Combination product of an aryl-substituted propanolamine derivative with at least one other active ingredient and the use of the product
OwnerHeiner Glombik, Wendelin Frick +2inventors
InventorsHeiner Glombik, Wendelin Frick, Hans-Ludwig Schafer, Werner Kramer
Life of this patent
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Abstract
The present invention is directed to an aryl-substituted propanolamine derivative of formula I 1 as described herein, a pharmaceutically acceptable salt or physiologically functional derivatives thereof, with an other active ingredient, or a pharmaceutically acceptable salt or physiologically functional derivatives thereof. The invention is also directed to the use of the combination product, pharmaceutical composition comprising the combination product and method for preparing the pharmaceutical composition.
Claims21
A composition of matter comprising a derivative of formula I
- 20
- in which
- R1 is phenyl optionally substituted by one to three mutually independent radicals, or heteroaryl optionally substituted by one to three mutually independent radicals, where the radicals are selected from the group consisting of 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, and wherein one or more hydrogen atom(s) in the alkyl radical is optionally replaced by fluorine, and wherein for the phenyl or pyridyl radical is optionally monosubstituted by methyl, methoxy or halogen;
- R2 is H, —OH, —CH2OH, —OMe, —CHO, or —NH2;
- R3 is saccharide residue, disaccharide residue, trisaccharide residue, or tetrasaccharide residue,
- wherein the saccharide residue, disaccharide residue, trisaccharide residue or tetrasaccharide residue is optionally substituted by one or more saccharide protective groups selected from the group of HO—SO2— and(HO)2—PO—;
- R4 is H, methyl, F, —OMe;
- R9 to R12 are, independently of one another, 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—, amino acid residue, or diamino acid residue, wherein the amino acid residue or diamino acid residue is optionally substituted by one or more amino acid protective groups, or a covalent bond;
- n is 0 or 1;or
- m is 0 or 1;and
- a pharmaceutically acceptable salt or physiologically functional derivatives thereof, with an other active ingredient, or a pharmaceutically acceptable salt or physiologically functional derivatives thereof. The invention is also directed to the use of the combination product, pharmaceutical composition comprising the combination product and method for preparing the pharmaceutical composition.
Dependencies are inferred from the claim text.