SUBSTITUTED 3-PHENYL-5-ALKOXY-1,3,4-OXADIAZOL-2-ONES AND THEIR APPLYING AS LIPASE INHIBITORS Russian patent published in 2005 - IPC

Abstract RU 2265600 C2

FIELD: organic chemistry, biochemistry.

SUBSTANCE: invention relates to substituted 3-phenyl-5-alkoxy-1,3,4-oxadiazol-2-ones of the formula (1):

wherein R1 means (C1-C6)-alkyl that can be substituted once or multiply with phenyl; R2 and R3 means independently of one another hydrogen atom, (C6-C10)-aryl, (C3-C8)-cycloalkyl, (C6-C10)-aryloxymethyl, O-benzyl can be substituted once or multiply with halogen atom, -CF3,, O-(C6-C10)-aryl or O-(C3-C8)-cycloalkyl, O-(C1-C6)-alkyl, that can be substituted once or multiply with fluorine atom or amino-group wherein amino-group, in turn, can be substituted once or multiply with (C1-C4)-alkyl; SO2-NH-(C1-C6)-alkyl substituted possibly with group N-[(C1-C6)-alkyl]2; SO2-NH-(2,2,6,6-tetramethylpiperidin-4-yl); SO2-NH-(C3-C8)-cycloalkyl substituted possible once or multiply with (C1-C4)-alkyl; SO2-N-[(C1-C6)-alkyl]2 or COX wherein X means N-[(C1-C6)-alkyl]2; and N-[(C1-C6)-alkyl-alkyl]2 can mean also pyrrolidine, piperidine, morpholine or piperizine group that if necessary can be substituted with (C1-C4)-alkyl; under condition that R2 and R3 don't mean hydrogen atom simultaneously, and to their physiologically acceptable salts and optical isomers. Compounds show inhibitory effect on activity of hormone-sensitivity lipase (HSL). Also, invention describes a method for preparing these compounds.

EFFECT: valuable medicinal and biochemical properties of compounds.

9 cl, 43 ex

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RU 2 265 600 C2

Authors

Petri Shtefan

Shenafinger Karl

Mjuller Gjunter

Baringkhaus Karl-Khajnts

Dates

2005-12-10Published

2000-08-22Filed