Benzimidazole derivatives as dual histamine H1 and histamine H4 receptor ligands
AssigneeBioprojet
InventorsIsabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Stéphane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
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Abstract
Novel benzimidazole enantiomeric derivatives, their process of preparation and their therapeutical uses as dual H1 and H4 receptor ligands are disclosed.
Claims13
A method of treating inflammation comprising administering to a patient in need thereof an (S)-enantiomer of formula (II):
- wherein:
- * denotes the asymmetric carbon exhibiting a defined (S)-enantiomer stereochemistry;
- X represents H or F;
- R1, R2, R3, and R4 are identical or different and independently represent H, halogen, alkyl or alkoxy;
- and
- wherein one of X, R1, R2, R3, or R4 does not represent H;
- or pharmaceutically acceptable salts, tautomers, hydrates, or solvates thereof;
- wherein the (S)-enantiomer has H1 and H4 affinity.
A method of treating inflammation comprising administering a pharmaceutical composition comprising the (S)-enantiomer of formula (II):
- wherein:
- * denotes the asymmetric carbon exhibiting a defined (S)-enantiomer stereochemistry;
- X represents H or F;
- R1, R2, R3, and R4 are identical or different and independently represent H, halogen, alkyl or alkoxy;
- and
- wherein one of X, R1, R2, R3, or R4 does not represent H;
- or pharmaceutically acceptable salts, tautomers, hydrates, or solvates thereof;
- and a pharmaceutically acceptable excipient;
- wherein the (S)-enantiomer has H1 and H4 affinity.
A method of treating inflammation comprising administering to a patient in need thereof an (S)-enantiomer of formula (II):
- wherein:
- * denotes the asymmetric carbon exhibiting a defined (S)-enantiomer stereochemistry;
- X represents H or F;
- R1, R2, R3, and R4 are identical or different and independently represent H, halogen, alkyl or alkoxy;
- and
- wherein one of X, R1, R2, R3, or R4 does not represent H;
- or pharmaceutically acceptable salts, tautomers, hydrates, or solvates thereof;
- wherein the (S)-enantiomer has H1 and H4 affinity.
Dependencies are inferred from the claim text.