Claims
- 1. A method for treating gallstones, comprising administering to a patient in need thereof an effective amount of a 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 may be optionally replaced by fluorine, and wherein phenyl and pyridyl may be unsubstituted 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.
- 2. A method according to claim 1, further comprising administering at least one further hypolipidemic active substance.
- 3. A method for treating arteriosclerotic phenomena related to hyperlipidemia, comprising administering to a patient in need thereof an effective amount of a 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—OH3, —O—(C1-C6)-alkyl-O—(C1-C6)-alkyl-phenyl, —(C1-C6)-alkylthio, or pyridyl, wherein one or more hydrogen(s) in the alkyl radicals may be optionally replaced by fluorine, and wherein phenyl and pyridyl may be unsubstituted 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.
- 4. A method according to claim 3, further comprising administering at least one further hypolipidemic active substance.
- 5. A method for preventing gallstones, comprising administering to a patient in need thereof an effective amount of a 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—OH3, —O—(C1-C6)-alkyl-O—(C1-C6)-alkyl-phenyl, —(C1-C6)-alkylthio, or pyridyl, wherein one or more hydrogen(s) in the alkyl radicals may be optionally replaced by fluorine, and wherein phenyl and pyridyl may be unsubstituted 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.
- 6. A method according to claim 5, further comprising administering in combination at least one further hypolipidemic active substance.
- 7. A method for preventing arteriosclerotic phenomena related to hyperlipidemia, comprising administering to a patient in need thereof an effective amount of a 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 may be optionally replaced by fluorine, and wherein phenyl and pyridyl may be unsubstituted 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.
- 8. A method according to claim 7, further comprising administering at least one further hypolipidemic active substance.
Priority Claims (1)
Number |
Date |
Country |
Kind |
198 45 405 |
Oct 1998 |
DE |
|
Parent Case Info
This is a division of application Ser. No. 09/410,084, filed Oct. 1, 1999, now U.S. Pat. No. 6,245,744 which is incorporated herein by reference.
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Entry |
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