发明名称 Substituted 10-aryl-11H-benzo[b]fluorenes and 7-aryl-5, 6-dihydro-benzo[a]anthracenes for selective effects on estrogen receptors
摘要 This invention provides a compound, or its possible salt, having the formula, wherein: R<SUP>e </SUP>and 'R<SUP>e </SUP>are OH, optionally independently etherified or esterified; Z is -CH<SUB>2</SUB>CH<SUB>2</SUB>- or -C(R<SUP>4</SUP>,R<SUP>5</SUP>)-, wherein R<SUP>4 </SUP>and R<SUP>5 </SUP>are independently H, (1C-2C)alkyl or form together a spiro(3C-5C)cycloalkyl; R<SUP>1 </SUP>is H, halogen, CF<SUB>3</SUB>, or (1C-4C)alkyl; R<SUP>2 </SUP>and R<SUP>3 </SUP>are independently H, halogen, -CF<SUB>3</SUB>, -OCF<SUB>3</SUB>, (1C-8C)alkyl, hydroxy, (1C-8C)alkyloxy, aryloxy, aryl(1C-8C)alkyl, halo(1C-8C)alkyl, -O(CH<SUB>2</SUB>)<SUB>m</SUB>X, wherein X is halogen or phenyl and m=2-4; -O(CH<SUB>2</SUB>)<SUB>m</SUB>NR<SUB>a</SUB>R<SUB>b</SUB>, -S(CH<SUB>2</SUB>)<SUB>m</SUB>NR<SUB>a</SUB>R<SUB>b </SUB>or -(CH<SUB>2</SUB>)<SUB>m</SUB>NR<SUB>a</SUB>R<SUB>b</SUB>, wherein m=2-4 and wherein R<SUB>a</SUB>, R<SUB>b </SUB>are independently (1C-8C)alkyl, (2C-8C)alkenyl, (2C-8C)alkynyl, or aryl, which alkyl, alkenyl and aryl can optionally be substituted with halogen, -CF<SUB>3</SUB>, -OCF<SUB>3</SUB>, -CN, -NO<SUB>2</SUB>, -OH, (1C-8C)alkoxy, aryloxy, carboxyl, (1C-8C)alkylthio, carboxylate, (1C-8C)alkyl, aryl, aryl(1C-8C)alkyl or halo(1C-8C)alkyl; or R<SUB>a </SUB>and R<SUB>b </SUB>form a 3-8 membered ring structure, optionally substituted with halogen, -CF<SUB>3</SUB>, -OCF<SUB>3</SUB>, -CN, -NO<SUB>2</SUB>, 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.
申请公布号 US7335659(B2) 申请公布日期 2008.02.26
申请号 US20040505631 申请日期 2004.08.19
申请人 N.V. ORGANON 发明人 LOOZEN HUBERT JAN JOZEF;WAGENER MARKUS;VEENEMAN GERRIT;ZWART EDUARD WILLEM
分类号 A61K31/496;C07D295/08;A61K31/05;A61K31/085;A61K31/095;A61K31/138;A61K31/36;A61K31/40;A61K31/428;A61K31/44;A61K31/4453;A61K31/506;A61K31/5375;A61P5/24;A61P5/30;A61P9/00;A61P13/08;A61P15/00;A61P19/10;A61P25/00;A61P25/24;A61P25/28;A61P35/00;A61P43/00;C07C39/17;C07C39/42;C07C43/225;C07C43/23;C07C49/753;C07C217/54;C07C217/58;C07C323/18;C07D207/12;C07D211/68;C07D211/70;C07D217/18;C07D239/42;C07D277/62;C07D277/66;C07D295/092;C07D317/54;C07D403/04 主分类号 A61K31/496
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