FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention proposes novel derivatives of thiazole that able for effective binding and activating PPARα and/or PPARγ simultaneously and, respectively, combine antiglycemic effect caused by activation of PPARγ with anti-dyslipidemic effect caused by activation of PPARα. Also, the claim describes compounds of the formula (I): wherein substitutes from R1 to R10 as well as X and Y are determined in the description and invention claim, and their pharmaceutically acceptable salts and esters also. Also, the proposed invention describes pharmaceutical compositions possessing antagonistic activity with respect to PPARα and/or PPARγ comprising compound of the formula (I) as an active component and pharmaceutically acceptable carrier and/or additive. Except for, the invention proposes claimed compounds as therapeutically active substances for treatment and/or prophylaxis of diseases mediated by agonists of PPARα and/or PPARγ, such as diabetes mellitus, non-insulin dependent diabetes mellitus, elevated blood pressure, increased level of lipids and cholesterol, atherosclerotic diseases, metabolic syndrome, endothelial dysfunction, procoagulant state, dyslipidemia, ovary polycystic syndrome, inflammatory or proliferative diseases.
EFFECT: valuable medicinal properties of compounds.
27 cl, 140 ex
Title | Year | Author | Number |
---|---|---|---|
N-SUBSTITUTED 1H-INDOLE-5-PROPIONIC ACIDS, PHARMACEUTICAL COMPOSITION CONTAINING THESE COMPOUNDS AND THEIR USING (VARIANTS) | 2003 |
|
RU2296759C2 |
CHIRAL DERIVATIVES OF OXAZOLARYLPROPIONIC ACID AND THEIR USING AS AGONISTS OR RECEPTOR ACTIVATED BY PEROXISOME PROLIFERATOR (PPAR AGONISTS) | 2003 |
|
RU2303593C2 |
OXAZOLE DERIVATIVES SUBSTITUTED WITH CARBOXYLIC ACIDS AS PPAR-ALPHA AND PPAR-GAMMA ACTIVATORS IN DIABETES TREATMENT | 2002 |
|
RU2278859C2 |
THIAZOLE-SUBSTITUTED INDOLYL-DERIVATIVES AND APPLICATION THEIROF AS PPAR MODULATORS | 2004 |
|
RU2344135C2 |
INDOLYL-DERIVATIVES, METHOD FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION, METHOD OF TREATMENT AND/OR PROPHYLAXIS OF DISEASES | 2003 |
|
RU2315767C2 |
PHENYL DERIVATIVES AS PPAR AGONISTS | 2004 |
|
RU2374230C2 |
OXADIAZOLONE DERIVATIVES AS PPAR-DELTA AGONISTS | 2005 |
|
RU2374243C2 |
DERIVATIVES OF THIAZOLE, METHOD OF THEIR SYNTHESIS, COMPOSITION BASED ON THEREOF AND INTERMEDIATE COMPOUND | 1999 |
|
RU2166503C2 |
HEXAFLUOROISOPROPANOL-SUBSTITUTED ETHER DERIVATIVES | 2005 |
|
RU2383524C2 |
BENZANNEALED COMPOUNDS AS PPAR ACTIVATORS | 2004 |
|
RU2367654C2 |
Authors
Dates
2007-04-10—Published
2003-08-21—Filed