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US 12,291,520 B2Granted
Galectin-3 inhibiting 2-hydroxycycloalkane-1-carbamoyl derivatives
AssigneeIdorsia Pharmaceuticals Ltd
InventorsMartin Bolli, John Gatfield, Corinna Grisostomi, Lubos Remen, Christoph Sager, Cornelia Zumbrunn
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Abstract
The present invention relates to compounds of Formula (I) wherein Ar1, Ar2, L, n, and R1 are as described in the description, their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of Formula (I), and especially to their use as Galectin-3 inhibitors.
Claims20
A compound of formula (I)
- wherein
- n represents the integer 1 or 2;
- Ar1 represents
- aryl which is mono-, di-, tri-, tetra-, or penta-substituted, wherein the substituents are independently selected from halogen;
- methyl;
- cyano;
- methoxy;
- trifluoromethyl;
- and trifluoromethoxy;
- 5- or 6-membered heteroaryl, wherein said 5- or 6-membered heteroaryl independently is unsubstituted, mono-or di-substituted, wherein the substituents are independently selected from halogen, methyl, cyano, and methoxy;
- or
- 9- or 10-membered heteroaryl, wherein said 9- or 10-membered heteroaryl independently is unsubstituted, or mono-substituted with methyl;
- R1 represents
- hydroxy;
- C1-3-alkoxy;
- —O—CO—C1-3-alkyl;
- —O—CH2—CH2—OH;
- or
- —O—CH2—CO—OH;
- L represents a direct bond or methylene;
- and
- Ar2 represents
- phenyl, wherein said phenyl is unsubstituted, mono-, di-or tri-substituted wherein the substituents are independently selected from C1-6-alkyl, C3-6-cycloalkyl, —CH2-C3-6-cycloalkyl, C1-3-fluoroalkyl, C1-3-fluoroalkoxy, C1-3-alkoxy, halogen, and cyano;
- 5- or 6-membered heteroaryl, wherein said 5- or 6-membered heteroaryl independently is unsubstituted, mono-, di-, or tri-substituted wherein the substituents are independently selected from C1-6-alkyl, C3-6-cycloalkyl, —CH2-C3-6-cycloalkyl, C1-3-fluoroalkyl, C1-3-fluoroalkoxy, C1-3-alkoxy, halogen, and cyano;
- 9-membered bicyclic heteroaryl or 10-membered bicyclic heteroaryl, wherein said 9- or 10-membered bicyclic heteroaryl independently is unsubstituted, mono-or di-substituted, wherein the substituents are independently selected from methyl, methoxy, and halogen;
- or
- naphthyl;
- or a pharmaceutically acceptable salt thereof.
25 more elements
Dependencies are inferred from the claim text.