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    • 1. 发明授权
    • Novel derivatives of 3-aryl-3-cycloalkyl-piperidine-2,6-dione
    • 3-芳基-3-环烷基 - 哌啶-2,6-二酮的新衍生物
    • US4839370A
    • 1989-06-13
    • US79964
    • 1987-07-31
    • Rolf W. HartmannChristine Batzl
    • Rolf W. HartmannChristine Batzl
    • A61K31/445A61K31/4427A61K31/451A61P3/00A61P35/00C07D211/26C07D211/88C07D401/04
    • C07D401/04C07D211/88
    • Novel 3-aryl-3-cycloalkyl-piperidine-2,6-dione derivatives of the general formula I: ##STR1## in which A is a 4-aminophenyl radical or a pyridyl-(4)-radical and R.sub.1 is a saturated or unsaturated C.sub.3 -C.sub.10 -cycloalkyl radical or a C.sub.3 -C.sub.12 -alkenyl radical as well as physiologically acceptable salts thereof. The compounds are useful as inhibitors of estrogen biosynthesis. The compounds are made by a process which includes the step of heating a compound of the formula II ##STR2## wherein A and R.sub.1 have the meanings given above, and in addition A may also be a phenyl radical or a 4-nitrophenyl radical, X and Y are the same or different and repesent CN or COOC.sub.1 -C.sub.6 -alkyl and X or Y may also be COOH or a carboxylic acid ester group of the formula COOC.sub.1 -C.sub.6 -alkyl group, in a high boiling solvent at a temperature between 50.degree. and 200.degree. C. in particular between 80.degree. and 100.degree. C., optionally in the presence of condensation agents to form a piperidine dione ring.
    • 通式I的新型3-芳基-3-环烷基 - 哌啶-2,6-二酮衍生物:其中A是4-氨基苯基或吡啶基 - (4) - 衍生物,R 1是饱和的 或不饱和C 3 -C 10 - 环烷基或C 3 -C 12 - 烯基以及其生理上可接受的盐。 该化合物可用作雌激素生物合成的抑制剂。 该化合物通过包括加热式II化合物II的步骤的方法制备,其中A和R 1具有上述含义,另外A也可以是苯基或4-硝基苯基, X和Y相同或不同,并且重复的CN或COOC 1 -C 6烷基,X或Y也可以是COOH或式COOC 1 -C 6 - 烷基的羧酸酯基,在高沸点溶剂中, 50℃和200℃,特别是80℃至100℃之间,任选在缩合剂存在下形成哌啶二酮环。