首页> 外国专利> Derivatives of 4,5-dihydro-4-oxofuran-2-carboxylic acid, especially for use as hypolipidemic agents, processes for their preparation, pharmaceutical compositions comprising them, tetrahydropyran-2,3,5-triones useful in the preparation of the said derivatives and a process for preparing these tetrahydropyran-2,3,5-triones

Derivatives of 4,5-dihydro-4-oxofuran-2-carboxylic acid, especially for use as hypolipidemic agents, processes for their preparation, pharmaceutical compositions comprising them, tetrahydropyran-2,3,5-triones useful in the preparation of the said derivatives and a process for preparing these tetrahydropyran-2,3,5-triones

机译:4,5-二氢-4-氧杂呋喃-2-羧酸的衍生物,特别是用作降血脂药,其制备方法,包含它们的药物组合物,可用于制备所述化合物的四氢吡喃-2,3,5-三酮衍生物和制备这些四氢吡喃-2,3,5-三酮的方法

摘要

Compounds of formula Iin which R1 and R2 each is lower alkyl, cyclo(lower)alkyl, lower alkoxy(lower)alkylene, phenyl or phenyl mono- or disubstituted with lower alkyl, lower alkoxy, halo, nitro or trifluoromethyl; or RI and R2 together form a -(CH2)m-X-(CH2)n- chain wherein m and n each is an integer from one to four and X is methylene, oxa or thia; or R1 and R2 together with the carbon atom to which they are joined form a spiro-[1,2,3,4-tetrahydronaphthalene]-1 or spiro[indan]-1 radical; R3 is hydrogen or lower alkyl; and R' is hydrogen, lower alkyl, cyclo(lower)alkyl, phenyl(lower)alkylene, amino-(lower)alkylene, lower alkylamino(lower)alkylene, di(lower alkyl)amino(lower)alkylene or 3-pyridinyl(lower)alkylene, or a therapeutically acceptable addition salt thereof are disclosed which possess hypolipidemic activity, and can be used in pharmaceutical compositions.;The compounds of formula I may be prepared by cyclising a corresponding compound of formula Xand if desired esterifying. Tetrahydropyran-2,3,5-trione intermediates are also disclosed.
机译:式I化合物 <图像文件=“ IMGA0001.GIF” he =“ 20” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 63” /> 其中R 1 和R 2 分别为低级烷基,环(低级)烷基,低级烷氧基(低级)亚烷基,苯基或被低级烷基,低级烷氧基单或二取代的苯基,卤素,硝基或三氟甲基;或R I 和R 2 一起形成-(CH 2 m -X-(CH 2 n -链,其中m和n各自为1-4的整数,X为亚甲基,氧杂或硫杂;或R 1 和R 2 以及与之相连的碳原子一起形成螺-[1,2,3,4-四氢萘] -1或螺[茚满] -1自由基; R 3 为氢或低级烷基;和R'是氢,低级烷基,环(低级)烷基,苯基(低级)亚烷基,氨基-(低级)亚烷基,低级烷基氨基(低级)亚烷基,二(低级烷基)氨基(低级)亚烷基或3-吡啶基(公开了具有降血脂活性并且可以用于药物组合物中的低级亚烷基或其治疗上可接受的加成盐。式I的化合物可以通过环化相应的式X的化合物来制备 <图像文件=“ IMGA0002.GIF” he =“ 19” imgContent =“ chem” imgFormat =“ GIF” inline =“ no” wi =“ 48” /> 所需的酯化。还公开了四氢吡喃-2,3,5-三酮中间体。

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