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US 2003/0195145 A1Published application
Methods of treatment with combinations of statin and aryl-substituted propanolamine derivatives
AssigneeAventis Pharma Deutschland GmbH
InventorsWendelin Frick, Reinhard Kirsch, Heiner Glombik, Werner Kramer, Hans-Ludwig Schafer
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Abstract
Substituted propanolamine derivatives, their pharmaceutically tolerated salts and physiologically functional derivatives thereof are described. Also described are compounds of formula I 1 in which the radicals have the abovementioned meanings, and their physiologically tolerated salts, physiologically functional derivates and processes for their preparation. The compounds are suitable as, for example, hypolipidemics.
Claims12
A compound of formula I
- 28
- 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-C1)-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 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 was unsubstituted or was 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 more elements
Dependencies are inferred from the claim text.