-2-(((3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl)methyl)sulfinyl)-1 H-benzimidazole or a salt thereof and a pharmaceutically acceptable excipient, carrier or diluent.

10. The method of claim 9 further comprising administering one to three other active ingredients.

11. The method of claim 10 wherein said crystalline compound and said other active ingredient are administered simultaneously or in intervals.

12. The method of claim 10 wherein said other active ingredient is selected from the group consisting of an anti-Helicobacter pylori action substance, an imidazole compound, a bismuth salt, a quinoline compound and combinations thereof.

13. The method of claim 12 wherein said anti-Helicobacter pylori action substance is selected from the group consisting of antibiotic penicillins, antibiotic macrolides and combinations thereof.

14. The method of claim 12 wherein said imidazole compound is metronidazole.

15. The method of claim 9 wherein said crystalline compound is (R)-2-(((3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl)methyl)sulfinyl)-1 H-benzimidazole.

16. The method of claim 15 wherein said crystalline compound has an X-ray powder diffraction analysis pattern with characteristic peaks at interplanar spacings (d) of 11.68, 6.77, 5.84, 5.73, 4.43, 4.09, 3.94, 3.89, 3.69, 3.41 and 3.11 Angstrom.

17. The method of claim 9 wherein said crystalline compound is (R)-2-(((3-methyl-4-(2,2,2-trifluoroethoxy)-2-pyridinyl)methyl)sulfinyl)-1 H-benzimidazole 1.5 hydrate and has an X-ray powder diffraction analysis pattern with characteristic peaks at interplanar spacings (d) of 13.22, 9.60, 8.87, 8.05, 6.61, 5.92, 5.65, 5.02, 4.49, 3.50 and 3.00 Angstrom.
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