Thiazole Derivatives and Use Thereof
AssigneeLaboratoires Serono SA
InventorsAnna Quattropani, Jerome Dorbais, David Covini, Gwenaelle Desforges, Thomas Rueckle
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Abstract
The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
Claims28
1-30. (canceled)
A thiazole derivative according to Formula (I),
- wherein R1 is selected from —C(O)R5, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl C1-C6-alkyl, heteroaryl C1-C6-alkyl, C3-C8 cycloalkyl C1-C6-alkyl or heterocycloalkyl C1-C6-alkyl;
- R2 is selected from H, halogen, C1-C6-alkyl, C2-C6-alkenyl or C2-C6-alkynyl;
- R3 is selected from H, halogen, C1-C6-alkyl, C2-C6-alkenyl or C2-C6-alkynyl;
- R4 is selected from —C(O)R6, aryl, heteroaryl, heterocycloalkyl or C3-C8 cycloalkyl;
- R5 is selected from H, hydroxyl, alkoxy, amino, aryl, heteroaryl, C3-C8 cycloalkyl or heterocycloalkyl;
- R6 selected from H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl C1-C6-alkyl, heteroaryl C1-C6-alkyl or amino;
- and
- X is selected from S or O;
- and isomers, enantiomers, diastereomers, racemates or pharmaceutically acceptable salts thereof.
A thiazole derivative according to Formula (Ia)
- wherein R1 is selected from —C(O)R5, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, aryl C1-C6-alkyl, heteroaryl C1-C6-alkyl, C3-C8 cycloalkyl C1-C6-alkyl or heterocycloalkyl C1-C6-alkyl
- R2 is selected from H, halogen, C1-C6-alkyl, C2-C6-alkenyl or C2-C6-alkynyl;
- R3 is selected from H, halogen, C1-C6-alkyl, C2-C6-alkenyl or C2-C6-alkynyl;
- R5 is selected from H, hydroxyl, alkoxy, amino, aryl, heteroaryl, C3-C8 cycloalkyl or heterocycloalkyl;
- X is selected from S or O;
- and isomers, enantiomers, diastereomers, racemates or pharmaceutically acceptable thereof, with the proviso that the compounds of formula Ia are not the following compounds:
- [4,5′-Bithiazole]-2-acetonitrile, 2′-amino-4′-methyl;
- 2′-amino-4′-methyl-(phenylhydrazono)-[4,5′-Bithiazole]-2-acetonitrile;
- 2′-amino-[(4-chlorophenyl)hydrazono]-4′-methyl-[4,5′-Bithiazole]-2-acetonitrile;
- or
- [4,5′-Bithiazole]-4′-carboxylic acid, 2′-amino-2-methyl-, ethyl ester.
A method of treating autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, erythrocyte deficiency, graft rejection or lung injuries comprising the administration of a pharmaceutically effective amount of a compound of Formula I or Formula Ia to an individual in need of treatment.
A pharmaceutical composition comprising at least one thiazole derivative of Formula I or Formula Ia and a pharmaceutically acceptable carrier, diluent or excipient thereof.
Dependencies are inferred from the claim text.