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Claims for Patent: 6,143,771

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Claims for Patent: 6,143,771

Title: Compounds
Abstract:The novel optically pure compounds Na.sup.+, Mg.sup.2+, Li.sup.+, K.sup.+, Ca.sup.2+ and N.sup.+ (R).sub.4 salts of (+)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H- benzimidazole or (-)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H- benzimidazole, in particular sodium and magnesium salt form thereof, where R is an alkyl with 1-4 carbon atoms, processes for the preparation thereof and pharmaceutical preparations containing the compounds as active ingredients, as well as the use of the compounds in pharmaceutical preparations and intermediates obtained by preparing the compounds.
Inventor(s): Lindberg; Per Lennart (Molndal, SE), von Unge; Sverker (Fjar.ang.s, SE)
Assignee: AstraZeneca AB (Sodertalje, SE)
Application Number:09/419,456
Patent Claims: 1. A pharmaceutical formulation for parenteral administration comprising an optically pure solid state Na.sup.+ salt of the (-)-enantiomer of 5-methoxy-2[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzi midazole as active ingredient, and a pharmaceutically acceptable carrier.

2. A pharmaceutical formulation for parenteral administration comprising an injection solution comprising an optically pure solid state Na.sup.+ salt of the (-)-enantiomer of 5-methoxy-2[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzi midazole as active ingredient, and a pharmaceutically acceptable carrier in the form of a pharmaceutically acceptable solvent having a volume sufficient to effect a solution having a concentration of 0.1 to 10% by weight of the active ingredient.

3. The pharmaceutical formulation according to claim 1 or 2, wherein the solid state salt is in substantially crystalline form.

4. The pharmaceutical formulation according to claim 1 or 2, further comprising a stabilizing agent, a buffering agent or a mixture thereof.

5. The pharmaceutical formulation for parenteral administration according to claim 1, comprising an injectable solution.

6. A method of inhibiting gastric acid secretion comprising the parenteral administration to a mammal including man in need of such treatment of a pharmaceutical formulation comprising a therapeutically effective amount of an optically pure solid state Na.sup.+ salt of the (-)-enantiomer of 5-methoxy-2[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzi midazole and a pharmaceutically acceptable carrier.

7. A method for the treatment of gastrointestinal inflammatory disease comprising the parenteral administration to a mammal including man in need of such treatment of a pharmaceutical formulation comprising a therapeutically effective amount of an optically pure solid state Na.sup.+ salt of the (-)-enantiomer of 5-methoxy-2[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzi midazole, and a pharmaceutically acceptable carrier.

8. The method according to claim 7, wherein a solution with the solvent carrier is prepared immediately before the administration.

9. The method according to claim 6 or 7, wherein the pharmaceutically acceptable carrier is in the form of a solvent.

10. The method of claim 7, wherein the solvent has a volume effecting a solution of a concentration of 0.1-10% by weight of the active ingredient.

11. A method of inhibiting gastric acid secretion comprising injecting a mammal including man in need of such treatment with a solution of an optically pure solid state Na.sup.+ salt of the (-)-enantiomer of 5-methoxy-2[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzi midazole and a pharmaceutically acceptable solvent having a volume sufficient to effect a solution having a concentration of 0.1 to 10% by weight of the active ingredient.

12. A method for the treatment of gastrointestinal inflammatory disease comprising injecting a mammal including man in need of such treatment with a solution of an optically pure solid state Na.sup.+ salt of the (-)-enantiomer of 5-methoxy-2[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzi midazole and a pharmaceutically acceptable solvent having a volume sufficient to effect a solution having a concentration of 0.1 to 10% by weight of the active ingredient.
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