发明名称 Substituted 2-alkylidene acetic acids and their derivatives
摘要 Novel compounds of the formula <FORM:1122879/C2/1> (wherein A is O, S, NH or N alkyl; R1 and R2 are H or alkyl; X is halogen, CHO, alkenyl, haloalkyl, hydroxyalkyl, alkoxy, alkythio, alkylsulphonyl, alkanoyl, cycloalkyl, amino, alkylamino, dialkylamino or C1- 5 alkanoylamino; and n is 1, 2, 3, 4 or 5) and their salts, esters and amides are prepared by treating a 2-halo-2-alkylidene acetic acid ester with an appropriately substituted phenol, thiophenol or aniline, and, if desired, hydrolysing the product to the free acid, which my be converted to a salt, ester or amide by known methods. 2 - Halo - 2 - alkylidene - acetic acid esters are prepared by dehydrohalogenation of 2,3-dihaloalkanoic acid esters.ALSO:Pharmaceutical compositions having hypocholesterolemic activity comprise 2-alkylideneacetic acids of the formula <FORM:1122879/A5-A6/1> (wherein A is O, S, NH or N alkyl; R1 and R2 are H or alkyl; X is halogen, CHO, alkenyl, halo alkyl, hydroxyalkyl, alkoxy, alkylthio, alkylsulphonyl, alkanoyl, cycloalkyl, amino, alkylamino, dialkylamino or C1-5 alkanoylamino; and n is 1, 2, 3, 4, or 5) or their salts, esters or amides and carriers therefor. They may also contain other known diuretics and saluretics. Oral and intravenous dosage forms are referred to.
申请公布号 GB1122879(A) 申请公布日期 1968.08.07
申请号 GB19660046240 申请日期 1966.10.17
申请人 MERCK & CO. INC. 发明人
分类号 A61K31/19;C07C51/09;C07C59/42;C07C59/58;C07C59/68;C07C59/70;C07C317/14 主分类号 A61K31/19
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