Claims
- 1. A combination, comprising at least one compound of formula I wherein:R1 is phenyl or heteroaryl, wherein the aromatic or heteroaromatic ring is unsubstituted, or is mono- to trisubstituted by fluorine, chlorine, bromine, iodine, —OH, —CF3, —NO2, —CN, —(C1-C8)-alkoxy, —(C1-C8)-alkyl, —NH2, —NH—R9, —N(R9)R10, —CHO, —COOH, —COOR11, —(C═O)—R12, —(C1-C6)-alkyl-OH, —(C1-C6)-alkyl(—OH)-phenyl, —(C1-C6)-alkyl-CF3, —(C1-C6)-alkyl-NO2, —(C1-C6)-alkyl-CN, —(C1-C6)-alkyl-NH2, —(C1-C6)-alkyl-NR—R9, —(C1-C6)-alkyl-N(R9)R10, —(C1-C6)-alkyl-CHO, —(C1-C6)-alkyl-COOH, —(C1-C6)-alkyl-COOR11, —(C1-C6)-alkyl-(C═O)—R12, —O—(C1-C6)-alkyl-OH, —O—O—(C1-C6)-alkyl-CF3, —O—(C1-C6)-alkyl-NO2, —O—(C1-C6)-alkyl-CN, —(C1-C6)-alkyl-NH2, —O—(C1-C6)-alkyl-NH—R9, —O—(C1-C6)-alkyl-N(R9)R10, —O—(C1-C6)-alkyl-CHO, —O—(C1-C6)-alkyl-COOH, —O—(C1-C6)-alkyl-COOR11, —O—(C1-C6)-alkyl-(C═O)—R12, —N—SO3H, —SO2—CH3, —O—(C1-C6)-alkyl-O—(C1-C6)-alkyl-phenyl, —(C1-C6)-alkylthio, or pyridyl, wherein one or more hydrogen(s) in the alkyl radicals is optionally replaced by fluorine, and wherein phenyl and pyridyl are unsubstiuted or monosubstituted by methyl, methoxy, or halogen; R2 is H, —OH, —CH2OH, —OMe, CHO, or —NH2; R3 is a sugar residue, disugar residue, trisugar residue, tetrasugar residue, wherein the sugar residue, disugar residue, trisugar residue or tetrasugar residue is unsubstituted or is mono- or polysubstituted by a sugar protective group, HO—SO2, or (HO)2—PO; R4 is H, methyl, F, or —OMe; R9 to R12 each independently of one another is H or —(C1-C8)-alkyl; Z is —NH—(C0-C16)-alkyl-C═O—, —O—(C0-C16)-alkyl-C═O—, —(C═O)m—(C1-C16)-alkyl-(C═O)n, an amino acid residue, a diamino acid residue, wherein the amino acid residue or diamino acid residue is unsubstituted, or mono- or polysubstituted by an amino acid protective group, or a covalent bond; n is 0 or 1; m is 0 or 1; or a pharmaceutically tolerated salt, or a physiologically functional derivative thereof, and at least one statin.
- 2. A pharmaceutical composition, comprising the combination as claimed in claim 1 and a pharmacologically tolerated excipient.
- 3. The pharmaceutical composition of claim 2, further comprising at least one hypolipidemic active substance.
- 4. A method for preventing gallstones, comprising administering to a patient in need thereof an effective amount of the combination as claimed in claim 1.
- 5. A method for treating gallstones, comprising administering to a patient in need thereof an effective amount of the combination as claimed in claim 1.
- 6. A method for treating hyperlipidemia, comprising administering to a patient in need thereof an effective amount of the combination as claimed in claim 1.
- 7. A method for preventing gallstones, comprising administering to a patient in need thereof an effective amount of the combination as claimed in claim 1 and at least one further hypolipidemic active substance.
- 8. A method for treating gallstones, comprising administering to a patient in need thereof an effective amount of the combination as claimed in claim 1 and at least one further hypolipidemic active substance.
- 9. A method for treating hyperlipidemia, comprising administering to a patient in need thereof an effective amount of the combination as claimed in claim 1 and at least one further hypolipidemic active substance.
- 10. A combination of claim 1, wherein said at least one statin comprises simvastatin, fluvastatin, pravastatin, cerivastatin, lovastatin, or atorvastatin.
