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US 7,582,664 B2Granted
Acylaminothiazole derivatives, preparation method thereof and use of same in therapeutics
AssigneeSanofi-Aventis
InventorsSylvie Baltzer, Viviane Van Dorsselaer
Life of this patent
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Abstract
The invention relates to a compound of formula (I): Wherein R1, R2, R2′, R3, R4 and R5 are as defined herein. The invention also relates to the use of said compound in therapeutics.
Claims20
A compound of the formula (I):
- wherein
- R1 represents:
- either a C1-6 alkyl optionally substituted with one to three substituents chosen from halogen, trifluoromethyl, hydroxyl, C1-6 alkoxy, C1-6 thioalkyl, thiophene or a phenyl;
- or C3-7 cycloalkyl, thiophene, benzothiophene, pyridyl, furyl or phenyl;
- said phenyl being optionally substituted with one to three substituents chosen from halogen atom, C1-6 alkyl, C1-6 alkoxy, hydroxyl, methylenedioxy, phenoxy, benzyloxy or trifluoromethyl;
- R2 and R′2 represent, independently of each other, hydrogen, halogen, hydroxyl, C1-3 alkoxy, C1-3 alkyl, C3-7 cycloalkyl, O—C(O)—C1-6 alkyl;
- or R2 and R′2 together form an oxo group;
- R3 represents hydrogen, C1-6 alkyl optionally substituted with hydroxyl, C1-6 cycloalkyl or C1-3 alkoxy;
- one or other of R4 and R5 represents a group Z:
- and one or other of R4 and R5 represents a group —C(X)R6;
- wherein
- G represents a single bond or —CH2—;
- Y represents a single bond, oxygen or sulfur, C1-4 alkylene or —N(W)—;
- said —C1-4 alkylene-group being optionally substituted with hydroxyl or C1-3 alkoxy;
- and wherein
- W represents hydrogen, C1-3 alkyl optionally substituted with phenyl, or phenyl;
- A and B represent, independently of each other, hydrogen or halogen, hydroxyl, C1-3 alkyl, C1-3 alkoxy, trifluoromethyl, trifluoromethoxy or —O—CHF2;
- X represents oxygen or sulfur;
- R6 represents C1-6 alkoxy, hydroxyl or —NR7R8;
- said C1-6 alkoxy group is optionally substituted with phenyl;
- and
- R7 and R8 represent, independently of each other, hydrogen;
- C1-6 alkyl optionally substituted with C3-7 cycloalkyl, C3-7 cycloalkenyl, C1-3 alkoxy, phenyl, morpholinyl or pyridyl;
- or C3-7 cycloalkyl, C1-6 alkoxy or phenyl;
- said C3-7 cycloalkyl and phenyl are optionally substituted with one or two substituents chosen from halogen, hydroxyl, C1-3 alkyl and C1-3 alkoxy;
- or
- R7 and R8, with the nitrogen atom that bears them, form an aziridine, azetidine, pyrrolidine, piperidine, morpholine or benzopiperidine ring;
- or
- said compound in the form of a salt, hydrate or a solvate;
- and
- with the proviso that when Y is a single bond or oxygen and Z is
- then A is other than hydrogen.
29 more elements
Dependencies are inferred from the claim text.