Thiazole derivatives and use thereof
AssigneeMerck Serono SA
InventorsAnna QUATTROPANI, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
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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, neturodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
Claims26
A thiazole according to Formula (I),
- wherein R1 is a moiety of the formula —NR5R6;
- R2, R3 and R5 are selected independently from H, C1-C6-alkyl, C2-C6-alkenyl and C2-C6-alkynyl;
- R4 is selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl and C2-C6-alkynyl and NR8R9 wherein R8 and R9 are independently selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkyl alkoxy carbonyl and C1-C6-alkyl acyloxy;
- R6 is selected from the group consisting of C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkyl alkoxy, aryl, heteroaryl, C3-C8-cycloalkyl, C3-C8-heterocycloalkyl, C1-C6-alkyl aryl, C1-C6-alkyl heteroaryl, C1-C6-alkyl C3-C8-cycloalkyl, C1-C6-alkyl C3-C8-heterocycloalkyl, C1-C6-alkyl acyl, C1-C6-alkyl carboxy, C1-C6-alkyl amino, C1-C6-alkyl aminocarbonyl, C1-C6-alkyl alkoxycarbonyl and C1-C6-alkyl acyl amino;
- or R5 and R6, together with the carbon atoms they are linked to, form a 5-8-membered saturated or aromatic ring containing optionally one or more heteroatoms selected from the group consisting of O, N and S;
- and
- X is O;
- as well as isomers thereof said thiazole being suitable as active ingredient in a medicament.
A thiazole according to Formula (I),
- wherein R1 is a moiety of the formula —NR5R6;
- R2, R3 and R5 are selected independently from H, C1-C6-alkyl, C2-C6-alkenyl and C2-C6-alkynyl;
- R4 is selected from the grout consisting of H, C1-C6-alkyl, C2-C6-alkenyl and C2-C6-alkynyl and NR8R9 wherein R8 and R9 are independently selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkyl alkoxy carbonyl and C1-C6-alkyl acyloxy;
- R6 is selected from the group consisting of C1-C6-alkyl, C2-C6-alkynyl, C1-C6-alkyl alkoxy, heteroaryl, C3-C8-cycloalkyl, C1-C6-alkyl C3-C8-cycloalkyl, C1-C6-alkyl C3-C8-heterocycloalkyl, C1-C6-alkyl acyl, C1-C6-alkyl carboxy, C1-C6-alkyl amino, C1-C6-alkyl aminocarbonyl, C1-C6-alkyl alkoxycarbonyl and C1-C6-alkyl acyl amino;
- or R5 and R6, together with the carbon atoms they are linked to, form a 5-8-membered saturated or aromatic ring containing optionally one or more heteroatoms selected from the group consisting of O, N and S;
- and
- X is O;
- as well as isomers, thereof.
A method for treating a patient in need thereof, said patient having symptoms caused by at least one of the following conditions:
- 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 said method comprising administering to said patient in need thereof a medicament comprising a thiazole according to Formula (I):
- wherein R1 is a moiety of the formula —NR5R6;
- R2, R3 and R5 are selected independently from H, C1-C6-alkyl, C2-C6-alkenyl and C2-C6-alkynyl;
- R4 is selected from the group consisting of H or C1-C6-alkyl, C1-C6-alkyl, C2-C6-alkenyl and C2-C6-alkynyl and NR8R9 wherein R8 and R9 are independently selected from the group consisting of C1-C6-alkyl, C2-C6-alkenyl and C2-C6-alkynyl;
- R6 is selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkyl alkoxy, aryl, heteroaryl, C3-C8-cycloalkyl, C3-C8-heterocycloalkyl, aryl C1-C6-alkyl, heteroaryl C1-C6-alkyl, C3-C8-cycloalkyl C1-C6-alkyl and C3-C8-heterocycloalkyl C1-C6-alkyl;
- or R5 and R6, together with the carbon atoms they are linked to, form a 5-8-membered saturated, partially unsaturated or aromatic ring containing optionally one or more heteroatoms selected from the group consisting of O, N and S;
- X is O;
- as well as isomers and mixtures thereof.
Dependencies are inferred from the claim text.