FIELD: organic synthesis. SUBSTANCE: invention provides novel amine derivatives of general formula I: (I), where R1 represents carbamoyl group optionally containing one or two alpha-substituents (described below), thiocarbamoyl group optionally containing one or two alpha-substituents (described below), sulfonyl group containing one alpha-substituent (described below), or carbonyl group containing one alpha- substituent (described below); R2 represents hydrogen atom; R3 C1-C10-alkyl group; W1,W2 and W3, each represents ordinary bond or C1-C8-alkylene group; X represents oxygen or sulfur atom; Y oxygen atom; Q sulfur atom; X group = CH- or nitrogen atom; Ar benzene or naphthalene ring; L represents 1-2 substituents in Ar ring, each being hydrogen or C1-C6-alkyl; alpha-substituents can be C1-C10-alkyl, C3-C10-cycloalkyl, or phenyl optionally substituted by 1-3 gamma-substituents (described below), etc.; gamma- substituents can be C1-C6-alkyl, halo-C1-C6-alkyl, C1-C6-alkoxy, halogen, hydroxy, cyano, nitro, or alkylenedioxy group; or their pharmaceutically acceptable salt or esters. Pharmaceutical composition exhibiting PPARγ- activating effect includes a compound I or its pharmaceutically acceptable salt or ester derivative in effective amount along with carrier or diluent. Agent containing compound I or its pharmaceutically acceptable salt or ester derivative is suitable for treatment of cancer. Treatment or prevention of cancer in warm-blooded animals consists in administration of effective amount of compound I or its pharmaceutically acceptable salt or ester derivative optionally in combination with PXR activator. EFFECT: extended choice of biologically active compounds with PPARγ-activating effect. 36 cl, 7 tbl, 109 ex
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Authors
Dates
2004-01-20—Published
2000-04-06—Filed