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Substituted 10-aryl-11H-benzobfluorenes and 7-aryl-5, 6-dihydro-benzoaanthracenes for selective effects on estrogen receptors
Substituted 10-aryl-11H-benzobfluorenes and 7-aryl-5, 6-dihydro-benzoaanthracenes for selective effects on estrogen receptors
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机译:取代10-芳基-11 H I>-苯并[ b I>]芴和7-芳基-5,6-二氢苯并[[I> a I>]]蒽对雌激素受体的选择性作用
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摘要
This invention provides a compound, or its possible salt, having the formula,; wherein: Re and ′Re are OH, optionally independently etherified or esterified; Z is —CH2CH2— or —C(R4,R5)—, wherein R4 and R5 are independently H, (1C-2C)alkyl or form together a spiro(3C-5C)cycloalkyl; R1 is H, halogen, CF3, or (1C-4C)alkyl; R2 and R3 are independently H, halogen, —CF3, —OCF3, (1C-8C)alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, —O(CH2)mX, wherein X is halogen or phenyl and m=2-4; —O(CH2)mNRaRb, —S(CH2)mNRaRb or —(CH2)mNRaRb, wherein m=2-4 and wherein Ra, Rb are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, which alkyl, alkenyl and aryl can optionally be substituted with halogen, —CF3, —OCF3, —CN, —NO2, —OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl or halo(1C-8C)alkyl; or Ra and Rb form a 3-8 membered ring structure, optionally substituted with halogen, —CF3, —OCF3, —CN, —NO2, hydroxy, hydroxy(1C-4C)alkyl, (1C-8C)alkoxy, aryloxy, (1C-8C)alkylthio, carboxyl, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl, halo(1C-8C)alkyl.
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机译:本发明提供了具有下式的化合物或其可能的盐: 化学>其中:R e Sup>和'R e Sup>是OH,任选地独立地被醚化或酯化; Z是–CH 2 Sub> CH 2 Sub>-或-C(R 4 Sup>,R 5 Sup>)-,其中R 4 Sup>和R 5 Sup>独立地为H,(1C-2C)烷基或一起形成螺(3C-5C)环烷基; R 1 Sup>是H,卤素,CF 3 Sub>或(1C-4C)烷基; R 2 Sup>和R 3 Sup>独立地为H,卤素,-CF 3 Sub>,-OCF 3 Sub>,(1C- 8C)烷基,羟基,(1C-8C)烷氧基,芳氧基,芳基(1C-8C)烷基,卤代(1C-8C)烷基,-O(CH 2 Sub>) m Sub> X,其中X是卤素或苯基且m = 2-4; —O(CH 2 Sub>) m Sub> NR a Sub> R b Sub>,-S(CH 2 Sub>) m Sub> NR a Sub> R b Sub>或-(CH 2 Sub>) m Sub> NR a Sub> R b Sub>,其中m = 2-4,其中R a Sub>,R b Sub>独立地(1C -8C)烷基,(2C-8C)烯基,(2C-8C)炔基或芳基,其中烷基,烯基和芳基可以任选地被卤素,-CF 3 Sub>,-OCF 3 Sub>,-CN,-NO 2 Sub>,-OH,(1C-8C)烷氧基,芳氧基,羧基,(1C-8C)烷硫基,羧酸根,(1C-8C)烷基,芳基,芳基(1C-8C)烷基或卤代(1C-8C)烷基;或R a Sub>和R b Sub>形成3-8元环结构,可选地被卤素,-CF 3 Sub>,-OCF 取代3 Sub>,-CN,-NO 2 Sub>,羟基,羟基(1C-4C)烷基,(1C-8C)烷氧基,芳氧基,(1C-8C)烷硫基,羧基,羧酸根, (1C-8C)烷基,芳基,芳基(1C-8C)烷基,卤代(1C-8C)烷基。
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