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US 2002/0177610 A1Published application
Combinations with statin and aryl-substituted propanolamine derivatives, their preparation, pharmaceuticals comprising them, and their use
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
- 26
- 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)-alky-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 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.