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the up - triphenylpropane derivatives and process for preparation triphenylpropene 1,1,2 - derivatives and compositions containing these new compounds.

机译:上三苯基丙烷衍生物和制备三苯基丙烯1,1,2-衍生物的方法以及含有这些新化合物的组合物。

摘要

New 1,1,2-triphenylpropane and -propene derivatives of the general formula (I), IMAGE wherein A and B each stand for hydrogen or they form together a valence bond, X and Y are identical or different and stand for phenyl group or a phenyl group having a halogen, hydroxy methoxymethoxy, C1-6 alkoxy or benzyloxy substituent in the para position, R1 is a C1-6 alkyl, epoxyalkyl, azidoalkyl, methoxymethyl or benzyl group or a group of the general formula (II), IMAGE wherein R2 and R3 each represent hydrogen or a C1-6 alkyl, hydroxyalkyl or haloalkyl group, or R2 and R3 form together with the adjacent nitrogen atom an up to 8-membered heterocyclic group, an up to 6-membered heterocyclic group optionally containing further hetero atom(s), which heterocyclic groups optionally have a lower alkyl or hydroxyalkyl substituent, a guanidino group, an aminoguanidino group or a nitroguanidino group, with the proviso that if A and B form together a valence bond and X and Y each stand for phenyl or X is phenyl and Y is p-methoxyphenyl, R1 may not stand for a dimethylaminoethyl, diethylaminoethyl, pyrrolidinoethyl, a piperidinoethyl or morpholinoethyl group in the (Z) isomers, stereoisomers and isomeric mixtures thereof, and acid addition salts of the basic compounds of the general formula (I) exert oestrogenic or antioestrogenic effects and furthermore inhibit the growth of the mammary tumor induced by 7,12-dimethyl-benz(a)anthracene.
机译:通式(I)的新的1,2,3-三苯基丙烷和-丙烯衍生物,,其中A和B各自代表氢或一起形成价键,X和Y相同或不同,并且代表苯基在对位上具有卤素,羟基甲氧基甲氧基,C 1-6烷氧基或苄氧基取代基的苯基或苯基,R 1为C 1-6烷基,环氧烷基,叠氮烷基,甲氧基甲基或苄基或通式(II)的基团,,其中R 2和R 3各自代表氢或C 1-6烷基,羟烷基或卤代烷基,或R 2和R 3与相邻的氮原子一起形成至多8元杂环基,至多6元杂环任选地包含另外的杂原子的基团,该杂环基任选地具有低级烷基或羟烷基取代基,胍基,氨基胍基或硝基胍基,条件是如果A和B一起形成价键并且X和Y各代表苯基或X是苯基且Y是对甲氧基苯基,R1不能代表(Z)的异构体,立体异构体和异构体混合物中的二甲氨基乙基,二乙氨基乙基,吡咯烷基乙基,哌啶子乙基或吗啉代乙基,通式(I)发挥雌激素作用或抗雌激素作用,并进一步抑制由7,12-二甲基-苯并(a)蒽诱导的乳腺肿瘤的生长。

著录项

  • 公开/公告号BE884716A

    专利类型

  • 公开/公告日1981-02-11

    原文格式PDF

  • 申请/专利权人 GYOGYSZERKUTATO INTEZET;

    申请/专利号BE19801009927

  • 发明设计人

    申请日1980-08-11

  • 分类号C07C;A61K;

  • 国家 BE

  • 入库时间 2022-08-22 16:21:34

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