- 11. A pharmaceutical composition, comprising the combination as claimed in claim 10 and a pharmacologically tolerated excipient.
- 12. The pharmaceutical composition of claim 11, further comprising at least one hypolipidemic active substance.
- 13. A method for preventing gallstones, comprising administering to a patient in need thereof an effective amount of the combination as claimed in claim 10.
- 14. A method for treating gallstones, comprising administering to a patient in need thereof an effective amount of the combination as claimed in claim 10.
- 15. A method for treating hyperlipidemia, comprising administering to a patient in need thereof an effective amount of the combination as claimed in claim 10.
- 16. A method for preventing gallstones, comprising administering to a patient in need thereof an effective amount of the combination as claimed in claim 10 and at least one further hypolipidemic active substance.
- 17. A method for treating gallstones, comprising administering to a patient in need thereof an effective amount of the combination as claimed in claim 10 and at least one further hypolipidemic active substance.
- 18. A method for treating hyperlipidemia, comprising administering to a patient in need thereof an effective amount of the combination as claimed in claim 10 and at least one further hypolipidemic active substance.
- 19. A combination, comprising at least one compound of formula I wherein:R1 is phenyl or heteroaryl, wherein the aromatic or heteroaromatic ring is unsubstituted, or is mono- to trisubstituted by fluorine, chlorine, bromine, iodine, —OH, —CF3, —NO2, —CN, —(C1-C8)-alkoxy, —(C1-C8)-alkyl, —NH2, —NH—R9, —N(R9)R10, —CHO, —COOH, —COOR11, —(C═O)—R12, —(C1-C6)-alkyl-OH, —(C1-C6)-alkyl(—OH)-phenyl, —(C1-C6)-alkyl-CF3, —(C1-C6)-alkyl-NO2, —(C1-C6)-alkyl-CN, —(C1-C6)-alkyl-NH2, —(C1-C6)-alkyl-NH—R9, —(C1-C6)-alkyl-N(R9)R10, —(C1-C6)-alkyl-CHO, —(C1-C6)-alkyl-COOH, —(C1-C6)-alkyl-COOR11, —(C1-C6)-alkyl-(C═O)—R12, —O—(C1-C6)-alkyl-OH, —O—(C1-C6)-alkyl-CF3, —O—(C1-C6)-alkyl-NO2, —O—(C1-C6)-alkyl-CN, —O—(C1-C6)-alkyl-NH2, —O—(C1-C6)-alkyl-NH—R9, —O—(C1-C6)-alkyl-N(R9)R10, —O—(C1-C6)-alkyl-CHO, —O—(C1-C6)-alkyl-COOH, —O—(C1-C6)-alkyl-COOR11, —O—(C1-C6)-alkyl-(C═O)—R12, —N—SO3H, —SO2—CH3, —O—(C1-C6)-alkyl-O—(C1-C6)-alkyl-phenyl, —(C1-C6)-alkylthio, or pyridyl, wherein one or more hydrogen(s) in the alkyl radicals is optionally replaced by fluorine, and wherein phenyl and pyridyl are unsubstiuted or monosubstituted by methyl, methoxy, or halogen; R2 is H, —OH, —CH2OH, —OMe, CHO, or —NH2; R3 is a sugar residue, disugar residue, trisugar residue, tetrasugar residue, wherein the sugar residue, disugar residue, trisugar residue or tetrasugar residue is unsubstituted or is mono- or polysubstituted by a sugar protective group, HO—SO2, or (HO)2—PO; R4 is H, methyl, F, or —OMe; R9 to R12 each independently of one another is H or —(C1-C8)-alkyl; Z is —NH—(C0-C16)-alkyl-C═O—, —O—(C0-C16)-alkyl-C═O—, —(C═O)m—(C1-C6)-alkyl-(C═O)n, an amino acid residue, a diamino acid residue, wherein the amino acid residue or diamino acid residue is unsubstituted, or mono- or polysubstituted by an amino acid protective group, or a covalent bond; n is 0 or 1; m is 0 or 1; or a pharmaceutically tolerated salt, or a physiologically functional derivative thereof, and pravastatin.
- 20. A pharmaceutical composition, comprising the combination as claimed in claim 19 and a pharmacologically tolerated excipient.
