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US 2020/0347089 A1Published application
Novel galactoside inhibitor of galectins
AssigneeGalecto Biotech AB
InventorFredrik ZETTERBERG
Life of this patent
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Abstract
An α-D-galactopyranose compound of the general formula (1). The α-D-galactopyranose compound of formula (1) is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-1 to a ligand in a mammal, such as a human. Furthermore, a method for treatment of a disorder relating to the binding of a galectin, such as galectin-1 to a ligand in a mammal, such as a human.
Claims16
1-18. (canceled)
A D-galactopyranose compound of formula (1)
- wherein the pyranose ring is α-D-galactopyranose,
- R1 is selected from the group consisting of
- wherein the asterix * indicates the carbon atom of the heteroaromatic ring that is covalently attached to the triazole group of formula (1);
- wherein R2 is selected from the group consisting of OH and halogen;
- R3 is selected from the group consisting of hydrogen, C1-6 alkyl and halogen;
- R4 is selected from the group consisting of OH and halogen;
- R5 is selected from the group consisting of hydrogen, C1-6 alkyl and halogen;
- B1 is selected from a) an aryl, optionally substituted with a group selected from a halogen;
- CN;
- —COOH;
- —CONR29R30, wherein R29 and R30 are independently selected from H, C1-3 alkyl, cyclopropyl, and iso-propyl;
- C1-3 alkyl, optionally substituted with a F;
- cyclopropyl, optionally substituted with a F;
- isopropyl, optionally substituted with a F;
- OC1-3 alkyl, optionally substituted with a F;
- SC1-3 alkyl, optionally substituted with a F;
- O-cyclopropyl, optionally substituted with a F;
- O-isopropyl, optionally substituted with a F;
- NR31R32, wherein R31 and R32 are independently selected from H, C1-3 alkyl and isopropyl;
- OH;
- and R33—CONH—, wherein R33 is selected from C1-3 alkyl and cyclopropyl;
- b) a heterocycle, optionally substituted with a group selected from a halogen;
- CN;
- —COOH;
- —CONR35R36, wherein R35 and R36 are independently selected from H, C1-3 alkyl, cyclopropyl, and iso-propyl;
- C1-3 alkyl, optionally substituted with a F;
- cyclopropyl, optionally substituted with a F;
- isopropyl, optionally substituted with a F;
- OC1-3 alkyl, optionally substituted with a F;
- O-cyclopropyl, optionally substituted with a F;
- SC1-3 alkyl, optionally substituted with a F;
- O-isopropyl, optionally substituted with a F;
- NR37R38, wherein R37 and R38 are independently selected from H, C1-3 alkyl and isopropyl;
- OH;
- and R39—CONH— wherein R39 is selected from C1-3 alkyl and cyclopropyl;
- or
- a pharmaceutically acceptable salt or solvate thereof.
34 more elements
Dependencies are inferred from the claim text.