Carboxylic Acid Derivative Containing Thiazole Ring and Pharmaceutical Use Thereof
AssigneeMitsubishi Phama Corporation
InventorsTakashi Tozawa, Osamu Tsuruta, Hiroshi Kitajima, Yoshiyuki Aoki, Naoko Ando, Hiroki Tamakawa
Life of this patent
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Abstract
According to the present invention, a compound represented by the following formula (I) having a superior PPARα agonist action and concurrently showing a hypolipidemic action can be provided, and further, a compound useful as a synthetic intermediate for the compound can be provided.
Claims22
A carboxylic acid derivative containing a thiazole ring represented by a following formula (I):
- [wherein R1 and R2 are the same or different and each is a hydrogen atom or an alkyl group, or R1 and R2 are bonded to each other to form a cycloalkyl group;
- R3 is a hydrogen atom or an alkyl group;
- R4 is a hydrogen atom, an alkyl group or an aryl group;
- n is an integer of 1 to 5;
- Y is an oxygen atom, a sulfur atom, —NR5—, —CONR5—, —NR5CO— or —NHCONR5— (wherein R5 is a hydrogen atom, an alkyl group, a cycloalkylalkyl group, an aryl group, an arylalkyl group, an arylalkenyl group, an aryloxyalkyl group, a heteroaryl group or a heteroarylalkyl group);
- and
- Z is a cycloalkyl group, an aryl group, an arylalkyl group, an arylalkenyl group, an aryloxyalkyl group, a heteroaryl group or a heteroarylalkyl group,
- wherein, in the aforementioned groups, an alkyl group, a cycloalkyl group, a cycloalkylalkyl group, an aryl group, an arylalkyl group, an arylalkenyl group, an aryloxyalkyl group, a heteroaryl group and a heteroarylalkyl group each optionally have substituent], or a pharmaceutically acceptable salt thereof or a hydrate thereof or a solvate thereof.
A carboxylic acid derivative containing a thiazole ring represented by
- (34) 2-[(4-{2-[(4′-fluorobiphenyl-4-yl)oxy]ethyl}-1,3-thiazol-2-yl)thio]-2-methylpropionic acid,
- or a pharmaceutically acceptable salt thereof or a hydrate thereof or a solvate thereof.
A carboxylic acid derivative containing a thiazole ring represented by
- (442) 2-[(4-{2-[heptyl(5-morpholin-4-ylpyrimidin-2-yl)amino]ethyl}-1,3-thiazol-2-yl)thio]-2-methylpropionic acid,
- or a pharmaceutically acceptable salt thereof or a hydrate thereof or a solvate thereof.
A carboxylic acid derivative containing a thiazole ring represented by
- (326) 2-{[4-(2-{(5-ethylpyrimidin-2-yl)[(1-phenyl-1H-pyrazol-4-yl)methyl]amino}ethyl)-1,3-thiazol-2-yl]thio}-2-methylpropionic acid,
- or a pharmaceutically acceptable salt thereof or a hydrate thereof or a solvate thereof.
A compound represented by the following formula (V):
- [wherein R1, R2, R3, R4 and n are as defined above;
- Q is —CO2R33 (wherein R33 is a hydrogen atom or an alkyl group), a hydroxyl group, a halogen atom, —OSO2R34 (wherein R34 is an alkyl group, an aryl group or a haloalkyl group), —N3, —NR35R36 (wherein R35 and R36 are the same or different and each is a hydrogen atom, an alkyl group, an arylalkyl group or a heteroarylalkyl group), NCO2OR37 (wherein R37 is an alkyl group, an arylalkyl group or a heteroarylalkyl group) or the following formula (VI)
- , wherein, in the aforementioned groups, an alkyl group, an aryl group, an arylalkyl group and a heteroarylalkyl group each optionally have substituent], provided that a compound represented by the following formula (VII) is excluded:
Dependencies are inferred from the claim text.