wherein   R¹ is -H, -OH, -O(C₁-C₄ alkyl), -OCOC₆H₅, -OCO(C₁-C₆ alkyl), or -OSO₂(C₄-C₆ alkyl);   R is -H, -OH, -O(C₁-C₄ alkyl), -OCOC₆H₅, -OCO(C₁-C₆ alkyl), or -OSO₂(C₄-C₆ alkyl);   n is 2 or 3; and   R³ is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;or a pharmaceutically acceptable salt thereof, and an effective amount of a second component which is a compound of formula II wherein   either R⁴ is H or a lower alkyl radical and R⁵ is a lower alkyl radical, or R⁴ and R⁵ are joined together with the adjacent nitrogen atom to form a heterocyclic radical;   R⁶ is H or a lower alkyl radical;   R⁷ 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;   R⁸ is H or OH; and   n is 2;or a pharmaceutically acceptable salt thereof."/> Preparations for inhibiting mammalian breast carcinoma with tamoxifen and analogs thereof, and certain naphthyl compounds
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Preparations 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制剂

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 wherein   R¹ is -H, -OH, -O(C₁-C₄ alkyl), -OCOC₆H₅, -OCO(C₁-C₆ alkyl), or -OSO₂(C₄-C₆ alkyl);   R is -H, -OH, -O(C₁-C₄ alkyl), -OCOC₆H₅, -OCO(C₁-C₆ alkyl), or -OSO₂(C₄-C₆ alkyl);   n is 2 or 3; and   R³ is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino;or a pharmaceutically acceptable salt thereof, and an effective amount of a second component which is a compound of formula II wherein   either R⁴ is H or a lower alkyl radical and R⁵ is a lower alkyl radical, or R⁴ and R⁵ are joined together with the adjacent nitrogen atom to form a heterocyclic radical;   R⁶ is H or a lower alkyl radical;   R⁷ 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;   R⁸ is H or OH; and   n is 2;or 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。 <图像文件=“ IMGA0001.GIF” he =“ 61” id =“ ia01” imgContent =“ chem” imgFormat =“ GIF” wi =“ 104” /> 其中R 1是-H,-OH,-O(C 1 -C 4烷基),-OCOC 3 H 4,-OCO(C 1 -C 4烷基)或-OSO 2(C 1 -C 4烷基);R是-H,-OH,-O(C 1 -C 4烷基),-OCOC 3 H 4,-OCO(C 1 -C 4烷基)或-OSO 2(C 1 -C 4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;或其药学上可接受的盐,以及有效量的第二种成分,它是式II化合物<!-EPO -> <化学id =“ chema02”> <图像文件= “ IMGA0002.GIF” he =“ 60” id =“ ia02” imgContent =“ chem” imgFormat =“ GIF” wi =“ 96” /> 其中R 5是H或低级烷基,R 4是低级烷基,或R 5和R 4与相邻的氮原子连接在一起形成杂环基。R 5是H或低级烷基。R 5是H,卤素,OH,低级烷基或为与相邻苯环一起形成萘基的丁1,3-二烯基。R 5为H或OH;和n是2;或其药学上可接受的盐。

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