Triphenylalkene derivatives and their use as selective estrogen receptor modulators,申请号US20000712252-传众专利搜索

Triphenylalkene derivatives and their use as selective estrogen receptor modulators

申请公布号：US6576645(B1)

申请号：US20000712252

申请日期：2000.11.15

申请公布日期：2003.06.10

申请人：

HORMOS MEDICAL OY LTD

发明人：SOEDERVALL MARJA-LIISA;KALAPUDAS ARJA;KANGAS LAURI;LAMMINTAUSTA RISTO;HAERKOENEN PIRKKO;VAANAENEN KALERVO

分类号：A61K31/4164;A61K31/085;A61K31/09;A61K31/10;A61K31/136;A61K31/138;A61K31/145;A61K31/192;A61K31/4453;A61P5/30;A61P5/32;A61P9/02;A61P13/02;A61P15/02;A61P15/12;A61P19/10;A61P25/04;A61P25/20;A61P25/24;A61P25/28;A61P43/00;C07C43/225;C07C43/23;C07C59/68;C07C211/10;C07C211/53;C07C215/16;C07C217/18;C07C217/20;C07C323/12;C07C323/25;C07D211/14;C07D233/61;C07D295/092;C07D521/00;(IPC1-7):A61K31/445;A61K31/415;C07D233/00;C07D211/21;C07D211/32

主分类号：A61K31/4164

摘要：The invention provides novel selective estrogen receptor modulator compounds of the general formula:wherein R1 and R2, which are the same or different area) H, halogen, OCH3, OH; or where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, -CH2C=CH or -CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; orc) -Y-(CH2)nCH2-O-R6where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, -CH2CH2OH, or -CH2CH2Cl; ord) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; andR3 is H, halogen, OH or -OCH3;stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.