US 11,111,219 B2Granted

Polysubstituted pyrimidines inhibiting the formation of prostaglandin E2, a method of production thereof and use thereof

AssigneeUstav Organicke Chemie A Biochemie Av Cr, V.V.I.

InventorsViktor Kolman, Filip Kalcic, Zlatko Janeba, Zdenek Zidek

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Abstract

The invention describes the pyrimidine-based compounds of the general formula I. Described compounds lower the production of the prostaglandin E2. In concentrations lowering production of this factor by 50%, these compounds have no negative effect on the cell viability and they are not cytotoxic. Furthermore, the method of production of the compounds of the general formula I is provided. A pharmaceutical composition comprising the polysubstituted pyrimidines according to the invention and the use of these compounds for the treatment of the inflammatory diseases are also provided.

Claims3

Dependent claims

Polysubstituted pyrimidines of the formula (I)

where
X1 is selected from the group consisting of —H, —F, —Cl, and alkyl;
X2 is selected from the group consisting of —H, —F, —Cl, and alkyl;
X3 is selected from the group consisting of —H, —F, —Cl, and alkyl;
X4 is selected from the group consisting of —H, —F, —Cl, and alkyl;
Y1 is selected from the group consisting of —H, —F, —Cl, and —OR, wherein R is alkyl;
Y2 is selected from the group consisting of —H, —F, —Cl, and —OR, wherein R is alkyl;
R1 is aryl as defined herein;
R2 is alkyl as defined herein;
or a pharmaceutically acceptable salt thereof,
wherein
alkyl in these cases is defined as a linear or branched C1-C10 carbon chain;
aryl in the above cases is defined as a hydrocarbon group containing 6 to 14 carbon atoms containing at least one aromatic ring, wherein the aryl may be unsubstituted or substituted with 1 to 5 substituents selected from the group of —F, —Cl, and —OR, wherein R is alkyl as defined herein.

10 more elements

Dependencies are inferred from the claim text.

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Abstract