- 21. A combination, comprising at least one compound of formula I wherein:R1 is phenyl or heteroaryl, wherein the aromatic or heteroaromatic ring is unsubstituted, or is mono- to trisubstituted by fluorine, chlorine, bromine, iodine, —OH, —CF3, —NO2, —CN, —(C1-C8)-alkoxy, —(C1-C8)-alkyl, —NH2, —NH—R9, —N(R9)R10, —CHO, —COOH, —COOR11, —(C═O)—R12, —(C1-C6)-alkyl-OH, —(C1-C6)-alkyl(—OH)-phenyl, —(C1-C6)-alkyl-CF3, —(C1-C6)-alkyl-NO2, —(C1-C6)-alkyl-CN, —(C1-C6)-alkyl-NH2, —(C1-C6)-alkyl-NH—R9, —(C1-C6)-alkyl-N(R9)R10, —(C1-C6)-alkyl-CHO, —(C1-C6)-alkyl-COOH, —(C1-C6)-alkyl-COOR11, —(C1-C6)-alkyl-(C═O)—R12, —O—(C1-C6)-alkyl-OH; —O—(C1-C6)-alkyl-CF3, —O—(C1-C6)-alkyl-NO2, —O—(C1-C6)-alkyl-CN, —O—(C1-C6)-alkyl-NH2, —O—(C1--C6)-alkyl-NH—R9, —O—(C1-C6)-alkyl-N(R9)R10, —O—(C1-C6)-alkyl-CHO, —O—(C1-C6)-alkyl-COOH, —O—(C1-C6)-alkyl-COOR11, —O—(C1-C6)-alkyl-(C═O)—R12, —N—SO3H, —SO2—CH3, —O—(C1-C6)-alkyl-O—(C1-C6)-alkyl-phenyl, —(C1-C6)-alkylthio, or pyridyl, wherein one or more hydrogen(s) in the alkyl radicals is optionally replaced by fluorine, and wherein phenyl and pyridyl are unsubstiuted or monosubstituted by methyl, methoxy, or halogen; R2 is H, —OH, —CH2OH, —OMe, CHO, or —NH2; R3 is a sugar residue, disugar residue, trisugar residue, tetrasugar residue, wherein the sugar residue, disugar residue, trisugar residue or tetrasugar residue is unsubstituted or is mono- or polysubstituted by a sugar protective group, HO—SO2, or (HO)2—PO; R4 is H, methyl, F, or —OMe; R9 to R12 each independently of one another is H or —(C1-C8)-alkyl; Z is —NH-(C0-C16)-alkyl-C═O—, —O—(C0-C16)-alkyl-C═O—, —(C═O)m—(C1-C16)-alkyl-(C═O)n, an amino acid residue, a diamino acid residue, wherein the amino acid residue or diamino acid residue is unsubstituted, or mono- or polysubstituted by an amino acid protective group, or a covalent bond; n is 0 or 1; m is 0 or 1; or a pharmaceutically tolerated salt, or a physiologically functional derivative thereof, and atorvastatin.
- 22. A pharmaceutical composition, comprising the combination as claimed in claim 21 and a pharmacologically tolerated excipient.
Priority Claims (1)
Number |
Date |
Country |
Kind |
198 45 405 |
Oct 1998 |
DE |
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Parent Case Info
This is a continuation of Ser. No. 09/833,676 filed, Apr. 13, 2001, which is a division of application Ser. No. 09/410,084, filed Oct. 1, 1999, now U.S. Pat. No. 6,245,744, all of which are incorporated herein by reference.
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Date |
Kind |
5571816 |
Kampe et al. |
Nov 1996 |
A |
5874451 |
Glombik et al. |
Feb 1999 |
A |
6391915 |
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May 2002 |
B2 |
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Number |
Date |
Country |
0 557 879 |
Sep 1993 |
EP |
0 869 121 |
Oct 1998 |
EP |
WO 9316055 |
Aug 1993 |
WO |
Non-Patent Literature Citations (3)
Entry |
English Abstracts, Derwent No. 93-274361/199335. |
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Continuations (1)
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Number |
Date |
Country |
Parent |
09/833676 |
Apr 2001 |
US |
Child |
09/985149 |
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US |