Benzothiepine 1, 1-dioxide derivatives, a process for their preparation, pharmaceuticals comprising these compounds, and their use

1. A coated pharmaceutical composition comprising at least one compound of formula I

in which

R 1 is methyl, ethyl, propyl, or butyl;

R 2 is H, OH, NH 2 , or NH—(C 1 –C 6 )-alkyl;

R 3 is a sugar radical, a disugar radical, a trisugar radical, or a tetrasugar radical, wherein said radicals are optionally mono- or polysubstituted by a sugar protective group;

R 4 is methyl, ethyl, propyl, or butyl;

R 5 is methyl, ethyl, propyl, or butyl;

Z is —(C═O) n —(C 0 –C 16 )-alkyl, —(C═O) n —(C 0 –C 16 )-alkyl-NH—, —(C═O) n —(C 0 –C 16 )-alkyl-O—, —(C═O) n —(C 1 –C 16 )-alkyl-(C═O) m , or a covalent bond;

n is 0 or 1;

m is 0 or 1;

or a pharmaceutically tolerable salt thereof, or a physiologically functional derivative thereof,

and at least one pharmacologically tolerable excipient.

2. A coated pharmaceutical composition as claimed in claim 1 , wherein in the formula I:

R 1 is ethyl, propyl, or butyl;

R 2 is H, OH, NH 2 , or NH—(C 1 –C 16 )-alkyl;

R 3 is a sugar radical or disugar radical, wherein said radicals are optionally mono- or polysubstituted by a sugar protective group;

R 4 is methyl, ethyl, propyl, or butyl;

R 5 is methyl, ethyl, propyl, or butyl;

Z is —(C═O) n —(C 0 –C 16 )-alkyl-, —(C═O) n —(C 0 –C 16 )alkyl-NH—, —(C═O) n —(C 0 –C 16 )-alkyl-O—, —(C═O) n —(C 1 –C 16 )-alkyl-(C═O) m , or a covalent bond;

n is 0 or 1; and

m is 0 or 1 .

3. A coated pharmaceutical composition as claimed in claim 1 , wherein in the formula I:

R 1 is ethyl or butyl;

R 2 is OH;

R 3 is a sugar radical, wherein the sugar radical is optionally mono- or polysubstituted by a sugar protective group;

R 4 is methyl;

R 5 is methyl; and

Z is —(C═O)–(C 0 –C 4 )-alkyl or a covalent bond.

4. A coated pharmaceutical composition as claimed in claim 1 , wherein the composition comprises a compound of the following structure:

or a pharmaceutically tolerable salt thereof.

5. A coated pharmaceutical composition as claimed in claim 1 , wherein the composition comprises a compound of the following structure:

or a pharmaceutically tolerable salt thereof.

6. A coated pharmaceutical composition as claimed in claim 1 , wherein the composition is a delayed-release composition.

7. A coated pharmaceutical composition as claimed in claim 1 , wherein the composition is acid-resistant.

8. A coated pharmaceutical composition as claimed in claim 1 , wherein the composition is an enteric composition.

9. A coated pharmaceutical composition as claimed in claim 1 , wherein the coating comprises cellulose acetate phthalate, polyvinyl acetate phthalate, hydroxypropylmethylcellulose phthalate or one or more anionic polymers of methacrylic acid and methyl methacrylate.

10. A coated pharmaceutical composition as claimed in claim 8 , wherein the coating comprises cellulose acetate phthalate, polyvinyl acetate phthalate, hydroxypropylmethylcellulose phthalate or one or more anionic polymers of methacrylic acid and methyl methacrylate.