首页> 外国专利> Method for inhibiting mammalian breast carcinoma with tamoxifen, and analogs thereof, and certain naphthyl compounds

Method for inhibiting mammalian breast carcinoma with tamoxifen, and analogs thereof, and certain naphthyl compounds

机译:他莫昔芬及其类似物和某些萘基化合物抑制哺乳动物乳腺癌的方法

摘要

The present invention provides a method of inhibiting hormone- dependent breast carcinoma in a mammal comprising administering to said mammal in need of treatment an effective amount of a first component which is a compound of formula I ##STR1## wherein R.sup.1 is --H, --OH, -- O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);PPR.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C. sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.4 -C.sub.6 alkyl);P Pn is 2 or 3; andPPR.sup.3 is 1-piperidinyl, 1- pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4- morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;P Por a pharmaceutically acceptable salt thereof, and an effective amount of a second component which is a compound of formula II ##STR2## wherein either R.sup.4 is H or a lower alkyl radical and R.sup.5 is a lower alkyl radical, or R.sup.4 and R.sup.5 are joined together with the adjacent nitrogen atom to form a heterocyclic radical;PPR. sup.6 is H or a lower alkyl radical;PPR.sup.7 is H, halo, OH, a lower alkyl radical, or is a buta-1,3-dienyl radical which together with the adjacent benzene ring forms a naphthyl radical;P P R.sup.8 is H or OH; andPPn is 2;P Por a pharmaceutically acceptable salt thereof.
机译:本发明提供了一种在哺乳动物中抑制激素依赖性乳腺癌的方法,该方法包括对需要治疗的所述哺乳动物给药有效量的第一组分,所述第一组分为式I的化合物,其中R.sup.1。是-H,-OH,-O(C.sub.1 -C.sub.4烷基),-OCOC.sub.6 H.sub.5,-OCO(C.sub.1- C.sub.6烷基)或--OSO.sub.2(C.sub.4 -C.sub.6烷基);

R> sup.2为--H,--OH ,-O(C 1 -C 4烷基),-OCOC.6 H 5,-OCO(C 1 -C 6烷基),或-OSO.sub.2(C.sub.4 -C.sub.6烷基);

n为2或3;和R 3是1-哌啶基,1-吡咯烷基,甲基-1-吡咯烷基,二甲基-1-吡咯烷基,4-吗啉代,二甲基氨基,二乙基氨基或1-六亚甲基亚氨基; P或其药学上可接受的盐,和有效量的第二组分,其为式II的化合物,其中R 4为H或低级烷基,R 5为H低级烷基或R 4和R 5与相邻的氮原子连接在一起形成杂环基。 sup.6是H或低级烷基; P.Rups.7是H,卤素,OH,低级烷基或为Buta-1,3-dienyl基,与相邻的苯环形成萘基; P 8 R为H或OH;并且P n = 2; P n或其药学上可接受的盐。

著录项

  • 公开/公告号US5658931A

    专利类型

  • 公开/公告日1997-08-19

    原文格式PDF

  • 申请/专利权人 ELI LILLY AND COMPANY;

    申请/专利号US19940309299

  • 发明设计人 HENRY U. BRYANT;ROBIN S. L. FUCHS-YOUNG;

    申请日1994-09-20

  • 分类号A61K31/445;A61K31/55;A61K31/40;A61K31/535;

  • 国家 US

  • 入库时间 2022-08-22 03:09:32

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